Pharmacology Flashcards Preview

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Flashcards in Pharmacology Deck (731):
1

rapidly hydrolyzed by AChE

Acetylcholine (TOPNOTCH)

2

resistant to AChE

Betanechol (TOPNOTCH)

3

for Bladder and bowel atony

Betanechol (TOPNOTCH)

4

Nonselective muscarinic and nicotinic agonist , used topically for glaucoma treatment

Carbachol (TOPNOTCH)

5

Partial muscarinic agonist; used for treatment of Glaucoma, Sjogren's syndrome and Sicca syndrome

Pilocarpine (TOPNOTCH)

6

Adverse Effects of Acetylcholine

CNS stimulation, miosis, cyclospasm, brochoconstriction, excessive GI and GU smooth muscle contraction, increased secretory activity of sweat gland, airways etc, vasodilation (TOPNOTCH)

7

activates autonomic post ganglionic neurons (both sympathetic and parasympathetic) and skeletal muscle neuromuscular end plants

Nicotine(TOPNOTCH)

8

used exclusively for smoking cessation

Varenicline (TOPNOTCH)

9

for Myasthenia gravis diagnosis (Tensilon test)

Edrophonium (TOPNOTCH)

10

for Myasthenia gravis treatment; reversal of nondepolarizing muscular blockade

Neostigmine (TOPNOTCH)

11

Long Acting Cholinesterase Inhibitors used as Scabicide and Insecticide

Malathion, Parathion (TOPNOTCH)

12

Competitively blocks all muscarinic receptors, antagonizes histamine and serotonin ; for motion sickness, dec. acid secretion in the GIT

Scopolamine (TOPNOTCH)

13

DOC for organophosphate poisoning

Atropine (TOPNOTCH)

14

for bradycardia, hypersalivation and to decrease airway secretion during general anesthesia

Atropine (TOPNOTCH)

15

Mydriatic, cycloplegic in eye examinations

Homatropine, Cyclopentolate, Tropicamide (TOPNOTCH)

16

Competitive nonselective antagonist at muscarinic receptors ; for BA and COPD, not as effective as SABAs but less tachycardia and arrhythmia

Ipratropium, Tiotropium (TOPNOTCH)

17

Nonselective muscarinic antagonist which reduces detrussor smooth muscle tone spasms

Oxybutinin (TOPNOTCH)

18

for decreasing urgency in mild cystitis and dec. bladder spasm after urologic surgery

Oxybutinin (TOPNOTCH)

19

Usual antidote for early stage (48h) cholinesterase inhibitor poisoning, Must be administered before 6-8 hours of organophosphate bond with cholinesterase occurs

Pralidoxime (TOPNOTCH)

20

Competitively blocks all Nn nicotinic Ach receptors ; for Hypertensive emergencies (obsolete)

Hexamethonium, Mecamylamine, Trimethaptan (TOPNOTCH)

21

DOC for Anaphylaxis

Epinephrine (TOPNOTCH)

22

used for Cardiac arrest, anaphylaxis, asthma, COPD, Hemostasis

Epinephrine (TOPNOTCH)

23

for cardiogenic Shock and heart failure

Norepinephrine (TOPNOTCH)

24

causes vasodilation in splanchnic and renal blood vessels ; for cardiogenic Shock and heart failure

Dopamine (TOPNOTCH)

25

Beta nonselective sympathomimetic, for Asthma

Isoproterenol (TOPNOTCH)

26

SE: Rebound nasal congestion, hypertension, stroke, MI

Phenylephrine (TOPNOTCH)

27

A2 agonist, for Hypertension, Cancer pain, opioid withdrawal

Clonidine (TOPNOTCH)

28

Sedation, rebound hypertension, dry mouth

Clonidine (TOPNOTCH)

29

Sedation, positive Coomb's test (Hemolytic anemia)

Methyldopa (TOPNOTCH)

30

A2 agonist; reserved for ophthalmologic use in glaucoma for reduction of intraocular pressure

Apraclonidine, Brimonidine (TOPNOTCH)

31

B1 agonist, for cardiogenic shock and acute heart failure

Dobutamine (TOPNOTCH)

32

DOC as Asthma reliever, Rapid development of tolerance

Albuterol/Salbutamol (TOPNOTCH)

33

D1 agonist, for Hypertension

Fenoldopam (TOPNOTCH)

34

D2 agonist, restores dopamine actions in the CNS for Parkinson's disease, prolactinemia

Bromocriptine (TOPNOTCH)

35

Irreversibly blocks A1 and A2 receptors resulting to indirect baroreflex activation

Phenoxybenzamine (TOPNOTCH)

36

Reversible A1 and A2 receptor antagonist, for Pheochromocytoma and Rebound hypertension

Phentolamine (TOPNOTCH)

37

Blocks A1, for Benign Prostatic Hyperplasia, Hypertension

Prazosin, Doxazosin, Terazosin (TOPNOTCH)

38

Slightly selective A1a blockade causing relaxation of prostatic smooth muscles > vascular smooth muscle ; for BPH

Tamsulosin (TOPNOTCH)

39

Beta blockade > A1 blockade

Labetalol (TOPNOTCH)

40

Blocks B1 and B2 receptors

Propranolol, Nadolol, Timolol (TOPNOTCH)

41

B1 > B2 blockade

Metoprolol, Atenolol, Alprenolol, Betaxolol, Nebivolol (TOPNOTCH)

42

B1, B2 with intrinsic sympathomimetic (partial agonist) effect

Pindolol, Acebutolol, Carteolol, Bopindolol, Oxprenolol, Celiprolol, Penbutolol (TOPNOTCH)

43

Beta blockade > A1 blockade

Carvedilol, Medoxalol, Bucindolol, Labetalol (TOPNOTCH)

44

B1 > B2 blockade; for rapid control of BP and arrhythmias, thyrotoxicosis and myocardial ischemia intraoperatively ; for Supraventricular tachycardia

Esmolol (TOPNOTCH)

45

BB with direct vasodilating effect

Nebivolol (TOPNOTCH)

46

BB with local anesthetic effect

Propranolol (TOPNOTCH)

47

BB which is safe in pregnant patients

Labetalol (TOPNOTCH)

48

Mydriasis without cycloplegia

Phenylephrine (TOPNOTCH)

49

Cholinesterase Inhbitors with poor lipid solubility, oral, DOA: 30min-2h

Neostigmine (TOPNOTCH)

50

lower BP by decreasing volume

Diuretics (TOPNOTCH)

51

Inhibit NA/CL transporter in distal convoluted tubule

Thiazide Diuretics (TOPNOTCH)

52

for mild to moderate hypertension(first line), Heart falure, Nephrogenic Diabetes Insipidius, Renal calcium stones

Thiazide Diuretics (TOPNOTCH)

53

Thiazide Diuretics

HCTZ, Chlorthalidone, Metolazone, Indapamide (TOPNOTCH)

54

hyperlipidemia, hyperuricemia, sulfa allergy, hyperglycemia, hypercalcemia

HCTZ, Chlorthalidone, Metolazone, Indapamide (TOPNOTCH)

55

Inhibit NA/K/2Cl transporter in thick ascending limb of loop of Henle

Loop Diuretics (TOPNOTCH)

56

Loop Diuretics

Furosemide, Torsemide, Bumetanide, Ethacynic Acid (TOPNOTCH)

57

Hypokalemic metabolic alkalosis, Potassium wasting, ototoxicity, hyperuricemia, nephrotoxicity, dehydration, hypomagnesemia,sulfa allergy, hypocalcemia

Loop Diuretics (TOPNOTCH)

58

activates a2 adrenergic receptors ; for hypertensive urgency

Clonidine (TOPNOTCH)

59

activates a2 adrenergic receptors, for pre eclampsia

Methyldopa (TOPNOTCH)

60

Taper use prior to discontinuation to avoid rebound hypertension ; readily enter the CNS

Clonidine (TOPNOTCH)

61

Irreversibly blocks the vesicular monoamine transporter(VMAT)

Reserpine (TOPNOTCH)

62

Block release of NE from the pre-synaptic neuron

Guanethidine, Guanadrel (TOPNOTCH)

63

alpha-1 blocker which is most selective for prostatic smooth muscle

Tamsulosin (TOPNOTCH)

64

Disadvantage of Prazosin compared to other alpha-1 blockers

short DOA (TOPNOTCH)

65

Release NO from endothelial cells, Relaxes arteriolar smooth muscle, causing vasolidation. Decreases afterload ; for pre-eclampsia, hypertension, heart failure

Hydralazine (TOPNOTCH)

66

drug induced lupus (hydralazine), reflex tachycardia

Hydralazine (TOPNOTCH)

67

Opens K+ channels in vascular smooth muscle, causing hyperpolarization, muscle relaxation and vasolidation

Minoxidil, Diazoxide (TOPNOTCH)

68

for alopecia / male pattern baldness, hypertension

Minoxidil (TOPNOTCH)

69

Constipation, Nausea, flushing,gingival hyperplasia, AV block, sinus node depression, Pretibial edema, dizziness

Non-dihydropyridine calcium channel blocker: Verapamil, Diltiazem (TOPNOTCH)

70

block voltage-gated L-type calcium channels (vascular > cardiac); for Angina, hypertension

Dihydropyridine calcium channel blocker: Nifedipine, Amlodipine, Nicardipine, Nisoldipine, Isradipine, Felodipine (TOPNOTCH)

71

relaxes venous and arteriolar smooth muscle

Nitroprusside (TOPNOTCH)

72

for acute heart failure, controlled hypotension, cardiogenic shock, hypertensive emergency

Nitroprusside (TOPNOTCH)

73

a thiazide derivative without a diuretic effect ; also induces insulin release (can be used to treat hypoglycemia in insulin-producing tumors)

Diazoxide (TOPNOTCH)

74

causes arteriolar vasolidation of the afferent and efferent arterioles

Fenoldopam (TOPNOTCH)

75

inhibit angiotensin converting enzyme ; for hypertension, heart failure

ACE inhibitors: Captopril, Enalapril, Lisinopril, Benazepril (TOPNOTCH)

76

slows down the progression of DM nephropathy and cardiac remodelling in heart failure

ACE inhibitors: Captopril, Enalapril, Lisinopril, Benazepril (TOPNOTCH)

77

competetively blocks Angiotensin 1 receptor site ; for hypertension

Angiotensin receptor blocker: Losartan, Valsartan, Irbesartan, Candesartan (TOPNOTCH)

78

inhibitor of renin's action on its substrate angiotensinogen

Aliskerin (TOPNOTCH)

79

releases nitric oxide(NO), relaxes smooth muscle, especially vascular, increases Cgmp (cyclic guanosine monophosphate); for cyanide poisoning

Amyl Nitrite (TOPNOTCH)

80

releases nitric oxide (NO), increases Cgmp (cyclic guanosine monophosphate) and relaxes smooth muscle especially vascular; for Angina, acute coronary syndromes

Nitroglycerin, Isosobide Dinitrate, Isosobide Mononitrate (TOPNOTCH)

81

Dangerous hypotension with PDE inhibitors

Nitroglycerin, Isosobide Dinitrate, Isosobide Mononitrate (TOPNOTCH)

82

block voltage-gated L-type calcium channels (cardiac > vascular); for Angina, Supraventricular tachycardia, migraine, hypertension

Non-dihydropyridine calcium channel blocker: Verapamil, Diltiazem (TOPNOTCH)

83

inhibits Na/K ATPase; increases intracellular Ca, increasing cardiac contractility; for heart failure, Nodal arrythmias

Digoxin (TOPNOTCH)

84

Arrythmogenesis increased hypokalemia, hypercalcemia, hypomagnesemia

Digoxin (TOPNOTCH)

85

Hyperkalemia exacerbates cardiac toxicity

Class 1 Antiarryhtmics (TOPNOTCH)

86

Prolong AP duration

Class 1A: Procainamide, Disopyramide, Quinidine (TOPNOTCH)

87

Shorten AP Duration

Class 1B: Lidocaine, Mexiletene, Tocainide, Phenytoin (TOPNOTCH)

88

No effect on AP Duration

Class 1C: Flecainide, Propafenone, Encainide, Moricizine (TOPNOTCH)

89

Group with the greatest risk for TDP

Class 3 Arryhytmics (TOPNOTCH)

90

for Post MI prophylaxis against sudden death, thyrotoxicosis, acute perioperative and thyrotoxic arrythmias, Supraventricular tachycardia

Class 2: Propranolol, Esmolol (TOPNOTCH)

91

has Class 1, 2 3 and 4 activity therefore is the MOST EFFICACIOUS of all anti-arrhythmics

Amiodarone (TOPNOTCH)

92

DOC for paroxysmal supraventricular tachycardia

Adenosine (TOPNOTCH)

93

for glaucoma, diuresis for edema with alkalosis.

Carbonic Anhydrase Inhibitors (TOPNOTCH)

94

Carbonic Anhydrase Inhibitors

Acetazolamide, Dorzolamide, Brinzolamide, Dichlorphenamide, Methaolamide (TOPNOTCH)

95

Efficacy decreasedby NSAIDs

Loop Diuretic, Thiazide Diuretics (TOPNOTCH)

96

For hypertension Hypercalciuria, Heart failure, Nephrogenic diabetes insipidius, renal calcium stones

Thiazide Diuretics: Hydrochlorothiazide, Chlorthalidone, Indapamide, Metolazone (TOPNOTCH)

97

Cause powerful diuresis and increased Ca excretion

Loop Diuretic: Furosemide, Bumetanide, Torsemide (TOPNOTCH)

98

Steroid inhibitors of cytoplasmic aldosterone receptor in cortical collecting ducts. Reduce K excretion;

Spironolactone, Eplerenone(Aldosterone Antagonist) (TOPNOTCH)

99

Inhibitor of ENaC (Epithelial sodium channels) in cortical collecting duct, reduces Na reabsorption and K excretion; for hypokalemia

Amiloride, Triamterene (TOPNOTCH)

100

reduces progression of DM nephropathy and reduces mortality post MI

Eplerenone (TOPNOTCH)

101

Osmotic Diuretics

Mannitol, Glycerin, Isosorbide, Urea (TOPNOTCH)

102

Transient volume expansion (hyponatremia, pulmonary edema; followed by hypernatremia) nausea, headache, dehydration, vomiting

Osmotic Diuretics SE (TOPNOTCH)

103

Agonists at V1 and v2 ADH receptors. Activate insertion of aquaporin water channels in collecting tubule.

Antidiuretic hormone, Desmopressin (TOPNOTCH)

104

Antagonist at V1a, V2 receptors; for SIADH and Hyponatremia

Conivaptan, Tolvaptan, Lixivaptan (TOPNOTCH)

105

more likely to block autonomic receptors, also has alpha1 blocking and local anesthetic effect

1st Generation antihistamines (TOPNOTCH)

106

Reversible blockade of histamine H1-receptor sites on tissues, No sedation and antimuscarinic effects

2nd Generation antihistamines (TOPNOTCH)

107

may cause arrhythmia due to blockade of cardiac potassium channels

acrivastine, astemizole, cetirizine, loratadine, and terfenadine (TOPNOTCH)

108

reduction of nocturnal acid secretion in gastirc and duodenal ulcer

H2 antagonists (TOPNOTCH)

109

True or False: H2 antagonists have H1-blocking effect

FALSE (TOPNOTCH)

110

True or False: Ranitidine is a CYP450 inhibitor

TRUE, but weak inhibitor only (TOPNOTCH)

111

Agonist at the 5HT1D receptor in the blood vessels causing vasocontriction ; 1st line treatment for Acute migraine and cluster headache attacks

5HT1D receptor agonist: Sumatriptan, Naratriptan, Almotriptan, Eletriptan, Frovatriptan, Rizatriptan, Zolmitriptan (TOPNOTCH)

112

Selectively block 5HT3 receptors ; For antiemesis in patients post-chemotherapy or post-operation

5HT3 receptor antagonist: Ondansetron, Granisetron, Dolasetron, Alosetron (TOPNOTCH)

113

can inc QRS and QT (proarrhythmic effect) duration so never use in patients with heart disease

Dolasetron (TOPNOTCH)

114

SE: gangrene (sec to Ischemia) in overdose, unusual hyperplasia of the retroperitoneal, retropleural or subendocardial cavity --> hydronephrosis, cardiac valvular and conduction system malfunction

Ergotamine (TOPNOTCH)

115

uterus becomes more sensitive to ergots during pregnancy, produce very powerful and long-lasting contraction leading to decreased bleeding, Never give before delivery of placenta

Ergonovine (TOPNOTCH)

116

PGE1 analogue, causes increased HCO3 and mucus secretion in stomach and uterine contraction

Misoprostol, Gemeprost (TOPNOTCH)

117

may also be used together with Mifepristone or Methotrexate as safe abortifacient

Misoprostol (TOPNOTCH)

118

Low concentrations contract, higher concentrations relax uterine and cervical smooth muscle, soften cervix at term before induction with oxytocin

Dinoprostone, Sulprostone (TOPNOTCH)

119

PGF2a analogue, increases outflow of aqueous humor thus reduces intraocular pressure; For glaucoma

Prostaglandin F2a analog: Latanoprost, Arboprost, Bimatoprost, Travoprost, Unoprostone (TOPNOTCH)

120

used primarily for pulmonary hypertension

Prostaglandin I2 analog: Epoprostenol, Beraprost, Iloprost, Treprostinil (TOPNOTCH)

121

SE: Tachycadia, Nervousness, tremors, restlessness, arrythmias when used excessively, loss of responsiveness (tolerance, tachyphylaxis)

Beta2-selective agonist (short-acting): Albuterol/Salbutamol, Levalbuterol, Terbutaline, Metaproterenol, Pirbuterol, Procaterol, Fenoterol (TOPNOTCH)

122

Increase asthma mortality when used alone; May precipitate arrhytmias; usual DOA: 12hrs

Beta2-selective agonist (long acting): Salmeterol, Formoterol, Cleneterol, Bambuterol (TOPNOTCH)

123

More effective and less toxic than beta agonists ith COPD

Muscarinic receptor antagonist: Ipratropium, Tiotropium (TOPNOTCH)

124

Phosphodiesterase inhibitor, Adenosine receptor antagonist, causes bronchodilation and inc. strength of contraction of diaphragm; For asthma esp in nocturnal attacks

Methylxanthines: Theophylline, Aminophylline, Pentoxifylline (TOPNOTCH)

125

Antidote in overdosage is BB. Higher clearance in adolescents and smokers. Narrow therapeutic window

Methylxanthines: Theophylline, Aminophylline, Pentoxifylline (TOPNOTCH)

126

Prevents calcium influx and stabilizes mast cells, preventing degranulation and release of histamine, leukotrienes and mediators; for Asthma prophylaxis and allergies

Mast cell Stabilizer: Cromolyn, Nedocromil, Lodoxamide (TOPNOTCH)

127

DOC for Asthma prophylaxis, First line treatment for moderate to severe BA, COPD

Corticosteroid: Fluticasone, Beclomethasone, Budesonide, Flunisolide, Mometasone, Triamcinolone, Ciclosenide (TOPNOTCH)

128

For status asthmaticus

use IV prednisolone or hydrocortisone (TOPNOTCH)

129

active metabolite of prednisone

prednisolone (TOPNOTCH)

130

Inhibitor of 5-lipoxygenase. Reduces synthesis of leukotrienes. Prevents airway inflammation and bronchoconstriction; For asthma prophylaxis

Zileuton (TOPNOTCH)

131

No bronchodilator action, not recommended for acute BA attack

Zileuton, Montelukast, Zafirlukast, Pranlukast (TOPNOTCH)

132

Binds IgE antibodies on sensitized mast cells and prevents activation by BA triggers and subsequent release of inflammatory mediators; For prophylaxis of severe, refractory asthma not responsive to all other drugs

Anti-IgE antibody: Omalizumab (TOPNOTCH)

133

bind GABA-A receptor subunits to increase frequency of chloride channel opening which causes membrane hyperpolarization

benzodiazepines (TOPNOTCH)

134

SE: anterograde amnesia, decreased psychomotor skills, unwanted daytime sedation, tolerance, dependence liability and rebound insomnia or anxiety

benzodiazepines (TOPNOTCH)

135

BZD that can be used for seizure disorders, Bipolar disorder and infantile spasm

Clonazepam (TOPNOTCH)

136

Why is Lorazepam preferred over Diazepam in status epilepticus

due to its long distribution halflife (TOPNOTCH)

137

date-rape drug

Flunitrazepam (TOPNOTCH)

138

BZD used for alcohol withdrawal

Diazepam and Chlordiazepoxide (TOPNOTCH)

139

antagonist at benzodiazepine sites on GABA-A receptor

Flumazenil (TOPNOTCH)

140

bind to GABA-A receptor sites to increase duration of chloride channel opening, block glutamic acid neurotransmission

barbiturates (TOPNOTCH)

141

which has greater dependence liability: barbiturates or benzodiazepine

barbiturates (TOPNOTCH)

142

Barbiturate with the highest lipid solubility

Thiopental (TOPNOTCH)

143

barbiturate for status epilepticus

Phenobarbital (TOPNOTCH)

144

SE: acute intermittent porphyria

barbiturates (TOPNOTCH)

145

High dose BZD and Barbs may suppress seizure but at the expenses of marked sedation EXCEPT for

Clonazepam and Phenobarbital (TOPNOTCH)

146

only interact with GABA-A receptors with alpha-1 subunit; For insomnia and sleep disorder esp when sleep onset is delayed

Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)

147

dependence liability and withdrawal symptoms is less than that of benzodiazepines

Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)

148

lack anti-convulsant, anti-anxiety and muscle relaxant effects, effects are reversed with Flumazenil, very rapid onset of action, may dec REM sleep

Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)

149

increasing use due to rapid onset with minimal effects on the sleep pattern and cause less daytime cognitive impairment as compared to BZD

Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)

150

partial agonist at 5-HT1A receptors and possibly D2 receptors, used For generalized anxiety disorders

Buspirone (TOPNOTCH)

151

slow onset of action (more than 1week), metabolized by CYP3A4, safe for pregnant patients

Buspirone (TOPNOTCH)

152

activates melatonin receptors (MT1 and MT2 receptors) in the suprachiasmatic nuclei in the CNS leading to dec latency of sleep onset

Ramelteon (TOPNOTCH)

153

block voltage-gated Na channel; DOC for generalized tonic-clonic seizures, DOC for partial seizures, can be used for migraine

Phenytoin, Fosyphenytoin, Mephenytoin, Ethotoin (TOPNOTCH)

154

SE: nystagmus, diplopia, sedation, gingival hyperplasia, hirsutism, anemias, peripheral neuropathy (absent DTRs), osteoporosis, fetal hydantoin syndrome, abnormalities in Vit D metabolism

Phenytoin, Fosyphenytoin, Mephenytoin, Ethotoin (TOPNOTCH)

155

preferred in prolonged therapy for status epilepticus because it is less sedating

phenytoin (TOPNOTCH)

156

block voltage-gated Na channels and decreases glutamate release; DOC for trigeminal neuralgia, DOC for generalized tonic-clonic seizures, DOC for partial seizures, for bipolar disorders

Carbamazepine, Oxcarbazepine (TOPNOTCH)

157

SE: diplopia, cognitive dysfunction, drowsiness, ataxia, blood dyscrasias, Stevens-Johnson syndrome, erythematous rash, teratogen (spina bifida and craniofacial anomalies), hyponatremia

Carbamazepine, Oxcarbazepine (hyponatremia) (TOPNOTCH)

158

may be used for acute manic phase and as prophylaxis in the depressive phase

Carbamazepine, Oxcarbazepine (TOPNOTCH)

159

blocks high-frequency firing of neurons which modifies amino acid metabolism; DOC for bipolar disorder (acute mania), DOC for generalized tonic-clonic seizures and absence seizure, partial seizures, myoclonic seizures, also used for Bipolar disorders

Valproic acid (TOPNOTCH)

160

anti-manic that is CYP450 inhibitor

Valproic acid (TOPNOTCH)

161

for status epilepticus in children ; primary anticonvulsant in infants, children and pregnant patients

Phenobarbital (TOPNOTCH)

162

inhibit low threshold (T-type) Ca currents esp in thalamic neurons ; DOC for absence seizure

Ethosuximide, Phensuximide, Methsuximide (TOPNOTCH)

163

blocks Ca channels, increases GABA release ; For neuropathic pain such as postherpetic neuralgia, partial seizures, migraine

Gabapentin, Pregabalin (TOPNOTCH)

164

structural analogues of GABA but does not activate GABA receptor directly ; also have the same effect on Ca currents like Ethosuximide

Gabapentin, Pregabalin (TOPNOTCH)

165

blocks Na and Ca channels and decreases glutamate, used for acute manic phase and as prophylaxis in the depressive phase

Lamotrigine (TOPNOTCH)

166

primarily undergoes glucuronidation reaction ; SE: dizziness, ataxia, nausea, rash, SJS / TEN

Lamotrigine (TOPNOTCH)

167

Bind synaptic protein selectively inhibiting hypersynchronization of epileptiform burst firing ; For generalized tonic-clonic seizures, partial seizures

Levetiracetam (TOPNOTCH)

168

not metabolized by CYP450 enzymes, eliminated in the kidneys in their unchanged form

Levetiracetam (TOPNOTCH)

169

multiple actions on synaptic function, probably via actions on phosphorylation (Na, Ca, GABA, AMPA-glutamate, carbonic anhydrase)

Topiramate, Felbamate (TOPNOTCH)

170

also facilitate the inhibitory actions of GABA but its exact MOA is still unknown

Felbamate (TOPNOTCH)

171

Antiseizure drugs with the most number of MOA, undergo both hepatic and renal metabolism

Topiramate, Felbamate (TOPNOTCH)

172

Irreversibly inactivates GABA aminotransaminase (GABA-T) which terminates the action of GABA ; For GTC seizure

Vigabatrin (TOPNOTCH)

173

Inhibits GABA transporter (GAT-1) in neurons and glia thus inhibiting its reuptake, leading to prolongation of GABA effects ; For partial seizures

Tiagabine (TOPNOTCH)

174

SE: visual field defects

Vigabatrin (TOPNOTCH)

175

Facilitates GABA-mediated inhibition, block brain NMDA and Ach-N receptors

Inhalational anesthetics (TOPNOTCH)

176

SE: megaloblastic anemia on prolonged exposure; Euphoria (laughing gas), bronchodilation

Nitrous Oxide (TOPNOTCH)

177

Lowest Potency (highest MAC) and least cardiotoxic

Nitrous Oxide (TOPNOTCH)

178

all inhaled anesthetcis cause bronchodilation except

Desflurane (TOPNOTCH)

179

SE: catecholamine-induced arrhythmias, peripheral vasodilation, bronchodilation

Isoflurane (TOPNOTCH)

180

SE: spike-and-wave activity in EEG, muscle twitching, breath-holding, myocardial depression, renal insufficiency (due to Flourine release), dec cardiac output, bronchodilation

Enflurane (TOPNOTCH)

181

has pungent odor which limits its use

Enflurane (TOPNOTCH)

182

SE: catecholamine-induced arrhythmias, myocardial depression, post-operative hepatitis, dec cardiac output, bronchodilation

Halothane (TOPNOTCH)

183

Highest potency and lowest MAC (very slow onset and recovery)

Methoxyflurane (TOPNOTCH)

184

a usual adjunct with inhalational anesthetics and IV opioids, has a slow onset but longer DOA

Midazolam (TOPNOTCH)

185

Blocks excitation by glutamate at NMDA receptors; For dissociative anesthesia (analgesia, amnesia and catatonia but with retained consciousness)

Ketamine (TOPNOTCH)

186

congener of Phencyclidine / angel dust

Ketamine (TOPNOTCH)

187

For general anesthesia to patients with limited cardiac or respiratory reserve

Etomidate (TOPNOTCH)

188

Interacts with mu, sigma, kappa receptors for endogenous opioid peptides ; For high risk patients who might not survive general anesthesia

Opioid analgesics: Fentanyl, morphine, alfentanil, remifentanil (TOPNOTCH)

189

SE: respiratory depression, chest wall rigidity (which may cause impaired ventilation) and constipation

Opioid analgesics: Fentanyl, morphine, alfentanil, remifentanil (TOPNOTCH)

190

Antidote is Naloxone / Naltrexone

Opioid toxicity (TOPNOTCH)

191

milk of anesthesia

Propofol, Fospropofol (TOPNOTCH)

192

Potentiates GABA-A receptors, blocks Na channels; For prolonged sedation esp in ICU patients and also in OPD surgeries

Propofol, Fospropofol (TOPNOTCH)

193

Blockade of Na channels slows which prevents axon potential propagation

Local Anesthetics (TOPNOTCH)

194

Shortest half-life among local anesthetics

Procaine (TOPNOTCH)

195

For local anesthesia, topical anesthesia

Benzocaine, Cocaine, Tetracaine (TOPNOTCH)

196

Use cautiously in sunburns, Topical only

Benzocaine (TOPNOTCH)

197

with intrinsic sympathomimetic activity so it does not need an alpha agonist (like epinephrine) to limit its systemic absorption

Cocaine (TOPNOTCH)

198

All local anesthetics are vasodilators EXCEPT

Cocaine (TOPNOTCH)

199

SE: light-headedness, sedation, restlessness, nystagmus, seizures, respiratory, CV depression, abuse liability, severe hypertension, cerebral hemorrhage, cardiac arrhythmia, MI

Cocaine (TOPNOTCH)

200

For local anesthesia, spinal anesthesia, epidural anesthesia, topical ophthalmic anesthesia

Tetracaine (TOPNOTCH)

201

Blockade of Na channels slows which prevents axon potential propagation; For local anesthesia, antiarrythmia (group 1B activity), used for post-MI and for digitalis toxicity

Lidocaine (TOPNOTCH)

202

For local anesthesia, dental anesthesia

Prilocaine (TOPNOTCH)

203

local anesthetic that can cause methemoglobinemia

Prilocaine (TOPNOTCH)

204

For local anesthesia, epidural anesthesia, intrathecal anesthesia

Bupivacaine (TOPNOTCH)

205

Use with caution in pregnant women and patients with cardiac disease (may cause heartblock, arrhyhtmia and hypotension)

Bupivacaine (TOPNOTCH)

206

Longest half-life among local anesthesia

Ropivacaine (TOPNOTCH)

207

Depolarizing Neuromuscular Blocker

Succinylcholine (TOPNOTCH)

208

Agonist at Ach-N receptors causing initial twitch then persistent depolarization

Succinylcholine (TOPNOTCH)

209

SE: muscle pain, hyperkalemia, increased intragastric pressure leading to regurgitation (aspiration), increased intraocular pressure, malignant hyperthermia

Succinylcholine (TOPNOTCH)

210

Metabolized by pseudocholinesterase ; may cause malignant hyperthermia if given together with inhaled anesthetics

Succinylcholine (TOPNOTCH)

211

a common SE for this group is Histamine release

Non-Depolarizing Neuromuscular Blocker (TOPNOTCH)

212

Undergoes Hoffman elimination (rapid spontaneous breakdown)

Atracurium (TOPNOTCH)

213

converted to Laudanosine which can cause seizures

Atracurium (TOPNOTCH)

214

short-acting Non-Depolarizing Neuromuscular Blocker

Mivacurium (TOPNOTCH)

215

intermediate-acting Non-Depolarizing Neuromuscular Blocker ; Undergoes elimination in bile

Vecuronium (TOPNOTCH)

216

Suggamadex is a novel reversal agent for

Rocuronium (TOPNOTCH)

217

Competitive antagonists at skeletal muscle nicotinic acetylcholine receptors; For skeletal muscle relaxation during intubation and general anesthesia

Non-Depolarizing Neuromuscular Blocker (TOPNOTCH)

218

long-acting Non-Depolarizing Neuromuscular Blocker; may cause heart block

Pancuronium (TOPNOTCH)

219

Relatively contraindicated in myocardial ischemia; reverse effects with neostigmine

Tubocurarine (TOPNOTCH)

220

a dopamine precursor

Levodopa (TOPNOTCH)

221

inhibits peripheral metabolism via dopa decarboxylase

carbidopa (TOPNOTCH)

222

SE: GI upset (emesis), dyskinesia (choreoathetosis), behavioural changes (anxiety, agitation, confusion, delusion), on-off phenomena, wearing-off phenomena, postural hypotension, tachycardia

Levodopa-carbidopa (TOPNOTCH)

223

Partial agonist at dopamine D2 receptors in brain

Bromocriptine, Pergolide (TOPNOTCH)

224

For Parkinson's disease which is levodopa intolerance, hyperprolactinemia

Bromocriptine, Pergolide (TOPNOTCH)

225

SE: anorexia, n/v, dyskinesia, postural hypotension, behavioural changes, erythromelalgia, pulmonary infiltrate

Bromocriptine (TOPNOTCH)

226

Partial agonist at dopamine D3 receptors in brain

Pramipexole (TOPNOTCH)

227

SE: Contraindicated for patients with active peptic ulcer disease, psychotic illnesss or recent MI

Pramipexole, Ropinirole (TOPNOTCH)

228

Partial agonist at dopamine D3 receptors, antagonist at 5-HT and alpha adrenoceptors

Apomorphine (TOPNOTCH)

229

For off-periods of Parkinson's disease, alcoholism, opiate addiction, erectile dysfunction, alzheimer's disease

Apomorphine (TOPNOTCH)

230

Selective inhibitors of MAO type B leading to decreased degradation of dopamine, increases response to levodopa/carbidopa

Selegiline, Rasagiline (TOPNOTCH)

231

Block L-dopa metabolism by inhibiting catechol-O-methyltransferase in periphery and CNS, prolongs response to levodopa

Entacapone, Tolcapone (TOPNOTCH)

232

T or F: Entacapone only acts in the periphery while Tolcapone acts both in the periphery and CNS

TRUE (TOPNOTCH)

233

enhances dopaminergic transmission by unknown mechanism, maybe by influencing the synthesis, release or reuptake of dopamine

Amantadine (TOPNOTCH)

234

SE: behavioral changes (restlessness, agitation, insomnia, hallucination, psychosis), livedo reticularis, GI disturbances, urinary retention, postural hypotension, peripheral edema

Amantadine (TOPNOTCH)

235

Decrease the excitatory actions of cholinergic neurons on cells in the striatum by blocking muscarinic receptors

Benztropine, Biperiden, Trihexyphenidyl, Orphenadrine (TOPNOTCH)

236

as adjunct for parkinson's disease and extrapyramidal symptoms caused by antipsychotics

Benztropine, Biperiden, Trihexyphenidyl, Orphenadrine (TOPNOTCH)

237

Blocks D2 receptos more than 5-HT2 receptors

Typical Antipsyhotics (TOPNOTCH)

238

Typical Antipsychotic, SE: retinal deposits and arryhthmias

Thioridazine (TOPNOTCH)

239

has the Strongest autonomic effects; only antipsychotic with fatal overdose

Thioridazine (TOPNOTCH)

240

For schizophrenia and other psychotic disorders, huntington's disease and tourette's syndrome

Haloperidol, Droperidol (TOPNOTCH)

241

SE: extrapyramidal dysfunction, tardive dyskinesia, hyperprolactinemia, neuroleptic malignant syndrome

Haloperidol, Droperidol (TOPNOTCH)

242

Only antipsychotic that reduces the risk of suicide

Clozapine (TOPNOTCH)

243

For schizophrenia (refractory, suicidal) and other psychotic disorders

Clozapine (TOPNOTCH)

244

Blocks 5-HT2 receptors more than D2 receptors

Atypical Antipsychotics (TOPNOTCH)

245

SE: Extrapyramidal dysfunction (less), hyperprolactinemia (less), postural hypotension, weight gain, hyperglycemia, hyperlipidemia, myocarditis, agranulocytosis, seizures, ileus, hypersalivation (sialotthea)

Clozapine (TOPNOTCH)

246

weight gain and hyperglycemia is prominent, safe in pregnancy

Olanzapine (TOPNOTCH)

247

SE: Extrapyramidal dysfunction (less), hyperprolactinemia (less), postural hypotension, weight gain, somnolence, fatigue, sleep paralysis, hypnagogic hallucinations, cataracts, priapism, QT prolongation (TDP) ; safe in pregnancy

Quetiapine (TOPNOTCH)

248

Only antipsychotic approved for schizophrenia in the youth

Risperidone (TOPNOTCH)

249

Increased mortality in elderly patients with dementia-related psychosis ; can cause TDP

Ziprasidone (TOPNOTCH)

250

Least sedating atypical antipsychotics

Aripiprazole (TOPNOTCH)

251

Uncertain MOA but the proposed MOA is by inhibiting the enzyme involved in the recycling of neuronal membrane phosphoinositides which causes depletion of phosphatidylinositol bisphosphate, thus consequently decreasing IP3 and DAG leading to decreased neurotransmission

Lithium (TOPNOTCH)

252

SE: Tremor, sedation, ataxia, aphasia, thyroid enlargement, hypothyroidism, reversible nephrogenic diabetes insipidus, edema, acneiform skin eruption, leukocytosis, teratogen (ebstein's anomaly), bradycardia

Lithium (TOPNOTCH)

253

Block NE and 5-HT transporters leading to potentiation of NT action at postsynaptic receptors

Tricyclic Antidepressants (TOPNOTCH)

254

Tricyclic Antidepressants

Imipramine, Clomipramine, Desipramine, Amitryptyline, Nortryptiline (TOPNOTCH)

255

For MDD (most effective), bipolar disorder, acute panic attacks, ADHD, chronic pain states, as sleeping aid, OCD ; this group is very useful for patients with psychomotor retardation, sleep disturbance, poor appetite and weight loss

Imipramine, Clomipramine, Desipramine, Amitryptyline, Nortryptiline (TOPNOTCH)

256

3Cs of TCA overdose

Coma, Cardiotoxicity, Convulsions (TOPNOTCH)

257

longterm use may lead to down-regulation of Beta receptors leading to a decrease in BP and depression of cardiac conduction

Tricyclic Antidepressants (TOPNOTCH)

258

Inhibits neuronal reuptake of serotonin by inhibiting Serotonin Transporter (SERT)

SSRI (TOPNOTCH)

259

SSRIs

Fluoxetine, Paroxetine, Citalopram, Escitalopram, Sertraline, Fluvoxamine (TOPNOTCH)

260

DOC for OCD, for MDD, anxiety, panic attacks, phobias, PTSD, GAD, bulimia, premenstrual dysphoric disorder, alcohol dependence

Fluoxetine, Paroxetine, Citalopram, Escitalopram, Sertraline, Fluvoxamine (TOPNOTCH)

261

This antidepressant group can decrease appetite leading to weight loss

SSRI (TOPNOTCH)

262

Inhibits neuronal reuptake of serotonin and norepinephrine by binding to transporters for both 5HT and NE

SNRI (TOPNOTCH)

263

SNRIs

Venlafaxine, Duloxetine, Desvenlafaxine (TOPNOTCH)

264

differ from TCA in lacking blockade of H1, M and alpha receptors ; Increased risk for suicide in children and adolescents

SNRIs (TOPNOTCH)

265

Blocks 5-HT2A receptors, weak inhibitor of NE and 5HT transporters

Serotonin antagonist (TOPNOTCH)

266

Antidepressant Serotonin antagonist

Trazodone, Nefazodone (TOPNOTCH)

267

Strong norepinephrine reuptake inhibitor and weak serotonin reuptake inhibitor, blocks dopamine D2 receptors

Tetracyclics: Amoxapine (TOPNOTCH)

268

Increases amine release from nerve endings by antagonism of presynaptic a2 adrenoceptors, also blocks serotonin 5-HT2A receptors

Tetracyclics: Mirtazapine (TOPNOTCH)

269

Inhibits neuronal reuptake of dopamine and norepinephrine, increase dopamine and norepinephrine activity

Tetracyclics: Bupropion (TOPNOTCH)

270

Inhibits MAO type A and type B, increases CNS levels of NE and serotonin

Phenelzine, tranylcypromine (TOPNOTCH)

271

MAO-B selective inhibitor

Selegiline (TOPNOTCH)

272

Triad of opioid overdose

miosis, coma, respiratory depression (TOPNOTCH)

273

Strong agonist at u receptors; For severe pain, pain associated with acute MI, for pulmonary edema

Morphine (TOPNOTCH)

274

morphine is metabolized in the body to _____ which has equal analgesic activity as morphine

morphine-6-glucuronide (TOPNOTCH)

275

Strong agonist at u receptors; For severe pain, adjunct in anesthesia, chronic pain and breakthrough cancer pain

Fentanyl (TOPNOTCH)

276

Strong agonist at u and k receptors, inhibits pain neurotransmission, muscarinic blocking actions; For moderate to severe pain, labor analgesia, spasmodic pain (biliary, renal), preoperative sedation

Meperidine (TOPNOTCH)

277

Only opioid that does not cause miosis and biliary contraction

Meperidine (TOPNOTCH)

278

opioid of choice for pain relief in pancreatitis

Meperidine (TOPNOTCH)

279

metabolized to normeperidine which can cause _____ therefore contraindicated in patients with ______

seizure, seizure disorder (TOPNOTCH)

280

full opioid agonist, Strong agonist at u receptors, inhibits pain neurotransmission, binds NMDA receptors and antagonizes the effects of glutamate; For moderate to severe pain, opioid dependence, opioid withdrawal

Methadone (TOPNOTCH)

281

used as maintenance therapy for opioid dependence

Methadone (TOPNOTCH)

282

Decreases sensitivity of cough receptors, depressing the medullary cough center through sigma receptors stimulation; For cough suppression

Dextrometorphan, codeine (TOPNOTCH)

283

codeine is metabolized by CYP2D6 to ______

morphine (TOPNOTCH)

284

SE: miosis, restlessness, respiratory depression, increased ICP, postural hypotension, urinary retention, pruritus, addiction liability

Opioid analgesics (TOPNOTCH)

285

Mixed Agonist-Antagonist: Strong agonist at k receptors, weak antagonist activity at u receptors

Nalbuphine, buprenorphine, butorphanol, pentazocine (TOPNOTCH)

286

Weak agonist at u receptors, inhibits pain neurotransmission; For mild to moderate pain, restless leg syndrome

Propoxyphene, levopropoxyphene, dextropropoxyphene (TOPNOTCH)

287

Competitively blocks u, sigma and k receptors, rapidly reverses effects of opioid agonists; For opioid overdose, opioid and alcohol dependence

Naloxone, naltrexone, nalmefene (TOPNOTCH)

288

Weak agonist at u receptors, inhibits neuronal reuptake of serotonin and norepinephrine; For moderate pain, chronic pain syndrome, neuropathic pain

Tramadol (TOPNOTCH)

289

Required for the biosynthesis of heme and heme containing proteins, including hemoglobin and myoglobin; For Iron deficiency anmia, iron supplementation

Ferrous sulfate, Ferrous gluconate, Ferrous Fumarate, Iron dextran, Sodiun Ferric Gluconate complex, Iron sucrose (TOPNOTCH)

290

Chelates excess iron; For acute and chronic iron poisoning

Deferoxamine, Deferasirox (TOPNOTCH)

291

Cofactor required for essential enzymatic reactions that form tetrahydrofolate, convert homocysteine to methionine and metabolize methymalonyl-CoA; For vitamin B12 deficiency, megaloblastic anemia

Cyanocobalamin, Hydroxocobalamin (TOPNOTCH)

292

Precursor of an essential donor of methyl groups used for synthesis of amino acids, purines and deoxynucleotide; For Megaloblastic anemia, prevention of neutral tube defects(spina bifida), prevention of coronary artery disease

Folic acid (TOPNOTCH)

293

Agonist of erythropoietin receptors expressed by red cell progenitors; For Anemia, associated with chronic renal failure, cancer, HIV infection and prematurity

Epoetin Alfa, Darbepoetin alfa, Methoxy Polyethylene Glycol- Epoetin Beta (TOPNOTCH)

294

Binds receptors on myeloid progenitors and stimulates cell maturation and proliferation ; Accelerates neutrophil recovery and reduces incidence of infection; For neutrophenia associated with chemotheraphy, myelodysplasia, and aplastic anemia

(G-CSF) Filgrastim, Sargamostim (GM-CSF), Pegfilgrastim (TOPNOTCH)

295

Recombinant form of an endogenous cytokine; activates IL -11 receptors ; For secondary prevention of thrombocytopenia in patients undergoing chemotheraphy

Oprelvekin(IL-11),Thrombopoietin (TOPNOTCH)

296

nhibits rate-limit in enzyme in cholesterol biosynthesis (HMG-CoA reductase), Increased hepatic cholesterol uptake, Increased high affinity LDL receptors which leads to decreased LDL levels

Simvastatin, Atorvastatin, Rosuvastatin, Fluvastatin, Pravastatin, Lovastatin, Pitavastatin, Cerivastatin (TOPNOTCH)

297

DOC for hypercholesterolemia(high LDL), decrease risk of acute coronary syndromes, ischemic stroke

Simvastatin, Atorvastatin, Rosuvastatin, Fluvastatin, Pravastatin, Lovastatin, Pitavastatin, Cerivastatin (TOPNOTCH)

298

Prominent SE of statins: ____

Hepatoxicity, Myopathy, Rhabdomyolysis (TOPNOTCH)

299

Increased risk of myopathy and rhabdomyolysis when statins are used with

Fibrates (TOPNOTCH)

300

non-absorbable polyemers that bind bile acids and similar steroids in the intestines preventing their reabsorption, increases cholesterol utilization for replacement, modestly lowers LDL levels by increasing hepatic LDL receptors

Bile Acid Binding Resin (TOPNOTCH)

301

Bile Acid Binding Resin

Colesevelam, Colestipol, Cholestyramine (TOPNOTCH)

302

SE: Constipation, Bloating, Gritty taste, Gallstone formation, steatorrhea, malabsortion of fat soluble substances (vitamin k, folate)

Colesevelam, Colestipol, Cholestyramine (TOPNOTCH)

303

Selective inhibitor of the NCP1L1 transporter decreasing intestinal absorption of cholesterol and other phytosterols, decreases cholesterol hepatic pool, increases hepatic LDL receptors

NPC1L1 transporter inhibitor (TOPNOTCH)

304

NPC1L1 transporter inhibitor

Ezetimibe (TOPNOTCH)

305

Cholesterol analog, takes the place of dietary and billiary cholesterol, decreasing intestinal absorption of cholesterol and other phytosterols

Sitosterol (TOPNOTCH)

306

Decreases VLDL synthesis and LDL cholesterol concentrations, decreases hormone-sensitive lipase activity leading to decreased LDL levels, Increases HDL cholesterol by decreasing its catabolism

Niacin (TOPNOTCH)

307

DOC for increasing HDL levels

Niacin (TOPNOTCH)

308

SE: Flushing, nausea, vomiting, Pruritus, Acanthosis nigricans, Rashes, Gastrointestinal irritation, Hepatoxicity (mild), Hyperuricemia, Impaired glucose tolerance, Arrythmias, Amyblopia

Niacin (TOPNOTCH)

309

Activates PPAR-_ and increases expression of lipoprotein lipase and apolipoproteins (apoA-I, apoA-II) leading to enhanced clearance of TG-rich lipoproteins, Lowers triglycerides, Increases HDL

Fibrates (TOPNOTCH)

310

DOC for hypertriglyceridemia

Fibrates (TOPNOTCH)

311

Fibrates

Gemfibrozil, Fenofibrate, Bezafibrate (TOPNOTCH)

312

Fibrates have higher risk of gallstone formation if given together with ____

resins (TOPNOTCH)

313

Nonselective, irreversible COX 1&2 inhibitor. Reduces platelet production of thromboxane A2, temporarily inhibit Prostacyclin synthesis

Aspirin (TOPNOTCH)

314

Uncoupler of oxidative phosphorylation, associated with Reye syndrome in children

Aspirin (TOPNOTCH)

315

Reversbily inhibits the binding of fibrin and other ligands to the platelet GPIIb-IIIa receptor

GPIIb-IIIa inhibitor: Abciximab, Eptifibatide,Tirofiban (TOPNOTCH)

316

For prevention or arterial thrombosis (MI, TIA, CVD), Inflammatory disorders (rheumatic fever, juvenile rheumatoid arthritis, kawasaki disease)

Aspirin (TOPNOTCH)

317

Inhibits phosphodiesterase III and increases cAMP in platelets and blood vessels, Inhibits platelet aggregation and causes vasolidation

PDE III inhibitor: Dipyridamole, Cilostazol (TOPNOTCH)

318

additional MOA: inhibit uptake of adenosine by endothelial cells and RBC, thus increasing adenosine levels leading to inhibition of platelet aggregation

PDE III inhibitor: Dipyridamole, Cilostazol (TOPNOTCH)

319

Irreversibly inhibits binding of ADP to platelet receptors,thus reducing platelet aggregation

ADP inhibitor: Clopidogrel,Ticlopidine, Prasugel (TOPNOTCH)

320

Activates antithrombin III which Inactivates thrombin or factor IIa, factor IXa & factor Xa by forming stable complexes with them

Heparin (TOPNOTCH)

321

SE: Bleeding, transient Heparin-induced thrombocytopenia, Osteoporosis with chronic use

Heparin (TOPNOTCH)

322

DOC for anticoagulation during pregnancy ; administered IV or SC ; Monitor with aPTT,

Heparin (TOPNOTCH)

323

Antidote for heparin toxicity

Protamine Sulfate (TOPNOTCH)

324

Binds and potentiates effect of antithrombin III on factor Xa (more selective for Xa)

LMWH (TOPNOTCH)

325

LMWH

Enoxaparin, Dalteparin, Tinzaparin, Danaparoid, Fondaparinux (TOPNOTCH)

326

Does not require aPTT monitoring, Protamine sulfate is only partially effective in reversing effects

LMWH: Enoxaparin, Dalteparin, Tinzaparin, Danaparoid, Fondaparinux (TOPNOTCH)

327

Binds to thrombin's ative site and inhibits its enzymatic action

Direct Thrombin Inhibitors: Lepirudin, Desirudin, Bivalirudin, Argatroban, Dabigatran (TOPNOTCH)

328

bind to free and bound factor Xa

Direct Oral Factor Xa inhibitor: Rivaroxaban, Apixaban (TOPNOTCH)

329

Inhibits vitamin K epoxide reductase (responsible for y-carboxylation of the vitamin K- dependent clotting (factors II, VII, IX, X, Protein C & Protein S)

Warfarin (TOPNOTCH)

330

For chronic anticoagulation (DVT, atrial fibrillation, valve replacement)

Warfarin (TOPNOTCH)

331

SE: Bleeding, Teratogen (bone defects, hemorrhage), warfarin-induced skin necrosis (transient hypercoagulability)

Warfarin (TOPNOTCH)

332

Monitor effects with PT-INR

Warfarin (TOPNOTCH)

333

Antidote forwarfarin toxicity

Vitamin K or FFP (TOPNOTCH)

334

Chemical antagonist of heparin. Reverses excessive anticlotting activity of unfractionated heparin

Protamine Sulfate (TOPNOTCH)

335

Tissue plasminogen activator analog. Converts plasminogen to plasmin, which degrades the fibrin and fibrinogen, causing thrombolysis

Alteplase, Anistreplase, Reteplase, Streptokinase, Tenecteplase, Urokinase (TOPNOTCH)

336

Tx should be done within 6 hrs, better if within 3hrs ; Antidote is AMINOCAPROIC ACID

Alteplase, Anistreplase, Reteplase, Streptokinase, Tenecteplase, Urokinase (TOPNOTCH)

337

Competitively inhibits plasminogen activation thus inhibiting fibrinolysis

Tranexamic acid (TOPNOTCH)

338

For Vitamin K deficiency, Antidote to warfarin, prevention of hemorrhagic diatheses in newborns

Vitamin K1, K2 (Phytonadione, Menaquinone) (TOPNOTCH)

339

Vasopressin V2 receptor agonist, Increases factor VIII activity of patients with mild hemophilia A or VWD

Desmopressin (TOPNOTCH)

340

low doses undergo first order kinetics while high doses undergo zero order reaction ; Long term use reduces the risk of colon cancer

Aspirin (TOPNOTCH)

341

COX-2 > COX-1 inhibition

Meloxicam & Piroxicam (TOPNOTCH)

342

NSAIDs that can be used to close PDA

Ibuprofen and Indomethacin (TOPNOTCH)

343

has significant analgesic effect but not anti-inflammatory effect

Ketorolac (TOPNOTCH)

344

SE: Gastrointestinal toxicity, pancreatitis, Nephrotoxicity, Serious hematologic reactions, BM suppression

Indomethacin (TOPNOTCH)

345

Selective COX-2 inhibitor

Celecoxib, Etoricoxib, Parecoxib (TOPNOTCH)

346

Rofecoxib and Valdecoxib withdrawn due to

increased incidence of thrombosis (TOPNOTCH)

347

Selectively inhibits COX-3 in the CNS, Weak COX-1 and COX-2 inhibitor in the periphery, Inhibits prostaglandin synthesis

Paracetamol (Acetaminophen) (TOPNOTCH)

348

Inhibits AICAR transformylase and thymidylate snythetase, with secondary effects on polymorphonuclear chemotaxis

Methotrexate (TOPNOTCH)

349

DMARD of choice for Rheumatoid arthritis

Methotrexate (TOPNOTCH)

350

Rescue agent for Methotrexate toxicity

Leucovorin (Folinic acid) (TOPNOTCH)

351

Binds to TNF-a inhibitor

Infliximab, Adalimumab, Etanercept (TOPNOTCH)

352

SE: Bacterial infections (URTIs), reactivation of latent tuberculosis, lymphoma, Demyelination, Reactivation of Hepatitis B, Auto antibody formation (ANA, anti dsDNA), infusion reactions, hepatoxicity, hematotoxicity, cardiotoxicity

TNF-a inhibitor: Infliximab, Adalimumab, Etanercept (TOPNOTCH)

353

Antidote for paracetamol toxicity

N-acetyl cysteine (TOPNOTCH)

354

Forms 6-thioguanine, suppressing inosinic acid synthesis, B-cell and T-cell function, Immunoglobulin production and interleukin-2 secretion

Azathioprine (TOPNOTCH)

355

Cannot give _______ with azathioprine (the drug reduces xanthine oxide catabolism of purine analogs, increasing 6-thioguanine nucleotides, leading to serve leukopenia)

Allopurinol (TOPNOTCH)

356

Suppression of T-lymphocyte leading to decreased leukocyte chemotaxis, stabilization of lysosomal enzymes, inhibition of DNA and RNA synthesis, trapping of free radicals

Chloroquine, Hydroxychloroquine (TOPNOTCH)

357

T or F: Chloroquine, Hydroxychloroquine are safe for pregnant patients

TRUE (TOPNOTCH)

358

Forms phospharamide mustard, which cross links DNA to prevent cell replication, Supresses T-cell and B-cell function

Cyclophosphamide (TOPNOTCH)

359

SE: hemorrhagic cystitis

Cyclophosphamide (TOPNOTCH)

360

Rescue agent for Cyclophosphamide toxicity

MESNA (TOPNOTCH)

361

Inhibits interleukin-1 and iterleukin-2 receptor production and secondarily inhibts macrophage-T-cell interaction and T-cell responsiveness

Cyclosporine (TOPNOTCH)

362

anti-IBD drug, active metabolite inhibits the release of inflammatory bowel cytokines

Sulfasalazine (TOPNOTCH)

363

Inhibits microtubule assembly and LTB4 production leading to decreased macrophage migration and phagocytosis

Microtubule assembly inhibtor: Colchicine (TOPNOTCH)

364

adverse effect which signals toxicity from colchicine

diarrhea (TOPNOTCH)

365

are weak acids that compete with uric acid for reabsorption in the PCT leading to increased uric acid excretion

Uricosuric agent: Probenecid, Sulfinpyrazone (TOPNOTCH)

366

may be given together with antimicrobial agents (particularly Pens) to prolong therapeutic effect by inhibiting renal tubular secretion of antibiotics

Probenecid (TOPNOTCH)

367

Active metabolite (alloxanthine) irreversibly inhibits xanthine oxidase and lowers production of uric acid

Xanthine oxidase inhibitor: Allopurinol, Febuxostat (TOPNOTCH)

368

1st line treatment of chronic gout, tumor lysis syndrome

Xanthine oxidase inhibitor: Allopurinol, Febuxostat (TOPNOTCH)

369

T or F: Allopurinol is more effective than Febuxostat

FALSE (TOPNOTCH)

370

Recombinant Growth hormone

Somatropin (TOPNOTCH)

371

Increases release of IGF-1 in the liver and carilage, stimulates skeletal muscle growth, amino acid transport, protein synthesis and cell proliferation

Somatropin (TOPNOTCH)

372

Recombinant IGF-1

Mecasermin (TOPNOTCH)

373

Somatostatin analog

Octreotide, Lanreotide (TOPNOTCH)

374

suppresses the release of growth hormones, glucagon, insulin, gastrin, IGF-1, serotonin and gastrointestinal peptides

Octreotide, Lanreotide (TOPNOTCH)

375

For Acromegaly, pituitary adenoma, carcinoid, gastrinoma, glucagonoma, variceal bleeding

Octreotide, Lanreotide (TOPNOTCH)

376

GH receptor antagonist ; For acromegaly

Pegvisomant (TOPNOTCH)

377

Gonadotropin analog (FSH analog) ; For Controlled ovarian hyperstimulation, infertility due to hypogonadism in men

Follitropin alfa, Follitropin beta, Urofollitropin (TOPNOTCH)

378

Gonadotropin analog (LH analog)

For Controlled ovarian hyperstimulation (ovulation induction), hypogonadotripic hypogonadism (TOPNOTCH)

379

SE: Headache, depression, edema, ovarian hyperstimulation syndrome, multiple pregnancies in women, gynecomastia in men

FHS and LH analogs (TOPNOTCH)

380

GnRH analog

Leuprolide, Gonadorelin, Goserelin, Histrelin, Nafarelin, Triptorelin (TOPNOTCH)

381

For Controlled ovarian hyperstimulation, endometriosis, myoma uteri, precocious puberty, postate CA

Leuprolide, Gonadorelin, Goserelin, Histrelin, Nafarelin, Triptorelin (TOPNOTCH)

382

there is exacerbation of symptoms in males with prostate CA and children with precocious puberty during the first few weeks of therapy

GnRH analog (TOPNOTCH)

383

For GnRH analogs: increased LH and FSH secretion with ________ administration , reduced LH and FSH secretion with ________ administration

intermittent ; prolonged continuous (TOPNOTCH)

384

GnRH antagonist

Ganirelix, Cetrorelix, Degarelix (TOPNOTCH)

385

For Controlled ovarian hyperstimulation (prevents premature LH surge), advanced prostate CA

Ganirelix, Cetrorelix, Degarelix (TOPNOTCH)

386

Does NOT cause tumor flare-up whe used for treatment of advanced prostate cancer

Ganirelix, Cetrorelix, Degarelix (TOPNOTCH)

387

_____ is used for prostate CA while _____ prevent LH surge in controlled ovulation

Degarelix ; Ganirelix (TOPNOTCH)

388

Dopamine agonist, partial agonist at dopamine D2 receptors in brain ; For Hyperprolactinemia, Pituitary adenoma, acromegaly, Parkinson's disease

Bromocriptine, Carbegoline (TOPNOTCH)

389

Activates oxytocin receptors stimulates uterine contraction and labor, stimulates mammary glands, lactation and milk let-down

Oxytocin (TOPNOTCH)

390

For Labor induction, labor augmentation, control of uterine hemorrhage post-delivery

Oxytocin (TOPNOTCH)

391

oxytocin antagonist used in preterm labor

ATOSIBAN (TOPNOTCH)

392

ADH agonist, Vasopressin V2 receptor agonist

Desmopressin (TOPNOTCH)

393

For Central DI, Hemphilia A, von Willebrand's disease, Variceal bleeding, primary nocturnal seizures

Desmopressin (TOPNOTCH)

394

SE: Fetal distress, placental abruption, uterine rupture, fluid retention, hyponatremia, heart failure, seizures, hypotension

Oxytocin (TOPNOTCH)

395

ADH antagonist, Antagonist at V1a and V2 receptors

Conivaptan, Tolvaptan (TOPNOTCH)

396

_____ may occur with rapid correction of hyponatremia

Central pontine myelinolysis (TOPNOTCH)

397

Which is more selective for V2 receptors, Conivaptan or Tolvaptan?

tolvaptan (TOPNOTCH)

398

Thryoid hormone ; For Hypothyroidism, myxedema coma

Levothyroxine (T4), Liothyronine (T3) (TOPNOTCH)

399

T or F: Liothyronine has a faster onset but shorter half-life

TRUE (TOPNOTCH)

400

Inhibits thyroid peroxidase reactions, blocks iodine organification, inhibits peripheral conversion of T4 into T3

Propylthiouracil (PTU) (TOPNOTCH)

401

Drug of choice for pregnant hyperthyroid patients

Propylthiouracil (PTU) (TOPNOTCH)

402

Inhibits thyroid peroxidase reactions, blocks iodine organification

Methimazole, Carbimazole (TOPNOTCH)

403

Inhibit iodine organification and hormone release leading to reduced size and vascularity of thyroid gland

Lugol Solution (Iodine in Potssium Iodide), Potassium Iodide (TOPNOTCH)

404

onset is more rapid (2-7 days) but effect is transient ; Should not be used alone (escape in 2-8 weeks); prevents radiation induced thryoid damage; prenatal exposure causes fetal goiter

Lugol Solution (Iodine in Potssium Iodide), Potassium Iodide (TOPNOTCH)

405

Beta blocker control HR and other cardiac abnormalities of severe thyrotoxicosis, slows pacemaker activity; inhibits peripheral conversion of T4 into T3

Propranolol, Esmolol, Metoprolol, Atenolol (TOPNOTCH)

406

_____ may be used to treat thyrotoxicosis-related arrhythmias

Esmolol (TOPNOTCH)

407

Iodide, emits beta rays causing destruction of thyroid parenchyma

Radioactive Iodine (TOPNOTCH)

408

For hyperthyroidism, permanent cure of thyrotoxicosis without surgery and no effect on other tissues

Radioactive Iodine (TOPNOTCH)

409

Preferred treatment for most patients due to ease of administration, effectiveness, low expense and absence of pain; contraindicated in pregnant women or nursing mothers

Radioactive Iodine (TOPNOTCH)

410

Low Potency Glucocorticoid (GC)

Desonide (TOPNOTCH)

411

Medium Potency GC

Fluticasone, Mometasone (TOPNOTCH)

412

High Potency GC

Desoximetasone, Clobetasol (TOPNOTCH)

413

Effects: stimulate gluconeogenesis, increased fat deposition, protein catabolism, inhibit cell-mediated immunologic functions, lymphotoxic, increased neutrophils, decreased lymphocytes, eosinpphils, basophils and monocytes, inhibit leukocyte migration, inhibit PLA2

Glucocorticoids (TOPNOTCH)

414

_____ is the active metabolite of prednisone

prednisolone (TOPNOTCH)

415

SE: Adrenal suppression, growth inhibition, muscle wasting, osteoporosis, salt retention, glucose intolerance, behavioral changes (psychosis)

Glucocorticoids (TOPNOTCH)

416

For supressession of inflammation and immune response, hematopoeitic cancers, transplant rejection, collagen and rheumatic disease, lung maturation in preterm labor

Glucocorticoids (TOPNOTCH)

417

strong agonist of mineralocorticoid receptors and moderate activation of glucorticoid receptors

Mineralocorticoid (TOPNOTCH)

418

Increases Na reabsorption, K and H excretion ; For Chronic adrenal insufficiency (Addison's disease), Congenital adrenal hyperplasia, adrenal replacement therapy post-adrenalectomy

Mineralocorticoid (TOPNOTCH)

419

Mineralocorticoid

Fludrocortisone, Deoxycorticosterone (TOPNOTCH)

420

Additive hypokalemia with loop diurectics and thiazides

Fludrocortisone, Deoxycorticosterone (TOPNOTCH)

421

Glucorticoid synthesis inhibitor, inhibits desmolase activity, blocking conversion of cholesterol to pregnenolone

Aminoglutethimide (TOPNOTCH)

422

Glucorticoid synthesis inhibitor, inhibits cholesterol side chain cleavage, cytochrome P450 enzymes and other enzymes necessary for synthesis of all steroids

Ketoconazole (TOPNOTCH)

423

Ketoconazole is CYP450 inhibitor or inducer?

Inhibitor (TOPNOTCH)

424

Glucorticoid synthesis inhibitor, selective inhibitor of steroid-11 hydroxylation

Metyrapone (TOPNOTCH)

425

DOC for pregnant patients with Cushing's syndrome

Metyrapone (TOPNOTCH)

426

competitive inhibitor at the GC receptor as well as progesterone receptor ; For Cushing's syndrome

Mifepristone (RU486) (TOPNOTCH)

427

also used as an approved abortifacient for medical abortion (usually together with misoprostol)

Mifepristone (RU486) (TOPNOTCH)

428

Activates etrogen receptors, leads to changes in rates of trasncription of estrogen-regulated genes

Estrogens: Ethinyl Estradiol, Mestranol, Estradiol cypionate, Premarin (TOPNOTCH)

429

Synthetic estrogen (nonsteroid); activates estrogen receptors; leads to changes in rates of transcription of estrogen-regulated genes ; For Atrophic vaginitis, hormone replacement therapy, prevention of adverse pregnancy outcomes, metastatic prostate CA

Diethylstilbestrol (TOPNOTCH)

430

associated with Infertility, ectopic pregnancy, clear cell vaginal adenocarcinoma in daughters of women who used this drug

Diethylstilbestrol (TOPNOTCH)

431

activates progesterone receptors, change rates of transcription of progesterone-regulated genes ; For Hormone replacement therapy, contraception, assisted reproduction, anovulation induction

Progestins: Norgestrel, Medroxyprogesterone, Norethindrone, Norgestimate, Desogestrel,Megestrol (TOPNOTCH)

432

IM depot preparation

Medroxyprogesterone Acetate (TOPNOTCH)

433

Must be taken within 72 hours of unprotected sexual intercourse

Levonorgestrel (TOPNOTCH)

434

Estrogen antagonist actions in breast tissue and CNS, Estrogen agonist effects in uterus, liver and bone

Tamoxifen, Torimefene (TOPNOTCH)

435

Estrogen antagonist actions in breast tissue, uterus, and CNS, Estrogen agonist effects in liver and bone

Raloxifene (TOPNOTCH)

436

Partial agonist in pituitary, reduces negative feedback by estradiol, increases FSH and LH output, For Induction of ovulation

Clomiphene (TOPNOTCH)

437

Reduces estrogen synthesisby inhibiting aromatase ; For breast CA, precocious puberty

Anastrozole, Letrozole, Exemestane (TOPNOTCH)

438

Ovarian inhibitor, weak cytochrome P450 inhibitor and partial agonist of progestin and androgen receptors ; For Endometriosis, Fibrocystic disease, Hemophilia, Angioneurotic edema

Danazol (TOPNOTCH)

439

Activates androgen receptors, promotes development of male characteristics, increases body muscle bulk and RBC production

Androgens: Testosterone, Fluoxymesterone, Methyltestosterone (TOPNOTCH)

440

Effects: induces secretory changes in the endometrium, stabilize the endometrium, affect carbohydrate metabolism and stimulate deposition of fat, high doses suppress FSH and LH secretion

progesterone (TOPNOTCH)

441

Effects: secondary sexual characteristics, fertility and libido, male pattern baldness, increases muscle mass, increased RBC production, decreased urea nitrogen excretion

Androgens: Testosterone, Fluoxymesterone, Methyltestosterone (TOPNOTCH)

442

anabolic steroids

Oxandrolone, Stanozolol, Nandrolone (TOPNOTCH)

443

Competitive antagonist at androgen receptor ; For Prostate CA, surgical castration

Flutamide, Bicalutamide, Nilutamide (TOPNOTCH)

444

Antagonist at androgen receptor. Marked progestational effect that suppresses the feedback enhancement of LH and FSH

Cyproterone (TOPNOTCH)

445

Androgen synthesis inhibitor, inhibits 5a reducase enzyme that converts testosterone to dihydrotestosterone ; For BPH, Male pattern baldness. Hirsutism

Finasteride, Dutasteride (TOPNOTCH)

446

Activates a Tyrosine Kinase typer of receptorsleading to a reducting of circulating glucose: promotes glucose transport and oxidation; glycogen, lipid, protein synthesis and regulation of gene expression

Insulin (TOPNOTCH)

447

Rapid Acting Insulin

Lispro, Aspart, Glulisine (TOPNOTCH)

448

Short Acting Insulin

Regular Insulin (TOPNOTCH)

449

Intermediate Acting Insulin

NPH, Lente (TOPNOTCH)

450

Long Acting Insulin

Detemir, Glargine, Ultralente, Lantus (TOPNOTCH)

451

peakless insulins

Long Acting Insulin (TOPNOTCH)

452

acts as an insulin secretagogue, increases insulin secretion from pancreatic beta cells by closing ATP sensitive K+ channels leading to depolarization of the B cell

Sulfonylureas (TOPNOTCH)

453

2nd generation sulfonylurea

Glipizide, Glibenclamide, Glimepiride, Gliclazide, Glyburide (TOPNOTCH)

454

1st generation sulfonylurea

Tolazamide, Tolbutamide, Chlorpropamide (TOPNOTCH)

455

T or F: 1st gen SUs have less hypoglycemia than 2nd gen

FALSE (TOPNOTCH)

456

Insulin Secretagogue, similar to sulfonylureas with some overlap in binding sites, reduces circulating glucose, increases glycogen, fat and protein formation and gene regulation

Meglitinides (TOPNOTCH)

457

Meglitinides

Repaglinide, Nateglinide (TOPNOTCH)

458

Least hypoglycemia among OHAs

Meglitinides (TOPNOTCH)

459

Reduced hepatic and renal gluconeogenesis with decreased endogenous glucose production, activates AMP-stimulated protein kinase leading to inhibition of gluconeogenesis

Biguanides (TOPNOTCH)

460

Biguanides

Metformin (TOPNOTCH)

461

DOC for obese diabetics

Metformin (TOPNOTCH)

462

Inhibits intestinal alpha-glucosidases , reduces conversion of starch and disacchardies to monosaccharidea, reduces post prandial hyperglycemia

Alpha Glucosidase Inhibitors (TOPNOTCH)

463

Alpha Glucosidase Inhibitors

Acarbose, Miglitol (TOPNOTCH)

464

Regulates gene expression by binding to PPAR-gamma and PPAR-alpha which increases tissue sensitivity, increases glucose uptake in muscle and adipose tissue, inhibits hepatic gluconeogenesis, effects on lipid metabolism and distribution of body fat, control of fasting and postprandial glucose, decreased risk of DM in high-risk patients

Thiazolidinediones (TOPNOTCH)

465

Thiazolidinediones

Pioglitazone, Rosiglitazone (TOPNOTCH)

466

binds to PPAR-gamma and PPAR-alpha

Pioglitazone (TOPNOTCH)

467

binds to PPAR-gamma ONLY

Rosiglitazone (TOPNOTCH)

468

SE: Fluid retention, weight gain, congestive heart failure, fractures esp in women, cardiovascular events, hepatotoxicity, macular edema, dyslipidemia, increased risk of MI

Thiazolidinediones (TOPNOTCH)

469

Analog of GLP-1, Binds to GLP-1 receptors which leads to reducetion of post-meal glucose excursions, increases glucose-mediated insulin release, lowers glucagon levels, slows gastric emptying time, produces satiety

Exenatide (TOPNOTCH)

470

Dipeptidyl Peptidase-4 Inhibitors, blocks degradation of GLP-1, raises circulating GLP-1 levels, reduces post-meal glucose excursions, increases glucose mediated insulin release, lowers glucagon levels, slows gastric emptying time, decreases appetite

Sitagliptin, Linagliptin (TOPNOTCH)

471

Analog of amylin, Binds to amylin receptors, reduce post-meal glucose excursions, lowers glucagon levels, slows gastric emptying, decreases appetite

Pramlintide (TOPNOTCH)

472

Bile acid binder, lowers glucose through unknown mechanisms

Colesevelam hydrochloride (TOPNOTCH)

473

INACTIVE Vitamin D

Cholecalciferol, Ergocalciferol (TOPNOTCH)

474

ACTIVE Vitamin D

Calcitriol, Doxercalciferol, Paricalcitol, Calcipotriene (TOPNOTCH)

475

Suppress the activity of osteoclasts in part via inhibition of farnesyl pyrophosphate synthesis, inhibit resorption and formation of bone by acting on the basic hydroxyapatite crystal structure

Bisphosphonates (TOPNOTCH)

476

Bisphosphonates

Alendronate, Risedronate, Ibandronate, Pamidronate, Zoledronate, Etidronate, Tiludronate, Zoledronic acid (TOPNOTCH)

477

Recombinant PTH, Acts via cognate G protein coupled receptors, stimulates bone formation when given in low intermittent doses

Teriparatide (TOPNOTCH)

478

Acts via cognate G protein coupled receptors; suppresses bone resorption ; For Paget's disease of the bone, hypercalcemia, osteoporosis, tumor marker for thyroid CA

Calcitonin (TOPNOTCH)

479

Interacts selectively with estrogen receptors, inhibits PTH-stimulated bone resorption without stimulating breast or endometrial hyperplasia, delay bone loss in post-menopausal women

Raloxifene (TOPNOTCH)

480

Monoclonal antibody, binds to RANKL and prevents it from stimulating osteoclast differentiation and function, blocks bone resorption

Denosumab (TOPNOTCH)

481

Activates the calcium sensing receptors in the parathyroid gland, inhibits PTH secretion

Calcium Receptor Antagonist: Cinacalcet (TOPNOTCH)

482

Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial cell walls

Penicillin, Cephalosporins (TOPNOTCH)

483

DOC for syphillis, for streptococcal, meningococcal, G+ bacilli, spirochete infection

Natural Penicillins: Penicillin G, Penicillin V (narrow spectrum penicillin) (TOPNOTCH)

484

For staphylococcal infections

Anti-Staphylococcal Penicillins: Methicillin, nafcillin, oxacillin, cloxacillin (very narrow spectrum) (TOPNOTCH)

485

all penicillins are excreted unchanged in the urine EXCEPT for _____which is excreted in the bile

Nafcillin (TOPNOTCH)

486

Pens For enterococci, Listeria, E. coli, Proteus, H. influenza, Moraxella

Extended Spectrum Penicillin: Ampicillin, Amoxicillin (TOPNOTCH)

487

Pens For Pseudomonas, Enterobacter, Klebsiella

Antipseudomonal Penicillin: Piperacillin, ticarcillin, carbenicillin (TOPNOTCH)

488

all Cephs have renal excretion EXCEPT ______

Cefoperazone and Ceftriaxone (TOPNOTCH)

489

Cephs for For surgical prophylaxis, bone infections, infections due to staph and strep, E. coli, Klebsiella, G+ cocci

First Generation Cephs (TOPNOTCH)

490

Increases nephrotoxicity of aminoglycosides

Cephs (TOPNOTCH)

491

For surgical prophylaxis, bone infections, infections due to staph strep and E. coli, Enterobacter, Neisseria, infections against anaerobes (Bacteroides), sinus ear and respiratory infections by Klebsiella andHemophilus

Second Generation Cephs (TOPNOTCH)

492

Second Generation Cephs

Cefamandole, cefaclor, cefonicid, cefuroxime, cefprozil, loracarbef, ceforanide, cefoxitin, cefmetazole, cefotetan (TOPNOTCH)

493

First Generation Cephs

Cefazolin, cefadroxil, cephalothin, cephapirin, cephradine, cephalexin (TOPNOTCH)

494

Cephs with slight less activity against G+ but extended G- activity

Second Generation Cephs (TOPNOTCH)

495

decreased gram + coverage, increased gram - activity (pseudomonas, bacteroides), against Providencia, Serratia, Neiserria, Haemophilus ; DOC for gonorrhea

Third Generation Cephs (TOPNOTCH)

496

DOC for gonorrhea

Ceftriaxone and Cefixime (TOPNOTCH)

497

Third Generation Cephs

Cefoperazone, cefotaxime, ceftizoxime, ceftriaxone, cefixime, cefpodoxime proxetil, cefdinir, ceftibuten (TOPNOTCH)

498

all can Third gen Cephs can penetrate the BBB EXCEPT _____

Cefoperazone and Cefixime (TOPNOTCH)

499

More resistant to beta-lactamase produced by Enterobacter, Haemophilus, Neisseria and Pneumococcal

Fourth Generation Cephs (TOPNOTCH)

500

Fourth Generation Cephs

Cefipime (TOPNOTCH)

501

Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial cell walls, wide coverage against gram + gram - bacteria and anaerobes ; For infections resistant to other antibiotics EXCEPT MRSA, DOC for Enterobacter, Citrobacter and Serratia

Carbapenems (TOPNOTCH)

502

Carbapenems

Imipenem-cilastatin , ertapenem, meropenem (TOPNOTCH)

503

Imipenem given with Cilastatin which acts as ______

Dehydropeptidase enzyme inhibitor (TOPNOTCH)

504

Monobactam

Aztreonam (TOPNOTCH)

505

Resistant to beta-lactamase, no activity against gram + bacteria or anaerobes

Aztreonam (TOPNOTCH)

506

No cross-allergenicity with Pens

Aztreonam (TOPNOTCH)

507

Inhibits inactivation of penicillins by bacterial beta-lactamase (penicillinase)

Beta-Lactamase Inhibitors (TOPNOTCH)

508

Beta-Lactamase Inhibitors

Clavulanic acid , sulbactam, tazobactam (TOPNOTCH)

509

Inhibits cell wall synthesis by binding to the D-Ala-D-Ala terminus of nascent peptidoglycan --> inhibit transglycosylation --> prevent elongation and cross-linking of peptidoglycan chain

Glycopeptides: Vancomycin, teicoplanin, telavancin (TOPNOTCH)

510

For MRSA, PRSP, as alternative for pseudomembranous colitis

Vancomycin (TOPNOTCH)

511

SE: red man syndrome, nephrotoxicity, ototoxicity, chills, fever, phlebitis

Vancomycin (TOPNOTCH)

512

Interferes with a late stage in cell wall synthesis in gram + organisms ; For gram + bacteria

Bacitracin (TOPNOTCH)

513

Reserved for topical use only due to marked nephrotoxicity

Bacitracin (TOPNOTCH)

514

Blocks incorporation of D-Ala into the pentapeptide side chain of the peptidoglycan ; For drug-resistant TB

Cycloserine (TOPNOTCH)

515

inhibits cytosolic enolpyruvate transferase --> prevents formation of N-acetylmuramic acid

Fosfomycin (TOPNOTCH)

516

same spectrum of activity as Vancomycin ; For VRE, VRSA, for G+ activity, against endocarditis and sepsis

Daptomycin (TOPNOTCH)

517

Inhibits transpeptidation (catalyzed by peptidyl transferase) by blocking the binding of aminoacyl moiety of the charged tRNA to the acceptor site o mRNA at 50S subunit, basteriostatic

Chloramphenicol (TOPNOTCH)

518

For meningitis (Strep pneumonia, H influenza, Neisseria meningitides), back up for Salmonella, Rickettsia, Bacteroides, Wide spectrum antibiotic

Chloramphenicol (TOPNOTCH)

519

Binds 30s ribosomal subunit thus preveting the binding of tRNA to mRNA, bacteriostatic ; Broad/Wide Spectrum (G+ and G-), anaerobes and atypicals

Tetracyclines (TOPNOTCH)

520

_____ has the broadest spectrum of all tetracyclines and has the longest t1/2 (30-36hrs)

Tigecycline (TOPNOTCH)

521

SE: GI disturbances (enetrocolitis, nausea, diarrhea, vomiting), teratogen (tooth enamel dysplasia/discoloration), hepatotoxicity, nephrotoxicity, photosensitivity n(esp. demeclocycline), vestibulotoxicity, candidiasis, bacterial superinfection with S. aureus and C. difficile, Fanconi syndrome

Tetracyclines (TOPNOTCH)

522

Tetracyclines

Tetracycline, doxycycline, minocycline, tigecycline, demeclocycline (TOPNOTCH)

523

Binds 30s ribosomal subunit, inhibit transpeptidation, bacteriostatic ; For community-acquired pneumonia, pertussis, diphtheria, chlamydial infections

Macrolides (TOPNOTCH)

524

Macrolides

Erythromycin, azithromycin, clarithromycin, telithromycin (TOPNOTCH)

525

______ is used as an alternative Ceftriaxone in Gonorrhea and to Pen G in syphilis

Azithromycin (TOPNOTCH)

526

______ is used for macrolide-resistance

telithromycin (TOPNOTCH)

527

a narrow spectrum macrolide, for G+ and anaerobe, low oral bioavailability

Fidaxomicin (TOPNOTCH)

528

as effective as Vancomycin as treatment for C. difficile possibly with lower relapse rate

Fidaxomicin (TOPNOTCH)

529

GI disturbance, skin rash, neutropenia, hepatic dysfunction, possible superinfection (Pseudomembranous colitis - C. difficile overgrowth)

Lincosamides: Clindamycin, lincomycin (TOPNOTCH)

530

Binds 30s ribosomal subunit, inhibit transpeptidation, bacteriostatic ; For anaerobic infections (Bacteroides), alternative against gram + cocci (MRSA), endocarditis prophylaxis esp in those allergic to Pens, PCP pneumonia, toxoplasmosis (+ Pyrimethamine), skin and soft tissue infection

Lincosamides: Clindamycin, lincomycin (TOPNOTCH)

531

Binds 50s ribosomal subunit, constricting the channel where polypeptides are extruded thus tRNA synthetase is also inhibited --> decreased free tRNA

Streptogramin: Quinupristin-Dalfopristin (TOPNOTCH)

532

Binds 23S rRNA of 50s ribosomal subunit, inhibit initiation by blockin formation of the tRNA-ribosome-mRNA ternary complex, bacteriostatic ; Reserved for infections caused by drug-resistant gram + cocci (MRSA, VRE, PRSP), Listeria, Corynebacteria

Oxazolidinone: Linezolid (TOPNOTCH)

533

For serious infections caused by aerobic gram _ bacteria (E.coli, Enterobacter, Klebsiella, Proteus, Providencia, Pseudomonas, Serratia, Haemophilus, Moraxella, Shigella), endocarditis, ocular infections

Aminoglycosides (TOPNOTCH)

534

Least resistance and narrowest therapeutic window ; used for streptomycin-resistant TB

Amikacin (TOPNOTCH)

535

For TB, tularaemia, bubonic plague, brucellosis

Streptomycin (TOPNOTCH)

536

SE: nephrotoxicity (reversible), ototoxicity (irreversible), neuromuscular blockade

Aminoglycosides in general (TOPNOTCH)

537

SE: hypersensitivity, nephrotoxicity (reversible), ototoxicity (irreversible), neuromuscular blockade, teratogen (congenital deafness), injection site reactions

Streptomycin (TOPNOTCH)

538

_____ is most ototoxic of all Aminoglycosides (AG) while _____ has the most skin reactions

kanamycin ; Neomycin (TOPNOTCH)

539

For drug-resistant gonorrhoea, gonorrhoea in penicillin allergic patients

Spectinomycin (TOPNOTCH)

540

For Treatment of serious infections caused by organisms resistant to other aminoglycosides

Netilmicin (TOPNOTCH)

541

Inhibits dihydropteroate synthase, bacteriostatic

Sulfonamides (TOPNOTCH)

542

low solubility in acidic urine causing formation of stones

Sulfonamides (TOPNOTCH)

543

Sequential blockade of dihydropteroate synthase and dihydrofolate reductase , bactericidal

Co-trimoxazole (Sulfamethoxazole + Trimethoprim) (TOPNOTCH)

544

SE: GI upset, acute hemolysis in G6PD deficiency, nephrotoxicity, hypersensitivity, hematotoxicity, kernicterus ; antifolate effects (megaloblastic anemia, leukopenia, granulocytopenia)

Co-trimoxazole (Sulfamethoxazole + Trimethoprim) (TOPNOTCH)

545

Inhibits DNA replication by binding to DNA gyrase and topoisomerase IV (G+) and Topoisomerase II (G-)

Fluoroquinolones (TOPNOTCH)

546

For infections of the urogenital and GI tract by G- (gonococci, E. coli, Klebsiela, Campylobacter, Enterobacter, Pseudomonas, Salmonella, Shigella), respiratory tract, skin and soft tissue infection

Fluoroquinolones (TOPNOTCH)

547

CI in pregnancy and in children (damage growing cartilage --> arthropathy)

Fluoroquinolones (TOPNOTCH)

548

GI distress, skin rashes, HA, dizziness, insomnia, increased LFT, phototoxicity, CNS effects (dizziness, headache), tendinitis and tendon rupture, opportunistic infection by Candida and Streptococci

Fluoroquinolones (TOPNOTCH)

549

Second Generation Fluoroquinolones

Ciprofloxacin, ofloxacin (TOPNOTCH)

550

First Generation Fluoroquinolones

Norfloxacin, Nalidixic acid (TOPNOTCH)

551

Third Generation Fluoroquinolones

Levofloxacin, Gemifloxacin, Moxifloxacin (TOPNOTCH)

552

Respiratory Quinolones

Levofloxacin, Gemifloxacin, Moxifloxacin (TOPNOTCH)

553

newest members of the Fluoroquinolone family and are condisered to have the broadest spectrum of activity with increased activity aginst anaerobes ang atypical agents

Moxifloxacin and Gemifloxacin (TOPNOTCH)

554

Fourth Generation Fluoroquinolones

Trovafloxacin, Gatifloxacin (TOPNOTCH)

555

FQ elimination is via kidneys by tubular secretion (may compete with probenecid for excretion) EXCEPT

Moxifloxacin (TOPNOTCH)

556

additional SE of which FQs: diabetes, hepatotoxicity

diabetes (gatifloxacin), hepatotoxicity (trovafloxacin) (TOPNOTCH)

557

Reactive reduction by ferredoxin forming free radicals that disrupt electron transport chain, bactericidal

Metronidazole, tinidazole (TOPNOTCH)

558

For anaerobic or mixed intra-abdominal infections, vaginitis (trichomonas, gardnerella), pseudomembranous colitis, brain abscess, protozoal infections

Metronidazole, tinidazole (TOPNOTCH)

559

DOC for amoebiasis, giardiasis and Pseudomembranous colitis

Metronidazole (TOPNOTCH)

560

single OD dose can prevent recurrent UTI

Nitrofurantoin (TOPNOTCH)

561

SE: GI irritation, metallic taste, headache, dark urine, leukopenia, dizziness, ataxia, neuropathy, seizures and disulfiram reaction

Metronidazole (TOPNOTCH)

562

acidification of urine enhances activity ; adjust dose in renal patients

Nitrofurantoin (TOPNOTCH)

563

Forms multiple reactive intermediates when acted upon by bacterial nitrofuran reductase, bactericidal ; For UTI (except Proteus and Pseudomonas)

Nitrofurantoin (TOPNOTCH)

564

Inhibits mycolic acid synthesis, bactericidal

Isoniazid (TOPNOTCH)

565

SE: hepatotoxicity, neurotoxicity (seizures, peripheral neuritis, insomnia, restlessness, muscle twitching), acute hemolysis in G6PD deficiency, drug-induced lupus

Isoniazid (TOPNOTCH)

566

Most impt drug in TB

Isoniazid (TOPNOTCH)

567

prevent neurotoxicity of Isoniazid by giving

pyridoxine (vit B6) (TOPNOTCH)

568

given as a sole drug for prophylaxis of close contacts of TB Px and skin test converters

Isoniazid (TOPNOTCH)

569

Inhibits DNA-dependent RNA polymerase, bactericidal

Rifamycin derivatives: Rifampicin, rifabutin, rifapentine, rifamixin (TOPNOTCH)

570

red-orange urine, light chain proteinuria, skin rash, thrombocytopenia, nephritis, hepatotoxicity, flulike syndrome, anemia, impair antibody response

Rifamycin derivatives: Rifampicin, rifabutin, rifapentine, rifamixin (TOPNOTCH)

571

CYP450 inhibitor: Rifampicin or INH

INH (TOPNOTCH)

572

CYP450 inducer: Rifampicin or INH

Rifampicin (TOPNOTCH)

573

Inhibits arabinosyl transferases involved in the synthesis of arabinogalactan in mycobacterial cell wall, bacteriostatic

Ethambutol (TOPNOTCH)

574

SE: dose-dependent visual disturbances (decreased visual acuity, red green color blindness, retrobulbar neuritis, retinal damage, optic neuritis), headache, confusion, hyperuricemia, peripheral neuritis

Ethambutol (TOPNOTCH)

575

Unknow MOA, bacteriostatic but can be bactericidal on actively dividing mycobacteria, is metabolized to pyrazinoic acid, t 1/2 is increased in liver and kidney disease

Pyrazinamide (TOPNOTCH)

576

SE: hepatotoxicity, nongouty polyarhtralgia, asymptomatic hyperuricemia, myalgia, GIT irritation, maculopapular rash, porphyria, photosensitivity ; CI in pregnancy

Pyrazinamide (TOPNOTCH)

577

Most hepatotoxic anti-TB drug

Pyrazinamide (TOPNOTCH)

578

Most active drug against M. leprae

Dapsone (TOPNOTCH)

579

_______ is a repository form of dapsone which has drug action that can last for several months

Acedapsone (TOPNOTCH)

580

Binds to guanine bases in bacterial DNA, bactericidal ; For leprosy

Clofazimine (TOPNOTCH)

581

Binds to ergosterol in fungal cell membranes, forming artificial pores, fungicidal

Amphotericin B (TOPNOTCH)

582

WIDEST antifungal spectrum

Amphotericin B (TOPNOTCH)

583

For systemic fungal infections (aspergillus, blastomyces, candida, Cryptococcus, histoplasma, mucor), for initial induction before followup treatment with azoles, can be used topically in mycotic corneal ulcers and keratitis

Amphotericin B (TOPNOTCH)

584

Accumulated in fungal cells by the action of permease and converted by cytosine deaminase to 5-FU, which inhibits thimidylate synthase, pyrimidine antimetabolite, fungistatic

Flucytosine (TOPNOTCH)

585

SE: infusion reactions (chills, fever, muscle spasms, vomiting, hypotension), dose limiting nephrotoxicity (decreased GFR, ATN with magnesium and potassium wasting, decreased erythropoietin), neurotoxicity (seizure, neuronal damage)

Amphotericin B (TOPNOTCH)

586

Inhibit 14-demethylase --> decreased ergosterol production --> increased permeability of cell membrane, Inhibits fungal P450-dependent enzymes blocking ergosterol synthesis, fungistatic

Ketoconazole (TOPNOTCH)

587

SE: GI disturbances (vomiting, diarrhea), rash, hepatotoxicity, drug interaction, gynecomastia, menstrual irregularities and infertility

Ketoconazole (TOPNOTCH)

588

DOC for candidiasis (esophageal, oropharyngeal, vulvovaginitis), coccidioidomycosis, cryptococcal meningitis (treatment and prophylaxis)

Fluconazole (TOPNOTCH)

589

alternative to Ampho B in the treatment of C. neoformans, as effective as Ampho B in candidemia

Fluconazole (TOPNOTCH)

590

DOC for blastomycosis, sporotrichosis, dermatophytosis esp onchomycosis, chromoblastomycosis ; alternative for infections due to Aspergillus, Coccidioides, Cryptococcus and Histoplasma , for esophageal candidiasis resistant to fluconazole

Itraconazole (TOPNOTCH)

591

co-DOC for invasive aspergillosis, alternative in candidemia, for fluconazole-resistant organisms, for candidal esophagitis and stomatitis in AIDS patients

Voriconazole (TOPNOTCH)

592

SE: GI disturbances (vomiting, diarrhea), rash, hepatotoxicity, blurring of vision in 30% of patients, CI in pregnancy

Voriconazole (TOPNOTCH)

593

as salvage therapy in invasive aspergillosis

Posaconazole (TOPNOTCH)

594

BROADEST spectrum triazole ; the only azole with activity against Rhizopus sp. (mucormycosis

Posaconazole (TOPNOTCH)

595

azoles that are limited to topical use because of systemic toxicity

Clotrimazole, miconazole, ketoconazole (TOPNOTCH)

596

Inhibit beta-glucan synthase which produces (1-->2) glycan which is a cell wall component, thus decreasing fungal cell wall synthesis, fungostatic

Echinocandins: Caspofungin, anidulafungin, micafungin (TOPNOTCH)

597

Interferes with microtubule function in dermatophytes, inhibits synthesis and polymerization of nucleic acids, fungistatic

Griseofulvin (TOPNOTCH)

598

Inhibits with ergosterol synthesis by inhibiting fungal squalene oxidase leading to increased squalene which interferes with ergosterol synthesis, fungicidal

Terbinafine (TOPNOTCH)

599

absorption is increased by intake of fatty meal

Griseofulvin (TOPNOTCH)

600

Binds to ergosterol in fungal cell membranes, forming artificial pores, fungicidal

Nystatin (TOPNOTCH)

601

For candidiasis ((oropharyngeal, esophageal and vaginal), for GI fungal infections in patients with impaired defense mechanisms

Nystatin (TOPNOTCH)

602

Activated by viral thymidine kinase (TK) to forms that inhibit viral DNA polymerase, guanosine analog, competitive substrate for DNA polymerase, causes chain termination after its incorporation into the viral DNA

Acyclovir, valacyclovir, penciclovir, famciclovir, docosanol (TOPNOTCH)

603

For infections due to HSV1, HSV2, VZV (mucocutaneous and genital herpes, prophylaxis in AIDS and in other Immunocompromised states such as organ transplant patients, herpes encephalitis, neonatal HSV infection etc.

Acyclovir, valacyclovir, penciclovir, famciclovir, docosanol (TOPNOTCH)

604

_____ is a prodrug that is converted to Acyclovir and reached plams levels 3-5x (longer t1/2) more than acyclovir

Valacyclovir (TOPNOTCH)

605

____ is a prodrug which is converted to Penciclovir in vivo

Famciclovir (TOPNOTCH)

606

Inhibits fusion between the HSV envelope and plasma membrane, prevents viral entry and subsequent replication

Docosanol (TOPNOTCH)

607

Inhibits viral DNA polymerase causing chain termination, guanosine derivative

Ganciclovir, valganciclovir (TOPNOTCH)

608

For infections due to CMV, HSV1, HSV2, VZV ; For prohylaxis and treatment of CMV retinitis and other CMV infections in the immunocompromised patients

Ganciclovir, valganciclovir (TOPNOTCH)

609

Inhibits viral DNA polymerase causing chain termination ; For CMV retinitis, mucocutaneous HSV infections, acyclovir-resistance, ganciclovir-resistance, genital warts and molluscum contangiosum

Cifodovir (TOPNOTCH)

610

Inhibits viral RNA polymerase, DNA polymerase, and HIV reverse transcriptase, binds to pyrophosphate binding site

Foscarnet (TOPNOTCH)

611

adenine analog ; For HSV, VZV, CMV

Vidarabine (TOPNOTCH)

612

pyrimidine analogs ; For herpes keratitis (HSV-1)

Idoxuridine, trifluridine (TOPNOTCH)

613

antisense oligonucleotide that binds to mRNA of CMV causing inhibition of early protein synthesis ; For CMV retinitis

Fomivirsen (TOPNOTCH)

614

Inhibit HIV reverse transcriptase after phosphorylation by cellular enzymes, acts as chain terminators via insertion into the growing DNA chain

NRTI (TOPNOTCH)

615

NRTIs

Abacavir, Didanosine (ddI), Emtricitabine, Lamivudine (3TC), Stavudine (d4T), Tenofovir, Zalcitabine (ddC),Zidovudine (ZDV) (TOPNOTCH)

616

Inhibits HIV reverse transcriptase, no phosphorylation required, do not compete with nucleoside triphosphate

NNRTI (TOPNOTCH)

617

NNRTIs

Delavirdine, efavirenz, etravirine, nevirapine (TOPNOTCH)

618

cleaves precursor polyprotein to form the final structural protein of the mature virion core, inhibits viral protein processing

Protease Inhibitor (TOPNOTCH)

619

Protease Inhibitor

Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir-Ritonavir, Nelfinavir, Ritonavir, Saquinavir, Tipranavir (TOPNOTCH)

620

Binds to gp41 subunit of viral envelope glycoprotein, preventing fusion of viral and cellular membranes

Fusion Inhibitor: Enfuvirtide (TOPNOTCH)

621

Blocks viral attachment by blocking CCR5, a transmembrane protein involved in the attachment of HIV to host cell

CCR5 receptor antagonist: Maraviroc (TOPNOTCH)

622

Inhibit early step replication and prevent uncoating by binding to M2 proton channels ; For influenza A and rubella

Uncoating inhibitors: Amantadine, rimantadine (TOPNOTCH)

623

Inhibits neuraminidase which cleaves sialic acid residues from viral proteins and surface proteins of infected cells , decrease release of progeny virus

Neuraminidase inhibitors: Oseltamivir, zanamivir (TOPNOTCH)

624

DOC for influenza (including H1N1)

Neuraminidase inhibitors: Oseltamivir, zanamivir (TOPNOTCH)

625

cytokine, increased activity of JAKS leading to phosphorylation of signal transducers and activation of transcription (STATS) which causes increased formation of antiviral proteins

Interferon (TOPNOTCH)

626

For chronic HBV, HCV infection, Kaposi sarcoma, genital warts, prevents dissemination of HZV in cancer patients and decreased CMV shedding after renal transplantation

Interferon (TOPNOTCH)

627

Inhibits HBV DNA polymerase causing chain termination after incorporation into the viral DNA

Adefovir, Dipivoxil, Telbivudine, Tenofovir (TOPNOTCH)

628

______ is a prodrug of Adefovir

Dipiroxil (TOPNOTCH)

629

_____is an anti-RT drug that is also effective in chronic HBV, it is active against lamivudine and entecavir-resistant strains

Tenofovir (TOPNOTCH)

630

guanosine nucleoside, inhibits DNA polymerase

Entecavir (TOPNOTCH)

631

Coinfection between HBV and HIV may increase the risk of pancreatitis with_____use

lamivudine (TOPNOTCH)

632

Inhibits guanosine triphosphate formation, prevents capping of viral mRNA, blocks RNA-dependent RNA polymerase, inhibit replication of many DNA and RNA viruses like Influenza A and B, parainfluenza, paramyxo viruses, HCV and HIV

Ribavirine (TOPNOTCH)

633

For HCV infection (with IFN ) and RSV infection, decreasesmortality in viral hemorrhagic fevers

Ribavirine (TOPNOTCH)

634

Prevents polymerization of heme into hemozoin, blood schizonticide

Chloroquine, hydroxychloroquine (TOPNOTCH)

635

Complexes with DNA to prevent strand separation, blocks DNA replication and transcription, blood schizonticide

Quinine, quinidine gluconate (TOPNOTCH)

636

DOC for malaria in pregnant patients

Quinine, quinidine gluconate (TOPNOTCH)

637

1st line drug (weekly administration) for prophylaxis in all areas with Chloroquine resistance)

Mefloquine (TOPNOTCH)

638

Forms electron-transferring redox compounds that act as cellular oxidants, tissue schizonticides, gametocides

Primaquine (TOPNOTCH)

639

Eradicates hypnozoites in the liver, preventing malarial relapse

Primaquine (TOPNOTCH)

640

______ disrupts mitochondrial electron transport, blood and tissue schizonticide, ______ inhibits folate synthesis, sporonticide

Atovaquone-proguanil (TOPNOTCH)

641

also effective against Mefloquine-resistant Falciparum infection

Atovaquone-proguanil (TOPNOTCH)

642

_____ is the DOC for uncomplicated falciparum malaria in the Philippines

Co-artem (TOPNOTCH)

643

DOC for asymptomatic cyst carrier of E. histolytica

Diloxanide Furoate (TOPNOTCH)

644

Inhibits protein synthesis, blocks ribosomal movement along messenger RNA, tissue amebicide ; back up drug for severe intestinal and extraintestinal amebiasis

Emetine, dehydroemetine (TOPNOTCH)

645

Inhibits protein synthesis, binds to 16S ribosomal subunit, luminal amebicide ; For intestinal amebiasis, cryptosporidiosis

Paromomycin (TOPNOTCH)

646

For metronidazole-resistant amebiasis, giardiasis, cryptosporidiosis (DOC)

Nitazoxanide (TOPNOTCH)

647

For prophylaxis and treatment of pneumocystosis (DOC), prophylaxis (T. gondii, I. belli)

Co-trimoxazole (TOPNOTCH)

648

For prophylaxis and treatment of toxoplasmosis (DOC)

Pyrimethamine-sulfadiazine (TOPNOTCH)

649

alternative drug for Toxoplasmosis is _____

Clindamycin (TOPNOTCH)

650

For African sleeping sickness (hemolymphatic stage),onchocerciasis (backup)

Suramin (TOPNOTCH)

651

Suicide inhibitor of ornithine decarboxylase; For advanced west African sleeping sickness (DOC)

Eflornithine (TOPNOTCH)

652

Organic arsenical, inhibits enzyme sulfhydryl groups in trypanosomes; DOC for African sleeping sickness

Melarsoprol (TOPNOTCH)

653

Inhibits trypanothione reductase; DOC for Chagas disease (Trypanosoma cruzi)

Nifurtimox (TOPNOTCH)

654

DOC for Leishmaniasis

Sodium Stibogluconate (TOPNOTCH)

655

Selectively inhibits microtubule synthesis and glucose uptake in nematodes, ovicidal ; For ascariasis, pinworm, whipworm

Mebendazole (TOPNOTCH)

656

Inhibits microtubule assembly, larvicidal and ovicidal ; For ascariasis, hookworm, whipworm, hydatid disease (DOC), threadworms, filariasis, larva migrans, cysticercosis

Albendazole (TOPNOTCH)

657

primary drug for ascariasis, ancylostomiasis, trichuriasis

Albendazole (TOPNOTCH)

658

DOC for filariasis and eye worm disease

Diethylcarbamazine (TOPNOTCH)

659

May cause mazzotti reaction when used for onchocerciasis

Diethylcarbamazine (TOPNOTCH)

660

Intensifies GABA-mediated neurotransmission in nematodes, immobilizes parasites ; DOC for strongyloidiasis

Ivermectin (TOPNOTCH)

661

Stimulates nicotinic receptors at NMJ of nematodes, causes depolarization-induced paralysis

Pyrantel pamoate (TOPNOTCH)

662

DOC for hookworm and roundworm infections

Pyrantel pamoate (TOPNOTCH)

663

DOC for trichinosis

Thiabendazole (TOPNOTCH)

664

DOC for trematodes (schistosoma, paragonimus, clonorchis, opistorchis) and cestodes (taenia, diphyllobothrium)

Praziquantel (TOPNOTCH)

665

Used with steroid when treating neurocysticercosis, contraindicated in ocular cysticercosis (may cause irreparable eye damage)

Praziquantel (TOPNOTCH)

666

Increases membrane permeability to calcium, cause muscle paralysis, vacualization and death

Praziquantel (TOPNOTCH)

667

Uncouples oxidative phosphorylation or by activating ATPases ; alternative drug for cestode infection (Taenia, diphyllobotrium)

Niclosamide (TOPNOTCH)

668

Forms DNA cross-links, resulting in inhibition of DNA synthesis and function, Cell-cycle nonspecific

Alkylating agents (TOPNOTCH)

669

Alkylating agents

Cyclophosphamide, chlorambucil, Cisplatin, Carboplatin, oxaliplatin, Procarbazine, Dacarbazine, Busulfan, Carmustine, lomustine (TOPNOTCH)

670

SE: bone marrow suppression, hemorrhagic cystitis, hepatotoxicity, alopecia, SIADH, pulmonary toxicity

Cyclophosphamide (TOPNOTCH)

671

Rescue therapy for cyclophosphamide

MESNA (TOPNOTCH)

672

Rescue therapy for Cisplatin

Amifostine (TOPNOTCH)

673

can penetrate the CSF, For Hodgkin's lymphoma, non-hodgkin's lymphoma, brain tumors

Procarbazine (TOPNOTCH)

674

SE: pulmonary fibrosis, adrenal insufficiency, skin pigmentation

Busulfan (TOPNOTCH)

675

Highly lipophilic allowing ease of passage through BBB into the CNS ; For brain tumors, melanoma, skin cancer

Carmustine, lomustine (TOPNOTCH)

676

Inhibits dihydrofolate reductase, decreases synthesis of thymidylate, amino acids, purine nucleotides; cell cycle specific

Methotrexate (TOPNOTCH)

677

Rescue therapy for methotrexate

Leucovorin (Folinic acid) (TOPNOTCH)

678

Inhibits de novo purine nucleotide synthesis, activated by HGPRT, cell cycle specific ; For acute leukemia (AML, ALL), CML

6-Mercaptopurine, 6-thioguanine, fludarabine, cladribine (TOPNOTCH)

679

Inhibits thymidylate synthase, causes thymineless death of cells, cell cycle specific

5-Fluorouracil (TOPNOTCH)

680

a deoxycytidine analog

Gemcitabine (TOPNOTCH)

681

Most specific for the S-phase of the cell cycle

Cytarabine (TOPNOTCH)

682

Prevents microtubule assembly, causes cell arrest at metaphase, cell cycle specific

Vinca alkaloid: Vincristine, Vinblastine (TOPNOTCH)

683

Inhibits DNA topoisomerase II, inhibits mitochondrial electron transport, cell cycle specific

Etoposide (TOPNOTCH)

684

Inhibits DNA topoisomerase I, cell cycle specific; For advanced ovarian cancer (2nd line), small cell lung cancer

Topotecan, irinotecan (TOPNOTCH)

685

Interferes with mitotic spindle, prevents microtubule disassembly into tubulin monomers, cell cycle specific

Paclitaxel, docetaxel (TOPNOTCH)

686

used in solid tumors like breast, ovarian, lung, gastroesophageal, prostate, bladder and head & neck cancers

Paclitaxel, docetaxel (TOPNOTCH)

687

Acts primarily in M phase of cancer cell cycle

Vinca alkaloid: Vincristine, Vinblastine (TOPNOTCH)

688

Intercalates between base pairs, inhibits topoisomerase II, generates free radicals cell cycle non-specific

Anthracycline: Doxorubicin, daunorubicin, idarubicin, epirubicin, mitoxantrone (TOPNOTCH)

689

Rescue therapy for Doxorubicin

dexrazoxane (TOPNOTCH)

690

Most specific for the G2 phase of cell cycle

Bleomycin (TOPNOTCH)

691

SE: pneumonitis, pulmonary fibrosis, alopecia, mucocutaneous reactions

Bleomycin (TOPNOTCH)

692

Binds to double stranded DNA, inhibits DNA-dependent RNA synthesis, cell cycle non-specific

Actinomycin D (TOPNOTCH)

693

Tyrosine kinase inhibitor of the protein product of bcr-abl oncogene in CML ; For CML, GIST

TK inhibitor: Imatinib, dasatinib, nilotinib (TOPNOTCH)

694

recognizes a surface protein in breast CA cells that overexpress Her-2-Neu receptors for epidermal growth factor

Trastuzumab (TOPNOTCH)

695

Inhibits binding of VEGF to VEGFR leading to inhibiton of VEGF signalling, inhibits tumor vascular permeability but enhances tumor blood flow and drug delivery

Bevacizumab (TOPNOTCH)

696

Binds to a surface protein in NHL cells, induces complement-mediated lysis, direct cytotoxicity and induction of apoptosis

Rituximab (TOPNOTCH)

697

Endogenous glycoproteins with antineoplastric, immunosuppressive and antiviral actions

Interferon alpha (TOPNOTCH)

698

Depletes serum asparagines ; For ALL, T-cell auxotrophic CA (leukemia and lymphomas) that require asparagine for growth

Asparaginase (TOPNOTCH)

699

Only vitamin that can cure cancer

All-Trans retinoic acid (TOPNOTCH)

700

For acute promyelocytic leukemia

All-Trans retinoic acid (TOPNOTCH)

701

Suppresses inflammation and immune response, may trigger apoptosis and work on nondividing cancer cells

Prednisone (TOPNOTCH)

702

Estrogen antagonist actions in breasts tissue and CNS, estrogen agonist effects in uterus, liver and bone

Tamoxifen (TOPNOTCH)

703

Androgen antagonist ; For prostate cancer

Flutamide (TOPNOTCH)

704

Increased LH, FSH secretion with intermittent administration, reduced LH and FSH secretion with prolonged continuous administration ; For prostate cancer

Leuprolide (TOPNOTCH)

705

Reduces estrogen synthesis by inhibiting aromatase; For breast cancer

Anastrazole (TOPNOTCH)

706

Effective againsts breast cancer that have become resistant to tamoxifen

Anastrazole (TOPNOTCH)

707

Neutralize stomach acid by reacting with protons in the lumen

Antacids (TOPNOTCH)

708

Impairs absorption of tetracyclines, flouroquinolones,itraconazole and iron

Antacids (TOPNOTCH)

709

Antacids

Magnesium-Aluminum Hydroxide, Calcium carbonate, Sodium bicarbonate (TOPNOTCH)

710

Competitive pharmacologic block of H2 receptors ; for peptic ulcer disease, Zollinger-Ellison syndrome, Gastroesophagal reflux, dyspepsia

H2 Receptor Blockers (TOPNOTCH)

711

H2 Receptor Blockers

Cimetidine, Ranitidine, Famotidine, Nizatidine (TOPNOTCH)

712

Highly effective in suppressing nocturnal acid secretion but only modest effect on meal- stimulated secretion

H2 Receptor Blockers (TOPNOTCH)

713

Irreversible blockade of H/K ATPase in active gastric panetal cells. Long lasting reduction of meal stimulated and nocturnal acid secretion

Proton Pump Inhibitors (TOPNOTCH)

714

Proton Pump Inhibitors

Omeprazole, Lansopraole, Rabeprazole, Pantoprazole, Esomeprazole (TOPNOTCH)

715

usually enetric coated, needs 3-4 days treatment to achieve full effectiveness

Omeprazole, Lansopraole, Rabeprazole, Pantoprazole, Esomeprazole (TOPNOTCH)

716

SE: Diarrhea, headache, abdominal pain, Malaabsorption (Vit B12, Ca, Fe, Zn), Infections (respiratory, enteric), Hypergastrinemia, Atrophic gastritis

Omeprazole, Lansopraole, Rabeprazole, Pantoprazole, Esomeprazole (TOPNOTCH)

717

Binds to injured tissue and forms a protective covering with ulcer beds. Accelerates healing of peptic ulcers and reduces recurrence rate

Sucralfate (TOPNOTCH)

718

Forms a protective coating on ulcerated tissue. Stimulates mucosal protective mechanisms, direct antimicrobial effects and sequestration of enterotoxins

Bismuth Salicylate (TOPNOTCH)

719

SE: Abdominal pain, Diarrhea, Uterine cramping, Miscarriage

Misoprostol (TOPNOTCH)

720

Activates EP receptors. Causes incresed HCO3 and mucus secretion in stomach. Uterine contraction

Misoprostol (TOPNOTCH)

721

SE: Black stools, darkening of tongue, Encephalopathy (Atraxia, headaches, confusion, seizures)

Bismuth Salicylate (TOPNOTCH)

722

Increases gastric emptying and intestinal motility

Metoclopramide, Domperidone, Erythromycin (TOPNOTCH)

723

______ and ______ block D receptors ; _______ stimulates motilin receptors

Metoclopramide and domperidone, Erythromycin (TOPNOTCH)

724

T or F: Domperidone does not cross the BBB (less toxic)

TRUE (TOPNOTCH)

725

Indigestible, hydrophilic colloids that absorb water, forming a bulky emollient gel that distends the colon and promotes peristasis

Bulk-forming Laxatives: Psyllium, Methylcellulose, Polycarbophil (TOPNOTCH)

726

Soften stool material, Permitting water and lipids to penetrate

Stool-softener: Docusate, Glycerine, Suppository, Mineral oil (TOPNOTCH)

727

Soluble but nonabsorbable compound that result in increased stool liquidity due to an obligate increase in fecal fluid

Osmotic Laxatives: Lactulose, Magnesium oxide, Sorbitol, Magnesium citrate, Sodium phosphate, Polyethylene Glycol (TOPNOTCH)

728

Directly stimulate enteric nervous system and colonic electrolyte and fluid secretion

Stimulant Laxatives: Bisacodyl, Aloe, Senna, Cascara, Castor oil (TOPNOTCH)

729

Activates opioid receptors in enteric nervous system. Slows motility with negligible CNS effects

Diphenoxylate, Loperamide, Kaolin+Pectin, Colloidal Bismuth (TOPNOTCH)

730

Blocks chemoreceptor trigger zone and enteric nervous system 5-HT3 receptors ; For Vomiting (Post chemothereaphy, postoperative)

Ondansetron, Granisetron, Dolasetron, Palonosetron (TOPNOTCH)

731

Probably inhibits production of eicosanoid inflammatory mediators ; for Inflammatory bowel disease (mild to moderate)

Mesalamine, Balsalazide, Olsalazine, Sulfasalazine (TOPNOTCH)