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Flashcards in Pharm_Part2 Deck (280):
1

1st generation H1 blockers

Diphenhydramine, dimenhydrinate, chlopheniramine Clinical uses: Allergy, motion sickness, sleep aid Toxicity: Sedation, antimuscarinic, anti-α-adrenergic

2

2nd generation H1 blockers

Loratadine, fexofenadine, desloratadine, cetirizine (-adine) Clinical uses: Allergy Toxicity: Far less sedating than 1st generation because of ↓ entry into CNS

3

ACE inhibitors: Names

Captopril, enalapril, lisinopril (-pril)

4

Acetazolamide

Mechanism: Carbonic anhydrase inhibitor. Causes self-limited NaHCO3 diuresis and reduction in total-body HCO3- stores Clinical use: Glaucoma, urinary alkalinization, metabolic alkalosis, altitude sickness Toxicity: Hyperchloremic metabolic acidosis, neuropathy, NH3 toxicity, sulfa allergy

5

Adalimumab

TNF-α inhibitors Mechanism: Anti-TNF antibody Clinical use: Rheumatoid arthritis, psoriasis, ankylosing spondylitis

6

Advantages (5) & Disadvantages (4) of Oral contraception

Advantages: Reliable (<1% failure); ↓ risk of endometrial and ovarian cancer; ↓ incidence of ectopic pregnancy; ↓ pelvic infections; regulation of menses Disadvantages: Taken daily; No protection against STDs; ↑ triglycerides; Depression, weight gain, nausea, hypertension; Hypercoagulable state

7

Albuterol

Asthma drug, relaxes bronchial smooth muscle (β2). Use during acute exacerbation.

8

Allopurinol

Gout drug, chronic gout. Inhibits xanthine oxidase. ↓ conversion of xanthine to uric acid. Also used in lymphoma and leukemia to prevent tumor lysis associated urate nephropathy. ↑ concentrations of azathioprine and 6-MP (both normally metabolized by xanthine oxidase)

9

Alzheimer's drugs: Two types

Memantine: NMDA receptor antagonist Donepezil: Acetylcholinesterase inhibitors

10

Anastrozole / exemestane

Aromatase inhibitors used in postmenopausal women with breast cancer

11

Anesthetics - General principles: Drug with ↓ solubility in blood

rapid induction and recovery time

12

Anesthetics - General principles: Drugs with ↑ solubility in lipids

↑potency = 1/MAC

13

Antidote: Benzodiazepines

Flumazenil (competitive antagonist at GABA benzodiazepine receptor)

14

Antidote: Neuromuscular blocking drugs

Neostigmine, edrophonium, and other cholinesterase inhibitors

15

Antidote: Tricyclic antidepressants

NaHCO3 for CV toxicity

16

Antipsychotic with low potency

Thioridazine, chlorpromazine - non neurologic side effects (anticholinergic, antihistamine, and α blockade effects)

17

Antipsychotics (neuroleptics): Names

Haloperidol + "-azine"s

18

Antipsychotics with high potency

Haloperidol, trifluoperazine, fluphenazine - neurologic side effects (extrapyramidal symptoms).

19

Arachidonic acid products

Lipoxygenase pathway yields Leukotrienes LTB4 is a neutrophil chemotactic agent LTC4, D4, E4 function in bronchoconstriction, vasoconstriction, contraction of smooth muscle, and ↑ vascular permeability PGI2 inhibits platelet aggregation and promotes vasodilation

20

Asthma drugs (7)

①non-specific β-agonists: Isoproterenol ②β2-agonists: Albuterol, Salmeterol ③Methylxanthines: Theophylline ④Muscarinic antagonists: Ipratropium ⑤Cromolyn ⑥Corticosteroids: Beclomethasone, prednisone ⑦Antileukotrienes: Zileuton; Zafirlukast / Montelukast

21

Atypical antipsychotics: Names

Olanzapine, clozapine, quetiapine, risperidone, aripiprazole, ziprasidone (-apine, -idone, aripiprazole)

22

Beclomethasone / prednisone

Asthma drug, inhibit the synthesis of virtually all cytokines. Inactivate NF-kB, the transcription factor that induces the production of TNF-α, among other inflammatory agents. 1st-line therapy for chronic asthma.

23

Biphosphonates (-dronate)

Mechanism: Inhibit osteoclast activity; reduce both formation and resorption of hydroxyapatite Clinical use: Malignancy-associated hypercalcemia, Paget's disease of the bone, post menopausal osteoporosis Toxicity: Corrosive esophagitis (except zoledronate), nausea, diarrhea, osteonecrosis of the jaw

24

Bosentan

Used to treat pulmonary hypertension. Competitively antagonizes endothelin-1 receptors, decreasing pulmonary vascular resistance.

25

Bupropion

Also used for smoking cessation. ↑ NE and dopamine via unknown mechanism. Toxicity: stimulant effects (tachycardia, insomnia), headache, seizure in bulimic patients. No sexual side effects.

26

Butorphanol

Mechanism: Partial agonist at opioid mu receptors, agonist at kappa receptors. Clinical use: Pain; causes less respiratory depression than full agonists Toxicity: Causes withdraw if on full opioid agonist

27

Clinical use: ACE inhibitors

Hypertension, CHF, diabetic renal disease

28

Clinical use: Acetaminophen

Antipyretic, analgesic, but lacking anti-inflammatory properties. Used instead of aspirin to prevent Reye's syndrome in children with viral infection.

29

Clinical use: Antipsychotics

Schizophrenia (primarily positive symptoms), psychosis, acute mania, Tourette's syndrome

30

Clinical use: Aspirin

Low dose (<300 mg/day): ↓ platelet aggregation. Intermediate dose (300-2400 mg/day): antipyretic and analgesic High dose: (2400-4000 mg/day): anti-inflammatory

31

Clinical use: Atypical antipsychotics

Schizophrenia - both positive and negative symptoms

32

Clinical use: Barbiturates

Sedative for anxiety, seizures, insomnia

33

Clinical use: Benzodiazepines

Anxiety, spasticity, status epilepticus, detoxification (especially alcohol withdrawal-DTs), night terrors, sleepwalking, general anesthetic (amnesia, muscle relaxation), hypnotic (insomnia)

34

Clinical use: Buspirone

Generalized anxiety disorder. Does not cause sedation, addiction, or tolerance. Does not interact with alcohol (vs. barbiturates, benzodiazepines)

35

Clinical use: Clomipramine

OCD

36

Clinical use: COX-2 inhibitors (celecoxib)

Rheumatoid and osteoarthritis; patients with gastritis or ulcers

37

Clinical use: Duloxetine

Depression, diabetic peripheral neuropathy, duloxetine has greater effect on NE

38

Clinical use: Imipramine

Bed wetting

39

Clinical use: K+-sparing diuretics

Hyperaldosteronism, K+ depletion, CHF

40

Clinical use: Lithium

Mood stabilizer for bipolar disorder; blocks relapse and acute manic events. Also SIADH.

41

Clinical use: Monoamine oxidase (MAO) inhibitors

Atypical depression, anxiety, hypochondiasis

42

Clinical use: Nonbenzodiazepine hypnotics

Insomnia (失眠)

43

Clinical use: Olanzapine

OCD, anxiety disorder, depression, mania, Tourette's syndrome

44

Clinical use: Phenytoin

Tonic-clonic seizures. Also a class IB antiarrhythmic.

45

Clinical use: Sildenafil / vardenafil

Erectile dysfunction

46

Clinical use: SSRIs

Depression, OCD, bulimia, social phobias

47

Clinical use: Tricyclic antidepressants

Major depression, fibromyalgia

48

Clinical use: Venlafaxine

Depression, generalized anxiety disorder

49

Clomiphene

Estrogen partial agonist, partial agonist at estrogen receptors in hypothalamus. Prevents normal feedback inhibition and ↑ release of LH and FSH from pituitary, which stimulates ovulation. Used to treat infertility and PCOS. May cause hot flashes, ovarian enlargement, multiple simultaneous pregnancies, and visual disturbances

50

CNS stimulants

Methylphenidate, dextroamphetamine, mixed amphetamine salts Mechanism: ↑ catecholamines at the synaptic cleft, especially NE and dopamine Clinical use: ADHD, narcolepsy, appetite control

51

Colchicine

Gout drug, acute gout (with NSAIDs). Binds and stabilizes tubulin to inhibit polymerization, impairing leukocyte chemotaxis and degranulation. GI side effects, especially if given orally. (Note: indomethacin is less toxic, also used in acute gout)

52

Complications: Succinylcholine

Hypercalcemia, hyperkalemia, hyperthermia

53

Contraindication: Barbiturates

in porphyria

54

Contraindication: Mannitol

Anuria, CHF

55

Contraindication: Monoamine oxidase (MAO) inhibitors

with SSRI or meperidine (to prevent serotonin syndrome)

56

Contraindication: Oral contraception

smokers > 35 years of age (↑ risk of cardiovascular events), patients with history of thromboembolism and stroke or history of estrogen-dependent tumor

57

Contraindications: Estrogens

ER-positive breast cancer, history of DVTs

58

Cromolyn

Asthma drug, prevents release of mediators from mast cells. Effective only for the prophylaxis of asthma. Not effective during an acute asthmatic attack. Toxicity is rare.

59

Dantrolene

Used in the treatment of malignant hyperthermia, which is caused by inhalation anesthetics (except N2O) and succinylcholine. Also used to treat neuroleptic malignant syndrome (a toxicity of antipsychotic drugs) MOA: prevents the release of Ca2+ from the sarcoplasmic reticulum of skeletal muscle

60

Dinoprostone

PGE2 analog causing cervical dilation and uterine contraction, inducing labor

61

Diuretics: electrolyte changes: Blood pH

↓(acidemia): Carbonic anhydrase inhibitors ↑(alkalemia): Loop diuretics and thiazides

62

Diuretics: electrolyte changes: Details

Check FA2011 page475, very important mechanisms!!!

63

Diuretics: electrolyte changes: Urine Ca2+

↑Loop diuretics ↓Thiazides

64

Diuretics: electrolyte changes: Urine K+

↑ in all except K+-sparing diuretics. Serum K+ may ↓ as a result.

65

Diuretics: electrolyte changes: Urine NaCl

↑ in all diuretics. Serum NaCl may ↓ as a result.

66

DOC: 1st line for acute Status epilepsy

Benzodiazepines

67

DOC: 1st line for seizures of eclampsia

MgSO4, benzodiazepines

68

DOC: 1st line for Status epilepsy prophylaxis

Phenytoin

69

DOC: 1st line for trigeminal neuralgia

Carbamazepine

70

DOC: 1st line of epilepsy drugs in pregnant women, children

Phenobarbital

71

DOC: Acute pulmonary edema, maintenance programs for addicts

Methadone

72

DOC: ADHD

Methylphenidate (Ritalin), Amphetamines (Dexedrine)

73

DOC: Alcohol withdrawal

Benzodiazepines

74

DOC: Anorexia/bulimia

SSRI

75

DOC: Anxiety

Benzodiazepines, Buspirone, SSRI

76

DOC: Atypical depression

MAO inhibitors, SSRIs

77

DOC: Bipolar disorder

"Mood stabilizers": Lithium, Valproic acid, Carbamazepine Atypical antipsychotics

78

DOC: Closure of a PDA

Indomethacin

79

DOC: Depression

SSRIs, SNRIs, TCAs

80

DOC: Depression with insomnia

Mirtazapine

81

DOC: Diarrhea

Loperamide / Diphenoxylate

82

DOC: Essential or familial tremors

β-blockers, e.g., propranolol

83

DOC: Obsessive-compulsive disorder

SSRIs, Clomipramine

84

DOC: Pain, cough suppression

Dextromethorphan

85

DOC: Panic disorder

SSRIs, TCAs, Benzodiazepines

86

DOC: Polycystic ovarian syndrome (to prevent hirsutism)

Ketoconazole and spironolactone

87

DOC: PTSD

SSRIs

88

DOC: Schizophrenia

Antipsychotics

89

DOC: Serotonin syndrome

Cyproheptadine, 5-HT2 receptor antagonist

90

DOC: Social phobias

SSRIs

91

DOC: Tourette's syndrome

Antipsychotics (haloperidol)

92

Donepezil

Alzheimer's drugs, also galantamine, rivastigmine. Mechanism: Acetylcholinesterase inhibitors. Toxicity: Nausea, dizziness, insomnia

93

Drug class: Amiodarone

Class III antiarrhythmics

94

Drug class: Amitriptyline

Tricyclic antidepressants

95

Drug class: Amoxapine

Tricyclic antidepressants

96

Drug class: Bretylium

Class III antiarrhythmics

97

Drug class: Chlordiazepoxide

Benzodiazepines

98

Drug class: Citalopram

SSRIs

99

Drug class: Clomipramine

Tricyclic antidepressants

100

Drug class: Desipramine

Tricyclic antidepressants

101

Drug class: Dextromethorphan

Opioid analgesics for cough

102

Drug class: Diatiazem

Calcium channel blockers

103

Drug class: diaze-, -pam, -lam

Benzodiazepines

104

Drug class: Diltiazem

Class IV antiarrhythmics

105

Drug class: Disopyramide

Class IA antiarrhythmics

106

Drug class: Dofetilide

Class III antiarrhythmics

107

Drug class: Doxepin

Tricyclic antidepressants

108

Drug class: Duloxetine

SNRIs

109

Drug class: Encainide

Class IC antiarrhythmics

110

Drug class: eszopiclone

Nonbenzodiazepine hypnotics

111

Drug class: Flecainide

Class IC antiarrhythmics

112

Drug class: Fluoxetine

SSRIs

113

Drug class: Ibutilide

Class III antiarrhythmics

114

Drug class: Imipramine

Tricyclic antidepressants

115

Drug class: Isocarboxazid

MAOI

116

Drug class: Ketorolac

NSAIDs

117

Drug class: Lidocaine

Class IB antiarrhythmics

118

Drug class: methimazole

Hyperthyroidism drug

119

Drug class: Mexiletine

Class IB antiarrhythmics

120

Drug class: Naproxen

NSAIDs

121

Drug class: Nifedipine

Calcium channel blockers

122

Drug class: Nortriptyline

Tricyclic antidepressants

123

Drug class: Paroxetine

SSRIs

124

Drug class: Phenelzine

MAOI

125

Drug class: Procainamide

Class IA antiarrhythmics

126

Drug class: Propafenone

Class IC antiarrhythmics

127

Drug class: Quinidine

Class IA antiarrhythmics

128

Drug class: Selegiline

MAOI, selective MAO-B inhibitor

129

Drug class: Sertraline

SSRIs

130

Drug class: Sotalol

Class III antiarrhythmics

131

Drug class: Thiopental

Barbiturates, used for induction of anesthesia

132

Drug class: Thiopentals

Barbiturates

133

Drug class: Tocainide

Class IB antiarrhythmics

134

Drug class: Tranylcypromine

MAOI

135

Drug class: Venlafaxine

SNRIs

136

Drug class: Verapamil

Calcium channel blockers

137

Drug class: Zaleplon

Nonbenzodiazepine hypnotics

138

Drug class: Zolpidem (Ambien)

Nonbenzodiazepine hypnotics

139

Drug use: Pirenzepine

Muscarinic antagonist

140

Drug use: Propantheline

Muscarinic antagonists

141

Epilepsy drug toxicities: Diplopia, ataxia, blood dyscrasias (agranulocytosis, aplastic anemia), liver toxicity, teratogenesis, induction of cytochrome P-450, SIADH, Stevens-Johnson syndrome

Carbamazepine

142

Epilepsy drug toxicities: Ethosuximide

EFGH - Ethosuximide, Fatigue, GI, Headache

143

Epilepsy drug toxicities: GI distress, fatigue, headache, urticaria, Stevens-Johnson syndrome

Ethosuximide

144

Epilepsy drug toxicities: GI distress, rare but fetal hepatotoxicity (measure LFTs), neural tube defects in fetus (spina bifida), tremor, weight gain. Contraindicated in pregnancy.

Valproic acid

145

Epilepsy drug toxicities: Nystagmus, diplopia, ataxia, sedation, gingival hyperplasia, hirsutism, megaloblastic anemia, teratogenesis (fetal hydantoin syndrome), SLE-like syndrome, induction of cytochrome P-450

Phenytoin

146

Epilepsy drug toxicities: Sedation, tolerance, dependence

Benzodiazepines

147

Epilepsy drug toxicities: Sedation, tolerance, dependence, induction of cytochrome P-450

Phenobarbital

148

Estrogens (ethinyl estradiol, DES, mestranol)

Mechanism: Bind estrogen receptors Clinical use: Hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women; use in men with androgen-dependent prostate cancer. Toxicity: ↑ risk of endometrial cancer, bleeding in postmenopausal women, ↑ risk of thrombi

149

Etanercept

TNF-α inhibitors Mechanism: Recombinant form of human TNF that binds TNF (Decoy receptor) Clinical use: Rheumatoid arthritis, psoriasis, ankylosing spondylitis

150

Ethacrynic acid

Mechanism: Phenoxyacetic acid dericative (NOT a sulfonamide). Essentially same action as furosemide. Clinical use: Diuresis in patients allergic to sulfa drugs Toxicity: Similar to furosemide; can be used in hyperuricemia, acute gout (never used to treat gout)

151

Evolution of EPS side effects

4h acute dystonia (muscle spasm, stiffness, oculogyric crisis) 4d akinesia (parkinsonian symptoms) 4wk akathisia (restlessness) 4mo tardive dyskinesia

152

Expectorants (2)

Guaifenesin: Expectorant - removes excess sputum; does not suppress cough reflex. N-acetylcysteine: Mucolytic - can loosen mucous plugs in CF patients. Also used as an antidote for acetaminophen overdose.

153

Fetal hydantoin syndrome

Intrauterine growth restriction with microcephaly and develop minor dysmorphic craniofacial features and limb defects including hypoplastic nails and distal phalanges (birth defects).

154

Finasteride (Propecia)

a 5α-reductase inhibitor (↓ conversion of testosterone to dihydrotestosterone). Useful in BPH. Also promotes hair growth - used to treat male-pattern baldness

155

Flutamide

a nonsteroidal competitive inhibitor of androgens at the testosterone receptor. Used in prostate carcinoma.

156

Furosemide

Mechanism: Sulfonamide loop diuretic. Inhibits cotransport system (Na+, K+, 2Cl-) of thick ascending limb of loop of Henle. Abolishes hypertonicity of medulla, preventing concentration of urine. ↑Ca2+ excretion Clinical use: Edematous states (CHF, cirrhosis, nephrotic syndrome, pulmonary edema), hypertension, hypercalcemia

157

Glaucoma drugs: Cholinomimetics

Direct: Pilocarpine, carbachol Indirect: Physostigmine, echothiophate

158

Glaucoma drugs: Diuretics

Acetazolamide, dorzolamide (-zolamide)

159

Glaucoma drugs: Emergencies

Pilocarpine

160

Glaucoma drugs: Prostaglandin

Latanoprost (PGF2α)

161

Glaucoma drugs: α-agonists

Epinephrine, Brimonidine

162

Glaucoma drugs: β-blockers

Timolol, betaxolol, carteolol

163

Hormone replacement therapy (HRT)

Used for relief or prevention of menopausal symptoms (e.g., hot flashes, vaginal atrophy) and osteoporosis (↑estrogen, ↓osteoclast activity) Unopposed estrogen replacement therapy (ERT) ↑ the risk of endometrial cancer, so progesterone is added. Possible ↑ CV risk

164

Huntington's drugs

Disease: ↑dopamine, ↓GABA+ACh Reserpine + tetrabenazine - amine depleting Haloperidol - dopamine receptor antagonist

165

Hydrochlorothiazide

Mechanism: Thiazide diuretic. Inhibits NaCl reabsorption in early distal tubule, reducing diluting capacity of the nephron. ↓ Ca2+ excretion Clinical use: Hypertension, CHF, idiopathic hypercalciuria, nephrogenic diabetes insipidus Toxicity: Hypokalemic metabolic alkalosis, hyponatremia, hyperglycemia, hyperlibidemia, hyperuricemia, and hypercalcemia. Sulfa allergy

166

Infliximab

TNF-α inhibitors Mechanism: Anti-TNF antibody Clinical use: Crohn's disease, rheumatoid arthritis, ankylosing spondylitis Toxicity: Predisposes to infections (reactivation of latent TB)

167

Intravenous anesthetics: Arylcyclohexylamines (Ketamine)

PCP analogs that act as dissociative anesthetics. Block NMDA receptors. Cardiocascular stimulants. Cause disorientation, hallucication, and bad dreams. ↑cerebral blood flow.

168

Intravenous anesthetics: Barbiturates

Thiopental - high potency, high lipid solubility, rapid entry into brain. Used for induction of anesthesia and short surgical procedures. Effect terminated by rapid redistribution into tissue and fat. ↓cerebral blood flow.

169

Intravenous anesthetics: Benzodiazepines

Midazolam most common drug used for endoscopy; used adjunctively with gaseous anesthetics and narcotics. May cause severe postoperative respiratory depression, ↓BP (treat overdose with flumazenil), and amnesia

170

Intravenous anesthetics: Opiates

Morphine, fentanyl used with other CNS depressants during general anesthesia

171

Intravenous anesthetics: Propofol

Used for rapid anesthesia induction and short procedures. Less postoperative nausea than thiopental. Potentiates GABA(A).

172

Ipratropium

Asthma drug, competitive block of muscarinic receptors, preventing bronchoconstriction. Also used for COPD, with ↓ production of mucus.

173

Isoproterenol

Asthma drug, relaxes bronchial smooth muscle (β2). Adverse effect is tachycardia (β1).

174

K+-sparing diuretics: Names

Spironolactone, Triamterene, Amiloride, Eplerenone

175

Latanoprost

PGF2α, ↑outflow of aqueous humor Side effects: Darkens color of iris (browning)

176

Leuprolide

Mechanism: GnRH analog with agonist properties when used in pulsatile fasion; antagonist properties when used in continuous fasion Clinical use: Infertility (pulsatile), prostate cancer (continuous - use with flutamide), uterine fibroids Toxicity: Antiandrogen, nausea, vomiting

177

Local enesthetics: Two groups

Esters - procaine, cocaine, tetracaine Amides - Lidocaine, mepivacaine, bupivacaine (amides have 2 i's in name)

178

Losartan

an angiotensin II receptor antagonist. It is not an ACE inhibitor and does not cause cough.

179

Mannitol

Mechanism: Osmotic diuretic, ↑tubular fluid osmolarity, producing ↑ urine flow Clinical use: Shock, drug overdose, ↑intracranial / intraocular pressure Toxicity: Pulmonary edema, dehydration

180

Maprotiline

Blocks NE reuptake. Toxicity: sedation, orthostatic hypotension.

181

Mechanism: ACE inhibitors

Inhibit angiotensin-converting enzyme, reducing levels of angiotensin II and preventing inactivation of bradykinin, a potent vasodilator. Renin release is ↑ due to loss of feedback inhibition

182

Mechanism: Acetaminophen

Reversibly inhibits cyclooxygenase, mostly in the CNS. Inactivated peripherally.

183

Mechanism: Antipsychotics

All typical antipsychotics block dopamine D2 receptors (↑[cAMP]1)

184

Mechanism: Aspirin

Irreversibly inhibit cyclooxygenase (both COX-1 and COX-2). Block prostaglandin synthesis.

185

Mechanism: Benzodiazepines

Facilitate GABA(A) action by ↑frequency of Cl- channel opening. ↓REM sleep. Most have long half-lives and active metabolites

186

Mechanism: Buspirone

Stimulates 5-HT1A receptors

187

Mechanism: COX-2 inhibitors (celecoxib)

Reversibly inhibit specifically the cyclooxygenase (COX) isoform 2, which is found in inflammatory cells and vascular endothelium and mediates inflammation and pain; spares COX-1, which helps maintain the gastric mucosa. Thus, should not have the corrosive effects of other NSAIDs on the GI lining.

188

Mechanism: L-dopa/carbidopa

↑level of dopamine in brain. Unlike dopamine, L-dopa can cross blood-brain barrier and is converted by dopa decarboxylase in the CNS to dopamine

189

Mechanism: Lithium

Possibly related to inhibition of phosphoinositol cascade

190

Mechanism: Local anesthetics

Block Na+ channels by binding to specific receptors on inner portion of channel. Preferentially bind to activated Na+ channels, so most effective in rapidly firing neurons. 3° amine local anesthetics penetrate membrane in uncharged form, then bind to ion channels as charged form

191

Mechanism: Monoamine oxidase (MAO) inhibitors

Nonselective MAO inhibition ↑ levels of amine neurotransmitters (NE, serotonin, dopamine)

192

Mechanism: Nonbenzodiazepine hypnotics

Act via the BZ1 receptor subtype and is reversed by flumazenil

193

Mechanism: Selegiline

Selectively inhibites MAO-B, which preferentially metabolizes dopamine over NE and 5-HT, thereby increasing the availability of dopamine

194

Mechanism: Sildenafil / vardenafil

Inhibit cGMP phosphodiesterase, causing ↑ cGMP, smooth muscle relaxation in the corpus cavernosum, ↑ blood flow, and penile erection. Sildenafil and vardenafil fill the penis.

195

Mechanism: SNRIs

Inhibit serotonin and NE reuptake

196

Mechanism: Spironolactone

a competitive aldosterone receptor antagonist in the cortical collecting tubule

197

Mechanism: SSRIs

Serotonin-specific reuptake inhibitors

198

Mechanism: Triamterene / Amiloride

act at the cortical collecting tubule by blocking Na+ channels in the DCT

199

Mechanism: Tricyclic antidepressants

Block reuptake of NE and serotonin

200

Memantine

Alzheimer's drug Mechanism: NMDA receptor antagonist; helps prevent excitotoxicity (mediated by Ca2+) Toxicity: Dizziness, confusion, hallucinations

201

Mifepristone (RU-486)

Mechanism: Competitive inhibitor of progestins at progesterone receptors Clinical use: Termination of pregnancy. Administered with misoprostol (PGE1) Toxicity: Heavy bleeding, GI effects (nausea, vomiting, anorexia), abdominal pain

202

Mirtazapine

α2 antagonist (↑ release of NE and serotonin) and potent 5-HT2 and 5-HT3 receptor antagonist. Toxicity: sedation, ↑ appetite, weight gain, dry mouth.

203

MOA: Atypical antipsychotics

Block 5-HT2, dopamine, α, and H1 receptors

204

MOA: Barbiturates

Facilitate GABA(A) action by ↑duration of Cl- channel opening, thus ↓neuron firing

205

MOA: Carbamazepine

↑Na+ channel inactivation

206

MOA: Ethosuximide

Blocks thalamic T-type Ca2+ channels

207

MOA: H1 blockers

Reversible inhibitors of H1 histamine receptors

208

MOA: Ketoconazole

Inhibits steroid synthesis (inhibits desmolase)

209

MOA: Opioids analgesics

Act as agonists at opioid receptors (mu=morphine, delta=enkephalin, kappa=dynorphin) to modulate synaptic transmission - open K+ channels, close Ca2+ channels → ↓synaptic transmission. Inhibit release of ACh, NE, 5-HT, glutamate, substance P

210

MOA: Phenytoin

Use-dependent blockade of Na+ channels; ↑refractory period; inhibition of glutamate release from excitatory presynaptic neuron

211

MOA: Spironolactone

Inhibits steroid binding

212

MOA: Valproic acid

↑Na+ channel inactivation, ↑GABA concentration

213

Molecular: GABA(A)-R

A ligand-gated chloride channel binded by benzos, barbs, and EtOH

214

Monitoring: Lithium

Narrow therapeutic window requires close monitoring of serum levels. Almost exclusively excreted by the kidneys; most is reabsorbed at the proximal convoluted tubules following Na+ reabsorption

215

Monoamine oxidase (MAO) inhibitors: Names

Phenelzine, tranylcypromine, isocarboxazid, selegiline (selective MAO-B inhibitor)

216

Name Inhaled anesthetics (3)

Halothane, -flurane, nitrous oxide

217

Neuroleptic malignant syndrome (NMS)

rigidity, myoglobinuria, autonomic instability, hyperpyrexia. Treatment: dantrolene, D2 agonists (e.g., bromocriptine) FEVER: Fever, Encephalopathy, Vitals unstable, Elevated enzymes, Rigidity of muscles

218

Neuromuscular blocking drugs: Two groups

Depolarizing: Succinylcholine Nondepolarizing: Tubocurarine, -curium, -curonium

219

NSAIDs

Ibuprofen, naproxen, indomethacin, ketorolac Mechanism: Reversibly inhibit cyclooxygenase (both COX-1 and COX-2). Block prostaglandin synthesis. Clinical use: Antipyretic, analgesic, anti-inflammatory. Toxicity: Renal damage, fluid retention, aplastic anemia, GI distress, ulcers.

220

Order of nerve blockade: Local anesthetics

Small myelinated fibers > Small unmyelinated fibers > Large myelinated fibers > Large unmyelinated fibers

221

Parkinson's disease drugs: Four groups

Agonize dopamine receptors: a.ergot: Bromocriptine b.non-ergot: pramipexole ropinirole ↑dopamine: Amantiadine, L-dopa/carbidopa Prevent dopamine breakdown: Selegiline, -capone Curb excess cholinergic activity: Benztropine

222

Principle: Local anesthetics in acidic tissue

In infected (acidic) tissue, alkaline anesthetics are charged and cannot penetrate membrane effectively. More anesthetic is needed in these cases.

223

Probenecid

Gout drug, chronic gout. Inhibits reabsorption of uric acid in PCT (also inhibits secretion of penicillin)

224

Progestins

Mechanism: Bind progesterone receptors, reduce growth, and ↑ vascularization of endometrium Clinical use: Used in oral contraceptives and in the treatment of endometrial cancer and abnormal uterine bleeding

225

Raloxifene

Estrogen partial agonist, agonist on the bone; reduces resorption of bone; used to treat osterporosis

226

Reason: Why not use salicylates to treat gout?

All but the highest doses depress uric acid clearance. Even high doses (5-6 g/day) have only minor uricosuric activity

227

Ritodrine / Terbutaline

β2-agonists that relax the uterus; reduce premature uterine contractions

228

Salmeterol

Asthma drug, long-acting agent for prophylaxis. Adverse effects are tremor and arrhythmia.

229

Seizures: Almost always from temporal lobe (mood changes, illusions, hallucinations); impaired consciousness and postictal state are present

Complex partial, DOC: Carbamazepine

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Seizures: Brief arrhythmic jerking movements, last < 1 sec, usually occur in clusters for a few minutes; no loss of consciousness

Myoclonic, DOC: Valproic acid

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Seizures: Brief episode of staring, but no postictal confusion

Absence, DOC: Ethosuximide, valproate

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Seizures: Generalized tonic extension of the extremities, followed by clonic rhythmic movements; loss of consciousness and prolonged postictal confusion are present

Tonic-clonic, DOC: Phenytoin, carbamazepine, and valproate

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Seizures: One body part is involved; no loss of consciousness and no postictal confusion

Simple partial, DOC: Carbamazepine

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Serotonin syndrome

Hyperthermia, myoclonus, cardiovascular collapse, flushing, diarrhea, seizures

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Short acting benzodiazepines (3)

Triazolam, Oxazepam, Midazolam → Highest addictive potential

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Side effects: Tricyclic antidepressants

Sedation, α-blocking effects, atropine-like side effects. 3° TCAs (amitriptyline) have more anticholinergic effects than do 2° TCAs (nortriptyline). Desipramine is the least sedating and has lower seizure threshold.

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SNRIs: Names

Venlafaxine, duloxetine

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SSRIs: Names

Fluoxetine, paroxetine, sertraline, citalopram

239

Steven-Johnson syndrome

Prodome of malaise and fever followed by rapid onset of erythmatous / purpuric macules (oral, ocular, genital). Skin lesions progress to epidermal necrosis and sloughing

240

Sumatriptan

Mechanism: 5-HT(1B/1D) agonist. Causes vasoconstriction, inhibition of trigeminal activation and vasoactive peptide release. Half-life < 2 hours Clinical use: Acute migraine, cluster headache attacks. Toxicity: Coronary vasospasm (contraindicated in patients with CAD or Prinzmetal's angina), mild tingling

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Tamoxifen

Estrogen partial agonist, antagonist on the breast tissue; used to treat and prevent recurrence of ER-positive breast cancer

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Tamsulosin

α1-antagonist used to treat BPH by inhibiting smooth muscle contraction. Selective for α1(A,D) receptors (found in prostate) vs. vascular α1(B) receptors

243

Tardive dyskinesia

stereotypic oral-facial movements due to long-term antipsychotic use. Often irreversible.

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Testosterone (methyltestosterone)

Mechanism: Agonist at androgen receptors Clinical use: Treat hypogonadism and promote development of 2° sex characteristics; stimulation of anabolism to promote recovery after burn or injury; treat with ER-positive breast cancer (exemastane) Toxicity: Causes masculinization in females; reduces intratesticular testosterone in males by inhibiting release of LH (via negative feedback), leading to gonadal atrophy. Premature closure of epiphyseal plates. ↑LDL, ↓HDL

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Theophylline

Asthma drug, likely causes bronchodilation by inhibiting phosphodiesterase, thereby ↓ cAMP hydrolysis. Usage is limited because of narrow therapeutic index (cardiotoxicity, neurotoxicity); metabolized by P-450. Blocks actions of adenosine.

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Toxicity: ACE inhibitors

Cough, Angioedema, Proteinuria, Taste changes, hypOtesion, Pregancy problems, Rash, Increased renin, Lower angiotensin II. CAPTOPRIL. Also, hyperkalemia. Avoid with bilateral renal artery stenosis because ACE inhibitors significantly ↓ GFR by preventing constriction of efferent arterioles

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Toxicity: Acetaminophen

Overdose produces hepatic necrosis; acetaminophen metabolite depletes glutathione and forms toxic tissue adducts in liver. N-acetylcysteine is antidote - regenertates glutathione.

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Toxicity: Antipsychotics

1. Highly lipid soluble and stored in body fat; thus, very slow to be removed from body. 2. Extrapyramidal system (EPS) side effects. 3. Endocrine side effects (e.g., dopamine receptor antaganism → hyperprolactinemia → galactorrhea) 4. Side effects arising from blocking muscarinic (dry mouth, constipation), α (hypotension), and histamine (sedation) receptors. 5. Neuroleptic malignant syndrome (NMS) / Tardive dyskinesia

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Toxicity: Aspirin

Gastric upset. Chronic use can lead to acute renal failure, interstitial nephritis, and upper GI bleeding. Reye's syndrome in children with viral infection.

250

Toxicity: Atypical antipsychotics

Fewer extrapyramidal and anticholinergic side effects than traditional antipsychotics

251

Toxicity: Barbiturates

Dependence, additive CNS depression effects with alcohol, respiratory or cardiovascular depression (can lead to death), drug interactions owing to induction of liver microsomal enzymes (cytochrome P-450)

252

Toxicity: Benzodiazepines

Dependence, additive CNS depression effects with alcohol. Less risk of respiratory depression and coma than with barbiturates

253

Toxicity: Bupivacaine

CNS excitation, severe cardiovascular toxicity

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Toxicity: Chlorpromazine

Corneal deposits

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Toxicity: Clozapine

may cause agranulocytosis

256

Toxicity: Cocaine

Hypertension, hypotension, and arrhythmias

257

Toxicity: COX-2 inhibitors (celecoxib)

↑ risk of thrombosis. Sulfa allergy. Less toxicity to GI mucosa (lower incidence of ulcers, bleeding than NSAIDs)

258

Toxicity: Enflurane

Proconvulsant

259

Toxicity: Halothane

Hepatotoxicity

260

Toxicity: K+-sparing diuretics

Hyperkalemia (can lead to arrhythmias), endocrine effects with aldosterone antaganists (e.g., spironolactone causes gynecomastia, antiandrogen effects)

261

Toxicity: L-dopa/carbidopa

Arrhythmias from peripheral conversion to dopamine. Long-term use can → dyskinesia following administration, akinesia between doses. Carbadopa, a peripheral decarboxylase inhibitor, is given with L-dopa in order to ↑ the bioavailability of L-dopa in the brain and to limit peripheral side effects

262

Toxicity: Lithium

Tremor, sedation, edema, heart block, hypothyroidism, polyurea (ADH antagonist causing nephrogenic diabetes insipidus). Fetal cardiac defects include Ebstein anomaly and malformation of the great vessels.

263

Toxicity: Methoxyflurane

Nephrotoxicity

264

Toxicity: Monoamine oxidase (MAO) inhibitors

Hypertensive crisis with tyramine ingestion (in many foods, such as wine and cheese) and β-agonists; CNS stimulation.

265

Toxicity: Nitrous oxide

Expansion of trapped gas

266

Toxicity: Nonbenzodiazepine hypnotics

Ataxia, headaches, confusion. Shorter duration because of rapid metabolism by liver enzymes. Unlike older sedative-hypnotics, cause only modest day-after psychomotor depression and few amnestic effects. Lower dependence risk than benzodiazepines

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Toxicity: Olanzapine / Clozapine

may cause significant weight gain

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Toxicity: Opioid analgesics

Addiction, respiratory depression, constipation, miosis (pinpoint pupils), additive CNS depression with other drugs. Tolerance does not develop to miosis and constipation.

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Toxicity: Phenytoin

Nystagmus, ataxia, diplopia, sedation, SLE-like syndrome, induction of cytochrome P-450. Chronic use produces gingival hyperplasia in children, peripheral neuropathy, hirsutism, megaloblastic anemia (↓folate absorption). Teratogenic (fetal hydantoin syndrome).

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Toxicity: Selegiline

May enhance the adverse effects of L-dopa

271

Toxicity: Sildenafil / vardenafil

Headache, flushing, dyspepsia, impaired blue-green color vision. Risk of life-threatening hypotension in patients taking nitrates.

272

Toxicity: SNRIs

↑ BP most common; also stimulant effects, sedation, nausea

273

Toxicity: SSRIs

Fewer than TCAs. GI distress, sexual dysfunction (anorgasmia). "Serotonin syndrome" with any drug that ↑ serotonin (e.g., MAO inhibitors)

274

Toxicity: Thioridazine

Retinal deposits

275

Toxicity: Tricyclic antidepressants

Tri-C's: Convulsions, Coma, Cardiotoxicity (arrhythmias); also respiratory depression, hyperpyrexia. Confusion and hallucinations in elderly due to anticholinergic side effects.

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Tramadol

Mechanism: Very weak opioid agonist; also inhibits serotonin and NE reuptake (works on multiple neurotransmitters - "tram it all" in) Clinical use: Chronic pain Toxicity: Similar to opioids. Decreases seizure threshold

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Trazodone

Primarily inhibits serotonin reuptake. Used for insomnia, as high doses are needed for antidepressant effects. Toxicity: sedation, nausea, priapism, postural hypotension.

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Tricyclic antidepressants: Names

Imipramine, amitriptyline, desipramine, nortriptyline, clomipramine, doxepin, amoxapine (-ipramine, -triptyline, doxepin, amoxapine)

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Zafirlukast, montelukast

block leukotriene receptors. Especially good for aspirin-induced asthma.

280

Zileuton

A 5-lipoxygenase pathway inhibitor. Blocks conversion of arachidonic acid to leukotrienes