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Flashcards in Pharmacology Deck (288):
1

Statins

- Treats hypercholesterolemia by inhibiting HMG-CoA reductase (inhibition of cholesterol synthesis)
- Leads to increased LDL receptor expression to increase LDL uptake

2

Oseltamvir

-Treats and prevents BOTH influenza A and B
- Impairs virion release by inhibiting NeurAminidase
- Prevents viral penetration of mucous secretions in respiratory epithelium

3

PTU

-Inhibits both organification of iodine (via thyroid peroxidase inhibition) AND peripheral conversion of T4 to T3
(Methimazole: only does inhibition of iodine organification)

4

MTX

Structurally similar to folate → irreversibly inhibits DHFR --> polyglutamated form (cannot move out of cell)

5

Ergonovine

Ergot alkaloid that can provoke coronary vasospasm

6

Bepridil

Ca2+ channel blocker used 2nd line as angina therapy, not used as an anti-hyprtensive

7

Ceftriaxone resistance:

by either beta-lactamases or altered PBP structure

8

Niacin's Mechanism and Side Effects

- Inhibits hepatic VLDL production and triglycerides
- increases HDL
- Acute gout flare is a possible side effect
- Hyperuricemia, hyperglycemia, and flushing
- Flushing can be reduced with Aspirin pretreatment

9

Nitrate Tolerance

Nitrates develop tolerance quickly so much have a nitrate free period every day

10

Mu Receptors

- opioids bind
- increase potassium efflux → hyperpolarization

11

Tx of Gouty Arthritis

NSAID, colchicine, and then glucocorticoids
- Uricosuric agents or Xanthine Oxidase inhibitors contraindicated in acute attacks (can worsen it); but they are good for prophylaxis

12

Antiarrhythmics Na+ Channel Binding Strength

1C > 1A > 1B
- Use dependence more prominent in 1C ( higher rates of depolarization → increased channel blockade because less time in resting state)

13

Reverse Use Dependence

Class III: K+ Channel Blockers

14

Minimal alveolar concentration (MAC):

% of anesthetic in inspired gas mixture that renders half of patients unresponsive to painful stimuli
- Lower the MAC, the higher the potency
- If anesthetics have a high blood/gas coefficient (meaning they dissolve more in blood), they will have a slower onset of action

15

ABPA

Asthma with aspergillus; high eosinophilia

16

Physostigmine

Cholinesterase inhibitor (Ach builds up); similar to edrophonium
- Both peripherally and centrally

17

Pilocarpine

Cholinergic Agonist

18

Phentolamine and Phenoxybenzamine

a-adrenergic antagonist
- Phentolamine has a half life of 20 min (irreversible)
- Phenoxybenzamine has a half life of 24 hours and is often used to treat pheochromocytoma (reversible)

19

Phenylephrine

a-adrenergic agonist

20

Amiodarone

Delayed onset interstitial pneumonitis + a lot of other side effects

21

Mifepristone

Inhibits progesterone receptors (induce abortion)
- Used with Misoprostol: PGE1 analog

22

Aspirin

Inhibition of COX pathways → promotes formation of leukotrienes that cause bronchoconstriction

23

Alpha 1, 2, beta 1 ,2 m 1-3. D1-2, H1-2, Vasopressin 1-2

QISS QIQ SIQ SQS
- Q: phospholipase C → DAG, IP3
- S: stimulate Adenylate cyclase → cAMP increase
- I: inhibit Adenylate cyclase → cAMP decrease

24

Red Man Syndrome

- Rapid infusion of vanco → red man syndrome due to widespread release of histamine (NOT IgE mediated allergic reaction)
- Can be prevented with a slower rate of infusion

25

Michaelis Menten

Y intercept - Vmax (up means decrease)
- Vmax is directly proportional to concentration
X intercept – Km (closer to Y line → Km increases → lesser affinity)

26

COX1

- In platelets prevents thromboxane formation (preventing platelet aggregation)
- Also does gastric protection
(Problem with NSAIDs)
- Selective COX 2 inhibitors (celecoxib) are good for pain (no effect on gastric mucosa)

27

Tx for MRSA

Ceftaroline (5)
- Vancomycin
- Daptomycin
- Linezolid
- Tigecycline

28

Pseudomonas Tx:

- Ceftazidime (3) and Cefepime (4)
- Ticarcillin or piperacillin (w/ clavulanate, tazobactam or sulbactam)

29

Cephalosporin Generations:

1: faz, phal
2: fox, fac, fur
3: tri, trax, tax
4: cefepime
5: ceftaroline

30

B-lactam that can be used in PCN Allergies

Aztreonam

31

Gram (-) Rod Tx:

aztreonam, cephalosporins (3), aminoglycosides

32

Gm (+):

vanco

33

Always give carbapenems:

cilastatin (it inhibits renal tubular secretion of the antibiotic)
eg. similar to giving penicillin w/ probenecid

34

Aminoglycosides

30s, misread mRNA (inhibiting initiation complex formation)
eg. gentamicin, amikacin, tobramicin

35

Tetracyclines

30s, block tRNA binding site
- For intracellular (rickettsia, mycoplasma, borrelia, chlamydia) (eg. Doxycycline)
eg. tetracyline, doxycycline, minocycline
- binds inorganic compounds (in bone and teeth) causing teeth discoloration and retarded bone formation

36

Linezolid

50s, blocks 70s formation

37

Chloramphenicol

50s, blocks peptidyl transferase

38

Macrolides

50S, blocks translocation (binds the 23S part of 50s)
Atypical pneumonia, STDs, Gm + cocci
eg. clarithromycin, erythromycin, azithromycin

39

Clindamycin

50S, blocks translocation (binds the 23S part of 50S)
- Anaerobes, GAS
- Causes C. Diff

40

Fluoroquinolines

(floxacins) inhibit DNA gyrase
- Atypical pneumonias, Gm – rods

41

Metronidazole

Makes free radicals to break DNA
- D. diff, gardnerella, giardia, anaerobes

42

Isoniazid

Decreased mycolic acid synthesis (must be activated with catalase peroxidase)
- 2 Mechanism of resistance:
decreased expression of catalase peroxidase or modification of protein target binding site
- may cause pyridoxine deficiency; acetylated for excretion (slow acetylators have increased risk of toxicity)
- Also is directly hepatotoxic in 10-20%

43

Rifampin

Inhibits DNA dep RNA pol
- Prophylaxis for meningococcal and Hib

44

Ethambutol

Inhibits mycobacterial cell wall synthesis by blocking arabinosyl transferase (inhibits carbohydrate polymerization
- central scotomas

45

Amphotericin B and Nystatin

Binds ergosterol and makes pores
Nystatin: topical because too toxic

46

Griseofulvin

Binds microtubules and inhibits mitosis (antifungal)
Also induces P450

47

Terbinafine

Inhibits fungal squalene epoxidase

48

Caspofungin

Inhibits cell wall synthesis (by inhibits b-glucan)

49

Inhaled gas anesthetics

- Poorly Soluble gas: saturates quickly, so partial pressure starts to rise, rapid equilibration with
- Highly soluble gas: saturates more slowly so need more to saturate, slower rise in partial pressure so lower onset and equilibration

50

Lipophilic Drugs

- Highly lipophilic drugs are preferentially metabolized by liver (poorly eliminated by kidney)

51

Milrinone

PDE3 inhibitor → increases cardiac contractility

52

Opioids: Tolerance Does Not Develop for _______

Miosis and constipation

53

Nitroglycerin has greatest effect on:

Large veins

54

Statin Metabolism

Metabolized by P450 (except pravastatin), inhibitors will increase concentration → more rhabdomyolysis → acute renal failure

55

CYP450 Inhibitors

Cimetidine
Ciprofloxacin
Erythromycin
Azoles
Grapefruit juice
Isoniazid
Ritonavir

56

Permissive

Something with no effect, will increase the effect of something else

57

Additive

When combined effect of drugs together is equal to the sum of their individual effects

58

Synergistic

Combined effect exceed the effect of the sum of both effects

59

Bile Acid Binding Resins (eg. Cholestyramine) Side Effect

- Cholesterol Gallstones (prevent absorption, so liver makes more cholesterol)
- Mild increase in triglycerides

60

Tx to Decrease Triglycerides

Fibrates (1st line) and Niacin

61

Clonidine

a2 agonist
- decreases peripheral vascular resistance

62

MTX vs 5FU

- MTX prevents reduction of TH4 while 5FU binds TH4 and thymidylate synthase in a stable intermediate form which decreases the amount of thymidylate synthase available
- 5FU cannot be overcome with addition of folinic acid or leucovorin

63

Beta Blockers Effect on AV Conduction

Slow AV conduction which prolongs the PR interval

64

Niacin Induced Flushing Due to:

Prostaglandins

65

Vancomycin Induced Flushing Due to:

Histamine (can be limited with slow infusion and anti-histamine treatmeant ahead of time)

66

Weight Loss Drugs

- dexfenfuramine, phenteramine, fenfluramine
- can cause cor pulmonale

67

Tx for Methanol or Antifreeze (ethylene glycol) Poisoning

Fomepizole (alcohol dehydrogenase inhibitor)

68

Tx for Arsenic, Lead, Mercury & Gold Poisoning

Dimercaprol
- EDTA can also be used for lead

69

Demeclocycline

- Tetracycline antibiotic that can be used to treat SIADH

70

Conivaptan or Tolvaptan

ADH Receptor Antagonists used to treat SIADH

71

Raltegravir

Integrase inhibitor that prevents HIV from integrating into chromosome of Host so host cell machinery cannot be used to make HIV mRNA

72

Entacapone and Tolcapone

- COMT inhibitor that increases bioavailability of levodopa by decreasing peripheral methylation
- Tolcapone inhibits BOTH peripheral and central methylation

73

SGTP2 inhibitors (eg. Canaglifozin)

- Lose glucose in urine due to osmotic diuresis
- Need to check renal status before using
- Can cause yeast infection

74

DPP4 inhibitors

prevent degradation of GLP to prolong its action in increasing insulin
(–gliptins)

75

GLP1 Analogs

Exenatide or Liraglutide

76

Ketoconazole

Inhibits testosterone synthesis pathways

77

Adrenergic, Muscarinic, Dopaminergic, Histamine, Vasopressin

QISS QIQ SIQ SQS
Q: GPCR
S: increase cAMP
I: decrease cAMP

78

CYP450 Inducers

Phenytoin, Phenobarbital, Rifampin, Carbamazepine, Griseofulvin

79

DRESS syndrome

Adverse drug reaction w/ eosinophilia

80

Low Volume of Distribution If:

Trapped in plasma
- Due to high MW, high plasma protein binding, hydrophilicity and high charge

81

High Volume of Distribution If:

Lipophilic, unbound, low charge, low MW can cross membranes more easily and access intracellular compartment → very large Vd

82

HAART

NNRTI: DEN (efavirenz)
Protease inhibitors: -navir
Integrase inhibitors: -tegra-
NRTI: everything else

83

Inhibitors of dihydrofolate reductase

Trimethoprim, methotrexate, and pyrimethamine

84

Pavilizumab

For RSV prevention: Ab to F (fusion) protein

85

Zidovudine

NRTI used to treat HIV: causes bone marrow suppression especially with gancyclovir
- Competitively binds reverse transcriptase and is incorporated as thymidine analog and since it does not have a 3OH group, cannot make 3-5' phosphodiester bond

86

Protease inhibitors: side effects

hyperglycemia, lipodystrophy, and p450 inhibition

87

NNRTI

Do not require phosphorylation
- MC ones include: Nevirapine, Efavirenz, and Delaviridine

88

TNF-a Inhibitors

may reactivate latent TB by decreasing macrophage function (maintain granulomas)
- Cord Factor (virulence) in Mycobacteria inhibits macrophage activation and TNFa release

89

TNF-a is the main mediator of:

- Paraneoplastic cachexia (wasting syndrome)
- Sepsis (also IL-6 and IL-1 are part of the response)

90

Alemtuzumab

CD52 inhibitor used for CLL

91

Cetuximab

EGFR antibody for colorectal and head/neck cancers

92

Natalizumab

Ab to a4-integrin for MS and Crohns
- Risk of PML from JC virus

93

Azathioprine/6-MP degraded by:

xanthine oxidase (which is inhibited by allopurinol) and TPMT in liver

94

ACE Inhibitors

Angioedema side effect (c1 inhibitor deficiency)
- ACE made in lung endothelium
- Don’t use in patients with bilateral renal artery stenosis → ARF (acute renal failure) because they are dependent on ACE for renal blood flow (can no longer constrict efferent arteriole to maintain GFR)

95

IFN's

IFNa- hepC
IFNb- MS
IFNy- for CGD

96

Ribavirin

HepC and RSV
- Inhibits RNA poly and IMP dehydrogenase → interferes with duplication of viral genome

97

Isoniazid

Must be activated by catalase peroxidase enzyme
- Inhibits mycolic acid synthesis (TB no longer is acid fast)
- Metabolized by acetylation → excreted in urine

98

Pyrazinamide

works best in an acidic environment to kill intracellular organisms like TB

99

Ondansetron and Metoclopramide work on:

floor of 4th ventricle
Ondensetron is a 5HT3 antagonist
Metoclopramide is a dopamine receptor antagonist (don't use in parkinson's patients)

100

Thiopental

Short acting anesthetic barbiturate
- After equilibrating in brain (takes about 1 min) it redistributes quickly to skeletal muscle and fat (resulting in rapid recovery from anesthesia)

101

Acetazolamide

Carbonic anhydrase inhibitor
- Can be used to treat narrow-angle glaucoma
- Works in proximal tubule of nephron
- Can cause metabolic acidosis by blocking NaHCO3 reabsorption

102

Succinylcholine (Neuromuscular Blockade)

May cause hyperkalemia (peak T waves)
- Burn pts more at risk because of leaking/damaged cells
- Strong Ach receptor agonist --> sustained depolarization (prevents muscle contraction)
- Antidote only for Phase II: ACHE inhibitors (eg. neostigmine)
- May cause malignant hyperthermia

103

Beta Blockers w/ Diabetics and Asthma/COPD

Diabetics w/ HTN → it can mask hypoglycemia
- Use an ACE inhibitor instead (prevents diabetic nephropathy)
- Can also exacerbate asthma and COPD

104

Essential Tremor Tx

Non-selective Beta Blocker or Primidone

105

Benadryl and Dramamine

- Diphenhydramine = Benadryl
- Dimenhydrinate = Dramamine

106

2nd Generation (histamine) H1-receptor blockers

Less side effects because does not cross BBB
- Loratidine, desloratidine, fexofenadine, cetirizine

107

Tx for UTI in Children

amoxicillin (w/ or w/out clavulanate), cefixime, ceftriaxone, cephalexin, nitrofurantoin, or sulfamethoxazole/trimethoprim

108

_________ are less effective when taken with Antacids

Fluoroquinolones (DNA gyrase inhibitors)

109

PCN allergy cross-allergenicity w/:

Cephalosporins

110

Chloramphenicol: Side effect

Can cause pancytopenia

111

Daptomycin

- Aw/ increased CPK and incidence of myopathy
- For gram + only
- Makes pores

112

Half-Life

t1/2 = (.7*Vd)/Cl

113

Treat Carcinoid Syndrome w/

Octreotide

114

Drug Efficacy

maximum effect of a drug (regardless of dose)

115

Competitive Antagonist

Changes ED50 (effective dose/potency): shift right
- Need a higher dose to overcome antagonist

116

Noncompetitive OR Irreversible competitive antagonist

Changes Emax (max effect/efficacy): shift down
- Increasing the dose will not help

117

Partial Agonist

Decreases max effect; variable potency

118

Tacrolimus

prevents Transcription of IL2; FKBP; Calcineurin inhibitor
- causes hyperglycemia

119

Sirolimus

prevents Signal transduction of IL2; MTOR

120

Cyclosporine

prevents Transcription of IL2: Calcineurin inhibitor
- nephrotoxic

121

Cimetidine: P450 effect

can decrease P450 metabolism of warfarin → easy bruising and bleeding

122

Anticholinergic Side Effects

hot as a hare, dry as a bone, blind as a bat, red as a beet, mad as a hatter

123

Rasburicase

effective in preventing and treating hyperuricemia and its renal manifestations from tumor lysis syndrome (it is similar to allopurinol)

124

Aminoglycosides must be administered _________

Parenterally

125

Anesthetics that block Na Channels

- Amide types have 2 I’s in the name
- Ester types have only one i
- Important to remember if a patient has an allergy to one type, can use the other type because there is no cross reaction
- Inhaled anesthetics (esp halothane) → hepatotoxicity (necrosis/shunken)

126

Foscarnet

- pyrophosphate analog that does NOT require activation
- Inhibits RNA pol (in herpesvirus) and reverse transcriptase (in HIV)
- for CMV
- Side effects: Hypocalcemia, hypomagnesia

127

Cidofovir

- does not require phosphorylation
- for CMV

128

Amphotericin B: can cause arrhythmias due to:

hypokalemia and hypomagnesia

129

Metformin contraindicated in:

renal failure

130

Heparin for DVT in

Pregnant (warfarin is normally drug of choice for DVT)

131

Carbamazepine:

- Blocks voltage gated Na+ channels
- Trigeminal neuralgia (triggered by eating or brushing teeth)
- Carbamazepine may cause blood dyscrasias (agranulocytosis or aplastic anemia), hepatotoxicity, and SIADH
- First line for Partial Seizures and General Tonic-Clonic

132

Rifampin as Monotherapy

- rarely used alone
- Can be used as monotherapy for meningococcal exposure
- Prophylaxis for close contacts of pts with meningitis
- AMPlifies CYP450 and increases metabolism of Warfarin and Phenytoin

133

Prevent Methotrexate Toxicity w/

Folinic Acid Supplementation

134

Vincristine: Side Effect

Peripheral Neuropathy

135

Warfarin Metabolism Increased w/

antiepileptics, rifampin and griseofulvin

136

Highest risk of drug-induced SLE

Hydralazine and procainamide

137

Thiazide: Side effects

Hypercalcemia, Hyperlipidemia/hypercholesterolemia, decreased insulin release (Hyperglycemia)

138

Tx of Coagulase (-)

Usually methicillin resistant so use Vancomycin

139

Primidone

For benign essential tremors (and also tourettes)
- Active metabolite is phenobarbital and phenylethylmalonomide
- So can be useful as a narrow spectrum anticonvulsant
- Beta blockers used as first line for essential tremor but not in pts with asthma

140

Statins used with Fibrates

- Risk of myopathy with Statins increases when combined with Fibrates (eg Gemfibrozil or fenofibrate)
- Simvastatin has highest risk of myopathy
- Statins also have a risk of hepatotoxicity

141

Cocaine

-Inhibits reuptake of NE, DA, and serotonin by NET
- Indirect sympathomimetic

142

Atropine Reversal

- Physostigmine which inhibits AchE both peripherally and centrally (due to its tertiary amine structure)
- Neostigmine and Edrophonium are also AchE inhibitors but only peripherally (they don’t cross BBB due to their quaternary amine structure)

143

Fluorinated Inhaled Anesthetics Effects

- increases cerebral blood flow but tend to depress everything else
- Can increase ICP

144

Understimulation of alpha1 receptors

lightheadedness and syncope with standing

145

Extended use of appetite suppressents

phentermine or fenfluramine are aw/ increased incidence of pulmonary hypertension → RV hypertrophy + cor pulmonale→ sudden cardiac death

146

TCAs

- inhibit reuptake of serotonin and NE
- MC cause of death is refractory hypotension and arrhythmias due to inhibition of fast Na+ channels
- can have antimuscarinic/anticholinergic effects (amytriptyline)
- may also have alpha adrenergic antagonist effects

147

Triptans

5HT1B and 5HT1D agonists (used for terminating migraines)
- induce vasoconstriction
- prevents CGRP release (vasoactive peptide)
- Don't used with CAD or prinzmetal angina

148

Loading Dose

(target concentration * Vd)/ bioavailability

149

Maintenance Dose

(target concentration * CL * interval of dosing)/bioavailability

150

Bioavailability

area under oral curve/ area under IV curve

151

Zero-order

- fixed amount eliminated
- PEA: phenytoin, ethanol. Aspirin

152

First-order

- fixed proportion eliminated (fraction so exponential)

153

To eliminate salicylates (aspirin):

alkalinize urine w/ bicarb

154

To eliminate amphetamines:

acidify urine w/ ammonium chloride

155

Elderly Lose Phase ______ of Drug Metabolism First

Phase 1 metabolism of drugs first (CYP450)

156

Mirtazipine

alpha2 autoreceptor antagonist (atypical antidepressant)

157

Meperidine

opioid

158

Tx Glaucoma

Cholinergic promoters better

159

ACHE inhibitors

-stigmines, donepezil, galantamine, and edrophonium ( side effects of cholinergics)
- Only physostigmine crosses CNS

160

Ipratropium and Tiotropium

antimuscarinics used for asthma and COPD

161

Oxybutynin and Darefenacin

antimuscarinics used for urge incontinence

162

Scopolamine

antimuscarinic for motion sickness

163

Glycopyrrolate

antimuscarinic for preop use to decrease airway secretions, drooling, and peptic ulcer

164

Tropicamide and Atropine

Antimuscarinics used for dilation and cycloplegia
- Atropine used for bradycardia

165

Dopamine

D1 and D2 receptors > Beta > alpha receptors

166

Dobutamine

B1 > B2, alpha (cardiac stress test)

167

Never give beta blockers to:

cocaine users (because unopposed a1 activation → severe hypertension)

168

Clonidine

- Alpha2 agonist for hypertensive emergency
- Also ethanol and opioid withdrawal
- DO NOT confuse with clomiphene (estrogen feed back inhibitor antagonist)

169

Theophylline

Bronchodilates by inhibiting PDE to increase cAMP (blocks actions of adenosine)
- Low therapeutic index (cardio and neurotoxic): seizures, arrhythmia, vomiting, abdominal pain

170

Tx for isolated systolic HTN

DHR Ca2+ Channel blockers (-dipines) or thiazides

171

Denosumab

RANKL antibody, prevents osteoclast action

172

Benzo w/ Short Half-life used for Insomnia

Triazolam

173

Amifostine

Use with platinum containing chemo agents (cisplatin) to prevent nephrotoxicity

174

Dexrazoxane

Iron chelator used with doxorubicin to prevent cardiotoxicity

175

Mesna

Used with cyclophosphamide to prevent hemorrhagic cystitis

176

Leucovorin

Used to treat methotrexate overdose

177

MRSA is resistant to:

ALL beta-lactam drugs including ones that are b-lactamase resistant (nafcillin) because it has an altered PBP

178

Nimodipine

Ca2+ Channel Blocker that ise used to prevent cerebral vasospasm following a subarachnoid hemorrhage

179

Theophylline Toxicity

Seizures and Tachyarrhythmias

180

gp41 inhibitor

enfurvitide (inhibits entry)

181

gp120 inhibitor

maraviroc (inhibits attachment)

182

Sulfahydryl group donor used to treat ________

Acetaminophen overdose

183

_______ to HIV+ Pregnant woman

Zidovudine

184

First Dose Effect w/ ACE inhibitors

First-dose hypotension
- predisposing factors: hyponatremia, hypovolemia due to diuretic use, renal impairment, heart failure, low BP, high renin or aldosterone

185

Drug Characteristics if Vd is plasma (3-5L)

high MW, high protein binding, high charge, hydrophilic

186

Piperacillin + Tazobactam is effective against:

Most Gm (-) enteric rods, including pseudomonas and Bacteroides

187

Cidofovir and Tenofovir

Nucleotides only need cellular kinase to be activated (not viral kinase)

188

T1/2=

(.693*Vd)/ CL

189

Ethosuximide

- blocks T-type Ca2+ channels
- Used for absence seizures

190

Opioids (8)

Morphine, fentanyl, codeine, loperamide, methadone, meperidine, dextromethorphan, diphenoxylate

191

Butorphanol

Partial agonist at Mu and agonist at kappa
- analgesia for severe pain (less respiratory depression)
- Can cause withdrawal symptoms if taken with a full opioid agonist and overdose is not easily reversed

192

Tramadol

Very weak opioid agonist
- also inhibits serotonin and NE reuptake
- decreases seizure threshold, risk of Serotonin Syndrome

193

Phenytoin vs Valproic Acid Uses

Phenytoin: all seizures + status epilepticus except absence
Valproic acid: all seizures except status epilepticus

194

Phenytoin Side effects

Nystagmus, gingival hyperplasia, hirsutism, megaloblastic anemia, fetal hydantoin (teratogen), SLE-like syndrome, p450 induction, SJS
- Zero-order Kinetics (use dependent)

195

Tx for Postherpetic neuralgia and peripheral neuropathy

Gabapentin (GABA analog that inhibits voltage gated Ca channels)

196

Barbiturates (Phenobarbital, pentobarbital, secobarbital, Thiopental)

Increased GABA duration of Cl- opening
-contraindicated in porphyria

197

Benzodiazepines (Zolam or Zepam)

Increased GABA frequency of Cl- opening
- Short acting: triazolam, oxazepam, alprazolam, and midazolam (more likely to fall but less withdrawal)
- increased risk of falls with hangover effect

198

Short acting benzodiazepines

Triazolam
Oxazepam
Alprazolam
Midazolam

199

Nonbenzo Hypnotics

Zolpidem, Zaleplon, Eszepiclone
Act on BZ1 subtype receptor
- less dependence risk

200

Less soluble in blood -->

rapid induction and recovery

201

Inhaled Anesthetics (Halothane, -Fluranes, and NO)

Respiratory and cardiac depression, increase cerebral blood flow
- halothane has hepatotoxicity, methoxyflurane has nephrotoxicity, enflurane is proconvulsant
- Risk of malignant hyperthermia (tx w/ dantrolene)

202

IV Anesthetics

Barbiturates
Benzodiazepines
Ketamine
Opioids
Propafol

203

IV Anesthetic: Barbiturate

Thiopental: very potent and lipid soluble
- induction of anesthesia and short procedures
- rapid redistribution into tissue and fat
- decreased cerebral blood flow

204

IV Anesthetic: Benzodiazepine

Midazolam: MC used for endoscopy
- used w/ gaseous anesthetics and narcotics
- May have severe post-op respiratory depression, low BP, and anterograde amnesia

205

IV Anesthetic: Ketamine

PCP analog (dissociative anesthetic)
- Blocks NMDA receptors (decreases morphine tolerance by blocking glutamate)
- Cardio stimulant
- Causes disorientation, hallucination, and bad dreams

206

IV Anesthetic: Opioid

Morphine and fentanyl (used w/ other depressants)

207

IV Anesthetic: Propofol

Used for sedation in ICU, rapid induction, short procedures
- Less post-op nausea than thiopental
- Potentiates GABAa

208

Local Anesthetics: Esters and Amides

Esters: -Caines; Amides: Caines but w/ 2 I's
- Block Na channels (prefer activated)
- Vasoconstrictors will enhance local action
- Nerve blockade: small > large; myelin> unmyelin (size factor predominates)
- Order of Loss: pain, temp, touch, pressure

209

Bupivicaine Side Effect

Severe Cardio toxicity

210

Local Anesthetics: Infected Tissue

Need more anesthetic in infected (acidic) tissue because alkaline anesthetics can't penetrate

211

Nondepolarizing Muscular Blockade: -curium and -uronium

- competitive antagonists w/ Ach
- Reverse with neostigmine (give w/atropine to prevent bradycardia), edrophonium, and other ACHE inhibitors

212

Dantrolene

Prevents release of Ca2+ from SR
- Tx for malignant hyperthermia and neuroleptic malignant syndrome

213

VMAT inhibitors

Tetrabenzine and Reserpine
- used for Huntingtons

214

D2 agonists for Parkinsons

Pramipexole and Ropinerole (non-ergots preferred) and Bromocriptine (ergot)

215

Amantadine

Antiviral that increases dopamine and can be used for Parkinsons

216

Selegiline

Selective MAO-B inhibitor for Parkinsons

217

Alzheimer's Drugs

Memantine: NMDA antagonist
Donepezil, galantamine, rivastigmine: ACHE inhibitors

218

Benztropine

Antimuscarinic that helps with Parkinsons by curbing excess cholinergic activity
- Use for drug induced Parkinsons

219

Tx of Alcohol Withdrawal

Diazepam, Chlordiazepoxide, Disulfiram

220

Antidepressants: Risk of Inducing _______

Mania (in susceptible patients)

221

Venlafaxine

Serotonin and NE reuptake inhibitor used for PTSD

222

Pentazocine

Opioid narcotic w/ partial agonist activity and weak antagonist activity at mu receptors
- can cause withdrawal symptoms in patients dependent or tolerant to morphine/opioids

223

Alpha2 vs Beta2: insulin

A2 inhibits insulin
B2 released insulin

224

Gancyclovir: adverse effect

Neutropenia (granulocytopenia)
- incidence is increased with co-administration of zidovudine

225

3 types of signal pathways

cAMP, IP3, and ion channels

226

Nicotinic Receptors

Ligand gates ion channels that open after binding Ach
- opening results in immediate influx of Na and Ca in and K out

227

Maternal to neonate HIV - prophylaxis

Zidovudone starting at 14 weeks to birth and postpartum to infant for 6 more weeks
reduced risk of transmission by 2/3s

228

DRESS Syndrome

Drug reaction 2-8 weeks after exposure
- common w/ anticonvulsants, allopurinol, sulfonamides, and antibiotics
- fever, general lymphadenopahy, facial edema, and diffuse morbilliform skin rash
- Eosinophili and atypical lymphocytosis

229

Crossing of Placenta

Water soluble materials DO NOT readily cross placenta (heparin)
Lipophilic materials easily cross (warfarin)

230

Tx for CMV Retinitis

Gancyclovir
Foscarnet
Cidofavir

231

Aciretin

synthetic retinoid used systemically to treat psoriasis
- strongly teratogenic
- retinoid medication function by binding nuclear receptors which subsequently function as transcription factors

232

Aminoglycosides used w/ Beta-lactams

Increased efficacy of aminoglycoside because beta lactam disrupts the bacterial cell wall and allows it to penetrate the bacteria and inhibit the 30S subunit

233

Orlistat

Weight loss agent for obesity
- inhibits intestinal lipase inhibiting fat absorption in gut

234

Tx for Bullous Pemphigoid

Tetracyclines

235

ACE inhibitor fetopathy (AIF)

Blockade of angiotensin II which is needed for normal renal development
- anuria, oligohydramnios (Potters), pulmonary hypoplasia, and calvarium defects

236

Paclitaxel in a Drug Eluting Coronary Artery Stent

Functions to decrease stent thrombosis by:
inhibiting intimal hyperplasia
- binds b-tubulin and prevent microtubule break down leading to cell cycle arrest and inhibition of cell division

237

Clopidogrel w/ Omeprazole

Clopidogrel is an inactive prodrug and requires activation by CYP2C19
Omeprazole inhibits CYP2C19 causing decreased efficacy of clopidogrel

238

Nandrolone

Anabolic steroid
- may be used in competitive atheletes

239

Jimson Weed

Mydriasis (gardener's pupil)
Anticholinergic

240

Itraconazole

Azoles: Inhibit ergosterol synthesis by inhibiting p450

241

Fenoldopam

Used to tx Hypertensive Crisis
- Selective D1 receptor agonist
- arteriolar dilation and natriuresis (improved renal perfusion)

242

Hypertensive Emergency: Tx with ________ or _________

Fenoldopam or Nitroprusside

243

HIV Prophylaxis: Pneumocystis jirovecii and Toxoplasma Gondii

Trimethoprim-sulfamethoxazole

244

HIV Prophylaxis: MAC complex

Azithromycin

245

Norepinephrine vs Epinephrine

E: Beta more than alpha
NE: Alpha more than beta

246

Methotrexate Side Effects

Stomatitis (painful mouth ulcer), hepatotoxicity, and myelosuppression

247

Mexiletine

Class IB Antiarrhythmic

248

Propafenone

Class IC Antiarrhythmic

249

Ibutilide or Dofetilide

Class III Antiarrhythmic

250

Flecainide

Class IC Antiarrhythmic

251

Gingival Hyperplasia is a side effect of:

Phenytoin

252

Opioids and Biliary Colic

Opioid action on Mu can cause contraction of smooth muscle cells in Sphincter of oddi causing constriction and spasm --> biliary colic due to increased pressure in bile duct and gall bladder

253

PPI: Osteoporosis

Long term acid suppression w/ proton pump inhibitors --> increased risk of osteoporotic hip fractures

254

Aspirins effect on Colon Adenocarcinoma

Increased activity of COX2 is linked to some forms of colon adenocarcinoma
- aspirin use may decrease adenomatous polyp formation

255

Cilostazol

PDE inhibitor (direct vasodilator) and inhibits platelet aggregation
- used in patients w/ intermittent claudication

256

Txt for Enterococci

Vanco/amplicillin + aminoglycoside

257

Tx for Wegeners

Cyclophosphamide and Corticosteroids

258

Her2neu breast cancer

Trastuzumab

259

ER breast cancer

Tamoxifen

260

Tx for Legionella

Macrolide or Fluoroquinolone

261

Tx for Sporothrix Schenkii

Oral Potassium iodide

262

Tx for Nephrogenic DI

Amiloride, hydrochlorothiazide, indomethacin

263

Tx H Pylori

PPI + clarithromycin + amoxicillin or metronidazole

264

Tx for Ricketsia

Doxycycline
- also Chloramphenicol

265

Tx for Chlamydia

Azithro or Doxycycline

266

Tx for Lyme

Ceftriaxone or Doxycycline

267

Tetracycline absorption inhibited by:

Milk (Ca2+), antacids (Ca+ or Mg+), or iron containing preparations

268

Tx Atypical Pneumonias w/

Macrolides or FQs

269

Binds 23 rRNA

Macrolides
- inhibit translocation

270

Tx for Anaerobes ABOVE diaphragm

Clindamycin

271

Tx for Anaerobes BELOW diaphragm

Metronidazole

272

Sulfonamides

Inhibit folate synthesis by inhibition of dihydropteroate synthase
- hypersensitivity, hemolysis in G6PD, nephrotoxic, photosensitive, kernicterus in infants, and displaces drugs from albumin

273

Aw/ tendon rupture and arthropathy in children

Fluoroquinolones

274

Mechanism of Metronidazole

free radicals that damage DNA

275

Drug induced lupus

Isoniazid, procainamide, and hydralazine

276

Prophylaxis of Strep Pharyngitis in child w/ prior Rheumatic Fever and Prophylaxis for Endocarditis prior to dental work

Penicililn

277

Prevention of postsurgical infection w/ S. Aureus

Cefazolin

278

Prevention of gonococcal or chlamydial conjunctivitis in a newborn

Erythromycin Ointment

279

Tx for VRE (Vanco Resistant)

Linezolid or Streptogranins (-pristin)

280

Lanosterol Synthesis inhibitor

Terbinafine (inhibits squalene epoxidase)

281

Ergosterol Synthesis inhibitor

- Conazoles
by inhibiting p450

282

Fungal Cell Wall Synthesis Inhibitor

Caspofungin
- inhibition of b glucan

283

Fungus Membrane Pore Formation

Amphotericin B (systemic) and Nystatin (swish and swallow)

284

5FU (flucytosine)

May be used for systemic fungal infections
inhibits DNA and RNA synthesis
- bone marrow suppression

285

Mechanism of Chloroquine

Prevents detox of heme into hemozoin (heme accumulates --> toxic)

286

IFN alpha used for: (6)

Hep B and C, Kaposi, Condyloma accuminatum, Hairy cell, RCC, melanoma

287

Basiliximab

Monoclonal Ab that blocks IL2R

288

In decompensated CHF, do not use:

Beta blockers
(can be used in compensated)