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USMLE Step 1 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Selegiline class, mechanism

A

MAO-B inhibitor, MAO-B metabolizes dopamine, slows the breakdown of dopamine

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2
Q

MAO-A inhibitors mechanism

A

preferentially slows the breakdown of norepinephrine and serotonin

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3
Q

Levidopa mechanism

A

dopamine precursor, increases circulating dopamine levels in the striatum
(given in combination with carbidopa, peripheral decarboxylase inhibitor, increases peripheral DA)

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4
Q

Three dopamine receptor agonists

A

bromocriptine
ropinirole
pramipexole

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5
Q

Benztropine and trihexyphenidyl drug class

A

antimuscarinic agents

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6
Q

Common sulfa drugs

A

Sulgonylureas: glyburide
NSAIDs: celecoxib
Diuretics: chlorthalidone, furosemide, bumetanide, (-amide, -ide)
Anticonvulsants: Zonisamide, Topiramate
Others: Bosentan, defetilide, dronedarone

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7
Q

Drug that damages DNA by forming toxic free radical metabolites

A

Metronidazole

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8
Q

Aminopenicillins and spectrum

A

Amoxicillin, ampicillin (penicillinase-sensitive)

H.influenzae
H.pylori
E.coli
Listeria
Proteus
Salmonella
Shigella
enterococci
Triple-therapy for H.pylori
Early stage or young Lyme Disease
coverage in asplenic or dental procedure
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9
Q

Drugs that Interrupt Cell Wall Synthesis

A 
Glycopeptides (peptidoglycan synthesis)
Penicillins + Antipseudomonals
Cephalosporins
Carbapenems
Monobactams
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10
Q

Penicillinase-resistant penicillins + Spectrum

A

Dicloxacillin
Nafcillin
Oxacillin

S.aureus (naf for staph) except MRSA

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11
Q

Drugs that interrupt folic acid synthesis

A

Sulfonamides

Trimethoprim

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12
Q

Antipseudomonals

A

Piperacillin, Ticarcillin

Same mechanism of penicillins with coverage for Pseudomonas and gram negative rods
Add a B-lactamase inhibitor

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13
Q

Drugs that inhibit prokaryotic enzymes topoisomerase II and IV, DNA gyrase

A

Fluoroquinolones (ciprofloxacin, etc)

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14
Q

B-lactamase inhibitors

A

Clavulanic Acid
Sulbactam
Taxobactam

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15
Q

Mechanism of penicillin

A

Bind penicillin-binding proteins (transpeptidases), block transpeptidase cross-linking of peptidoglycan in the cell wall, activate autolytic enzymes

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16
Q

Mechanism of Cephalosporins

A

B-lactam drugs that inhibit cell wall synthesis and peptidoglycan cross-linking

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17
Q

Coverage of penicillin

A

Gram positive organisms (S.pneumo, S.pyo, Actino)
Gram negative cocci (N.menin)
Spirochetes (T.pallidum)

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18
Q

1st generation cephalosporins + spectrum

A

Cefazolin, cephalexin

Gram positive cocci + Proteus, E.coli, Klebsiella

Pre-surgical prophylaxis

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19
Q

2nd generation cephalosporins + spectrum

A

cefoxitin, cefaclor, cefuroxime

1st gen + Haemophilis inf, Enterobacter, Neisseria, Serratia

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20
Q

3rd generation cephalosporins + spectrum

A

ceftriaxone (meningitis, gonorrhea, Lyme)
cefotaxime
ceftazidime (Pseudomonas)

serious gram negative infections resistant to other B-lactams

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21
Q

4th generation cephalosporins + spectrum

A

Cefepime

Pseudomonas

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22
Q

5th generation cephalosporins + spectrum

A

Ceftaroline

broad gram + and gram - including MRSA, not pseudomonas

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23
Q

Resistance to cephalosporins is based on

A

Structural change in penicillin-binding proteins (transpeptidases)

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24
Q

Vancomycin mechanism and clinical use

A

Inhibits cell wall peptidoglycan formation by binding D-ala-D-ala, not susceptible to B-lactamases

Gram positive only

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25
Q

Carbapenems mechanism and clinical use

A

inhibit cell wall synthesis, administer imipenam with cilastatin to decrease renal tubule inactivation

Use in life-threatening infections or after drug failure due to severe side effects: GI distress, skin rash, CNS toxicity/seizures

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26
Q

Amphotericin B mechanism and use

A

Bind ergosterol –> pores in membrane

Systemic mycoses or Intrathecally for fungal meningitis
Supplement K+ and Mg2+

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27
Q

Nystatin mechanism and use

A

Bind ergosterol –> pores in membrane

Topical use only: oral candidiasis, diaper rash, vaginal

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28
Q

Azoles mechanism and use

A

Inhibit fungal ergosterol synthesis via 14-a-demethylase/P450 enzyme

Local/less serious systemic mycoses:

  • chronic suppression of cryptococcal in AIDS
  • chronic suppression candidal infections
  • topical fungal infections
  • SE testosterone inhibition, liver dysfunction
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29
Q

Echinocandins drugs, mechanism, use

A

-fungin

Inhibit cell wall synthesis of B-glucan

Invasive aspergillosis, candida

  • SE GI upset, flushing (histamine)
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30
Q

Flucytosine mechanism, use

A

Inhibit DNA/RNA synthesis by conversion to 5-fluorouracil by cytosine deaminase

Use for systemic infections in combination with amphotericin B

  • SE: bone marrow suppression
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31
Q

Griseofulvin mechanism, use

A

Interferes with microtubule function, disrupts mitosis, deposits in keratin containing tissues (nails)

Oral treatment of superficial infections, inhibits growth of dermatophytes (tinea, ringworm)

  • SE: teratogenic, carcinogenic, confusion, headaches, increased P-450 and warfarin metabolism
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32
Q

Oseltamivir, Zanamivir mechanism, use

A

Inhibit influenza NEURAMINIDASE –>
Decrease release of progeny
Use in first 48 hours

Treat/prevent Influenza A & B

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33
Q

Acyclovir, Famciclovir, Valacyclovir mechanism, use

A

Inhibit viral DNA polymerase by chain termination
(Guanosine analogs monophosphorylated by viral thymidine kinase –> mechanism of resistance)

Use for HSV and VZV, weak EBV
Prophylaxis in immunocompromised, no effect on latent

Valacyclovir = prodrug acyclovir (better oral bioavailbility)

  • SE crystalline nephropathy, acute renal failure
    (prevent with hydration)
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34
Q

Ganciclovir mechanism, use

A

Inhibit viral DNA polymerase by chain termination
(Guanosine analog 5’ monophosphate formed by CMV viral kinase –> mechanism of resistance)

Use for CMV, especially in immunicompromised

Valgancyclovir = prodrug ganciclovir (better oral bioavailability)

  • SE leukopenia, neutropenia, thrombocytopenia, renal toxicity, more toxic to host than acyclovir
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35
Q

Foscarnet mechanism, use

A

Viral DNA/RNA polymerase inhibitor, HIV reverse transcriptase inhibitor, binds to pyrophosphate-binding site or enzyme

Use in CMV retinitis if ganciclovir fails, in acyclovir-resistant HSV

  • SE nephrotoxicity, electrolyte abnormalities can lead to seizures
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36
Q

CYP450 Inhibitors

A

Increase warfarin effect –> increase bleeding

PICK EGS (protease inhib, isoniazid, cimetidine, erythromycin, grapefruit juice, sulfonamides)

Acetaminophen, Azoles, Amiodarone, Cimetidine, Clarithromycin, Cranberry juice, Fluoroquinolones, Fluoxetine, Ginkgo biloba, Grapefruit, Isoniazid, Omeprazole, Ritonavir, Thyroid Hormone

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37
Q

CYP450 Inducers

A

Decrease warfarin effect –> Clotting risk

Carbamezapine
Cyclophosphamide
Ginseng
Griseofulvin
Modafinil
OCPs
Phenobarbital + other barbs
Phenytoin
Rifampin
St. John's wort
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38
Q

Cholestyramine interaction with warfarin

A

Binds warfarin in intestine –> reduces uptake

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39
Q

High risk of drug-induced lupus

A 
Hydralazine
Procainamide
Isoniazid
Minocycline
Quinidine
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40
Q

Sulfonylureas, meglitinides mechanism, class, side effects

A

Mechanism: Inhibit B-cell K-atp channels, increase insulin secretion

“Insulin secretagogues” glyburide, glimipride, glipizide
Repaglinite, Metaglinide

SE: HYPOGLYCEMIA, weight gain

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41
Q

Metformin mechanism, class, side effects

A

Mechanism: Stimulate AMPK, decrease glucose production, decrease hepatic gluconeogenesis, decrease insulin resistance

“Biguanides”

SE: lactic acidosis
check creatinine before use

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42
Q

Pioglitazone mechanism, class, side effects

A

Mechanism: activate transcription regulator PPAR-y, decrease insulin resistance

“Thiazolidinediones”

SE: fluid retention, heart failure, weight gain

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43
Q

Exenatide, liragluitide mechanism, class, side effects

A

Mechanism: increase glucose-dependent insulin secretion, decrease glucagon secretion, delay gastric emptying

“GLP-1 agonists”

SE: Pancreatitis

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44
Q

Sitagliptin, saxagliptin mechanism, class, side effects

A

Mechanism: Increase endogenous GLP-1 and GIP levels

“DPP4 inhibitors”

SE: nasopharyngitis

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45
Q

acarbose, miglitol mechanism, class, side effects

A

Mechanism: reduce intestinal disaccharide absorption

“a-glucosidase inhibitors “

SE: diarrhea, flatulence

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46
Q

canagliflozin, dapagliflozin mechanism, class, side effects

A

Mechanism: increase renal glucose excretion

“SGLT2 inhibitors”

SE: UTI, hypotension

47
Q

Factor Xa inhibitors

A

Direct: Rivaroxaban, Apixaban

Indirect: Fondaparinux

48
Q

Thrombin/IIa inhibitors

A

Direct: Argatroban, Bivalirudin, Dabigatran

Bind to thrombin active site
Use to treat HIT

49
Q

Vitamin K antagonists act on…

A

Factors II, VII, IX, X

50
Q

Weak antiandrogen drug that decreases synthesis of steroid hormones in gonads and adrenals

A

Ketoconazole

51
Q

Decreases peripheral conversion of testosterone to DHT by inhibiting alpha-reductase

A

Finasteride

52
Q

Aromatase inhibitor mechanism, example

A

Decrease peripheral conversion of androgens to estrogen

Anastrozole

53
Q

Androgen receptor inhibitor

A

Flutamide, blocks stimulatory effect of androgens

54
Q

GP IIb/IIIa receptor antagonist

A

Abciximab

–> Inhibits platelet aggregation

55
Q

Organophosphate poisoning effect and treatment

A

Organophosphates irreversibly inhibit

Atropine (reverses muscarinic only, doesn’t reverse paralysis)
Pralidoxime (restores cholinesterase, reverses both muscarinic and nicotinic)

56
Q

Isoniazid clinical use, mechanism, side effects

A

Use as part of treatment for tuberculosis with Ethambutol, Rifampin, Pyrazinamide

Inhibition of mycolic acid synthesis, activation by mycobacterial catalase peroxidase

Neurotoxicity (give B6/pyrox), hepatotoxicity

57
Q

Ethambutol clinical use, mechanism, side effects

A

Tuberculosis

Inhibit synthesis of mycobacterial cell wall

Optic neuropathy

58
Q

Pyrazinamide clinical use, mechanism of resistance, side effects

A

Tuberculosis

Unknown, Must be activated by mycobacterial enzyme pyrazinamidase

Hepatotoxicity, hyperuricemia

59
Q

Rifampin clinical use, mechanism of resistance, side effects

A

Tuberculosis, but not specific

Mutation in DNA polymerase necessary for transcription and RNA prolongation

GI side effects, rash, red-orange body fluids

60
Q

Nitroprusside

A

Vasodilator

Metabolized to nitric acid + cyanide

61
Q

Phenytoin mechanism, side effects

A

Inhibits electrical activity by blocking voltage-gated Na channels

SE: CNS ataxia, nystagmus; gingival hyperplasia, folic acid metabolism interference, P450 inducer, fetal hydantoin syndrome

62
Q

Cocaine mechanism, side effects

A

Blocks re-uptake of NE, 5-HT, and DA in CNS

SE: cardiac ischemia, hypertension, seizures

63
Q

How do you treat cyanide toxicity?

A

Sodium nitrate: promotes methamaglobin formation
Sodium thiosulfate: sulfur donor
Hydroxocobalamin: cobalt binds cyanide, excreted in urine

64
Q

Lower incidence of torsades-de-pointes than other QT-prolonging drugs

A

Amiodarone

65
Q

Class I Antiarrhythmic drugs

A

Sodium channel blockers
Class IA - disopyramide, procainamide, quinidine
–> Prolong APD, slow AP conduction velocity

Class IB - Lidocaine, Mexiletine, Phenytoin
–> Shorten APD

Class IC - Flecainide, Propafenone
–> Slow AP conduction velocity

66
Q

Class II Antiarrhythmic drugs

A

Beta receptor blockers
Atenolol, Metoprolol, Esmolol, Carvedilol

Slow sinus node discharge rate
Slow AV nodal conduction

67
Q

Class III Antiarrhythmic drugs

A

Potassium channel blockers
Amiodarone, Dronedarone, Dofetilide, Sotalol (also II)

Prolong APD/QT interval

68
Q

Class IV Antiarrhythmic drugs

A

Non-dihydropyridine CCBs
Verapamil, Diltiazem

Slow sinus node discharge rate
Slow AV nodal conduction

69
Q

COX-2 inhibitor

A

Celecoxib

Acts only at site of inflammation

70
Q

Irreversibly inhibits platelet aggregation by acetylating serine residues

71
Q

Drugs that inhibit both COX1 and COX2

A 
Diclofenac
Fenoprofen
Ibuprofen
Indomethacin
Ketorolac
Piroxicam
72
Q

Drugs that may cause aplastic anemia

A

Carbamazepine, chloramphenicol, sulfonamides

73
Q

Benzodiazepine mechanism of action

A

Bind allosterically to GABA receptor, increase frequency of chloride channel opening

74
Q

Barbituates mechanism of action

A

Bind allosterically to GABA receptor, increase the duration of chloride channel opening (or, at high dose, GABA agonist)

75
Q

Buspirone mechanism of action

A

partial agonist of 5ht1a receptor

76
Q

Antibiotics that act on the 50s subunit

A

chloramphenicol, clindamycin, linezolid, macrolides

77
Q

Antibiotics that act on the 30s subunit

A

tetracycline, doxycycline, aminoglycosides

78
Q

Improves survival in CHF

A

spironolactone, other mineralocorticoid receptor antagonists

79
Q

Alpha-1 agonists

A

Epinephrine
Norepinephrine
Phenylephrine
Methoxamine

80
Q

Beta-1 agonists

A 
Epinephrine
Dopamine
Dobutamine
Isoproterenol
Norepinephrine
81
Q

Beta-2 agonists

A

Epinephrine
Isoproterenol
Terbutaline
Ritodrine

82
Q

Epinephrine effect on a1, a2, B1, B2 receptors

A

Agonist a1, a2, B1, B2

83
Q

Isoproterenol effect on a1, a2, B1, B2 receptors

A

Agonist at B1, B2

84
Q

Norepinephrine effect on a1, a2, B1, B2 receptors

A

Agonist at a1, a2, B1

85
Q

Phentolamine effect on a1, a2, B1, B2 receptors

A

a1, a2 antagonist

86
Q

Propranolol effect on a1, a2, B1, B2 receptors

A

B1, B2 antagonist

87
Q

Inhibit nucleic synthesis

A

Fluoroquinolines, rifampin

88
Q

Inhibit folic acid synthesis

A

Sulfonamides, trimethoprim, pyrimethamine

89
Q

MAO inhibitors example, use

A

phenelzine, tranylcypromine, selegiline

atypical depression, treatment-resistant depression

90
Q

Best anticoagulant to use during pregnancy

A

Low-Molecular-Weight Heparins (enoxaparin)

91
Q

Loop diuretics

  • Examples
  • Mechanism
  • Location of action
  • Side Effects
A

Furosemide, bumetanide, tosemide

Thick ascending limb

Hypokalemia, hypoMg, hypoCa, OTOTOXICITY

92
Q

Thiazide diuretics

  • Examples
  • Mechanism
  • Location of action
  • Side effects
A

Chlorthalidone, Hydrochlorothiazide

Enhance Na, Cl, water excretion via inhibition of Na/Cl symporter

Distal convoluted tubule

Hyperuricemia, Hypercalcemia, HypoK, HypoNa

93
Q

Potassium-sparing diuretics

  • Examples
  • Mechanism
  • Location of action
  • Side effects
A

Triamterene, Spironolactone, Amiloride

Collecting duct

Hyperkalemia
Sp: gynecomastia, antiandrogen

94
Q

Carbonic anhydrase inhibitors

  • Examples
  • Mechanism
  • Location of action
  • Side effects
A

Acetazolamide

Block the resorption of NaHCO3 in Proximal tubule

Metabolic acidosis

95
Q

Osmotic diuretics

  • Examples
  • Mechanism
  • Location of action
  • Side effects
A

Mannitol

Reduce Na/water reabsorption in proximal tubule and Loop of Henle

Hypernatremia, pulmonary edema

96
Q

Bind bile acids in the GI tract

A

Cholestyramine, Colestipol, Colesevelam

–> divert hepatic cholesterol to synthesize new bile acids, increase uptake of LDL, reduce blood LDL levels

SE: GI upset, impaired absorption of nutrients and drugs, hypertriglyceridemia

97
Q

Low potency typical antipsychotics

High potency typical antipsychotics

A 
Low = non neuro side effects, 
High = pyramidal/neuro side effects

Chlorpromazine, Thioridizine (Cheating Thieves are low)

Trifluroperazine, Fluphenizine, Haloperidol (Try to Fly High)

98
Q

May be used for the acute treatment of delirium with agitation and psychosis

A

Haloperidol

99
Q

Short acting benzodiazepines

A

Triazolam, Oxazepam, Midazolam

–> sleep or panic

100
Q

Intermediate acting (6-24hr) benzodiazepines

A

Alprazolam, lorazepam, temazepam

  • -> sleep
  • -> lorazepam for withdrawal
101
Q

Long acting benzodiazepines

A

Diazepam, chlordiazepoxide, flurazepam

–> withdrawal

102
Q

Bipolar disorder

A

Lithium, valproic acid, atypical antipsychotics (olanz, cloz, queti, risper)

103
Q

5-ht specific reuptake inhibitors

A

SSRIs

fluozetine, paroxetine, sertraline, citalopram

104
Q

5-ht and NE reuptake inhibitors

A

SNRIs

venlafaxine, duloxetine

105
Q

Block reuptake of NE and 5-ht

A

Tricyclic antidepressants

amitriptyline, nortriptyline, imipramine, desipramine, clomipramine, doxepin, amoxapine

106
Q

non-selective monoamine oxidase inhibitor that increases levels of amine neurotransmitters NE, 5-ht and DA

A

phenelzine, selegiline (B), tranylcypromine, isocarboxazid

107
Q

Increase NE and DA through unknown mechanism

A

Bupropion (atypical) - smoking cessation, anxiety disorder, not panic attacks

108
Q

Blocks 5-ht2 and a1 adrenergic receptors

A

Trazodone (atypical) - insomnia

109
Q

Treatment for schizophrenia

A

Atypical antipsychotics (olanz, cloz, queti, risper)

110
Q

Panic disorder

A

SSRIs, venlafaxine, benzodiazepines

111
Q

Obsessive-compulsive disorder

A

SSRIs, clomipramine

112
Q

PTSD

A

SSRIs, venlafaxine

113
Q

Atypical antipsychotics

A 
Olanzapine
Clozapine
Quetiapine
Risperidone
Aripiprazole
Ziprasidone

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