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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
Carbapenems mechanism and clinical use
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
26
Amphotericin B mechanism and use
Bind ergosterol --> pores in membrane Systemic mycoses or Intrathecally for fungal meningitis Supplement K+ and Mg2+
27
Nystatin mechanism and use
Bind ergosterol --> pores in membrane | Topical use only: oral candidiasis, diaper rash, vaginal
28
Azoles mechanism and use
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
29
Echinocandins drugs, mechanism, use
-fungin Inhibit cell wall synthesis of B-glucan Invasive aspergillosis, candida - SE GI upset, flushing (histamine)
30
Flucytosine mechanism, use
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
31
Griseofulvin mechanism, use
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
32
Oseltamivir, Zanamivir mechanism, use
Inhibit influenza NEURAMINIDASE --> Decrease release of progeny Use in first 48 hours Treat/prevent Influenza A & B
33
Acyclovir, Famciclovir, Valacyclovir mechanism, use
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)
34
Ganciclovir mechanism, use
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
35
Foscarnet mechanism, use
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
36
CYP450 Inhibitors
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
37
CYP450 Inducers
Decrease warfarin effect --> Clotting risk ``` Carbamezapine Cyclophosphamide Ginseng Griseofulvin Modafinil OCPs Phenobarbital + other barbs Phenytoin Rifampin St. John's wort ```
38
Cholestyramine interaction with warfarin
Binds warfarin in intestine --> reduces uptake
39
High risk of drug-induced lupus
``` Hydralazine Procainamide Isoniazid Minocycline Quinidine ```
40
Sulfonylureas, meglitinides mechanism, class, side effects
Mechanism: Inhibit B-cell K-atp channels, increase insulin secretion "Insulin secretagogues" glyburide, glimipride, glipizide Repaglinite, Metaglinide SE: HYPOGLYCEMIA, weight gain
41
Metformin mechanism, class, side effects
Mechanism: Stimulate AMPK, decrease glucose production, decrease hepatic gluconeogenesis, decrease insulin resistance "Biguanides" SE: lactic acidosis check creatinine before use
42
Pioglitazone mechanism, class, side effects
Mechanism: activate transcription regulator PPAR-y, decrease insulin resistance "Thiazolidinediones" SE: fluid retention, heart failure, weight gain
43
Exenatide, liragluitide mechanism, class, side effects
Mechanism: increase glucose-dependent insulin secretion, decrease glucagon secretion, delay gastric emptying "GLP-1 agonists" SE: Pancreatitis
44
Sitagliptin, saxagliptin mechanism, class, side effects
Mechanism: Increase endogenous GLP-1 and GIP levels "DPP4 inhibitors" SE: nasopharyngitis
45
acarbose, miglitol mechanism, class, side effects
Mechanism: reduce intestinal disaccharide absorption "a-glucosidase inhibitors " SE: diarrhea, flatulence
46
canagliflozin, dapagliflozin mechanism, class, side effects
Mechanism: increase renal glucose excretion "SGLT2 inhibitors" SE: UTI, hypotension
47
Factor Xa inhibitors
Direct: Rivaroxaban, Apixaban Indirect: Fondaparinux
48
Thrombin/IIa inhibitors
Direct: Argatroban, Bivalirudin, Dabigatran Bind to thrombin active site Use to treat HIT
49
Vitamin K antagonists act on...
Factors II, VII, IX, X
50
Weak antiandrogen drug that decreases synthesis of steroid hormones in gonads and adrenals
Ketoconazole
51
Decreases peripheral conversion of testosterone to DHT by inhibiting alpha-reductase
Finasteride
52
Aromatase inhibitor mechanism, example
Decrease peripheral conversion of androgens to estrogen Anastrozole
53
Androgen receptor inhibitor
Flutamide, blocks stimulatory effect of androgens
54
GP IIb/IIIa receptor antagonist
Abciximab | --> Inhibits platelet aggregation
55
Organophosphate poisoning effect and treatment
Organophosphates irreversibly inhibit Atropine (reverses muscarinic only, doesn't reverse paralysis) Pralidoxime (restores cholinesterase, reverses both muscarinic and nicotinic)
56
Isoniazid clinical use, mechanism, side effects
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
Ethambutol clinical use, mechanism, side effects
Tuberculosis Inhibit synthesis of mycobacterial cell wall Optic neuropathy
58
Pyrazinamide clinical use, mechanism of resistance, side effects
Tuberculosis Unknown, Must be activated by mycobacterial enzyme pyrazinamidase Hepatotoxicity, hyperuricemia
59
Rifampin clinical use, mechanism of resistance, side effects
Tuberculosis, but not specific Mutation in DNA polymerase necessary for transcription and RNA prolongation GI side effects, rash, red-orange body fluids
60
Nitroprusside
Vasodilator | Metabolized to nitric acid + cyanide
61
Phenytoin mechanism, side effects
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
Cocaine mechanism, side effects
Blocks re-uptake of NE, 5-HT, and DA in CNS SE: cardiac ischemia, hypertension, seizures
63
How do you treat cyanide toxicity?
Sodium nitrate: promotes methamaglobin formation Sodium thiosulfate: sulfur donor Hydroxocobalamin: cobalt binds cyanide, excreted in urine
64
Lower incidence of torsades-de-pointes than other QT-prolonging drugs
Amiodarone
65
Class I Antiarrhythmic drugs
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
Class II Antiarrhythmic drugs
Beta receptor blockers Atenolol, Metoprolol, Esmolol, Carvedilol Slow sinus node discharge rate Slow AV nodal conduction
67
Class III Antiarrhythmic drugs
Potassium channel blockers Amiodarone, Dronedarone, Dofetilide, Sotalol (also II) Prolong APD/QT interval
68
Class IV Antiarrhythmic drugs
Non-dihydropyridine CCBs Verapamil, Diltiazem Slow sinus node discharge rate Slow AV nodal conduction
69
COX-2 inhibitor
Celecoxib | Acts only at site of inflammation
70
Irreversibly inhibits platelet aggregation by acetylating serine residues
Aspirin
71
Drugs that inhibit both COX1 and COX2
``` Diclofenac Fenoprofen Ibuprofen Indomethacin Ketorolac Piroxicam ```
72
Drugs that may cause aplastic anemia
Carbamazepine, chloramphenicol, sulfonamides
73
Benzodiazepine mechanism of action
Bind allosterically to GABA receptor, increase frequency of chloride channel opening
74
Barbituates mechanism of action
Bind allosterically to GABA receptor, increase the duration of chloride channel opening (or, at high dose, GABA agonist)
75
Buspirone mechanism of action
partial agonist of 5ht1a receptor
76
Antibiotics that act on the 50s subunit
chloramphenicol, clindamycin, linezolid, macrolides
77
Antibiotics that act on the 30s subunit
tetracycline, doxycycline, aminoglycosides
78
Improves survival in CHF
spironolactone, other mineralocorticoid receptor antagonists
79
Alpha-1 agonists
Epinephrine Norepinephrine Phenylephrine Methoxamine
80
Beta-1 agonists
``` Epinephrine Dopamine Dobutamine Isoproterenol Norepinephrine ```
81
Beta-2 agonists
Epinephrine Isoproterenol Terbutaline Ritodrine
82
Epinephrine effect on a1, a2, B1, B2 receptors
Agonist a1, a2, B1, B2
83
Isoproterenol effect on a1, a2, B1, B2 receptors
Agonist at B1, B2
84
Norepinephrine effect on a1, a2, B1, B2 receptors
Agonist at a1, a2, B1
85
Phentolamine effect on a1, a2, B1, B2 receptors
a1, a2 antagonist
86
Propranolol effect on a1, a2, B1, B2 receptors
B1, B2 antagonist
87
Inhibit nucleic synthesis
Fluoroquinolines, rifampin
88
Inhibit folic acid synthesis
Sulfonamides, trimethoprim, pyrimethamine
89
MAO inhibitors example, use
phenelzine, tranylcypromine, selegiline atypical depression, treatment-resistant depression
90
Best anticoagulant to use during pregnancy
Low-Molecular-Weight Heparins (enoxaparin)
91
Loop diuretics - Examples - Mechanism - Location of action - Side Effects
Furosemide, bumetanide, tosemide Thick ascending limb Hypokalemia, hypoMg, hypoCa, OTOTOXICITY
92
Thiazide diuretics - Examples - Mechanism - Location of action - Side effects
Chlorthalidone, Hydrochlorothiazide Enhance Na, Cl, water excretion via inhibition of Na/Cl symporter Distal convoluted tubule Hyperuricemia, Hypercalcemia, HypoK, HypoNa
93
Potassium-sparing diuretics - Examples - Mechanism - Location of action - Side effects
Triamterene, Spironolactone, Amiloride Collecting duct Hyperkalemia Sp: gynecomastia, antiandrogen
94
Carbonic anhydrase inhibitors - Examples - Mechanism - Location of action - Side effects
Acetazolamide Block the resorption of NaHCO3 in Proximal tubule Metabolic acidosis
95
Osmotic diuretics - Examples - Mechanism - Location of action - Side effects
Mannitol Reduce Na/water reabsorption in proximal tubule and Loop of Henle Hypernatremia, pulmonary edema
96
Bind bile acids in the GI tract
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
Low potency typical antipsychotics High potency typical antipsychotics
``` Low = non neuro side effects, High = pyramidal/neuro side effects ``` Chlorpromazine, Thioridizine (Cheating Thieves are low) Trifluroperazine, Fluphenizine, Haloperidol (Try to Fly High)
98
May be used for the acute treatment of delirium with agitation and psychosis
Haloperidol
99
Short acting benzodiazepines
Triazolam, Oxazepam, Midazolam --> sleep or panic
100
Intermediate acting (6-24hr) benzodiazepines
Alprazolam, lorazepam, temazepam - -> sleep - -> lorazepam for withdrawal
101
Long acting benzodiazepines
Diazepam, chlordiazepoxide, flurazepam --> withdrawal
102
Bipolar disorder
Lithium, valproic acid, atypical antipsychotics (olanz, cloz, queti, risper)
103
5-ht specific reuptake inhibitors
SSRIs fluozetine, paroxetine, sertraline, citalopram
104
5-ht and NE reuptake inhibitors
SNRIs venlafaxine, duloxetine
105
Block reuptake of NE and 5-ht
Tricyclic antidepressants amitriptyline, nortriptyline, imipramine, desipramine, clomipramine, doxepin, amoxapine
106
non-selective monoamine oxidase inhibitor that increases levels of amine neurotransmitters NE, 5-ht and DA
phenelzine, selegiline (B), tranylcypromine, isocarboxazid
107
Increase NE and DA through unknown mechanism
Bupropion (atypical) - smoking cessation, anxiety disorder, not panic attacks
108
Blocks 5-ht2 and a1 adrenergic receptors
Trazodone (atypical) - insomnia
109
Treatment for schizophrenia
Atypical antipsychotics (olanz, cloz, queti, risper)
110
Panic disorder
SSRIs, venlafaxine, benzodiazepines
111
Obsessive-compulsive disorder
SSRIs, clomipramine
112
PTSD
SSRIs, venlafaxine
113
Atypical antipsychotics
``` Olanzapine Clozapine Quetiapine Risperidone Aripiprazole Ziprasidone ```

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