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USMLE Step 1 > Microbiology - Pharmacology > Flashcards

Microbiology - Pharmacology Flashcards

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1
Q

How do penicillin drugs work?

A

Binds to penicillin-binding proteins (transpeptidases) and blocks cross-linking of peptidoglycan

Can be inactivated by penicillinase/β-lactam

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2
Q

Penicillin G

A

Penicillinase-sensitive penicillin

IV and IM forms

Bactericidal from gram + cocci/rods, gram - cocci, spirochetes

SA: hypersensitivity reactions, hemolytic anemia

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3
Q

Penicillin V

A

Penicillinase-sensitive penicillin

Oral

Bactericidal from gram + cocci/rods, gram - cocci, spirochetes

SA: hypersensitivity reactions, hemolytic anemia

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4
Q

Ampicillin

A

Extended-spectrum penicillinase-sensitive aminopenicillin

Can be combined with clavulanic acid (β-lactamase inhibitor)

SA: hypersensitivity reactions, rash, pseudomembranous colitis

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5
Q

Amoxicillin

A

Extended-spectrum penicillinase-sensitive aminopenicillin

Better oral bioavailability than ampicillin

Can be combined with clavulanic acid (β-lactamase)

SA: hypersensitivity reactions, rash, pseudomembranous colitis

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6
Q

Oxacillin

A

Narrow-spectrum penicillinase-resistant penicillin

Resistant to penicillinase (bulky R group blocks access to β-lactam ring)

Indicated for MSSA

SA: hypersensitivity reactions, interstitial nephritis

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7
Q

Nafcillin

A

Narrow-spectrum penicillinase-resistant penicillin

Resistant to penicillinase (bulky R group blocks access to β-lactam ring)

Indicated for MSSA

SA: hypersensitivity reactions, interstitial nephritis

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8
Q

Dicloxacillin

A

Narrow-spectrum penicillinase-resistant penicillin

Resistant to penicillinase (bulky R group blocks access to β-lactam ring)

Indicated for MSSA, mastitis

SA: hypersensitivity reactions, interstitial nephritis

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9
Q

Ticarcillin

A

Extended-spectrum antipseudomonal carboxypenicillin

Can be combined with a β-lactamase inhibitor (clavulanic acid, sulbactam, tazobactam)

Indicated for pseudomonas and gram - rods

SA: hypersensitivity reactions

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10
Q

Piperacillin

A

Extended-spectrum antipseudomonal carboxypenicillin

Can be combined with a β-lactamase inhibitor (clavulanic acid, sulbactam, tazobactam)

Indicated for pseudomonas and gram - rods

SA: hypersensitivity reactions

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11
Q

How do cephalosporins work?

A

β-lactam drugs that inhibit cell wall synthesis by inhibiting peptidoglycan cross-linking

Less susceptible to penicillinases

Bactericidal

Low cross-reactivity with penicillins

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12
Q

Cefazolin

A

1st generation cephalosporin

Indicated for gram + cocci, Proteus mirabilis, E. coli, Klebsiella pneumoniae

Used prior to surgery to prevent S. aureus wound infections

SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides

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13
Q

Cephalexin

A

1st generation cephalosporin

Indicated for gram + cocci, Proteus mirabilis, E. coli, Klebsiella pneumoniae

SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides

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14
Q

Cefoxitin

A

2nd generation cephalosporin

Indicated for gram + cocci, Haemophilus pneumoaniae, Enterobacter aerogenes, Neisseria, Proteius mirabilis, E. coli, Klebsiella pneumoniae, Serratia marcescens

SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides

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15
Q

Cefaclor

A

2nd generation cephalosporin

Indicated for gram + cocci, Haemophilus pneumoaniae, Enterobacter aerogenes, Neisseria, Proteius mirabilis, E. coli, Klebsiella pneumoniae, Serratia marcescens

SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides

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16
Q

Cefuroxime

A

2nd generation cephalosporin

Indicated for gram + cocci, Haemophilus pneumoaniae, Enterobacter aerogenes, Neisseria, Proteius mirabilis, E. coli, Klebsiella pneumoniae, Serratia marcescens

SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides

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17
Q

Ceftriaxone

A

3rd generation cephalosporin

Indicated for serious gram - infections resistant to other β-lactams like meningitis and gonorrhea

SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides

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18
Q

Cefotaxime

A

3rd generation cephalosporin

Indicated for serious gram - infections resistant to other β-lactams

SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides

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19
Q

Ceftazidime

A

3rd generation cephalosporin

Indicated for serious gram - infections resistant to other β-lactams like pseudomonas

SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides

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20
Q

Cefepime

A

4th generation cephalosporin

↑ activity against Pseudomonas and gram + organisms

SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides

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21
Q

Ceftaroline

A

5th generation cephalosporin

Broad gram + and gram - coverage including MRSA but not Pseudomonas

SA: hypersensitivity reactions, vitamin K deficiency, ↑ nephrotoxicity of aminoglycosides

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22
Q

How do monobactams (e.g. aztreonam) work?

A

Monobactams bind to penicillin-binding proteins to prevent peptidoglycan cross-linking of the cell wall

Synergistic with aminoglycosides

No cross-allergenicity with penicillins

Resistant to β-lactamase

Indicated for gram - rods only in patients allergic to penicillins or have renal insufficiency and cannot tolerate aminoglycosides

SA: GI upset

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23
Q

Imipenem

A

Broad-spectrum β-lactamase-resistent carbapenem

Indicated for gram + cocci, gram - rods, and anaerobes

SA: GI distress, skin rash, CNS toxicity/seizures

Always administer with dilastin (inhibitor of renal dehydropeptidase I) to decreased inactivation of the drug in the renal tubules

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24
Q

Meropenem

A

Broad-spectrum β-lactamase-resistent carbapenem

Indicated for gram + cocci, gram - rods, and anaerobes

SA: GI distress, skin rash, decreased risk of CNS toxicity/seizures

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25
Q

Ertapenem

A

Broad-spectrum β-lactamase-resistent carbapenem

Indicated for gram + cocci, gram - rods, anaerobes, limited pseudomonas coverage

SA: GI distress, skin rash, CNS toxicity/seizures

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26
Q

Doripenem

A

Broad-spectrum β-lactamase-resistent carbapenem

Indicated for gram + cocci, gram - rods, anaerobes, limited pseudomonas coverage

SA: GI distress, skin rash, CNS toxicity/seizures

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27
Q

Vancomycin

A

Glycopeptide that binds to D-ala D-ala portion of cell wall precursors to inhibit cell wall peptidoglycan formation

Bactericidal

Indicated for gram + only, including MRSA and C. difficile (oral formulation)

SA: nephrotoxicity, ototoxicity, thrombophlebitis, red man syndrome (prevent with slow infusion rate and antihistamines)

Resistance via amino acid modifatio to D-ala D-lac

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28
Q

Mnemonic for antibiotics that inhibit protein synthesis

A

Buy AT 30, CCEL at 50

30S inhibitors:

A = aminoglycosides (bactericidal)

T = tetrocyclines (bacteriostatic)

50S inhibitors:

C = chloramphenicol, clindamycin (bacteriostatic)

E = erythromycin (macrolides) (bacteriostatic)

L = linezolid (variable)

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29
Q

How do aminoglycosides work?

A

Aminoglycosides inhibit the formation of the initition complex and cause misreading of mRNA and block translocation

Require O2 for uptake so ineffective against anaerobes

Bactericidal

Resistance when bacterial transferase enzymes inactivate the drug by acetylation, phosphorylation, or adenylation

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30
Q

Gentamicin

A

Aminoglycoside (inhibits initiation complex and translocation)

Indicated for severe gram - rod infections

Synergistic with β-lactam antibiotics

SA: nephrotoxicity (especially when used with cephalosporins), neuromuscular blockade, ototoxicity (esp. when used with loop diuretics), teratogen

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31
Q

Neomycin

A

Aminoglycoside (inhibits initiation complex and translocation)

Indicated for severe gram - rod infections, good for bowel surgery

Synergistic with β-lactam antibiotics

SA: nephrotoxicity (especially when used with cephalosporins), neuromuscular blockade, ototoxicity (esp. when used with loop diuretics), teratogen

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32
Q

Amikacin

A

Aminoglycoside (inhibits initiation complex and translocation)

Indicated for severe gram - rod infections

Synergistic with β-lactam antibiotics

SA: nephrotoxicity (especially when used with cephalosporins), neuromuscular blockade, ototoxicity (esp. when used with loop diuretics), teratogen

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33
Q

Tobramycin

A

Aminoglycoside (inhibits initiation complex and translocation)

Indicated for severe gram - rod infections

Synergistic with β-lactam antibiotics

SA: nephrotoxicity (especially when used with cephalosporins), neuromuscular blockade, ototoxicity (esp. when used with loop diuretics), teratogen

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34
Q

Streptomycin

A

Aminoglycoside (inhibits initiation complex and translocation)

Indicated for severe gram - rod infections

Synergistic with β-lactam antibiotics

SA: nephrotoxicity (especially when used with cephalosporins), neuromuscular blockade, ototoxicity (esp. when used with loop diuretics), teratogen

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35
Q

How do tetracyclines work?

A

Binds to 30S and prevents attachment of tRNA

Limited CNS penetration

Avoid taking with milk (Ca2+), antacids (Ca2+ or Mg2+), or iron-containing preparations because divalent cations inhibit absorption in the gut

Resistance 2/2 plasmid-encoded transport pumps

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36
Q

Tetracycline

A

Tetracycline (prevents tRNA binding to 30S)

Indicated for rickettsia (Lyme), Mycoplasma pneumoniae, and chlamydia, acne

SA: GI distress, discoloration of teeth and inhibition of bone growth in children → contraindicated in pregnancy, photosensitivity

Avoid milk, antacid, iron 2/2 ↓ uptake in the gut

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37
Q

Doxycycline

A

Tetracycline (prevents tRNA binding to 30S)

Indicated for rickettsia (Lyme), Mycoplasma pneumoniae, and chlamydia, acne

SA: GI distress, discoloration of teeth and inhibition of bone growth in children → contraindicated in pregnancy, photosensitivity

Avoid milk, antacid, iron 2/2 ↓ uptake in the gut

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38
Q

Minocycline

A

Tetracycline (prevents tRNA binding to 30S)

Indicated for rickettsia (Lyme), Mycoplasma pneumoniae, and chlamydia, acne

SA: GI distress, discoloration of teeth and inhibition of bone growth in children → contraindicated in pregnancy, photosensitivity

Avoid milk, antacid, iron 2/2 ↓ uptake in the gut

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39
Q

How do macrolides work?

A

Binds to 50S to block translocation

SA: GI motility, prolonged QT → arrhythmias, acute cholestatic hepatitis, rash, eosinophilia, increases serum concentration of theophyllines and oral anticoagulants

Resistance from methylation of 23S rRNA-binding site preventing binding

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40
Q

Azithromycin

A

Macrolide (binds to 50S preventing translocation)

Indicated for atypical pneumonias including MAC, chlamydia, gram + cocci

SA: GI motility, prolonged QT → arrhythmias, acute cholestatic hepatitis, rash, eosinophilia, increases serum concentration of theophyllines and oral anticoagulants

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41
Q

Clarithromycin

A

Macrolide (binds to 50S preventing translocation)

Indicated for atypical pneumonias, chlamydia, gram + cocci

SA: GI motility, prolonged QT → arrhythmias, acute cholestatic hepatitis, rash, eosinophilia, increases serum concentration of theophyllines and oral anticoagulants

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42
Q

Erythromycin

A

Macrolide (binds to 50S preventing translocation)

Indicated for atypical pneumonias, chlamydia, gram + cocci, prophylaxis for gonococcal or chlamydia conjuctivitis in newborn

SA: GI motility, prolonged QT → arrhythmias, acute cholestatic hepatitis, rash, eosinophilia, increases serum concentration of theophyllines and oral anticoagulants

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43
Q

Cloramphenicol

A

Blocks peptidyltransferase at 50S

Bacteriostatic

Indicated for bacterial meningitis, Rocky Mountain Spotted Fever

SA: amenia, a plastic anemia, gray baby syndrome (premature infants lack UDP-glucuronyl transferase)

Resistance from plasma-encoded acetyltransferase inactivation

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44
Q

Clindamycin

A

Blocks translocation at 50S

Bacteriostatic

Indicated for oral and lung anaerobic infections, invasive Group A strep (Treats anaerobes above the diaphragm)

SA: pseudomembranous colitis, fever, diarrhea

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45
Q

Sulfamethoxazole (SMX)

A

Sulfonamide antibiotic inhibits dihydropteroate synthase blocking conversion of para-aminobenzoic acid (PABA) and pteridine to dihydropteroic acid in the folic acid pathway

Indicated for gram +, gram -, Nocardia, Chlamydia

SA: hypersensitivity reactions, hemolysis if G6PD deficient, nephrotoxicity, photosensitiity, kernicterus in infants, displace other drugs from albumin (e.g. warfarin)

Resistance via altered dihydropteroate synthase, ↓ uptake, ↑ PABA synthesis

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46
Q

Sulfisoxazole

A

Sulfonamide antibiotic inhibits dihydropteroate synthase blocking conversion of para-aminobenzoic acid (PABA) and pteridine to dihydropteroic acid in the folic acid pathway

Indicated for gram +, gram -, Nocardia, Chlamydia

SA: hypersensitivity reactions, hemolysis if G6PD deficient, nephrotoxicity, photosensitiity, kernicterus in infants, displace other drugs from albumin (e.g. warfarin)

Resistance via altered dihydropteroate synthase, ↓ uptake, ↑ PABA synthesis

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47
Q

Sulfadiazine

A

Sulfonamide antibiotic inhibits dihydropteroate synthase blocking conversion of para-aminobenzoic acid (PABA) and pteridine to dihydropteroic acid in the folic acid pathway

Indicated for gram +, gram -, Nocardia, Chlamydia

SA: hypersensitivity reactions, hemolysis if G6PD deficient, nephrotoxicity, photosensitiity, kernicterus in infants, displace other drugs from albumin (e.g. warfarin)

Resistance via altered dihydropteroate synthase, ↓ uptake, ↑ PABA synthesis

48
Q

Trimethoprim (TMP)

A

Inhibits dihydrofolate reductase preventing conversion of dihydrofolic acid to tetrahydrofolic acid in the folic acid pathway

Used with SMX for UTIs, Shigella, Salmonella, PCP treatment and prophylaxis, toxoplasmosis prophylaxis

SA: megaloblastic anemia, leukopenia, granulocytopenia

49
Q

How do fluoroquinolones work?

A

Inhibits DNA gyrase (topoisomerase II) and topoisomerase IV

Bactericidal

Avoid taking with antacids

SA: GI upset, superinfections, skin rashes, headache, dizziness, tendonitis, tendon rupture in patients > 60 taking prednisone, prolonged QT interval, cartilage damage → contraindicated in pregnancy, breastfeeding, children < 18

Resistance from efflux pumps, mutation in DNA gyrase

50
Q

Ciprofloxacin

A

Fluoroquinolong (inhibits DNA gyrase/topoisomerase II and topoisomerase IV)

Bactericidal

Avoid taking with antacids

Indicated for gram - rods in urinary and GI tracks, Pseudomonas, Neisseria, meningococcal prophylaxis in adults

SA: GI upset, superinfections, skin rashes, headache, dizziness, tendonitis, tendon rupture in patients > 60 taking prednisone, prolonged QT interval, cartilage damage → contraindicated in pregnancy, breastfeeding, children < 18

51
Q

Metronidazole

A

Forms free radical toxic metabolites that damage DNA

Bactericidal, antiprotozoal

Indicated for Giardia, Entamoeba, Gardnerella vaginalis, anaerobes, H. pylori (anaerobic infections below the diaphragm)

SA: disulfiram-like reaction (severe flushing, tachycardia, hypotension) with alcohol, headache, metallic taste

52
Q

Isoniazid (INH)

A

↓ synthesis of mycolic acids

Bacterial KatG encodes catalse-peroxidase which converts INH to active metabolite

Indicated for TB treatment and prophylaxis

SA: neurotoxicity → take pyridoxine/vitmain B6, hepatotoxicity, lupus (“INH injures neurons and hepatocytes”)

53
Q

Rifampin

A

Inhibits DNA-dependent RNA polymerase

Indicated for TB as part of RIPE, meningococcal prophylaxis in children, Hib prophylaxis, delays resistance to dapsone in leprosy

SA: minor hepatotoxicity, drug interactions (induces P450), red/orange body fluids

54
Q

Rifabutin

A

Inhibits DNA-dependent RNA polymerase

Indicated for TB as part of RIPE, MAC, meningococcal prophylaxis, Hib prophylaxis, delays resistance to dapsone in leprosy

SA: minor hepatotoxicity, red/orange body fluids, fewer drug interactions (less induction of P450 compared to rifampin) → better in patients with HIV

55
Q

Pyrazinamide

A

Acidifies intracellular environment

Indicated for TB as part of RIPE

SA: hyperuricemia, hepatotoxicity

56
Q

Ethambutol

A

Blocks arabinosyltransferase → ↓ carbohydrate polymerase of mycobacterium cell wall

Indicated for TB as part of RIPE

SA: optic neuropathy (red-green colorblindness)

57
Q

HIV/AIDS prophylaxis

A

CD4 count < 200 → TMP-SMX for PCP

CD4 count < 100 → TMP-SMX for toxo

CD4 count < 50 → azithromycin for MAC

58
Q

Antibiotics effective against MRSA

A

Vancomycin

Daptomycin

Linezolid (can cause serotonin syndrome)

Tigecycline

Ceftaroline

59
Q

Amphotericin B

A

Antifungal binds ergosterol and forms membrane pores

Indicated for serious, systemic mycoses

Supplement K+ and Mg2+ 2/2 altered renal tubule permeability

SA: fever/chills, hypotension, nephrotoxicity → prevent with adequate hydration, arrhythmias, anemia, IV phlebitis; liposomal amphortericin decreases toxicity

60
Q

Nystatin

A

Topical antifungal binds ergosterol and forms membrane pores

Indicated for oral candidiasis, diaper rash, vaginal candidiasis

61
Q

Fluconazole

A

Antifungal inhibits P-450 enzyme that forms sterol (ergosterol)

Indicated for local and less serious systemic mycoses, chronic suppression of cryptococcal meningitis in AIDS and candidal infections of all types

SA: inhibits testosterone synthesis, liver dysfunction

62
Q

Ketoconazole

A

Antifungal inhibits P-450 enzyme that forms sterol (ergosterol)

Indicated for local and less serious systemic mycoses

SA: inhibits testosterone synthesis → gynecomastia, liver dysfunction

63
Q

Itraconazole

A

Antifungal inhibits P-450 enzyme that forms sterol (ergosterol)

Indicated for local and less serious systemic mycoses, Blastomyces, Coccidioides, Histoplasma

SA: inhibits testosterone synthesis, liver dysfunction

64
Q

Clotrimazole

Miconazole

A

Topical antifungal inhibits P-450 enzyme that forms sterol (ergosterol)

Indicated for local and less serious systemic mycoses

SA: inhibits testosterone synthesis, liver dysfunction

65
Q

Flucytosine

A

Antifungal is converted into 5-fluorouracil by cytosine deaminase to prevent DNA and RNA biosynthesis

Used with amphotericin B to treat systemic fungal infections, especially Cryptococcus meningitis)

SA: bone marrow suppression

66
Q

Caspofungin

Micafungin

Anidulafungin

A

Antifungal echinocandin inhibits synthesis of β-glucan inhibiting cell wall synthesis

Indicated for invasive aspergillosis and candida

SA: GI upset, flushing (via histamine release)

67
Q

Terbinafine

A

Inhibits fungal enzyme squaline epoxidase

Indicated for dermatophytoses, especially onychomycosis

SA: GI upset, headaches, hepatotoxicity, taste disturbance

68
Q

Griseofulvin

A

Antifungal interferes with microtubule formations thus disrupting mitosis; deposits in keratin-containing tissues

Indicated for oral treatment of superfician infections, inhibits growth of dermatophytes (tinea, ringworm)

SA: teratogenic, carcinogenic, confusion, headache, induce P-450

69
Q

Treatment of protozoal infections

A

Toxoplasmosis → pyrimethamine

Trypanosoma brucei → suramin and malarsoprol

Trypanosoma cruzi → nifurtimox

Leishmaniasis → sodium stibogluconate

70
Q

Chloroquine

A

Blocks detoxification of heme into hemozoin → build-up of heme is toxic to plasmodia

Indicated for plasmodial species other than P. falciparum (resistant 2/2 efflux pump)

SA: retinopathy, pruritus

71
Q

Artemether/lumefantrine

A

Treatment for P. falciparum

72
Q

Atovaquone/proguanil

A

Treatment for P. falciparum

73
Q

Quinidine in U.S.

Qauinine elsewhere

Artesunate

A

Treatment for life-threatening malaria

74
Q

Treatmet against flukes?

A

Praziquantel

75
Q

Zanamivir

A

Treats influenza A and B by inhibiting influenza neuraminidase preventing release of progeny virus

76
Q

Oseltamivir

A

Treats influenza A and B by inhibiting influenza neuraminidase preventing release of progeny virus

77
Q

Ribavirin

A

Inhibits inosine monophosphate dehydrogenase preventing synthesis of guanine nucleotides

Indicated for RSV, chronic hepatitis C

SA: hemolytic anemia, severe teratogen

78
Q

Acyclovir

Famciclovir (for VZV)

Valacyclovir (prodrug of acyclovir with better oral bioavailability)

A

Monophosphorylated by viral thymidine kinase forming guanosine analogs which inhibits DNA polymerase by chain termination

Indicated for HSV, VZV, weakly active against EBV

SA: obstructive crystalline nephropathy and acute renal failure if not adequately hydrated

Resistance 2/2 mutated viral thymidine kinase

79
Q

Ganciclovir

Valganciclovir (prodrug of ganciclovir with better oral bioavailability)

A

Converted to 5’-monophosphate (guanosine analog) by CMV viral kinase that preferentially inhibits viral DNA polymerase

Indicated for CMV, esp in immunocompromised

SA: leukopenia, neutropenia, thrombocytopenia, renal toxicity

Resistance 2/2 mutated CMV DNA polymerase or lack of viral kinase

80
Q

Foscarnet

A

Binds to pyrophosphate-binding site of viral DNA polymerase (does not require activation with viral kinase)

Indicated for CMV retinitis in immunocompromised patients when ganciclovir fails, acyclovir-resistant HSV

Resistance 2/2 mutated DNA polymerase

81
Q

Cidofovir

A

Inhibits viral DNA polymerase (doesn’t require activation by viral kinases)

Indicated for CMV retinitis in immunocompromised patients, acyclovir-resistant HSV

SA: nephrotoxicity (coadminister with probenecid and IV saline)

82
Q

HAART

A

2 NRTIs + 1 NNRTI OR 1 protease inhibitor OR 1 integrase inhibitor

83
Q

Which anti-retrovirals have activity against HBV?

A

Lamivudine (NRTI) Tenofovir (Nucleotide RTI) Emtricitabine (NRTI)

84
Q

Zidovudine (AZT)

A

Nucleoside Reverse Transcriptase Inhibitor (NRTI) → drug phosphorylated and competitively inhibits nucleotide binding to reverse transcriptase to terminate DNA (lack 3’ OH group)

SA: lactic acidosis, bone marrow suppression (reversed with G-CSF and EPO), peripheral neuropathy, macrocytic anemia

Used as prophylaxis or treatment of HIV; safe in pregnancy to reduce transmission

85
Q

Emtricitabine

A

Nucleoside Reverse Transcriptase Inhibitor (NRTI) → drug phosphorylated and competitively inhibits nucleotide binding to reverse transcriptase to terminate DNA (lack 3’ OH group)

SA: lactic acidosis, bone marrow suppression (reversed with G-CSF and EPO), peripheral neuropathy

Treats HIV and HBV

86
Q

Abacavir

A

Nucleoside Reverse Transcriptase Inhibitor (NRTI) → drug phosphorylated and competitively inhibits nucleotide binding to reverse transcriptase to terminate DNA (lack 3’ OH group)

Need to genotype patient to prevent hypersensitivity reaction

SA: lactic acidosis, bone marrow suppression (reversed with G-CSF and EPO), peripheral neuropathy

87
Q

Lamivudine

A

Nucleoside Reverse Transcriptase Inhibitor (NRTI) → drug phosphorylated and competitively inhibits nucleotide binding to reverse transcriptase to terminate DNA (lack 3’ OH group)

SA: lactic acidosis, bone marrow suppression (reversed with G-CSF and EPO), peripheral neuropathy

Treats HIV and HBV

Safe during pregnancy

88
Q

Didanosine

A

Nucleoside Reverse Transcriptase Inhibitor (NRTI) → drug phosphorylated and competitively inhibits nucleotide binding to reverse transcriptase to terminate DNA (lack 3’ OH group)

SA: lactic acidosis, bone marrow suppression (reversed with G-CSF and EPO), peripheral neuropathy, pancreatitis

89
Q

Stavudine

A

Nucleoside Reverse Transcriptase Inhibitor (NRTI) → drug phosphorylated and competitively inhibits nucleotide binding to reverse transcriptase to terminate DNA (lack 3’ OH group)

SA: lactic acidosis, bone marrow suppression (reversed with G-CSF and EPO), peripheral neuropathy

90
Q

Tenofovir

A

Nucleotide Reverse Transcriptase Inhibitor (NRTI) → competitively inhibits nucleotide binding to reverse transcriptase to terminate DNA (lack 3’ OH group)

SA: bone marrow suppression (reversed with G-CSF and EPO), peripheral neuropathy, rash

Doesn’t require primary phosphorylation so effective in resting cells

Nephrotoxic (Fanconi’s syndrome –> phosphaturia, glucosuria)

91
Q

Nevirapine

A

Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI) → binds to and inhibits reverse transcriptase at a site different from NRTI (doesn’t require phosphorylation)

Prophylaxis in pregnancy

Side effects include rash, hepatotoxicity, drug-drug interactions (CYP3A4), Stevens Johnson Syndrome

92
Q

Efavirenz

A

Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI) → binds to and inhibits reverse transcriptase at a site different from NRTI (doesn’t require phosphorylation)

Side effects include rash, hepatotoxicity, drug-drug interactions (CYP3A4), vivid dreams, CNS symptoms

Contraindicated in pregnancy

93
Q

Delavirine

A

Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI) → binds to and inhibits reverse transcriptase at a site different from NRTI (doesn’t require phosphorylation)

Side effects include rash, hepatotoxicity, drug-drug interactions (CYP3A4)

Contraindicated in pregnancy

94
Q

Maraviroc

A

Inhibits binding of gp120 to CCR5 on T cells/monocytes

Not effective if CXCR4 tropism

SA: skin reaction at injection site

95
Q

Enfuviritide

A

Locks gp41 in extended conformation inhibiting viral entry

Injected subcutaneously

SA: skin reaction at injection site

96
Q

Raltegravir

A

Reversible integrase inhibitor prevents integration of viral genome into host cell chromosome

SA: hypercholesterolemia

97
Q

Atazanavir

A

HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA

SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities

Lower incidence of lipodystrophy

98
Q

Darunavir

A

HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA

SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities

Given with ritonavir

99
Q

Fosamprenavir

A

HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA

SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities

100
Q

Indinavir

A

HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA

SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities, nephropathy (nephrolithiasis), hematuria

101
Q

Lopinavir

A

HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA

SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities

Given with rito_navir_

Recommended during pregnancy

102
Q

Ritonavir

A

HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA

SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities

Recommended during prenancy

Strongly inhibits CYP3A4 → boosts other drug concentrations

103
Q

Saquinavir

A

HIV-1 protease inhibitor → prevents maturation of new virus by inhibiting cleavage of mRNA

SA: lipodystrophy, dyslipidemia, hyperglycemia, insulin resistance, cardiac conduction abnormalities

104
Q

Sofosbuvir

A

Inhibits HCV RNA synthesis by inhibiting polymerase

Genotyping to determine if combination therapy needed (IFNα and ribavirin)

105
Q

Boceprevir

A

HCV protease inhibitor

Use with IFNα and ribavarin

106
Q

Telaprevir

A

HCV protease inhibitor

Use with IFNα and ribavarin

107
Q

Simeprevir

A

HCV protease inhibitor

Use with IFNα and ribavarin

108
Q

Pentamidine

A

IV form treats PCP

Aerosolized form is PCP prophylaxis (but not protection against disseminated PCP or toxo)

Side effects include nephrotoxicity, hypoglycemia, hepatotoxicity, hypotension, pancreatitis, prolong QT (torsades), low magnesium

109
Q

Dapsone

A

Inhibits synthesis of dihydrofolic acid

Treatment or prophylaxis for PCP (also protects against toxo)

Treatment for Hansen’s disease

Comes in liquid form

Check for G6PD deficiency –> hemolytic anemia

Side effect include rash, fever, bone marrow suppression

Contraindicated in patients with a sulfa allergy

110
Q

Which antibiotics are concentration-dependent?

A

Aminoglycosides

Daptomycin

Quinolones

111
Q

Which antibiotics are time-dependent?

A

β-lactams

Vancomycin

112
Q

Which antibiotics are AUC?

A

Chloramphenicol

Clindamycin

Tetracycline

Glycopeptides

Macrolides

Sulfonamides

113
Q

Which antibiotics are bactericidal?

A

β-lactams

Aminoglycosides

Vancomycin (variable)

Daptomycin (variable)

Fluoroquinolones

Metronidazole T

ype B streptogramins

Nitrofurantoin

Rifamycins

114
Q

Which antibiotics are bacteriostatic?

A

Macrolides

Tetracylines

Sulfonamides

Chloramphenicol (variable)

Clindamycin

Trimethoprim

Linezolid

115
Q

Interferon-alpha

A

Indicated for chronic hepatitis B and C, Kaposi sarcoma, hairy cell leukemia, condyloma acuminatum, renal cell carcinoma, malignant melanoma

SA: neutropenia, myopathy

116
Q

Interferon-beta

A

Indicated for multiple sclerosis

SA: neutropenia, myopathy

117
Q

Interferon-gamma

A

Indicated for chronic granulomatous disease

SA: neutropenia, myopathy

USMLE Step 1 (20 decks)

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