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.► FARMACOLOGIA CLÍNICA - JP > USMLE Antibiotics > Flashcards

USMLE Antibiotics Flashcards

1
Q

Penicillin mechanism

A

Blocks cell wall synthesis by inhibiting peptidoglycan cross-linking

  • Binds to penicillin binding proteins in peptidoglycan
  • activates autolytic enzymes
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2
Q

penicillin use

A

Gram + organisms:
- S. pneumoniae, S. pyogenes, Actinomyces

Also:
- Neisseria meningitidis, Treponema pallidum, & Syphilis

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3
Q

penicillin toxicity

A

hypersensitivity reactions, hemolytic anemia

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4
Q

penicillinase resistant penicillins

A

methicillin, nafcillin, dicloxacillin

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5
Q

penicillinase resistant penicillin use

A

Staph aureus

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6
Q

penicillinase resistant penicillin toxicity

A

hypersensitivity; methicillin: interstitial nephritis

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7
Q

aminopenicillins

A

ampicillin, amoxacillin

amOxicillin has greater Oral bioavailability

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8
Q

aminopenicillin mechanism

A
  • Same as penicillin but wider spectrum
  • Penicillinase sensitive
  • Combine w/ Clavulanic acid to protect against B-lactams
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9
Q

aminopenicillin use

A

Same as Penicillin, but wider spectrum

–H. influenza, E coli, Listeria monocytogenes, Proteus mirabilis, Salmonella, Shigella, Klebsiella, Enterococci

(Aminopenicillin HELPSS Kill Enterococci)

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10
Q

aminopenicillin toxicity

A

hypersensitivity, ampicillin rash, pseudomembranous colitis

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11
Q

antipseudomonal drugs

A

ticarcillin, piperacillin, carbenicillin

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12
Q

antipseudomonal mechanism

A

same as penicillin; wider spectrum

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13
Q

antipseudomonal use

A

Pseudomonas and gram negative rods

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14
Q

antipsuedomonal toxicity

A

hypersensitivity reaction

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15
Q

beta lactamase inhibitor mechanism

A

inhibit beta lactamase (protects penicillins from destruction)

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16
Q

beta lacatamase drugs

A

clavulanic acid, sulbactam, tazobactam

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17
Q

bacteriostatic antibiotics

A

Macrolides (Azithromycin, Clarithromycin, Erythromycin)

  • Tetracyclines (Tetracycline, Doxycycline, Demeclocycline, Minocycline)
  • Clindamycin
  • Sulfonamides (Sulfamethoxazole, Sulfisoxazole, Sulfadiazine)
  • Trimethoprim
  • Chloramphenicol
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18
Q

bactericidal antibiotics

A

vancomycin, fluoroquinolones, penicillin, aminoglycosides, cephalosporins, metronidazole

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19
Q

1st generation cephalosporins

A

Cefazolin, Cephalexin

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20
Q

1st generation cephalosporin coverage

A

Gram + Cocci: Proteus, E. coli, Klebsiella

“PEcK”

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21
Q

cephalosporin mechanism

A

beta lactams; inhibit cell wall synthesis but less susceptible to penicillinases

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22
Q

2nd generation cephalosporins

A

Cefoxitin, Cefaclor, Cefuroxime

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23
Q

2nd generation cephalosporin coverage

A

Gram + Cocci:
H. influenzae, Enterobacter aerogenes, Neisseria, Proteus mirabilis, E. coli, Klebsiella pneumoniae, Serratia marcescens

“HEN PEcKS”

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24
Q

3rd generation cephalosporins

A

ceftriaxone, ceftazidime, cefotaxime

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25
Q

3rd generation cephalosporin coverage

A

Serious gram negative infections, resistant to other B-lactams:

Ceftriaxone: Neisseria meningitidis & Gonorrhea

Ceftazidime: Pseudomonas

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26
Q

4th generation cephalosporins

A

Cefepime

- inc’d activity against Pseudomonas & gram + organisms

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27
Q

cephalosporin toxicity

A

hypersensitivity, vitamin K deficiency, cross-hypersensitivity with penicillins, increase nephrotoxicity of aminoglycosides, reaction with alcohol

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28
Q

aztreonam mechanism

A

beta lactamase resistant monobactam; binds penicillin binding protein

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29
Q

aztreonam use

A

gram negative rods only

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30
Q

aztreonam toxicity

A

occasional GI upset

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31
Q

imipenem/cilastin mechanism

A

beta-lactamase resistant carbapenem; cilastin is a renal dihydropeptidase 1 (to decrease renal inactivation)

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32
Q

imipenem use

A

broad spectrum; gram + cocci, gram - rods and anaerobes

use limited to life-threatening or refractory infections because of side effects

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33
Q

imipenem toxicity

A

GI distress, skin rash, CNS toxicity (seizures) at high plasma levels

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34
Q

vancomycin mechanism

A

inhibits cell wall mucopeptide formation by binding D ala D ala portion of cell wall precursors

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35
Q

vancomycin use

A

gram + only; use reserved for resistant infections–Staph aureus, enterococci, C diff

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36
Q

vancomycin toxicity

A

nephrotoxicity, ototoxicity, thrombophlebitis, red man syndrome, but well-tolerated in general

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37
Q

resistance to vancomycin

A

amino acid change from D-ala D-ala to D-ala D-lac

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38
Q

30s ribosomal inhibitors

A

tetracyclins, aminoglycosides

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39
Q

50s ribosomal inhibitors

A

clindamycin, chloramphenicol, erythromycin, linezolid, lincomycin

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40
Q

aminoglycoside drugs

A

gentamicin, neomycin, amikacin, tobramycin, streptomycin

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41
Q

aminoglycoside mechanism

A

inhibit initiation of protein synthesis by binding to & distorting the structure of prokaryotic 30S ribosomal unit

  • this causes misreading of mRNA
  • require O2 for uptake
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42
Q

aminoglycoside use

A

no anaerobe coverage; severe gram - rod infections; synergistic with beta lactams; neomycin for bowel surgery

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43
Q

aminoglycoside toxicity

A

nephrotoxicity (esp with cephalosporins), ototoxicity (esp with loop diuretics), teratogen

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44
Q

aminoglycoside resistance

A

drug modification via transferases

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45
Q

tetracycline mechanism

A

binds to 30s and prevents attachment of amino-acyl tRNA; limited CNS penetration

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46
Q

tetracycline use

A

borrelia burgdorferi, H. pylori, Mycoplasma. Rickettsia, Chlamydia (accumulates intercellularly); demeclocycline is ADH antagonist so used in SIADH

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47
Q

tetracycline administration consideration

A

absorption inhibited by milk, antacids, iron preparations; can be used in patients with renal failure because fecally eliminated

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48
Q

tetracycline toxicity

A

GI distress, teeth discoloration, inhibition of bone growth in children, photosensitivity

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49
Q

tetracycline resistance

A

decreased uptake or increased efflux

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50
Q

macrolide drugs

A

erythromycin, azithromycin, clarithromycin

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51
Q

macrolide mechanism

A

binds to 50s subunit and blocks translocation (binds to 23s RNA)

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52
Q

macrolide use

A

atypical pneumonias (mycoplasma, chlamydia, legionella), URIs, STDs, gram positive cocci (in pts allergic to penicillin), Neisseria

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53
Q

macrolide toxicity

A

prolonged QT, GI discomfort, acute cholestatic hepatitis, eosinophilia, skin rashes, increases serum concentration of theophyllines and oral anticoagulants

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54
Q

macrolide resistance

A

methylation of 23s binding site

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55
Q

chloramphenicol mechanism

A

binds to 50s ribosome, inhibits peptidyltransferase activity

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56
Q

chloramphenicol use

A

meningitis (H flu, Neisseria meningitis, Strep pneumo)

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57
Q

clindamycin mechanism

A

binds to the 50 S ribosome, blocks peptide bond formation (bacteriostatic)
(blocks translocation step)

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58
Q

clindamycin use

A

anaerobic infections in aspiration pneumonia or lung abscesses

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59
Q

clindamycin toxicity

A

psuedomembranous colitis, fever, diarrhea

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60
Q

sulfonamide mechanism

A

Blocks nucleotide synthesis by inhibiting folic acid synthesis (involved in methylation)

  • PABA antimetabolites (compete w/ PABA to) inhibit dihydropteroate synthetase; inhibit bacterial folic acid production (bacteriostatic)
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61
Q

sulfonamide use

A

gram positive, gram negative, Nocardia, chlamydia, simple UTI, also opportunistic infection prophylaxis in HIV patients

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62
Q

sulfonamide toxicity

A

hypersensitivity reactions, hemolysis in G6PD deficiency, nephrotoxicity, photosensitivity, kernicterus in infants, displaces warfarin and other drugs from albumin binding

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63
Q

sulfonamide resistance

A

altered bacterial dihydropteroate synthetase, decreased uptake or increased PABA synthesis

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64
Q

trimethoprim mechanism

A

Blocks nucleotide synthesis by inhibiting folic acid synthesis (involved in methylation)

  • Inhibits bacterial dihydrofolate reductase (bacteriostatic)
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65
Q

trimethoprim use

A

used in combo with sulfamethoxazole for recurrent UTI’s, Shigella. Salmonella, pneumocystis

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66
Q

trimethoprim toxicity

A

megaloblastic anemia, leukopenia, granulocytopenia; lurcovorin rescue to supplement with folinic acid

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67
Q

fluoroquinolone mechanism

A

inhibit bacterial DNA gyrase (bactericidal)

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68
Q

sulfonamide drugs

A

sulfamethoxazole, sulfisoxazole, sulfadiazine

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69
Q

fluoroquinolone drugs

A

ciprofloxacin, norfloxacin, ofloxacin, sparfloxacin, moxifloxacin, gatifloxacin, enxoxacin, nalidixic acid (a quinolone)

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70
Q

fluoroquinolone use

A

gram negative rods of urinary and GI tracts, Neisseria, some gram positive, also has action vs. psuedomonas

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71
Q

fluoroquinolone toxicity

A

GI upset, rash, superinfection, headache, dizziness; contraindicated in pregnant women because of risk or cartilage damage, tendonitis and tendon rupture in adults, legs cramps and myalgias in kids; do not take with antacids

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72
Q

fluoroquinolone resistance

A

chromosomal DNA gyrase mutation

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73
Q

metronidazole mechanism

A

forms free radical toxic metabolites in bacterial cell that damages DNA; bactericidal and anti-protozoal

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74
Q

metronidazole use

A

anaerobes, giardia, entamoeba histolytica, trichomonas, gardnerella vaginalis; used in H. pylori triple therapy

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75
Q

metronidazole toxicity

A

disulfuram like reaction with alcohol; headache; metallic taste

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76
Q

polymixin drugs

A

polymixin B, colistimethate

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77
Q

polymixin mechanism

A

bind to cell membranes of bacteria and disrupt osmotic properties; catatonic and basic proteins that act as detergents

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78
Q

polymixin toxicity

A

neurotoxicity, acute renal tubular necrosis

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79
Q

polymixin use

A

resistant gram - infections

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80
Q

TB treatments

A

rifampin, isoniazide, ethambutol, pyrazinamide (isoniazid is prophylaxis)

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81
Q

Mycobacterium avium treatment

A

azithromycin, rifampin, ethambutol, streptomycin

82
Q

mycobacterium leprae treatment

A

rifampin, dapsone, clofazimine

83
Q

ethambutol toxicity

A

optic neuropathy

84
Q

pyrazinamide toxicity

A

hepatotoxicity

85
Q

ethambutol mechanism

A

blocks arabinosyltransferase to decrease carbohydrate polymerization of cell wall

86
Q

isoniazid mechanism

A

decreases synthesis of mycolic acids; need bacterial catalase peroxidase to convert isoniazid to active metabolite

87
Q

clinical use of isoniazid

A

TB

88
Q

isoniazid toxicity

A

neurotoxicity, hepatotoxicity, lupus, pyradoxime (B6) deficiency–supplementation can prevent neurotoxicity and maybe lupus

89
Q

rifampin mechanism

A

inhibits DNA-dependent RNA polymerase

90
Q

rifampin use

A

TB, delays dapsone resistance in leprosy, Neisseria and H.flu prophylaxis

91
Q

rifampin toxicity

A

minor hepatotoxicity, P450 inducer, orange body fluids

92
Q

rifampin resistance

A

mutation in RNA polymerase

93
Q

meningococcal prophylaxis

A

rifampin, minocycline

94
Q

gonorrhea prophylaxis

A

ceftriaxone

95
Q

syphylis prophylaxis

A

penicillin G

96
Q

recurrent UTI prophylaxis

A

TMP-SMX

97
Q

pneumocystis prophylaxis

A

TMP-SMX, aerosolized pentamidine

98
Q

endocarditis prophylaxis in surgical/dental procedures

A

penicillins

99
Q

mycobacterium avium prophylaxis

A

azithromycin

100
Q

amphotericin B mechanism

A

binds ergosterol in fungal membrane and forms pores that allow leakage of electrolytes; does not cross BBB

101
Q

amphotericin B use

A

serious systemic mycoses (crypococcus, blastomyces, coccidiodes, aspergillus, histoplasma, candida)

102
Q

amphotericin B toxicity

A

fever/chills, hypotension, nephrotoxicity, arrhythmias, anemia, IV phlebitis; liposomal amphotericin reduces toxicity

103
Q

nystatin mechanism

A

binds ergosterol in fungal membrane and forms pores that allow leakage of electrolytes

104
Q

nystatin use

A

topical only because too toxic for systemic use; “swish and swallow” for oral thrush, topical for diaper rash or vaginal candidiasis

105
Q

nystatin toxicity

A

too toxic for systemic use but not absorbed in GI tract

106
Q

azole drugs

A

fluconazole, ketoconazole, clotrimazole, miconazole, itraconazole, voriconazole

107
Q

azole mechanism

A

inhibit ergosterol synthesis by inhibiting the P450 enzyme that converts lanosterol to ergosterol

108
Q

azole use

A

systemic mycoses

109
Q

fluconazole use

A

cryptococcal meningitis in AIDS patients (can cross BBB), candidal infections

110
Q

ketoconazole use

A

blastomyces, histoplasma, coccidiodes, candida, hypercortisolism

111
Q

clotrimazole, miconazole use

A

for topical fungal infections

112
Q

azole toxicity

A

hormone synthesis inhibition (gynecomastia) liver dysfunction, CYP 450 inhibitor, fever, chills

113
Q

flucytosine mechanism

A

inhibits DNA synthesis by conversion to 5-FU

114
Q

flucytosine use

A

systemic fungal infections in combo with amphotericin B (candida, crypto)

115
Q

flucytosine toxicity

A

nausea, vomiting, diarrhea, bone marrow suppression

116
Q

caspofungin mechanism

A

inhibits cell wall synthesis by inhibiting synthesis of beta glucan

117
Q

caspofungin use

A

invasive aspergillosis

118
Q

caspofungin toxicity

A

GI upset, flushing

119
Q

terbinafine mechanism

A

inhibits fungal squalene epoxidase

120
Q

terbinafine use

A

dermatophytoses (especially onychomycosis)

121
Q

griseofulvin mechanism

A

interferes with microtubule function; disrupts mitosis; deposits in keratin-containing tissues

122
Q

griseofulvin use

A

oral treatment of superficial infections; dermatophytes (tinea, ringworm)

123
Q

griseofulvin toxicity

A

P450 inducer (increases warfarin metabolism), teratogenic, carcinogenic, confusion, headaches

124
Q

pyrimethamine mechanism

A

selectively inhibits plasmodial dihydrofolate reductase (best for . falciparum)

125
Q

pyrimethamine use

A

for toxoplasmosis with sulfadiazine

126
Q

suramin mechanism

A

inhibits enzymes involved in energy metabolism; no CNS involvement

127
Q

suramin use

A

anti-protozoal; blood-borne trypanosoma brucei

128
Q

melarsoprol mechanism

A

inhibits sulfhydryl groups in parasite enzymes; CNS involvement

129
Q

melarsoprol use

A

anti-protozoal, CNS penetration of trypanosoma brucei

130
Q

nifurtimox mechanism

A

forms intracellular oxygen radical that are toxic to the organism

131
Q

sodium stibogluconate mechanism

A

inhibits glycolysis at PFK reaction

132
Q

nifurtimox use

A

anti-protozoal, trypanosoma cruzi

133
Q

sodium stibogluconate use

A

anti-protozoal; leishmania

134
Q

chloroquine mechanism

A

blocks plasmodium heme polymerase, leading to accumulation of hemoglobin breakdown products that destroy the organism

135
Q

mefloquine mechanism

A

unknown

136
Q

chloroquine use

A

malaria

137
Q

mefloquine use

A

chloroquine resistant malaria

138
Q

quinine mechanism

A

unknown, maybe blocks protozoal protein/nuclei acid synthesis

139
Q

quinine use

A

chloroquine resistant malaria when use in combination with pyrimethamine, sulfonamide, babesia

140
Q

mebendazole mechanism

A

inhibits glucose uptake and microtubule synthesis

141
Q

mebendazole use

A

anti-helminthic

142
Q

pyrantel pamoate mechanism

A

stimulates nicotinic receptors at neuromuscular junction; depolarization-induced paralysis; no effect on tapeworms or flukes

143
Q

pyrantel pamoate use

A

anti-helminthic

144
Q

ivermectin mechanism

A

intensifies GABA-mediated neurotransmission and causes immobilization; doesn’t cross BBB (so no effect on humans)

145
Q

ivermectin use

A

anti-helminthic

146
Q

diethylcarbamazine mechanism

A

unknown

147
Q

diethycarbamazine use

A

anti-helminthic

148
Q

praziquantel mechanism

A

increases membrane permeablility to Ca, causing contraction and paralysis in flukes and tapeworms

149
Q

praziquantel use

A

anti-helminthic

150
Q

primaquine use

A

plasmodium vivax and ovale

151
Q

amantadine mechanism

A

blocks viral penetration/uncoating (M2 protein); causes release of dopamine from intact nerve terminals

152
Q

amantidine use

A

Parkinson’s; prophylaxis and treatment for Influenza A (only A!)

153
Q

amantidine toxicity

A

ataxia, dizziness, slurred speech

154
Q

amantidine resistance

A

mutated M2 protein (most Influenza A strains are resistant)

155
Q

zanamivir and oseltamivir mechanism

A

inhibit influenza neuraminidase, decreases progeny release

156
Q

zanamivir and oseltamivir use

A

influenza A and B (give early or as prophylaxis!)

157
Q

ribavirin mechanism

A

inhibits synthesis of guanine nucleosides by competitively inhibiting IMP dephydrogenase

158
Q

ribavirin use

A

RSV, chronic Hep C

159
Q

ribavirin toxicity

A

hemolytic anemia; severe teratogen

160
Q

acyclovir mechanism

A

monophosphorylated by HSV/VZV thymidine kinase; guanosine analog; chain termination of DNA polymerase

161
Q

acyclovir use

A

HSV (mucocutaneous lesions and encephalitis), VZV, EBV; not effective for latent virus; prophylaxis in immunocompromised patients

162
Q

acyclovir toxicity

A

generally well-tolerated

163
Q

acyclovir resistance

A

lack of viral thymidine kinase

164
Q

ganciclovir mechanism

A

Guanosine analog

- Preferentially inhibits viral DNA polymerase (also interferes with human DNA polymerase)

165
Q

ganciclovir use

A

CMV (esp. in immunocompromised patients – HIV)

166
Q

ganciclovir toxicity

A

leukopenia, neutropenia, thrombocytopenia, renal toxicity
(general –> anemia)
(more toxic to host enzymes than Acyclovir)

167
Q

ganciclovir resistance

A

mutated DNA polymerase or lack of viral kinase

168
Q

foscarnet mechanism

A

viral DNA polymerase inhibitor that binds to pyrophosphate binding site of enzyme; doesn’t need activation

169
Q

foscarnet use

A

CMV retinitis when ganciclovir fails; also acyclovir resistant HSV

170
Q

foscarnet toxicity

A

nephrotoxicity

171
Q

foscarnet resistance

A

mutated DNA polymerase

172
Q

saquinavir class

A

protease inhibitor

173
Q

ritonavir class

A

protease inhibitor

174
Q

indinavir class

A

protease inhibitor

175
Q

nelfinavir class

A

protease inhibitor

176
Q

amprenavir class

A

protease inhibitor

177
Q

protease inhibitor mechanism

A

prevent maturation of new viruses (protease cleaves the polypeptide products of HIV mRNA into functional parts)

178
Q

protease inhibitor toxicity

A

hyperglycemia, GI intolerance, lipodystrophy, thrombocytopenia

179
Q

zidovudine class

A

NRTI (nucleoside reverse transcriptase inhibitor)

180
Q

didanosine class

A

NRTI (nucleoside reverse transcriptase inhibitor)

181
Q

zalcitabine class

A

NRTI

182
Q

stavudine class

A

NRTI

183
Q

NRTI mechanism

A

Competitively inhibit nucleotide binding to reverse transcriptase and terminated DNA chain (lack a 3’OH group)
- must be phosphorylated by thymidine kinase (except Tenofovir, which is a nucleoTide analog)

184
Q

zidovudine use

A

HIV general prophylaxis and during pregnancy to reduce risk of fetal transmission

185
Q

NRTI toxicity

A

bone marrow suppression (give EPO and G-CSF), peripheral neuropathy, lactic acidosis, rash, megaloblastic anemia

186
Q

nevirapine class

A

NNRTI

187
Q

efavirenz class

A

NNRTI

188
Q

delaviridine class

A

NNRTI

189
Q

NNRTI mechanism

A

bind to reverse transcriptase at site different from NRTIs; do not need to be phosphorylated for activation

190
Q

NNRTI toxicity

A

bone marrow suppression (give EPO and G-CSF), peripheral neuropathy, lactic acidosis, rash, megaloblastic anemia

191
Q

enfuviritide class

A

fusion inhibitor

192
Q

fusion inhibitor mechanism

A

bind viral gp41 subunit; inhibit conformational change for fusion with CD4 cells; blocks entry and replication

193
Q

enfuvirtide toxicity

A

hypersensitivity reactions, injection site reaction, increased risk of bacterial pneumonia

194
Q

interferon mechanism

A

glycoproteins synthesized by virus-infected cells that blocks replication of viruses

195
Q

interferon use

A

alpha: HBV and HCV, Kaposi’s sarcoma; beta: MS; gamma: NADPH oxidase deficiency

196
Q

interferon toxicity

A

neuropenia

197
Q

antibiotics to avoid in pregnancy

A

fluoroquinolones, sulfonamides, aminoglycosides, metronidazole, tetracyclines, ribavirin, griseofulvin, chloramphenicol

198
Q

HAART therapy

A

2 NRTIs and 1 protease inhibitor or 2 NRTIs and 1 NNRTI

199
Q

Didanosine - toxicity?

A

Pancreatitis

200
Q

Cutaneous drug hypersensitivity such as SJS & TEN are associated w/ what 2 antiretroviral medications?

A

Nevirapine & Efavirenz

.► FARMACOLOGIA CLÍNICA - JP (50 decks)

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