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Pharmacology > Antimicrobials, Antifungals and Antiprotozoal > Flashcards

Antimicrobials, Antifungals and Antiprotozoal Flashcards

1
Q

Inhibition of peptidoglycan crosslinking by blocking transpeptidase

A

Penicillin, cephalosporins, methicillin, ampicillin, piperacillin, aztreonam, imipenem

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2
Q

Inhibit peptidoglycan synthesis

A

Bacitracin, Vancomycin

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3
Q

Damage DNA

A

Metronidazole

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4
Q

Block 30s

A

Aminoglycosides, Tetracyclines

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5
Q

Block 50s

A

Macrolides, Chloramphenicol, Clindamycin, Streptogramins (Quinupristin, dalfopristin), linezolid

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6
Q

Penicillins

A

structural analogs of D-ala, D-ala

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7
Q

Methicillin toxicity

A

Interstitial nephritis

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8
Q

Ampicillin/Amoxicillin HELPSS kill enterococci

A

H. influenzae, E. coli, Listeria, Proteus, Salmonella, Shigella, enterococci

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9
Q

Beta-lactamase producers

A

Staph. aureus, H. influenzae, Bacteroides, other Gram -ve bacteria

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10
Q

1st generation cephalosporins

A

Cefazoline, Cephalexin: gram +ve cocci- Proteus, E. coli, Klebsiella pneumoniae

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11
Q

1st generation cephalosporins

A

prophylactically used within 2 hr of the first incision during surgery

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12
Q

2nd generation cephalosporin

A

Cefoxitin, Cefaclor, Cefuroxime: Gram +ve cocci- H. influenzae, Enterobacter aerogenes, Neisseria, Proteus, E. coli, Klebsiella, Serratia

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13
Q

3rd generation cephalosporin

A

Ceftriaxone, Cefotaxime, Ceftazidime: Better activity against Gram -ve bacteria due to Beta-lactamase resistant properties

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14
Q

3rd generation cephalosporin

A

Ceftriaxone: meningitis and gonorrhea; Ceftazidime: Pseudomonas

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15
Q

4th generation cephalosporin

A

Cefepime: Pseudomonas and Gram +ve organisms

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16
Q

Cefamandole

A

Disulfiram-like reaction

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17
Q

Cephalosporine toxicity

A

Increased nephrotoxicity of Aminoglycosides

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18
Q

Aztreonam

A

inhibits cell wall synthesis by binding to PBP3, Beta-lactamase resistant; synergistic with aminoglycosides

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19
Q

Activity against Gram -ve rods only

A

Aztreonam

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20
Q

For penicillin allergic patients and those with renal insufficiency who cannot tolerate aminoglycosides

A

Aztreonam

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21
Q

Imipenem

A

Inhibits cell wall synthesis by binding to PBP; Beta-lactamase resistant

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22
Q

Imipenem

A

Broad spectrum- Gram +ve cocci, Gram -ve rods, anaerobes

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23
Q

Always administered with Cilastatin

A

Imipenem (Cilastatin is inhibitor of renal dihydropeptidase-I, an enzyme which inactivates imipenem in renal tubules)

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24
Q

Imipenem toxicity

A

Seizures

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25
Q

Meropenem

A

Reduced risk of seizures and stable to dihydropeptidase-I

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26
Q

Binds to D-ala D-ala and inhibits cell wall mucopeptide formation

A

Vancomycin

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27
Q

Vancomycin

A

Used for multidrug resistance

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28
Q

Vancomycin toxicity (NOT)

A

Nephrotoxicity, Ototoxicity, Thromnbophlebitis, Flushing

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29
Q

Red man syndrome

A

Vancomycin due to histamine release; pretreat with antihistamines

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30
Q

Vancomycin resistance

A

Plasmid/Transposon acquired: Van A ligase substitutes D-lactate for D-alanine that prevents binding of vancomycin to its binding site

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31
Q

Prevents muco-peptide transfer into growing cell wall

A

Bacitracin

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32
Q

Depolarization of cellular membrane by disrupting bacterial membrane through creation of transmembrane channels

A

Daptomycin

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33
Q

Daptomycin (lipopeptide)

A

treatment for invasive MRSA

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34
Q

Inactivated by surfactant thus ineffective for pneumonia

A

Daptomycin

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35
Q

Daptomycin- Adverse reactions

A

Myopathy, CPK elevation

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36
Q

Linezolid

A

Inhibits protein synthesis: Binds to 50s and prevents formation of functional initiation complex

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37
Q

Linezolid- Adverse reactions

A

Thrombocytopenia, Optic neuritis, Serotonin syndrome

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38
Q

Antibiotic with high risk for serotonin syndrome

A

Linezolid

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39
Q

Require O2 for uptake therefore ineffective against anaerobes

A

AminOglycosides

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40
Q

Aminoglycosides: MOA

A

Inhibit formation of initiation complex, cause misreading of mRNA

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41
Q

Resistance to aminoglycosides

A

Acetylation, phosphorylation or adenylation- plasmid/transposon acquired; In pseudomonas- decreased entry into bacteria

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42
Q

Aminoglycosides

A

Gram -ve rods

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43
Q

Aminoglycosides toxicity

A

Nephrotoxicity (increase with cephalosporin), Ototoxicity (when used with loop diuretcis), Teratogens

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44
Q

Gentamicin in large doses or intrapleurally

A

Neuromuscular paralysis

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45
Q

Tetracyclines: MOA

A

bind to 30s and inhibit binding of aminoacyl-tRNA to A-site

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46
Q

Tetracycline clinical use

A

Borrelia, Mycoplasma, Rickettsia, Chlamydia

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47
Q

Tetracyclines toxicity

A

Discoloration of teeth, inhibition of bone growth in childern, photosensitivity

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48
Q

Tetracyclines resistance

A

Efflux pump

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49
Q

Doxycycline

A

fecal elimination, can be given in patients with renal failure

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50
Q

Doxycycline side effects

A

photosensitivity, pill-induced esophagitis

51
Q

Pill-induced esophagitis

A

Doxycycline

52
Q

Divalent cations inhibit their absorption in gut (e.g. milk, antacids or iron-containing preps)

A

Tetracyclines

53
Q

A tetracycline used as a diuretic in SIADH

A

Demeclocycline- ADH antagonist

54
Q

Macrolides

A

inhibit translocation by binding to 23s rRNA of the 50s ribisomal subunit

55
Q

Macrolides

A

Atypical pneumonia

56
Q

Erythromycin

A

Prolong QT, acute cholestatic hepatitis, eosinophilia, skin rashes

57
Q

Macrolides

A

Inhibit p450 - increase serum concentrations of theophyllines and oral anticoagulants

58
Q

Macrolide resistance

A

Efflux pump, methylation of 23s rRNA binding site

59
Q

Macrolide noncompliance

A

MCC GI discomfort

60
Q

Inhibits peptidyltransferase thus blocking peptide bond formation

A

Chloramphenicol

61
Q

Chloramphenicol side effects

A

Anemia (dose-dependent), Aplastic anaemia (dose-independent), Gray Baby Syndrome (premature infants lack UDP-glucuronyltransferase)

62
Q

Chloramphenicol resistance

A

plasmid-encoded acetyltransferase inactivates drug

63
Q

Clindamycin

A

inhibit translocation (50s)

64
Q

Anaerobic infections

A

Above the diaphragm- clindamycin; below- metronidazole

65
Q

Clindamycin

A

Rx for aspiration pneumonia or lung abscesses

66
Q

Clindamycin side effect

A

Pseudomembranous colitis

67
Q

Inhibit dihydropteroate synthase (PABA antimetabolites)

A

Sulfonamides (Sulfamethoxazole, Sulfisoxazole, Sulfadiazine)

68
Q

Inhibit dihydrofolate reductase

A

Trimethoprim

69
Q

Sulfonamides side effects

A

Hypersensitivity, hemolysis in G6-PD deficiency, nephrotoxicity (tubulointerstitial nephritis), photosensitivity, kernicterus in infants, displace other drugs from albumin (e.g. warfarin)

70
Q

Trimothoprim side effects

A

Megaloblastic anemia, leukopenia, granulocytopenia, hyperkalemia, toxic epidermal necrolysis, Stevens-Johnson syndrome

71
Q

In high doses (e.g. to treat pneumocystis in AIDS), can act as a K-sparing diuretic–Hyperkalemia

A

Trimethoprim

72
Q

Inhibit DNA-gyrase (topoisomerase-II) and induce fractures in bacterial chromosome

A

Fluoroquinolones

73
Q

Must not be taken with antacids

A

Fluoroquinolones and Tetracyclines

74
Q

Fluoroquinolones side effects

A

Adults: damage to cartilage, tendonitis and tendon rupture; Kids: leg cramps and myalgia

75
Q

Binds to DNA–> unravels DNA helical structure–> breaks DNA strands (DNA damage)

A

Metronidazole

76
Q

Pyridoxine (Vit B6 analogue)

A

INH

77
Q

Bacterial catalase-peroxidase (KatG) needed to form active drug

A

INH

78
Q

INH side effects

A

Neurotoxicity, Seizures, Hepatotoxicity, drug-induced lupus

79
Q

INH resistance

A

Decreased activity of bacterial catalase peroxidase; modification of protein target binding site for INH

80
Q

Drugs metabolized by Acetylation

A

INH, Dapsone, Hydralazine, Proacainamide

81
Q

anti- TB drug that prevents transcription of DNA into mRNA

A

Rifampin

82
Q

Rifampin: MOA

A

Inhibits DNA-dependent RNA-polymerase (Primase)

83
Q

Drug used for meningococcal prophylaxis and for chemoprophylaxis in contacts of children with H. influenzae type B

A

Rifampin

84
Q

Rifampin: side effects

A

Amplifies P-450 (RifAMPin), Red/Orange body fluids

85
Q

Rifampin + Vancomycin

A

MRSA endocarditis

86
Q

Staph. endocarditis

A

Nafcillin + Gentamycin

87
Q

anti-TB drug that inhibits mycolic acid production by blocking mycobacterial pyrazinamidase

A

Pyrazinamide

88
Q

anti-TB drug that works best at low pH (acidic) hence effective against intracellular (mycobacteria in phagolysosomes within macrophages) organisms.

A

Pyrazinamide

89
Q

Drug that delays resistance to Dapsone in leprosy patients

A

Rifampin

90
Q

Pyrazinamide side effects

A

Hyperuricemia, Hepatotoxicity

91
Q

anti-TB drug that decreases carbohydrate polymerization of mycobacterial cell wall by blocking arabinosyltransferase

A

Ethambutol

92
Q

Ethambutol toxicity

A

Red-green color blindness, decreased visual acuity, central scotoma

93
Q

Resistance mechanism by increasing activity of enzymes involved in cell wall polysaccharide synthesis

A

Ethambutol resistance

94
Q

Empiric therapy for community-acquired pneumonia

A

Outpatient: Macrolide; Inpatient: Fluoroquinolone; ICU: Beta-lactam + fluoroquinolone or azithromycin

95
Q

Binds ergosterole–> pokes holes

A

Amphotericin B

96
Q

Amphotericin B

A

serious systemic mycosis; intrathecally for fungal meningitis; supplement with potassium and magnesium

97
Q

Amphotericin B toxicity

A

fever and chills, hypotension, nephrotoxicity, arrythmia, anemia, IV phlebitis; hydration reduces nephrotoxicity

98
Q

Amphotericin B

A

Hypokalemia–> weakness and arrhythmia; T-wave flattening, ST-depression, prominent U-wave, premature atrial and ventricular contractions; ventricular tachycardia or fibrillation

99
Q

Amphotericin B

A

severe toxicity (anemia) in HIV +ve patient taking AZT (Zidovudine)

100
Q

Premedicate with antipyretic and antihistaminics for this antifungal drug

A

Amphotericin B

101
Q

antifungal drug causing toxicity due to binding to human cell membrane cholesterol

A

Amphotericin B

102
Q

antifungals that inhibit ergosterol synthesis by inhibiting p-450 and thus blocking conversion of lanosterol to ergosterol

A

Azoles

103
Q

Cryptococcal meningitis in AIDS: DOC

A

Fluconazole

104
Q

drug that blocks synthesis of hormones and causes gynecomastia

A

Ketoconazole

105
Q

antifungal drug used in hypercortisolism

A

Ketoconazole

106
Q

Azole side effect

A

Liver dysfunction, gynecomastia and p-450 inhibition

107
Q

Avoid these drugs with azoles

A

warfarin, oral hypoglycemics, cyclosporine, tacrolimus, phenytoin, INH, Rifampin

108
Q

antifungal that inhibits both fungal DNA and RNA

A

Flucytosine

109
Q

Flucytosine toxicity

A

Bone marrow suppression

110
Q

antifungal that inhibits cell wall synthesis by inhibiting 1,3-Beta-D-glucan (major polysaccharide component of fungal cell wall

A

Caspofungin

111
Q

DOC for invasive aspergillosis

A

Caspofungin (CAsper)

112
Q

Caspofungin toxicity

A

Flushing

113
Q

antifungal that inhibits the fungal enzyme Squaline epoxide and thus decreases ergosterol synthesis

A

Terbinafine

114
Q

drug to treat dermatophytosis especially onychomycosis

A

Terbinafine

115
Q

Terbinafine side effects

A

Abnormal LFTs, visual disturbances

116
Q

antifungal that interferes with microtubule function and disrupts mitosis

A

Griseofulvin

117
Q

antifungal that revs up cytpchrome P450 and increases warfarin metabolism that further decreases effectiveness of warfarin and requires to increase the dosage of warfarin

A

Griseofulvin

118
Q

Griseofulvin side effects

A

Teratogenic, Headache

119
Q

Rx for Toxoplasmosis or P. falciparum

A

Pyrimethamine

120
Q

Rx for T. brucei

A

Suramin and Melarsoprol

121
Q

Rx for T. cruzi

A

Nifurtimox

122
Q

Rx for Cryptosporidiosis

A

Nitazoxanide

123
Q

Rx for leishmaniasis

A

Sodium stibogluconate

Pharmacology (5 decks)

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