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Pharmacology > Microbe drugs > Flashcards

Microbe drugs Flashcards

1
Q

Penicillin G, V (mechanism and resistance)

A

Beta-lactam antibiotics (penicillinase-sensitive) -> bactericidal
Structural analog of D-Ala-D-Ala -> binds PBP (penicillin-binding proteins) -> covalently binds transpeptidase -> blocks X-linking of peptidoglycan -> blocks cell wall synthesis
Resistance: structural changes in PBP

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2
Q

Penicillin G, V (3 uses)

A

G+ orgs (S pneumoniae, S. pyogenes, Actinomyces)
G- cocci (incld N. meningitidis)
Spirochetes (incl T. pallidum)

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3
Q

Penicillin G, V (3 side effects)

A

Hypersensitivity
Hemolytic anemia
Resistance in bacteria w/ beta-lactamase (MRSA)

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4
Q

Ampicillin, amoxicillin (mechanism)

A 
Beta-lactam antibiotics (aminopenicillines, still penicillinase-sensitive so used w. clavulanic acid) -> bactericidal
Binds PBP (penicillin-binding proteins; transpeptidases) -> blocks X-linking of peptidoglycan -> blocks cell wall synthesis
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5
Q

Ampicillin, amoxicillin (uses)

A

Added spectrum from normal penicillins -> HELPSS enterococci (H. influenzae, E. coli, L. monocytogenes, P. mirabilis, Salmonella, Shigella)

Nornal penicillin spectrum:
G+ orgs (S pneumoniae, S. pyogenes, Actinomyces)
G- cocci (incld N. meningitidis)
Spirochetes (incl T. pallidum)

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6
Q

Ampicillin, amoxicillin (3 side effects)

A

Pseudomembranous colitis
Hypersensitivity, rash
Resistance in bacteria w/ beta-lactamase (MRSA)

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7
Q

Oxacillin, nafcillin, dicloxacillin (mechanism)

A

Beta-lactam antibiotics (penicillinase-resistant - bulky R group blocks access of beta lactamase) -> bactericidal
Binds PBP (penicillin-binding proteins; transpeptidases) -> blocks X-linking of peptidoglycan -> blocks cell wall synthesis
This means any resistance is from ALTERED PBP, NOT beta lactamase

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8
Q

Oxacillin, nafcillin, dicloxacillin (use)

A

Nafcillin for MSSA

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9
Q

Oxacillin, nafcillin, dicloxacillin (2 side effects)

A

Interstitial nephritis

Hypersensitivity

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10
Q

Ticarcillin, piperacillin (mechanism)

A 
Beta-lactam antibiotics (anti-pseudomonals, still penicillinase-sensitive so used w. clavulanic acid) -> bactericidal
Binds PBP (penicillin-binding proteins; transpeptidases) -> blocks X-linking of peptidoglycan -> blocks cell wall synthesis
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11
Q

Ticarcillin, piperacillin (2 uses)

A

Pseudomonas

G- rods, including ANAEROBES (so good for bacterioids)

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12
Q

Ticarcillin, piperacillin (side effect)

A

Hypersensitivity

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13
Q

Clavulanic acid (mechanism and use)

A

Beta lactamase inhibitor

Added to penicillinase-sensitive penicillin antibiotics

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14
Q

Sulbactam (mechanism and use)

A

Beta lactamase inhibitor

Added to penicillinase-sensitive penicillin antibiotics

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15
Q

Tazobactam (mechanism and use)

A

Beta lactamase inhibitor

Added to penicillinase-sensitive penicillin antibiotics

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16
Q

Cephalosporins (mechanism and resistance)

A 
Beta-lactam antibiotics (but less susceptible to penicillinases) -> bactericidal
Binds PBP (penicillin-binding proteins; transpeptidases) -> blocks X-linking of peptidoglycan -> blocks cell wall synthesis
Resistance: structural changes in PBP
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17
Q

1st gen cephalosporins (2 names and 3 uses)

A

“Jeremy LIN drives LEX” -> cefazoLIN, cephaLEXin
G+ cocci
PEcK: P. mirabilis, E. coli, Klebsiella pneumoniae
Cefazolin used pre-op to prevent S. aureus wound infections

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18
Q

List orgs not covered by cephalosporins

A

“LAME” -> Listeria, Atypicals (Chlamydia, Mycoplasma), MRSA (except ceftaroline), Enterococci

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19
Q

2nd gen cephalosporins (3 names and 2 uses)

A

“Two make her happy, buy some Fake Fox Fur” -> ceFOXitin, ceFAClor, ceFURoxime
G+ cocci
HEN PEcKs: H. influenzae, Enterobacter aerogenes, Neisseria spp, P. mirabilis, E. coli, Klebsiella pneumoniae, Serratia marcescens

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20
Q

3rd gen cephalosporins (3 names and 3 uses)

A

“Tri, Tax, Taz” -> cefTRIaxone, cefoTAXime, cefTAZidime
Serious G– infections resistant to other beta lactams
Ceftrixone - meningitis and gonorrhea
Ceftaxidime - pseudomonas

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21
Q

4th gen cephalosporin (1 name and 2 uses)

A

Cefepime

Increased activity against Pseudomonas & G+

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22
Q

5th gen cephalosporin (1 name and 2 uses)

A

Ceftaroline
Broad G+ (incl MRSA - the only one of cephalosporins that does this)
Broad G-
Does NOT cover Pseudomonas tho

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23
Q

Cephalosporin (3 side effects)

A

Vit K deficiency
Increases nephrotoxicity of amonoglycocides
Hypersensitivity (cross-reactivity w/ penicillins)

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24
Q

Aztreonam (mechanism)

A

Monobactam (resistant to beta lactamases)
Binds to PBP3 -> prevents peptidoglycan X-linking -> inhibits cell wall synthesis
Synergistic w/ aminoglycoside

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25
Q

Aztreonam (use)

A

G- rods only, for penicillin-allergic and those w/ renal insufficiency (can’t tolerate aminoglycosides)
Can’t use for G+ or anaerobes

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26
Q

Aztreonam (side effect)

A

GI upset, but usually non-toxic (don’t even have cross-allergenicity w/ penicillins)

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27
Q

“-penems” (mechanism)

A

Carbapenems: imipenem, meropenem, ertapenem, doripenem
Peptidoglycan X-linking inhibitor -> inhibits cell wall synthesis
Use imipenem w/ cilastatin (competitively inhibits renal dehydropeptidase I -> inhibits inactivation of drug in renal tubules)
Meropenem is stable to renal dehydropeptidase I

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28
Q

“-penems” (3 uses)

A

Wide spectrum but only for life-threatening infections (significant side effects)
G+ cocci
G- rods
Anaerobes

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29
Q

“-penems” (3 side effects)

A

Seizures (meropenem has lower risk)
Skin rash
GI distress

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30
Q

Vancomycin (mechanism)

A

Binds D-ala D-ala portion of cell wall precursors -> inhibits cell wall peptidoglycan formation (prevents transpeptidation)
Bactericidal
Resistance thru plasmid/transposon-mediated modification of D-ala D-ala to D-ala D-lac

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31
Q

Vancomycin (3 uses)

A

G+ only -> serious, multidrug-resistant orgs -> MRSA, enterococci, Clostridium difficile (oral for pseudomembranous colitis)

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32
Q

Vancomycin (side effects)

A 
Well-tolerated in general but can have:
Nephrotoxicity
Ototoxicity
Thrombophlebitis
Red man syndrome (diffuse flushing, prevented by pretreatment w/ antihistamines and slow infusion rate -> this is mediated by histamines NOT IgE like penicillins or prostaglandins like niacin!)
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33
Q

Aminoglycosides (mechanism)

A 
GNATS: Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin -> don't confuse suffix w/ macrolides
30S inhibitor (bacterial ribosome) -> inhibits protein synthesis (causes misreading of mRNA, blocks translocation)
Bactericidal
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34
Q

Aminoglycosides (2 uses)

A

GNATS: Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin
Severe G- rods (synergistic w/ beta-lactam antibiotics)
Neomycin for bowel surgery
Requires O2 for uptake so ineffective against anaerobes

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35
Q

Aminoglycosides (side effects)

A

GNATS: Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin
NNOT: Nephrotoxicity (esp w/ cephalosporins; ATN), Neuromuscular blockade (flaccid paralysis), Ototoxicity (esp w/ loop diuretics), Teratogen

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36
Q

Aminoglycosides (resistance)

A

GNATS: Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin
Plasmids/transposons encode bacterial transferase enzymes inactivate drug by acetylation, phosphorylation, or adenylation

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37
Q

“-cycline” (mechanism)

A 
Tetracycline, doxycycline, minocycline
30S inhibitor (bacterial ribosome) -> inhibits protein synthesis (prevents attachment of aminoacyl-tRNA)
Bacteriostatic
Limited CNS penetration
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38
Q

“-cycline” (4 uses)

A

Borrelia burgdorferi
M. pneumoniae
Acne
Intracellular bac: Rickettsia, Chlamydia

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39
Q

“-cycline” (side effects)

A

Pseudotumor cerebri in teens using tetracycline for acne
Teeth discoloration
GI distress
Inhibits bone growth in children
Photosensitivity
Can’t use in pregnancy
Don’t take w/ milk, antacids, or iron-containing stuff b/c divalent cations inhibit absorption in gut
Can use doxycycline w/ renal failure (fecally eliminated)

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40
Q

“-cycline” (resistance)

A

Plasmid-encoded transport pumps decrease uptake and increase efflux

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41
Q

Macrolides (mechanism)

A 
Azithromycin, clarithromycin, erythromycin -> don't confuse suffix w/ aminoglycosides
50S inhibitor (bacterial ribosome) -> inhibits protein synthesis (blocking translocation)
Bacteriostatic
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42
Q

Macrolides (4 uses)

A

Azithromycin, clarithromycin, erythromycin
Atypical pneumonias (Mycoplasma, Chlamydia, Legionella)
M. avium-intracellulare (used prophylactically when CD4 < 50 cells/mm3 in HIV)
STDs (erythromycin ointment used to prevent conjunctivitis in newborn)
G+ cocci (strep infections in pts allergic to penicillin)

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43
Q

Macrolides (side effects)

A

Azithromycin, clarithromycin, erythromycin
MACRO: gi Motility issues, Arrhythmia caused by prolonged qt, acute Cholestatic hepatitis, Rash, eOsinophilia
Increases serum conc of theophyllines and oral anticoagulants

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44
Q

Macrolides (resistance)

A

Methylation of 23S rRNA-binding site

Transmembrane efflux pumps

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45
Q

Chloramphenicol (mechanism)

A 
50S inhibitor (bacterial ribosome) -> inhibits protein synthesis (blocks peptidyltransferase)
Bacteriostatic
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46
Q

Chloramphenicol (2 uses)

A

Limited b/c of toxicities but used in developing countries b/c of low cost
Meningitis (H. influenzae, Neisseria, Strep pneumoniae)
Rocky mountain spotted fever

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47
Q

Chloramphenicol (side effects)

A

Anemia, aplastic anemia

Gray baby syndrome in premies (lacking liver UDP-glucuronyl transferase)

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48
Q

Chloramphenicol (resistance)

A

Plasmid-encoded acetyltransferase inactivates drug

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49
Q

Clindamycin (mechanism)

A 
50S inhibitor (bacterial ribosome) on 23S site (same as macrolides) -> inhibits protein synthesis (blocks translocation/peptide transfer)
Bacteriostatic
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50
Q

Clindamycin (2 uses)

A

Anaerobic infections ABOVE diaphragm (Bacteroides, C. perfringens) - aspiration pneumonia, lung abscesses, oral infections (below diaphragm use metronidazole)
Group A strep

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51
Q

Clindamycin (3 side effects)

A

Pseudomembranous colitis
Fever
Diarrhea

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52
Q

Sulfonamides (mechanism and resistance)

A

Sulfamethoxazole (SMX), sulfisoxazole, sulfadiazine
Inhibits bacterial dihydropteroate synthase -> inhibits folate synthesis (can’t go from PABA to DHF)
Bacteriostatic
Resistance - altered enzyme

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53
Q

Sulfonamides (5 uses)

A 
Sulfamethoxazole (SMX), sulfisoxazole, sulfadiazine
G+
G-
Nocardia
Chlamydia
Simple UTI (triple sulfas or SMX)
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54
Q

Sulfonamides (6 side effects)

A

G6PD hemolysis
Nephrotoxicity (tubulointerstitial nephritis)
Photosensitivity
Hypersensitivity
Kernicterus in infants
Displaces other drugs from albumin (like warfarin)

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55
Q

Trimethoprim, Pyrimethamine (mechanism and resistance)

A

Inhibits bacterial dihydrofolate reductase -> inhibits folate synthesis (can’t go from DHF to THF, basically one step after sulfonamides)
Bacteriostatic
Resistance: salvage metabolic pathway

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56
Q

Trimethoprim, Pyrimethamine (5 uses)

A 
TMP-SMX combo for 
UTIs
Shigella, Salmonella
Pneumocystis jirovecii (AIDs prophylaxis when CD4 < 200 cells/mm3)
Malaria
Pneumonia tx and prophylaxis
Toxoplasmosis prophylaxis
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57
Q

Trimethoprim, Pyrimethamine (3 side effects)

A

TMP = Treats Marrow Poorly (allevaited w/ supplemental folinic acid)
Megaloblastic anemia
Leukopenia
Granulocytopenia

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58
Q

“-oxacin” (mechanism)

A

Fluoroquinolones
Inhibits DNA gyrase (topoisomerase II) and topoisomerase IV
Bactericidal

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59
Q

“-oxacin” (4 uses)

A

G- rods of urinary and GI tracts (ciprofloxacin and levofloxacin food for Pseudomonas)
Neisseria
Some G+
Moxifloxacin mainly for infections that cause exacerbation of COPD, sinusitis, CAP (poor anti-pseudomonal)
INEFFECTIVE against anaerobes

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60
Q

“-oxacin” (4 side effects)

A

Can’t take w/ antacids
SBJ stuff: tendonitis, rupture (esp elderly or taking prednisone), leg cramps, myalgia
QT prolongation in some
CI in pregnant, nursing mothers, and children (damage to cartilage)

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61
Q

“-oxacin” (3 resistance mechanisms)

A

Chr-encoded mutation in DNA gyrase
Plasmid-mediated resistance
Efflux pumps

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62
Q

Linezolid (mechanism)

A

Inhibits 50S bacterial ribosome -> prevents formation of initiation complex -> inhibits protein synthesis

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63
Q

Metronidazole (mechanism)

A

Forms free radical toxic metabolites that damage bacterial DNA
Bactericidal

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64
Q

Metronidazole (6 uses)

A

Antiprotozoal & antibacterial
GET GAP -> Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, Anaerobes (below diaphragm, as opposed to clindamycin which treats above diaphragm), Pylori (part of triple therapy w/ PPI and chlarithromycin)

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65
Q

Metronidazole (3 side effects)

A

Disulfiran-like rxn w/ alcohol (severe flushing, tachycardia, hypotension)
Headache
Metallic taste

66
Q

Isoniazid (INH) (mechanism)

A

Decreases synthesis of mycolic acids -> so LOSES ACID-FASTNESS
Need bacterial catalase-peroxidase (encoded by KatG) to convert to active metabolite
Chemically related to pyridoxine (B6)

67
Q

Isoniazid (INH) (use)

A

TB (as part of RIPE tx w/ Rifampin, INH, Pyrazinamide, Ethambutol)

68
Q

Isoniazid (INH) (side effects)

A

Diff HL bet. fast and slow acetylators
Neurotoxicity (prevented w/ pyrdoxine/B6)
Hepatotoxicity
Acquired sideroblastic anemia (depleting B6 which is required in the rate-limiting step of heme synthesis - ALA synthetase)

69
Q

Nalidixic acid (mechanism)

A

Quinolone
Inhibits DNA gyrase (topoisomerase II) and topoisomerase IV
Bactericidal

70
Q

Nalidixic acid (3 uses)

A

G- rods of urinary and GI tracts (incl Pseudomonas)
Neisseria
Some G+

71
Q

Nalidixic acid (4 side effects)

A

Can’t take w/ antacids
SBJ stuff: tendonitis, rupture (esp elderly or taking prednisone), leg cramps, myalgia
QT prolongation in some
CI in pregnant, nursing mothers, and children (damage to cartilage)

72
Q

Nalidixic acid (3 resistance mechanisms)

A

Chr-encoded mutation in DNA gyrase
Plasmid-mediated resistance
Efflux pumps

73
Q

Rifamycins (mechanism)

A

Rifampin, rifabutin

Inhibits DNA-dependent RNA polymerase

74
Q

Rifamycins (3 uses)

A

Rifampin, rifabutin
TB (as part of RIPE tx w/ Rifampin, INH, Pyrazinamide, Ethambutol)
Leprosy (delays resistance to dapsone for tuberculoid form; adds in clofazimine for lepromatous form)
M. avium-intracellulare (rifabutin)
Meningococcal prophylaxis in contacts of children w. HiB

75
Q

Rifamycins (side effects)

A

Rifampin, rifabutin
Drug interactions (rifampin is an inducer of P450, so use rifabutin in HIV pts)
Orange body fluids! (stains contact lenses)
Minor hepatotoxicity

76
Q

Pyrazinamide (mechanism)

A

Acidify intracellular environment via conversion to pyrazinoic acid (TB engulfed by macrophages are found in acidic phagolysosomes) -> so only one of TB drugs that works best against intracellular TB
Need BACTERIAL ENZYME pyrazinamidase for this conversion!

77
Q

Pyrazinamide (use)

A

TB (as part of RIPE tx w/ Rifampin, INH, Pyrazinamide, Ethambutol) -> pyrazinamide good against INTRACELLULAR TB (unlike other ones listed which are good for extracellular TB)

78
Q

Pyrazinamide (2 side effects)

A

Hyperuricemia

Hepatotoxicity

79
Q

Ethambutol (mechanism)

A

Blocks arabinosyltransferase -> decreases carbohydrate polymerization of mycobacterium cell wall

80
Q

Ethambutol (use)

A

TB (as part of RIPE tx w/ Rifampin, INH, Pyrazinamide, Ethambutol)

81
Q

Ethambutol (side effect)

A

Red-green color blindness

82
Q

Linezolid (3 side effects)

A

Serotonin syndrome
Thrombocytopenia
Optic neuritis

83
Q

Linezolid (2 uses)

A

MRSA (along w/ vancomycin and daptomycin), VRE

84
Q

“-pristin” (mechanism and use)

A

Streptogramins: quinupristin, dalfopristin
50S inhibitor -> inhibits protein synthesis
Used for VRE

85
Q

Isoniazid (INH) (resistance)

A

Decreased activity of bacterial catalase peroxidase (can’t activate the drug)

86
Q

Amphotericin B (mechanism and resistance)

A 
Binds ergosterol (unique to fungi) to form membrane pores -> leakage of electrolytes
Resistance from decreased incorporation of ergosterol into cell membrane
87
Q

Amphotericin B (6 uses)

A 
Serious systemic mycoses:
Cryptococcus (w/ or w/out flucytosine for meningitis)
Bastomyces
Coccidioides
Histoplasma
Candida
Mucor
88
Q

Amphotericin B (5 side effects)

A

Infusion-related rxns (prevent w/ antipyretics and antihistamines: shake and bake (fever/chills), hypotension
Nephrotoxicity (prevented by hydration and supplement K+ and Mg2+ b/c of altered renal tubule permeability -> ALWAYS TRACK THESE 2 IONS)
Arrhythmias (from kidney messing up -> lower K+)
Anemia (from suppression of EPO)
IV phlebitis
Liposomal amphotericin reduces toxicity

89
Q

Nystatin (mechanism and resistance)

A 
Binds ergosterol (unique to fungi) to form membrane pores -> leakage of electrolytes
Topical only (too toxic for systemic)
Resistance from decreased incorporation of ergosterol into cell membrane
90
Q

Nystatin (2 uses)

A

Topical for
Candidiasis: oral (swish and swallow) or vaginal -> 1st line for oral candidiasis in pts WITHOUT advanced immunodeficiency
Diaper rash

91
Q

“-nazole” or “-mazole” (mechanism)

A

Fluconazole, ketoconazole, clotrimazole, miconazole, itraconazole, voriconazole
Inhibits lanosterol 14a-demethylase (P450 enzyme) that converts lanosterol to ergosterol -> so inhibits ergosterol synthesis -> inhibits cell membrane synthesis

92
Q

“-nazole” or “-mazole” (3 uses)

A

For less serious systemic mycoses
Fluconazole: HIV-assc cryptococcal meningitis, candidal infections of all types
Itraconazole for Blastomyces, Coccidioides, Hitoplasma
Clotrimazole and miconazole for topical fungal infections (oral thrush)

93
Q

“-nazole” or “-mazole” (side effects)

A 
Gynecomastia esp w/ ketoconazole bc it inhibits testosterone synthesis
Liver dysfx (bc it inhibits cytochrome P450)
94
Q

Flucytosine (mechanism)

A

Converted by cytosine deaminase to 5-fluorouracil

Interferes w/ thymidylate synthetase -> inhibits DNA and RNA synthesis

95
Q

Flucytosine (2 uses)

A

Systemic fungal infections

Combo w/ amphotericin B to treat meningitis caused by Cryptococcus

96
Q

Flucytosine (side effects)

A

Bone marrow suppression (CI in HIV pts)

97
Q

“-fungin” (mechanism)

A

Echinocandins: caspofungin, micafungin, anidulafungin

Inhibits beta glucan synthesis -> inhibits fungal cell wall synthesis

98
Q

“-fungin” (2 uses)

A

Invasive aspergillosis

Candida

99
Q

“-fungin” (2 side effects)

A

GI upset

Flushing (by histamine release)

100
Q

Terbinafine (mechanism)

A

Inhibits fungal enzyme squalene epoxidase -> so inhibits lanosterol synthesis (precursor to ergosterol) -> inhibits cell membrane synthesis

101
Q

Terbinafine (use)

A

Dermatophytoses (esp onychomycosis, tinea corporis)

102
Q

Terbinafine (4 side effects)

A

GI upset
Headaches
Hepatotoxicity
Taste disturbance

103
Q

Griseofulvin (mechanism)

A

Interferes w/ microtubule fx -> disrupts fungal mitosis -> concentrated in keratin-containing tissues (nails, stratum corneum)

104
Q

Griseofulvin (2 uses)

A

Oral for superficial fungal infections

Dermatophytes (tinea, ringworm)

105
Q

Griseofulvin (4 side effects)

A

Teratogenic
Carcinogenic
Confusion/headaches
Induces P450 and warfarin metab

106
Q

Pyrimethamine (use)

A

Toxoplasmosis

107
Q

Suramin (use)

A

Trypanosoma brucei

108
Q

Melarsoprol (use)

A

Trypanosoma brucei

109
Q

Nifurtimox (use)

A

T. cruzi

110
Q

Sodium stibogluconate (use)

A

Leishmaniasis

111
Q

Chloroquine (mechanism)

A

Blocks Plasmodium heme polymerase -> blocks detox of heme into hemozoin -> heme accumulates and becomes toxic to plasmodia

112
Q

Chloroquine (use)

A

For erythrocytic forms (like mefloquine)

Plasmodial species other than P. falciparum (high resistance -> from membrane pump that decrease intracel conc of drug)

113
Q

Chloroquine (2 side effects)

A

Retinopathy!

Pruritus (esp in dark-skinned individuals)

114
Q

Artemether/lumefantrine (use)

A

P. falciparum

115
Q

Atovaquone/proguanil (use)

A

P. falciparum

Atovaquone + azithromycin for Babesia

116
Q

Quinidine (use)

A

Life-threatening malaria

Use quinine in other countries

117
Q

Artesunate (use)

A

Life-threatening malaria

118
Q

Praziquantel (mechanism and 2 uses)

A

Immobilize helminths
For
Flukes (trematodes): all of them -> Schistosoma, Clonorchis sinensis
Tapeworms (cestodes): all of them except for Echinococcus -> so Taenia solium (but use albendazole for neurocysticercosis), diphyllobothrium latum (fish)

119
Q

“-bendazole” (mechanism and 3 uses)

A

Immobilize helminths (acts on microtubules)
For
Intestinal roundworms (nematodes): all of them except for Strongyloides -> so enterobius vermicularis (pinworm), ascaris lumbricoides (giant roundworm), strongyloides stercoralis (threadworm), ancylostoma duodenale & necator americanus (hookworms), trichuris trichulura (whipworm)
Tissue roundworms (nematodes): toxocara canis
Tapeworms (cestodes): echinococcus granulosus, taenia solium (for neurocysticercosis)

120
Q

Pyrantel pamoate (mechanism and use)

A

Immobilize helminths, for pregnant (second line after bendazoles)
For intestinal roundworms (nematodes): all of them except for Strongyloides -> so enterobius vermicularis (pinworm), ascaris lumbricoides (giant roundworm), ancylostoma duodenale & necator americanus (hookworms)

121
Q

Ivermectin (mechanism and 2 uses)

A 
Immobilize helminths
For
Intestinal roundworms (nematodes): strongyloides stercoralis (threadworm)
Tissue roundworms (nematodes): onochocerca volvulus (river blindness)
122
Q

Diethylcarbamazine (mechanism and uses)

A 
Immobilize helminths
For
Tissue roundwormds (nematodes): loa loa (fly), wuchereria bancrofti
123
Q

Interferons (uses)

A

IFN-a: HBV, HCV, Karposi’s sarcoma, Condyloma acuminatum, Hairy cell leukemia
IFN-b: MS
IFN-g (increases expression of MHC class I & II and improves Ag presentation): chronic granulomatous disease

124
Q

“-mivir” (mechanism and use)

A

Zanamivir, oseltamivir
Inhibits influenza neuraminidase -> decreases viral progeny release
For tx and prevention of influenza A and B

125
Q

Ribavirin (mechanism)

A

Competitively inhibits inosine monophosphate DH -> inhibits synthesis of guanine nucleotide
Direct inhibition of HCV RNA polymase (by ribavirin triphosphate)
Induces defective 5’-cap formation on viral mRNA transcript -> inefficient translation
Enhances Th1-mediated immunity while inhibiting Th2

126
Q

Ribavirin (2 uses)

A

RSV, chronic HCV

127
Q

Ribavirin (2 side effects)

A

Hemolytic anemia

Severe teratogen

128
Q

Acyclovir, famciclovir, valacyclovir (mechanism)

A

Guanosine analog
HSV/VZV thymidine kinase (infected cells only) monophosphorylates it -> cellular enzyme triphosphorylates it -> preferentially inhibits viral DNA polymerase by chain termination
Valacyclovir is a prodrug of acyclovir and has better oral bioavailability

129
Q

Acyclovir, famciclovir, valacyclovir (3 uses)

A

Prophylaxis in immunocompromised pts
HSV: mucocutaneous and genital lesions, encephalitis
VZV: use famciclovir for herpes zoster
No effect on latent form
Weak/no activity against EBV and CMV (because they don’t produce the same thymidine kinsae)

130
Q

Acyclovir, famciclovir, valacyclovir (side effects)

A

Obstructive crystalline nephropathy -> renal failure

Prevented/tx by aggressive IV hydration

131
Q

Acyclovir, famciclovir, valacyclovir (mechanism of resistance)

A

Mutated viral thymidine kinase

132
Q

Ganciclovir, valganciclovir (mechanism)

A

Guanosine analog
CMV viral kinase 5’-monophosphates it -> cellular kinase triphosphates it -> preferentially inhibits viral DNA polymerase
Valganciclovir is a prodrug of gangiclovir and has better oral bioavailability

133
Q

Ganciclovir, valganciclovir (use)

A

CMV (esp in immunocompromised) -> but don’t use if already on zidovudine b/c neutropenia will be made worse

134
Q

Ganciclovir, valganciclovir (side effects)

A

Leukopenia (NEUTROPENIA especially), thrombocytopenia
Renal toxicity
More toxic to host enzymes than acyclovir

135
Q

Ganciclovir, valganciclovir (2 mechanisms of resistance)

A

Mutated CMV DNA polymerase

Lack of viral kinase

136
Q

Foscarnet (mechanism)

A

Viral DNA polymerase inhibitor (pyrophosphate analog)
Also binds HCV reverse transcriptase
Does NOT require activation by viral kinase (like acyclovir, famciclovir, valacyclovir, ganciclovir, valganciclovir)

137
Q

Foscarnet (2 uses)

A

CMV retinitis in immunocompromised (when ganciclovir fails)

Acyclovir-resistant HSV

138
Q

Foscarnet (side effects)

A

Nephrotoxic

Seizures (from Ca2+ chelation & renal wasting of magnesium)

139
Q

Foscarnet (mechanism of resistance)

A

Mutated DNA polymerase

140
Q

Cidofovir (mechanism)

A

Preferentially inhibits viral DNA polymerase
Does NOT require phosphorylation by viral kinase
Long HL

141
Q

Cidofovir (2 uses)

A

CMV retinitis in immunocompromised

Acyclovir-resistant HSV

142
Q

Cidofovir (side effect)

A

Nephrotoxicity -> coadminister w/ probenecid and IV saline to prevent this

143
Q

HAART therapy combination?

A
  • 2 NRTIs

- 1 NNRTI OR 1 protease inhibitor OR 1 integrase inhibitor

144
Q

“-navir” (mechanism and use)

A

Protease inhibitor -> prevents maturation of new viruses
Ritonavir can inhibit P450 -> boosts other drug conc
Part of HIV HAART

145
Q

“-navir” (side effects)

A

Hyperglycemia
GI intolerance (nausea/diarrhea)
Lipodystrophy (fat redistribution, hyperTG)
Indinavir: nephropathy (crystallization), hematuria

146
Q

“-dine”, “-bine”, “-sine”, Tenofovir, Abacavir (mechanism)

A

EXCEPT delavirdine (that’s NNRTI)
NRTIs (blocks RNA -> DNA)
Competitively inhibits nucleotide binding to reverse transcriptase -> terminates DNA chain (lacks 3’OH group)
Tenofovir is nucleotide (so doesn’t need thymidine kinase like other ones which are nucleoside)

147
Q

“-dine”, “-bine”, “-sine”, Tenofovir, Abacavir (use)

A 
EXCEPT delavirdine (that's NNRTI)
NRTIs, part of HIV HAART
Zidovudine: general prophylaxis and during pregnancy -> reduces vertical transmission
148
Q

“-dine”, “-bine”, “-sine”, Tenofovir, Abacavir (side effects)

A 
EXCEPT delavirdine (that's NNRTI)
Bone marrow suppression (reversed w/ G-CSF, erythropoietin)
Peripheral neuropathy
Lactic acidosis (nucleosides only)
Rash (non-nucleosides)
Anemia (zidovudine)
Pancreatitis (didanosine)
149
Q

Efavirenz, nevirapine, delavirdine (mechanism and use)

A 
"vir" in the middle
NNRTIs (blocks RNA -> DNA)
Binds reverse transcriptase (at a site diff from NRTIs)
Don't require phosphorylation
Part of HIV HAART
150
Q

Efavirenz, nevirapine, delavirdine (side effects)

A

“vir” in the middle
Rash (can be severe like Stevens-Johnson and TEN)
Hepatotoxicity (life-threatening hepatic failure w/ encephalopathy)
Efavirenz: vivid dreams and CNS sx
Efavirenz and delavirdine CI in pregnancy

151
Q

Raltegravir (mechanism and use)

A 
Integrase inhibitor (blocks DNA -> mRNA)
Reversibly inhibits HIV integrase
Part of HIV HAART
152
Q

Raltegravir (side effects)

A

Hypercholesterolemia

153
Q

Enfuvirtide (mechanism, use, and side effect)

A

Fusion inhibitor
Binds gp41 and inhibits viral PENETRATION
Part of HIV HAART
Skin rxn at injection site

154
Q

Maraviroc (mechanism, use, and side effect)

A

Prevents ATTACHMENT -> binds CCR-5 on surface T cells/monocytes -> inhibits interaction w/ gp120
Part of HIV HAART
Skin rxn at injection site

155
Q

Interferons (2 side effects)

A

Neutropenia, myopathy

156
Q

Groups of antibiotics that bind 30S and 50S?

A

“buy AT 30, CCEL (sell) at 50”
30S: Aminoglycosides, Tetracyclines
50S: Chloramphenicol, Clindamycin, Erythromycin (macrolides), Linezolid

157
Q

Daptomycin (mechanism and use)

A

Depolarize cellular membrane
For MRSA (along w/ vancomycin and linezolid)
Not effective against G-, and inactivated by pulm surfactant (so can’t use for lung infection/pneumonia)

158
Q

Daptomycin (side effect)

A

Myopathy (CPK elevation)

159
Q

Interferons a and b (mechanism)

A

Paracrine signaling -> stimulate neibouring cells to synthesize antiviral proteins that degrade intracellular mRNA and impair protein synthesis (both of host and virus!)

160
Q

Fidaxomicin (mechanism and use)

A

Impairs RNA polymerase -> impairs protein synthesis -> bacteriocidal
Oral w/ minimal systemic absorption
For recurrent C. diff refractory to metronidazole and oral vancomycin

161
Q

Primaquine (use)

A

For P. vivax and P. ovale LIVER schizonts (mefloquine/chloroquine takes care of erythrocytic phase only)

162
Q

Puromycin (mechanism)

A

Analog of aminocyl-tRNA -> causes premature release of unfinished peptide chain

Pharmacology (12 decks)

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