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Pharmacology Topnotch > VII - Topnotch Pharma Flash Cards - Antibiotics/Chemotherapeutic Drugs > Flashcards

VII - Topnotch Pharma Flash Cards - Antibiotics/Chemotherapeutic Drugs

1
Q

Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial cell walls

A

Penicillin, Cephalosporins (TOPNOTCH)

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2
Q

DOC for syphillis, for streptococcal, meningococcal, G+ bacilli, spirochete infection

A

Natural Penicillins: Penicillin G, Penicillin V (narrow spectrum penicillin) (TOPNOTCH)

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3
Q

For staphylococcal infections

A

Anti-Staphylococcal Penicillins: Methicillin, nafcillin, oxacillin, cloxacillin (very narrow spectrum) (TOPNOTCH)

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4
Q

all penicillins are excreted unchanged in the urine EXCEPT for _____which is excreted in the bile

A

Nafcillin (TOPNOTCH)

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5
Q

Pens For enterococci, Listeria, E. coli, Proteus, H. influenza, Moraxella

A

Extended Spectrum Penicillin: Ampicillin, Amoxicillin (TOPNOTCH)

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6
Q

Pens For Pseudomonas, Enterobacter, Klebsiella

A

Antipseudomonal Penicillin: Piperacillin, ticarcillin, carbenicillin (TOPNOTCH)

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7
Q

all Cephs have renal excretion EXCEPT ______

A

Cefoperazone and Ceftriaxone (TOPNOTCH)

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8
Q

Cephs for For surgical prophylaxis, bone infections, infections due to staph and strep, E. coli, Klebsiella, G+ cocci

A

First Generation Cephs (TOPNOTCH)

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9
Q

Increases nephrotoxicity of aminoglycosides

A

Cephs (TOPNOTCH)

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10
Q

For surgical prophylaxis, bone infections, infections due to staph strep and E. coli, Enterobacter, Neisseria, infections against anaerobes (Bacteroides), sinus ear and respiratory infections by Klebsiella andHemophilus

A

Second Generation Cephs (TOPNOTCH)

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11
Q

Second Generation Cephs

A

Cefamandole, cefaclor, cefonicid, cefuroxime, cefprozil, loracarbef, ceforanide, cefoxitin, cefmetazole, cefotetan (TOPNOTCH)

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12
Q

First Generation Cephs

A

Cefazolin, cefadroxil, cephalothin, cephapirin, cephradine, cephalexin (TOPNOTCH)

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13
Q

Cephs with slight less activity against G+ but extended G- activity

A

Second Generation Cephs (TOPNOTCH)

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14
Q

decreased gram + coverage, increased gram - activity (pseudomonas, bacteroides), against Providencia, Serratia, Neiserria, Haemophilus ; DOC for gonorrhea

A

Third Generation Cephs (TOPNOTCH)

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15
Q

DOC for gonorrhea

A

Ceftriaxone and Cefixime (TOPNOTCH)

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16
Q

Third Generation Cephs

A

Cefoperazone, cefotaxime, ceftizoxime, ceftriaxone, cefixime, cefpodoxime proxetil, cefdinir, ceftibuten (TOPNOTCH)

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17
Q

all can Third gen Cephs can penetrate the BBB EXCEPT _____

A

Cefoperazone and Cefixime (TOPNOTCH)

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18
Q

More resistant to beta-lactamase produced by Enterobacter, Haemophilus, Neisseria and Pneumococcal

A

Fourth Generation Cephs (TOPNOTCH)

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19
Q

Fourth Generation Cephs

A

Cefipime (TOPNOTCH)

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20
Q

Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial cell walls, wide coverage against gram + gram - bacteria and anaerobes ; For infections resistant to other antibiotics EXCEPT MRSA, DOC for Enterobacter, Citrobacter and Serratia

A

Carbapenems (TOPNOTCH)

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21
Q

Carbapenems

A

Imipenem-cilastatin , ertapenem, meropenem (TOPNOTCH)

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22
Q

Imipenem given with Cilastatin which acts as ______

A

Dehydropeptidase enzyme inhibitor (TOPNOTCH)

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23
Q

Monobactam

A

Aztreonam (TOPNOTCH)

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24
Q

Resistant to beta-lactamase, no activity against gram + bacteria or anaerobes

A

Aztreonam (TOPNOTCH)

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25
Q

No cross-allergenicity with Pens

A

Aztreonam (TOPNOTCH)

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26
Q

Inhibits inactivation of penicillins by bacterial beta-lactamase (penicillinase)

A

Beta-Lactamase Inhibitors (TOPNOTCH)

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27
Q

Beta-Lactamase Inhibitors

A

Clavulanic acid , sulbactam, tazobactam (TOPNOTCH)

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28
Q

Inhibits cell wall synthesis by binding to the D-Ala-D-Ala terminus of nascent peptidoglycan –> inhibit transglycosylation –> prevent elongation and cross-linking of peptidoglycan chain

A

Glycopeptides: Vancomycin, teicoplanin, telavancin (TOPNOTCH)

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29
Q

For MRSA, PRSP, as alternative for pseudomembranous colitis

A

Vancomycin (TOPNOTCH)

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30
Q

SE: red man syndrome, nephrotoxicity, ototoxicity, chills, fever, phlebitis

A

Vancomycin (TOPNOTCH)

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31
Q

Interferes with a late stage in cell wall synthesis in gram + organisms ; For gram + bacteria

A

Bacitracin (TOPNOTCH)

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32
Q

Reserved for topical use only due to marked nephrotoxicity

A

Bacitracin (TOPNOTCH)

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33
Q

Blocks incorporation of D-Ala into the pentapeptide side chain of the peptidoglycan ; For drug-resistant TB

A

Cycloserine (TOPNOTCH)

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34
Q

inhibits cytosolic enolpyruvate transferase –> prevents formation of N-acetylmuramic acid

A

Fosfomycin (TOPNOTCH)

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35
Q

same spectrum of activity as Vancomycin ; For VRE, VRSA, for G+ activity, against endocarditis and sepsis

A

Daptomycin (TOPNOTCH)

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36
Q

Inhibits transpeptidation (catalyzed by peptidyl transferase) by blocking the binding of aminoacyl moiety of the charged tRNA to the acceptor site o mRNA at 50S subunit, basteriostatic

A

Chloramphenicol (TOPNOTCH)

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37
Q

For meningitis (Strep pneumonia, H influenza, Neisseria meningitides), back up for Salmonella, Rickettsia, Bacteroides, Wide spectrum antibiotic

A

Chloramphenicol (TOPNOTCH)

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38
Q

Binds 30s ribosomal subunit thus preveting the binding of tRNA to mRNA, bacteriostatic ; Broad/Wide Spectrum (G+ and G-), anaerobes and atypicals

A

Tetracyclines (TOPNOTCH)

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39
Q

_____ has the broadest spectrum of all tetracyclines and has the longest t1/2 (30-36hrs)

A

Tigecycline (TOPNOTCH)

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40
Q

SE: GI disturbances (enetrocolitis, nausea, diarrhea, vomiting), teratogen (tooth enamel dysplasia/discoloration), hepatotoxicity, nephrotoxicity, photosensitivity n(esp. demeclocycline), vestibulotoxicity, candidiasis, bacterial superinfection with S. aureus and C. difficile, Fanconi syndrome

A

Tetracyclines (TOPNOTCH)

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41
Q

Tetracyclines

A

Tetracycline, doxycycline, minocycline, tigecycline, demeclocycline (TOPNOTCH)

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42
Q

Binds 30s ribosomal subunit, inhibit transpeptidation, bacteriostatic ; For community-acquired pneumonia, pertussis, diphtheria, chlamydial infections

A

Macrolides (TOPNOTCH)

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43
Q

Macrolides

A

Erythromycin, azithromycin, clarithromycin, telithromycin (TOPNOTCH)

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44
Q

______ is used as an alternative Ceftriaxone in Gonorrhea and to Pen G in syphilis

A

Azithromycin (TOPNOTCH)

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45
Q

______ is used for macrolide-resistance

A

telithromycin (TOPNOTCH)

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46
Q

a narrow spectrum macrolide, for G+ and anaerobe, low oral bioavailability

A

Fidaxomicin (TOPNOTCH)

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47
Q

as effective as Vancomycin as treatment for C. difficile possibly with lower relapse rate

A

Fidaxomicin (TOPNOTCH)

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48
Q

GI disturbance, skin rash, neutropenia, hepatic dysfunction, possible superinfection (Pseudomembranous colitis - C. difficile overgrowth)

A

Lincosamides: Clindamycin, lincomycin (TOPNOTCH)

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49
Q

Binds 30s ribosomal subunit, inhibit transpeptidation, bacteriostatic ; For anaerobic infections (Bacteroides), alternative against gram + cocci (MRSA), endocarditis prophylaxis esp in those allergic to Pens, PCP pneumonia, toxoplasmosis (+ Pyrimethamine), skin and soft tissue infection

A

Lincosamides: Clindamycin, lincomycin (TOPNOTCH)

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50
Q

Binds 50s ribosomal subunit, constricting the channel where polypeptides are extruded thus tRNA synthetase is also inhibited –> decreased free tRNA

A

Streptogramin: Quinupristin-Dalfopristin (TOPNOTCH)

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51
Q

Binds 23S rRNA of 50s ribosomal subunit, inhibit initiation by blockin formation of the tRNA-ribosome-mRNA ternary complex, bacteriostatic ; Reserved for infections caused by drug-resistant gram + cocci (MRSA, VRE, PRSP), Listeria, Corynebacteria

A

Oxazolidinone: Linezolid (TOPNOTCH)

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52
Q

For serious infections caused by aerobic gram _ bacteria (E.coli, Enterobacter, Klebsiella, Proteus, Providencia, Pseudomonas, Serratia, Haemophilus, Moraxella, Shigella), endocarditis, ocular infections

A

Aminoglycosides (TOPNOTCH)

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53
Q

Least resistance and narrowest therapeutic window ; used for streptomycin-resistant TB

A

Amikacin (TOPNOTCH)

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54
Q

For TB, tularaemia, bubonic plague, brucellosis

A

Streptomycin (TOPNOTCH)

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55
Q

SE: nephrotoxicity (reversible), ototoxicity (irreversible), neuromuscular blockade

A

Aminoglycosides in general (TOPNOTCH)

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56
Q

SE: hypersensitivity, nephrotoxicity (reversible), ototoxicity (irreversible), neuromuscular blockade, teratogen (congenital deafness), injection site reactions

A

Streptomycin (TOPNOTCH)

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57
Q

_____ is most ototoxic of all Aminoglycosides (AG) while _____ has the most skin reactions

A

kanamycin ; Neomycin (TOPNOTCH)

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58
Q

For drug-resistant gonorrhoea, gonorrhoea in penicillin allergic patients

A

Spectinomycin (TOPNOTCH)

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59
Q

For Treatment of serious infections caused by organisms resistant to other aminoglycosides

A

Netilmicin (TOPNOTCH)

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60
Q

Inhibits dihydropteroate synthase, bacteriostatic

A

Sulfonamides (TOPNOTCH)

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61
Q

low solubility in acidic urine causing formation of stones

A

Sulfonamides (TOPNOTCH)

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62
Q

Sequential blockade of dihydropteroate synthase and dihydrofolate reductase , bactericidal

A

Co-trimoxazole (Sulfamethoxazole + Trimethoprim) (TOPNOTCH)

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63
Q

SE: GI upset, acute hemolysis in G6PD deficiency, nephrotoxicity, hypersensitivity, hematotoxicity, kernicterus ; antifolate effects (megaloblastic anemia, leukopenia, granulocytopenia)

A

Co-trimoxazole (Sulfamethoxazole + Trimethoprim) (TOPNOTCH)

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64
Q

Inhibits DNA replication by binding to DNA gyrase and topoisomerase IV (G+) and Topoisomerase II (G-)

A

Fluoroquinolones (TOPNOTCH)

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65
Q

For infections of the urogenital and GI tract by G- (gonococci, E. coli, Klebsiela, Campylobacter, Enterobacter, Pseudomonas, Salmonella, Shigella), respiratory tract, skin and soft tissue infection

A

Fluoroquinolones (TOPNOTCH)

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66
Q

CI in pregnancy and in children (damage growing cartilage –> arthropathy)

A

Fluoroquinolones (TOPNOTCH)

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67
Q

GI distress, skin rashes, HA, dizziness, insomnia, increased LFT, phototoxicity, CNS effects (dizziness, headache), tendinitis and tendon rupture, opportunistic infection by Candida and Streptococci

A

Fluoroquinolones (TOPNOTCH)

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68
Q

Second Generation Fluoroquinolones

A

Ciprofloxacin, ofloxacin (TOPNOTCH)

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69
Q

First Generation Fluoroquinolones

A

Norfloxacin, Nalidixic acid (TOPNOTCH)

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70
Q

Third Generation Fluoroquinolones

A

Levofloxacin, Gemifloxacin, Moxifloxacin (TOPNOTCH)

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71
Q

Respiratory Quinolones

A

Levofloxacin, Gemifloxacin, Moxifloxacin (TOPNOTCH)

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72
Q

newest members of the Fluoroquinolone family and are condisered to have the broadest spectrum of activity with increased activity aginst anaerobes ang atypical agents

A

Moxifloxacin and Gemifloxacin (TOPNOTCH)

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73
Q

Fourth Generation Fluoroquinolones

A

Trovafloxacin, Gatifloxacin (TOPNOTCH)

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74
Q

FQ elimination is via kidneys by tubular secretion (may compete with probenecid for excretion) EXCEPT

A

Moxifloxacin (TOPNOTCH)

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75
Q

additional SE of which FQs: diabetes, hepatotoxicity

A

diabetes (gatifloxacin), hepatotoxicity (trovafloxacin) (TOPNOTCH)

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76
Q

Reactive reduction by ferredoxin forming free radicals that disrupt electron transport chain, bactericidal

A

Metronidazole, tinidazole (TOPNOTCH)

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77
Q

For anaerobic or mixed intra-abdominal infections, vaginitis (trichomonas, gardnerella), pseudomembranous colitis, brain abscess, protozoal infections

A

Metronidazole, tinidazole (TOPNOTCH)

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78
Q

DOC for amoebiasis, giardiasis and Pseudomembranous colitis

A

Metronidazole (TOPNOTCH)

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79
Q

single OD dose can prevent recurrent UTI

A

Nitrofurantoin (TOPNOTCH)

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80
Q

SE: GI irritation, metallic taste, headache, dark urine, leukopenia, dizziness, ataxia, neuropathy, seizures and disulfiram reaction

A

Metronidazole (TOPNOTCH)

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81
Q

acidification of urine enhances activity ; adjust dose in renal patients

A

Nitrofurantoin (TOPNOTCH)

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82
Q

Forms multiple reactive intermediates when acted upon by bacterial nitrofuran reductase, bactericidal ; For UTI (except Proteus and Pseudomonas)

A

Nitrofurantoin (TOPNOTCH)

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83
Q

Inhibits mycolic acid synthesis, bactericidal

A

Isoniazid (TOPNOTCH)

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84
Q

SE: hepatotoxicity, neurotoxicity (seizures, peripheral neuritis, insomnia, restlessness, muscle twitching), acute hemolysis in G6PD deficiency, drug-induced lupus

A

Isoniazid (TOPNOTCH)

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85
Q

Most impt drug in TB

A

Isoniazid (TOPNOTCH)

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86
Q

prevent neurotoxicity of Isoniazid by giving

A

pyridoxine (vit B6) (TOPNOTCH)

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87
Q

given as a sole drug for prophylaxis of close contacts of TB Px and skin test converters

A

Isoniazid (TOPNOTCH)

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88
Q

Inhibits DNA-dependent RNA polymerase, bactericidal

A

Rifamycin derivatives: Rifampicin, rifabutin, rifapentine, rifamixin (TOPNOTCH)

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89
Q

red-orange urine, light chain proteinuria, skin rash, thrombocytopenia, nephritis, hepatotoxicity, flulike syndrome, anemia, impair antibody response

A

Rifamycin derivatives: Rifampicin, rifabutin, rifapentine, rifamixin (TOPNOTCH)

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90
Q

CYP450 inhibitor: Rifampicin or INH

A

INH (TOPNOTCH)

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91
Q

CYP450 inducer: Rifampicin or INH

A

Rifampicin (TOPNOTCH)

92
Q

Inhibits arabinosyl transferases involved in the synthesis of arabinogalactan in mycobacterial cell wall, bacteriostatic

A

Ethambutol (TOPNOTCH)

93
Q

SE: dose-dependent visual disturbances (decreased visual acuity, red green color blindness, retrobulbar neuritis, retinal damage, optic neuritis), headache, confusion, hyperuricemia, peripheral neuritis

A

Ethambutol (TOPNOTCH)

94
Q

Unknow MOA, bacteriostatic but can be bactericidal on actively dividing mycobacteria, is metabolized to pyrazinoic acid, t 1/2 is increased in liver and kidney disease

A

Pyrazinamide (TOPNOTCH)

95
Q

SE: hepatotoxicity, nongouty polyarhtralgia, asymptomatic hyperuricemia, myalgia, GIT irritation, maculopapular rash, porphyria, photosensitivity ; CI in pregnancy

A

Pyrazinamide (TOPNOTCH)

96
Q

Most hepatotoxic anti-TB drug

A

Pyrazinamide (TOPNOTCH)

97
Q

Most active drug against M. leprae

A

Dapsone (TOPNOTCH)

98
Q

_______ is a repository form of dapsone which has drug action that can last for several months

A

Acedapsone (TOPNOTCH)

99
Q

Binds to guanine bases in bacterial DNA, bactericidal ; For leprosy

A

Clofazimine (TOPNOTCH)

100
Q

Binds to ergosterol in fungal cell membranes, forming artificial pores, fungicidal

A

Amphotericin B (TOPNOTCH)

101
Q

WIDEST antifungal spectrum

A

Amphotericin B (TOPNOTCH)

102
Q

For systemic fungal infections (aspergillus, blastomyces, candida, Cryptococcus, histoplasma, mucor), for initial induction before followup treatment with azoles, can be used topically in mycotic corneal ulcers and keratitis

A

Amphotericin B (TOPNOTCH)

103
Q

Accumulated in fungal cells by the action of permease and converted by cytosine deaminase to 5-FU, which inhibits thimidylate synthase, pyrimidine antimetabolite, fungistatic

A

Flucytosine (TOPNOTCH)

104
Q

SE: infusion reactions (chills, fever, muscle spasms, vomiting, hypotension), dose limiting nephrotoxicity (decreased GFR, ATN with magnesium and potassium wasting, decreased erythropoietin), neurotoxicity (seizure, neuronal damage)

A

Amphotericin B (TOPNOTCH)

105
Q

Inhibit 14-demethylase –> decreased ergosterol production –> increased permeability of cell membrane, Inhibits fungal P450-dependent enzymes blocking ergosterol synthesis, fungistatic

A

Ketoconazole (TOPNOTCH)

106
Q

SE: GI disturbances (vomiting, diarrhea), rash, hepatotoxicity, drug interaction, gynecomastia, menstrual irregularities and infertility

A

Ketoconazole (TOPNOTCH)

107
Q

DOC for candidiasis (esophageal, oropharyngeal, vulvovaginitis), coccidioidomycosis, cryptococcal meningitis (treatment and prophylaxis)

A

Fluconazole (TOPNOTCH)

108
Q

alternative to Ampho B in the treatment of C. neoformans, as effective as Ampho B in candidemia

A

Fluconazole (TOPNOTCH)

109
Q

DOC for blastomycosis, sporotrichosis, dermatophytosis esp onchomycosis, chromoblastomycosis ; alternative for infections due to Aspergillus, Coccidioides, Cryptococcus and Histoplasma , for esophageal candidiasis resistant to fluconazole

A

Itraconazole (TOPNOTCH)

110
Q

co-DOC for invasive aspergillosis, alternative in candidemia, for fluconazole-resistant organisms, for candidal esophagitis and stomatitis in AIDS patients

A

Voriconazole (TOPNOTCH)

111
Q

SE: GI disturbances (vomiting, diarrhea), rash, hepatotoxicity, blurring of vision in 30% of patients, CI in pregnancy

A

Voriconazole (TOPNOTCH)

112
Q

as salvage therapy in invasive aspergillosis

A

Posaconazole (TOPNOTCH)

113
Q

BROADEST spectrum triazole ; the only azole with activity against Rhizopus sp. (mucormycosis

A

Posaconazole (TOPNOTCH)

114
Q

azoles that are limited to topical use because of systemic toxicity

A

Clotrimazole, miconazole, ketoconazole (TOPNOTCH)

115
Q

Inhibit beta-glucan synthase which produces (1–>2) glycan which is a cell wall component, thus decreasing fungal cell wall synthesis, fungostatic

A

Echinocandins: Caspofungin, anidulafungin, micafungin (TOPNOTCH)

116
Q

Interferes with microtubule function in dermatophytes, inhibits synthesis and polymerization of nucleic acids, fungistatic

A

Griseofulvin (TOPNOTCH)

117
Q

Inhibits with ergosterol synthesis by inhibiting fungal squalene oxidase leading to increased squalene which interferes with ergosterol synthesis, fungicidal

A

Terbinafine (TOPNOTCH)

118
Q

absorption is increased by intake of fatty meal

A

Griseofulvin (TOPNOTCH)

119
Q

Binds to ergosterol in fungal cell membranes, forming artificial pores, fungicidal

A

Nystatin (TOPNOTCH)

120
Q

For candidiasis ((oropharyngeal, esophageal and vaginal), for GI fungal infections in patients with impaired defense mechanisms

A

Nystatin (TOPNOTCH)

121
Q

Activated by viral thymidine kinase (TK) to forms that inhibit viral DNA polymerase, guanosine analog, competitive substrate for DNA polymerase, causes chain termination after its incorporation into the viral DNA

A

Acyclovir, valacyclovir, penciclovir, famciclovir, docosanol (TOPNOTCH)

122
Q

For infections due to HSV1, HSV2, VZV (mucocutaneous and genital herpes, prophylaxis in AIDS and in other Immunocompromised states such as organ transplant patients, herpes encephalitis, neonatal HSV infection etc.

A

Acyclovir, valacyclovir, penciclovir, famciclovir, docosanol (TOPNOTCH)

123
Q

_____ is a prodrug that is converted to Acyclovir and reached plams levels 3-5x (longer t1/2) more than acyclovir

A

Valacyclovir (TOPNOTCH)

124
Q

____ is a prodrug which is converted to Penciclovir in vivo

A

Famciclovir (TOPNOTCH)

125
Q

Inhibits fusion between the HSV envelope and plasma membrane, prevents viral entry and subsequent replication

A

Docosanol (TOPNOTCH)

126
Q

Inhibits viral DNA polymerase causing chain termination, guanosine derivative

A

Ganciclovir, valganciclovir (TOPNOTCH)

127
Q

For infections due to CMV, HSV1, HSV2, VZV ; For prohylaxis and treatment of CMV retinitis and other CMV infections in the immunocompromised patients

A

Ganciclovir, valganciclovir (TOPNOTCH)

128
Q

Inhibits viral DNA polymerase causing chain termination ; For CMV retinitis, mucocutaneous HSV infections, acyclovir-resistance, ganciclovir-resistance, genital warts and molluscum contangiosum

A

Cifodovir (TOPNOTCH)

129
Q

Inhibits viral RNA polymerase, DNA polymerase, and HIV reverse transcriptase, binds to pyrophosphate binding site

A

Foscarnet (TOPNOTCH)

130
Q

adenine analog ; For HSV, VZV, CMV

A

Vidarabine (TOPNOTCH)

131
Q

pyrimidine analogs ; For herpes keratitis (HSV-1)

A

Idoxuridine, trifluridine (TOPNOTCH)

132
Q

antisense oligonucleotide that binds to mRNA of CMV causing inhibition of early protein synthesis ; For CMV retinitis

A

Fomivirsen (TOPNOTCH)

133
Q

Inhibit HIV reverse transcriptase after phosphorylation by cellular enzymes, acts as chain terminators via insertion into the growing DNA chain

A

NRTI (TOPNOTCH)

134
Q

NRTIs

A

Abacavir, Didanosine (ddI), Emtricitabine, Lamivudine (3TC), Stavudine (d4T), Tenofovir, Zalcitabine (ddC),Zidovudine (ZDV) (TOPNOTCH)

135
Q

Inhibits HIV reverse transcriptase, no phosphorylation required, do not compete with nucleoside triphosphate

A

NNRTI (TOPNOTCH)

136
Q

NNRTIs

A

Delavirdine, efavirenz, etravirine, nevirapine (TOPNOTCH)

137
Q

cleaves precursor polyprotein to form the final structural protein of the mature virion core, inhibits viral protein processing

A

Protease Inhibitor (TOPNOTCH)

138
Q

Protease Inhibitor

A

Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir-Ritonavir, Nelfinavir, Ritonavir, Saquinavir, Tipranavir (TOPNOTCH)

139
Q

Binds to gp41 subunit of viral envelope glycoprotein, preventing fusion of viral and cellular membranes

A

Fusion Inhibitor: Enfuvirtide (TOPNOTCH)

140
Q

Blocks viral attachment by blocking CCR5, a transmembrane protein involved in the attachment of HIV to host cell

A

CCR5 receptor antagonist: Maraviroc (TOPNOTCH)

141
Q

Inhibit early step replication and prevent uncoating by binding to M2 proton channels ; For influenza A and rubella

A

Uncoating inhibitors: Amantadine, rimantadine (TOPNOTCH)

142
Q

Inhibits neuraminidase which cleaves sialic acid residues from viral proteins and surface proteins of infected cells , decrease release of progeny virus

A

Neuraminidase inhibitors: Oseltamivir, zanamivir (TOPNOTCH)

143
Q

DOC for influenza (including H1N1)

A

Neuraminidase inhibitors: Oseltamivir, zanamivir (TOPNOTCH)

144
Q

cytokine, increased activity of JAKS leading to phosphorylation of signal transducers and activation of transcription (STATS) which causes increased formation of antiviral proteins

A

Interferon (TOPNOTCH)

145
Q

For chronic HBV, HCV infection, Kaposi sarcoma, genital warts, prevents dissemination of HZV in cancer patients and decreased CMV shedding after renal transplantation

A

Interferon (TOPNOTCH)

146
Q

Inhibits HBV DNA polymerase causing chain termination after incorporation into the viral DNA

A

Adefovir, Dipivoxil, Telbivudine, Tenofovir (TOPNOTCH)

147
Q

______ is a prodrug of Adefovir

A

Dipiroxil (TOPNOTCH)

148
Q

_____is an anti-RT drug that is also effective in chronic HBV, it is active against lamivudine and entecavir-resistant strains

A

Tenofovir (TOPNOTCH)

149
Q

guanosine nucleoside, inhibits DNA polymerase

A

Entecavir (TOPNOTCH)

150
Q

Coinfection between HBV and HIV may increase the risk of pancreatitis with_____use

A

lamivudine (TOPNOTCH)

151
Q

Inhibits guanosine triphosphate formation, prevents capping of viral mRNA, blocks RNA-dependent RNA polymerase, inhibit replication of many DNA and RNA viruses like Influenza A and B, parainfluenza, paramyxo viruses, HCV and HIV

A

Ribavirine (TOPNOTCH)

152
Q

For HCV infection (with IFN ) and RSV infection, decreasesmortality in viral hemorrhagic fevers

A

Ribavirine (TOPNOTCH)

153
Q

Prevents polymerization of heme into hemozoin, blood schizonticide

A

Chloroquine, hydroxychloroquine (TOPNOTCH)

154
Q

Complexes with DNA to prevent strand separation, blocks DNA replication and transcription, blood schizonticide

A

Quinine, quinidine gluconate (TOPNOTCH)

155
Q

DOC for malaria in pregnant patients

A

Quinine, quinidine gluconate (TOPNOTCH)

156
Q

1st line drug (weekly administration) for prophylaxis in all areas with Chloroquine resistance)

A

Mefloquine (TOPNOTCH)

157
Q

Forms electron-transferring redox compounds that act as cellular oxidants, tissue schizonticides, gametocides

A

Primaquine (TOPNOTCH)

158
Q

Eradicates hypnozoites in the liver, preventing malarial relapse

A

Primaquine (TOPNOTCH)

159
Q

______ disrupts mitochondrial electron transport, blood and tissue schizonticide, ______ inhibits folate synthesis, sporonticide

A

Atovaquone-proguanil (TOPNOTCH)

160
Q

also effective against Mefloquine-resistant Falciparum infection

A

Atovaquone-proguanil (TOPNOTCH)

161
Q

_____ is the DOC for uncomplicated falciparum malaria in the Philippines

A

Co-artem (TOPNOTCH)

162
Q

DOC for asymptomatic cyst carrier of E. histolytica

A

Diloxanide Furoate (TOPNOTCH)

163
Q

Inhibits protein synthesis, blocks ribosomal movement along messenger RNA, tissue amebicide ; back up drug for severe intestinal and extraintestinal amebiasis

A

Emetine, dehydroemetine (TOPNOTCH)

164
Q

Inhibits protein synthesis, binds to 16S ribosomal subunit, luminal amebicide ; For intestinal amebiasis, cryptosporidiosis

A

Paromomycin (TOPNOTCH)

165
Q

For metronidazole-resistant amebiasis, giardiasis, cryptosporidiosis (DOC)

A

Nitazoxanide (TOPNOTCH)

166
Q

For prophylaxis and treatment of pneumocystosis (DOC), prophylaxis (T. gondii, I. belli)

A

Co-trimoxazole (TOPNOTCH)

167
Q

For prophylaxis and treatment of toxoplasmosis (DOC)

A

Pyrimethamine-sulfadiazine (TOPNOTCH)

168
Q

alternative drug for Toxoplasmosis is _____

A

Clindamycin (TOPNOTCH)

169
Q

For African sleeping sickness (hemolymphatic stage),onchocerciasis (backup)

A

Suramin (TOPNOTCH)

170
Q

Suicide inhibitor of ornithine decarboxylase; For advanced west African sleeping sickness (DOC)

A

Eflornithine (TOPNOTCH)

171
Q

Organic arsenical, inhibits enzyme sulfhydryl groups in trypanosomes; DOC for African sleeping sickness

A

Melarsoprol (TOPNOTCH)

172
Q

Inhibits trypanothione reductase; DOC for Chagas disease (Trypanosoma cruzi)

A

Nifurtimox (TOPNOTCH)

173
Q

DOC for Leishmaniasis

A

Sodium Stibogluconate (TOPNOTCH)

174
Q

Selectively inhibits microtubule synthesis and glucose uptake in nematodes, ovicidal ; For ascariasis, pinworm, whipworm

A

Mebendazole (TOPNOTCH)

175
Q

Inhibits microtubule assembly, larvicidal and ovicidal ; For ascariasis, hookworm, whipworm, hydatid disease (DOC), threadworms, filariasis, larva migrans, cysticercosis

A

Albendazole (TOPNOTCH)

176
Q

primary drug for ascariasis, ancylostomiasis, trichuriasis

A

Albendazole (TOPNOTCH)

177
Q

DOC for filariasis and eye worm disease

A

Diethylcarbamazine (TOPNOTCH)

178
Q

May cause mazzotti reaction when used for onchocerciasis

A

Diethylcarbamazine (TOPNOTCH)

179
Q

Intensifies GABA-mediated neurotransmission in nematodes, immobilizes parasites ; DOC for strongyloidiasis

A

Ivermectin (TOPNOTCH)

180
Q

Stimulates nicotinic receptors at NMJ of nematodes, causes depolarization-induced paralysis

A

Pyrantel pamoate (TOPNOTCH)

181
Q

DOC for hookworm and roundworm infections

A

Pyrantel pamoate (TOPNOTCH)

182
Q

DOC for trichinosis

A

Thiabendazole (TOPNOTCH)

183
Q

DOC for trematodes (schistosoma, paragonimus, clonorchis, opistorchis) and cestodes (taenia, diphyllobothrium)

A

Praziquantel (TOPNOTCH)

184
Q

Used with steroid when treating neurocysticercosis, contraindicated in ocular cysticercosis (may cause irreparable eye damage)

A

Praziquantel (TOPNOTCH)

185
Q

Increases membrane permeability to calcium, cause muscle paralysis, vacualization and death

A

Praziquantel (TOPNOTCH)

186
Q

Uncouples oxidative phosphorylation or by activating ATPases ; alternative drug for cestode infection (Taenia, diphyllobotrium)

A

Niclosamide (TOPNOTCH)

187
Q

Forms DNA cross-links, resulting in inhibition of DNA synthesis and function, Cell-cycle nonspecific

A

Alkylating agents (TOPNOTCH)

188
Q

Alkylating agents

A

Cyclophosphamide, chlorambucil, Cisplatin, Carboplatin, oxaliplatin, Procarbazine, Dacarbazine, Busulfan, Carmustine, lomustine (TOPNOTCH)

189
Q

SE: bone marrow suppression, hemorrhagic cystitis, hepatotoxicity, alopecia, SIADH, pulmonary toxicity

A

Cyclophosphamide (TOPNOTCH)

190
Q

Rescue therapy for cyclophosphamide

A

MESNA (TOPNOTCH)

191
Q

Rescue therapy for Cisplatin

A

Amifostine (TOPNOTCH)

192
Q

can penetrate the CSF, For Hodgkin’s lymphoma, non-hodgkin’s lymphoma, brain tumors

A

Procarbazine (TOPNOTCH)

193
Q

SE: pulmonary fibrosis, adrenal insufficiency, skin pigmentation

A

Busulfan (TOPNOTCH)

194
Q

Highly lipophilic allowing ease of passage through BBB into the CNS ; For brain tumors, melanoma, skin cancer

A

Carmustine, lomustine (TOPNOTCH)

195
Q

Inhibits dihydrofolate reductase, decreases synthesis of thymidylate, amino acids, purine nucleotides; cell cycle specific

A

Methotrexate (TOPNOTCH)

196
Q

Rescue therapy for methotrexate

A

Leucovorin (Folinic acid) (TOPNOTCH)

197
Q

Inhibits de novo purine nucleotide synthesis, activated by HGPRT, cell cycle specific ; For acute leukemia (AML, ALL), CML

A

6-Mercaptopurine, 6-thioguanine, fludarabine, cladribine (TOPNOTCH)

198
Q

Inhibits thymidylate synthase, causes thymineless death of cells, cell cycle specific

A

5-Fluorouracil (TOPNOTCH)

199
Q

a deoxycytidine analog

A

Gemcitabine (TOPNOTCH)

200
Q

Most specific for the S-phase of the cell cycle

A

Cytarabine (TOPNOTCH)

201
Q

Prevents microtubule assembly, causes cell arrest at metaphase, cell cycle specific

A

Vinca alkaloid: Vincristine, Vinblastine (TOPNOTCH)

202
Q

Inhibits DNA topoisomerase II, inhibits mitochondrial electron transport, cell cycle specific

A

Etoposide (TOPNOTCH)

203
Q

Inhibits DNA topoisomerase I, cell cycle specific; For advanced ovarian cancer (2nd line), small cell lung cancer

A

Topotecan, irinotecan (TOPNOTCH)

204
Q

Interferes with mitotic spindle, prevents microtubule disassembly into tubulin monomers, cell cycle specific

A

Paclitaxel, docetaxel (TOPNOTCH)

205
Q

used in solid tumors like breast, ovarian, lung, gastroesophageal, prostate, bladder and head & neck cancers

A

Paclitaxel, docetaxel (TOPNOTCH)

206
Q

Acts primarily in M phase of cancer cell cycle

A

Vinca alkaloid: Vincristine, Vinblastine (TOPNOTCH)

207
Q

Intercalates between base pairs, inhibits topoisomerase II, generates free radicals cell cycle non-specific

A

Anthracycline: Doxorubicin, daunorubicin, idarubicin, epirubicin, mitoxantrone (TOPNOTCH)

208
Q

Rescue therapy for Doxorubicin

A

dexrazoxane (TOPNOTCH)

209
Q

Most specific for the G2 phase of cell cycle

A

Bleomycin (TOPNOTCH)

210
Q

SE: pneumonitis, pulmonary fibrosis, alopecia, mucocutaneous reactions

A

Bleomycin (TOPNOTCH)

211
Q

Binds to double stranded DNA, inhibits DNA-dependent RNA synthesis, cell cycle non-specific

A

Actinomycin D (TOPNOTCH)

212
Q

Tyrosine kinase inhibitor of the protein product of bcr-abl oncogene in CML ; For CML, GIST

A

TK inhibitor: Imatinib, dasatinib, nilotinib (TOPNOTCH)

213
Q

recognizes a surface protein in breast CA cells that overexpress Her-2-Neu receptors for epidermal growth factor

A

Trastuzumab (TOPNOTCH)

214
Q

Inhibits binding of VEGF to VEGFR leading to inhibiton of VEGF signalling, inhibits tumor vascular permeability but enhances tumor blood flow and drug delivery

A

Bevacizumab (TOPNOTCH)

215
Q

Binds to a surface protein in NHL cells, induces complement-mediated lysis, direct cytotoxicity and induction of apoptosis

A

Rituximab (TOPNOTCH)

216
Q

Endogenous glycoproteins with antineoplastric, immunosuppressive and antiviral actions

A

Interferon alpha (TOPNOTCH)

217
Q

Depletes serum asparagines ; For ALL, T-cell auxotrophic CA (leukemia and lymphomas) that require asparagine for growth

A

Asparaginase (TOPNOTCH)

218
Q

Only vitamin that can cure cancer

A

All-Trans retinoic acid (TOPNOTCH)

219
Q

For acute promyelocytic leukemia

A

All-Trans retinoic acid (TOPNOTCH)

220
Q

Suppresses inflammation and immune response, may trigger apoptosis and work on nondividing cancer cells

A

Prednisone (TOPNOTCH)

221
Q

Estrogen antagonist actions in breasts tissue and CNS, estrogen agonist effects in uterus, liver and bone

A

Tamoxifen (TOPNOTCH)

222
Q

Androgen antagonist ; For prostate cancer

A

Flutamide (TOPNOTCH)

223
Q

Increased LH, FSH secretion with intermittent administration, reduced LH and FSH secretion with prolonged continuous administration ; For prostate cancer

A

Leuprolide (TOPNOTCH)

224
Q

Reduces estrogen synthesis by inhibiting aromatase; For breast cancer

A

Anastrazole (TOPNOTCH)

225
Q

Effective againsts breast cancer that have become resistant to tamoxifen

A

Anastrazole (TOPNOTCH)

Pharmacology Topnotch (8 decks)

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