VII - Topnotch Pharma Flash Cards - Chemotherapeutic Drugs Preview

Pathology PLE 2015 > VII - Topnotch Pharma Flash Cards - Chemotherapeutic Drugs > Flashcards

Flashcards in VII - Topnotch Pharma Flash Cards - Chemotherapeutic Drugs Deck (225):
1

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

Penicillin, Cephalosporins (TOPNOTCH)

2

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

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

3

For staphylococcal infections

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

4

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

Nafcillin (TOPNOTCH)

5

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

Extended Spectrum Penicillin: Ampicillin, Amoxicillin (TOPNOTCH)

6

Pens For Pseudomonas, Enterobacter, Klebsiella

Antipseudomonal Penicillin: Piperacillin, ticarcillin, carbenicillin (TOPNOTCH)

7

all Cephs have renal excretion EXCEPT ______

Cefoperazone and Ceftriaxone (TOPNOTCH)

8

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

First Generation Cephs (TOPNOTCH)

9

Increases nephrotoxicity of aminoglycosides

Cephs (TOPNOTCH)

10

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

Second Generation Cephs (TOPNOTCH)

11

Second Generation Cephs

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

12

First Generation Cephs

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

13

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

Second Generation Cephs (TOPNOTCH)

14

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

Third Generation Cephs (TOPNOTCH)

15

DOC for gonorrhea

Ceftriaxone and Cefixime (TOPNOTCH)

16

Third Generation Cephs

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

17

all can Third gen Cephs can penetrate the BBB EXCEPT _____

Cefoperazone and Cefixime (TOPNOTCH)

18

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

Fourth Generation Cephs (TOPNOTCH)

19

Fourth Generation Cephs

Cefipime (TOPNOTCH)

20

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

Carbapenems (TOPNOTCH)

21

Carbapenems

Imipenem-cilastatin , ertapenem, meropenem (TOPNOTCH)

22

Imipenem given with Cilastatin which acts as ______

Dehydropeptidase enzyme inhibitor (TOPNOTCH)

23

Monobactam

Aztreonam (TOPNOTCH)

24

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

Aztreonam (TOPNOTCH)

25

No cross-allergenicity with Pens

Aztreonam (TOPNOTCH)

26

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

Beta-Lactamase Inhibitors (TOPNOTCH)

27

Beta-Lactamase Inhibitors

Clavulanic acid , sulbactam, tazobactam (TOPNOTCH)

28

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

Glycopeptides: Vancomycin, teicoplanin, telavancin (TOPNOTCH)

29

For MRSA, PRSP, as alternative for pseudomembranous colitis

Vancomycin (TOPNOTCH)

30

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

Vancomycin (TOPNOTCH)

31

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

Bacitracin (TOPNOTCH)

32

Reserved for topical use only due to marked nephrotoxicity

Bacitracin (TOPNOTCH)

33

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

Cycloserine (TOPNOTCH)

34

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

Fosfomycin (TOPNOTCH)

35

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

Daptomycin (TOPNOTCH)

36

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

Chloramphenicol (TOPNOTCH)

37

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

Chloramphenicol (TOPNOTCH)

38

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

Tetracyclines (TOPNOTCH)

39

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

Tigecycline (TOPNOTCH)

40

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

Tetracyclines (TOPNOTCH)

41

Tetracyclines

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

42

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

Macrolides (TOPNOTCH)

43

Macrolides

Erythromycin, azithromycin, clarithromycin, telithromycin (TOPNOTCH)

44

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

Azithromycin (TOPNOTCH)

45

______ is used for macrolide-resistance

telithromycin (TOPNOTCH)

46

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

Fidaxomicin (TOPNOTCH)

47

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

Fidaxomicin (TOPNOTCH)

48

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

Lincosamides: Clindamycin, lincomycin (TOPNOTCH)

49

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

Lincosamides: Clindamycin, lincomycin (TOPNOTCH)

50

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

Streptogramin: Quinupristin-Dalfopristin (TOPNOTCH)

51

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

Oxazolidinone: Linezolid (TOPNOTCH)

52

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

Aminoglycosides (TOPNOTCH)

53

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

Amikacin (TOPNOTCH)

54

For TB, tularaemia, bubonic plague, brucellosis

Streptomycin (TOPNOTCH)

55

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

Aminoglycosides in general (TOPNOTCH)

56

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

Streptomycin (TOPNOTCH)

57

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

kanamycin ; Neomycin (TOPNOTCH)

58

For drug-resistant gonorrhoea, gonorrhoea in penicillin allergic patients

Spectinomycin (TOPNOTCH)

59

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

Netilmicin (TOPNOTCH)

60

Inhibits dihydropteroate synthase, bacteriostatic

Sulfonamides (TOPNOTCH)

61

low solubility in acidic urine causing formation of stones

Sulfonamides (TOPNOTCH)

62

Sequential blockade of dihydropteroate synthase and dihydrofolate reductase , bactericidal

Co-trimoxazole (Sulfamethoxazole + Trimethoprim) (TOPNOTCH)

63

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

Co-trimoxazole (Sulfamethoxazole + Trimethoprim) (TOPNOTCH)

64

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

Fluoroquinolones (TOPNOTCH)

65

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

Fluoroquinolones (TOPNOTCH)

66

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

Fluoroquinolones (TOPNOTCH)

67

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

Fluoroquinolones (TOPNOTCH)

68

Second Generation Fluoroquinolones

Ciprofloxacin, ofloxacin (TOPNOTCH)

69

First Generation Fluoroquinolones

Norfloxacin, Nalidixic acid (TOPNOTCH)

70

Third Generation Fluoroquinolones

Levofloxacin, Gemifloxacin, Moxifloxacin (TOPNOTCH)

71

Respiratory Quinolones

Levofloxacin, Gemifloxacin, Moxifloxacin (TOPNOTCH)

72

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

Moxifloxacin and Gemifloxacin (TOPNOTCH)

73

Fourth Generation Fluoroquinolones

Trovafloxacin, Gatifloxacin (TOPNOTCH)

74

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

Moxifloxacin (TOPNOTCH)

75

additional SE of which FQs: diabetes, hepatotoxicity

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

76

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

Metronidazole, tinidazole (TOPNOTCH)

77

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

Metronidazole, tinidazole (TOPNOTCH)

78

DOC for amoebiasis, giardiasis and Pseudomembranous colitis

Metronidazole (TOPNOTCH)

79

single OD dose can prevent recurrent UTI

Nitrofurantoin (TOPNOTCH)

80

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

Metronidazole (TOPNOTCH)

81

acidification of urine enhances activity ; adjust dose in renal patients

Nitrofurantoin (TOPNOTCH)

82

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

Nitrofurantoin (TOPNOTCH)

83

Inhibits mycolic acid synthesis, bactericidal

Isoniazid (TOPNOTCH)

84

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

Isoniazid (TOPNOTCH)

85

Most impt drug in TB

Isoniazid (TOPNOTCH)

86

prevent neurotoxicity of Isoniazid by giving

pyridoxine (vit B6) (TOPNOTCH)

87

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

Isoniazid (TOPNOTCH)

88

Inhibits DNA-dependent RNA polymerase, bactericidal

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

89

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

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

90

CYP450 inhibitor: Rifampicin or INH

INH (TOPNOTCH)

91

CYP450 inducer: Rifampicin or INH

Rifampicin (TOPNOTCH)

92

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

Ethambutol (TOPNOTCH)

93

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

Ethambutol (TOPNOTCH)

94

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

Pyrazinamide (TOPNOTCH)

95

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

Pyrazinamide (TOPNOTCH)

96

Most hepatotoxic anti-TB drug

Pyrazinamide (TOPNOTCH)

97

Most active drug against M. leprae

Dapsone (TOPNOTCH)

98

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

Acedapsone (TOPNOTCH)

99

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

Clofazimine (TOPNOTCH)

100

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

Amphotericin B (TOPNOTCH)

101

WIDEST antifungal spectrum

Amphotericin B (TOPNOTCH)

102

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

Amphotericin B (TOPNOTCH)

103

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

Flucytosine (TOPNOTCH)

104

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)

Amphotericin B (TOPNOTCH)

105

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

Ketoconazole (TOPNOTCH)

106

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

Ketoconazole (TOPNOTCH)

107

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

Fluconazole (TOPNOTCH)

108

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

Fluconazole (TOPNOTCH)

109

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

Itraconazole (TOPNOTCH)

110

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

Voriconazole (TOPNOTCH)

111

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

Voriconazole (TOPNOTCH)

112

as salvage therapy in invasive aspergillosis

Posaconazole (TOPNOTCH)

113

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

Posaconazole (TOPNOTCH)

114

azoles that are limited to topical use because of systemic toxicity

Clotrimazole, miconazole, ketoconazole (TOPNOTCH)

115

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

Echinocandins: Caspofungin, anidulafungin, micafungin (TOPNOTCH)

116

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

Griseofulvin (TOPNOTCH)

117

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

Terbinafine (TOPNOTCH)

118

absorption is increased by intake of fatty meal

Griseofulvin (TOPNOTCH)

119

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

Nystatin (TOPNOTCH)

120

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

Nystatin (TOPNOTCH)

121

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

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

122

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.

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

123

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

Valacyclovir (TOPNOTCH)

124

____ is a prodrug which is converted to Penciclovir in vivo

Famciclovir (TOPNOTCH)

125

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

Docosanol (TOPNOTCH)

126

Inhibits viral DNA polymerase causing chain termination, guanosine derivative

Ganciclovir, valganciclovir (TOPNOTCH)

127

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

Ganciclovir, valganciclovir (TOPNOTCH)

128

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

Cifodovir (TOPNOTCH)

129

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

Foscarnet (TOPNOTCH)

130

adenine analog ; For HSV, VZV, CMV

Vidarabine (TOPNOTCH)

131

pyrimidine analogs ; For herpes keratitis (HSV-1)

Idoxuridine, trifluridine (TOPNOTCH)

132

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

Fomivirsen (TOPNOTCH)

133

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

NRTI (TOPNOTCH)

134

NRTIs

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

135

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

NNRTI (TOPNOTCH)

136

NNRTIs

Delavirdine, efavirenz, etravirine, nevirapine (TOPNOTCH)

137

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

Protease Inhibitor (TOPNOTCH)

138

Protease Inhibitor

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

139

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

Fusion Inhibitor: Enfuvirtide (TOPNOTCH)

140

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

CCR5 receptor antagonist: Maraviroc (TOPNOTCH)

141

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

Uncoating inhibitors: Amantadine, rimantadine (TOPNOTCH)

142

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

Neuraminidase inhibitors: Oseltamivir, zanamivir (TOPNOTCH)

143

DOC for influenza (including H1N1)

Neuraminidase inhibitors: Oseltamivir, zanamivir (TOPNOTCH)

144

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

Interferon (TOPNOTCH)

145

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

Interferon (TOPNOTCH)

146

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

Adefovir, Dipivoxil, Telbivudine, Tenofovir (TOPNOTCH)

147

______ is a prodrug of Adefovir

Dipiroxil (TOPNOTCH)

148

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

Tenofovir (TOPNOTCH)

149

guanosine nucleoside, inhibits DNA polymerase

Entecavir (TOPNOTCH)

150

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

lamivudine (TOPNOTCH)

151

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

Ribavirine (TOPNOTCH)

152

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

Ribavirine (TOPNOTCH)

153

Prevents polymerization of heme into hemozoin, blood schizonticide

Chloroquine, hydroxychloroquine (TOPNOTCH)

154

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

Quinine, quinidine gluconate (TOPNOTCH)

155

DOC for malaria in pregnant patients

Quinine, quinidine gluconate (TOPNOTCH)

156

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

Mefloquine (TOPNOTCH)

157

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

Primaquine (TOPNOTCH)

158

Eradicates hypnozoites in the liver, preventing malarial relapse

Primaquine (TOPNOTCH)

159

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

Atovaquone-proguanil (TOPNOTCH)

160

also effective against Mefloquine-resistant Falciparum infection

Atovaquone-proguanil (TOPNOTCH)

161

_____ is the DOC for uncomplicated falciparum malaria in the Philippines

Co-artem (TOPNOTCH)

162

DOC for asymptomatic cyst carrier of E. histolytica

Diloxanide Furoate (TOPNOTCH)

163

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

Emetine, dehydroemetine (TOPNOTCH)

164

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

Paromomycin (TOPNOTCH)

165

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

Nitazoxanide (TOPNOTCH)

166

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

Co-trimoxazole (TOPNOTCH)

167

For prophylaxis and treatment of toxoplasmosis (DOC)

Pyrimethamine-sulfadiazine (TOPNOTCH)

168

alternative drug for Toxoplasmosis is _____

Clindamycin (TOPNOTCH)

169

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

Suramin (TOPNOTCH)

170

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

Eflornithine (TOPNOTCH)

171

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

Melarsoprol (TOPNOTCH)

172

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

Nifurtimox (TOPNOTCH)

173

DOC for Leishmaniasis

Sodium Stibogluconate (TOPNOTCH)

174

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

Mebendazole (TOPNOTCH)

175

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

Albendazole (TOPNOTCH)

176

primary drug for ascariasis, ancylostomiasis, trichuriasis

Albendazole (TOPNOTCH)

177

DOC for filariasis and eye worm disease

Diethylcarbamazine (TOPNOTCH)

178

May cause mazzotti reaction when used for onchocerciasis

Diethylcarbamazine (TOPNOTCH)

179

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

Ivermectin (TOPNOTCH)

180

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

Pyrantel pamoate (TOPNOTCH)

181

DOC for hookworm and roundworm infections

Pyrantel pamoate (TOPNOTCH)

182

DOC for trichinosis

Thiabendazole (TOPNOTCH)

183

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

Praziquantel (TOPNOTCH)

184

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

Praziquantel (TOPNOTCH)

185

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

Praziquantel (TOPNOTCH)

186

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

Niclosamide (TOPNOTCH)

187

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

Alkylating agents (TOPNOTCH)

188

Alkylating agents

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

189

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

Cyclophosphamide (TOPNOTCH)

190

Rescue therapy for cyclophosphamide

MESNA (TOPNOTCH)

191

Rescue therapy for Cisplatin

Amifostine (TOPNOTCH)

192

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

Procarbazine (TOPNOTCH)

193

SE: pulmonary fibrosis, adrenal insufficiency, skin pigmentation

Busulfan (TOPNOTCH)

194

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

Carmustine, lomustine (TOPNOTCH)

195

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

Methotrexate (TOPNOTCH)

196

Rescue therapy for methotrexate

Leucovorin (Folinic acid) (TOPNOTCH)

197

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

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

198

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

5-Fluorouracil (TOPNOTCH)

199

a deoxycytidine analog

Gemcitabine (TOPNOTCH)

200

Most specific for the S-phase of the cell cycle

Cytarabine (TOPNOTCH)

201

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

Vinca alkaloid: Vincristine, Vinblastine (TOPNOTCH)

202

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

Etoposide (TOPNOTCH)

203

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

Topotecan, irinotecan (TOPNOTCH)

204

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

Paclitaxel, docetaxel (TOPNOTCH)

205

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

Paclitaxel, docetaxel (TOPNOTCH)

206

Acts primarily in M phase of cancer cell cycle

Vinca alkaloid: Vincristine, Vinblastine (TOPNOTCH)

207

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

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

208

Rescue therapy for Doxorubicin

dexrazoxane (TOPNOTCH)

209

Most specific for the G2 phase of cell cycle

Bleomycin (TOPNOTCH)

210

SE: pneumonitis, pulmonary fibrosis, alopecia, mucocutaneous reactions

Bleomycin (TOPNOTCH)

211

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

Actinomycin D (TOPNOTCH)

212

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

TK inhibitor: Imatinib, dasatinib, nilotinib (TOPNOTCH)

213

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

Trastuzumab (TOPNOTCH)

214

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

Bevacizumab (TOPNOTCH)

215

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

Rituximab (TOPNOTCH)

216

Endogenous glycoproteins with antineoplastric, immunosuppressive and antiviral actions

Interferon alpha (TOPNOTCH)

217

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

Asparaginase (TOPNOTCH)

218

Only vitamin that can cure cancer

All-Trans retinoic acid (TOPNOTCH)

219

For acute promyelocytic leukemia

All-Trans retinoic acid (TOPNOTCH)

220

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

Prednisone (TOPNOTCH)

221

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

Tamoxifen (TOPNOTCH)

222

Androgen antagonist ; For prostate cancer

Flutamide (TOPNOTCH)

223

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

Leuprolide (TOPNOTCH)

224

Reduces estrogen synthesis by inhibiting aromatase; For breast cancer

Anastrazole (TOPNOTCH)

225

Effective againsts breast cancer that have become resistant to tamoxifen

Anastrazole (TOPNOTCH)