VII - Topnotch Pharma Flash Cards - Chemotherapeutic Drugs
1
Q
Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial cell walls
A
Penicillin, Cephalosporins (TOPNOTCH)
2
Q
DOC for syphillis, for streptococcal, meningococcal, G+ bacilli, spirochete infection
A
Natural Penicillins: Penicillin G, Penicillin V (narrow spectrum penicillin) (TOPNOTCH)
3
Q
For staphylococcal infections
A
Anti-Staphylococcal Penicillins: Methicillin, nafcillin, oxacillin, cloxacillin (very narrow spectrum) (TOPNOTCH)
4
Q
all penicillins are excreted unchanged in the urine EXCEPT for _____which is excreted in the bile
A
Nafcillin (TOPNOTCH)
5
Q
Pens For enterococci, Listeria, E. coli, Proteus, H. influenza, Moraxella
A
Extended Spectrum Penicillin: Ampicillin, Amoxicillin (TOPNOTCH)
6
Q
Pens For Pseudomonas, Enterobacter, Klebsiella
A
Antipseudomonal Penicillin: Piperacillin, ticarcillin, carbenicillin (TOPNOTCH)
7
Q
all Cephs have renal excretion EXCEPT ______
A
Cefoperazone and Ceftriaxone (TOPNOTCH)
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)
9
Q
Increases nephrotoxicity of aminoglycosides
A
Cephs (TOPNOTCH)
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)
11
Q
Second Generation Cephs
A
Cefamandole, cefaclor, cefonicid, cefuroxime, cefprozil, loracarbef, ceforanide, cefoxitin, cefmetazole, cefotetan (TOPNOTCH)
12
Q
First Generation Cephs
A
Cefazolin, cefadroxil, cephalothin, cephapirin, cephradine, cephalexin (TOPNOTCH)
13
Q
Cephs with slight less activity against G+ but extended G- activity
A
Second Generation Cephs (TOPNOTCH)
14
Q
decreased gram + coverage, increased gram - activity (pseudomonas, bacteroides), against Providencia, Serratia, Neiserria, Haemophilus ; DOC for gonorrhea
A
Third Generation Cephs (TOPNOTCH)
15
Q
DOC for gonorrhea
A
Ceftriaxone and Cefixime (TOPNOTCH)
16
Q
Third Generation Cephs
A
Cefoperazone, cefotaxime, ceftizoxime, ceftriaxone, cefixime, cefpodoxime proxetil, cefdinir, ceftibuten (TOPNOTCH)
17
Q
all can Third gen Cephs can penetrate the BBB EXCEPT _____
A
Cefoperazone and Cefixime (TOPNOTCH)
18
Q
More resistant to beta-lactamase produced by Enterobacter, Haemophilus, Neisseria and Pneumococcal
A
Fourth Generation Cephs (TOPNOTCH)
19
Q
Fourth Generation Cephs
A
Cefipime (TOPNOTCH)
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)
21
Q
Carbapenems
A
Imipenem-cilastatin , ertapenem, meropenem (TOPNOTCH)
22
Q
Imipenem given with Cilastatin which acts as ______
A
Dehydropeptidase enzyme inhibitor (TOPNOTCH)
23
Q
Monobactam
A
Aztreonam (TOPNOTCH)
24
Q
Resistant to beta-lactamase, no activity against gram + bacteria or anaerobes
A
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)
