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166 Cards in this Set
- Front
- Back
Drug
|
Mech
|
|
Amantadine
|
blocks viral uncoating of influenza A via inhibition of the integral membrane ion channel M2; preventing release of ribonucleoproteins from the virion interior
|
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Rimantadine
|
inhibits M2 ion channel, blocks viral uncoating, prevents virus contents from entering cell nucleus
|
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Acyclovir
|
Nucleoside analog; Converted to monophosphate then triphosphate (not a prodrug though) by a viral thymidine kinase, inhibiting DNA synthesis and viral replication
|
|
Valacyclovir
|
prodrug of acyclovir
|
|
Famciclovir
|
Prodrug of Penciclovir
|
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Oseltamivir
|
Neuraminidase Inhibitors (NO cleavage of sialic acid/hemagglutinin); virus stuck to cell, not released
|
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Zanamivir
|
Neuraminidase Inhibitors (NO cleavage of sialic acid/hemagglutinin); virus stuck to cell, not released
|
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Ribavirin
|
Fraudulent guanosine nucleotide, interferes with DNA replication or RNA synthesis
|
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Enfuvirtide
|
binds to first heptad-repeat (HR1) in gp41, inhibits gp41 conformational change; prevents membrane fusion
|
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Zidovudine
|
thymidine analog for HIV RNA-dependent DNA polymerase; phosphorylate to active form
|
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Abacavir
|
guanosine analog
|
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Lamivudine
|
cytosine nucleoside analog
|
|
Adefovir
|
adenosine analog
|
|
Telbivudine
|
thymidine analog
|
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Didanosine
|
Nucleoside/tide Reverse Transcriptase Inhibitors
|
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Stavudine
|
Nucleoside/tide Reverse Transcriptase Inhibitors
|
|
Emtricitabine
|
Nucleoside/tide Reverse Transcriptase Inhibitors
|
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Entecavir
|
Nucleoside/tide Reverse Transcriptase Inhibitors
|
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Tenofovir
|
prodrug, nucleotide reverse transcriptase inhibitor
|
|
Efavirenz
|
NNRTI, works like NTRI except does NOT need to be phosphorylated
|
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Nevirapine
|
NNRTI
|
|
Delavirdine
|
NNRTI
|
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Atazanavir
|
inhibits viral proteases, limits cleavage of HIV proteins gag and pol, decreased proteins for transformation to mature infectious form
|
|
Fosamprenavir
|
Prodrug, protease Inhibitors
|
|
Indinavir
|
Protease Inhibitors
|
|
Ritonavir
|
Protease Inhibitors
|
|
Saquinavir
|
Protease Inhibitors
|
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Tipranavir
|
Protease Inhibitors
|
|
Raltegravir
|
Inhibits integrase, prevents viral DNA from integrating into human DNA
|
|
Maraviroc
|
Binds to chemokine coreceptor CCR5 on human CD4, inhibits interaction of CCR5 and gp120 of virus
|
|
Interferon
|
binds to cognate RTKs→ Jak/STAT signaling pathway to eventually induce transcription of genes involved in viral defense (inhibitors of viral protein synthesis)
|
|
Ivermectin
|
opens glutamate sensitive chloride channels, muscle paralysis
|
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Albendazole
|
degeneration of cytoplasmic microtubules, glucose depletion, death of worm
|
|
Mebendazole
|
degeneration of cytoplasmic microtubules, glucose depletion, death of worm
|
|
Thiabendazole
|
degeneration of cytoplasmic microtubules, glucose depletion, death of worm
|
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Triciabendazole
|
degeneration of cytoplasmic microtubules, glucose depletion, death of worm
|
|
Praziquantel
|
Increased Ca2+ permeability, contractile paralysis, detachment of suckers
|
|
Oxamniquine
|
tetrahydroquinolone derivative
|
|
Nitazoxanide
|
nitrosthiazolyl-salicylamide derivative
|
|
Amantadine
|
inhibits M2 ion channel, blocks viral uncoating, prevents virus contents from entering cell nucleus
|
|
Rimantadine
|
inhibits M2 ion channel, blocks viral uncoating, prevents virus contents from entering cell nucleus
|
|
Acyclovir
|
Nucleoside analog, inhibiting DNA synthesis and viral replication
|
|
Valacyclovir
|
prodrug of acyclovir
|
|
Famciclovir
|
Prodrug of Penciclovir
|
|
Oseltamivir
|
Neuraminidase Inhibitors (NO cleavage of sialic acid/hemagglutinin); virus stuck to cell, not released
|
|
Zanamivir
|
Neuraminidase Inhibitors (NO cleavage of sialic acid/hemagglutinin); virus stuck to cell, not released
|
|
Ribavirin
|
Fraudulent guanosine nucleotide, interferes with DNA replication or RNA synthesis
|
|
Enfuvirtide
|
binds to first heptad-repeat (HR1) in gp41, inhibits gp41 conformational change; prevents membrane fusion
|
|
Zidovudine
|
has triple nitrogen group that, when incorporated into RT as a thymidine nucleoSide analog, blocks addition of another base, freezing transcription and causing chain termination→ inhibits viral replication. Requires riple phosphorylation by thymidine kinase, which is only active during S phase--> only works on rapid-cycling cells
|
|
Zidovudine
|
thymidine analog for HIV RNA-dependent DNA polymerase; phosphorylate to active form
|
|
Abacavir
|
guanosine analog
|
|
Lamivudine
|
cytosine nucleoside analog
|
|
Adefovir
|
adenosine analog
|
|
Telbivudine
|
thymidine analog
|
|
Didanosine
|
Nucleoside/tide Reverse Transcriptase Inhibitors
|
|
Stavudine
|
Nucleoside/tide Reverse Transcriptase Inhibitors
|
|
Emtricitabine
|
Nucleoside/tide Reverse Transcriptase Inhibitors
|
|
Entecavir
|
Nucleoside/tide Reverse Transcriptase Inhibitors
|
|
Tenofovir
|
prodrug, nucleotide reverse transcriptase inhibitor
nucleoTide, so doesn't require phosphorylation |
|
Efavirenz
|
NNRTI, works like NTRI except does NOT need to be phosphorylated
does NOT require phosphorylation; binds to allosteric site on RT, shutting it down |
|
Nevirapine
|
NNRTI
does NOT require phosphorylation; binds to allosteric site on RT, shutting it down |
|
Delavirdine
|
NNRTI
does NOT require phosphorylation; binds to allosteric site on RT, shutting it down |
|
Atazanavir
|
inhibits viral proteases, limits cleavage of HIV proteins gag and pol, decreased proteins for transformation to mature infectious form
|
|
Fosamprenavir
|
Prodrug, protease Inhibitors
|
|
Indinavir
|
Protease Inhibitors
|
|
Ritonavir
|
Protease Inhibitors
|
|
Saquinavir
|
Protease Inhibitors
|
|
Tipranavir
|
Protease Inhibitors
|
|
Raltegravir
|
Inhibits integrase, which is responsible for 3' processing (cleavage of viral cDNA), carrying the cDNA to the nucleus, and ligating the ends to the host chromosome; upstream of protease inhibitors, downstream of RT
|
|
Maraviroc
|
selectively & reversibly binds CCR5 on CD4+ cells→ inhibits intxn b/w CCR5 and gp120 on virus, inhibiting virus's conformational changes required for HIV-1 fusion with CD4 cells
|
|
Interferon
|
binds to its receptor, activates transcription for genes involved in viral defense
|
|
Ivermectin
|
opens glutamate sensitive chloride channels, muscle paralysis
|
|
Albendazole
|
degeneration of cytoplasmic microtubules, glucose depletion, death of worm
|
|
Mebendazole
|
degeneration of cytoplasmic microtubules, glucose depletion, death of worm
|
|
Thiabendazole
|
degeneration of cytoplasmic microtubules, glucose depletion, death of worm
|
|
Triciabendazole
|
degeneration of cytoplasmic microtubules, glucose depletion, death of worm
|
|
Praziquantel
|
Increased Ca2+ permeability, contractile paralysis, detachment of suckers
|
|
Oxamniquine
|
tetrahydroquinolone derivative
|
|
Nitazoxanide
|
nitrosthiazolyl-salicylamide derivative
|
|
β lactams
|
Binds to transpeptidase, blocking final cross-linking step in peptidoglycan cell wall synthesis. Also messes up osmotic regulation, leading to cell lysis
|
|
β-lactamase inhibitors
|
irreversible inhibitors of β-lactamase
|
|
Glycopeptides
|
Inhibits polymerization of glycan monomers (upstream of β-lactam activity), also impairs RNA synthesis and increases permeability of cytoplasmic membrane
|
|
Polypeptides
|
inhibits transfer of peptidoglycan monomers to site of cell wall synthesis
|
|
Fluroquinolones (FQNs)
|
Blocks DNA gyrases (topoisomerases II and IV which live in bacteria) to introduce strand breaks, inhibiting DNA synthesis and transcirption
|
|
Sulfonamides
|
Depletes nucleotides via competitive inhibition of dihydropteroate synthetase, thereby blocking folic acid production and thus inhibiting DNA synthesis
|
|
Trimethoprim
|
inhibits dihydrofolate reductase, thereby blocking folic acid production and DNA synthesis
|
|
Aminoglycosides
|
Irreversible binding to 30S to inhibit protein synthesis and create wacky proteins too (dominant negative effect); Blocks initiation, elicits premature termination, and incorporates incorrect amino acids
|
|
Macrolides
|
Reversible binding to 50S inhibits translocation from A to P, inhibiting protein synthesis
|
|
Tetracyclines
|
Reversible binding to 30S blocking access to A site, inhibiting protein synthesis
|
|
Chloramphenicol
|
Reversibly binds to 50S, preventing access to A site
|
|
Tetracyclines
|
Reversible binding to 30S blocking access to A site, inhibiting protein synthesis
|
|
Streptogramins
|
Bind to 50S
|
|
Lincosamides - Clindamycin
|
Reversibly binds 50S preventing peptide bond formation and inhibiting protein synthesis
|
|
Oxazolidinones - Linezolid
|
Binds to P site of 50S, inihbiting initiation of protein synthesis
|
|
Metronidazole
|
Prodrug; forms highly reactive nitro radical anion that damages DNA
|
|
Chloroquine (Aralen)
|
raises pH in parasite vesicles, inhibiting parasite growth
|
|
Mefloquine
|
interferes with ability of schizont to use hemoglobin
|
|
Quinine (Qualaquin)
|
Depresses oxygen uptake and carb metabolism; Intercalates in DNA but not a fraudulent nucleotide
|
|
Atovaquone
|
inhibits mito electron transport, inhibiting nucleic acid synthesis
|
|
Proguanil
|
prodrug that inhibits dihydrofolate reductase, which inhibits nucleotide synthesis
|
|
Primaquine
|
Disrupts mitochondria and binds to DNA
|
|
Artemether
|
Inhibit SR and ER Ca2+ ATPase; depletion of Ca2+
|
|
Dapsone
|
Competitive antagonist of PABA (paraaminobenzoic acid) => inhibition of folic acid synthesis
|
|
Epinephrine
|
Exhibits agonist activity at ALL adrenergic receptors = +inotropic and +chronotropic effects; splanchnic vasoconstriction and skeletal muscle vasodilation; relaxation of GI, uterine and bronchial smooth muscle; elevation in serum glucose, lactate and FFA
|
|
Anti-histamines
|
binds to histamine receptor and blocks their activation; H1 receptor inverse agonist
bronchodilation, vaso/venoconstriction; dilation of endothelial cells; desensitization of afferent nerve terminals; ↓ in HR and contractility; ↓ gastric acid; sleepiness |
|
Cyclosporine
|
Inhibits transcription of Il-2 => inhibition of T cell activation; blocks interaction btw cyclophilin (or FKBP) and calcineurin
|
|
Sirolimus
|
Blocks interaction btw FKBP-12 and mTOR (kinase), mTOR cannot phosphorylate Cdk2
|
|
Mycophenolate Mofetil
|
MPA (mycophenolic acid) inhibits IMPDH (inosine monophosphate dehydrogenase) => inhibition of de novo guanosine nucleotide synthesis => inhibition of T/B cell proliferation
|
|
Muromonab-CD3
|
binds to CD3 receptor on thymocytes and T cells => disrupts TCR mediated signalling
|
|
Anti-thymocyte globin
|
Cytotoxic Ab directed at CD2, CD3, CD4, CD8, CD11a, CD18, CD25, CD44, CD45, HLA class I and class II => inhibition of lymphocyte function and direct cytotoxicity of lymphocytes
|
|
Amphotericin B
|
"pore-formation; binds to ergosterol to alter permeability and leak cell components; May also cause oxidation-dependent stimulation of macrophages
" |
|
Nystatin
|
"pore-formation; binds to ergosterol to alter permeability and leak cell components; May also cause oxidation-dependent stimulation of macrophages
" |
|
Flucytosine
|
prodrug; fraudulent nucleotide; inhibits thymidylate synthase, which interferes with RNA and protein synthesis
|
|
Fluconazole (Diflucan)
|
Blocks 14a-demethylase; inhibition of lanosterol to ergosterol
|
|
Miconazole
|
Blocks 14a-demethylase; inhibition of lanosterol to ergosterol
|
|
Clotrimazole
|
Blocks 14a-demethylase; inhibition of lanosterol to ergosterol
|
|
Caspofungin
|
Inhibits B-glucan synthase that disrupts cell wall synthesis and integrity
|
|
Terbinafine
|
inhibits squalene epoxidase, which accumulates toxic amounts of squalene and decreased sterol production resulting in membrane transport dysfunction
|
|
Griseofulvin
|
Blocks microtubule polymerization, disrupting mitotic spindle formation and mitosis
|
|
Rifampin
|
Inhibits b subunit of bacterial RNA polymerase, suppressing RNA transcription
|
|
Isoniazid/INH
|
Prodrug; inhibits enoyl-ACP reductase of fatty acid synthase → inhibition of mycolic acid synthesis → dysfunctional MB cell walls
|
|
Pyrazinamide
|
Prodrug; lowers ambient pH, inhibiting growth of bacteria
|
|
Ethambutol
|
Unclear; may inhibit arabinosyl transferase→ inhibition of arabinogalactan, a component of the MB cell wall
|
|
Aspirin
|
Irreversible inhibitor of COX, covalently modifies COX-1 and COX-2; Low dose aspirin inhibits thromboxane production, but does not affect prostacyclin production = ANTICOAGULANT
|
|
Celecoxib
|
Selective COX-2 inhibitor; Inhibit prostacyclin production, but not thromboxane production = PROCOAGULANT
|
|
Rofecoxib
|
Selective COX-2 inhibitor; Inhibit prostacyclin production, but not thromboxane production = PROCOAGULANT
|
|
Ibuprofen
|
Non-selective COX inhibitor; Reversible inhibits platelet function and increases bleeding time
|
|
Ketoprofen
|
Non-selective COX inhibitor
|
|
Naproxen
|
Non-selective COX inhibitor
|
|
Flurbiprofen
|
Non-selective COX inhibitor
|
|
Oxaprozin
|
Non-selective COX inhibitor
|
|
Acetaminophen
|
Non-selective COX inhibitor
|
|
NSAID (general)
|
inhibit the cyclooxygenase enzyme, inhibits conversion of aa to prostaglandins and thromboxanes
|
|
Penicillin G
|
Binds to transpeptidase, blocking final cross-linking step in peptidoglycan cell wall synthesis. Also messes up osmotic regulation, leading to cell lysis
|
|
Penicillin V
|
Binds to transpeptidase, blocking final cross-linking step in peptidoglycan cell wall synthesis. Also messes up osmotic regulation, leading to cell lysis
|
|
Nafcillin
|
Binds to transpeptidase, blocking final cross-linking step in peptidoglycan cell wall synthesis. Also messes up osmotic regulation, leading to cell lysis
|
|
Oxacillin
|
Binds to transpeptidase, blocking final cross-linking step in peptidoglycan cell wall synthesis. Also messes up osmotic regulation, leading to cell lysis
|
|
Dicloxacillin
|
Binds to transpeptidase, blocking final cross-linking step in peptidoglycan cell wall synthesis. Also messes up osmotic regulation, leading to cell lysis
|
|
Ampicillin
|
Binds to transpeptidase, blocking final cross-linking step in peptidoglycan cell wall synthesis. Also messes up osmotic regulation, leading to cell lysis
|
|
Clavulanic acid
|
irreversible inhibitors of β-lactamase
|
|
Sulbactam
|
irreversible inhibitors of β-lactamase
|
|
Vancomycin
|
Inhibits polymerization of glycan monomers (upstream of β-lactam activity), also impairs RNA synthesis and increases permeability of cytoplasmic membrane
|
|
Bacitracin
|
inhibits transfer of peptidoglycan monomers to site of cell wall synthesis
|
|
Quinupristin
|
Bind to 50S
|
|
Dalfopristin
|
Bind to 50S
|
|
Clindamycin
|
Reversibly binds 50S preventing peptide bond formation and inhibiting protein synthesi
|
|
Linezolid
|
Binds to P site of 50S, inihbiting initiation of protein synthesis
|
|
Pyrimethamine
|
DHFR inhibitor
|
|
Tacrolimus
|
Binds to FKBP-12, complex of which then inhibits calcineurin and NFAT and IL-2 transcription
|
|
Everolimus
|
= Sirolimus
binds to FKBP-12→ complex binds to and inhibits mTOR from phosphorylating and activating Cdk2 (which allows cell cycle to advance)→ inhibits G1-S phase progression |
|
Methotrexate
|
competitive inhibitor of DHFR, which is nec. for synthesis of folates, pyrimidines, nucleotides and cellular division
|
|
Ivermectin Use:
|
Onchocerca volvulus, Strongyloidiasis
|
|
Albendazole, Mebendazole, Thiabendazole Triclabendazole Uses:
|
Broad → neurocysticercosis, Echinococcus granulosus, Asceris, hookworms
|
|
Praziquantel Use
|
most flatworms (cestodes and trematodes) inc. schistosomiasis
|
|
Diethylcarbamazepine Use
|
treats lymphatic filariasis
|
|
Ozamniquine use
|
alternative treatment for Schistosoma mansoni
|
|
Pyrantel Use
|
active against ascariasis, enterobiases, trichostrongylus, and hookworms
|
|
Nitrazoxanide Use
|
cryptosporidiosis and giardiasis in kids; also activity against Ascaris
|
|
Cyclosporine and Tacrolimus Use
|
Rheumatoid arthritis, psoriasis, ulcerative colitis, prophylaxis of acute GVHD (cyclosporine) or tx of chronic GVHD
|
|
Sirolimus and Everolimus Use
|
prophylaxis of organ rejection in renal transplants
|
|
Mycophenolate Mofetil Use
|
prophylaxis of organ rejection in renal, cardiac, or hepatic transplants; tx of chronic GVHD
|
|
Methotrexate Use
|
prevention of acute GVHD, esp. after HSCT
|
|
Muromonab-CD3 Use
|
prevention of transplant rejection
|
|
List all 5 MRSA agents:
|
1) 5th generation Cephalosporins (Ceftobiprole, Ceftaroline)
2) Vancomycin 3) Sulfonamides 4) Streptogramins (Quinupristin, Dalfopristin) 5) Linezolid |
|
List all Pseudomonas agents
|
1) 3rd and 4th generations Penicillins (Ticarcillin, Pipercillin)
2) Aztreonam 3) Carbapenems 4) 3rd-5th Cephalosporins 5) FQNs 6) Aminoglycosides 7) Tetracyclines |