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166 Cards in this Set

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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
Rimantadine
inhibits M2 ion channel, blocks viral uncoating, prevents virus contents from entering cell nucleus
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
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
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
Efavirenz
NNRTI, works like NTRI except does NOT need to be phosphorylated
Nevirapine
NNRTI
Delavirdine
NNRTI
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, 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
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
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