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TB and HIV drugs
TB and HIV drugs
13
Medical
Professional
01/16/2008

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Cards

Term
Isoniazid
Definition
  • first line TB drug; cidal in growing org, narrow
  • Mech: activated by mycobacterial catalase peroxidase->INH forms complex with NAD and NADP. INH-NAD->inhib mycolic acid syn. INH-NADP->inhib mycobact DHF Reductase
  • Tox: INH neuropathy, hepatotox
Term
Rifampicin
Definition
  • 1st line TB drug
  • Mech: binds mycobact RNA pol-> inhib transcription (Euk RNAP not affected)
  • Induces P450 enzymes->increase metab of OC, hormones, coumadin
Term
Pyrazinamide
Definition
  • 1st line TB drug
  • Mech: Inhib FA Synthetase 1-> inhib building blocks for mycolic acid synthesis-> inhib wall formation
  • Wide distrib., hydrol/oxid in liver, renal elim
  • Tox: flushing, transient arthralgia, gout, hepato
Term
Ethambutol
Definition
  • 1st line TB drug, static
  • Mech: Inhib arabinogalactan syn and disrupts mycolic acid attachment in mycobact. cell wall
  • Wide distrib, including CNS; renal elim
  • Tox: optic neuritis, loss of visual acuity, loss of abil to perceive green
Term
Azidothymidine (AZT)
Definition
  • Nucleoside RTI, Anti-AIDS
  • Mech: AZT is phosphorylated by TK->AZT-TP->selective for HIV-RT; chain terminator
  • Tox: bone marrow suppression, granulocytopenia, anemia, neurotox, N,V, headache, insomnia, myalgia
Term
Stavudine (d4T)
Definition
  •  Mech: RTI, chain terminator after uptake/Pation in host
  • Contraindicated w/ AZT--antagonistic
  • Tox: 20% periph neuropathy, 1% pancreatitis (incr w/ ddl), lactic acidosis
Term
Dideoxyinosine (ddI)
Definition
  • Mech: RTI, DNA Chain terminator after cellular phosphorylation; some selectivity for HIV-RT and mitochondrial DNAP
  • Can be used in place of AZT
  • Tox: periph neuropathy, pancreatitis, neutropenia, steatosis, hepatotox.
Term
Lamivudine (3TC)
Definition
  • Mech: RTI, chain terminator
  • Less active, less toxic than AZT
  • Resistance arises, with cross resistance to ddI, abacavir; prevents resistance to AZT
  • Used for HIB, hep B/C
Term
Abacavir
Definition
  • Mech: Guanosine nt analog, potent RTI, chain terminator; Metab by etoh dehydrog, elim urine
  • Penetrates CNS
  • Tox: Hypersensitivity rxns, fever, rash, Resp
Term
Tenofovir (PMPA)
Definition
  • Mech: Pated to triphospate-> nt RTI; incorporated as chain terminator; weak inhib host DNAP
  • Used in combo but not w/ tenofovir/abacavir/3TC
  • Effective in resistant HIV strains
  • 1 daily dose
  • Tox: reduced
Term
Nevirapine, delavirdine, efavirenz
Definition
  • NNRTI
  • Mech: metab in liver by P450 leading to induction or acute competition(nevirapine induces, delavirdine inhib P450 enzymes)
  • Combine with NRTIs
  • Cross res occurs bet NNRTIs
  • Tox: Fever, nausea, CNS, hepato, rash
Term
Protease Inhibitors
Definition
  • Saquin-, indin-, riton-, nelfin-, ampren-, atazan-, tipran-, darun-, fosampren-, topin-avir
  • Mech: prevent cleavage of HIV protein precursors by HIV encoded aspartate proteases
  • Metab by hepatic P450 enzymes
  • Tox: NVD, ab pain, incr liver enzymes, diabetes, incr cholesterol, renal failure
Term
Enfuvirtide (Fuzeon, T-20)
Definition
  • Entry Inhibitor
  • Mech: Binds HIV surface prot gp41, precents binding to T-cells at CD4
  • Tox: NVD, neuropathy, insomnia, fatigue, depression
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