Term
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Definition
Class: anti-viral, nucleoside analogue
Mechanism: competitive inhibitor of nucleic acid polymerases, suicide substrate (no 3'-OH), activated by viral enzyme
Indication: HSV, VZV, CMB
Adverse Effects: associated with rapid high Iv dose, neprhotoxicity
Drug interactions: other neprhotoxic drugs, Zidovudine (may cause extreme lethargy)
Absorption: oral (F=10-30%), topical
Distribution: wide, CSF=50%serum
Elimination: kidney
Half-life: 3hrs |
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Term
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Definition
Class: anti-viral, nucleoside analogue
Mechanism: competitive inhibitor of nucleic acid polymerases, chain terminator, activated by viral enzyme
Indication: CMV (pneumonia or retinitis), typically in immunocompromised
Adverse Effects: more toxic than acyclovir, but more potent vs. CMV, bone marrow suppresion, nephrotoxicity
Drug interactions: other nephrotoxic drugs
Absorption: intravitreal, IV, oral (F=6-9%)
Distrubtion: wide, CSF=50%serum
Elimination: kidney
Half-life: 3hrs |
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Term
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Definition
Class: anti-viral, non-nucleoside polymerase inhibitor
Mechanism: mimics ATP and inhibits viral DNA pol, RNA pol and HIV RT
Indication: CMV retinitis if gangciclovir fails usually immunocompromised, HSV and VZV if acyclovir fails
Adverse effects: nephrotoxicity, hypocalcemia (headache and anxiety)
Drug interactions: other nephrotoxic drugs, penatamine (increase hypocalcemia risk)
Absorption: IV only
Elimination: kidney |
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Term
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Definition
Class: anti-viral, inhibit uncoating
Mechanism: target M2 viral proton channel, inhibits uncoating
Indication: Influenza A (prophylaxis and tx)
Adverse effects: CNS - ataxia, insomnia, seizures
Drug interactions: antihistamines, anticholinergics, alcohol (increase CNS effects)
Absorption: oral, rapid and total
Distribution: penetrates nasal and lung secretions
Elimination: >90% unchanged in urine
Half-life 12-18hrs (young adult), double for elderly or renal impairment |
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Term
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Definition
Class: anti-viral, blocks viral release
Mechanism: sialic acid analogue, inhibits neuraminidase which normally cleaves sialic acid for relase of virus from host cell
Indication: Influenza A & B, only w/in 48hr of onset, active against amantadine resistant Influenza A
Adverse effects: mild to moderate GI distress, might have assoc. behavioral problems long-term
Absorption: rapid oral
Elimination: 1* kidney, decreased dsoe for children and renal impairment |
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Term
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Definition
Class: anti-viral, blocks mRNA metabolism
Mechanism: guanosine analong inhibits IMPDH which normally makes the GTP for RNA and DNA synthesis
Indication: chronic hepatitis C (oral w/ IFN) and RSV in children (inhaled)
Contraindication: pregnancy (totally not used, 6mo washout period after long-term tx)
Adverse Effects: hemolytic anemia (dose-related, reversible)
Absorption: oral or inhaled
Distribution: wide, CSF, conc. in RBCs (half-life up to 40 days)
Elimination: hepatic metabolism, renal excretion |
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Term
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Definition
Class: anti-retroviral, NRTI
Mechanism: competitive inhibitor of viral RT, chain terminator, host cell activates by phosphorylation
Indication: suppression of HIV infection in combo therapy, elevates CD4
Drug interactions: poop tons
Adverse effects: granulocytopenia (up to 45%), anemia, headache, nausea, lactic acidosis (mitochondrial damage), hepatotoxicity
Absorption: oral (60-65%), higher for most NRTIs, IV possible
Distributio: lipophilic, CSF60%serum
Elimination: kidney, rapid |
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Term
NRTI drug interactions
(what other drugs do to them) |
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Definition
Acetaminophen/aspirin - slow glucoronide formation, block elimination
Alcohol, estrogens, pentamidine, tetracyclines, sulfonamides - increases risk of pancreatitis
Cisplastin, isoniazid, metronidazole, vincristine - increase risk of peripheral neurophathy
Cytotoxic drugs - interfere with absorption
Fluoroquinolones, tetracyclines, ketoconazole - interfere with oral absoprtion
Probenecid/nephrotoxic drugs - slow renal excretion, increase toxicity
Ribavirin, stavudine - blocks phosphorylation required for anti-HIV activity |
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Term
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Definition
class: anti-retroviral
oral, gell only 39% reduction in infection rate |
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Term
| tenofovir + emtricitabine |
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Definition
oral, pill only 50-60% reduction in infection rate
class: anti-retroviral |
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Term
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Definition
Class: anti-retroviral, NNRTI
Mechanism: non-competitive inhibitors of HIV RT
Indication: HIV suppression combo therapy
Adverse effects: allergice reaction (rash, life threatening <2%), liver toxicity
Drug interactions: increases protease inhibitor metabolism (increase PI dose), rifampicin lovers NVP levels [don't co-administer]
Absorption: oral(F=>90%), lower for other NNRTIs
Distribution: highly lipophilic, wide
Elimination: hepatic, induces CYP450s
Half-life: 25-30hrs |
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Term
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Definition
Class: anti-retroviral, protease inhibitor
Mechanism: inhibits HIV protease
Indication: HIV suppression combo therapy
Adverse Effects: altered lipid metabolism ("buffalo hump"), hyperglycemia, nephrolithiasis (kidney stones)
Drug interactions: CYP3A4 metabolized drugs may increase in conc. or may increase the metabolism of PIs
Absorption: oral(F=60-65%), impaired by high fat meal
Elimination: <20% excreted unchanged, CYP3A4 metabolism |
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Term
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Definition
3+ classes of anti-retroviral drugs
Zidovudine - NNRTI
Protease inhibitor
NNRTI |
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