Term
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Definition
nucleotide reverse transcriptase inhibitor
MOA: inhibits RT and terminates DNA chain elongation
USE: HIV pts and chronic hep B infections
TOX: flatulence, some renal toxicity
DI: do not give with didanisone, lamuvidine, abacavir combo |
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Term
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Definition
MOA: bind to cellular receptors -> JAK/STAT pathway; induce many proteins -> inhibit protein synthesis
USE: genital warts, chronic hep B and C, kaposi's sarcoma in HIV pts, multiple myelomas, MS
-Peg-interferon 2A + Ribavirin -> chronic hep C
TOX: IM or SC injection give flu-like symptoms, high dose/chronic therapy -> bone marrow suppression, fatigue, inc suscep. to bacterial infections, anorexia, diarrhea, psychiatric syndrome (depression and anxiety) |
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Term
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Definition
fusion inhibitors
E-MOA: binds to HIV viral envelope glycoprotein and prevents conformational change
E-USE: injected twice daily in HIV pts, used with other drugs
E-TOX: pain, redness, nodule and cyst formation at site of injection
M-MOA: maraviroc is a chemokine receptor 5 inhibitor
M-USE: HIV pts
M-TOX: most common are cough, fever, dizziness, headache, lowered blood pressure, nausea, bladder irritation, may cause liver problems and cardiac events, an increased risk for some infections, slight increase in cholesterol levels |
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Term
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Definition
protease inhibitor combo
PK: lopinavir is metabolized by CYP3A, ritonavir is inhibitor of CYP3A -> raise levels of lopinavir
USE: treat HIV strains that are resistant to multiple protease inhibitors
TOX: well tolerated, diarrhea, nausea, fatigue, headache, hyperlipidemia, hyperglycemia, altered body fat
DI: inhibit activity of CYP4A4 and CYP2D6 |
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Term
| Atazanavir, Indinavir, Ritonavir, Lopinavir, Nelfinavir, Amprenavir, Saquinavir |
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Definition
protease inhibitors
MOA: interfere with proteoylsis of gag-pol precursor -> nonfunctional virions
USE: HIV pts must take drugs continuously in combo with AZT and Lamivudine or other NRTI
MOR: cross resistance often occurs among protease inhibitors, but HIV strains may still be susceptible to Amprenavir
TOX: well tolerated, sometimes get nausea, vomiting, diarrhea, lipodystrophy, hyperglycemia |
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Term
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Definition
non-nucleoside reverse transcriptase inhibitor
MOA: binds and inhibits RT
USE: in combo with Zidovudine and Didanosine, least potent NNRTI
DI: inhibits CYP3A4,drugs that induce CYP3A4 reduce levels of delaviridine, also inhibits CYP2C9 |
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Term
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Definition
non-nucleoside reverse transcriptase inhibitor
MOA: alters conformation of RT
USE: in combo with Didanosine or Stavudine
TOX: rash, fever, nausea, severe dermatological effects and fatal hepatotoxicity
DI: st. john's wort -> lowers conc. of nevirapine, nevirapine induces CYP3A4, nevirapine lowers plasma conc. of ethinyl estradiol so pts should be given alternative birth control |
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Term
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Definition
| nucleoside reverse transcriptase inhibitor MOA: inhibits RT and terminates DNA chain elongation USE: given with AZT or alone for those who cannot tolerate AZT-treatment, Hep B and HIV MOR: RT becomes mutated TOX: peripheral neuropathy, rash and stomatitis on initial treatments |
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Term
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Definition
nucleoside reverse transcriptase inhibitor
MOA: inhibits RT and terminates DNA chain elongation
USE: HIV infected adults and children in combo with AZT and Lamivudine or protease inhibitor
TOX: hypersensitivity resulting in fever, GI distress, malaise, rash |
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Term
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Definition
nucleoside reverse transcriptase inhibitor
MOA: inhibits RT and terminates DNA chain elongation
USE: pts with HIV in combo with AZT (resistance to AZT develops more slowly when used in combo), hep B
TOX: pancreatitis in pediatric pts
-triziir: zidovudien, lamivudine, abacavir; also lamivudine and abacavir |
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Term
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Definition
nucleoside reverse transcriptase inhibitor
MOA: inhibits RT and terminates DNA chain elongation
USE: HIV infections
TOX: peripheral neuropathy, potentially fatal lactic acidosis, peripheral lipoatrophy, central fat accumulation, hyperlipidemia |
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Term
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Definition
nucleoside reverse transcriptase inhibitor
MOA: inhibits RT and terminates DNA chain elongation
USE: pts with AZT-resistant HIV infections
MOR: RT becoes mutated
TOX: pancreatitis (fatal), GI disturbances, dose-limiting peripheral neuropathy, non-cirrhotic portal HTN (fatal)
DI: toxicity increases when combo with stavudine |
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Term
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Definition
nucleoside reverse transcriptase inhibitor
MOA: thymidine kinase converts drug to AZT-TP which is incorporated into viral DNA and terminates chain elongation
USE: HIV pts (protects fetus from become infected by HIV mother)
MOR: mutated RT that has lower affinity for AZT-TP
TOX: bone marrow (anemia and leukopenia), headaches; potentially fatal lactic acidosis, peripheral lipoatrophy, central fat accumulation, hyperlipidemia
DI: Probenecid, Acetaminophen, Lorazepam, Indomethacin, Cimetidine -> increase toxicity of AZT
-Trizivir: Zidovudine, Lamivudine, Abacavir |
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Term
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Definition
synthetic guanosine analog
MOA: inhibits viral mRNA synthesis
USE: ribavirin w/ IFN -> hep C; infants and young children with respiratory syncytial virus infection -> bronchiolitis and pneumonia, influenza A and B, parainfluenza, paramyoxvirus, arenavirus, HIV
TOX: aerosol well tolerated, systemic doses -> anemia, teratogenic -> no pregnant women |
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Term
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Definition
neuraminidase inhibitors
MOA: inhibit neuraminidases -> decreased release of virus from infected cells, increased formation of viral aggregates, decreased viral spread
Z-USE: shortens duration and may be used to prevent flu (within 30 hrs of onset)
Z-TOX: nasal and throat discomfort, headaches, bronchospasm in asthma pts
O-USE: shortens the duration and may be used to prevent flu (within 36 hrs of onset)
O-TOX: nausea (reduced if taken with food), vomiting, headaches
-both treat influenza A and B, H1N1 |
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Term
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Definition
iodinated thymidine analog
MOA: inhibits viral DNA synthesis, incorporated into viral and cellular DNA -> more susceptible to breaks -> error-prone transcription
USE: topical txt of HSV keratitis
TOX: pain, inflammation, edema of eyes or lips |
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Term
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Definition
pyrimidine analog
MOA: inhibits viral DNA synthesis
USE: HSV keratoconjunctivitis and keratitis
TOX: inflammation of cornea
-replaced the drug Idoxuridine |
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Term
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Definition
inorganic pyrophosphate analog
MOA: reversibly inhibit viral DNA and RNA polymerases
USE: IV treatment for CMV retinitis in HIV-infected pts who are resistant to ganciclovir, herpes pts resistant to acyclovir
TOX: nephrotoxicity, anemia, nausea, fever, hypocalcemia, hypomagnesemia |
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Term
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Definition
guanine nucleoside analog
MOA: comp inhibit viral DNA polymerase, block elongation
USES: CMV retinitis in immunocomp pts, prevention of CMV in transplant pts
TOX: dose-dependent neutropenia, CNS effects (heachache, behavioral changes, convulsions, coma), carcinogenic
-half life: > 24 hrs
-ganciclovir conc. 10X that of acyclovir |
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Term
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Definition
guanine nucleoside analog
MOA: viral thymidine kinase gene phosphorylates drug -> acyclovir triphosphate which competes with dGTP and incorporated into DNA -> premature chain termination
USES: HSV and VZV
MOR: due to altered/deficient thymidine kinase or polymerase
TOX: nausea, headache, diarrhea, vomiting, transient renal dysfunction @ high doses or when given IV to dehydrated pt
-oral or IV admin (systemic)
-half life: 2.5hrs |
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