Term
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Definition
1. MOA- blocks viral penetration/uncoating (M2 protein); may buffer pH of endosome- also causes the release of dopamine from intact nerve terminals
2. Clinical use: prophylaxis and treatment of Influenza A, Parkinson's disease
3. Toxicity- ataxia, dizziness, slurred speech
4. Resistance- mutated M2 protein, 90% of influenza strains are resistant so not used
"A man to dine" takes off his coat
Amantadine blocks influenza A and RubellA and causes problems with the cerebellA
Rimantidine is a derivative with fewer CNS side effects, does not cross the BBB |
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Term
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Definition
1.Inhibits synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenase thus interfering with mRNA synthesis
2. Clinical use for RSV, chronic Hep C (with INF alpha)
3. Toxicity- hemolytic anemia, severe teratogen |
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Term
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Definition
1. 2 deoxyguanosine analog converted to acyclovir-TP by thymidine kinase; preferentially inhibits viral DNAP by chain termination
2. Used in HSV (mucocutaneous, genital and encephalitis), VZV (famciclovir) and EBV
3. no effect on latent forms of HSV and VZV
4. Toxicity- generally well tolerated; some nephrotoxicity and neurotoxicity
5. Resistnace by lack of thymidine kinase |
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Term
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Definition
1. 5'-monophosphate formed by a CMV viral kinase or HSV/VZV thymidine kinase; guanine analog which preferentially inhibits viral DNAP, triphosphate formed by cellular kinases
2. cross-resistance with acyclovir (mutated CMV DNAP or lack of viral kinase)
3. Toxicity- leukopenia, neutropenia, thrombocytopenia, renal toxicity (more toxic than acyclovir) |
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Term
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Definition
1. pyrophosphate (non-nucleotide) analog complexes with viral DNAP- does not require activation by viral kinase
2. Use- CMV retinitis in immunocompromised patients when ganciclovir fails; acyclovir resistant HSV
3. nephrotoxicity- direct damage to renal tubules; hydrate with NS
4. Ca and P supplement for BM suppression
5. Resistance by mutated DNAP |
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Term
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Definition
1.Saquinavir, Ritonavir, Amprenavir, Atazanvir, fosamprenavir, lopinavir, nelfinavir, indinavir
2. Prevent cleavage of precursor proteins necessary for HIV maturation
3. Toxicity- GI intolerance, hyperglycemia, lipodystrophy, thrombocytopenia (indinavir)
3. Ritonavir increases concentration of other protease inhibitors and is used to potentiate their effects
4. NAVIR TEASE a proTEASE
5. Do not take simvastatin, lovastatin, rifampin, midazolam, ergotamine or st johns wort
6. Use azole, rifabutin, OC, anticonvulsants, methadone, and viagra with caution
7. azoles and rifabutin decrease PI
8. rifampin and rifabutin decrease PI |
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Term
Nucleoside Reverse Transcriptase Inhibitors |
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Definition
1.Zidovudine (ZDV, formerly AZT), didanosine (ddI), Zalcitabine (ddC), Stavudine (d4T), lamivudine (3TC), Abacavir
2. require phosphorylation to inhibit DNAP
Have you dined with my nuclear family |
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Term
Non-Nucleoside Reverse Transcriptase Inhibitors |
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Definition
1. Nevirapine, Efavirenz, Delaviridine
2. MOA- preferentially inhibit RT of HIV, prevent incorporation of DNA copy of viral genome into host DNA
4. Do not take simvastatin, lovastatin, rifampin, midazolam, ergotamine or st johns wort
5. Use azole, rifabutin, OC, anticonvulsants, methadone, and viagra with caution |
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Term
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Definition
1. glycoproteins from human leukocytes that block various stages of viral RNA and DNA synthesis; induce ribonuclease that degrades viral mRNA
2. INF-alpha for chronic hep B and C, or Kaposi's sarcoma
3. INF-beta for multiple sclerosis
4. INF-gamma for NADPH oxidase deficiency
5. Toxicity- neutropenia |
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Term
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Definition
1. Converted to acyclovir by GI
2. Better BA, only oral
3. Better tolerated, but less side effects compared to acyclovir |
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Term
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Definition
1. Guanine analog similar to acyclovir
2. cross-resistant with acyclovir |
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Term
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Definition
1. opthalmic agents for keratitis
2. lack of viral selective leading to excessive toxicity if used systemically |
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Term
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Definition
1. Abreva- topical cream
2. inhibits fusion between plasma membrane and HSV envelope |
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Term
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Definition
1. prodrug of ganciclovir makes po better |
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Term
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Definition
1. nucleotide analog inhibiting DNAP
2. cross resistance
3. dose dependent nephrotoxicity (avoid CrCl <55 ml/min)
4. Used for CMV retinitis with probenecid and NS |
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Term
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Definition
1. Oseltamivir- metabolized to GS4071 for prophylaxis of influenza A or B
2. Neuraminidase is located on the surface of the virus and cleaves terminal sialic acid residue from host receptor and viral GP to promote release
3. Nasal Zanamavir- avoid in pts with chronic respiratory disease |
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Term
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Definition
1. pyrimidine nucleoside analog phos IC
2. inhibits hep B DNAP and HIV RT
3. RT mutations occur rapidly when monotherapy
4. myalgias
5. pancreatitis in pediatrics>adults |
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Term
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Definition
1. guanosine analog inhibiting HBV DNAP
2. not active v lamibudine resistance |
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Term
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Definition
1. Adenine nucleotide
2. nephrotoxicity
3. active against lamivudine resistance
4. improves liver and seroconversion |
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Term
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Definition
1. inhibits HBV polymerase
2. myopathy
3. cross-resistance with lamivudine |
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Term
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Definition
1. goal is suppression not eradication
2. HBeAg +, HBV DNA, elevated ALT
3. AntiHBe = resistance
4. Continue treatment 6 months after seroconversion |
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Term
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Definition
1. Goal is to eradicate virus and limit liver damage
2. HCV antibody, RNA quantity, genotype
3. IFN + ribavirin for 24 week if G1 or G4 and 48 weeks if G2 or G3 |
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Term
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Definition
1.Inhibit viral DNA insertion |
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Term
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Definition
1.Enfuvirtide
2. bind gp41 and CCR5 inhibiting conformational change required for fusion with CD4 cells therefore blocking entry and subsequent replication
3. Toxicity: hypersensitivity reactions, reactions at subcutaneous injection site, increased risk of bacterial pneumonia
4. Used in patients with persistent viral replication in spite of antiviral therapy |
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Term
Toxicity of Reverse Transcriptase inhibitors |
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Definition
Bone marrow suppression, peripheral neuropathy, lactic acidosis (nucleosides), rash (non-nucleosides), megaloblastic anemia (ZDV) |
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Term
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Definition
1. inhibit influenza neuraminidase, decreasing release of viral progeny
2. Used for influenza A and B |
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