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55 Cards in this Set
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Herpes
Acyclovir (Zovirax) |
Effective with low toxicity
Effective against Herpes Simplex 1&2 Less potent against Varicella-Zoster |
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Herpes
Valacyclovir (Valtrex) |
Pro drug of Acyclovir
Higher plasma concentrations |
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Herpes
Acyclovir mechanism |
1) Phsophoylated by Viral thymidine kinase
2) Increased uptake into infected cells 3) Competes with dGTP 4) Inhibits viral DNA polymerase |
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Herpes
Acyclovir Pharmacokinetics |
Applied topically, orally, or IV
Excreted by Kidneys Taken 3-5 times per day |
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Herpes
Acyclovir Uses |
1) Genital Herpes
2) Less effective against treating recurrent herpes 3) Topically for Herpes Keratitis 4) IV for Herpes encephalitis/neonatal 5) Prophylaxis in organ transplant/ immunocomprimised (AIDS) for all herpes viruses |
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Herpes
Acyclovir side effects |
1) Minimal and Rare
2) Somnolence and lethargy w/ zidovidine (AZT) 3) IV=renal tubular obstruction with Cyclosporine, prevent with hydration 4) Safe in pregnancy |
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Herpes
Famciclovir (Famvir) |
1) TX Herpes Zoster or recurrent herpes
2) Phosphorylated by viral thymidine kinase, competative inhibition of DNA polymerase 3) Excreted by Kidneys 4) Longer t1/2 than Acyclovir, 2 a day dosing 5) Converted to Penciclovir |
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Herpes
Penciclovir (Denavir) |
Topical agent for Herpes Labialis
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Herpes
Docosanol (Abreva) |
1) Topically for cold sores
2) Inhibits fusion of plasma membrane and Herpes virus envelope 3) Use before sore develops to prevent it |
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CMV and/or Herpes
Ganciclovir Sodium (Cytovene) |
1) Guanosine analogue
2) Very effective against CMV, 3) More toxicity 4) CMV=phosphorylated by viral proteinkinase phosphotransferase 5) Herpes=phosphorylated by Thymidine kinase 6) Not well absorbed orally |
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CMV and/or Herpes
Gancyclovir Sodium Uses |
IV to treat life or sight threatening CMV infections
Transplant patients Ocular implant patients |
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CMV and/or Herpes
Gancyclovir Toxicity |
IV with zidovudine=Neutropenia and Thrombocytopenia
Nausea Headache |
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CMV and/or Herpes
Foscarnet (Foscavir) |
1) Analogue to inorganic pyrophosphate
2) Inhibits Viral DNA polymerase, RNA polymerase, and reverse transcriptase 3) TX acyclovir resistant HSV and CMV retinitis |
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CMV and/or Herpes
Foscarnet Side effects |
Nephrotoxic
Renal insufficiency Hypocalcemia |
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CMV and/or Herpes
Fomivirsen |
Antisense compound
Inhibits Protein synthesis Opthalmic- Intravitreal injection SE- ocular inflammation and visual impairment |
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Influenza Drugs
Amantadine (Symmetrel) Rimantadine (Flumadine) |
Blocks uncoating of the virus
Well absorbed t0.5 20hrs 90% excreted by kidneys |
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Influenza Drugs
Amantadine (Symmetrel) Rimantadine (Flumadine) Uses |
Prevention and treatment of Influenza A2 (Asian) for High risk patients
Does not affect Influenza B |
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Influenza Drugs
Amantadine (Symmetrel) Rimantadine (Flumadine) Side effects |
Nausea
Mild dopamine angonist CNS effects:Hallucinations Rimantidine does not cross BBB |
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Influenza Drugs
Oseltamivir (Tamiflu) Zanamivir (Relenza) |
1) Neuraminidase inhibitors for Flu A and B
2) Inhibit release of virus from infected cells 3) Kidney excretion 4) Some resistance Influenza A 5) Zanamivir intranasally or oral inhaler |
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Influenza Drugs
Oseltamivir (Tamiflu) Zanamivir (Relenza) Side Effects |
Zanamivir:
1) Worsen Respiratory function in patients with COPD 2) Bronchospasm in Asthma Oseltamivir: Nausea and Vomiting |
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RSV Drugs
Ribavirin (Virazole) |
Purine Nucleoside analogue
Tx: RSV, HSV, Flu Combined with Interferon for TX of Hepatitis C |
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RSV Drugs
Ribavirin (Virazole) Mechanism |
Inhibits viral mRNA, protein synthesis and viral replication
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RSV Drugs
Ribavirin (Virazole) Uses |
Hospitalized infants and children with severe Lower respiratory tract infection given Aerosol
Lassa Fever: IV Hep C: orally with IFN-alph 2b or 2a |
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RSV Drugs
Ribavirin (Virazole) Toxicity |
Pregnancy Category X
Dyspnea, Chest soreness Cardiac arrest, Hypotension Can be absorbed Passively pregnant women should not administer it |
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RSV Drugs
Palivizumab (Synagis) |
1) Monoclonal antibody
2) Confers passive immunity 3) Once a month in high risk infants 4) Elevates Aminotransferase levels |
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Hepatitis C and B
Interferon alfa 2b and 2a mechanism |
1) Inhibit viral protein synthesis and replication
2) Induce host cell to produce enzymes that inhibit translation and synthesis of viral messenger RNA 3) Administered parentally, IV, IM, Sub Q or into lesion |
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Hepatitis C and B
Interferon alfa 2b and 2 Uses |
Hepatitis C and B
Warts and herpetic keratitis |
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Hepatitis C and B
Interferon alfa 2b and 2 Toxicity |
1) Flu like syndrome
2) Musculoskeletal effects 3) G.I. effects 4) Depression and suicide (give antidepressants) 5) Hematological effects: cytopenias 6) Cardiovascular effects: hypotension |
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Hepatitis C and B
Lamivudine (Epivir) |
1) DOC Hep B
2) Inhibits DNA polymerase and reverse transcriptase 3) Resistance may develop 4) Well tolerated |
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Hepatitis C and B
Adefovir (Hepsera) |
1) Inhibits DNA polymerase
2) Renal toxicity 3) Lactic acidosis 4) Dizziness |
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Reverse Transcriptase Inhibitors
Zidovudine (Retrovir) |
Deoxythymidine analogue
Inhibits Viral Transcriptase Virus may become resistant |
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Reverse Transcriptase Inhibitors
Zidovudine (Retrovir) Pharmacokinetics |
Absorbed rapidly
First pass metabolism Majority Liver, Rest Kidney Short action( 3 hours) Given 5 times a day |
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Reverse Transcriptase Inhibitors
Zidovudine (Retrovir) Uses |
1) HIV, AIDS, Advanced AIDS related complex
2) Early: regression of Kaposi 3) Pregnancy: reduce transmission to baby 4) High Dose: AIDS demetia 5) Psoriasis 6) Adult T cell leukemia |
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Reverse Transcriptase Inhibitors
Zidovudine (Retrovir) Toxicity |
Myelosupression-Anemia, Neutropenia
Extreme caution with patient with bone marrow supression CNS GI Lactic acidosis Hepatotoxicity Discontinue is metabolic acidosis or increasing aminotransferase levels are detected |
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Reverse Transcriptase Inhibitors
Zidovudine (Retrovir) Drug interaction |
1) Increase toxicity when administered with neurotoxic, nephrotoxic, or affect bone marrow
2) Acetaminophen or ganciclovir: Granulocytopenia 3) Acyclovir: smnolence and lethargy 4) Cimetidine and benzo: inhibit liver metabolism 5) Probenacid: impair elimination of zidovudine |
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Reverse Transcriptase Inhibitors
Lamivudine (Epivir, 3TC) |
Cytosine analogue
Competative inhibitor of reverse transcriptase Combined with zidovudine Well tolerated |
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Reverse Transcriptase Inhibitors
Tenofovir (Viread) |
Adenosine analogue
Give with food DOC with emtricitabine for naive pts SE: nausea, vomiting, ab pain, flatuence |
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Reverse Transcriptase Inhibitors
Emtricititabine (Emtriva) |
Cytosine analogue
Cross resistance likely with lamivudine Effective against HBV SE: Diarrhea, nausea, rash |
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Reverse Transcriptase Inhibitors
Didanosine, ddI (Videx) |
Inhibits mitochondrial DNA synthesis
Peripheral neuropathy |
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Reverse Transcriptase Inhibitors
Didanosine, ddI (Videx) Uses |
Combination with zidovudine for patients intolerant or resistant to zidovudine
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Reverse Transcriptase Inhibitors
Didanosine, ddI (Videx) Toxicity |
1) Pancreatitis-prior alcoholism, pentamidine
2) Peripheral neuropathy 3) Anemia and ganulocytopenia 4) Hyperuricemia 5) Discontinue if lactic acidosis or hepatotoxicity develop |
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Reverse Transcriptase Inhibitors
Abacavir (Ziagen) |
1) Guanosine analogue
2) Serious hypersensitivity-immediatly stop drug and do not restart drug 3) Nausea, vomiting, Diarrhea |
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Non Nucleotide Reverse Transcriptase Inhibitors
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Bind directly to reverse transcriptase
Do not require phosphorylation Combined with Zidovudine Metabolized by CYP3A4 |
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Non-nucleotide Reverse Transcriptase Inhibitors
Efavirenz (sustiva) |
1) DOC unless pregnant: teratogenic
2) Induces CYP3A4 decreases effectiveness of OCP and Methadone 3) SE: Dizziness, drowsiness, insomnia, headache |
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Non-nucleotide Reverse Transcriptase Inhibitors
Nevirapine (Viramune) |
1) Used in pregnancy
2) Induces CYP3A4-OCP methadone 3) Ketoconazole, cimetidine and macrolides inhibit metabolism 4) Steven-Johnson syndrome 5) Hepatitis |
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Protease inhibitors
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1) Inhibit proteases
2) Combine with Reverse transcriptase inhibitors 3) Poor bioavailability(CYP3A4) 4) St. Johns Wort renders them ineffective |
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Protease Inhibitors
Side effects |
1) Altered body fat distribution
2) Insulin resistance 3) High Cholesterol 4) Bleeding in pt with hemophilia A or B |
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Protease Inhibitors
Atazenavir (Reyataz) |
1) No cross resistance
2) Once a day administration 3) Less effect on Lipoproteins 4) Increase bilirubin due to UGT1A1 inhibition 5) SE: Rash and nausea |
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Protease Inhibitors
Ritonavir (Norvir) |
1) Can be used alone
2) Inhibits CYP3A4 3) Inhibits metabolism of other protease inhibitors, is used together to increase levels of Protease inhibitor 4) Specifically indicated with drugs that are metabolized by CYP3A4 |
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Protease Inhibitors
Ritonavir Toxicity |
Burning or tingling around mouth or in periphery
Elevated liver enzymes |
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Protease Inhibitors
Saquinavir (Invirase, Fortovase) |
Levels increase with Grapefruit juice
GI side effects |
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Protease Inhibitors
Indinavir (Crixivan) |
Good Bioavailability
Nephrolithiasis Asymptomatic hyperbilirubinemia |
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Protease Inhibitors
Lopinavir/ritonavir (Kaletra) |
Ritonavir is added to increase bioavailability of lopinavir
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Enfuvirtide (Fuzeon)
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1) No cross resistance with other antiretrovirals
2) Must be given sub Q 3) Injection site reactions common 4) Fusion inhibitors |
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Raltegravir (Isentress)
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Integrase inhibitor
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