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112 Cards in this Set
- Front
- Back
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Which drugs are used to treat herpes?
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1) acyclovir
2) cidofovir 3) foscarnet |
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What drugs are used for influenza?
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1) amantadine
2) zanamivir |
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Which drugs are used for HBV and HCV?
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1) INF-alpha
2)lamivudine 3) ribavirin |
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What is the MOA of acyclovir?
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it is a guanosine analog that is activated to form acyclovir triphosphate. It acts competitively at DNA polymerase and terminates DNA elongation
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Can acyclovir be used against both HSV1 and HSV2? What other virus can it be used for?
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1) yes
2) varicella zoster |
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Lack of what enzyme makes HSV resistant to nucleotide analogs? Which drugs will it be resistant to?
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Lack of thymidine kinase (TK-) make it resistant to acyclovir, famciclovir, ganciclovir and valacyclovir
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What is the function of thymidine kinase?
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viral enzyme that phosphorylates nucleotide analog drugs like acyclovir, penciclovir, ganciclovir, amciclovir, and valacyclovir
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When is acyclovir commonly given?
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herpes skin lesions, and prophylaxis in AIDS patients and other immunocompromised patients
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In general acyclovir is not given via IV. In what case would it?
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IV administration for severe herpes causing encephalitis and neonatal HSV infection
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What are the toxic effects of acyclovir when used IV?
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delirium, tremor, seizures, hypotension and nephrotoxicity
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What is the difference between penciclovir and acyclovir as far as MOA?
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penciclovir does not cause chain termination like acyclovir it only inhibits DNA polymerase
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What is famciclovir?
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a prodrug converted to pencicloivr in the liver
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What is the MOA of docosanol and what is it used for?
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it prevents fusion of HSV envelope with the plasma membrane. it is used topically
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What is MOA of ganciclovir? What viruses is it used for?
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1) a guanine derivative that is triphosphorylated to inhibit DNA poly and causes chain termination
2) CMV and HSV |
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How does resistance to ganciclovir occur in CMV?
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mutations in viral genes encoding phosphotransferases and DNA pol
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What are the toxicities of ganciclovir and what is it used for?
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1) used for CMV retinits and CMV infections in immunocompromised
2) leukopenia, thrombocytopenia, mucositis, hepatic dysfunction, seizures |
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What is cidofovir used for?
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it is effective against CMV retinitis, mucocutaneos HSV resistant to acyclovir and used in GENITAL WARTS
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What is the main toxicity of cidofovir? What drugs should you be weary of using in combination with?
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nephrotoxicity... want to be careful when using in conjunction with other nephrotoxic compounds like aminoglycosides and amphoticerin B
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What is the MOA of cidofovir?
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host kinases activate and they inhibit DNA poly
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What viruses can cidofovir be used against?
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CMV, HSV, adenovirus, HPV
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Acyclovir is the first choice for HSV. When would cidofovir be given? why
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in given when HSV resistance is present because it is not dependent on thymidine kinase only on host enzymes for its activation
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How does resistance to cidofovir occur?
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gene mutations in DNA poly
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What is valganciclovir?
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A prodrug of ganciclovir that can be given orally
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What is the MOA of foscarnet?
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it is a phosphonoformate derivative that does not require phosphorylation for activity. It inhibits viral RNA poly, DNA poly, and HIV reverse transcriptase
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How does resistance to foscarnet occur?
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mutations in polymerase genes
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Which of the following drugs does not require any modification to be effective?
1) ganciclovir 2) acyclovir 3) cidofovir 4) foscarnet |
foscarnet
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When is foscarnet given?
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For CMV infections including retinitis and has activity against ganciclovir-resistant CMV and for thymidine deficient HSV that are resistant to acyclovir
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What are side effects of foscarnet?
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nephrotoxicity, electrolyte imbalances, genitourinary ulceration, CNS effects
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Which of the following drugs does not require any modification to be effective?
1) ganciclovir 2) acyclovir 3) cidofovir 4) foscarnet |
foscarnet
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Why would you want to carefully monitor someone with CHF taking foscarnet?
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foscarnet causes hypocalcemia which may further weaken the hearts ability to pump
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What is vidarabine used against and what is it?
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it is a adenine analog used against HSV, VZV, and CMV
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When is foscarnet given?
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For CMV infections including retinitis and has activity against ganciclovir-resistant CMV and for thymidine deficient HSV that are resistant to acyclovir
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What are side effects of foscarnet?
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nephrotoxicity, electrolyte imbalances, genitourinary ulceration, CNS effects
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Why would you want to carefully monitor someone with CHF taking foscarnet?
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foscarnet causes hypocalcemia which may further weaken the hearts ability to pump
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What is vidarabine used against and what is it?
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it is a adenine analog used against HSV, VZV, and CMV
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Is vidarabine used systemically? What is it primarily used for?
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no it is too toxic. It is used for herpes keratitis but has little effect on genital lesions
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What are the adverse effects of vidarabine?
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GI irritation, parestheisas, tremor, convulsions and hepatic dysfunction
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What are idoxuridine and trifluridine used for?
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herpes keratitis (HSV-1)
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What is fomivirsen and what is it used to treat?
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it is an antisense oligonucleotide of CMV RNA. It binds and prevents early translation
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What is fomivirsen used?
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in is injected intravitreally for treatment of CMV retinitis
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What are side effects of fomivisen?
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iritis, vitreitis and increased intraocular pressure, vision changes
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Most NRTIs are prodrugs converted by host enzymes to what?
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triphosphates
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What is the MOA of NRTI's?
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inhibit reverse transcriptase and terminate growing DNA chains
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What gene is mutated allowing resistance to NRTIs?
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pol gene
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What is abacavir?
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a guanosine analog
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What else is 3TC known as?
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lamivudine
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What is the other name for zidovudine?
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AZT
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D4T is also known as?
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stavudine
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ddC is also known as?
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zalcitabine
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didanosine is also known as?
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ddI
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Which NRTI is associated with hypersensitivity in 5% of recipients and culminates in death?
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abacavir
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Which NRTIs are dose limited because of their adverse effects on the pancreas?
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1) ddI note that pancreatitis occurs more with alcohol than with hypertriglyceridemia
2) zalcitabine |
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What are the toxic effects of didanosine?
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PANCREATITIS, peripheral neuropathy, hepatic dysfunction, hyperuricemia and CNS effects
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Who is it contraindicated to give emtricitabine to?
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pregnant patients, children, people with hepatic and/or renal dysfunction
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What NRTI can cause hyperpigmentation of the palms and soles and asthenia?
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emtricitabine
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which NRTI is also effective against HBV?
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lamivudine (3TC)
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Which NRTIs are dose limited because of their ability to cause peripheral neuropathy?
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stavudine (d4T) and zalcitabine (ddC)
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Which NRTI has the highest rate of lactic acidosis and hepatic steatosis?
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stavudine (d4T)
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Which NRTI is a nucleotide?
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tenofovir
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Which NRTI has been reported to cause faconis syndrome and acute renal failure?
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tenofovir
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What is faconis syndrome?
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proximal convuluted tubule unable to reabsorb glucose, proteins, etc
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What are common side effects of zalcitabine?
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peripheral neuropathy, pancreatitis, esophageal ulceration, stomatitis, and arthralgias
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Which NRTI's primary toxic effect is bone marrow suppression?
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AZT (zidovudine)
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What what adverse effects occur in someone taking AZT?
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bone marrow suppression, anemia, neutropenia, thrombocytopenia, actue cholestatic hepatitis
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What are common effects amongst all the NRTIs?
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lactic acidosis, hepatomegaly with steatosis
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What is the MOA of NNTRIs? How are they different from NTRIs?
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bind to a site on RT different from the binding site of NRTIs and do not need to be phosphorylated. Note that the two types do not compete with one another
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What is a major problem of the NNRTI delavirdine?
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delavirdine is metabolized by both CYP3A4 and CYP2D6, therefore it affects the metabolism of several other drugs
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blood levels of which drugs are decreased by taking delviridine?
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antacids, phenytoin, ddI, rifampin and nelfinavir
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blood levels of delavirdine are increased by what drugs?
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azole antifungals and macrolides
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Which drugs are increased by taking delavirdine?
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benzo, nifedipine, protease inhibitors, quinidine and warfarin becuase it is metabolized by CYP3A4 and CYP2D6
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Can delavirdine or efavirenz be given during pregnancy?
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no they are teratogenic
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Which NNRTI can cause CNS dysfunction, skin rash and elevate plasma cholesterol as its side effects?
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efavirenz
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Which HIV drug is good at preventing vertical transmission? When is it administered?
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nevirapine is given at the onset of labor and to the neonate
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What are the side effects of nevirapine?
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hypersensitivity rash, steven-johnson syndrome and toxic epidermal necrolysis
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What enzyme do protease inhibitors work against?
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aspartate protease (HIV-1 protease)
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how does resistance to protease inhibitors come about?
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mutations in the pol gene which contains the aspartate protease
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what hepatic enzymes are inhibited by protease inhibitors?
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CYP3A4
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What type of drug is amprenavir?
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PI
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How can all PIs be identified based on their name?
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they all have navir in their name
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What type of drug is fosamprenavir?
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PI
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Which PI causes hyperbilirubinemia, long QT, skin rash, peripheral neuropathy, and inhibits both CYP3A4 and CYP2C9?
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atazanavir: note that it is not associated with metabolic syndrome like most PIs
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What drugs will have increased serum levels when taken with indinavir?
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histamines, benzos, and rifampin
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What are some of the side effects of indinavir?
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thrombocytopenia, hyperbilirubinemia, nephrolithiasis
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Why is it important to take indinavir with plenty of water?
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to prevent kidney damage
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Which PI causes more insulin resistance?
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indinavir
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Why is lopinavir given with ritonavir?
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ritonavir is an enhancer for lopinavir because it inhibits CYP3A4 metabolism of lopinavir
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Which PI has the best safety profile during pregnancy?
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nelfinavir
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What are the adverse effects of saquinavir?
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nausea, diarrhea, DYSPEPSIA, RHINIITIS
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What effects do PIs have on sugars and lipids in the body?
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they cause hyperglycemia and insulin resistance and altered fat distribution
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An HIV infected woman taking HAART has a buffalo hump, gynecomastia and truncal obesity. Which drug in the HAART regimen is responsible for this?
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PIs
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What drug binds gp41?
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enfuvirtide
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what is the fusion inhibitor drug?
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enfuvirtide
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Which strain of influenza are amantadine and rimantadine effective against? What is their MOA?
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1) influenza A not B
2) inhibit early step in viral replication by binding to M2 protein |
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What is the function of the M2 protein?
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influenza uses this protein to acidify the viral core to activate RNA transcriptase
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A person is given amantadine at 72 hours post infection. How effective will this be?
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not very... needs to be given in first 48 hours
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Which strain of influenza causes seasonal flu in the US? What is it resistant to?
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H3N2 is resistant to amantadine
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Which anti viral agent can cause dizziness, ataxia, and slurred speech?
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amantadine and rimantadine
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What drugs are effective against both strains of influenza? What is their MOA?
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1) oseltamivir and zanamivir
2) they inhibit neuraminidases |
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What is the function of neuraminidase?
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to cleave sialic acid from host and virus particles and to promote viral release and prevent clumping of virions
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What is the MOA of IFN-alpha?
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it is a cytokine that acts at host receptors increasing JAKS which activate STAT which increase production of antiviral proteins.
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What is the main antiviral protein that is activated by IFN-alpha?
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a ribonuclease that preferentially degrades viral mRNA
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What cell does INF-alpha activate?
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NK cells bitches which destroy infected hepatocytes
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When is INF-alpha used?
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1) for chronic HBV and in conjunction with ribavirin for chronic HCV
2) kaposi sarcoma, papillomatosis, and topically for genital warts 3) prevent dissemination of herpes zoster and CMV after transplantation |
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What drug is given to prevent CMV shedding after transplantation?
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IFN-alpha
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What are the side effects of IFN-alpha?
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flu-like symptoms, neutropenia, profound fatigue, myalgia, REVERSIBLE HEARING LOSS, THYROID DYSFUNCTION, severe depression
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What is the MOA of adefovir?
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following phosphorylation it competively inhibits HBV DNA polymerase and causes chain termination by incorporating into viral DNA
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What are the adverse affects of adefovir dipivoxil?
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nephrotoxicity is dose limiting, lactic acidosis, hepatomegaly with steatosis
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What is the MOA of entecavir?
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it is a guanosine nucleoside that inhibits HBV DNA polymerase
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Ribavirin is active against what?
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DNA and RNA viruses including influenza A, B, parainfluenza, RSV, paramyxoviruses, HCV, and HIV
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How does ribavirin inhibit viruses?
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1) inhibits GTP formation
2) prevents viral mRNA capping 3) block RNA dependent RNA polymerase |
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Which anti viral drug causes does dependent hemolytic anemia?
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ribavirin
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is ribavirin teratorgenic?
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yes
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