Term
Identify what the following drugs blocks in the cell replication cycle
Acyclovir
Interon
Maraviroc
Amantadine
Fomivirsen
adefovir
Oseltamivir
Zanamivir
enfuvirtide
docosanol
rimantadine
cidofovir
ganciclovir
foscarnet |
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Definition
Acyclovir-RNA/DNA genome replication
Interferon-transcription
Maraviroc-binding/fusion
Amantadine-uncoating
Fomivirsen-translation
adefovir-RNA/DNA genome replication
Oseltamivir-budding
Zanamivir-budding
enfuvirtide-bind/fusion
docosanol-bind/fusion
rimantadine-uncoating
cidofovir-RNA/DNA genome replication
ganciclovir-RNA/DNA genome replication
foscarnet-RNA/DNA genome replication |
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Term
(Enfuvirtide or Marviroc) binds to CCR5 (CCR5 inhibitor-binding)
(Enfuvirtide or Marviroc) binds to gp41 (fusion inhibitor)
What type of virus are these drugs specific for |
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Definition
Maraviroc – binds to CCR5 (CCR5 inhibitor)
Enfuvirtide – binds to gp41 (fusion inhibitor)
(specific for HIV) |
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Term
| What drug is a long-chain saturated alcohol that blocks fusion between the cellular and viral envelope membranes, inhibiting viral entry into cell and be applied topically to treat recurrent orolabial herpes (cold sores)? |
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Definition
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Term
*Amantadine and Rimantadine works on what types of viruses?
What does it inhibit? |
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Definition
Influenza A ONLY!
Inhibit uncoating of the virus (thus replication) by interfering with the influenza A virus M2 protein, which serves as an ion channel
Influenza B M2 protein is too different |
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Term
| What is the only step in the virus life cycle that we do not have an antiviral drug to? |
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Definition
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Term
Which drug has a longer half-life and does not require dosage adjustment in renal failure; less side effects? (Amantadine or Rimantadine)
Are these drugs cross-resistant to each other (if resistant to one, will be resistant to the other) |
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Definition
Rimantadine
Yes-100% cross-resistant to each other |
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Term
| What is the family of cytokines that evoke antiviral, antiproliferative, and immunomodulating effects by inhibiting transcription? |
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Definition
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Term
What are 3 major classes of interferons prepared by recombinant technology and which one is responsible for antiviral effects?
Does it effect DNA, RNA, or both viruses? |
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Definition
rIFN-alpha: 2a and 2b -->antiviral effects
rIFN-beta
rIFN-gamma
both DNA and RNA |
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Term
| What is the chemical attachment to interferons that enhances plasma half-life, reduces renal clearance, allows for once a week administration |
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Definition
| Pegylated interferon (polyethylene glycol [PEG]) |
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Term
| What is the family of cytokines that evoke antiviral, antiproliferative, and immunomodulating effects by inhibiting transcription? |
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Definition
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Term
What are 3 major classes of interferons prepared by recombinant technology and which one is responsible for antiviral effects?
Does it effect DNA, RNA, or both viruses? |
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Definition
rIFN-alpha: 2a and 2b -->antiviral effects
rIFN-beta
rIFN-gamma
both DNA and RNA |
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Term
| What is the chemical attachment to interferons that enhances plasma half-life, reduces renal clearance, allows for once a week administration |
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Definition
| Pegylated interferon (polyethylene glycol [PEG]) |
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Term
| In order to treat CHRONIC Hep B, CHRONIC Hep C, and HPV genital warts, what would you give them? |
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Definition
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Term
| In a patient with high relapse rates of chronic hep C and given interferon, how you adjust their treatment? In a non responder, how would you adjust their treatment? |
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Definition
| High relapse rates – prolonged treatment (12 – 18 months) and possibly higher doses increase likelihood of sustained responses Non-responders benefit from combination treatment with ribavirin and pegIFN alpha-2a and 2b |
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Term
| Are the major side effects with interferon therapy? |
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Definition
Flu-like syndrome
Depression |
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Term
| What is the drug whose nucleotide sequence is similar to a sequence in mRNA that encodes proteins needed for production of infectious cytomegalovirus and inhibits cytomegalovirus replication by blocking translation through an antisense mechanism |
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Definition
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Term
| What drug is used for cytomegalovirus retinitis in patients with AIDS resistant to cidofovir, ganciclovir or foscarnet. Adverse events include mostly ocular; blurred vision, inflammation, photophobia |
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Definition
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Term
| *What drug is a nucleoside analog of GUANOSINE that is phosphorylated intracellularly to the ACTIVE triphosphate form (doesn't do anything unless a virus is present) to inhibit chain elongation/genome replication |
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Definition
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Term
| What drug is used to treat Herpes simplex virus infections (HSV-1 and 2) and acute treatment of herpes zoster (shingles) and varicella (chickenpox) and poorly absorbed orally |
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Definition
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Term
| What drug is the L-valine ester of acyclovir (prodrug of acyclovir); Not active, it must be hydrolyzed in the intestine and/or liver to acyclovir and ultimately intracellular acyclovir triphosphate (significantly enhanced absorption/better orally/reduced dosing compared to acyclovir) |
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Definition
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Term
| What drug is a PHOSPHATE nucleotide analog of adenosine,phosphorylated by cellular enzymes which inhibits viral polymerases, leads to chain termination/inhibits genome replication in order to treat chronic hepatitis B infection? |
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Definition
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Term
| What is the prodrug of adefovir? |
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Definition
| Pro-drug: adefovir dipivoxil (Hepsera) converted by esterases |
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Term
| *What drug is a PYROPHOSPHATE analog (no phosphorylation needed) that directly inhibits viral DNA polymerase by preventing cleavage of the pyrophosphate from nucleoside triphosphates and blocking viral DNA synthesis, given by IV infusion, and treats cytomegalovirus and herpes zoster |
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Definition
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Term
| You can combine Foscarnet with _____ for cytomegalovir in patients that relapse on either drug alone |
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Definition
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Term
| * what drug is phosphorylated by cellular enzyme to a triphosphate and inhibits HBV DNA polymerase, leads to chain termination/inhibit genome replication for Chronic hepatitis B and HIV, renally excreted; low cytotoxicity except patients with HIV co-infection at risk of pancreatitis |
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Definition
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Term
| What is the problem with lamivudine? |
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Definition
| Hep B resistance (why combination therapy is preferred) |
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Term
| What drug is a Guanosine analog, phosphorylated by cellular kinases to triphosphate form, has activity against RNA and DNA viruses, and inhibits *3 different enzymes (inosine monophosphate dehydrogenase, Viral RNA polymerase, Viral mRNA guanylyltransferase (stops 5’-capping of mRNA)) |
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Definition
| Ribavirin (RTP-active triphosphate form) |
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Term
| What drug is used for Influenza virus, respiratory syncytial virus (RSV) in children, Chronic hepatitis C infection (with interferon alpha-2b) but cause dose-dependent hemolytic anemia? |
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Definition
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Term
What is the prodrug to Ganciclovir?
Penciclovir? |
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Definition
Valganciclovir
Famciclovir |
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Term
*Oseltamivir and Zanamivir work on what types of viruses?
What does it inhibit? |
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Definition
Influenza A and B!! (Amantadine and Rimantadine- influenza A only)
Inhibits neuraminidase (enzyme that cleaves sialic acid inside of cell to allow budding) |
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Term
| What drug is an ethyl ester prodrug, cleave by intestinal or hepatic esterases to the active form that inhibits neuraminidase on influenza A and B, good bioavailability, and prodrug and active for renally eliminated (less sick for a shorter duration of time) |
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Definition
| oseltamivir (oseltamivir carboxylate-active form) |
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Term
| If a virus is resistant to amantadine, rimantadine, and zanamivir, what drug would you give them? |
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Definition
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Term
| What is the sialic acid analog that inhibits neuraminidase from influenza A and B but has poor oral bioavailability (given as dry powder inhalation) and treats acute influenza? |
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Definition
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Term
| Should Zanamivir be given to patients with asthma? |
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Definition
| No-Not recommended in patients with underlying airways disease (such as asthma or chronic obstructive pulmonary disease) because can cause wheezing and broncospasm |
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Term
| What are the goals of chronic hep B therapy? |
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Definition
Suppression of viral replication (Elimination of circulating HBV DNA)
Normalization of serum aminotransferase activity
Decrease in inflammation on liver biopsy
Reduction in long-term sequelae of HBV-associated liver disease (cirrhosis, hepatocellular carcinoma) |
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Term
| What drug is a guanosine analog, phosphorylated to active triphosphate form, which inhibits HBV reverse transcriptase and can cross resistance with lamivudine. Treat chronic Hep B |
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Definition
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Term
| What drug is a thymidine analog, phosphorylated by cellular kinases to active triphosphate form, which inhibits HBV reverse transcriptase/DNA polymerase leading to DNA chain termination and is more effective than lamivudine and adefovir for chronic hep B |
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Definition
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Term
What drug is a nucleotide reverse transcriptase inhibitor used for HIV treatment and is also approved for treatment of chronic HBV infection.
What is it's prodrug? |
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Definition
Tenofovir
prodrug: tenofovir disoproxil fumarate |
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Term
| If a HBV patient is resistance against lamivudine and entecavir, what drug should you give them? |
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Definition
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Term
| What are the primary and secondary goals of hepatitis C therapy? |
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Definition
Primary objective = sustained viral response
-No virus
-Arrest progression
-No symptoms
Secondary objective = delay/prevent
-Reduce progression of fibrosis and cirrhosis
-Prevent liver decompensation and heptocellular carcinoma |
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Term
| What is the treatment for hepatitis C? |
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Definition
| Peg interferon + Ribavirin |
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Term
| What are the main categories for HIV drugs? |
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Definition
Fusion inhibitors
Entry inhibitors
Reverse transcriptase inhibitors
-Nucleoside or nucleotide (NRTI)
-Non-nucleoside (NNRTI)
Integrase inhibitors
Protease inhibitors |
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Term
| *Maraviroc, an HIV entry inhibitor, inhibits (CCR5, CXCR4, or both)? |
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Definition
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Term
| Enfuvirtide, an HIV fusion inhibitor, is administered how? |
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Definition
| subcutaneous injection twice a day = not used much |
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Term
| *What HIV protease inhibitor is potent CYP450 inhibitor (causes a lot of PK and drug-drug interaction, can enhance other drugs) |
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Definition
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