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Valacyclovir
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Acyclovir
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anti viral
Antiviral pharm
| Drug | action/type | bioavailability/absorption | CSF penetration | elimination | side effects/contraindications | protein binding |
|---|---|---|---|---|---|---|
| Valacyclovir | prodrug converted rapidly and completely to acyclovir | increases oral bioavailibity to 50% over acyclovir | (blank) | (blank) | well tolerated, nausea, diarrhea, and headache | (blank) |
| Acyclovir | a purine analog that needs to be converted to nucleoside tiphosphate for activity, active against HSV1&2, EBV, VZV, CMV; resistance due to absence or depression of viral thymidine kinase | orally (10-30%) or IV administration | has good CSF penetration | eliminated unmetabolized by kidney | nausea, vomiting headache, crystalline nephropathy or neurotoxicity | (blank) |
| Famciclovir | prodrug that is converted to penciclovir --> similar activity to acyclovir, used for HSV1&2, VZV, EBV, HBV | well absorbed | (blank) | (blank) | (blank) | (blank) |
| Trifluridine | inhibits DNA synthesis; active against HSV1&2, vacinia, and some adenoviruses | 1% solution effective for primary kerato conjuctivitis and recurrent epithelial keratitis due to HSV1&2 | (blank) | (blank) | (blank) | (blank) |
| Ganciclovir | inhibits replication of CMV; used to treat CMV retinitis, colitis, oresophagitis | administerd IV, orally, or intraocular | penetrates CSF | eliminated unchanged by kidney | dose limiting toxicities--> reversible neutropenia and thrombocytopenia; others--> CNS toxicity, fever, rash, sbnormal liver function and retinal detachment | (blank) |
| Valganciclovir | rapidly metabolized in intestinal wall and liver to ganciclovir, indicated for the treatment of CMV retinitis | well absorbed | (blank) | renal | (blank) | (blank) |
| cidofovir | cytosine nucleotide analog with invitro activity against CMV,HSV1&2, VZV, EBV, HHV6&8, adenovirus,poxvirus,polyomaviruses, and HPV; inhibits viral DNA | half life 17-65 hrs | poor | via kidney--> must be administered with probenecid which blocks tubular secretion and decreases nephrotoxicity | Nephrotoxicity, decreased intraocular pressure, and hypersensitivity to probenecid | (blank) |
| Amantadine and Rimantadine | inhibit uncoating of single stranded RNA viruses, used for influenza A | absorbed from the GI tract | (blank) | amantadine-->kidney, rimantadine--> liver | causes mild CNS effects and GI intolerance | (blank) |
| ribivirin | inhibits uncapping of viral messenger RNA, monotherapy not effective | bioavailability 64% and increased by high fat meals and decreased by antacids | (blank) | eliminated in urine | hemolytic anemia may be dose limiting, depression, fatigue, irritablility, rash, sough, insommnia, nausea, pruritis; ABSOLUTE CONTRAINIDICATIONS--> Anemia, end stage renal failure, sever heart desiese and pregnancy | (blank) |
| Zidovudine | (blank) | orally absorbed | some CNS penetration | metabolized in liver and cleared by renal tubular secretion | headache, diarrhea,fever: Dose Limiting--> granulocytopenia and anemia | (blank) |
| Didanosine | (blank) | oral absorption 40%, decreased by 50% with food | excreted unchanged by renal filtration | Dose Limiting Toxicities--> pancreatitis and sensory peripheral neuropathy others--> diarrhea, hepatitis, esophageal ulceration, cardiomyopathy, gouty attacks | Low | |
| stavudine | competitive inhibitor of reverse transcritase and a terminator of DNA chain elongation | high oral bioavailability that is not food dependant | 55% of plasma concentration | kidney | DOSE LIMITING--> peripheral neuropathy | (blank) |
| Lamivudine | (blank) | oral bioavailability >80% and not food dependent | (blank) | eliminated unchanged in urine | headache, insomnia, fatigue, GI discomfort | (blank) |
| Zalcitabine | (blank) | intracellular half life plasma levels decrease 25-40% with food, bioavailability . 80% | 20% fo plasma | (blank) | (blank) | (blank) |
| Abacavir | (blank) | well absorbed orally, unaffected by food | 1/3 of plasma concentration | metabolized in liver excreted in urine | hypersensitivity reactions | (blank) |
| Tenofovir | competitivly inhibits HIV reverse transcriptase | oral bioavailability increased by high fat meal | (blank) | eleminated by kidney | GI complaints | (blank) |
| Nevirapine | (blank) | oral bioavilability good, not food dependant | 45% of plasma concentration | (blank) | severe life threatening skin rashes, including stevens Johnson syndrome and toxic epidermal necrolysis: use gradual dose escalation over two weeks; fulminant hepatitis may appear, LFT's recomended; other adverse effects fever, nausea, headache, somnolence | (blank) |
| Delavirdine | (blank) | oral bioavialability 85%, is reduced by antacids | CSF levels low | (blank) | skin rash, headache, fatigue, nausea, diarrhea, increased liver enzymes: pregnancy should be avioded | extensively protein bound |
| Efavirenz | (blank) | well absorbed, increased by high fat | CSF levels low | metabolized by liver, eliminated in feces | CNS and skin rash ( both of which may resolve on their own, nausea, vomiting, diarrhea, crystalluria, elevated aminotransferace and an increase in choesterol | Highly bound to albumin >99% |
| Saquinavir | best tolerated protease inhibitor but least effective because of bioavailability | must be taken with high fat meals for adequate absorbtion | (blank) | (blank) | GI disturbances | (blank) |
| Ritonavir | (blank) | taken with meals | (blank) | excreted by feces | GI disturbances, parathesias, elevated LFT's, altered taste, hypertriglyceridemia; nausea, vomiting and abdominal pain typically occur during the first week, escalate dose over 4-5 days | (blank) |
| Amprenavir | (blank) | rapidly absorbed from GI tract, not food dependant, high fat meals decrease absorption | (blank) | (blank) | nausea, diarrhea, vomiting, perioral perethesias, depression, and rash; contraindicated in young children and pregnant | (blank) |
| Indinavir | (blank) | must be taken on an empty stomach, bioavailability 65% | highest CSF penetration of protease inhibitors | exretion is fecal | indirect hyperbilrubinemia, nephrolithiasis (consume 48 oz of H2O) thrombocytopenia, increased aminotransferases, nausea, diarrhea, irritability- rarely hemolytic anemia | (blank) |
| Nelfinavir | (blank) | higher absorption in fed state | (blank) | metabolized by CYP3A, excreted in feces | diarrhea and flatulence | (blank) |
| Enfuvirtide | blocks entry into cell, lacks cross resistance | SQ administration | (blank) | metabolized by proteolytic hdrolysis | hypersensivity | (blank) |
| Lamivudine | lower dose and less frequent dosing, used for Hepatitis | (blank) | (blank) | (blank) | safe for decompensated liver disease, progression to liver fibrosis less frequent, excellent safety profile | (blank) |
| Adefovir | nucleotide analog, inhibits HBV DNA polymerase | 59% not food dependant | (blank) | excreted by kidney | dose dependant nephrotoxicity, lactic acidosis and severe hepatomegally with steatosis | (blank) |
| interferon alpha | used for HBV and HCV, suppresses cell proliferation and viral replication | SQ or IM | (blank) | excretion is by kidney with minor biliary excretion | flu like symptoms, increased aminotransferase, induction of autoantibodies, nausea, fatigue, headache, arthralgias; CONTRAINDICATED--> for depression, nuetropenia, decompensated cirrhosis, siezures, organ transplant, or pregnancy | (blank) |
| Pegylated interferon alpha | reduced clearance and sustained absorption results in stedier drug concentration and less frequent doses | use in combination with ribavirin is more effective than monotherapy | (blank) | renal clearance | (blank) | (blank) |
| DOC for influenza A | amantidine | (blank) | (blank) | (blank) | (blank) | (blank) |
| DOC for RSV | Ribavirin | (blank) | (blank) | (blank) | (blank) | (blank) |
| DOC for CMV retinitis | Ganciclovir | (blank) | (blank) | (blank) | (blank) | (blank) |
| SE for ganciclovir | Neutro, leuko and thrombocytopenia | (blank) | (blank) | (blank) | (blank) | (blank) |
| Anti-viral agents associated with Stephen Johnson syndrome | Nevirapine, amprenavir | (blank) | (blank) | (blank) | (blank) | (blank) |
| HIV antiviral class known to have severe drug interactions by causing inhibition of metabolism | Protease inhibitors | (blank) | (blank) | (blank) | (blank) | (blank) |
| Antivirals that are teratogens | Delavirdine, efavirenz, and ribavirin | (blank) | (blank) | (blank) | (blank) | (blank) |
| Antivirals associated with neutropenia | Ganciclovir, zidovudine, saquinavir, and interferon | (blank) | (blank) | (blank) | (blank) | (blank) |
| HIV med used to reduce transmission during birth | AZT | (blank) | (blank) | (blank) | (blank) | (blank) |
| Anti-viral with a dose limiting toxicity of pancreatitis | Didanosine | (blank) | (blank) | (blank) | (blank) | (blank) |
Created by:
swohlers
Popular Pharmacology sets