HIV fusion inhibitor - binds to gp41 and prevents gp41 from refolding & bringing HIV and Tcell close enough to fuse - subcu 2x/day, $20,000/yr (enFUvirtide blocks FUsion)

HIV fusion inhibitor - blocks HIV entry by binding human CCR5 coreceptor - metabolized by p450s - Resistance due to mutant strains that use CXCR4 to gain entry

HIV NRTI (nucleoside RT inhibitor) - long 1/2 life, can be taken as pill 1x/day, no big drug metabolism interactions - fluorinated lamivudine analog (emTRICitabine TRICks RT into terminating the nucleotide chain)

HIV NNRTI - 2x/day pull - reserved for pts with resistance/failing other therapies (eTRAVirine prevents the active domains of RT from TRAVeling).

HIV integrase inhibitor - no p450 interaction - 2x/daily pill - used to be reserved now first-line therapy (ralTEGravir - anti-inTEGrase)

HIV integrase inhibitor - Part of 4-drug combo Stribild (elviTEGravir/CObicstat/emTRICitabine/Tenofovir) - CObicstat acts to boost concentration of elviTEGravir (ElviTEGravir - anti-inTEGrase, CObicstat COoperates)

HIV integrase inhibitor - does not require boosting - 1x/day pill not formulated yet - active in pts resistent to earlier integrate inhibitors (DoluTEGravir inTEGrase inhibitor)

HIV protease inhibitor - works against isolates resistant to other PI's - better tolerated than tipranavir - CYP3A inhibitor (DARunavir = Tasmanian DARedevil --> protease inhibitor)

HIV protease inhibitor - non-peptide structure is unique - increased efficacy in the face of other mutations - CYP3A iinhibitor (tiPranavir Protease inhibitor)

Herpes, CMV nucleoside analog - prodrug, chain terminator - requires viral thymidine kinase for first phosphotase, making it less toxic to humans - oral, topical and IV, generally well tolerated orally - Resistance due to HSV-TK mutations and viral DNA polymerase

Herpes, CMV - blocks viral DNA and RNA pol, directly blocks HIV RT - binds enzyme pocket, holds tri-P, prevents cleavage - specific for viral pol's - activity remains against ganciclovir and cidofovir resistant strains

Viral Drugs Flashcards by Lauren Battaglia

Enfuvirtide

HIV fusion inhibitor

binds to gp41 and prevents gp41 from refolding & bringing HIV and Tcell close enough to fuse
subcu 2x/day, $20,000/yr

(enFUvirtide blocks FUsion)

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Maraviroc

HIV fusion inhibitor

blocks HIV entry by binding human CCR5 coreceptor
metabolized by p450s
Resistance due to mutant strains that use CXCR4 to gain entry

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Emtricitabine

HIV NRTI (nucleoside RT inhibitor)

long 1/2 life, can be taken as pill 1x/day, no big drug metabolism interactions
fluorinated lamivudine analog

(emTRICitabine TRICks RT into terminating the nucleotide chain)

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Tenofovir

HIV NRTI (nuceloside RT inhibitor)
- Syntehtic adenosine analog with a phosphate and protective groups (overcome rate-limiting P step)
- Little interaction with p450s
- Single dose per day or combo pill with emtricitabine (Truvada)
- used against HIV also
(Tenofovir is a nucleoTide RT inhibitor)

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Truvada

HIV Fixed-dose NRTI combination drug, can be used as prophylaxis in sex workers and spouses of HIV+ pts

emTRICitabine and Tenofovir

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Stribilid

HIV combination drug

ElviTEGravir (integrase inhibitor)/cobicistat (booster)/emTRICitabine/Tenofovir

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Etravirine

HIV NNRTI

2x/day pull
reserved for pts with resistance/failing other therapies

(eTRAVirine prevents the active domains of RT from TRAVeling).

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Raltegravir

HIV integrase inhibitor

no p450 interaction
2x/daily pill
used to be reserved now first-line therapy

(ralTEGravir - anti-inTEGrase)

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Elvitegravir

HIV integrase inhibitor

Part of 4-drug combo Stribild (elviTEGravir/CObicstat/emTRICitabine/Tenofovir)
CObicstat acts to boost concentration of elviTEGravir

(ElviTEGravir - anti-inTEGrase, CObicstat COoperates)

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Dolutegravir

HIV integrase inhibitor

does not require boosting
1x/day pill not formulated yet
active in pts resistent to earlier integrate inhibitors

(DoluTEGravir inTEGrase inhibitor)

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Atazanavir

HIV protease inhibitor
- processed by CYP3A4, toxic side effects reduce compliance, but 1x/day dose is better than predecessor drugs
(aTAZanavir –> think Taz likes to cleave everything in his path like a protease)

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Darunavir

HIV protease inhibitor

works against isolates resistant to other PI’s
better tolerated than tipranavir
CYP3A inhibitor

(DARunavir = Tasmanian DARedevil –> protease inhibitor)

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Tipranavir

HIV protease inhibitor

non-peptide structure is unique
increased efficacy in the face of other mutations
CYP3A iinhibitor

(tiPranavir Protease inhibitor)

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Ritonavir

HIV protease inhibitor that also inhibits p450s so it is used as a booster in combination drugs with aTAZanavir and DARunavir protease inhibitors.

(RITonavir gets RIT of p450s)

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Entecavir

currently recommended drug for Hep B, used with Tenofovir

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Peg-interferon

HepB drug that is no longer prevalent due to adverse side effects; sometimes used in pregnancy because known to be safe for fetus

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Rituximab

Preemptively put them on Hep B anti-viral therapy if they are on Rituximab or any other immune-compromising therapy. They would be on Rituximab if they needed to have their immune system suppressed (i.e. for transplant etc)

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Acyclovir

Herpes, CMV nucleoside analog

prodrug, chain terminator
requires viral thymidine kinase for first phosphotase, making it less toxic to humans
oral, topical and IV, generally well tolerated orally
Resistance due to HSV-TK mutations and viral DNA polymerase

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Cidofovir

Herpes, CMV nucleoside analog
- chain terminator, prodrug
- taken up by infected and non-infected cells
- first phosphate already present on the drug, 2 more added by host enzymes
- resistence due to viral DNA pol mutations
- long half-life (advantage)
- dose-dependant nephrotoxicity (disadvantage)
-

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Foscarnet

Herpes, CMV

blocks viral DNA and RNA pol, directly blocks HIV RT
binds enzyme pocket, holds tri-P, prevents cleavage
specific for viral pol’s
activity remains against ganciclovir and cidofovir resistant strains

Amantadine

Influenza viral entry inhibitor

bind the M2 viral channel protein, blocking the unseating process
resistance when M2 gets mutated

Rimantidine

Influenza viral entry inhibitor

bind the M2 viral channel protein, blocking the unseating process
resistance when M2 gets mutated

Zanamivir

Influenza viral exit inhibitor

viral neuramidase inhibitor prevents sialic residue cleavage, reduces viral escape from infected cells, preventing spread of virus to other cells
inhaler

Oseltamivir

Influenza viral exit inhibitor

viral neuramidase inhibitor prevents sialic residue cleavage, reduces viral escape from infected cells, preventing spread of virus to other cells
H1N1 likely resistant
orally

Interferons

HBV&HCV - human proteins with antiviral immunmodulating and anti proliferative actions by activating JAK/STAT pathway - horrible adverse effects (hepatotoxicity, neurotoxicity, autoimmune disorders, psych disorders, nephrotoxicity) - PEG increases its half-life from 2-->54 hours - reduces p450 metabolism of other drugs - never used alone, use with Ribavirin

Telbivudine

HBV nuceloside analog

Tenofovir ^^

HBV nucleoside analog

Entecavir

HBV nucleoside analog

Adefovir

HBV nucleoside analog

Ribavirin

HCV nucleoside analog (looks like guanine) - used with IFN - tetratogenic in animals, keep away from pregnant women - aerosolized may cause conjunctivitis, wheezing, rash

Sofosbuvir

HCV nucleoside analog - latest and greatest! - genotypes 1&4: use with PEG-IFN/RBV - genotypes 2&3: use with RBV - first all-oral therapy - SVR 90% - SVR 100% achieved with drugs still in development - 1st Phosphate included - no drug-drug interactions - resistance develops slowly

Simiprevir

HCV protease inhibitor - recent drug - 80% SVR in all pts (naive or experienced w treatment) - once/day orally, lower side effects

Famciclovir

HSV nucleoside analog (chain terminator) | - not good, mutagenic in animal models and should be avoided during pregnancy

Ganciclovir

HSV nucleoside analog (chain terminator) - many adverse affects (teratogenic, carcinogenic, mutagenic) - HIV/immunocompromised pts need these drugs

Trifluridine

Topical HSV drug, too toxic for anything other than ophthalmic use

Vidarabine

Topical HSV drug, too toxic for anything other than ophthalmic use

Teleprevir

HCV Protease Inhibitor - used with PEG-IFN/RBV - inhibit HCV NS3 serine protease - Taken with food multiple x/day - resistance develops quickly - don't use alone!

Boceprevir

HCV Protease Inhibitor - used with PEG-IFN/RBV - Taken with food multiple x/day - resistance develops quickly - don't use alone!

Daclatasvir

HCV NS5A inhibitor - protein has no enzymatic function but inhibition blocks viral RNA replication and packaging - binding pocket conserved: broad coverage

Ledipasvir

HCV NS5A inhibitor - protein has no enzymatic function but inhibition blocks viral RNA replication and packaging - binding pocket conserved: broad coverage

Entecavir

HBV nucleoside analog - prodrug - unique chain termination: entecavir gets incorporated, a few more bases are added before nucleic acid is so distorted the chain cannot finish - treat for life. expensive, ultimately resistance (2 mutations)

Adefovir

- prodrug, 1st phosphate included - effective after lamivudine resistance and entecavir cross resistance - reserved for when drug resistance occurs toward other drugs

Telbivudine

HBV nucleoside analog | - lamivudine resistant strains are cross-resistant to telbivudine

5-fluorocytosine

5FC, anti fungal drug structural analog of cytosine that fungi convert to an analog of dTMP. Inhibits thymine synthesis and blocks fungal DNA synthesis. Combo with amphotericin due to 5FC resistance

Polyenes

Anti fungal - bind ergosterol in membrane, increase permeability, cause loss of small molecules from cell

Amphotericin

anti fungal used for systemic or deep-seated infections, target ergosterol

Nystatin

topical anti-fungal targets ergosterol

Echinocandins

anti fungal | block cell-wall polysaccharide synthesis

Pentamidine

Anti fungal, inhibits self splicing in pneumocystis carnii | selective for fungal because self splicing does not occur in humans