Exam 2: Antiretroviral Agents, Kumar - Matching

Terms in this set (93)

Fusion Inhibitor

a synthetic 36-amino acid peptide derived from HIV-1 gp41 transmembrane protein

binds to the gp41 subunit of envelope protein; prevents the conformational changes required for the fusion of the viral and cellular membranes

administered by subQ injection -- only drug that must be given parenterally

High cost - reserved for patients who failed other regimens

No resistance has developed against this.

Viral tropism test is necessary before tx.

Restricted for only CCR5/M-tropic virus.

Didanosine (ddI)

Lamivudine (3TC)

Emtricitabine (FTC)

Stavudine (d4T)

Tenofovir (TDF)

Zalcitabine (ddC)

Zifovudine (AZT)

Delavirdine (DLV)

Efavirenz (EFV)

Etravirine (ETV)

Nevirapine (NVP)

Rilpivirine (RPV)

Which NRTI is the least preferred do to high toxicity and short half-life/frequent dosing?

Zalcitabine (ddC)

Preg Cat D NRTI

Didanosine (ddI)

Preg Cat D NRTI

Zalcitabine (ddC)

Preg Cat D NRTI

Stavudine (d4T)

Need HLA-B*5701 screening before tx due to fatal hypersensitivity syndrome.

Didanosine (ddI)

Lamivudine (3TC)

Fluorinated analog of Lamivudine (3TC)

Emtricitabine (FTC)

Emtricitabine (FTC)

Stavudine (d4T)

Contraindicated w/Zidovudine (AZT) and Didanosine (ddI)

Stavudine (d4T)

Tenofovir (TDF)

Should be taken after a high fat meal to increase bioavailability

Tenofovir (TDF)

Decreases bone density

Tenofovir (TDF)

Should be taken with antacids.

Zalcitabine (ddC)

Can cause oral ulcerations

Zalcitabine (ddC)

1st agent approved for HIV tx in 1987

Zidovudine (AZT)

Initially considered a highly toxic drug used to poison HIV patients (govt conspiracy)

Zidovudine (AZT)

Approved for prevention of prenatal infection during pregnancy

Zidovudine (AZT)

Zidovudine (AZT)

Can cause myelosuppression, anemia, neutropenia - very toxic.

Zidovudine (AZT)

Approved for prevention of mother to child infection during pregnancy

Nevirapine (NVP)

Closely monitor patients on methadone for opioid withdrawal

Nevirapine (NVP)

Immediately discontinue if severe rashes occur

Nevirapine (NVP)

Never prescribe to patients with high CD4 counts (women > 250; men > 400)

Nevirapine (NVP)

Never patients with a history of alcohol abuse, co-infection with hep B or C, and in patients who are older or women

Nevirapine (NVP)

Never recommended to pregnant women

Efavirenz (EFV)

Can cause CNS toxicity in 50% of pts

Efavirenz (EFV)

Immediately discontinue if severe rashes occur

Efavirenz (EFV)

Never prescribe to patients with psychiatric illnesses

Efavirenz (EFV)

Never patients with a history of alcohol abuse, co-infection with hep B or C, and in patients who are older or women

Efavirenz (EFV)

Never recommended to pregnant women

Delavirdine (DLV)

NNRTI with least occurrence of Steven-Johnsons Syndrome.

Delavirdine (DLV)

Drug of choice for treatment experienced patients

Etravirine (ETR)

Drug of choice for ARV-naive patients (1st tx)

Rilpivirine (RPV)

Can cause prolonged QTc

Rilpivirine (RPV)

Immediately discontinue and never re-administer if hypersensitivity occurs

Dolutegravir (DTG)

Approved in 2013; given daily for treatment naive patients, given BID for treatment experienced patients

Dolutegravir (DTG)

Metabolized by UGT1A1 and CYP3A4

Dolutegravir (DTG)

Can cause nephrotoxicity

Elvitegravir (EVG)

Metabolized by UGT1A1 (but NOT CYP3A4)

Raltegravir (RAL)

Can cause Steven-Johnsons Syndrome (not an NNRTI)

Raltegravir (RAL)

Protease Inhibitor (PI)

Amprenavir (APV)

Protease Inhibitor (PI)

Fosamprenavir (FPV)

Protease Inhibitor (PI)

Atazanavir (ATV)

Protease Inhibitor (PI)

Darunavir (DRV)

Protease Inhibitor (PI)

Indinavir (IDV)

Protease Inhibitor (PI)

Lopinavir/Ritonavir (LPV/r)

Protease Inhibitor (PI)

Nelfinavir (NFV)

Protease Inhibitor (PI) BOOSTER only

Ritonavir (RTV)

Protease Inhibitor (PI)

Saquinavir (SQV)

Protease Inhibitor (PI)

Tipranavir (TPV)

Only Protease Inhibitor (PI) that should be taken on an empty stomach and NOT with a high fat meal

Indinavir (IDV)

Do not administer to patient with sulfa allergy.

Darunavir (DRV)

Do not administer to patient with sulfa allergy.

Fosamprenavir (FPV)

Do not administer to patient with sulfa allergy.

Tiprinavir (TPV)

Prodrug of Amprenavir.

Fosamprenavir (FPV)

Potent inhibitor of CYP3A4. Increases serum concentrations of other Protease Inhibitors.

Ritonavir (RTV)

Paresthesias very common at therapeutic dose.

Ritonavir (RTV)

Can cause QT prolongation if combined with Saquinavir (SQV)

Ritonavir (RTV)

Often used as a booster for other Protease Inhibitors.

Ritonavir (RTV)

Structurally similar to Ritonavir (RTV) but 3-10x more potent.

Lopinavir (LPV)

Requires an acidic medium. Take on an empty stomach.

Indinavir (IDV)

Can cause nephrolithiasis - kidney stones. Drink plenty of water.

Indinavir (IDV)

One of two NON-peptide protease inhibitors.

Darunavir (DRV)

One of two NON-peptide protease inhibitors.

Tiprinavir (TPV)

The ONLY Protease Inhibitor that does not require RTV boost.

Nelfinavir (NFV)

Protease Inhibitor that is recommended during pregnancy.

Nelfinavir (NFV)

Protease Inhibitor that can cross blood brain barrier.

Atazanavir (ATV)

Can cause nephrolithiasis - kidney stones. Drink plenty of water.

Atazanavir (ATV)

No activity against against HIV. Pharmacokinetic booster only.

Cobicistat (Tyboost)

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