Hiv Drugs

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Nucleoside Reverse Transcriptase Inhibitors (NRTI)

Back 1

MOA: inhibits viral reverse transcriptase
Toxicities: Lactic acidosis, hepatomegaly, steatosis
Elination: all renal except ZDV (glucuronidation)

Includes:
Zidovudine (ZDV)- used in pregnancy, causes: anemia, granulocytopenia, headache.
Lamivudine- causes GI, insomnia, neuropathy, pancreatitis
Tenofovir (TDF)- hypersensitivity
Emtricitabine (FTC) - hypersensitivity
Didanosine- short half life, not used
Stavudine- short half life not used
Abacavir - short half life not used

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Non Nucleoside Reverse Transcriptase Inhibitors (NNRTI)

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MOA: blocks HIV-1 reverse transcriptase
Elimination through CYP- 450 3A4

Includes:
Nevirapine (NVP)- induces CYP 450, rapid resistance, steven johnson syndorme and hypersensitivity
Efavirenz- Induces CYP 450, same as NVP plus CNS problems
Delavirdine- same as other two

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Fusion Inhibitor

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Enfuvirtide

MOA: inhibits fusion of viral and cellular membranes to prevent entry of HIV into cells
Metabolized into constituent AA
Toxicity: injection site reactions, bacterial pneumonia and hypersensitivity

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Entry Inhibitor

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Maraviroc (MVC)

MOA: inhibits CCR5 and blocks free virus attachment to host cell
Metabolized by CYP 450 3A4
Toxicities: GI pain, cough, airway infection, orthostatic hypotension, allergies
*no induction or inhibition of CYP

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Integrase Inhibitor

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Raltegravir (RAL)

MOA: blocks enzyme for combination of viral DNA and host DNA

Toxicity: nausea, headache, diarrhea, fever, CPK elevation, hupercholesterolemia

*no CYP induction or inhibition

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Protease Inhibitors

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MOA: inhibits HIV 1 and 2 protease
CYP 450 3A4 elimination
Includes:
Saquinavir- used in combo with Ritonavir,
Ritonavir
Nelfinavir- resistance
Lopinavir- used with ritonavir, resistance
Atazanavir- hyperbilirubinemia, rash and prolonged PR interval, antacids are contraindicated
Fosamprenavir