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Antiviral HIV Pharm

Life cycle of HIV ? * binds to CD4+ or CCR5 --> into membrane --> reverse transcrition to make DS DNA --> put RNA in to be into cells
Antiretroviral drug classes ? * Nucleoside analogs (NRTIs or nukes) ----Nonnucleoside reverse transcriptase inhibitors (NNRTIs or non-nukes) ----Protease inhibitors (PIs) ----Integrase inhibitors ----Fusion inhibitors ----Entry inhibitors – CCR5 antagonists
Usu initial combo ? * 2 nukes + 1 PI or II or NNRTI
Nucleoside analogs ? * Lamivudine ---Zidovudine (AZT) ---Stavudine ---Didanosine
Protease Inhibitors (PIs) ? * Ritonavir (RTV) ---Indinavir ---Fosamprenavir ---Nelfinavir ---Saquinavir
Nonnucleoside RT Inhibitors (NNRTIs) ? * Efavirenz* ----Nevirapine
Fusion inhibitor ? * Enfuvirtide
Entry Inhibitor – CCR5 antagonist ? * Maraviroc
Integrase inhibitor ? * Raltegravir
Nucleoside analog MOA ? * incorporates itself as a triphosphate in to the viral DNA to stop viral replication
Nucleoside analogs Side Effects ? * minimal drug/drug interactions..... * Black Box Warning --> Lactic acidosis with hepatic steatosis ...... * Zidovudine - bone marrow depression = anemia
Preferred in pregnant pts ? * Zidovudine
Nonnucleoside Reverse transcriptase Inhibitors (NNRTIs) MOA ? * Same target….but binds to unique site that causes a confirmational change in enzyme so it doesn't work ..... * Bind directly to HIV-RT and are direct acting
NNRTIs – Advantages ? * Efavirenz - 1 pill a day..... * Nevirapine - safe in pregnancy
NNRTIs – Disadvantages ? * Efavirenz - neuropsych effects, teratogenic,use p450, tons of drud/drug interactions ..... * Nevirapine - hypersensitivity rash and hepatitis
Protease inhibitors MOA ? * Competitive inhibition of viral protease, Preventing immature virions from becoming mature
Addition of ritonavir to Lopinavir ? * makes Lopinavir a multiple dose a day drug to a one day dosed.... RTV is often used with other PIs to boost them
PI Drug Interactions ? * Eliminated by hepatic metabolism (CYP3A4) so watch in using other drugs that inhibit or induce it
Toxicity of PIs ? * GI issues , hepatotoxicity , lipodystroophy (moves fat to other places) , hyperlipidemia , and insulin resistance
Integrase inhibitor MOA ? * Blocks HIV integrase from inserting viral genome into host cell DNA..... *given injection SubQ
Fusion inhibitor MOA ? * Blocks the entry of HIV-1 into CD4+ cells. ---Binds gp41 subunit HIV envelope glycoprotein
Fusion inhibitor Side Effects ? * * Also see little wasp sting reactions where it is injected
Entry inhibitor MOA ? * Binds CCR5 and blocks the HIV gp120 from associating with the receptor. HIV is then unable to bind and enter cells .... * need to do receptor tests bc if HIV binds to other ones, this drug won't work, only on CCR5......
Created by: thamrick800