Antiviral HIV Pharm
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Life cycle of HIV ? | * binds to CD4+ or CCR5 --> into membrane --> reverse transcrition to make DS DNA --> put RNA in to be into cells
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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
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Usu initial combo ? | * 2 nukes + 1 PI or II or NNRTI
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Nucleoside analogs ? | * Lamivudine
---Zidovudine (AZT)
---Stavudine
---Didanosine
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Protease Inhibitors (PIs) ? | * Ritonavir (RTV)
---Indinavir
---Fosamprenavir
---Nelfinavir
---Saquinavir
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Nonnucleoside RT Inhibitors (NNRTIs) ? | * Efavirenz*
----Nevirapine
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Fusion inhibitor ? | * Enfuvirtide
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Entry Inhibitor – CCR5 antagonist ? | * Maraviroc
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Integrase inhibitor ? | * Raltegravir
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Nucleoside analog MOA ? | * incorporates itself as a triphosphate in to the viral DNA to stop viral replication
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Nucleoside analogs Side Effects ? | * minimal drug/drug interactions..... * Black Box Warning --> Lactic acidosis with hepatic steatosis ...... * Zidovudine - bone marrow depression = anemia
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Preferred in pregnant pts ? | * Zidovudine
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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
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NNRTIs – Advantages ? | * Efavirenz - 1 pill a day..... * Nevirapine - safe in pregnancy
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NNRTIs – Disadvantages ? | * Efavirenz - neuropsych effects, teratogenic,use p450, tons of drud/drug interactions ..... * Nevirapine - hypersensitivity rash and hepatitis
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Protease inhibitors MOA ? | * Competitive inhibition of viral protease, Preventing immature virions from becoming mature
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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
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PI Drug Interactions ? | * Eliminated by hepatic metabolism (CYP3A4)
so watch in using other drugs that inhibit or induce it
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Toxicity of PIs ? | * GI issues , hepatotoxicity , lipodystroophy (moves fat to other places) , hyperlipidemia , and insulin resistance
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Integrase inhibitor MOA ? | * Blocks HIV integrase from inserting viral genome into host cell DNA..... *given injection SubQ
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Fusion inhibitor MOA ? | * Blocks the entry of HIV-1 into CD4+ cells. ---Binds gp41 subunit HIV envelope glycoprotein
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Fusion inhibitor Side Effects ? | * * Also see little wasp sting reactions where it is injected
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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......
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Created by:
thamrick800
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