| Question | Answer |
| 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...... |
