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HIV Pharmacology
For Pharmacology NURS 422
| Term | Definition |
|---|---|
| Virus | Smallest infective agent Most common cause of disease in humans Consists of DNA & RNA Surrounded by protein shell Parasitic - Cannot survive without a host Drugs interrupt replication cycle in viruses Short 1/2 lives |
| Virus (Cont.) | Can stick to cell membrane, causing phagocytosis. Can stick to sell surface and inject genetic material into host cell Makes envelope to surround viral capsid |
| Acyclovir | ANTIVIRAL AGENT Active only against HSV (Herpes Simplex Virus), VZV (Varicella Zoster Virus aka Chickenpox), CMV (Cytomegalovirus), but is resistant to CMV |
| Acyclovir MOA | Suppresses synthesis of viral DNA - Inhibits DNA polymerase - Incorporates itself into growing viral DNA strand |
| Acyclovir Administration | PO (low bioavailability), IV (most often), Topical Execrated through kidneys; dosage is lowered for patients with CKD |
| Acyclovir Side Effects | PO: GI IV: Infusion site reactions, reversible nephrotoxicity due to deposition in renal tubules. INFUSE SLOWLY (over 1-2 hours) |
| Antiretroviral Therapy | DELAY disease progression, AVOID drug resistance, MINIMIZE clinical manifestations, PROLONG survival. Pre & Post-Exposure Prophylaxis (PrEP) 6 drug classes w/many agents; only a fraction are used |
| Classification of Antiretroviral Drugs | Fusion Inhibitors Entry Inhibitors - CCR5 Co-receptor antagonists Nucleoside/-tide Reverse Transcriptase Inhibitors (NRTIs) Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs) Integrase Inhibitors Protease Inhibitors |
| Abacavir | NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR (NRTI) Usually given in pairs. I.e: ABC/3TC (Abacavir + lamivudine) Can be taken with or without food |
| Abacavir MOA | Suppresses synthesis of viral DNA by stopping reverse transcriptase. Prodrug - competitively binds to viral reverse transcriptase Once incorporated into DNA strand, stops RT from adding more bases, thus not allowing DNA to grow |
| Abacavir Adverse Effects | BLACK BOX WARNING FOR HYPERVENTILATION May impair mitochondrial function (Lactic acidosis, fatty/enlarged liver, pancreatitis, myopathies) |
| Abacavir Adverse Effects (Cont.) | Hypersensitivity (in the 1st 6 weeks) 5-8% Fatigue & Headache - 10% Lipodystrophy (cushing-like syndrome) |
| Abacavir Contraindications | Genetic testing required. People who test positive for HLA-B*5701 should NEVER take this drug Avoid in patients w/ CAD Interacts with alcohol = increases ABC levels |
| Efavirenz (Sustiva) | NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR (NNRTI) Rarely used now Taken orally once a day ONLY ACTIVE IN HIV-1 Paired w/NRTI to decease viral load CAN CROSS BBB |
| Efavirenz MOA | DIRECTLY binds to active center of reverse transcriptase and causes direct inhibition of RT activity |
| Efavirenz Drug Interactions | Ritonavir = Creates toxic levels of Efavirenz |
| Efavirenz Adverse Effects | Teratogenicity - Avoid in pregnancy Transient CNS effects (feeling drunk) Maculopapular Rash |
| Darunavir | PROTEASE INHIBITOR Very effective HIGH side effect profile |
| Darunavir MOA | Prevents maturation of HIV by blocking protease. Binds to active site in HIV protease. HIGH HIV resistance, which is why this drug is NEVER used alone |
| Protease Inhibitors Adverse Effects | Hyperglycemia/Diabetes Lipodystrophy Hyperlipidemia Elevated Liver Enzymes Prolongation PR Interval |
| Protease Inhibitors Drug Interactions | Drugs that reduce/inhibit cytochrome P-450 (MANY DRUG INTERACTIONS) Statins = Inhibits metabolism; increases risk of rhabdomylosis |
| Darunavir Adverse Effects | Elevated blood lipid levels - 25% Rash - 10% CYP-system interactions; can increase levels of cardiac drugs |
| Ritonavir | PROTEASE INHIBITOR - BOOSTER Powerful inhibitor, substrate & reducer of hepatic CYP 450 |
| Ritonavir MOA | "Boosts" the serum concentration of other PIs Allows for lower dosing of boosted drug and decreases pill burden (REDUCES side effects) |
| Ritonavir Side Effects | GI Intolerance Hyperlipidemia |
| Raltegravir | INTERGRASE STRAND TRANSFER INHIBITOR (INSTI) 1st in its class Better viral suppression than NNRTI or PI HIGH risk of HIV resistance - need to be taken with other antiretroviral drugs |
| Raltegravir MOA | Inhibits integrase - DOES NOT allow HIV to enter into host cell. Prevents integration of viral DNA |
| INSTI Adverse Effects | Tolerated very well Insomnia, dizziness Diarrhea, nausea, headache, fatigue, itching Women MUST use birth control - FDA pregnancy risk |
| Raltegravir Adverse Effects | Elevated liver enzymes Rare severe hypersensitivity reaction - SJS (Steven Johnson Syndrome) |
| Dolutegravir Adverse Effects | ALSO INSTI Lowers risk of HIV resistance MANY drug interactions |
| Enfuvirtide (Fuzeon/T20) | FUSION INHIBITOR 1st and only in its class Never used alone Approved in children older than 6 "Drug of Last Resort" BID subQ Dosing |
| Enfuvirtide MOA | Blocks fusion between viral and target cell membranes - NO entry of HIV into cells |
| Enfuvirtide Adverse Effects | Significant injection site reactions Pneumonia Hypersensitivity Reactions |
| Enfuvirtide Considerations | Pt. must show signs that their viral load is increasing DESPITE treatment Pt. must be treatment intelligent Only used when patients are resistant to other ARTs |
| Maraviroc (Selzentry) | ENTRY INHIBITOR - CCR5 ANTAGONIST Approved in 2009 as first line treatment combined with 2 other NRTIs Effective only in HIV-1 Tropism testing required BEFORE treatment and should be done if pt. is unresponsive to drug BID Dosing |
| Maraviroc MOA | Blocks infection by blocking CCR5 and preventing HIV binding to cell membrane, thus HIV is unable to enter host cell Best for earlier infection when CCR5 tropic virus predominates |
| Maraviroc Side Effects | Strong hepatotoxicity Hypersensitivity reactions |
| Atripla | COMBINATION ANTIRETROVIRAL FIXED DOSE DRUG 2 NRTI (Tenofovir/FTV) + 1 NNRTI (Efavirenz) PO once daily Do not used in pregnancy Effective in pts whose HIV is sensitive to all 3 components of drug |
Created by:
mkeita2
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