Comparative Chart: Zidovudine, Efavirenz, Lopinavir, Dolutegravir, Enfuvirtide, Maraviroc
Comparative Chart: Zidovudine, Efavirenz, Lopinavir, Dolutegravir, Enfuvirtide, Maraviroc
| Drug | Pharmacokinetics | Drug-Drug Interactions | Common Side Effects |
|---|---|---|---|
| Zidovudine (NRTI) | Oral bioavailability ~60–70% Half-life: ~1 hr (plasma), ~3–4 hrs (intracellular) Renal excretion |
Competes with other drugs for glucuronidation Increased toxicity with other myelosuppressive agents |
Anemia, neutropenia, headache, GI upset, lactic acidosis |
| Efavirenz (NNRTI) | Oral bioavailability: ~45% (↑ with high-fat meals) Half-life: ~40–55 hrs Hepatic metabolism (CYP2B6, 3A4) |
Potent CYP3A4 inducer – ↓ levels of many drugs (e.g., oral contraceptives, antifungals, statins) | CNS effects (vivid dreams, dizziness), rash, hepatotoxicity |
| Lopinavir (PI) | Poor oral bioavailability unless boosted (usually with ritonavir) Half-life: ~5–6 hrs Hepatic metabolism (CYP3A) |
Ritonavir inhibits CYP3A → ↑ Lopinavir levels Significant DDI with many drugs: statins, sedatives, anticoagulants |
Hyperlipidemia, diarrhea, insulin resistance, QT prolongation |
| Dolutegravir (INSTI) | Good oral bioavailability Half-life: ~13–15 hrs Metabolized by UGT1A1 and CYP3A4 |
Interacts with polyvalent cations (↓ absorption) Rifampin ↓ DTG levels Minor CYP3A4 interactions |
Insomnia, headache, weight gain, ↑ creatinine (not nephrotoxic) |
| Enfuvirtide (Fusion Inhibitor) | Subcutaneous only Half-life: ~3.8 hrs Catabolism via proteolysis (non-CYP) |
No major CYP interactions Minimal DDIs |
Injection site reactions (98%), hypersensitivity, bacterial pneumonia |
| Maraviroc (CCR5 Antagonist) | Oral bioavailability: ~23% Half-life: ~14–18 hrs Metabolized by CYP3A4 and P-gp |
CYP3A4 inhibitors (e.g., ketoconazole) ↑ levels CYP inducers (e.g., rifampin) ↓ levels |
Hepatotoxicity, rash, orthostatic hypotension, upper respiratory infections |
Summary Highlights:
-
Zidovudine: Watch for hematologic toxicity.
-
Efavirenz: CNS side effects; avoid with CYP3A4 substrates.
-
Lopinavir: Strong CYP3A4 interactions; metabolic effects.
-
Dolutegravir: Fewer interactions; caution with cation-containing antacids.
-
Enfuvirtide: Injection only, no CYP-related interactions.
-
Maraviroc: Requires CCR5 tropism testing; CYP3A4-dependent.
- GET MORE MCQ: Click Here