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ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Integrase inhibitors
cabotegravir
J05AJ04
Forms & Strengths
- Oral tablet: 30 mg
- Extended-release injectable suspension (Vocabria): 400 mg/2 mL
- Extended-release injectable suspension (Apretude): 600 mg/3 mL
Adult Dosing
- HIV Treatment (oral lead-in): 30 mg orally once daily with rilpivirine 25 mg for 28 days
- HIV Treatment (injection): 600 mg intramuscularly once monthly (or 800 mg every 2 months) with rilpivirine
- HIV Pre-Exposure Prophylaxis (PrEP): 600 mg intramuscularly every 2 months (optional 30 mg oral lead-in for 28 days)
Pediatric Dosing
- Not recommended for pediatric patients weighing less than 35 kg
- Safety and efficacy not established in children and adolescents under 12 years of age
Indications
- Treatment of HIV-1 infection in combination with rilpivirine in virologically suppressed adults
- Pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection in at-risk adults and adolescents weighing at least 35 kg
Mechanism of Action
- Integrase strand transfer inhibitor (INSTI)
- Inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral DNA integration, essential for the HIV replication cycle
Contraindications
- Previous hypersensitivity reaction to cabotegravir
- Co-administration with strong CYP3A4/UGT1A1 inducers (e.g., carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, rifapentine, St. John's wort) due to risk of significant decrease in plasma concentrations
Adverse Reactions
- Injection site reactions (pain, tenderness, nodule, swelling)
- Headache
- Pyrexia or fatigue
- Musculoskeletal events (myalgia, back pain)
- Nausea and diarrhea
- Hepatotoxicity (elevated transaminases)
Drug Interactions
- Strong UGT1A1 or CYP3A4 inducers significantly decrease cabotegravir concentrations; co-administration is contraindicated
- May increase plasma concentrations of rifabutin
- No significant pharmacokinetic interactions expected with oral contraceptives, methadone, or most other antiretrovirals
Curated Content: Needs Vetting Before Put to Clinical Use