Adult: In patients who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen without present or past evidence of viral resistance to, and no prior virological failure with NNRTI and INI agents: In combination with rilpivirine inj: Initially, 600 mg for 1 dose at month 2, to be started on the last day of oral lead-in therapy, then 400 mg every month from month 3 onwards. Alternatively, initially, 600 mg for 2 doses at months 2 and 3, to be started on the last day of oral lead-in therapy, then 600 mg every 2 months from month 5 onwards. Maintenance doses may be administered up to 7 days before or after the scheduled dose. Refer to specific product guidelines for detailed dosing recommendations and instructions on how to manage missed doses.
Oral HIV-1 infection
Adult: As short-term treatment in patients who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen without present or past evidence of viral resistance to, and no prior virological failure with non-nucleoside reverse transcriptase inhibitors (NNRTI) and integrase inhibitors (INI) agents: As oral lead-in therapy, in combination with rilpivirine: 30 mg once daily for approx 1 month (at least 28 days). Refer to specific product guidelines for detailed dosing recommendations and instructions on how to manage missed doses.
Administration
May be taken with or without food.
Contraindications
Hypersensitivity. Lactation. Concomitant use with rifampicin, rifapentine, carbamazepine, oxcarbazepine, phenytoin or phenobarbital.
Special Precautions
Patient with risk factors for virological failure (e.g. HIV-1 A6/A1 subtype, BMI ≥30 kg/m2, archived rilpivirine resistance mutations). Not recommended for initiating treatment in patients with hepatitis B co-infection. Hepatic impairment. Children. Pregnancy.
Adverse Reactions
Significant: Hypersensitivity reactions, hepatotoxicity, immune reactivation syndrome (in patients with severe immune deficiency prior to treatment), depressive disorders (e.g. altered or depressed mood, depression, mood swings, suicidal ideation or attempt). Gastrointestinal disorders: Abdominal pain, diarrhoea, nausea, flatulence, vomiting, abdominal distress. General disorders and administration site conditions: Pyrexia, fatigue, malaise, asthenia, inj site reactions (e.g. pain, discomfort, nodule, induration, warmth, swelling, bruising, haematoma, erythema, pruritus). Investigations: Increased weight, BUN, transaminase, serum creatinine. Metabolism and nutrition disorders: Decreased appetite. Musculoskeletal and connective tissue disorders: Myalgia, back pain. Nervous system disorders: Headache, dizziness, somnolence; vasovagal reactions (inj). Psychiatric disorders: Insomnia, anxiety, abnormal dreams. Respiratory, thoracic and mediastinal disorders: Upper respiratory tract infection. Skin and subcutaneous tissue disorders: Rash.
Patient Counseling Information
This drug may cause dizziness, fatigue, and somnolence, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor LFTs; signs and symptoms of hypersensitivity and/or skin reactions, mood changes, or liver toxicity. Assess virologic control of HIV (under 50 copies/mL).
Drug Interactions
May decrease the plasma concentration with rifabutin and antacids (e.g. Mg, Al, Ca); administer antacids 2 hours before or 4 hours after oral cabotegravir. Potentially Fatal: May decrease plasma concentrations leading to loss of efficacy with strong inducers of UGT1A1 or UGT1A9 (e.g. phenytoin, phenobarbital, carbamazepine, oxcarbazepine, rifampicin, rifapentine).
Action
Description: Mechanism of Action: Cabotegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral DNA integration which is essential for the HIV replication cycle. Pharmacokinetics: Absorption: Rapidly absorbed (oral). Increased absorption with high fat meal. Time to peak plasma concentration: 3 hours (oral); 7 days (inj). Distribution: Volume of distribution: 12.3 L. Plasma protein binding: Approx >99%. Metabolism: Metabolised primarily by UGT1A1, and to a lesser extent by UGT1A9. Excretion: Via faeces (59%; 47% as unchanged drug); urine (27% as glucuronide metabolite). Elimination half-life: 41 hours (oral); 5.6-11.5 weeks (inj).
Chemical Structure
Cabotegravir Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 54713659, Cabotegravir. https://pubchem.ncbi.nlm.nih.gov/compound/Cabotegravir. Accessed Nov. 23, 2022.
Storage
Tab: Store below 30°C. Intact vials: Store between 2-25°C. Do not freeze. Store susp in a syringe at 25°C for ≤2 hours.
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