APRETUDE
CABOTEGRAVIR
What it does
Cabotegravir is a medication used to help prevent and treat HIV infection.
Commonly used for: HIV prevention (pre-exposure prophylaxis), HIV treatment (antiretroviral therapy)
Read more in plain English ↓Plain-language summary for general understanding - not medical advice. Always follow your pharmacist/doctor.
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Sourcing - Kenya onlyRegistration & product details
Source: Rwanda Food and Drugs Authority · fetched 2026-03-11 22:07:03 · updated 2026-09-17 02:30:43
Drug Interactions
1Unknown (1)
Cabotegravir - decreases exposure
Rifampicinmodestlydecreasestheexposuretocabotegravir. Avoid.rStudy
Data from BNF 85 (British National Formulary). This is not a substitute for professional medical advice. Matched via: exact
About this medicine
Cabotegravir is a medication used to help prevent and treat HIV infection.
What it treats
- HIV prevention (pre-exposure prophylaxis)
- HIV treatment (antiretroviral therapy)
How it works
Cabotegravir works by blocking the virus from multiplying in the body, helping to keep the immune system strong.
Who it's for
This medication is for individuals at high risk of HIV infection or those already living with HIV.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: Cabotegravir
BNF-referencedCabotegravir is an antiretroviral medication that functions as an inhibitor of HIV integrase, thereby preventing the integration of viral genetic material into the host genome. This mechanism effectively hampers the replication of the HIV virus. It is used in the treatment of HIV-1 infection, typically in combination with other antiretroviral drugs. Cabotegravir is available in both oral and injectable forms, providing flexibility in treatment approaches.
Indications
- HIV-1 infection in combination with other antiretroviral drugs
Dosage
Adults: Initially 600 mg for 1 dose at month 2, to be started on the last day of oral lead-in therapy with cabotegravir and rilpivirine, then maintenance 400 mg every month from month 3 onwards.
Mechanism of action
Cabotegravir binds to the active site of HIV integrase, preventing strand transfer of the viral genome into the host genome, and preventing replication of the virus.
Pharmacodynamics
Cabotegravir is an integrase inhibitor that reduces viral replication. It has a long duration of action, with the oral formulation taken daily and the injectable form administered monthly. Patients must be informed of potential risks, including hypersensitivity reactions, hepatotoxicity, and possible effects on mental health, such as depression.
Pharmacokinetics
Cabotegravir exhibits a long half-life, allowing for once-daily oral dosing and monthly intramuscular administration. The pharmacokinetics may be influenced by factors such as liver function and possible drug interactions, particularly with medications like rifampicin that can decrease cabotegravir exposure. The medication is metabolized primarily in the liver.
Adverse effects
- Headache
- Dizziness
- Somnolence
- Fatigue
- Nausea
- Diarrhoea
- Gastrointestinal discomfort
- Hypersensitivity reactions
- Skin reactions
- Insomnia
- Asthenia
- Concentration impaired
- Anxiety
Interactions
- Rifampicin (modestly decreases exposure to cabotegravir)
Precautions
- Caution in patients with chronic hepatitis B or C due to increased risk of hepatic side effects
- Counsel patients regarding the risk of hypersensitivity, hepatotoxicity, and depression
- Caution required when driving or operating skilled tasks due to potential effects on concentration
Pregnancy
Manufacturer advises use only if potential benefit outweighs risk due to limited information available.
Breast-feeding
Limited information available; consult product literature for specific guidance.
Storage
Store at room temperature, protect from moisture and light. Check specific manufacturer's guidelines for details.
Formulations
- Modified-release tablets (600 mg)
- Intramuscular injection (initially 600 mg, then maintenance 400 mg monthly)
- Powder and solvent for solution for injection
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Molecular reference: Cabotegravir
PubChem CID 54713659Molecular formula: C19H17F2N3O5
Mechanism of action
Cabotegravir binds to the active site of HIV integrase, preventing strand transfer of the viral genome into the host genome, and preventing replication of the virus.
Pharmacodynamics
Cabotegravir is an inhibitor of HIV integrase, which reduces viral replication. It has a long duration of action as the oral tablet is given daily and the intramuscular suspension is given monthly. Patients should be counselled regarding the risk of hypersensitivity, hepatotoxicity, and depression.
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
This drug in other countries
The same active ingredient registered across other registries we cover - including different brands.