Cabotegravir is an HIV-1 integrase strand transfer inhibitor (INSTI) that must be used in combination with Rilpivirine. It is indicated for the short-term treatment of virologically suppressed adult patients with HIV-1.

How to Use Cabotegravir

Oral Lead-in Phase

Purpose: To assess the patient's tolerance to Cabotegravir and prepare for the subsequent transition to long-acting injectables (e.g., CABENUVA).

Administration: Orally administer 30mg Cabotegravir plus 25mg Rilpivirine once daily with food, for approximately 1 month (at least 28 days). The last oral dose should be administered on the same day as the first CABENUVA injection.

Temporary Regimen for Missed Injections

If a patient plans to miss a CABENUVA injection by more than 7 days, oral treatment should be initiated instead: 30mg Cabotegravir plus 25mg Rilpivirine daily, until injections are resumed.

The first oral dose should start approximately 1 month after the last injection.

Precautions for Medication Use

Dietary Requirements

When used in combination with Rilpivirine, the medication must be taken with meals. Cabotegravir taken alone has no dietary restrictions.

Drug Interactions

Concomitant use with aluminum/magnesium-containing antacids should be avoided; an interval of at least 2 hours or 4 hours is required between administrations.

Dosage Adjustment and Contraindications of Cabotegravir

Situations Not Requiring Dosage Adjustment

Mild to moderate renal impairment (creatinine clearance ≥ 30mL/min)

Mild to moderate hepatic impairment (Child-Pugh Class A/B)

Contraindications

Allergy History: Contraindicated in patients with a hypersensitivity reaction to Cabotegravir.

Drug Contraindications: Anticonvulsants (e.g., Carbamazepine, Phenytoin) and antituberculous drugs (e.g., Rifampicin, Rifapentine).

Adverse Reactions Requiring Vigilance

Hepatic Toxicity: Monitor liver function; discontinue the drug if suspected liver injury occurs.

Depressive Symptoms: Prompt evaluation is needed if mood swings or suicidal ideation occur.

Cabotegravir Administration in Special Populations

Pregnant Women

Risk Information: Animal studies have shown that high doses may delay parturition or increase the risk of stillbirth; human data are limited.

The use of Cabotegravir during pregnancy requires a careful weighing of benefits and risks. It is recommended to enroll in the Antiretroviral Pregnancy Registry (APR).

Lactating Women

Breastfeeding is Contraindicated: HIV-1 can be transmitted through breast milk, and the effects of Cabotegravir on infants are unknown.

Pediatric and Geriatric Populations

Pediatric Patients: Efficacy data have not been established.

Geriatric Patients: Use with caution, as this population may be accompanied by decreased hepatic or renal function or the risk of polypharmacy.

Patients with Hepatic or Renal Impairment

Severe Hepatic Impairment (Child-Pugh Class C): Use with caution.

End-Stage Renal Disease: No dosage adjustment is required, and dialysis does not affect drug clearance (due to high protein binding).