Cabotegravir is an HIV-1 integrase strand transfer inhibitor (INSTI). As the active ingredient in VOCABRIA, it can be used both for the treatment of HIV-1 infection and pre-exposure prophylaxis (PrEP) against HIV-1.
Precautions for Cabotegravir Administration
Contraindications
History of allergic reactions: Contraindicated in patients who have had a hypersensitivity reaction to cabotegravir.
Contraindicated drug interactions: Concomitant use with UGT1A1 enzyme inducers such as carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampicin, and rifapentine is prohibited. These drugs can significantly reduce the plasma concentration of cabotegravir, leading to loss of efficacy.
HIV-1 infection status: When used for PrEP, it is contraindicated in individuals who are HIV-1 positive or have an unknown infection status.
Precautions for Special Populations
Pregnancy: Limited human data on cabotegravir use during pregnancy are available. Animal studies have shown that high doses may delay parturition and increase the risk of stillbirth. The benefits and risks of use should be carefully weighed.
Lactation: Cabotegravir can pass into animal milk; human data on its presence in breast milk are lacking. Considerations should include the risk of HIV transmission, the development of viral resistance, and potential effects on the infant.
Adolescents: Adolescents aged 12 years and older with a body weight of ≥35 kg may use cabotegravir, but enhanced adherence support and monitoring are required.
Management of Drug Interactions
Antacids containing polyvalent cations: Administration should be separated by at least 2 hours.
Anticonvulsants and antimycobacterial drugs: Most are contraindicated (listed in the "Contraindications" section above).
Rifabutin: Dosage adjustment of APRETUDE is required; concomitant use with CABENUVA is prohibited.
Clinical Monitoring for Cabotegravir
HIV-1 Screening and Monitoring
HIV-1 negativity must be confirmed before initiating treatment or PrEP.
During APRETUDE use, screening should be performed at least once every 3 months.
If symptoms of acute HIV infection occur or there is a recent high-risk exposure, FDA-approved testing methods should be used.
If antigen/antibody testing is negative, confirmation via RNA testing is required.
Hypersensitivity Reaction Monitoring
Monitor for Stevens-Johnson Syndrome/Toxic Epidermal Necrolysis (SJS/TEN).
Monitor for angioedema, urticaria, and other hypersensitivity manifestations.
Key monitoring points: The oral lead-in phase helps identify individuals at high risk of hypersensitivity.
If severe rash, fever, mucosal damage, facial edema, or other hypersensitivity symptoms occur, discontinue the drug immediately.
Liver function (transaminases) and clinical manifestations should be monitored.
Liver Function Monitoring
For HIV-1 treatment: Routine monitoring of liver enzymes is recommended; if hepatotoxicity is suspected, discontinue the drug.
For PrEP: Clinical and laboratory monitoring of liver function should be considered; if hepatotoxicity is suspected, discontinue the drug.
Patients with pre-existing liver disease or significantly elevated transaminases are at increased risk of hepatotoxicity.
Mental Health Monitoring
For HIV-1 treatment: Reports of low mood, depression, and suicidal ideation/behavior may occur.
For PrEP: Depression, persistent depressive disorder, and other mental health issues may occur.
Key monitoring points: Timely assessment of the correlation between symptoms and the drug is required, and the benefits and risks of continuing treatment should be weighed.
