Cabotegravir is an HIV-1 integrase strand transfer inhibitor (INSTI) and serves as the active ingredient in VOCABRIA. It is indicated 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 experienced a hypersensitivity reaction to cabotegravir.
Contraindications due to 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 therapeutic efficacy.
HIV-1 infection status: When used for PrEP, it is contraindicated in individuals who are HIV-1 positive or have an unknown HIV-1 infection status.
Precautions for Special Populations
Pregnancy: Limited data are available on the use of cabotegravir in human pregnancy. Animal studies have shown that high doses may delay parturition and increase the risk of stillbirth. The benefits and risks should be carefully weighed before use.
Lactation: Cabotegravir can pass into animal milk, while data on its presence in human milk are lacking. Considerations should include the risk of HIV transmission, the development of viral resistance, and potential effects on the infant.
Adolescents: Cabotegravir can be used in adolescents aged 12 years and older with a body weight of ≥ 35 kg, 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 from cabotegravir.
Anticonvulsants and antimycobacterial drugs: Most of these drugs are contraindicated (listed earlier in the text).
Rifabutin: Dosage adjustment of APRETUDE is required; concomitant use with CABENUVA is prohibited.
Clinical Monitoring for Cabotegravir
HIV-1 Screening and Monitoring
Confirmation of HIV-1 negativity is mandatory before initiating treatment.
During treatment with APRETUDE, screening should be performed at least once every 3 months.
When symptoms of acute HIV infection occur or recent high-risk exposure is reported, FDA-approved testing methods should be used.
If antigen/antibody testing is negative, confirmation should be obtained via RNA testing.
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 reactions.
Immediately discontinue the drug if severe rash, fever, mucosal lesions, facial edema, or other related symptoms occur.
Monitor liver function (transaminases) and clinical manifestations.
Liver Function Monitoring
For HIV-1 infection treatment: Routine monitoring of liver enzymes is recommended; discontinue the drug if hepatotoxicity is suspected.
For PrEP use: Consider clinical and laboratory monitoring; discontinue the drug if hepatotoxicity is suspected.
Patients with pre-existing liver disease or significantly elevated transaminases face an increased risk of hepatotoxicity.
Mental Health Monitoring
For HIV-1 infection treatment: Reports of low mood, depression, and suicidal ideation/behavior may occur.
For PrEP use: Conditions such as depression and persistent depressive disorder may occur.
Key monitoring points: Promptly assess the correlation between symptoms and the drug, and weigh the benefits and risks of continuing treatment.
