Pronunciation:
ka-boe-teg-ra-vir
Trade Name(s)
Ther. Class.
Pharm. Class.
integrase strand transfer inhibitors instis
Inhibits HIV-1 integrase, which is required for viral replication.
Therapeutic Effect(s):
Absorption: Increased with high-fat meals after oral administration.
Distribution: Widely distributed to extravascular tissues.
Protein Binding: >99%.
Metabolism and Excretion: Primarily metabolized by the uridine diphosphate glucuronosyltransferase (UGT) 1A1 enzyme system, with some involvement of UGT1A9. Primarily excreted in feces as unchanged drug (47%), with 27% excreted in urine as metabolites.
Half-life: PO: 41 hr; IM: 5.6–11.5 wk.
TIME/ACTION PROFILE (plasma concentrations)
ROUTE | ONSET | PEAK | DURATION |
---|---|---|---|
PO | unknown | 3 hr | 24 hr |
IM | unknown | 7 days | 2 mo |
Contraindicated in:
Use Cautiously in:
GI: diarrhea, HEPATOTOXICITY, nausea
Local: injection site reactions
MS: ↑ creatine kinase (injection)
Neuro: abnormal dreams, anxiety, depression, dizziness, fatigue, headache, insomnia, mood disturbances
Misc: fever, HYPERSENSITIVITY REACTIONS (including angioedema)
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
Drug-Drug
Strong UGT1A1 inducers, including carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, rifapentine may significantly ↓ levels and effectiveness; concurrent use contraindicated.
HIV-1 Treatment
Oral Lead-in Dosing to Assess Tolerability of Cabotegravir
PO (Adults and Children ≥12 yr and ≥35 kg): 30 mg once daily (taken with rilpivirine 25 mg once daily). Continue for ≥28 days to assess tolerability prior to initiating cabotegravir/rilpivirine extended-release injection (Cabenuva) therapy. The last dose of oral cabotegravir should be taken on the same day that cabotegravir/rilpivirine extended-release injection (Cabenuva) therapy is initiated.
Oral Dosing to Replace Planned Missed Doses of Cabotegravir/Rilpivirine Extended-Release Injection (Cabenuva)
PO (Adults and Children ≥12 yr and ≥35 kg): To replace planned missed cabotegravir/rilpivirine extended-release injections (Cabenuva) for patients on monthly dosing schedule (if patient plans to miss scheduled monthly injection by >7 days): 30 mg once daily (with rilpivirine 25 mg once daily) initiated at the same time as missed injection of cabotegravir/rilpivirine and then continued until day the cabotegravir/rilpivirine extended-release injection (Cabenuva) is restarted (oral replacement therapy can be continued for up to 2 mo). To replace planned missed cabotegravir/rilpivirine extended-release injections (Cabenuva) for patients on every 2-month dosing schedule (if patient plans to miss scheduled every 2-month injection by >7 days): 30 mg once daily (with rilpivirine 25 mg once daily) initiated the same time as missed injection of cabotegravir/rilpivirine and then continued until day the cabotegravir/rilpivirine extended-release injection (Cabenuva) is restarted (oral replacement therapy can be continued for up to 2 mo).
HIV-1 Pre-exposure Prophylaxis
May initiate with cabotegravir oral lead-in therapy (to assess tolerability of cabotegravir) prior to cabotegravir IM injections or may precede directly to cabotegravir IM injections without oral lead-in.Oral Lead-in Therapy
PO (Adults and Children ≥12 yr and ≥35 kg): 30 mg once daily. Continue for ≥28 days to assess tolerability prior to initiating IM therapy (see Initiation Injection Therapy section below).
Initiation Injections
IM (Adults and Children ≥12 yr and ≥35 kg): With oral lead-in therapy: 600 mg once monthly for 2 consecutive mo (second initiation injection may be administered up to 7 days before or after the date the individual is scheduled to receive the injection), then proceed with Continuation Injections. First initiation injection should be given on the last day of oral cabotegravir lead-in therapy or within 3 days of the last dose of oral cabotegravir lead-in therapy (see Oral Lead-in Therapy section above to assess tolerability of cabotegravir). Without oral lead-in therapy: 600 mg once monthly for 2 consecutive mo (second initiation injection may be administered up to 7 days before or after the date the individual is scheduled to receive the injection), then proceed with Continuation Injections.
Continuation Injections
IM (Adults and Children ≥12 yr and ≥35 kg): 600 mg every 2 mo starting 2 mo after the last initiation injection (injection may be administered up to 7 days before or after the date the individual is scheduled to receive the injection).
Missed Doses of Injection
PO (Adults and Children ≥12 yr and ≥35 kg): Planned missed injections: If a patient plans to miss a scheduled every 2-mo dose of cabotegravir extended-release injection (Apretude) by >7 days, use cabotegravir 30 mg once daily to replace one every 2-mo injection. The first dose of oral therapy should be taken approximately 2 mo after the last dose of cabotegravir extended-release injection (Apretude) and continued until the day that injection dosing is restarted or within 3 days of injection dosing being restarted. For oral PrEP durations >2 months, use an alternative oral regimen for PrEP. Unplanned missed injections: If a scheduled injection visit is missed or delayed by >7 days and oral dosing has not been taken in the interim, clinically reassess to determine if injection therapy remains appropriate.
Tablets (Vocabria): 30 mg
Extended-release suspension for injection (Apretude): 200 mg/mL
Monitor for anxiety, depression (especially in patients with a history of psychiatric illness), suicidal ideation, and paranoia during therapy.
Monitor for signs and symptoms of hypersensitivity reactions (severe rash, or rash accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, oral blisters or lesions, conjunctivitis, facial edema, hepatitis, eosinophilia, angioedema, difficulty breathing) during therapy. Discontinue cabotegravir immediately if reactions occur.
Lab Test Considerations:
Monitor liver functions tests periodically during therapy.
Advise patient to notify health care professional if signs and symptoms of allergic reaction (fever, generally ill feeling, tiredness, muscle or joint aches, trouble breathing, blisters or sores in mouth, blisters, redness or swelling of eyes, swelling of mouth, face, lips, or tongue), liver problems (yellow skin or white part of eyes, dark or "tea-colored" urine, light-colored stools, nausea or vomiting, loss of appetite, pain, aching, or tenderness on the right side of stomach area, itching) or depression (feeling sad or hopeless, feeling anxious or restless, have thoughts of hurting yourself (suicide) or have tried to hurt yourself) occur.