Formulary
Cabotegravir: Indications, Dosing, Side Effects and Interactions
Cabotegravir is an inhibitor of HIV integrase.
MedNext Academy | 6 min read
Cabotegravir: Indications, Dosing, Side Effects and Interactions
Cabotegravir is an inhibitor of HIV integrase.
Drug action
Cabotegravir is an inhibitor of HIV integrase.
Indications and dose
**Pre-exposure prophylaxis of HIV-1 infection [oral lead-in therapy] (specialist use only)**
- **Adult** (By Mouth): 30 mg once daily for approximately 1 month (at least 28 days) then, if tolerated, switch to intramuscular treatment with cabotegravir at month 2, for oral dose recommendations if cabotegravir injection is missed-consult product literature.
**Pre-exposure prophylaxis of HIV-1 infection (specialist use only)**
- **Adult** (By Intramuscular Injection): Initially 600 mg every month for 2 doses, to be started on the last day of oral lead-in therapy with cabotegravir or within 3 days thereafter (if used), then maintenance 600 mg every 2 months, to be given 2 months after previous injection.
**HIV-1 infection [oral lead-in therapy, in combination with rilpivirine] (specialist use only)**
- **Adult** (By Mouth): 30 mg once daily for approximately 1 month (at least 28 days) then, if tolerated, switch to intramuscular treatment with cabotegravir and rilpivirine at month 2, for oral dose recommendations if cabotegravir injection and rilpivirine injection are missed-consult product literature.
**HIV-1 infection [in combination with rilpivirine prolonged-release injection] (specialist use only)**
- **Adult** (By Intramuscular Injection): Initially 600 mg for 1 dose, to be started on the last day of oral lead-in therapy with cabotegravir and rilpivirine (if used), or on the last day of current regimen, then maintenance 400 mg every month, to be given 1 month after initial injection, alternatively initially 600 mg every month for 2 doses, to be started on the last day of oral lead-in therapy with cabotegravir and rilpivirine (if used), or on the last day of current regimen, then maintenance 600 mg every 2 months, to be given 2 months after previous injection.
**Pre-exposure prophylaxis of HIV-1 infection [oral lead-in therapy] (specialist use only) for Apretude tablets**
- **Child 12-17 years (body-weight 35 kg and above)** (By mouth): 30 mg once daily for approximately 1 month (at least 28 days) then, if tolerated, switch to intramuscular treatment with cabotegravir at month 2, for oral dose recommendations if cabotegravir injection is missed-consult product literature.
**Pre-exposure prophylaxis of HIV-1 infection (specialist use only) for Apretude injection**
- **Child 12-17 years (body-weight 35 kg and above)** (By intramuscular injection): Initially 600 mg every month for 2 doses, to be started on the last day of oral lead-in therapy with cabotegravir or within 3 days thereafter (if used), then maintenance 600 mg every 2 months, to be given 2 months after previous injection.
**HIV-1 infection [oral lead-in therapy, in combination with rilpivirine] (specialist use only) for Vocabria tablets**
- **Child 12-17 years (body-weight 35 kg and above)** (By mouth): 30 mg once daily for approximately 1 month (at least 28 days) then, if tolerated, switch to intramuscular treatment with cabotegravir and rilpivirine at month 2, for oral dose recommendations if cabotegravir injection and rilpivirine injection are missed-consult product literature.
**HIV-1 infection [in combination with rilpivirine prolonged-release injection] (specialist use only) for Vocabria injection**
- **Child 12-17 years (body-weight 35 kg and above)** (By intramuscular injection): Initially 600 mg for 1 dose, to be started on the last day of oral lead-in therapy with cabotegravir and rilpivirine (if used), or on the last day of current regimen, then maintenance 400 mg every month, to be given 1 month after initial injection, alternatively initially 600 mg every month for 2 doses, to be started on the last day of oral lead-in therapy with cabotegravir and rilpivirine (if used), or on the last day of current regimen, then maintenance 600 mg every 2 months, to be given 2 months after previous injection.
Cautions
When used for HIV-1 infection [in combination with rilpivirine prolonged-release injection] Co-infection with hepatitis B or C; risk factors for virological failure When used for HIV-1 infection [oral lead-in therapy, in combination with rilpivirine] Co-infection with hepatitis B or C; risk factors for virological failure Cautions, further information Risk factors for virological failure When used for HIV-1 infection [oral lead-in therapy, in combination with rilpivirine] or HIV-1 infection [in combination with rilpivirine prolonged-release injection]: Use with caution in patients with HIV-1 subtype A6/A1 or BMI of 30 kg/m 2 or more, if treatment history uncertain and pre-treatment resistance analyses absent. M
Side effects
General side-effects: Common or very common Anxiety; asthenia; depression; diarrhoea; dizziness; feeling hot; fever; flatulence; gastrointestinal discomfort; headache; malaise; myalgia; nausea; skin reactions; sleep disorders; vomiting; weight increased Uncommon Angioedema; drowsiness; hepatotoxicity; suicidal behaviours Specific side-effects: Frequency not known With intramuscular use Pancreatitis
Interactions
**Severe interactions:**
- Table 2 Drug interactions Medicinal products by therapeutic areas Interaction Geometric mean change (%) Recommendations concerning co-administration HIV-1 Antiviral medicinal products Non-nucleoside...
- Non-nucleoside Reverse Transcriptase Inhibitor: Rilpivirine Cabotegravir AUC 12% C max 5% C 14% Rilpivirine AUC 1% C max 4% C 8% Rilpivirine did not significantly change cabotegravir...
- Antimycobacterials Rifampicin Cabotegravir AUC 59% C max 6% Rifampicin significantly decreased cabotegravir plasma concentration which is likely to result in loss of therapeutic effect.
- Rifabutin Cabotegravir AUC 21% C max 17% C 26% Rifabutin did not significantly change cabotegravir plasma concentration.
- Oral Contraceptives Ethinyl estradiol (EE) and Levonorgestrel (LNG) EE AUC 2% C max 8% C 0% LNG AUC 12% C max 5% C 7% Cabotegravir did not significantly change ethinyl estradiol and...
**Other interactions (11):**
- Effect of other agents on the pharmacokinetics of cabotegravir Cabotegravir is primarily metabolised by uridine diphosphate glucuronosyl transferase (UGT) 1A1 and to a lesser extent by UGT1A9.
- Medicinal products which are strong inducers of UGT1A1 or UGT1A9 are expected to decrease cabotegravir plasma concentrations leading to lack of efficacy (see section 4.3 and table 2 below).
- In poor metabolizers of UGT1A1, representing a maximum clinical UGT1A1 inhibition, the mean AUC, C max and C tau of oral cabotegravir increased by up to 1.5-fold (see section 5.2).
- Cabotegravir is a substrate of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), however, because of its high permeability, no alteration in absorption is expected when...
- Effect of cabotegravir on the pharmacokinetics of other medicinal products In vivo , cabotegravir did not have an effect on midazolam, a cytochrome P450 (CYP) 3A4 probe.
- In vitro , cabotegravir did not induce CYP1A2, CYP2B6, or CYP3A4.
Pregnancy
With oral use: Avoid unless potential benefit outweighs risk-no information available. M With intramuscular use: Avoid unless potential benefit outweighs risk-may remain in systemic circulation for up to 12 months or longer after last prolonged-release injection. M
Breast feeding
With oral use: Avoid-present in milk in animal studies. M With intramuscular use: Avoid-may be present in milk for up to 12 months or longer after last prolonged-release injection. M
Hepatic impairment
Caution in severe impairment (no information available). M
Medicinal forms
Tablet,Injection
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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