Formulary
Rilpivirine: Indications, Dosing, Side Effects and Interactions
Rilpivirine clinical drug profile including indications, dosing, side effects, cautions and interactions.
MedNext Academy | 4 min read
Rilpivirine: Indications, Dosing, Side Effects and Interactions
Rilpivirine clinical drug profile including indications, dosing, side effects, cautions and interactions.
Indications and dose
**HIV-1 infection [in combination with other antiretroviral drugs] (specialist use only)**
- **Adult** (By Mouth Using Film-Coated Tablets): 25 mg once daily, dose to be taken with food.
**HIV-1 infection [oral lead-in therapy, in combination with cabotegravir] (specialist use only)**
- **Adult** (By Mouth Using Film-Coated Tablets): 25 mg once daily for approximately 1 month (at least 28 days) with food 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 cabotegravir prolonged-release injection] (specialist use only)**
- **Adult** (By Intramuscular Injection): Initially 900 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 600 mg every month, to be given 1 month after initial injection, alternatively initially 900 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 900 mg every 2 months, to be given 2 months after previous injection.
**HIV-1 infection [in combination with other antiretroviral drugs] (specialist use only) for rilpivirine**
- **Child 2-17 years (body-weight 25 kg and above)** (By mouth using film-coated tablets): 25 mg once daily, dose to be taken with food.
**HIV-1 infection [oral lead-in therapy, in combination with cabotegravir] (specialist use only) for rilpivirine**
- **Child 12-17 years (body-weight 35 kg and above)** (By mouth using film-coated tablets): 25 mg once daily for approximately 1 month (at least 28 days) with food 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 cabotegravir prolonged-release injection] (specialist use only) for rilpivirine**
- **Child 12-17 years (body-weight 35 kg and above)** (By intramuscular injection): Initially 900 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 600 mg every month, to be given 1 month after initial injection, alternatively initially 900 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 900 mg every 2 months, to be given 2 months after previous injection.
Cautions
Acute porphyrias ; co-infection with hepatitis B or C; risk factors for virological failure Cautions, further information Risk factors for virological failure 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 Depression; dizziness; drowsiness; gastrointestinal discomfort; headache; nausea; sleep disorders; vomiting Specific side-effects: Common or very common With intramuscular use Anxiety; asthenia; diarrhoea; feeling hot; fever; flatulence; malaise; myalgia; skin reactions; weight increased With oral use Appetite decreased; dry mouth; fatigue; rash Uncommon With intramuscular use Hepatotoxicity With oral use Immune reconstitution inflammatory syndrome Frequency not known With intramuscular use Pancreatitis
Interactions
**Severe interactions:**
- In a clinical study, oral rilpivirine (25 mg once daily) did not significantly affect the pharmacokinetics of digoxin.
**Other interactions (37):**
- Rilpivirine, in combination with cabotegravir injection, is intended for use as a complete regimen for the treatment of HIV-1 infection and should not be administered with other antiretroviral...
- From a drug interaction perspective, there are no limitations on the use of other antiretroviral medicinal products after discontinuing rilpivirine.
- For the oral lead-in rilpivirine treatment and in case missed doses are replaced by oral rilpivirine treatment, refer to the oral rilpivirine tablet SmPC for information about drug interactions.
- Medicinal products that affect rilpivirine exposure Rilpivirine is primarily metabolised by cytochrome P450 (CYP)3A.
- Medicinal products that induce or inhibit CYP3A may thus affect the clearance of rilpivirine (see section 5.2).
- Coadministration of rilpivirine and medicinal products that induce CYP3A has been observed to decrease the plasma concentrations of rilpivirine, which could reduce the therapeutic effect of...
Pregnancy
With oral use: Use only if potential benefit outweighs risk-no toxicity observed in animal studies. If used, monitoring of viral load is recommended. M With intramuscular use: Avoid unless potential benefit outweighs risk-no information available. May remain in systemic circulation for up to 4 years after last prolonged-release injection. If used, monitoring of viral load is recommended. 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 4 years after last prolonged-release injection. M
Hepatic impairment
Manufacturer advises caution in moderate impairment (limited information available); avoid in severe impairment (no information available).
Renal impairment
Manufacturer advises caution in severe impairment.
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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