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Rilpivirine Dosage

Medically reviewed by Drugs.com. Last updated on Feb 15, 2021.

Applies to the following strengths: 25 mg

Usual Adult Dose for:

Usual Pediatric Dose for:

Additional dosage information:

Usual Adult Dose for HIV Infection

25 mg orally once a day

Comments (for Treatment of HIV-1 in Combination with Cabotegravir):
-The manufacturer product information for cabotegravir-rilpivirine IM should be consulted before starting this drug to ensure therapy with cabotegravir-rilpivirine IM is appropriate.
-This drug should be taken with cabotegravir tablets (30 mg orally once a day) at about the same time each day with a meal; the manufacturer product information for cabotegravir tablets should be consulted.
-To assess tolerability of this drug, oral lead-in should be used for about 1 month (at least 28 days) before the initiation of cabotegravir-rilpivirine IM.
-The final oral dose should be administered on the same day injections with cabotegravir-rilpivirine are started.
-If a patient plans to miss a scheduled cabotegravir-rilpivirine injection visit by more than 7 days, daily oral therapy may be used to replace up to 2 consecutive monthly injection visits; the first dose of oral therapy should be administered about 1 month after the last injection dose of cabotegravir-rilpivirine IM and continued until the day injection dosing is restarted. The manufacturer product information for cabotegravir-rilpivirine IM should be consulted to resume monthly injection dosing.

Uses:
-In combination with other antiretroviral agents, for the treatment of HIV-1 infection in antiretroviral therapy-naive patients with plasma HIV-1 RNA up to 100,000 copies/mL at the start of therapy
-In combination with cabotegravir tablets, for short-term treatment of HIV-1 infection in patients who are virologically suppressed (HIV-1 RNA less than 50 copies/mL) on a stable antiretroviral regimen with no history of treatment failure and with no known/suspected resistance to either cabotegravir or rilpivirine, for use as:
---Oral lead-in to assess tolerability of this drug before starting rilpivirine IM (a component of cabotegravir-rilpivirine IM)
---Oral therapy for patients who will miss planned injection dosing with cabotegravir-rilpivirine IM

Usual Pediatric Dose for HIV Infection

12 years or older, weighing at least 35 kg: 25 mg orally once a day

Use: In combination with other antiretroviral agents, for the treatment of HIV-1 infection in antiretroviral therapy-naive patients with plasma HIV-1 RNA up to 100,000 copies/mL at the start of therapy

Renal Dose Adjustments

Mild or moderate renal dysfunction: No adjustment recommended.
Severe renal dysfunction, ESRD: Caution and increased monitoring for side effects recommended.

Liver Dose Adjustments

Mild or moderate liver dysfunction (Child-Pugh A or B): No adjustment recommended.
Severe liver dysfunction (Child-Pugh C): Data not available

Dose Adjustments

If used with rifabutin: Increase dose to 50 mg orally once a day.
-When rifabutin is stopped: Decrease dose to 25 mg orally once a day.

The use of cabotegravir-rilpivirine IM with rifabutin is contraindicated.

Precautions

CONTRAINDICATIONS:
-Coadministration with drugs that may significantly decrease rilpivirine plasma levels due to CYP450 3A enzyme induction or gastric pH increase
-Coadministration with carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, rifapentine, proton pump inhibitors (e.g., esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole), systemic dexamethasone (more than a single dose), St. John's wort

Safety and efficacy have not been established in pediatric patients younger than 12 years or weighing less than 35 kg.

Consult WARNINGS section for additional precautions.

Dialysis

Data not available

Comments:
-This drug is highly bound to plasma proteins; significant removal via hemodialysis or peritoneal dialysis is unlikely.

Other Comments

Administration advice:
-Treatment of HIV-1 in Therapy-Naive Patients: Use in combination with other antiretroviral drugs.
-Administer with a meal; a protein drink alone does not replace a meal.
-Administer antacids (e.g., aluminum/magnesium hydroxide, calcium carbonate) at least 2 hours before or at least 4 hours after this drug; administer H2-receptor antagonists at least 12 hours before or at least 4 hours after this drug.
-Consult the manufacturer product information regarding missed doses.

Storage requirements:
-Store at 25C (77F); excursions permitted to 15C to 30C (59F to 86F).
-Store in original bottle to protect from light.

General:
-Limitations of Use (Treatment of HIV-1 in Therapy-Naive Patients): More patients starting this drug with HIV-1 RNA greater than 100,000 copies/mL had virologic failure (HIV-1 RNA at least 50 copies/mL) compared to those with HIV-1 RNA up to 100,000 copies/mL.
-Treatment of HIV-1 in Therapy-Naive Patients: No dose adjustment is needed for pregnant patients already on a stable regimen with this drug before pregnancy who are virologically suppressed (HIV-1 RNA less than 50 copies/mL); since lower drug exposures were observed during pregnancy, viral load should be monitored closely.

Monitoring:
-General: Viral load in pregnant patients
-Hepatic: Liver function tests (before and during therapy) and for hepatotoxicity (during therapy) in patients with underlying hepatic disease or marked baseline transaminase elevations; liver enzymes in patients with no preexisting hepatic dysfunction or other risk factors

Patient advice:
-Read the US FDA-approved patient labeling (Patient Information).
-Contact healthcare provider at once if rash develops; stop this drug immediately and seek medical care if rash develops with fever, blisters, mucosal involvement, eye inflammation (conjunctivitis), severe allergic reaction (causing swelling of the face/eyes/lips/mouth/tongue/throat, which may lead to difficulty swallowing/breathing), and/or any signs/symptoms of liver problems.
-Seek medical evaluation at once if depressive symptoms develop.
-Notify healthcare provider at once of any signs/symptoms of infection.

Frequently asked questions

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.