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 IM are started.
• If a patient plans to miss a scheduled monthly injection of cabotegravir-rilpivirine IM by more than 7 days, daily oral therapy may be used for up to 2 months to replace missed injection visits.
• The first dose of oral therapy should be started at about the same time as the planned missed injection and continued until the day injection dosing is restarted.
• For oral therapy with this drug and cabotegravir tablets of durations longer than 2 months, an alternative oral regimen is recommended (which may include this drug).
• The manufacturer product information for cabotegravir-rilpivirine IM should be consulted to resume monthly injection dosing.
• If a patient plans to miss a scheduled every-2-month injection of cabotegravir-rilpivirine IM by more than 7 days, daily oral therapy may be used for up to 2 months to replace 1 missed scheduled every-2-month injection.
• The first dose of oral therapy should be started at about the same time as the planned missed injection and continued until the day injection dosing is restarted.
• For oral therapy with this drug and cabotegravir tablets of durations longer than 2 months, an alternative oral regimen is recommended (which may include this drug).
• The manufacturer product information for cabotegravir-rilpivirine IM should be consulted to resume every-2-month injection dosing.

• 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:

• At least 35 kg: 25 mg orally once a day

• 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 IM are started.
• If a patient plans to miss a scheduled monthly injection of cabotegravir-rilpivirine IM by more than 7 days, daily oral therapy may be used for up to 2 months to replace missed injection visits.
• The first dose of oral therapy should be started at about the same time as the planned missed injection and continued until the day injection dosing is restarted.
• For oral therapy with this drug and cabotegravir tablets of durations longer than 2 months, an alternative oral regimen is recommended (which may include this drug).
• The manufacturer product information for cabotegravir-rilpivirine IM should be consulted to resume monthly injection dosing.
• If a patient plans to miss a scheduled every-2-month injection of cabotegravir-rilpivirine IM by more than 7 days, daily oral therapy may be used for up to 2 months to replace 1 missed scheduled every-2-month injection.
• The first dose of oral therapy should be started at about the same time as the planned missed injection and continued until the day injection dosing is restarted.
• For oral therapy with this drug and cabotegravir tablets of durations longer than 2 months, an alternative oral regimen is recommended (which may include this drug).
• The manufacturer product information for cabotegravir-rilpivirine IM should be consulted to resume every-2-month injection dosing.

• 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

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

Coadministration with rifabutin: Rilpivirine 50 mg orally once a day

• When rifabutin is stopped: Rilpivirine 25 mg orally once a day

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

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.

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

• 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.

• 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

• Read the US FDA-approved patient labeling (Patient Information).
• Contact health care 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 health care provider at once of any signs/symptoms of infection.

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