Dosing & Uses
Dosage Forms & Strengths
tablet
- 25mg
HIV-1 Infection
Indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in treatment-naïve adult patients with HIV-1 RNA <100,000 copies/mL
25 mg PO qDay; administer with a meal
Dose during pregnancy
- May continue use for pregnant patients on a stable rilpivirine regimen before pregnancy and who are virologically suppressed (ie, HIV-1 RNA <50 copies/mL)
- 25 mg PO qDay; administer with a meal
- Lower exposures of rilpivirine were observed during pregnancy, therefore viral load should be monitored closely
HIV Infection in Combination with Cabotegravir
Indicated in combination with cabotegravir PO as a complete regimen for short-term treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral therapy (ART) regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine
Indication specifics
- Oral lead-in to assess tolerability of rilpivirine before administration of rilpivirine extended-release injectable IM suspension, a component of Cabenuva (cabotegravir; rilpivirine extended-release injectable suspensions)
- Oral therapy for patients who will miss planned IM injection dosing with Cabenuva
Oral lead-in dosing prior to Cabenuva
- 25 mg PO qDay plus cabotegravir 30 mg PO qDay for at least 28 days to assess tolerability
- Take last oral dose on the same day injections with Cabenuva started
Oral replacement dose for planned missed Cabenuva injections
- If a patient plans to miss scheduled Cabenuva (cabotegravir; rilpivirine) extended-release injectable suspensions by >7 days, take daily PO therapy to replace up to 2 consecutive monthly or 1 scheduled every-2-month injection visit(s)
- 25 mg PO qDay plus cabotegravir 30 mg PO qDay as replacement for up to 2 consecutive months
- Take first dose of oral therapy at approximately the same time as the planned missed injection and continue until the day injection dosing restarted
Dosage Modifications
Renal impairment
- Mild-to-moderate renal impairment: No dose adjustment required
- Severe renal impairment or ESRD: Used with caution and with increased monitoring for adverse effects, plasma concentrations may be increased because of altered drug absorption, distribution, and metabolism secondary to renal dysfunction
- Dialysis: Highly bound to plasma proteins, unlikely to be significantly removed by hemodialysis or peritoneal dialysis
Hepatic impairment
- Mild-to-moderate hepatic impairment (Child-Pugh Classes A and B): No dose adjustment required
- Severe hepatic impairment (Child-Pugh Class C): Has not been studied
Dosage Forms & Strengths
tablet
- 25mg
HIV-1 Infection
Indicated in combination with other antiretroviral agents for treatment of HIV-1 infection in treatment-naïve adolescents aged 12-17 yr with HIV-1 RNA ≤100,000 copies/mL
<12 years: Safety and efficacy not established
12-17 years (weight ≥35 kg): 25 mg PO qDay; administer with a meal (see Administration)
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (21)
- carbamazepine
carbamazepine decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration of carbamazepine with NNRTIs may result in a loss of virologic response and possible resistance to the NNRTI.
- dexamethasone
dexamethasone decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class.
- dexlansoprazole
dexlansoprazole decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Contraindicated. Concurrent use may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels.
- efavirenz
efavirenz decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be used in combination with NNRTIs.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
rilpivirine, elvitegravir/cobicistat/emtricitabine/tenofovir DF. Other (see comment). Contraindicated. Comment: Elvitegravir/cobicistat/emtricitabine/tenofovir is a complete regimen for HIV and should not be administered with other antiretrovirals.
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class.
- esomeprazole
esomeprazole decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Contraindicated. Concurrent use may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels.
- etravirine
etravirine decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be used in combination with NNRTIs.
- fosphenytoin
fosphenytoin decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class.
- lansoprazole
lansoprazole decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Contraindicated. Concurrent use may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels.
- nevirapine
nevirapine decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be used in combination with NNRTIs.
- omeprazole
omeprazole decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Contraindicated. Concurrent use may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels.
- oxcarbazepine
oxcarbazepine decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class.
- pantoprazole
pantoprazole decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Contraindicated. Concurrent use may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels.
- phenobarbital
phenobarbital decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class.
- phenytoin
phenytoin decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class.
- rabeprazole
rabeprazole decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Contraindicated. Concurrent use may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels.
- rifampin
rifampin decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class.
- rifapentine
rifapentine decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class.
- St John's Wort
St John's Wort decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class.
- vonoprazan
vonoprazan will decrease the level or effect of rilpivirine by inhibition of GI absorption. Applies only to oral form of both agents. Contraindicated.
Serious - Use Alternative (28)
- amisulpride
amisulpride and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug. ECG monitoring is recommended if coadministered.
- anagrelide
anagrelide and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- artemether
artemether and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- bedaquiline
bedaquiline and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- betibeglogene autotemcel
rilpivirine, betibeglogene autotemcel. Other (see comment). Avoid or Use Alternate Drug. Comment: Do not take antiretroviral medications for at least 1 month before mobilization or expected duration for elimination of the medications, and until all cycles of apheresis are completed. Antiretroviral medications may interfere with manufacturing of apheresed cells.
- buprenorphine
buprenorphine and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- ceritinib
ceritinib and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- desflurane
desflurane and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- dofetilide
dofetilide increases toxicity of rilpivirine by QTc interval. Avoid or Use Alternate Drug.
- efavirenz
efavirenz and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- elivaldogene autotemcel
elivaldogene autotemcel, rilpivirine. Either decreases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Patients should not take antiretroviral medications for at least 1 month before initiating medications for stem cell mobilization, for the duration of the medications? elimination, and until all cycles of apheresis are completed.
- encorafenib
encorafenib and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- entrectinib
entrectinib and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- eribulin
eribulin and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- fexinidazole
fexinidazole and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels or prolong QT interval.
- hydroxychloroquine sulfate
hydroxychloroquine sulfate and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- isoflurane
isoflurane and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- lefamulin
lefamulin and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- macimorelin
macimorelin and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug. Macimorelin causes an increase of ~11 msec in the corrected QT interval. Avoid coadministration with drugs that prolong QT interval, which could increase risk for developing torsade de pointes-type ventricular tachycardia. Allow sufficient washout time of drugs that are known to prolong the QT interval before administering macimorelin.
- mobocertinib
mobocertinib and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.
- ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC)
ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC) will increase the level or effect of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of Viekira Pak with rilpivirine once daily is not recommended due to potential for QT interval prolongation with higher concentrations of rilpivirine
- oxaliplatin
oxaliplatin and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- ribociclib
ribociclib increases toxicity of rilpivirine by QTc interval. Avoid or Use Alternate Drug.
- rifabutin
rifabutin decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministered, increase rilpivirine dose to 50 mg PO once daily; when rifabutin coadministration is stopped, decrease rilpivirine dose to 25 mg once daily.
- sevoflurane
sevoflurane and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- siponimod
siponimod and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- umeclidinium bromide/vilanterol inhaled
rilpivirine increases toxicity of umeclidinium bromide/vilanterol inhaled by QTc interval. Avoid or Use Alternate Drug. Exercise extreme caution when vilanterol coadministered with drugs that prolong QTc interval; adrenergic agonist effects on the cardiovascular system may be potentiated.
- vilanterol/fluticasone furoate inhaled
rilpivirine increases toxicity of vilanterol/fluticasone furoate inhaled by QTc interval. Avoid or Use Alternate Drug. Exercise extreme caution when vilanterol coadministered with drugs that prolong QTc interval; adrenergic agonist effects on the cardiovascular system may be potentiated.
Monitor Closely (137)
- albuterol
albuterol and rilpivirine both increase QTc interval. Use Caution/Monitor.
- alfuzosin
rilpivirine and alfuzosin both increase QTc interval. Use Caution/Monitor.
alfuzosin and rilpivirine both increase QTc interval. Use Caution/Monitor. - aluminum hydroxide
aluminum hydroxide decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should be given at least 2 hr before or at least 4 hr after rilpivirine. For the combination product dolutegravir/rilpivirine, antacids should be given at least 4 hr before or at least 6 hr afterwards.
- amiodarone
rilpivirine increases toxicity of amiodarone by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- amitriptyline
rilpivirine increases toxicity of amitriptyline by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- amoxapine
rilpivirine increases toxicity of amoxapine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- apomorphine
rilpivirine increases toxicity of apomorphine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- arformoterol
arformoterol and rilpivirine both increase QTc interval. Use Caution/Monitor.
- aripiprazole
aripiprazole and rilpivirine both increase QTc interval. Use Caution/Monitor.
- arsenic trioxide
rilpivirine increases toxicity of arsenic trioxide by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- artemether/lumefantrine
rilpivirine increases toxicity of artemether/lumefantrine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- asenapine
rilpivirine increases toxicity of asenapine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- asenapine transdermal
asenapine transdermal and rilpivirine both increase QTc interval. Use Caution/Monitor.
- aspirin/citric acid/sodium bicarbonate
aspirin/citric acid/sodium bicarbonate decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should be given at least 2 hr before or at least 4 hr after rilpivirine. For the combination product dolutegravir/rilpivirine, antacids should be given at least 4 hr before or at least 6 hr afterwards.
- atazanavir
atazanavir increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Rilpivirine is not expected to affect the plasma concentrations of co-administered protease inhibitors. .
- atomoxetine
atomoxetine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- azithromycin
rilpivirine increases toxicity of azithromycin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- calcium acetate
calcium acetate decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- calcium carbonate
calcium carbonate decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should be given at least 2 hr before or at least 4 hr after rilpivirine. For the combination product dolutegravir/rilpivirine, antacids should be given at least 4 hr before or at least 6 hr afterwards.
- calcium chloride
calcium chloride decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- calcium citrate
calcium citrate decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- calcium gluconate
calcium gluconate decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- calcium/vitamin D
calcium/vitamin D decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- chlorpromazine
rilpivirine increases toxicity of chlorpromazine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- cimetidine
cimetidine will decrease the level or effect of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Concurrent use, may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels. Administer H2 antagonists at least 12 hours before or at least 4 hours after rilpivirine.
- ciprofloxacin
rilpivirine increases toxicity of ciprofloxacin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- citalopram
rilpivirine increases toxicity of citalopram by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- clarithromycin
clarithromycin increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Where possible, alternatives such as azithromycin should be considered.
rilpivirine increases toxicity of clarithromycin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes. - clomipramine
rilpivirine increases toxicity of clomipramine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- clozapine
clozapine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- conivaptan
conivaptan increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- crizotinib
crizotinib increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Dose reduction may be needed for coadministered drugs that are predominantly metabolized by CYP3A.
- cyclobenzaprine
rilpivirine increases toxicity of cyclobenzaprine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- dasatinib
rilpivirine increases toxicity of dasatinib by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- degarelix
rilpivirine increases toxicity of degarelix by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- desipramine
rilpivirine increases toxicity of desipramine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- deutetrabenazine
deutetrabenazine and rilpivirine both increase QTc interval. Use Caution/Monitor. At the maximum recommended dose, deutetrabenazine does not prolong QT interval to a clinically relevant extent. Certain circumstances may increase risk of torsade de pointes and/or sudden death in association with drugs that prolong the QTc interval (eg, bradycardia, hypokalemia or hypomagnesemia, coadministration with other drugs that prolong QTc interval, presence of congenital QT prolongation).
- didanosine
didanosine, rilpivirine. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Applies to didanosine chewable tablets and powder for oral solution; administer 2 hr before or several hours after didanosine oral solution or chewable tablet administration; no dose adjustment is required when rilpivirine is coadministered with didanosine. Didanosine is to be administered on an empty stomach and at least two hours before or at least four hours after rilpivirine (which should be administered with a meal).
- disopyramide
rilpivirine increases toxicity of disopyramide by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- dofetilide
rilpivirine increases toxicity of dofetilide by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- dolasetron
rilpivirine increases toxicity of dolasetron by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- donepezil
donepezil and rilpivirine both increase QTc interval. Use Caution/Monitor.
- doxepin
doxepin and rilpivirine both increase QTc interval. Use Caution/Monitor.
- dronedarone
rilpivirine increases toxicity of dronedarone by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- droperidol
rilpivirine increases toxicity of droperidol by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- eliglustat
eliglustat and rilpivirine both increase QTc interval. Use Caution/Monitor.
- erythromycin base
erythromycin base increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Where possible, alternatives such as azithromycin should be considered.
rilpivirine increases toxicity of erythromycin base by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes. - erythromycin ethylsuccinate
erythromycin ethylsuccinate increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Where possible, alternatives such as azithromycin should be considered.
rilpivirine increases toxicity of erythromycin ethylsuccinate by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes. - erythromycin lactobionate
erythromycin lactobionate increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Where possible, alternatives such as azithromycin should be considered.
rilpivirine increases toxicity of erythromycin lactobionate by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes. - erythromycin stearate
erythromycin stearate increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Where possible, alternatives such as azithromycin should be considered.
rilpivirine increases toxicity of erythromycin stearate by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes. - escitalopram
rilpivirine increases toxicity of escitalopram by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
escitalopram increases toxicity of rilpivirine by QTc interval. Use Caution/Monitor. - famotidine
famotidine will decrease the level or effect of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Concurrent use, may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels. Administer H2 antagonists at least 12 hours before or at least 4 hours after rilpivirine.
- fingolimod
fingolimod and rilpivirine both increase QTc interval. Use Caution/Monitor.
- flecainide
rilpivirine increases toxicity of flecainide by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- fluconazole
fluconazole increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No rilpivirine dose adjustment is required. Clinically monitor for breakthrough fungal infections when azole antifungals are co-administered with rilpivirine.
rilpivirine increases toxicity of fluconazole by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes. - fluoxetine
rilpivirine increases toxicity of fluoxetine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- fosamprenavir
fosamprenavir increases effects of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Rilpivirine is not expected to affect the plasma concentrations of co-administered protease inhibitors. .
- foscarnet
rilpivirine increases toxicity of foscarnet by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- fostemsavir
rilpivirine and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.
- gemifloxacin
rilpivirine increases toxicity of gemifloxacin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- gilteritinib
gilteritinib and rilpivirine both increase QTc interval. Use Caution/Monitor.
- granisetron
granisetron and rilpivirine both increase QTc interval. Use Caution/Monitor.
- haloperidol
rilpivirine increases toxicity of haloperidol by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- hydroxyzine
hydroxyzine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- ibuprofen/famotidine
ibuprofen/famotidine, rilpivirine. increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Combination of rilpivirine and H2-receptor antagonists should be used with caution as coadministration may cause significant decreases in rilpivirine plasma concentrations (increase in gastric pH). Administer famotidine at least 12 hours before or at least 4 hours after rilpivirine.
- ibutilide
ibutilide increases toxicity of rilpivirine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
rilpivirine increases toxicity of ibutilide by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes. - iloperidone
rilpivirine increases toxicity of iloperidone by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- indapamide
rilpivirine increases toxicity of indapamide by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- indinavir
indinavir increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- isoniazid
isoniazid increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- isradipine
rilpivirine increases toxicity of isradipine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- itraconazole
itraconazole increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No rilpivirine dose adjustment is required. Clinically monitor for breakthrough fungal infections when azole antifungals are co-administered with rilpivirine.
itraconazole and rilpivirine both increase QTc interval. Use Caution/Monitor. - ketoconazole
ketoconazole increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No rilpivirine dose adjustment is required. Clinically monitor for breakthrough fungal infections when azole antifungals are co-administered with rilpivirine.
- lapatinib
rilpivirine increases toxicity of lapatinib by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- levofloxacin
rilpivirine increases toxicity of levofloxacin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- levoketoconazole
levoketoconazole increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No rilpivirine dose adjustment is required. Clinically monitor for breakthrough fungal infections when azole antifungals are co-administered with rilpivirine.
- lithium
lithium and rilpivirine both increase QTc interval. Use Caution/Monitor.
- lopinavir
lopinavir increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No dose adjustment is required during concurrent use.
rilpivirine increases toxicity of lopinavir by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes. - lumefantrine
rilpivirine increases toxicity of lumefantrine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- magnesium chloride
magnesium chloride decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- magnesium gluconate
magnesium gluconate decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- magnesium oxide
magnesium oxide decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should be given at least 2 hr before or at least 4 hr after rilpivirine. For the combination product dolutegravir/rilpivirine, antacids should be given at least 4 hr before or at least 6 hr afterwards.
- magnesium sulfate
magnesium sulfate decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- maprotiline
rilpivirine increases toxicity of maprotiline by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- mefloquine
rilpivirine increases toxicity of mefloquine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- methadone
rilpivirine, methadone. Other (see comment). Use Caution/Monitor. Comment: No dose adjustments are required when initiating co-administration of methadone with rilpivirine. However, clinical monitoring is recommended as methadone maintenance therapy may need to be adjusted in some patients.
rilpivirine increases toxicity of methadone by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes. - mirtazapine
mirtazapine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- moxifloxacin
moxifloxacin increases toxicity of rilpivirine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
rilpivirine increases toxicity of moxifloxacin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes. - nefazodone
nefazodone increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nelfinavir
nelfinavir increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nilotinib
rilpivirine increases toxicity of nilotinib by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- nizatidine
nizatidine will decrease the level or effect of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Concurrent use, may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels. Administer H2 antagonists at least 12 hours before or at least 4 hours after rilpivirine.
- nortriptyline
rilpivirine increases toxicity of nortriptyline by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- octreotide
rilpivirine increases toxicity of octreotide by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- ofloxacin
rilpivirine increases toxicity of ofloxacin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- olanzapine
olanzapine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- orlistat
orlistat will decrease the level or effect of rilpivirine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Loss of virological control reported in HIV-infected patients taking orlistat concomitantly. Exact mechanism is unclear, but may include a drug-drug interaction that inhibits systemic absorption of the antiretroviral drug. Monitor HIV RNA levels frequently and if increased HIV viral load confirmed, discontinue orlistat.
- osilodrostat
osilodrostat and rilpivirine both increase QTc interval. Use Caution/Monitor.
- ozanimod
ozanimod and rilpivirine both increase QTc interval. Modify Therapy/Monitor Closely. The potential additive effects on heart rate, treatment with ozanimod should generally not be initiated in patients who are concurrently treated with QT prolonging drugs with known arrhythmogenic properties.
- paliperidone
rilpivirine increases toxicity of paliperidone by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- pazopanib
rilpivirine increases toxicity of pazopanib by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- pentamidine
rilpivirine increases toxicity of pentamidine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- pimozide
rilpivirine increases toxicity of pimozide by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- posaconazole
posaconazole increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No rilpivirine dose adjustment is required. Clinically monitor for breakthrough fungal infections when azole antifungals are co-administered with rilpivirine.
rilpivirine increases toxicity of posaconazole by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes. - potassium chloride
potassium chloride decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- primaquine
primaquine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- procainamide
rilpivirine increases toxicity of procainamide by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- propafenone
rilpivirine increases toxicity of propafenone by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- protriptyline
rilpivirine increases toxicity of protriptyline by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- quetiapine
rilpivirine increases toxicity of quetiapine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- quinidine
rilpivirine increases toxicity of quinidine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- quinine
rilpivirine increases toxicity of quinine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- ranolazine
rilpivirine increases toxicity of ranolazine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- risperidone
rilpivirine increases toxicity of risperidone by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- ritonavir
ritonavir increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No dose adjustment is required during concurrent use.
rilpivirine increases toxicity of ritonavir by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes. - romidepsin
rilpivirine increases toxicity of romidepsin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- saquinavir
saquinavir increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Rilpivirine is not expected to affect the plasma concentrations of co-administered protease inhibitors. .
rilpivirine increases toxicity of saquinavir by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes. - selpercatinib
selpercatinib increases toxicity of rilpivirine by QTc interval. Use Caution/Monitor.
- sertraline
sertraline and rilpivirine both increase QTc interval. Use Caution/Monitor.
- sodium zirconium cyclosilicate
sodium zirconium cyclosilicate will decrease the level or effect of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Check specific recommendations for drugs that exhibit pH-dependent solubility that may affect their systemic exposure and efficacy. In general, administer drugs at least 2 hr before or after sodium zirconium cyclosilicate.
- solifenacin
solifenacin and rilpivirine both increase QTc interval. Use Caution/Monitor.
- sotalol
rilpivirine increases toxicity of sotalol by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- sunitinib
rilpivirine increases toxicity of sunitinib by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- tacrolimus
rilpivirine increases toxicity of tacrolimus by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- telavancin
rilpivirine increases toxicity of telavancin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- thioridazine
rilpivirine increases toxicity of thioridazine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- thiothixene
rilpivirine increases toxicity of thiothixene by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- tipranavir
tipranavir increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Rilpivirine is not expected to affect the plasma concentrations of co-administered protease inhibitors. .
- toremifene
rilpivirine increases toxicity of toremifene by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- trimagnesium citrate anhydrous
trimagnesium citrate anhydrous decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- trimipramine
rilpivirine increases toxicity of trimipramine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- valbenazine
valbenazine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- vandetanib
rilpivirine increases toxicity of vandetanib by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- voclosporin
voclosporin, rilpivirine. Either increases effects of the other by QTc interval. Use Caution/Monitor.
- voriconazole
voriconazole increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No rilpivirine dose adjustment is required. Clinically monitor for breakthrough fungal infections when azole antifungals are co-administered with rilpivirine.
rilpivirine increases toxicity of voriconazole by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes. - vorinostat
rilpivirine increases toxicity of vorinostat by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- ziprasidone
rilpivirine increases toxicity of ziprasidone by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
Minor (2)
- chloroquine
chloroquine increases toxicity of rilpivirine by QTc interval. Minor/Significance Unknown.
- crizotinib
crizotinib and rilpivirine both increase QTc interval. Minor/Significance Unknown.
Adverse Effects
1-10%
Depressive disorders (4%)
Insomnia (3%)
Headache (3%)
Rash (3%)
Increased AST (2%; grade 3 or higher)
ALT increased (19%)
Abnormal dreams (1%)
Nausea (1%)
Suicidal ideation (4-8%)
Abdominal pain (1%)
Vomiting (1%)
Fatigue (1%)
Dizziness (1%)
Posmarketing reports
Severe skin and hypersensitivity reactions including DRESS (Drug Reaction with Eosinophilia and Systemic Symptoms)
Warnings
Contraindications
Hypersensitivity
Coadministration with drugs (eg, CYP inducers like phenobarbital, dexamethasone, oxcarbazepine, phenytoin, or carbamazepine) where significant decreases in rilpivirine plasma concentrations may occur, which may result in loss of virologic response and possible resistance and cross-resistance to other NNRTIs
Contraindicated with drugs that increase gastric pH (eg, esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole) that may decrease rilpivirine absorption and result in decreased rilpivirine plasma concentrations
Cautions
Coadministration with other NNRTIs may either increase or decrease rilpivirine; avoid use with other NNRTIs
May increase risk for depressive disorders
Hepatic adverse effects reported; patients with underlying hepatitis B or C, or marked increased transaminases prior to treatment may be at increased risk; monitor for hepatotoxicity before initiating and during treatment
Redistribution/accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and “cushingoid appearance” have been observed in patients receiving antiretroviral therapy
Immune reconstitution syndrome: During initial phase of combination ART treatment, patients whose immune system responds may develop an inflammatory response to indolent or residual opportunistic infections (eg, Mycobacterium avium complex, CMV, Pneumocystis pneumonia, TB)
Severe skin and hypersensitivity reactions reported, including cases of drug reaction with eosinophilia and systemic symptoms (DRESS), with rilpivirine-containing regimens; immediately discontinue treatment if hypersensitivity or rash with systemic symptoms or elevations in hepatic serum biochemistries develop and closely monitor clinical status, including hepatic serum biochemistries
Virologic failure & resistance
- More rilpivirine treated individuals with HIV-1 RNA >100,000 copies/mL at the start of therapy experienced virologic failure compared to those with <100,000 copies/mL
- Observed virologic failure rate in rilpivirine treated individuals conferred a higher rate of overall treatment resistance and cross-resistance to the NNRTI class compared to efavirenz
- More individuals treated with rilpivirine developed lamivudine/emtricitabine associated resistance compared to efavirenz
Drug interaction overview
- Drugs that induce or inhibit CYP3A may affect clearance of rilpivirine
- Coadministration with CYP3A4 inducers may decrease plasma concentrations of rilpivirine and result in loss of virologic response and possible resistance to rilpivirine OR to non-nucleoside reverse transcriptase inhibitors (NNRTIs)
- Coadministration with CYP3A4 inhibitors may increase plasma concentrations of rilpivirine
- Coadministration with drugs that increase gastric pH may decrease plasma concentrations of rilpivirine and result in loss of virologic response and possible resistance to rilpivirine or to NNRTIs
- In healthy subjects, rilpivirine 75 mg PO qDay (3 times rilpivirine dose) and 300 mg PO qDay (12 times rilpivirine dose) have been shown to prolong the QTc interval; consider alternatives when coadministered with a drug with a known risk of torsade de pointes
Pregnancy & Lactation
Pregnancy
Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) 1-800-258-4263
Available data from the APR show no difference in the overall risk of birth defects for rilpivirine compared with the background rate for major birth defects of 2.7% in the Metropolitan Atlanta Congenital Defects Program (MACDP) reference population
Based on experience of HIV-1-infected pregnant women who completed a clinical trial through postpartum period with a rilpivirine-based regimen, no dose adjustments are required for pregnant patients who are already on a stable dose regimen prior to pregnancy and who are virologically suppressed (HIV-1 RNA less than 50 copies per mL); the recommended dosage is one 25 mg tablet once daily taken orally with a meal; lower exposures of drug were observed during pregnancy, therefore viral load should be monitored closely
Animal data
- In animal reproduction studies, no adverse developmental outcomes were observed when drug was administered orally at exposures up to 15 (rats) and 70 (rabbits) times exposure in humans at recommended dose of 25 mg once daily
Lactation
Unknown whether distributed in human breast milk; there are no data on presence of drug in human milk, effects on breastfed infant, or on milk production; drug is present in rat milk
The CDC recommends that women in the United States should not breastfeed their infants because of risk of the following
- Postnatal HIV transmission (in HIV-negative infants)
- Developing viral resistance (in HIV-positive infants)
- Adverse reactions in nursing infants
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Antiviral agent; diarylpyrimidine non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1
Inhibits HIV-1 replication by noncompetitive inhibition of HIV-1 reverse transcriptase
Does not inhibit the human cellular DNA polymerases alpha, beta, and gamma
Absorption
Bioavailability: Absolute bioavailability unknown
Peak Plasma Time: 4-5 hr
Peak Plasma Concentration: 80 ng/mL (mean)
AUC: 2397 ng•h/mL (mean)
Food: Exposure ~40% lower when taken in a fasted condition as compared to a normal caloric meal (533 kcal) or high-fat high-caloric meal (928 kcal); when taken with only a protein-rich nutritional drink, exposures were 50% lower than when taken with a meal
Distribution
Protein Bound: 99.7% (primarily to albumin)
Metabolism
Metabolized primarily by CYP3A
Elimination
Half-life: 50 hr
Excretion: feces (85%), urine (6.1%) bile, other
Administration
Oral Administration
Must administer with a meal
Must be able to take with a meal of at least 500 calories on a regular schedule (a protein drink alone does not constitute a meal)
If coadministered with antacids should only be administered either at least 2 hr before or at least 4 hr after rilpivirine
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Edurant oral - | 25 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
rilpivirine HCl oral
RILPIVIRINE - ORAL
(RIL-pi-VIR-een)
COMMON BRAND NAME(S): Edurant
USES: Rilpivirine is used with other HIV medications to help control HIV infection. It helps to decrease the amount of HIV in your body so your immune system can work better. This lowers your chance of getting HIV complications (such as new infections, cancer) and improves your quality of life. This medication is usually prescribed to people who have not taken any HIV medications before. Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). It blocks the virus from growing and infecting more cells.Rilpivirine is not a cure for HIV infection. To decrease your risk of spreading HIV disease to others, continue to take all HIV medications exactly as prescribed by your doctor. Use an effective barrier method (latex or polyurethane condoms/dental dams) during sexual activity as directed by your doctor. Do not share personal items (such as needles/syringes, toothbrushes, and razors) that may have contacted blood or other body fluids. Consult your doctor or pharmacist for more details.
HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start using rilpivirine and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with a meal as directed by your doctor, usually once daily. The dosage may be based on other medications you are taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Medications which reduce or block stomach acid (such as proton pump inhibitors/PPIs, H2 blockers, antacids) may reduce the absorption of rilpivirine, making it work less well. Do not take PPIs (such as omeprazole, lansoprazole) while using this medication. If you take antacids, take the antacids at least 2 hours before or at least 4 hours after rilpivirine. If you take H2 blockers (such as famotidine, ranitidine), take them at least 12 hours before or at least 4 hours after rilpivirine.It is very important to continue taking this medication (and other HIV medications) exactly as prescribed by your doctor. Do not take less of this drug than prescribed or stop taking it (or other HIV medicines) even for a short time unless directed to do so by your doctor. Doing so may cause the amount of virus to increase and/or make the infection more difficult to treat (resistant).Do not increase your dose or take this medication more often than prescribed. Your condition will not improve any faster, and the risk of serious side effects may increase.For the best effect, take this medication at evenly spaced times. To help you remember, take this medication at the same time every day.
SIDE EFFECTS: Headache or trouble sleeping may occur. If either of these effects lasts or gets worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.As your immune system gets stronger, it can begin to fight off infections you already had, possibly causing disease symptoms to come back. You could also have symptoms if your immune system becomes overactive. This reaction may happen at any time (soon after starting HIV treatment or many months later). Get medical help right away if you have any serious symptoms, including: unexplained weight loss, severe tiredness, muscle aches/weakness that doesn't go away, headaches that are severe or don't go away, joint pain, numbness/tingling of the hands/feet/arms/legs, vision changes, signs of infection (such as fever, chills, swollen lymph nodes, trouble breathing, cough, non-healing skin sores), signs of an overactive thyroid (such as irritability, nervousness, heat intolerance, fast/pounding/irregular heartbeat, bulging eyes, unusual growth in the neck/thyroid known as a goiter), signs of a certain nerve problem known as Guillain-Barre syndrome (such as unsteadiness, loss of coordination, trouble swallowing/speaking/chewing, trouble moving your eyes), signs of liver disease (such as nausea/vomiting that doesn't stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine).Tell your doctor right away if you have any serious side effects, including: mental/mood changes (such as depression, thoughts of suicide).Changes in body fat may occur while you are taking this medication (for example, increased fat in the upper back and stomach areas, decreased fat in the arms and legs). The cause and long-term effects of these changes are unknown. Discuss the risks and benefits of treatment with your doctor, as well as the possible use of exercise to reduce this side effect.Rilpivirine can commonly cause a rash that is usually not serious. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe reaction. Get medical help right away if you develop any rash.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking rilpivirine, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease, liver disease (such as hepatitis B, hepatitis C), mental/mood disorders (such as depression).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Tell your doctor if you are pregnant before using this medication. Treatment can lower the risk of passing HIV infection to your baby. Discuss the risks and benefits with your doctor.It is unknown if this medication passes into breast milk. Because breast milk can transmit HIV, do not breast-feed.
DRUG INTERACTIONS: See also How to Use section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: orlistat, other HIV NNRTIs (such as efavirenz, nevirapine), a certain combination HIV medication (elvitegravir/cobicistat/emtricitabine/tenofovir), proton pump inhibitors (PPIs such as esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole).Other medications can affect the removal of rilpivirine from your body, which may affect how rilpivirine works. Examples include dexamethasone, macrolide antibiotics (such as erythromycin), rifamycins (such as rifampin, rifapentine), St. John's wort, certain drugs used to treat seizures (such as carbamazepine, oxcarbazepine, phenobarbital, phenytoin, primidone), a certain combination product used to treat chronic hepatitis C (ombitasvir/paritaprevir/ritonavir/dasabuvir), among others.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: fast/irregular heartbeat, severe dizziness, fainting.
NOTES: Do not share this medication with others.Laboratory and/or medical tests (such as viral load, T-cell counts, liver function tests) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.Keep all medical and laboratory appointments.
MISSED DOSE: If you miss a dose and it is within 12 hours of the time you usually take the dose, take it with a meal as soon as you remember. If it is more than 12 hours from the time you usually take the dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Store this drug in its original bottle. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised September 2022. Copyright(c) 2022 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
