Dosing & Uses
Dosage Forms & Strengths
emtricitabine/rilpivirine/tenofovir AF
tablet
- 200mg/25mg/25mg
HIV Infection
Indicated as a complete regimen for treatment of HIV-1 infection in treatment-naïve adults with HIV-1 RNA ≤100,000 copies/mL, and in certain virologically suppressed (HIV-1 RNA <50 copies/mL) patients on a stable antiretroviral therapy (ART) regimen at start of therapy in order to replace their current ART regimen
1 tablet (emtricitabine 200 mg/rilpivirine 25 mg/tenofovir 25 mg) PO qDay with food
Dosage Modifications
Coadministration with rifabutin
- Add 1 tablet of rilpivirine 25 mg with Odefsey for the duration of rifabutin coadministration
Renal impairment
- Mild-to-moderate (eCrCl ≥30 mL/min): No dosage adjustment necessary
- Severe (CrCl 15 to <30 mL/min): Not recommended
-
CrCl ≤15 mL/min
- Receiving chronic hemodialysis: On days of hemodialysis, administer daily dose after hemodialysis completion
- Not receiving chronic hemodialysis: Not recommended
Hepatic impairment
- Mild-to-moderate (Child-Pugh A or B): No dosage adjustment required
- Severe (Child-Pugh C): Not recommended; data are insufficient in this population
Dosing Considerations
Prior to initiation and during treatment
- Test for hepatitis B virus (HBV) infection
- Assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein in all patients
- Assess serum phosphorus in chronic kidney disease patients
Limitation of use
- Rilpivirine-treated patients who had >100,000 copies/mL HIV-1 RNA at the start of therapy experienced more virologic failure (HIV-1 RNA ≥50 copies/mL) compared with rilpivirine-treated patients with ≤100,000 copies/mL
Dosage Forms & Strengths
emtricitabine/rilpivirine/tenofovir AF
tablet
- 200mg/25mg/25mg
HIV Infection
Indicated as a complete regimen for treatment of HIV-1 infection in treatment-naïve adults and adolescents (≥12 yr) who weigh ≥35 kg and in certain virologically suppressed (HIV-1 RNA <50 copies/mL) patients on a stable ART regimen at start of therapy in order to replace their current ART regimen
<12 years or <35 kg: Safety and efficacy not established
≥12 years and weight ≥35 kg: 1 tablet (emtricitabine 200 mg/rilpivirine 25 mg/tenofovir 25 mg) PO qDay with food
Dosage Modifications
Coadministration with rifabutin
- Add 1 tablet of rilpivirine 25 mg with Odefsey for the duration of rifabutin coadministration
Renal impairment
- Mild-to-moderate (eCrCl ≥30 mL/min): No dosage adjustment necessary
- Severe (CrCl 15 to <30 mL/min): Not recommended
-
CrCl ≤15 mL/min
- Receiving chronic hemodialysis: On days of hemodialysis, administer daily dose after hemodialysis completion
- Not receiving chronic hemodialysis: Not recommended
Hepatic impairment
- Mild-to-moderate (Child-Pugh A or B): No dosage adjustment required
- Severe (Child-Pugh C): Not recommended; data are insufficient in this population
Dosing Considerations
Prior to initiation and during treatment
- Test for hepatitis B virus (HBV) infection
- Assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein in all patients
- Assess serum phosphorus in chronic kidney disease patients
Limitation of use
- Rilpivirine-treated patients who had >100,000 copies/mL HIV-1 RNA at the start of therapy experienced more virologic failure (HIV-1 RNA ≥50 copies/mL) compared with rilpivirine-treated patients with ≤100,000 copies/mL
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (8)
- 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
emtricitabine, 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.
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.
- fezolinetant
tenofovir AF will increase the level or effect of fezolinetant by affecting hepatic enzyme CYP1A2 metabolism. Contraindicated. Fezolinetant AUC and peak plasma concentration are increased if coadministered with drugs that are weak, moderate, or strong CYP1A2 inhibitors
- lamivudine
emtricitabine and lamivudine both increase risk of immune reconstitution syndrome. Contraindicated. Coadministration of emtricitabine containing products and lamivudine containing products should be avoided. Combination will result in therapeutic duplication.
emtricitabine, lamivudine. Other (see comment). Contraindicated. Comment: Coadministration of emtricitabine containing products and lamivudine containing products should be avoided. Combination will result in therapeutic duplication.
Serious - Use Alternative (37)
- adagrasib
adagrasib, rilpivirine. Either increases effects of the other by QTc interval. Avoid or Use Alternate Drug. Each drug prolongs the QTc interval, which may increased the risk of Torsade de pointes, other serious arryhthmias, and sudden death. If coadministration unavoidable, more frequent monitoring is recommended for such patients.
- 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
emtricitabine, 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.
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.
- cabotegravir
emtricitabine, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.
- buprenorphine buccal
buprenorphine buccal and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine subdermal implant
buprenorphine subdermal implant and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine transdermal
buprenorphine transdermal and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine, long-acting injection
buprenorphine, long-acting injection 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, emtricitabine. 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.
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.
- leniolisib
leniolisib will increase the level or effect of tenofovir AF by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- letermovir
tenofovir AF will decrease the level or effect of letermovir by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Coadministration of letermovir with P-gp inducers is not recommended.
- 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.
- sotorasib
sotorasib will decrease the level or effect of tenofovir AF by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If use is unavoidable, refer to the prescribing information of the P-gp substrate for dosage modifications.
- tepotinib
tepotinib will increase the level or effect of tenofovir AF by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If concomitant use unavoidable, reduce the P-gp substrate dosage if recommended in its approved product labeling.
- tetrabenazine
tetrabenazine and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
Monitor Closely (196)
- abacavir
abacavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- acalabrutinib
acalabrutinib increases levels of tenofovir AF by Other (see comment). Use Caution/Monitor. Comment: Acalabrutinib may increase exposure to coadministered BCRP substrates by inhibition of intestinal BCRP.
- acyclovir
acyclovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.
- adefovir
adefovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.
- 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.
- apalutamide
apalutamide will decrease the level or effect of tenofovir AF by increasing elimination. Use Caution/Monitor. Apalutamide weakly induces BCRP and may decrease systemic exposure of drugs that are BCRP substrates.
- 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. .
atazanavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor. - atomoxetine
atomoxetine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- berotralstat
berotralstat will increase the level or effect of tenofovir AF by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor or titrate P-gp substrate dose if coadministered.
- cabozantinib
tenofovir AF will increase the level or effect of cabozantinib by Other (see comment). Use Caution/Monitor. MRP2 inhibitors increase cabozantinib toxicity
- celecoxib
emtricitabine, celecoxib. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- 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.
- cidofovir
cidofovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.
- 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.
- darolutamide
darolutamide will increase the level or effect of tenofovir AF by Other (see comment). Modify Therapy/Monitor Closely. Darolutamide is a BCRP inhibitor. Avoid coadministration with BCRP inhibitors. If use is unavoidable, closely monitor for adverse reactions and consider dose reduction of BCRP substrate drug (refer BCRP substrate prescribing information).
- 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).
- diclofenac
emtricitabine, diclofenac. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- 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).
- diflunisal
emtricitabine, diflunisal. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- 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.
- duvelisib
tenofovir AF will decrease the level or effect of duvelisib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- efavirenz
efavirenz and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- elagolix
elagolix will increase the level or effect of tenofovir AF by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- eliglustat
eliglustat and rilpivirine both increase QTc interval. Use Caution/Monitor.
- encorafenib
encorafenib will increase the level or effect of tenofovir AF by Other (see comment). Modify Therapy/Monitor Closely. Encorafenib (a BCRP inhibitor) may increase the concentration and toxicities of BCRP substrates. Closely monitor for signs and symptoms of increased exposure and consider adjusting the dose of these substrates.
- enfuvirtide
emtricitabine and enfuvirtide both increase risk of immune reconstitution syndrome. 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. - etodolac
emtricitabine, etodolac. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- 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.
- fenoprofen
emtricitabine, fenoprofen. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- 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.
- flurbiprofen
emtricitabine, flurbiprofen. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- fosamprenavir
fosamprenavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
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.
- fostamatinib
fostamatinib will increase the level or effect of tenofovir AF by decreasing metabolism. Use Caution/Monitor. Concomitant use of fostamatinib may increase concentrations of BCRP substrate drugs. Monitor for toxicities of BCRP substrate drug that may require dosage reduction when given concurrently with fostamatinib.
- ganciclovir
ganciclovir, emtricitabine. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Use alternatives if available. Increased risk of hematologic toxicity.
ganciclovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine. - 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.
- glecaprevir/pibrentasvir
glecaprevir/pibrentasvir will increase the level or effect of tenofovir AF by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates.
- 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
emtricitabine, ibuprofen. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- ibuprofen IV
emtricitabine, ibuprofen IV. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- 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. - ifosfamide
ifosfamide, tenofovir AF. Either increases toxicity of the other by nephrotoxicity and/or ototoxicity. Modify Therapy/Monitor Closely. Monitor electrolytes and renal function.
- 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 and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
indinavir increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - indomethacin
emtricitabine, indomethacin. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- 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.
- istradefylline
istradefylline will increase the level or effect of tenofovir AF by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of P-gp substrates in clinical trials. Consider dose reduction of sensitive P-gp substrates.
- 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.
- ketoprofen
emtricitabine, ketoprofen. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- ketorolac
emtricitabine, ketorolac. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- 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.
- lonafarnib
lonafarnib will increase the level or effect of tenofovir AF by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Lonafarnib is a weak P-gp inhibitor. Monitor for adverse reactions if coadministered with P-gp substrates where minimal concentration changes may lead to serious or life-threatening toxicities. Reduce P-gp substrate dose if needed.
- 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.
- meclofenamate
emtricitabine, meclofenamate. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- mefenamic acid
emtricitabine, mefenamic acid. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- 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.
- meloxicam
emtricitabine, meloxicam. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- 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. - nabumetone
emtricitabine, nabumetone. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- naproxen
emtricitabine, naproxen. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- 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.
nelfinavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor. - nevirapine
emtricitabine and nevirapine both increase risk of immune reconstitution syndrome. 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.
- nirmatrelvir
nirmatrelvir will increase the level or effect of tenofovir AF by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration may increase tenofovir systemic exposures.
- nirmatrelvir/ritonavir
nirmatrelvir/ritonavir will increase the level or effect of tenofovir AF by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration may increase tenofovir systemic exposures.
- 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 tenofovir AF 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.
orlistat will decrease the level or effect of emtricitabine 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.
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.
- oteseconazole
oteseconazole will increase the level or effect of tenofovir AF by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- oxaprozin
emtricitabine, oxaprozin. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- 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.
- piroxicam
emtricitabine, piroxicam. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- 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.
- regorafenib
regorafenib will increase the level or effect of tenofovir AF by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.
- ribavirin
ribavirin increases toxicity of emtricitabine by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Use alternatives if available. Increased risk of lactic acidosis.
- 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 and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
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.
- safinamide
safinamide will increase the level or effect of tenofovir AF by Other (see comment). Use Caution/Monitor. Safinamide and its major metabolite may inhibit intestinal BCRP. Monitor BCRP substrates for increased pharmacologic or adverse effects.
- saquinavir
saquinavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- 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. - sarecycline
sarecycline will increase the level or effect of tenofovir AF by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor for toxicities of P-gp substrates that may require dosage reduction when coadministered with P-gp inhibitors.
- 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.
- stavudine
emtricitabine and stavudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- stiripentol
stiripentol will increase the level or effect of tenofovir AF by Other (see comment). Use Caution/Monitor. Stiripentol is a BCRP transport inhibitor. Consider dosage reduction for BCRP substrates if adverse effects are experienced when coadministered.
- sulindac
emtricitabine, sulindac. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- 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.
- tafamidis
tafamidis will increase the level or effect of tenofovir AF by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.
- tafamidis meglumine
tafamidis meglumine will increase the level or effect of tenofovir AF by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.
- 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.
- tenofovir DF
emtricitabine and tenofovir DF both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- 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 and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
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. . - tolmetin
emtricitabine, tolmetin. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.
- 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.
- tucatinib
tucatinib will increase the level or effect of tenofovir AF by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Consider reducing the dosage of P-gp substrates, where minimal concentration changes may lead to serious or life-threatening toxicities.
- ublituximab
ublituximab decreases effects of rilpivirine by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely.
ublituximab decreases effects of emtricitabine by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. - valacyclovir
valacyclovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.
- valbenazine
valbenazine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- valganciclovir
valganciclovir, emtricitabine. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Use alternatives if available. Increased risk of hematologic toxicity.
valganciclovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine. - 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, tenofovir AF. Either increases toxicity of the other by nephrotoxicity and/or ototoxicity. Modify Therapy/Monitor Closely. Coadministration with drugs associated with nephrotoxicity may increase the risk for acute and/or chronic nephrotoxicity.
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.
- zidovudine
emtricitabine and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.
- 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 (3)
- chloroquine
chloroquine increases toxicity of rilpivirine by QTc interval. Minor/Significance Unknown.
- crizotinib
crizotinib and rilpivirine both increase QTc interval. Minor/Significance Unknown.
- nirmatrelvir/ritonavir
nirmatrelvir/ritonavir will increase the level or effect of emtricitabine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
Adverse Effects
>10%
Headache (rilpivirine) (19%)
Depression (rilpivirine) (19%)
Somnolence (rilpivirine) (14%)
Nausea (rilpivirine) (11%)
1-10%
Nausea (10%)
Mild/moderate depression (rilpivirine) (9%)
Dizziness (rilpivirine) (8%)
Abdominal pain (rilpivirine) (8%)
Vomiting (rilpivirine) (6%)
Rash (rilpivirine) (6%)
Headache (2%)
Sleep disturbances (2%)
Severe depression (rilpivirine) (1%)
Flatulence (1%)
Abnormal dreams (1%)
Diarrhea (1%)
Frequency Not Defined
Lactic acidosis
Exacerbation of hepatitis B in coinfected patients
Postmarketing Reports
Rilpivirine
- Metabolism and nutrition disorders: Weight increased
- Skin and subcutaneous tissue disorders: Severe skin and hypersensitivity reactions including DRESS (Drug Reaction with Eosinophilia and Systemic Symptoms)
- Renal and urinary disorders: Nephrotic syndrome
Tenofovir alafenamide
- Skin and subcutaneous tissue disorders: Angioedema, urticaria, and rash
- Acute renal failure, acute tubular necrosis, proximal renal tubulopathy, and Fanconi syndrome
Warnings
Black Box Warnings
Post treatment acute exacerbation of hepatitis B
- Severe acute exacerbations of hepatitis B reported with coinfection of HBV and HIV-1 and have discontinued emtricitabine (FTC) or tenofovir, which are components of Complera
- Closely monitor hepatic function with both clinical and laboratory follow-up for at least several months after discontinuing treatment in patients who are coinfected with HIV-1 and HBV; if appropriate, initiation of antihepatitis B therapy may be warranted
Contraindications
Coadministration of the following drugs
- Anticonvulsants (eg, carbamazepine, oxcarbazepine, phenobarbital, phenytoin)
- Antimycobacterials (eg, rifabutin, rifampin, rifapentine)
- Glucocorticoid systemic dexamethasone (more than a single dose)
- St. John’s wort
- Proton pump inhibitors (eg, esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole)
Cautions
Severe acute exacerbation of hepatitis B in patients coinfection with HIV-1 and HBV (see Black Box Warnings)
Severe skin and hypersensitivity reactions reported, including cases of drug reaction with eosinophilia and systemic symptoms (DRESS) with rilpivirine (RPV)-containing regimens; discontinue therapy immediately if signs or symptoms of severe skin or hypersensitivity reactions develop, including but not limited to, severe rash or rash accompanied by fever, blisters, mucosal involvement, conjunctivitis, facial edema, angioedema, hepatitis, or eosinophilia; monitor and initiate appropriate therapy
Depressive disorders (including depressed mood, depression, dysphoria, major depression, mood altered, negative thoughts, suicide attempt, suicidal ideation) reported with rilpivirine; promptly evaluate patients with severe depressive symptoms to assess whether symptoms are related to therapy, and to determine whether risks of continued therapy outweigh benefits
Fat redistribution and accumulation observed with ART therapy
Decreases in bone mineral density (BMD) and cases of osteomalacia associated with proximal renal tubulopathy reported with tenofovir; consider monitoring BMD with a history of pathologic fracture or if risk factors for bone loss exist
Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases reported; suspend treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity (which may include hepatomegaly and steatosis even in the absence of marked transaminase elevations)
Immune reconstitution syndrome
- Immune reconstitution syndrome reported in patients treated with combination antiretroviral therapy; during initial phase of combination antiretroviral treatment, patients whose immune system responds may develop inflammatory response to indolent or residual opportunistic infections, including Mycobacterium avium infection, cytomegalovirus, Pneumocystis jirovecii pneumonia (PCP), or tuberculosis, which may necessitate further evaluation and treatment
- Autoimmune disorders, including Graves’ disease, polymyositis, Guillain-Barré syndrome, and autoimmune hepatitis, have been reported to occur in the setting of immune reconstitution, however, the time to onset is more variable and can occur many months after initiation of treatment
Hepatotoxicity
- Hepatic adverse events reported in patients receiving an RPV-containing regimen; patients with underlying hepatitis B or C virus infection, or marked elevations in liver-associated tests prior to treatment, may be at increased risk for worsening or development of liver-associated test elevations
- A few cases of hepatic toxicity reported in adult patients receiving an RPV-containing regimen who had no preexisting hepatic disease or other identifiable risk factors
- Appropriate laboratory testing prior to initiating therapy and monitoring for hepatotoxicity during therapy is recommended in patients with underlying hepatic disease, such as, hepatitis B or C, or in patients with marked elevations in liver-associated tests prior to treatment initiation
- Liver-associated test monitoring should be considered for patients without preexisting hepatic dysfunction or other risk factors
New onset or worsening renal impairment
- Postmarketing cases of renal impairment, including acute renal failure, proximal renal tubulopathy (PRT), and Fanconi syndrome reported with TAF-containing products; while most of these cases were characterized by potential confounders that may have contributed to reported renal events, it is also possible these factors may have predisposed patients to tenofovir-related adverse
- Therapy is not recommended in patients with estimated creatinine clearance of 15 to <30 mL/min, or patients with estimated creatinine clearance <15 mL/min who are not receiving chronic hemodialysis
- Patients taking tenofovir prodrugs who have impaired renal function and those taking nephrotoxic agents, including nonsteroidal anti-inflammatory drugs are at increased risk of developing renal-related adverse reactions
- Prior to or when initiating therapy, and during treatment on a clinically appropriate schedule, assess serum creatinine, estimated creatinine clearance, urine glucose and urine protein in all patients
- In patients with chronic kidney disease, also assess serum phosphorus; discontinue therapy in patients who develop clinically significant decreases in renal function or evidence of Fanconi syndrome
Drug interactions overview
- Coadministration with P-gp/BCRP inhibitors may increase absorption and plasma concentration of tenofovir AF; P-gp inducwea may decrease ]absorption of TAF, resulting in decreased plasma concentration of TAF, which may lead to loss of therapeutic effect of Odefsey and development of resistance
- Coadministration with drugs that reduce renal function or compete for active tubular secretion may increase concentrations of FTC, tenofovir, and other renally eliminated drugs
-
Rilpivirine
- Rilpivirine is a CYP3A4 substrate
- Coadministration with CYP3A inducers may decrease plasma levels of RPV and loss of virologic response and possible resistance to RPV or to the class of NNRTIs
- Coadministration with CYP3A inhibitor may increase plasma levels of RPV
- Supratherapeutic rilpivirine doses (ie, 75 mg and 300 mg qDay) shown to prolong the QTc interval; caution when coadministered with a drug known to increase risk of torsade de pointes
- Rilpivirine use with proton pump inhibitors is contraindicated and use of RPV with H2-receptor antagonists requires staggered administration (see Contraindications)
Pregnancy
Pregnancy
Pregnancy exposure registry monitors pregnancy outcomes in individuals exposed to treatment during pregnancy
Register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263
Available data from the APR show no statistically significant difference in the overall risk of major birth defects for emtricitabine (FTC), rilpivirine (RPV) or tenofovir alafenamide (TAF) compared with the background rate for major birth defects of 2.7% in a US reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP); the rate of miscarriage is not reported in the APR
TAF use in women during pregnancy has not been evaluated; emtricitabine (FTC) and rilpivirine (RPV) use during pregnancy has been evaluated in a limited number of women reported to the APR
Available data show no difference in the risk of overall major birth defects for FTC (2.4%) compared with the background rate for major birth defects of 2.7%
Based on HIV-1-infected pregnant individuals who completed a clinical trial through postpartum period with an RPV-based regimen, no dose adjustments are required for pregnant patients who are already on a stable RPV-containing regimen prior to pregnancy and who are virologically suppressed (HIV-1 RNA <50 copies per mL)
Closely monitor viral load; lower exposures of RPV were observed during pregnancy
Lactation
The Centers for Disease Control and Prevention recommend that HIV-infected mothers not breastfeed their infants, to avoid risking postnatal transmission of HIV
Based on published data, FTC has shown to be present in human breast milk;
Unknown if RPV and TAF are present in human breast milk; RPV is present in rat milk and tenofovir has been shown to be present in the milk of lactating rats and rhesus monkeys after administration
Because of the potential for: HIV transmission (in HIV-negative infants); developing viral resistance (in HIV-positive infants); and adverse reactions in a breastfed infant similar to those seen in adults, instruct mothers not to breastfeed
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
Emtricitabine: Nucleoside reverse transcriptase inhibitor (NRTI); following phosphorylation, interferes with HIV viral DNA polymerase and inhibits viral replication; cytosine analogue
Rilpivirine: Antiviral agent; diarylpyrimidine non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1; inhibits HIV-1 replication by noncompetitive inhibition of HIV-1 reverse transcriptase
Tenofovir AF: An NRTI and prodrug of tenofovir; inhibits HIV-1 RT by competing with the natural substrate deoxyadenosine 5′-triphosphate and, after incorporation into DNA, by DNA chain termination
Absorption
Peak plasma concentration: 2.1 mcg/mL (emtricitabine); 0.16 mcg/mL (TAF)
Peak plasma time: 4hr (rilpivirine); 3hr (emtricitabine); 1hr (TAF)
AUC: 11.7 mcg·hr per mL (emtricitabine); 2.2 mcg·hr per mL (rilpivirine); 0.21 mcg·hr per mL (TAF)
Distribution
Protein bound: ~99% (rilpivirine); <4% (emtricitabine); ~80% (TAF)
Metabolism
Rilpivirine is metabolized by CYP3A4 pathway
Emtricitabine is not significantly metabolized
Tenofovir AF is converted from tenofovir AF to tenofovir through hydrolysis primarily by carboxyesterase 1 (CES1) in primary hepatocytes; also metabolized by Cathepsin A in peripheral blood mononuclear cells (PBMCs) and minimally metabolized by CYP3A4
Elimination
Half-life: 50 hr (rilpivirine); 10 hr (emtricitabine); 0.51 hr (TAF)
Excretion in urine: 6% (rilpivirine); 70% (emtricitabine); <1% (TAF)
Excretion in feces: 85% (rilpivirine); 13.7% (emtricitabine); 31.7 % (TAF)
Administration
Oral Administration
Take with food
Storage
Store <30°C (86°F)
Keep container tightly closed
Dispense only in original container
Images
Formulary
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