Dosing & Uses
Dosage Forms & Strengths
dolutegravir/rilpivirine
tablet
- 50mg/25mg
- equivalent to 52.6mg dolutegravir sodium/27.5mg rilpivirine hydrochloride
HIV Infection
Indicated as complete regimen to replace current antiretroviral (ART) regimen in virologically suppressed adults
Patients with no history of treatment failure and no known substitutions associated with resistance to dolutegravir or rilpivirine
HIV-1 RNA <50 copies/mL on a stable ART regimen for ≥6 months: 1 tablet (dolutegravir 50 mg/rilpivirine 25 mg) PO qDay
Dosage Modifications
See also Contraindications
Renal impairment
- Mild-to-moderate (CrCl ≥30 mL/min): No dosage adjustment is necessary
- Severe (CrCl <30 mL/min) or end-stage renal disease: Increased monitoring for adverse effects is recommended
Hepatic impairment
- Mild-to-moderate (Child-Pugh A or B): No dosage adjustment is necessary
- Severe (Child-Pugh C): Effect on the pharmacokinetics of dolutegravir or rilpivirine is unknown
Coadministration with dolutegravir/rilpivirine and other drugs
- Rifabutin: Take an additional 25-mg tablet of rilpivirine for the duration of the rifabutin coadministration
- Metformin: Limit total daily dose of metformin to 1000 mg/day either when starting metformin or dolutegravir/rilpivirine; when starting or stopping dolutegravir/rilpivirine, metformin dose may require an adjustment; monitor blood glucose when initiating concomitant use and after withdrawal of dolutegravir/rilpivirine
- Macrolides or ketolides (eg, clarithromycin, erythromycin, telithromycin): Consider alternant antibiotics (eg, azithromycin) if possible
- Medications containing polyvalent cations (eg, Mg or Al) (cation-containing products or laxatives, sucralfate buffered medications): Administer 4 hr before or 6 hr after taking products containing polyvalent cations
- Methadone: No dose adjustment for dolutegravir/rilpivirine is necessary; methadone maintenance therapy may need to be adjusted in some patients
- Oral calcium and iron supplements (eg, multivitamins containing calcium or iron [non-antacid]): Administer dolutegravir/rilpivirine and supplements containing calcium or iron together with a meal or take these supplements 4 hr before or 6 hr after taking dolutegravir/rilpivirine
-
Drugs affecting gastric pH
- Antacids (eg, aluminum or magnesium hydroxide, calcium carbonate): Administer dolutegravir/rilpivirine 4 hr before or 6 hr after taking antacids
- H2-receptor antagonists (eg, famotidine, cimetidine, nizatidine, ranitidine): Administer dolutegravir/rilpivirine at least 4 hr before or 12 hr after taking H2-receptor antagonists
Dosing Considerations
Pregnancy testing recommended in patients with childbearing potential before initiating therapy
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (5)
- 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.
- dofetilide
dolutegravir will increase the level or effect of dofetilide by decreasing renal clearance. Contraindicated. Dolutegravir inhibits the renal organic cation transporter, OCT2; risk of life-threatening arrhythmias caused by increased systemic exposure to dofetilide
- efavirenz
efavirenz decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be used in combination with NNRTIs.
Serious - Use Alternative (51)
- 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.
- aluminum hydroxide/magnesium carbonate
aluminum hydroxide/magnesium carbonate will decrease the level or effect of dolutegravir by cation binding in GI tract. Avoid or Use Alternate Drug. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations
- 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
dolutegravir, 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
dolutegravir, 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.
- carbamazepine
carbamazepine will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration; insufficient data to recommend dosage adjustment
- 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.
efavirenz will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Increase dolutegravir dose to 50 mg BID when coadministered with strong UGT1A/CYP3A inducers - elivaldogene autotemcel
elivaldogene autotemcel, dolutegravir. 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.
- etravirine
etravirine will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Etravirine (a strong UGT1A/CYP3A inducer) significantly reduces dolutegravir plasma concentrations, but the effect of etravirine is mitigated by coadministration of lopinavir/ritonavir or darunavir/ritonavir, and is expected to be mitigated by atazanavir/ritonavir; do not use with etravirine without coadministration of atazanavir/ritonavir, darunavir/ritonavir, or lopinavir/ritonavir
- 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.
- fosamprenavir
fosamprenavir will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Increase dolutegravir dose to 50 mg BID when coadministered with strong UGT1A/CYP3A inducers (eg, fosamprenavir/ritonavir)
- fosphenytoin
fosphenytoin will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration; insufficient data to recommend dosage adjustment
- 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.
- magnesium citrate
magnesium citrate will decrease the level or effect of dolutegravir by cation binding in GI tract. Avoid or Use Alternate Drug. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations
- magnesium gluconate
magnesium gluconate will decrease the level or effect of dolutegravir by cation binding in GI tract. Avoid or Use Alternate Drug. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations
- magnesium oxide
magnesium oxide will decrease the level or effect of dolutegravir by cation binding in GI tract. Avoid or Use Alternate Drug. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations
- 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.
- nevirapine
nevirapine will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration; insufficient data to recommend dosage adjustment
- 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.
- oxcarbazepine
oxcarbazepine will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration; insufficient data to recommend dosage adjustment
- phenobarbital
phenobarbital will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration; insufficient data to recommend dosage adjustment
- phenytoin
phenytoin will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration; insufficient data to recommend dosage adjustment
- Prussian blue
Prussian blue will decrease the level or effect of dolutegravir by cation binding in GI tract. Avoid or Use Alternate Drug. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations
- 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.
- rifampin
rifampin will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Increase dolutegravir dose to 50 mg BID when coadministered with strong UGT1A/CYP3A inducers
- St John's Wort
St John's Wort will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration; insufficient data to recommend dosage adjustment
- 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.
- sucralfate
sucralfate will decrease the level or effect of dolutegravir by cation binding in GI tract. Avoid or Use Alternate Drug. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations
- tetrabenazine
tetrabenazine and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- tipranavir
tipranavir will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Increase dolutegravir dose to 50 mg BID when coadministered with strong UGT1A/CYP3A inducers (eg, tipranavir/ritonavir)
- 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.
Monitor Closely (150)
- 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.
aluminum hydroxide will decrease the level or effect of dolutegravir by cation binding in GI tract. Use Caution/Monitor. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations; use alternative therapy if available - 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.
- calcium acetate
calcium acetate will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.
- 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 will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.
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 will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.
- 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.
- dalfampridine
dolutegravir will increase the level or effect of dalfampridine by Other (see comment). Modify Therapy/Monitor Closely. dolutegravir inhibits OCT2 and multidrug and toxin extrusion transporter 1
- 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. - eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of dolutegravir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dose of dolutegravir to 50 mg PO q12hr for treatment naïve or treatment experienced INSTI-naïve.
- 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.
- ferric maltol
ferric maltol will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.
- ferrous fumarate
ferrous fumarate will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.
- ferrous gluconate
ferrous gluconate will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.
- ferrous sulfate
ferrous sulfate will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.
- 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 hydroxide
magnesium hydroxide will decrease the level or effect of dolutegravir by cation binding in GI tract. Use Caution/Monitor. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations; use alternative therapy if available
- 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.
- magnesium supplement
magnesium supplement will decrease the level or effect of dolutegravir by Other (see comment). Modify Therapy/Monitor Closely. Drug may form a chelate with polyvalent cations; may decrease absorption by the intestinal tract; applies to oral forms; may administer under fasting conditions 2 hr before administering polyvalent cation or 6 hr after
- 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.
- metformin
dolutegravir will increase the level or effect of metformin by decreasing renal clearance. Modify Therapy/Monitor Closely. Dolutegravir inhibits the renal organic cation transporter, OCT2; when used with metformin, limit total daily dose of metformin to 1,000 mg either when starting metformin or dolutegravir; when stopping dolutegravir, adjustment of metformin dose may be necessary; monitor blood glucose when initiating concomitant use and after withdrawal of dolutegravir
- 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. - multivitamins
multivitamins will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.
- multivitamins, vision
multivitamins, vision will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.
- 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 dolutegravir 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.
- selenium
selenium will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir at least 2 h before or 6 h after polyvalent cations. Administer the dolutegravir/rilpivirine combination at least 4 h before or 6 h after polyvalent cations.
- 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 sulfate/?magnesium sulfate/potassium chloride
sodium sulfate/?magnesium sulfate/potassium chloride decreases levels of dolutegravir by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Administer dolutegravir at least 2 hr before or 6 hr after each dose to avoid chelation with magnesium. .
- sodium sulfate/potassium sulfate/magnesium sulfate
sodium sulfate/potassium sulfate/magnesium sulfate decreases levels of dolutegravir by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Administer dolutegravir at least 2 hr before or 6 hr after each dose to avoid chelation with magnesium. .
- 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.
- ublituximab
ublituximab decreases effects of rilpivirine by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely.
ublituximab decreases effects of dolutegravir by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. - valbenazine
valbenazine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- zinc
zinc will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir at least 2 hr before or 6 hr after oral zinc salts.
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%
Dolutegravir
- Lipase, Grade 2 (5%)
- Hyperglycemia, Grade 2 (4%)
- ALT, Grade 2 (2%)
- Total bilirubin, Grade 2 (2%)
- Creatine kinase, Grade 3 or 4 (1%)
- Lipase, Grade 3 or 4 (2%)
Rilpivirine
- Lipase, Grade 2 (5%)
- Hyperglycemia, Grade 3 or 4 (5%)
- Total bilirubin, Grade 2 (4%)
- Creatine kinase, Grade 3 or 4 (2%)
- Lipase, Grade 3 or 4 (2%)
<1%
ALT, Grade 3 or 4
AST, Grade 3 or 4
Creatine kinase, Grade 2
Hyperglycemia, Grade 3 or 4
Postmarketing Reports
Musculoskeletal disorders: Arthralgia, myalgia
Hepatobiliary disorders: Acute liver failure, hepatotoxicity
Renal and genitourinary disorders: Nephrotic syndrome
Skin and subcutaneous tissue disorders: Severe skin and hypersensitivity reactions including DRESS (drug rash with eosinophilia and systemic symptoms)
Warnings
Contraindications
Documented hypersensitivity to dolutegravir or rilpivirine
Concomitant use with other drugs
- Also see Cautions and Dosage Modifications
- Dofetilide, carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, rifapentine, dexamethasone, St. John’s wort, esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole
Cautions
Depressive disorders (including depressed mood, depression, dysphoria, major depression, mood altered, negative thoughts, suicide attempt, and suicidal ideation) have been associated with rilpivirine
May 18, 2018: The FDA issued a safety alert regarding the potential risk of neural tube birth defects (see Pregnancy)
Hepatotoxicity
- Hepatic adverse events were reported in patients receiving a dolutegravir- or rilpivirine-containing regimen; patients with underlying hepatitis B or C or marked elevations in transaminases prior to treatment may be at increased risk for worsening or development of transaminase elevations
- Drug-induced liver injury leading to acute liver failure has been reported with dolutegravir-containing products; monitor for hepatotoxicity
Skin and hypersensitivity reactions
- Hypersensitivity reactions (eg, rash, constitutional findings, and sometimes organ dysfunction, including liver injury) have been reported
- Severe skin and hypersensitivity reactions have been reported during postmarketing experience, including cases of DRESS, with rilpivirine-containing regimens
- Discontinue treatment immediately if signs or symptoms of severe skin or hypersensitivity reactions develop (see Contraindications)
Drug interactions overview
- Also see Dosage Modifications
- Concomitant use of dolutegravir/rilpivirine and other drugs may result in known or potentially significant drug interactions, loss of therapeutic effect of dolutegravir/rilpivirine, possible development of resistance, or possible increases in toxicities of dolutegravir/rilpivirine
- Because dolutegravir/rilpivirine is a complete regimen, coadministration with other antiretroviral medications is not recommended
- Dolutegravir inhibits the renal organic cation transporters (OCT)2 and multidrug and toxin extrusion transporter (MATE)1; thus, it may increase plasma concentrations of drugs eliminated via OCT2 or MATE1 (eg, dofetilide and metformin)
Potential for other drugs to affect dolutegravir
- Dolutegravir is metabolized by uridine diphosphate (UDP)-glucuronosyl transferase (UGT)1A1 with some contribution from CYP3A; dolutegravir is also a substrate of UGT1A3, UGT1A9, breast cancer resistance protein (BCRP), and p-glycoprotein (P-gp) in vitro
- Drugs that induce those enzymes and transporters may decrease dolutegravir plasma concentrations and reduce the therapeutic effect of dolutegravir
- Coadministration of dolutegravir and other drugs that inhibit these enzymes may increase dolutegravir plasma concentrations
Potential for other drugs to affect rilpivirine
- 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 dolutegravir/rilpivirine dose) and 300 mg PO qDay (12 times dolutegravir/rilpivirine dose) have been shown to prolong the QTc interval; consider alternatives to dolutegravir/rilpivirine 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) at 1-800-258-4263
Dolutegravir has been shown to cross the placenta; data from a birth outcome surveillance study has identified an increased risk of neural tube defects when dolutegravir, a component of the drug combination, is administered at time of conception compared with non-dolutegravir-containing antiretroviral regimens
As defects related to closure of neural tube occur from conception through first 6 weeks of gestation, embryos exposed to dolutegravir from time of conception through first 6 weeks of gestation are at potential risk
In addition, 2 of 5 birth defects (encephalocele and iniencephaly), which have been observed with dolutegravir use, although often termed neural tube defects, may occur post-neural tube closure, the time period of which may be later than 6 weeks of gestation, but within first trimester
Due to limited understanding of types of reported neural tube defects associated with dolutegravir use and because date of conception may not be determined with precision, an alternative treatment should be considered at time of conception through first trimester of pregnancy
Initiation of therapy is not recommended in individuals actively trying to become pregnant unless there is no suitable alternative
In individuals of childbearing potential currently on therapy who are actively trying to become pregnant, or if pregnancy is confirmed in first trimester, assess risks and benefits of continuing therapy versus switching to another antiretroviral regimen and consider switching to an alternative regimen
Advise pregnant individuals of the potential risk to embryo exposed to drug from time of conception through first trimester of pregnancy; a benefit-risk assessment should consider factors such as feasibility of switching, tolerability, ability to maintain viral suppression, and risk of transmission to the infant against the risk of neural tube defects
Animal data
- In animal reproduction studies, no evidence of adverse developmental outcomes was observed with dolutegravir or rilpivirine
- During organogenesis in the rat and rabbit, systemic exposures (AUC) to dolutegravir were less than (rabbits) and 38 times (rats) and exposures to rilpivirine were 15 (rats) and 70 (rabbits) times the exposure at the recommended human dose (RHD)
- In rat prenatal and postnatal development studies, maternal systemic exposures (AUC) to dolutegravir and rilpivirine were ~32 and 63 times, respectively, exposures of each component in humans at the RHD
Potential risk of neural tube birth defects
- Serious cases of neural tube birth defects involving the brain, spine, and spinal cord reported in babies born to women treated with dolutegravir
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Recommendations
- Patients should not discontinue dolutegravir without consulting a healthcare professional because stopping your medicine can cause the HIV infection to worsen
- Pregnant women stopping dolutegravir-containing regimen without switching to alternative HIV medicines could cause the amount of virus to increase and spread HIV to your baby
- Healthcare providers should weigh the benefits and the risks of dolutegravir when prescribing antiretroviral medicines to women of childbearing age; consider alternative antiretroviral medicines; discuss the relative risks and benefits of appropriate alternative antiretroviral therapies
- Women of childbearing age who decide to take a dolutegravir-containing regimen should consistently use effective birth control (contraception) while on HIV treatment; women should discuss their healthcare professionals about an effective birth control method to use while taking a dolutegravir-containing regimen
- Perform pregnancy testing before initiating a dolutegravir-containing regimen in women of childbearing age to exclude pregnancy
Lactation
The Centers for Disease Control and Prevention do not recommend HIV-1-infected mothers in the United States breastfeed their infants to avoid risking postnatal transmission of HIV-1 infection
Dolutegravir and lamivudine are present in human milk; there is no information on effects of the drug components on the breastfed infant or effects on milk production
When administered to lactating rats, dolutegravir and rilpivirine were present in milk
Because of potential for HIV-1 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 if they are receiving therapy
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
Dolutegravir
- Integrase strand transfer inhibitor (INSTI); inhibits catalytic activity of HIV-1 integrase, an HIV-encoded enzyme required for viral replication
Rilpivirine
- Antiviral agent; diarylpyrimidine 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
Peak plasma concentration: 3.67 mcg/mL (dolutegravir); 0.13 mcg/mL (rilpivirine)
Peak plasma time: 3 hr (dolutegravir); 4 hr (rilpivirine)
AUC ratio, moderate-fat meal: 1.87 (dolutegravir); 1.57 (rilpivirine)
AUC ratio, high-fat meal: 1.87 (dolutegravir); 1.72 (rilpivirine)
Distribution
Protein bound: ~99%
Blood-to-ratio: 0.5 (dolutegravir); 0.7 (rilpivirine)
Metabolism
Dolutegravir: Primarily metabolized by UGT1A1; CYP3A (minor)
Rilpivirine: Primarily metabolized by CYP3A
Excretion
Half-life: 14 hr (dolutegravir); 50 hr (rilpivirine)
Excretion, urine: 31% (dolutegravir), <1% (unchanged dolutegravir); 6.5% (rilpivirine), <1% (unchanged rilpivirine)
Excretion, feces: 64% (dolutegravir), 53% (unchanged dolutegravir); 85% (rilpivirine), 25% (unchanged rilpivirine)
Administration
Oral administration
Take with a meal
Storage
Tablets
- Store at room temperature, 20-25°C (68-77°F); excursions permitted 15-30°C (59-86°F)
- Store and dispense in original package, protect from moisture, and keep bottle tightly closed
- Do not remove desiccant
Images
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.
