Dosing & Uses
Dosage Forms & Strengths
Cabotegravir and rilpivirine are copackaged as 2 separate IM injections
Each dosing kit also contains 2 syringes, 2 syringe labels, 2 vial adapters, and 2 needles for IM injection (23-gauge, 1.5-inch)
Vial stoppers are not made with natural rubber latex
injection, IM suspension 400mg/600mg kit
- Cabotegravir: 400mg/2mL
- Rilpivirine: 600mg/2mL
injection, IM suspension 600mg/900mg kit
- Cabotegravir: 600mg/3mL
- Rilpivirine: 900mg/3mL
HIV Infection
Indicated as a complete regimen for treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults and adolescents to replace a current stable antiretroviral therapy (ART) regimen in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine
May administer with optional oral lead-in therapy (at least 28 days) or direct-to-injection
Optional oral lead-in dosing
- May use oral lead-in for ~1 month (at least 28 days) before initiating to assess tolerability of cabotegravir and rilpivirine for monthly- or every-2-month dosage regimens
- Cabotegravir (Vocabria) 30 mg plus rilpivirine (Edurant) 25 mg qDay for ~1 month (at least 28 days) to ensure medications are well tolerated
Once-monthly regimen
- Administer each drug as 2 separate IM injections
-
One-time initiating injection
- Initiate on last day of current ART therapy or oral lead-in (if used)
- Cabotegravir 600 mg (3 mL) IM PLUS
- Rilpivirine 900 mg (3 mL) IM
-
Continuation injections every month
- Administer once monthly after initial injections
- Cabotegravir 400 mg (2 mL) IM qMonth PLUS
- Rilpivirine 600 mg (2 mL) IM qMonth
- Give up to 7 days before or after scheduled monthly injections
Every 2-month regimen
- Administer each drug as 2 separate IM injections
-
Initiating injections
- Initiate on last day of current ART therapy or oral lead-in (if used)
- Cabotegravir 600 mg (3 mL) IM qMonth x 2 PLUS
- Rilpivirine 900 mg (3 mL) IM qMonth x 2
- Give up to 7 days before or after scheduled second initiation injections
-
Continuation injections every 2 months
- Initiate at Month 3, and then every 2 months thereafter
- Cabotegravir 600 mg (3 mL) IM every 2 months PLUS
- Rilpivirine 900 mg (3 mL) IM every 2 months
- Give up to 7 days before or after scheduled injections
Dosage Modifications
Renal impairment
- Mild-to-moderate (CrCl 30 to <90 mL/min): No dosage adjustment required
- Severe (CrCl <15 mL/min) or ESRD: Increased monitoring recommended
- ESRD not on dialysis: Pharmacokinetic effects of each drug are unknown
- Dialysis: Cabotegravir and rilpivirine are >99% protein bound; dialysis is not expected to alter systemic exposure
Hepatic impairment
- Mild or moderate (Child-Pugh A or B): No dosage adjustment required
- Severe (Child-Pugh C): Pharmacokinetic effects are unknown
Dosing Considerations
Switching from monthly to every-2-month continuation dosing schedule
- Administer 1 month after last monthly continuation injection and then every 2 months thereafter
- Cabotegravir 600 mg (3 mL) IM PLUS
- Rilpivirine 900 mg (3 mL) IM
- Administer both injections at separate gluteal injection sites (on opposite sides or 2 cm apart) during same visit
Switching from every-2-month to monthly continuation dosing schedule
- Administer 2 months after last every-2-month continuation injection and then monthly thereafter
- Cabotegravir 400 mg (2 mL) IM PLUS
- Rilpivirine 600 mg (2 mL) IM
- Administer both injections at separate gluteal injection sites (on opposite sides or 2 cm apart) during same visit
Patient selection
- Must be administered by a healthcare professional
- Before initiating, carefully select patients who agree to required monthly or every 2-month dosing schedule
- Discuss 2 dosing options before initiating and select most appropriate dosing frequency for patient
HIV Infection
Indicated as a complete regimen for treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults and adolescents aged ≥12 years who weigh at least 35 kg to replace a current stable antiretroviral therapy (ART) regimen in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine
<12 years: Safety and efficacy not established
≥12 years (weight ≥35 kg): May administer with optional oral lead-in therapy (at least 28 days) or direct-to-injection
Optional oral lead-in dosing
- May use oral lead-in for ~1 month (at least 28 days) before initiating to assess tolerability of cabotegravir and rilpivirine for monthly- or every-2-month dosage regimens
- Cabotegravir (Vocabria) 30 mg plus rilpivirine (Edurant) 25 mg qDay for ~1 month (at least 28 days) to ensure medications are well tolerated
Once-monthly regimen
- Administer each drug as 2 separate IM injections
-
One-time initiating injection
- Initiate on last day of current ART therapy or oral lead-in (if used)
- Cabotegravir 600 mg (3 mL) IM PLUS
- Rilpivirine 900 mg (3 mL) IM
-
Continuation injections every month
- Administer once monthly after initial injections
- Cabotegravir 400 mg (2 mL) IM qMonth PLUS
- Rilpivirine 600 mg (2 mL) IM qMonth
- Give up to 7 days before or after scheduled monthly injections
Every 2-month regimen
- Administer each drug as 2 separate IM injections
-
Initiating injections
- Initiate on last day of current ART therapy or oral lead-in (if used)
- Cabotegravir 600 mg (3 mL) IM qMonth x 2 PLUS
- Rilpivirine 900 mg (3 mL) IM qMonth x 2
- Give up to 7 days before or after scheduled second initiation injections
-
Continuation injections every 2 months
- Initiate at Month 3, and then every 2 months thereafter
- Cabotegravir 600 mg (3 mL) IM every 2 months PLUS
- Rilpivirine 900 mg (3 mL) IM every 2 months
- Give up to 7 days before or after scheduled injections
Dosage Modifications
Renal impairment
- Mild-to-moderate (CrCl 30 to <90 mL/min): No dosage adjustment required
- Severe (CrCl <15 mL/min) or ESRD: Increased monitoring recommended
- ESRD not on dialysis: Pharmacokinetic effects of each drug are unknown
- Dialysis: Cabotegravir and rilpivirine are >99% protein bound; dialysis is not expected to alter systemic exposure
Hepatic impairment
- Mild or moderate (Child-Pugh A or B): No dosage adjustment required
- Severe (Child-Pugh C): Pharmacokinetic effects are unknown
Dosing Considerations
Switching from monthly to every-2-month continuation dosing schedule
- Administer 1 month after last monthly continuation injection and then every 2 months thereafter
- Cabotegravir 600 mg (3 mL) IM PLUS
- Rilpivirine 900 mg (3 mL) IM
- Administer both injections at separate gluteal injection sites (on opposite sides or 2 cm apart) during same visit
Switching from every-2-month to monthly continuation dosing schedule
- Administer 2 months after last every-2-month continuation injection and then monthly thereafter
- Cabotegravir 400 mg (2 mL) IM PLUS
- Rilpivirine 600 mg (2 mL) IM
- Administer both injections at separate gluteal injection sites (on opposite sides or 2 cm apart) during same visit
Patient selection
- Must be administered by a healthcare professional
- Before initiating, carefully select patients who agree to required monthly or every 2-month dosing schedule
- Discuss 2 dosing options before initiating and select most appropriate dosing frequency for patient
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (31)
- apalutamide
apalutamide will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.
- 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.
carbamazepine will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response. - cigarette smoking
cigarette smoking will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.
- 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.
- desogestrel
desogestrel will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.
- dexlansoprazole
dexlansoprazole decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Contraindicated. Concurrent use may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels.
- efavirenz
efavirenz decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be used in combination with NNRTIs.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
rilpivirine, elvitegravir/cobicistat/emtricitabine/tenofovir DF. Other (see comment). Contraindicated. Comment: Elvitegravir/cobicistat/emtricitabine/tenofovir is a complete regimen for HIV and should not be administered with other antiretrovirals.
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class.
- esomeprazole
esomeprazole decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Contraindicated. Concurrent use may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels.
- etravirine
etravirine decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be used in combination with NNRTIs.
- fosphenytoin
fosphenytoin decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class.
- lamotrigine
lamotrigine will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.
- lansoprazole
lansoprazole decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Contraindicated. Concurrent use may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels.
- nevirapine
nevirapine decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be used in combination with NNRTIs.
- nicotine gum
nicotine gum will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.
- nicotine inhaled
nicotine inhaled will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.
- nicotine intranasal
nicotine intranasal will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.
- nicotine lozenge
nicotine lozenge will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.
- nicotine transdermal
nicotine transdermal will decrease the level or effect of cabotegravir by increasing elimination. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.
- omeprazole
omeprazole decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Contraindicated. Concurrent use may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels.
- oxcarbazepine
oxcarbazepine decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class.
- pantoprazole
pantoprazole decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Contraindicated. Concurrent use may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels.
- phenobarbital
phenobarbital will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.
phenobarbital decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class. - phenytoin
phenytoin will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.
phenytoin decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class. - primidone
primidone will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.
- rabeprazole
rabeprazole decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Contraindicated. Concurrent use may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels.
- rifabutin
rifabutin will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response. Note: Rifabutin can be coadministered with cabotegravir PO; however, it is contraindicated with Cabenuva (cabotegravir; rilpivirine) extended-release injectable suspensions.
- rifampin
rifampin decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class.
rifampin will increase the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response. - rifapentine
rifapentine decreases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated. Rilpivirine should not be co-administered with strong CYP 3A4 inducers. Potential for loss of virologic response and possible resistance to rilpivirine or to the NNRTI class.
- testosterone
testosterone will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.
Serious - Use Alternative (62)
- abacavir
abacavir, 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.
- 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.
- atazanavir
atazanavir, 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.
- bedaquiline
bedaquiline and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- betibeglogene autotemcel
cabotegravir, 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. - bictegravir
bictegravir, 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
buprenorphine and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- darunavir
darunavir, 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.
- delavirdine
delavirdine, 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.
- desflurane
desflurane and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- didanosine
didanosine, 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.
- dofetilide
dofetilide increases toxicity of rilpivirine by QTc interval. Avoid or Use Alternate Drug.
- dolutegravir
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.
- doravirine
doravirine, 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.
- efavirenz
efavirenz and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
efavirenz, 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. - elivaldogene autotemcel
elivaldogene autotemcel, cabotegravir. 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. - elvitegravir
elvitegravir, 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.
- encorafenib
encorafenib and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF, 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.
- emtricitabine
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.
- enfuvirtide
enfuvirtide, 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.
- 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.
- etravirine
etravirine, 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.
- 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, 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.
- fostemsavir
fostemsavir, 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.
- hydroxychloroquine sulfate
hydroxychloroquine sulfate and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- ibalizumab
ibalizumab, 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.
- indinavir
indinavir, 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.
- isoflurane
isoflurane and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- lamivudine
lamivudine, 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.
- 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.
- maraviroc
maraviroc, 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.
- 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.
- nelfinavir
nelfinavir, 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.
- nevirapine
nevirapine, 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.
- 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.
- raltegravir
raltegravir, 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.
- 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.
- ritonavir
ritonavir, 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.
- saquinavir
saquinavir, 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.
- 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.
- stavudine
stavudine, 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.
- tenofovir DF
tenofovir DF, 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.
- tetrabenazine
tetrabenazine and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- tipranavir
tipranavir, 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.
- umeclidinium bromide/vilanterol inhaled
rilpivirine increases toxicity of umeclidinium bromide/vilanterol inhaled by QTc interval. Avoid or Use Alternate Drug. Exercise extreme caution when vilanterol coadministered with drugs that prolong QTc interval; adrenergic agonist effects on the cardiovascular system may be potentiated.
- vilanterol/fluticasone furoate inhaled
rilpivirine increases toxicity of vilanterol/fluticasone furoate inhaled by QTc interval. Avoid or Use Alternate Drug. Exercise extreme caution when vilanterol coadministered with drugs that prolong QTc interval; adrenergic agonist effects on the cardiovascular system may be potentiated.
- zidovudine
zidovudine, 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.
Monitor Closely (148)
- 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 cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir. - aluminum hydroxide/magnesium carbonate
aluminum hydroxide/magnesium carbonate will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir.
- 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.
- aluminum hydroxide/magnesium trisilicate
aluminum hydroxide/magnesium trisilicate will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir.
- 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.
aspirin/citric acid/sodium bicarbonate will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir. - 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. .
- calcium carbonate
calcium carbonate will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir.
- atomoxetine
atomoxetine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- azithromycin
rilpivirine increases toxicity of azithromycin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- calcium acetate
calcium acetate decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- calcium carbonate
calcium carbonate decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should be given at least 2 hr before or at least 4 hr after rilpivirine. For the combination product dolutegravir/rilpivirine, antacids should be given at least 4 hr before or at least 6 hr afterwards.
- calcium chloride
calcium chloride decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- calcium citrate
calcium citrate decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- calcium gluconate
calcium gluconate decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- calcium/vitamin D
calcium/vitamin D will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer polyvalent cation products at least 2 hr before or 4 hr after taking oral cabotegravir.
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.
- magaldrate
magaldrate will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir.
- cimetidine
cimetidine will decrease the level or effect of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Concurrent use, may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels. Administer H2 antagonists at least 12 hours before or at least 4 hours after rilpivirine.
- ciprofloxacin
rilpivirine increases toxicity of ciprofloxacin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- citalopram
rilpivirine increases toxicity of citalopram by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- clarithromycin
clarithromycin increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Where possible, alternatives such as azithromycin should be considered.
rilpivirine increases toxicity of clarithromycin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes. - clomipramine
rilpivirine increases toxicity of clomipramine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- clozapine
clozapine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- conivaptan
conivaptan increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- crizotinib
crizotinib increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Dose reduction may be needed for coadministered drugs that are predominantly metabolized by CYP3A.
- cyclobenzaprine
rilpivirine increases toxicity of cyclobenzaprine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- dasatinib
rilpivirine increases toxicity of dasatinib by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- degarelix
rilpivirine increases toxicity of degarelix by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- desipramine
rilpivirine increases toxicity of desipramine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- deutetrabenazine
deutetrabenazine and rilpivirine both increase QTc interval. Use Caution/Monitor. At the maximum recommended dose, deutetrabenazine does not prolong QT interval to a clinically relevant extent. Certain circumstances may increase risk of torsade de pointes and/or sudden death in association with drugs that prolong the QTc interval (eg, bradycardia, hypokalemia or hypomagnesemia, coadministration with other drugs that prolong QTc interval, presence of congenital QT prolongation).
- didanosine
didanosine, rilpivirine. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Applies to didanosine chewable tablets and powder for oral solution; administer 2 hr before or several hours after didanosine oral solution or chewable tablet administration; no dose adjustment is required when rilpivirine is coadministered with didanosine. Didanosine is to be administered on an empty stomach and at least two hours before or at least four hours after rilpivirine (which should be administered with a meal).
- disopyramide
rilpivirine increases toxicity of disopyramide by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- dofetilide
rilpivirine increases toxicity of dofetilide by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- dolasetron
rilpivirine increases toxicity of dolasetron by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- donepezil
donepezil and rilpivirine both increase QTc interval. Use Caution/Monitor.
- doxepin
doxepin and rilpivirine both increase QTc interval. Use Caution/Monitor.
- dronedarone
rilpivirine increases toxicity of dronedarone by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- droperidol
rilpivirine increases toxicity of droperidol by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- eliglustat
eliglustat and rilpivirine both increase QTc interval. Use Caution/Monitor.
- erythromycin base
erythromycin base increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Where possible, alternatives such as azithromycin should be considered.
rilpivirine increases toxicity of erythromycin base by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes. - erythromycin ethylsuccinate
erythromycin ethylsuccinate increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Where possible, alternatives such as azithromycin should be considered.
rilpivirine increases toxicity of erythromycin ethylsuccinate by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes. - erythromycin lactobionate
erythromycin lactobionate increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Where possible, alternatives such as azithromycin should be considered.
rilpivirine increases toxicity of erythromycin lactobionate by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes. - erythromycin stearate
erythromycin stearate increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Where possible, alternatives such as azithromycin should be considered.
rilpivirine increases toxicity of erythromycin stearate by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes. - escitalopram
rilpivirine increases toxicity of escitalopram by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
escitalopram increases toxicity of rilpivirine by QTc interval. Use Caution/Monitor. - famotidine
famotidine will decrease the level or effect of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Concurrent use, may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels. Administer H2 antagonists at least 12 hours before or at least 4 hours after rilpivirine.
- fingolimod
fingolimod and rilpivirine both increase QTc interval. Use Caution/Monitor.
- flecainide
rilpivirine increases toxicity of flecainide by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- fluconazole
fluconazole increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No rilpivirine dose adjustment is required. Clinically monitor for breakthrough fungal infections when azole antifungals are co-administered with rilpivirine.
rilpivirine increases toxicity of fluconazole by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes. - fluoxetine
rilpivirine increases toxicity of fluoxetine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- fosamprenavir
fosamprenavir increases effects of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Rilpivirine is not expected to affect the plasma concentrations of co-administered protease inhibitors. .
- foscarnet
rilpivirine increases toxicity of foscarnet by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- fostemsavir
rilpivirine and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.
- gemifloxacin
rilpivirine increases toxicity of gemifloxacin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsades de Pointes.
- gepirone
gepirone and rilpivirine both increase QTc interval. Modify Therapy/Monitor Closely.
- 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 will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer polyvalent cation products at least 2 hr before or 4 hr after taking oral cabotegravir.
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 citrate
magnesium citrate will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer polyvalent cation products at least 2 hr before or 4 hr after taking oral cabotegravir.
- 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 cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir.
- magnesium oxide
magnesium oxide will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer antacid products at least 2 hr before or 4 hr after taking oral cabotegravir.
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.
- ublituximab
ublituximab decreases effects of cabotegravir by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely.
- maprotiline
rilpivirine increases toxicity of maprotiline by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- mefloquine
rilpivirine increases toxicity of mefloquine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- methadone
rilpivirine, methadone. Other (see comment). Use Caution/Monitor. Comment: No dose adjustments are required when initiating co-administration of methadone with rilpivirine. However, clinical monitoring is recommended as methadone maintenance therapy may need to be adjusted in some patients.
rilpivirine increases toxicity of methadone by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes. - mirtazapine
mirtazapine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- moxifloxacin
moxifloxacin increases toxicity of rilpivirine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
rilpivirine increases toxicity of moxifloxacin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes. - nefazodone
nefazodone increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nelfinavir
nelfinavir increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nilotinib
rilpivirine increases toxicity of nilotinib by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- nizatidine
nizatidine will decrease the level or effect of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Concurrent use, may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels. Administer H2 antagonists at least 12 hours before or at least 4 hours after rilpivirine.
- nortriptyline
rilpivirine increases toxicity of nortriptyline by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- octreotide
rilpivirine increases toxicity of octreotide by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- ofloxacin
rilpivirine increases toxicity of ofloxacin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- olanzapine
olanzapine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- orlistat
orlistat will decrease the level or effect of rilpivirine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Loss of virological control reported in HIV-infected patients taking orlistat concomitantly. Exact mechanism is unclear, but may include a drug-drug interaction that inhibits systemic absorption of the antiretroviral drug. Monitor HIV RNA levels frequently and if increased HIV viral load confirmed, discontinue orlistat.
- osilodrostat
osilodrostat and rilpivirine both increase QTc interval. Use Caution/Monitor.
- ozanimod
ozanimod and rilpivirine both increase QTc interval. Modify Therapy/Monitor Closely. The potential additive effects on heart rate, treatment with ozanimod should generally not be initiated in patients who are concurrently treated with QT prolonging drugs with known arrhythmogenic properties.
- paliperidone
rilpivirine increases toxicity of paliperidone by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- pazopanib
rilpivirine increases toxicity of pazopanib by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- pentamidine
rilpivirine increases toxicity of pentamidine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- pimozide
rilpivirine increases toxicity of pimozide by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- posaconazole
posaconazole increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No rilpivirine dose adjustment is required. Clinically monitor for breakthrough fungal infections when azole antifungals are co-administered with rilpivirine.
rilpivirine increases toxicity of posaconazole by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes. - potassium chloride
potassium chloride decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- primaquine
primaquine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- procainamide
rilpivirine increases toxicity of procainamide by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- propafenone
rilpivirine increases toxicity of propafenone by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- protriptyline
rilpivirine increases toxicity of protriptyline by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- quetiapine
rilpivirine increases toxicity of quetiapine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- quinidine
rilpivirine increases toxicity of quinidine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- quinine
rilpivirine increases toxicity of quinine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- quizartinib
quizartinib, rilpivirine. Either increases effects of the other by QTc interval. Modify Therapy/Monitor Closely. Monitor patients more frequently with ECG if coadministered with QT prolonging drugs.
- ranolazine
rilpivirine increases toxicity of ranolazine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- risperidone
rilpivirine increases toxicity of risperidone by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- ritonavir
ritonavir increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No dose adjustment is required during concurrent use.
rilpivirine increases toxicity of ritonavir by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes. - romidepsin
rilpivirine increases toxicity of romidepsin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- saquinavir
saquinavir increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Rilpivirine is not expected to affect the plasma concentrations of co-administered protease inhibitors. .
rilpivirine increases toxicity of saquinavir by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes. - selpercatinib
selpercatinib increases toxicity of rilpivirine by QTc interval. Use Caution/Monitor.
- sertraline
sertraline and rilpivirine both increase QTc interval. Use Caution/Monitor.
- sodium zirconium cyclosilicate
sodium zirconium cyclosilicate will decrease the level or effect of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Check specific recommendations for drugs that exhibit pH-dependent solubility that may affect their systemic exposure and efficacy. In general, administer drugs at least 2 hr before or after sodium zirconium cyclosilicate.
- solifenacin
solifenacin and rilpivirine both increase QTc interval. Use Caution/Monitor.
- sotalol
rilpivirine increases toxicity of sotalol by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- sunitinib
rilpivirine increases toxicity of sunitinib by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- tacrolimus
rilpivirine increases toxicity of tacrolimus by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- telavancin
rilpivirine increases toxicity of telavancin by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- thioridazine
rilpivirine increases toxicity of thioridazine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- thiothixene
rilpivirine increases toxicity of thiothixene by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- tipranavir
tipranavir increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Rilpivirine is not expected to affect the plasma concentrations of co-administered protease inhibitors. .
- toremifene
rilpivirine increases toxicity of toremifene by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- trimagnesium citrate anhydrous
trimagnesium citrate anhydrous decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Coadministration of antacids with rilpivirine may cause significant decreases in rilpivirine plasma concentrations because of increased gastric pH. If antacids must be administered, they should given at least 2 hr before or at least 4 hr after rilpivirine.
- trimipramine
rilpivirine increases toxicity of trimipramine by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- ublituximab
ublituximab decreases effects of rilpivirine by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely.
- valbenazine
valbenazine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- vandetanib
rilpivirine increases toxicity of vandetanib by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- voclosporin
voclosporin, rilpivirine. Either increases effects of the other by QTc interval. Use Caution/Monitor.
- voriconazole
voriconazole increases levels of rilpivirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No rilpivirine dose adjustment is required. Clinically monitor for breakthrough fungal infections when azole antifungals are co-administered with rilpivirine.
rilpivirine increases toxicity of voriconazole by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes. - vorinostat
rilpivirine increases toxicity of vorinostat by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- zinc
zinc will decrease the level or effect of cabotegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer polyvalent cation containing products at least 2 hr before or 4 hr after oral cabotegravir.
- ziprasidone
rilpivirine increases toxicity of ziprasidone by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
Minor (2)
- chloroquine
chloroquine increases toxicity of rilpivirine by QTc interval. Minor/Significance Unknown.
- crizotinib
crizotinib and rilpivirine both increase QTc interval. Minor/Significance Unknown.
Adverse Effects
>10%
Injection site reactions, all grades (83%)
Injection site reactions, ≥Grade 2 (37%)
1-10%
All grades
- Pyrexia (8%)
- Fatigue (5%)
- Headache (4%)
- Musculoskeletal pain (3%)
- Nausea (3%)
- Sleep disorders (2%)
- Dizziness (2%)
- Rash (2%)
Grade ≥2
- Pyrexia (2%)
- Fatigue (1%)
- Musculoskeletal pain (1%)
Grade 3 or 4 laboratory parameters
- Creatine phosphokinase ≥10 x ULN (8%)
- Lipase ≥3 x ULN (5%)
- ALT/AST ≥5 x ULN (2%)
<2%
- Gastrointestinal disorders: Abdominal pain (including upper abdominal pain), gastritis, dyspepsia, vomiting, diarrhea, and flatulence
- Hepatobiliary disorders: Hepatotoxicity
- Investigations: Weight increase
- Psychiatric disorders: Anxiety (including anxiety and irritability), depression, abnormal dreams
- Skin and hypersensitivity reactions: Hypersensitivity reactions
<1%
Grade ≥2
- Total bilirubin ≥2.6 x ULN
- Headache
- Nausea
- Sleep disorders
- Dizziness
- Rash
Postmarketing Reports
Renal and genitourinary disorders: Nephrotic syndrome
Skin and subcutaneous tissue disorders: Severe skin and hypersensitivity reactions, including drug reaction with eosinophilia and systemic symptoms (DRESS)
Hypersensitivity reactions (including angioedema and urticaria)
Warnings
Contraindications
Documented hypersensitivity
UGT1A1 or CYP3A inducers
- Coadministration with UGT1A1 inducers and/or CYP3A inducers may significantly decrease cabotegravir and/or rilpivirine plasma concentrations owing to possible loss of virologic response
- Examples of UGT1A1 inducers include carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifabutin, rifampin, and rifapentine
- Examples of CYP3A inducers include systemic glucocorticoids (eg, >1 dose of dexamethasone) and St John’s wort
Cautions
Serious postinjection reactions were reported within minutes after injection of rilpivirine, including dyspnea, agitation, abdominal cramping, flushing, sweating, oral numbness, and changes in blood pressure; symptoms began to resolve within a few minutes after injection; these events may have been associated with inadvertent (partial) IV administration; observe patient for 10 minutes after injection
Hepatotoxicity reported in patients with or without known preexisting hepatic disease or known risk factors; monitoring of liver chemistries recommended; discontinue treatment if hepatotoxicity suspected
Depressive disorders (including depressed mood, depression, mood altered, mood swings) reported; promptly evaluate if symptoms emerge; determine whether risks of continued therapy outweigh benefits
To minimize the potential risk of developing viral resistance, it is essential to initiate an alternative, fully suppressive antiretroviral regimen ≤1 month after final injections when dosed monthly and ≤2 months after final injections when dosed every 2 months; if virologic failure is suspected, switch to an alternative regimen as soon as possible
Hypersensitivity
- Serious or severe hypersensitivity reactions reported with other integrase inhibitors
- Discontinue immediately if signs or symptoms of hypersensitivity reactions develop (including, but not limited to, severe rash, or rash accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, mucosal involvement [oral blisters or lesions], conjunctivitis, facial edema, hepatitis, eosinophilia, angioedema, difficulty breathing, bronchospasm, rash/urticaria, dizziness, pain (eg, back and chest)
- Postmarketing experience with rilpivirine-containing regimens has included drug reaction with eosinophilia and systemic symptoms (DRESS)
- Monitor clinical status, including liver transaminases, and initiate appropriate therapy as warranted
Postinjection reactions
- Serious postinjection reactions were reported within minutes after injection of rilpivirine
- Symptoms included dyspnea, agitation, abdominal cramping, flushing, sweating, oral numbness, and changes in blood pressure
- Symptoms began to resolve within minutes after injection, with some patients receiving supportive care
- These events may have been associated with accidental IV administration during IM injection procedure
- Carefully follow Instructions for Use when preparing and administering
- Slowly inject suspensions via IM injection, and avoid accidental IV administration
- Observe patients briefly (~10 minutes) after the injection
- If postinjection reaction occurs, monitor, and treat as clinically indicated
Drug interaction overview
- Caution if coadministered with drugs that may cause torsade de pointes
-
Other antiretroviral medications for HIV-1 infection
- Cabotegravir plus rilpivirine is a complete ART regimen
- Coadministration with other ARTs is not recommended
- Residual concentrations of IM cabotegravir and rilpivirine may remain in the systemic circulation of patients for prolonged periods (up to 12 months or longer); these residual concentrations are not expected to affect the exposures of ARTs initiated after discontinuation of cabotegravir and rilpivirine
-
UGT1A1 or UGT1A9 inducers
- Contraindicated
- Cabotegravir is primarily metabolized by UGT1A1 with some contribution from UGT1A9
- Strong UGT1A1 or 1A9 inducers are expected to decrease cabotegravir plasma concentrations and may result in loss of virologic response
-
CYP3A inducers
- Contraindicated
- Rilpivirine is primarily metabolized by CYP3A
- Strong CYP3A inducers are contraindicated with rilpivirine owing to concern for decreased rilpivirine plasma concentrations and potential loss of virologic response
-
QT-prolonging drugs or strong CYP3A inhibitors
- Caution if coadministered with drugs that prolong QT interval or drugs that may raise rilpivirine systemic exposure
- QT prolongation may occur with rilpivirine peak plasma concentrations 4.4-fold and 11.6-fold higher than those observed with rilpivirine 600 IM qMonth
-
Macrolide or ketolide antibiotics
- Macrolides are expected to increase rilpivirine concentrations and are associated with torsade de pointes
- When possible, consider azithromycin, which increases rilpivirine concentrations less than other macrolides
-
Polyvalent cation-containing products
- Modify dosage schedule
- Coadministration with antacids containing polyvalent cations (eg, aluminum, magnesium hydroxide, calcium carbonate) may decrease cabotegravir absorption
- Administer antacids at least 2 hr before or 4 hr after taking cabotegravir
Pregnancy & Lactation
Pregnancy
Encourage patients to register for the Antiretroviral Pregnancy Registry (APR) by calling 1-800-258-4263
Data are insufficient regarding use during pregnancy to adequately assess drug-associated risk of birth defects and miscarriage
While there are insufficient human data to assess the risk of neural tube defects (NTDs) with exposure to cabotegravir during pregnancy, NTDs were associated with dolutegravir, another integrase inhibitor
Cabotegravir and rilpivirine are detected in systemic circulation for up to 12 months or longer after discontinuing; therefore, consider potential for fetal exposure during pregnancy
Rilpivirine human data
- Prospective reports to APR to PO rilpivirine-containing regimens during the first trimester of pregnancy (>390 reports) and during second/third trimester of pregnancy (>170 reports), the prevalence of birth defects was 1.3% and 1.1% following first and second/third trimester exposures, respectively, compared with the background birth defect rate of 2.7% in the US reference population
Lactation
Unknown if present in human breast milk, affects human milk production, or effects on breastfed infants
CDC recommends that women in the United States should not breastfeed their infants because of risk of the following H4
Postnatal HIV transmission (in HIV-negative infants)
Developing viral resistance (in HIV-positive infants)
Adverse reactions in nursing infants
Animal data
- Animal lactation studies have not been conducted; however, cabotegravir and rilpivirine were detected in plasma of nursing pups on lactation days 10 and 7 respectively in rat prenatal and postnatal development study
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
Cabotegravir: HIV-1 integrase strand transfer inhibitor (INSTI); cabotegravir, an analog of dolutegravir, prevents viral DNA integration into the host genome and inhibits HIV replication
Rilpivirine: Non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1; inhibits HIV-1 replication by noncompetitive inhibition of HIV-1 reverse transcriptase
Absorption
Peak plasma time
- Cabotegravir: 7 days
- Rilpivirine: 3-4 days
Peak plasma concentration
- Cabotegravir, monthly IM: 4.2 mcg/mL
- Rilpivirine, monthly IM: 116 ng/mL
AUC
- Cabotegravir, monthly IM: 2,415 mcg⋅h/mL
- Rilpivirine, monthly IM: 65,603 ng⋅h/mL
Distribution
Protein bound: >99%
Metabolism
Cabotegravir: Metabolized by UGT1A1 (major) and UGT1A9 (minor)
Rilpivirine: Metabolized primarily by CYP3A
Elimination
Half-life
- Cabotegravir: 5.6-11.5 weeks
- Rilpivirine: 13-28 weeks
Excretion
- Cabotegravir: Urine 27%; feces 59%
- Rilpivirine: Urine 6%; feces 85%
Administration
IM Preparation
Remove from refrigerator and wait at least 15 minutes to allow vials to come to room temperature; not to exceed 25ºC (77ºF)
Vials may remain in the carton at room temperature for up to 6 hr; discard if not used within 6 hr
Inspect visually for particulate matter and discoloration before administration; cabotegravir vial has a brown tint to the glass which may limit visual inspection
Shake each vial vigorously until suspensions look uniform before injecting; small air bubbles are expected and acceptable
Do not mix with any other product or diluent
Once cabotegravir and rilpivirine suspensions have been drawn into their separate syringes, administer as soon as possible; suspension may remain in syringes for up to 2 hr; discard if 2 hr exceeded
IM Administration
Suspension are for gluteal intramuscular injections
No further dilution or reconstitution needed
Ventrogluteal site recommended; administer each injection at separate gluteal injection sites (on opposite sides or 2 cm apart) during the same visit
Do not administer by any other route or anatomical site
Consider patient’s BMI to ensure needle length is sufficient to reach the gluteus muscle; longer needle lengths (not included in the dosing kit) may be required for patients with higher BMI (eg, >30 kg/m2) to ensure that injections are administered IM as opposed to SC
Administration order of cabotegravir and rilpivirine injections is not important
Monitor patient for 10 minutes after injection to observe for injection related adverse effects
Missed injections on monthly dosing schedule
- Adherence to dosing schedule is strongly recommended to avoid viral resistance
- Reassess patients to ensure resumption of therapy remains appropriate
-
Plan to miss scheduled injection > 7 days
- Cabotegravir 30 mg plus rilpivirine 25 mg PO qDay for up to 2 months to replace missed injection visits
- Take first dose ~1 month after last injection and continue until day injection dosing is restarted
-
Missed or delayed monthly injections >7 days and no interim PO therapy
- Clinically reassess patient to determine if resumption remains appropriate
- If injection dosing continues, see below for resuming IM injection dosing
- Time since last injection ≤2 months: Resume cabotegravir 400 mg and rilpivirine 600 mg IM
- Time since last injection >2 months: Reinitiate with cabotegravir 600 mg and rilpivirine 900 mg IM once, then continue to follow with cabotegravir 400 mg and rilpivirine 600 mg IM qMonth
Missed injections on every 2-month dosing schedule
- Adherence to dosing schedule is strongly recommended to avoid viral resistance
- Reassess patients to ensure resumption of therapy remains appropriate
-
Plan to miss scheduled injection >7 days
- Cabotegravir 30 mg plus rilpivirine 25 mg PO qDay for up to 2 months to replace 1 missed injection visit
- Take first dose ~2 months after last injection and continue until day injection dosing is restarted
-
Missed or delayed monthly injections >7 days and no interim PO therapy
- Clinically reassess patient to determine if resumption remains appropriate
- If injection dosing continues, see below for resuming IM injection dosing for injection 2 (month 3), injection 3 (month 5), or thereafter
- Time since last injection ≤2 months: Resume cabotegravir 600 mg and rilpivirine 900 mg IM as soon as possible, then continue every 2 months thereafter
- Time since last injection >2 months: Reinitiate with cabotegravir 600 mg and rilpivirine 900 mg IM once, followed by second initiation injection dose 1 month later; continue to follow every 2 months thereafter
Storage
Kit
- Refrigerate at 2-8ºC (36-46ºF) in original carton until ready to use
- Vial stoppers are not made with natural rubber latex
- Do not freeze
- Do not mix with any other product or diluent
- Vials removed from refrigerator may be stored at room temperature (not to exceed 25ºC [77ºF]) in the carton at room temperature for up to 6 hr; do not return to refrigerator
- Discard if not used within 6 hr
Drawn suspensions
- Administer as soon as possible, but may remain in syringe for up to 2 hr
- Do not return to refrigerator
- Discard filled syringes and needles if stored >2 hr
Images
Formulary
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- View the formulary and any restrictions for each plan.
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