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Drug Interactions between cabotegravir and rifampin

This report displays the potential drug interactions for the following 2 drugs:

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Interactions between your drugs

Major

rifAMPin cabotegravir

Applies to: rifampin and cabotegravir

CONTRAINDICATED: Coadministration with inducers of uridine diphosphate glucuronosyltransferase (UGT)1A1 or 1A9 may decrease the plasma concentrations of cabotegravir. Cabotegravir is primarily metabolized by UGT1A1 and to a lesser extent by UGT 1A9. In 15 study subjects given a single 30 mg dose of cabotegravir with the UGT 1A1 inducer rifampin (600 mg once daily), mean cabotegravir peak plasma concentration (Cmax) and systemic exposure (AUC) were reduced by 6% and 59%, respectively. Loss of therapeutic efficacy of cabotegravir may occur.

MANAGEMENT: According to the manufacturer of cabotegravir, due to the potential for loss of therapeutic efficacy, its concomitant use with UGT 1A1 inducers including, but not limited to carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, and rifapentine is considered contraindicated.

References (7)
  1. (2021) "Product Information. Cabenuva (cabotegravir-rilpivirine)." ViiV Healthcare ULC
  2. (2021) "Product Information. Vocabria (cabotegravir)." ViiV Healthcare
  3. Lee LSU, Pham PA, Flexner C (2012) "Unexpected drug-drug interactions in human immunodeficiency virus (HIV) therapy: induction of UGT1A1 and bile efflux transporters by Efavirenz" National Library of Medicine, 41, p. 559-562
  4. Miners JO, Polasek TM, Hulin JA, Rowland A, Meech R (2023) "Drug-drug interactions that alter the exposure of glucuronidated drugs: Scope, UDP-glucuronosyltransferase (UGT) enzyme selectivity, mechanisms (inhibition and induction), and clinical significance" Pharmacol Ther, 248, p. 108459
  5. Song I, Borland J, Chen S, Guta P, Lou Y, Wilfret D, Wajima T, Savina P, Peppercorn AF, castellino s, wagner d, Hosking L, Mosteller M, Rubio JP (2014) "Effects of enzyme inducers efavirenz and tipranavir/ritonavir on the pharmacokinetics of the HIV integrase inhibitor dolutegravir" Eur J Clin Pharmacol, 70, p. 1173-1179
  6. Marvanova M (2016) "Pharmacokinetic characteristics of antiepileptic drugs (AEDs)" National Library of Medicine, 6, p. 8-20
  7. Lemaitre F, Grégoire M, Monchaud C, Bouchet S, Saint-Salvi B, Polard E (2022) "Management of drug-drug interactions with nirmatrelvir/ritonavir in patients treated for Covid-19: Guidelines from the French Society of Pharmacology and Therapeutics (SFPT)" National Library of Medicine, 77, p. 509-521

Drug and food interactions

Moderate

rifAMPin food

Applies to: rifampin

GENERALLY AVOID: Concurrent use of rifampin in patients who ingest alcohol daily may result in an increased incidence of hepatotoxicity. The increase in hepatotoxicity may be due to an additive risk as both alcohol and rifampin are individually associated with this adverse reaction. However, the exact mechanism has not been established.

ADJUST DOSING INTERVAL: Administration with food may reduce oral rifampin absorption, increasing the risk of therapeutic failure or resistance. In a randomized, four-period crossover phase I study of 14 healthy male and female volunteers, the pharmacokinetics of single dose rifampin 600 mg were evaluated under fasting conditions and with a high-fat meal. Researchers observed that administration of rifampin with a high-fat meal reduced rifampin peak plasma concentration (Cmax) by 36%, nearly doubled the time to reach peak plasma concentration (Tmax) but reduced overall exposure (AUC) by only 6%.

MANAGEMENT: The manufacturer of oral forms of rifampin recommends administration on an empty stomach, 30 minutes before or 2 hours after meals. Patients should be encouraged to avoid alcohol or strictly limit their intake. Patients who use alcohol and rifampin concurrently or have a history of alcohol use disorder may require additional monitoring of their liver function during treatment with rifampin.

References (6)
  1. (2022) "Product Information. Rifampin (rifAMPin)." Akorn Inc
  2. (2022) "Product Information. Rifampicin (rifampicin)." Mylan Pharmaceuticals Inc
  3. (2023) "Product Information. Rifadin (rifampicin)." Sanofi
  4. (2024) "Product Information. Rifadin (rifaMPICin)." Sanofi-Aventis Australia Pty Ltd
  5. Peloquin CA, Namdar R, Singleton MD, Nix DE (2024) Pharmacokinetics of rifampin under fasting conditions, with food, and with antacids https://pubmed.ncbi.nlm.nih.gov/9925057/
  6. (2019) "Product Information. Rofact (rifampin)." Bausch Health, Canada Inc.

Therapeutic duplication warnings

No warnings were found for your selected drugs.

Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.

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Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
Unknown No interaction information available.

Further information

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