Carbamazepine with Dolutegravir Interaction Details

Brand Names Associated with Carbamazepine

Brand Names Associated with Dolutegravir

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Nov 25, 2023

Interaction Effect

Reduced dolutegravir exposure and reduced efficacy of dolutegravir

Interaction Summary

CarBAMazepine (a CYP3A and UGT1A1 inducer) coadministered with dolutegravir (CYP3A and UGT1A1 substrate) significantly reduced dolutegravir exposure (AUC by 49%, Cmax by 33%), shortened t(1/2) from 12.9 to 7.31 hours, and increased clearance by 95%. Dolutegravir dose adjustment is required in adult and pediatric patients . Whenever possible, use alternatives to carBAMazepine in INSTI-experienced patients with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance . When administering dolutegravir-containing combination products, separate the additional dolutegravir dose by 12 hours.

Severity

Major

Onset

Unspecified

Evidence

Established

How To Manage Interaction

If concomitant use of carBAMazepine and dolutegravir is required, adjust the dolutegravir dose to 50 mg twice daily in treatment-naive or treatment-experienced, integrase strand transfer inhibitor (INSTI)-naive adults and in pediatric patients 25 kg or greater . In pediatrics weighing 6 to less than 25 kg, administer an additional weight-based dose of dolutegravir; (6 to less than 10 kg) 15 mg; (10 to less than 14 kg) 20 mg; (14 to less than 20 kg) 25 mg; (20 to less than 25 kg) 30 mg . Whenever possible, use alternative agents for carBAMazepine in INSTI-experienced patients with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance . When administering dolutegravir-containing combination products, separate the additional dolutegravir dose by 12 hours .

Mechanism Of Interaction

Induction of CYP3A-mediated dolutegravir metabolism by carBAMazepine

Literature Reports

A) carBAMazepine (a CYP3A and UGT1A1 inducer) coadministered with dolutegravir (a CYP3A and UGT1A1 substrate) compared with dolutegravir administered alone significantly reduced mean dolutegravir AUC(0 to tau) from 53.8 to 27.4 mcg x hr/mL, Cmax from 4.16 to 2.77 mcg/mL, plasma concentration at the end of the dosing interval from 1.2 to 0.325 mcg/mL, and t(1/2) from 12.9 to 7.31 hours. Dolutegravir clearance was significantly increased from 0.929 to 1.83 L/hr. Healthy subjects (N=14) received dolutegravir 50 mg daily plus carBAMazepine 300 mg every 12 hours for 5 days .

B) The coadministration of carBAMazepine 300 mg twice daily in patients treated with dolutegravir 50 mg/day significantly decreased the dolutegravir Cmax by 33% and AUC by 49% compared with dolutegravir alone .

Carbamazepine Overview

• Carbamazepine is used alone or in combination with other medications to control certain types of seizures in people with epilepsy. It is also used to treat trigeminal neuralgia (a condition that causes facial nerve pain). Carbamazepine extended-release capsules (Equetro brand only) are also used to treat episodes of mania (frenzied, abnormally excited or irritated mood) or mixed episodes (symptoms of mania and depression that happen at the same time) in patients with bipolar I disorder (manic-depressive disorder; a disease that causes episodes of depression, episodes of mania, and other abnormal moods). Carbamazepine is in a class of medications called anticonvulsants. It works by reducing abnormal electrical activity in the brain.

Dolutegravir Overview

• Dolutegravir is used with other medications to treat human immunodeficiency virus (HIV) infection in adults and children 4 weeks of age and older who weigh at least 6.6 lbs (3 kg). It is also used in combination with rilpivirine (Edurant) to treat HIV in certain adults to replace their current HIV medication(s) that has been taken for at least 6 months. Dolutegravir is in a class of medications called HIV integrase inhibitors. It works by decreasing the amount of HIV in your blood and increasing the number of immune cells that help fight infections in your body. Although dolutegravir does not cure HIV, using it along with other medications may decrease your chance of developing acquired immunodeficiency syndrome (AIDS) and HIV-related illnesses such as serious infections or cancer. Taking these medications along with practicing safer sex and making other lifestyle changes may decrease the risk of transmitting (spreading) the HIV virus to other people.

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Definitions

Severity Categories

Contraindicated

These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.

Major

This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.

Moderate

This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.

Minor

While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.

Onset

Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.

Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.

Evidence

Level of documentation of the interaction.

Established: The interaction is documented and substantiated in peer-reviewed medical literature.

Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.

How To Manage The Interaction

Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.

It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.

Mechanism Of Interaction

The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.

Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.

Where Does Our Information Come From?

Information for our drug interactions is compiled from several drug compendia, including:

• Gold Standard Drug Database
• Micromedex
• Lexicomp
• DrugBank

The prescribing information for each drug, as published on DailyMED, is also used. 

Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.

The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.