Glyburide with Bosentan Interaction Details
Brand Names Associated with Glyburide
- DiaBeta®
- Glyburide
- Glynase®
- Micronase®
Brand Names Associated with Bosentan
- Bosentan
- Tracleer®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Nov 21, 2023
Interaction Effect
Increased risk of liver enzyme elevations
Interaction Summary
An increased risk of elevated liver aminotransferases was observed in subjects receiving bosentan concomitantly with glyBURIDE. Plasma concentrations of glyBURIDE were decreased by approximately 30% when coadministered with bosentan. Plasma concentrations of other oral hypoglycemic agents that are predominantly metabolized by cytochrome P450 2C9 or 3A4 isozyme are expected to be reduced with coadministration of bosentan. Consider the possibility of worsened glucose control in patients using these agents.
Severity
Contraindicated
Onset
Rapid
Evidence
Probable
How To Manage Interaction
Concomitant administration of bosentan and glyBURIDE is contraindicated. Alternative hypoglycemic agents should be considered.
Mechanism Of Interaction
Induction of cytochrome P450 2C9-mediated metabolism of glyBURIDE
Literature Reports
A) Concomitant administration of bosentan and glyBURIDE results in decreased exposure to both drugs. Twelve healthy subjects were enrolled in a randomized, 2-way crossover study. Treatment A consisted of bosentan 125 mg twice daily for 10 days plus glyBURIDE 2.5 mg twice daily on days 6 to 10. Treatment B consisted of glyBURIDE 2.5 mg twice daily for 10 days plus concomitant bosentan 125 mg twice daily on days 6 to 10. On days 5 and 10 of treatment A and treatment B, plasma concentrations of bosentan and its metabolites and of glyBURIDE were measured. Bosentan decreased the plasma concentration of glyBURIDE approximately 40% (p less than 0.05). GlyBURIDE decreased the AUC of bosentan and its metabolites 20% and 30% (p less than 0.05). The observed pharmacodynamic effect between bosentan and glyBURIDE cannot be explained by this pharmacokinetic study .
Glyburide Overview
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Glyburide is used along with diet and exercise, and sometimes with other medications, to treat type 2 diabetes (condition in which the body does not use insulin normally and, therefore, cannot control the amount of sugar in the blood). Glyburide is in a class of medications called sulfonylureas. Glyburide lowers blood sugar by causing the pancreas to produce insulin (a natural substance that is needed to break down sugar in the body) and helping the body use insulin efficiently. This medication will only help lower blood sugar in people whose bodies produce insulin naturally. Glyburide is not used to treat type 1 diabetes (condition in which the body does not produce insulin and, therefore, cannot control the amount of sugar in the blood) or diabetic ketoacidosis (a serious condition that may occur if high blood sugar is not treated).
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Over time, people who have diabetes and high blood sugar can develop serious or life-threatening complications, including heart disease, stroke, kidney problems, nerve damage, and eye problems. Taking medication(s), making lifestyle changes (e.g., diet, exercise, quitting smoking), and regularly checking your blood sugar may help to manage your diabetes and improve your health. This therapy may also decrease your chances of having a heart attack, stroke, or other diabetes-related complications such as kidney failure, nerve damage (numb, cold legs or feet; decreased sexual ability in men and women), eye problems, including changes or loss of vision, or gum disease. Your doctor and other healthcare providers will talk to you about the best way to manage your diabetes.
Bosentan Overview
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Bosentan is used to treat pulmonary arterial hypertension (PAH, high blood pressure in the vessels that carry blood to the lungs) in adults and children 3 years of age and older. Bosentan may improve the ability to exercise and slow the worsening of symptoms in patients with PAH. Bosentan is in a class of medications called endothelin receptor antagonists. It works by stopping the action of endothelin, a natural substance that causes blood vessels to narrow and prevents normal blood flow in people who have PAH.
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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:
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.