Ketoconazole with Almotriptan Interaction Details
Brand Names Associated with Ketoconazole
- Ketoconazole
- Nizoral®
Brand Names Associated with Almotriptan
- Almotriptan
- Axert®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Dec 02, 2023
Interaction Effect
Increased almotriptan exposure
Interaction Summary
In a randomized, open-label, two-way, crossover pharmacokinetic study (n=16), a clinically significant increase in the Cmax (61%) and AUC (57%) of almotriptan (a CYP3A4 substrate) was observed with concomitant administration of ketoconazole (a potent CYP3A4 inhibitor); however, there were no associated changes to the adverse event profile and vital signs associated with almotriptan administration. A starting dose of almotriptan 6.25 mg and a maximum daily dose of almotriptan 12.5 mg is recommended in patients receiving concomitant therapy with a potent CYP3A4 inhibitor, such as ketoconazole; concomitant use of these agents should be avoided in patients with renal or hepatic impairment .
Severity
Moderate
Onset
Delayed
Evidence
Established
How To Manage Interaction
The concomitant administration of almotriptan and ketoconazole (a strong CYP3A4 inhibitor) may cause increased exposure to almotriptan. Use a starting dose of almotriptan 6.25 mg and a maximum daily dose of almotriptan 12.5 mg in patients receiving concomitant therapy with a potent CYP3A4 inhibitor, such as ketoconazole. In patients with renal or hepatic impairment, concomitant use of almotriptan and potent CYP3A4 inhibitors should be avoided. Monitor patients for signs and symptoms of increased almotriptan levels including hypertension and arrhythmias.
Mechanism Of Interaction
Inhibition of CYP3A4-mediated almotriptan metabolism
Literature Reports
A) A statistically significant increase in maximum plasma concentration (Cmax) and area under the concentration-time curve (AUC) of almotriptan was observed with concomitant administration of ketoconazole. Sixteen volunteers were included in a randomized, open-label, two-way crossover study. Each subject received both of the following treatments with a 1-week washout period: (A) ketoconazole 400 mg on day 1 to 3 and almotriptan 12.5 mg on day 2 and (B) almotriptan 12.5 mg on day 2. The mean AUC for almotriptan was increased by 57% with concomitant ketoconazole administration, and the mean Cmax was increased by 61%. Oral clearance and volume of distribution of almotriptan were decreased with ketoconazole coadministration. Renal clearance of almotriptan was reduced approximately 16% by ketoconazole. While the effects were clinically significant, there were no associated changes to the adverse event profile and vital signs associated with almotriptan administration. Based on these results, no dosage adjustment is necessary when ketoconazole and almotriptan are coadministered .
Ketoconazole Overview
-
Ketoconazole is used to treat fungal infections when other medications are not available or cannot be tolerated. Ketoconazole should not be used to treat fungal meningitis (infection of the membranes surrounding the brain and spinal cord caused by a fungus) or fungal nail infections. Ketoconazole is in a class of antifungals called imidazoles. It works by slowing the growth of fungi that cause infection.
Almotriptan Overview
-
Almotriptan is used to treat the symptoms of migraine headaches (severe, throbbing headaches that sometimes are accompanied by nausea and sensitivity to sound and light). Almotriptan is in a class of medications called selective serotonin receptor agonists. It works by narrowing blood vessels around the brain, stopping pain signals from being sent to the brain, and blocking the release of certain natural substances that cause pain, nausea, and other symptoms of migraine. Almotriptan does not prevent migraine attacks or reduce the number of headaches you have.
Return To Our Drug Interaction Homepage
Feedback, Question Or Comment About This Information?
Ask Dr. Brian Staiger, PharmD, our medical editor, directly! He's always more than happy to assist.
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.