Sertraline with Mexiletine Interaction Details
Brand Names Associated with Sertraline
- Sertraline
- Zoloft®
Brand Names Associated with Mexiletine
- Mexiletine
- Mexitil®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Nov 08, 2023
Interaction Effect
Increased CYP2D6 substrate exposure
Interaction Summary
Concomitant use of sertraline (a CYP2D6 inhibitor) with a CYP2D6 substrate may increase the exposure of the CYP2D6 substrate. If coadministration is required, decrease the dosage of the CYP2D6 substrate as necessary; conversely, an increase in the dosage of a CYP2D6 substrate may be needed with discontinuation of sertraline.
Severity
Major
Onset
Unspecified
Evidence
Theoretical
How To Manage Interaction
Concomitant use of sertraline (a CYP2D6 inhibitor) with a CYP2D6 substrate may increase the exposure of the CYP2D6 substrate. If coadministration is required, decrease the dosage of the CYP2D6 substrate as necessary; conversely, an increase in the dosage of a CYP2D6 substrate may be needed with discontinuation of sertraline.
Mechanism Of Interaction
Inhibition of CYP2D6 substrate metabolism by sertraline
Literature Reports
A) In drug interactions studies, PARoxetine demonstrated the following effects on drugs metabolized by CYP2D6. PARoxetine 20 mg once daily at steady-state increased a single dose of desipramine 100 mg Cmax, AUC, and t(1/2) by approximately 2-, 5-, and 3-fold, respectively. In patients stabilized on risperiDONE 4 to 8 mg/day, daily PARoxetine 20 mg increased mean plasma concentrations of risperiDONE by 4-fold, decreased 9-hydroxyrisperiDONE concentrations by 10%, and increased concentrations of the active moiety by 1.4-fold. In healthy volunteers who were extensive CYP2D6 metabolizes, steady-sate atomoxetine AUC values were 6- to 8-fold higher and Cmax values were 3- to 4-fold higher with concomitant PARoxetine compared with atomoxetine alone. Mean digoxin steady-state AUC decreased by 15% in the presence of PARoxetine. In a study with propranolol 80 mg twice daily for 18 days, the steady-state plasma concentrations of propranolol were unaltered during coadministration with PARoxetine 30 mg once daily for the final 10 days .
Sertraline Overview
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Sertraline is used to treat depression, obsessive-compulsive disorder (bothersome thoughts that won't go away and the need to perform certain actions over and over), panic attacks (sudden, unexpected attacks of extreme fear and worry about these attacks), posttraumatic stress disorder (disturbing psychological symptoms that develop after a frightening experience), and social anxiety disorder (extreme fear of interacting with others or performing in front of others that interferes with normal life). It is also used to relieve the symptoms of premenstrual dysphoric disorder, including mood swings, irritability, bloating, and breast tenderness. Sertraline is in a class of antidepressants called selective serotonin reuptake inhibitors (SSRIs). It works by increasing the amounts of serotonin, a natural substance in the brain that helps maintain mental balance.
Mexiletine Overview
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Mexiletine is used to treat certain types of ventricular arrhythmias (abnormal heart rhythms). Mexiletine is in a class of medications called antiarrhythmics. It works by blocking certain electrical signals in the heart to stabilize the heart rhythm.
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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.