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The Triptan Formulations

How to Match Patients and Products

  • Therapy in Practice
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Abstract

The 5-HT1b/1d receptor agonists (the ‘triptans’) are migraine-specific agents that have revolutionised the treatment of migraine. They are usually the drugs of choice to treat a migraine attack in progress. Different triptans are available in various strengths and formulations, including oral tablets, orally disintegrating tablets, nasal sprays and subcutaneous injections. In Europe, sumatriptan is also available as a suppository.

Specific differences among the triptans exist, as evidenced by different pharmacological profiles including half-life, time to peak plasma concentrations, peak plasma concentrations, area under the concentration-time curve, metabolism and drug-drug interaction profiles. How or whether these differences translate to clinical efficacy and tolerability advantages for one agent over another is not well differentiated. However, delivery systems may play an important role in onset of action.

Given that the clinical distinctions among these agents are subtle, identification of the most appropriate triptan for an individual patient requires consideration of the specific characteristics of the patient and knowledge of patient preference, an accurate history of the efficacy of previous acute-care medications and individual features of the drug being considered. The selection of an acute antimigraine drug also depends upon the stratification of the patient’s migraine attack by peak intensity, time to peak intensity, level of associated symptoms such as nausea and vomiting, time to associated symptoms, comorbid diseases and concomitant treatments that might cause drug-drug interactions.

Individual patient response to the triptans seems to be idiosyncratic and possibly genetically determined. Therefore, a set of specific questions can be used to determine whether a currently used triptan is optimally effective, whether the dose needs to be increased or whether another triptan should be tried.

The clinician has in his/her armamentarium an ever-expanding variety of triptans, available in multiple formulations and dosages, which have good safety and tolerability profiles. Continued clinical use will yield familiarity with the various triptans, and it should become possible for the interested physician to match individual patient needs with the specific characteristics of a triptan to optimise therapeutic benefit. Use of the methods outlined in this review in choosing a triptan for an individual patient is probably more likely to lead to migraine relief than making an educated guess as to which triptan is most appropriate.

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Article Open access 03 April 2023

Raghavendra Ramachanderan, Stefan Schramm & Bernd Schaefer

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Acknowledgements

This study was conducted without financial support. The authors have participated in research and/or lectures sponsored by GlaxoSmithKline, AstraZeneca, Merck Sharpe & Dohme, Pfizer and other major pharmaceutical companies.

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Authors and Affiliations

  1. Department of Neurology, College of Physicians and Surgeons, Columbia University, New York, New York, USA

    Alan M. Rapoport

  2. The New England Center for Headache, P.C., 778 Long Ridge Road, Stamford, Connecticut, 06902-1251, USA

    Alan M. Rapoport, Stewart J. Tepper, Marcelo E. Bigal & Fred D. Sheftell

  3. Department of Neurology, Yale University School of Medicine, New Haven, Connecticut, USA

    Stewart J. Tepper

  4. Department of Neurology, Albert Einstein College of Medicine, New York, New York, USA

    Marcelo E. Bigal

  5. New York Medical College, New York, New York, USA

    Fred D. Sheftell

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  1. Alan M. Rapoport
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Correspondence to Alan M. Rapoport.

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Rapoport, A.M., Tepper, S.J., Bigal, M.E. et al. The Triptan Formulations. CNS Drugs 17, 431–447 (2003). https://doi.org/10.2165/00023210-200317060-00005

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