From the Guidelines
Sumatriptan is a prime example of a 5HT1 agonist, specifically targeting the 5HT1B and 5HT1D receptor subtypes, as noted in the study published in the American Family Physician in 2002 1. This classification places it within the triptan class of medications, which are primarily used to treat acute migraine attacks. The mechanism of action of sumatriptan involves binding to serotonin receptors in cranial blood vessels, causing vasoconstriction and reducing inflammation, while also inhibiting the release of pain-causing neuropeptides, as described in the context of migraine management 1. Key points about sumatriptan and other 5HT1 agonists include:
- They are available in multiple formulations, including oral tablets, nasal sprays, and injectable forms, which allows for flexibility in administration based on patient needs and symptoms 1.
- The efficacy of these medications can vary, with sumatriptan showing effectiveness in 70 to 82 percent of patients, according to the study 1.
- Other examples of 5HT1 agonists, such as zolmitriptan, rizatriptan, and naratriptan, have similar mechanisms but different pharmacokinetic profiles, which can influence their onset of action and duration of effect 1.
- It is crucial to consider contraindications, such as coronary artery disease, uncontrolled hypertension, and recent use of MAOIs, due to the risk of serious cardiovascular effects, as highlighted in the guidelines 1. The choice of a specific 5HT1 agonist should be guided by the patient's medical history, the characteristics of the migraine attacks, and the side effect profile of the medication, emphasizing the importance of personalized treatment plans in clinical practice 1.
From the FDA Drug Label
Eletriptan hydrobromide tablets contain eletriptan hydrobromide, which is a selective 5-hydroxytryptamine 1B/1D (5-HT1B/1D) receptor agonist. Zolmitriptan tablets, USP contain zolmitriptan USP, which is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist.
An example of a 5HT 1 agonist is eletriptan or zolmitriptan 2 3.
- Key points:
- Eletriptan and zolmitriptan are selective 5-HT1B/1D receptor agonists.
- They are used for the treatment of migraine headache.
From the Research
5HT 1 Agonist Examples
- Triptans, such as sumatriptan, zolmitriptan, rizatriptan, eletriptan, naratriptan, almotriptan, and frovatriptan, are examples of 5-HT1B/1D receptor agonists 4, 5, 6, 7, 8
- Lasmiditan is a selective 5-HT1F receptor agonist that has been shown to be effective in acute migraine treatment 4
- Ergotamine and dihydroergotamine are also 5-HT1B and 5-HT1D agonists, but they have a broader range of receptor activity and are less specific than the triptans 5
Mechanism of Action
- The mechanism of action of 5-HT1B/1D agonists involves inhibiting neurogenic inflammation, which is mediated through serotoninergic control mechanisms 8
- The binding of sumatriptan to central 5-HT1B receptors has been shown to be associated with a decrease in 5-HT1B receptor binding, which may contribute to its therapeutic effect 7