Cardiovascular Safety of 5Ht1B/1D Agonists—Is There a Cause for Concern?

@article{Dahlf1998CardiovascularSO,
  title={Cardiovascular Safety of 5Ht1B/1D Agonists—Is There a Cause for Concern?},
  author={Carl G. H. Dahl{\"o}f and Nirmal Mathew},
  journal={Cephalalgia},
  year={1998},
  volume={18},
  pages={539 - 545}
}
Several well-controlled clinical trials have been perfonned in patient populations where the 5HT18/10 agonist sumatriptan (tablet or subcutaneous injection) has been convincingly demonstrated to have good efficacy in the acute treatmern t of lrJgraine attacks (1, 2). On average, three out of four patients have become totally painfree or have obtained considerable relief from headache, nausea, and photophobia (I, 2). Prescribing procedures for surnatriptan differ from cou....,tryto cO'Jntrj, but… 

Tolerability of the Triptans

A report on a very large population of patients tested during clinical trials and in postmarketing studies, confirms that these triptans are safe and well tolerated when correctly used.

Sumatriptan: Pharmacological Basis and Clinical Results

  • C. Dahlöf
  • Medicine
    Current medical research and opinion
  • 2001
All triptans appear to be very similar with respect to efficacy and tolerability as well as safety in clinical practice, in particular after dose adjustments have been made.

Rizatriptan: a new 5-HT1B/1D receptor agonist for the treatment of migraine.

Rizatriptan is an effective and well-tolerated acute treatment for migraine, which may offer some advantages over oral sumatripta, which has a shorter Tmax and greater bioavailability.

Tolerability and Efficacy of Almotriptan in the Long-Term Treatment of Migraine

This large, open study indicates that the new, specific 5-HT1B/1D agonist almotriptan, at a dose of 12.5 mg, is a well tolerated and effective treatment for migraine pain when used over a period of up to 1 year.

Integrating the triptans into clinical practice

  • C. Dahlöf
  • Medicine, Psychology
    Current opinion in neurology
  • 2002
The triptans are becoming the first‐line alternatives in the acute pharmacological treatment of migraine, at least for attacks of moderate‐to‐severe intensity, and the tablet is the most commonly used triptan formulation.

Pharmacokinetics and Pharmacodynamics of the Triptan Antimigraine Agents

The pharmacological properties of the triptans (time to peak plasma concentration, half-life, bioavailability and receptor binding) are reviewed and related to efficacy and time of onset and the effects of concomitant medication, food, age and disease are considered.

Safety Trial with the 5Ht1B/1D Agonist Avitriptan (BMS-180048) in Patients with Migraine who have Experienced Pressure, Tightness, and/or pain in the Chest, Neck, and/or throat following Sumatriptan

It is concluded that the typical 5HT1B/1D agonist-induced chest/throat/neck symptoms are most unlikely to be of cardiovascular origin.

The safety of triptans in the treatment of patients with migraine.

  • D. Jamieson
  • Medicine, Psychology
    The American journal of medicine
  • 2002

Over-the-Counter Triptans for Migraine

The availability of triptans OTC is a logical development for the better management of a common, benign, self-limiting but nonetheless burdensome disorder that is currently grossly undertreated.
...

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311C90: Increasing the options for therapy with effective acute antimigraine 5HT1B/1D receptor agonists

Clinical studies have shown 311C90 to be rapidly and consistently effective in relieving migraine headache, with initial doses of between 2.5 and 5 mg providing an optimal balance between efficacy and safety considerations.

Tolerability Profile of Zolmitriptan (Zomig™; 311C90), a Novel Dual Central and Peripherally Acting 5HT1B/1D Agonist: International Clinical Experience Based on > 3000 Subjects Treated with Zolmitriptan

Zolmitriptan is well tolerated, particularly at the recommended dose of 2.5 mg, and is well suited as an acute oral treatment for migraine in the outpatient setting, and has a well-defined dose-response, proving highly effective and optimizing the benefit/risk ratio of treatment.

Tolerability profile of zolmitriptan (Zomig; 311C90), a novel dual central and peripherally acting 5HT1B/1D agonist. International clinical experience based on > 3000 subjects treated with zolmitriptan.

Zolmitriptan is well tolerated, particularly at the recommended dose of 2.5 mg, and is well suited as an acute oral treatment for migraine in the outpatient setting, despite pre-clinical and neurophysiological evidence of a dual peripheral and central action of zolMITriptan.

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A central action now proved experimentally in animals and in humans for 5-HT1B/D agonists such as zolmitriptan may be advantageous for the antimigraine efficacy, but it could also increase sedation.

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Oral administration of sumatriptan 100mg consistently achieved significantly greater response rates than a fixed combination of ergotamine 2mg plus caffeine 200mg during 3 consecutive migraine attacks and was also more effective than aspirin 900mg plus metoclopramide 10mg orally in a similar study.

Zolmitriptan, a 5‐HT1B/1D receptor agonist for the acute oral treatment of migraine: a multicentre, dose‐range finding study

The dose response data suggest that lower doses of oral zolmitriptan would also offer significant efficacy, and the most commonly reported adverse events were asthenia, dizziness, paraesthesia and feelings of heaviness.

Safety Trial with the 5Ht1B/1D Agonist Avitriptan (BMS-180048) in Patients with Migraine who have Experienced Pressure, Tightness, and/or pain in the Chest, Neck, and/or throat following Sumatriptan

It is concluded that the typical 5HT1B/1D agonist-induced chest/throat/neck symptoms are most unlikely to be of cardiovascular origin.

Long-term experience with sumatriptan in the treatment of migraine.

In long-term studies the high efficacy of sumatriptan is maintained, and the adverse event profile is unchanged and unaffected by attack frequency, which is consistent with previous studies.

How Does Sumatriptan Nasal Spray Perform in Clinical Practice?

The overall impression of sumatriptan nasal spray is that it is user friendly and useful in the acute treatment of migraine attacks of moderate intensity.

Sumatriptan. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the acute treatment of migraine and cluster headache.

Pooled data from nearly 5000 patients treated with either oral or subcutaneous sumatriptan in clinical trials indicate that it is well tolerated, however, migraine recurrence within 24 or 48 hours of initial symptom resolution developed in approximately 40% of patientstreated with sum atriptan, irrespective of route of administration.
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