Cardiovascular Safety of 5Ht<sub>1B/1D</sub> Agonists—Is There a Cause for Concern?

Dahlöf, Carl; Mathew, N. T.

doi:10.1046/j.1468-2982.1998.1808539.x

Cited by 53 publications

(32 citation statements)

References 55 publications

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“…Chest symptoms, generally a sensation of pressure or tightness, are a well recognised side effect of sumatriptan [10], although generally these symptoms do not appear to be related to cardiovascular abnormalities [24]. Chest symptoms have also been reported with other triptans [16, 17, 18, 19, 20, 21, 22, 23].…”

Section: Discussionmentioning

confidence: 99%

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

Pascual¹,

Falk

Docekal³

et al. 2001

Eur Neurol

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Background: Almotriptan is a highly specific 5-HT_1B/1D receptor agonist, which acts selectively on blood vessels of the brain. Short-term studies have demonstrated that almotriptan provides rapid, effective and reliable relief of migraine attacks, while offering excellent tolerability. Purpose: To assess the long-term tolerability and efficacy of oral almotriptan 12.5 mg administered for every migraine attack over a 1-year period. Methods: A total of 762 patients treated 13,751 attacks (1–97 per patient); 61.5% of attacks were treated with one 12.5-mg dose, while for 38.5% of attacks, patients took a second dose within 24 h. Results: Three hundred and ninety-one patients (51.3%) experienced a total of 1,617 adverse events (AEs). The majority (88.6%) of AEs were of mild-to-moderate intensity, and only 28.8% of AEs were considered to be related to the study drug. Only 2 patients experienced serious AEs possibly related to almotriptan, syncope and chest pain; both recovered without any sequelae. Patients reported at least 1 AE in 11% of attacks treated. The incidence of AEs decreased during the study. Only 6 (0.8%) study withdrawals were due to AEs considered to be related to almotriptan. Tolerability was not compromised in patients taking 2 doses of almotriptan or in those using migraine prophylactics. Patient age or sex did not influence the incidence of AEs. There was no evidence of tachyphylaxis in those patients completing the study. Pain relief at 2 h after the initial dose was achieved in 84.2% of moderate/severe attacks. Patients were pain free at 2 h after dose in 58.2% of all attacks. Older patients (>40 years) tended to respond better than younger ones (<40 years). Efficacy was not modified by use of migraine prophylactics or hormonal contraceptives. Efficacy measurements were consistent on treating repeated moderate/severe migraine attacks. Conclusion: This large, open study indicates that the new, specific 5-HT_1B/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.

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Section: Discussionmentioning

confidence: 99%

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

Pascual¹,

Falk

Docekal³

et al. 2001

Eur Neurol

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“…For example, this may be experienced as a burning and painful sensation in the skin when taking a normally tempered shower or a dislike of being touched, especially after injection of the sumatriptan [52][53][54]. Furthermore, triptans seem to facilitate ongoing afferent nociceptive sensory nerve activity or how it is perceived [42,52,[54][55][56]. For example, the pain associated with arthritis, burned skin, gastritis, infection, or severe headache has been reported to be enhanced for a shorter (minutes) or longer (hours) time with triptan treatment [57].…”

Section: Triptansmentioning

confidence: 99%

“…The mechanism behind triptan-induced allodynia/hyperalgesia is unknown, but possibly could be due to an altered function of primary afferent fibers [42,58]. This type of triptan-induced allodynia also may provide a plausible explanation for side effects that are typical for this class of drugs, such as pressure, tightness, or pain in the chest, neck, or throat [52,54,56,57,59,60].…”

Section: Triptansmentioning

confidence: 99%

Cutaneous allodynia and migraine: Another view

Dahlöf¹

2006

Current Science Inc

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The paradigm of early treatment of the migraine attack at mild pain intensity has become one alternative to circumventing the problem of compromised oral absorption of symptomatic drugs due to migraine-induced gastrointestinal dysmotility. Early treatment also has been proposed to be advantageous because most migraineurs could be less responsive to delayed treatment, owing to the development of central sensitization of the trigeminal pain transmission. Ranking the underlying principles, it seems that the improved response to an oral triptan formulation at mild migraine symptom intensity has more to do with less impaired gastrointestinal absorption in the early stage of the attack than decreasing the time and preventing chances for central sensitization and development of cutaneous allodynia. Furthermore, parenteral administration of a triptan is always more likely to provide relief of symptoms than conventional tablets, even when it is used later in the course of the migraine attack. Individually tailored use of the available triptan formulations will increase, without any doubt, the within-migraineur consistency of response. It also will reduce the overall proportion of migraine attacks or migraineurs not responding to triptan treatment. Notwithstanding, the recommendation of early treatment during the migraine attack when the pain is mild remains valid.

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“…Patients also may experience a warm/hot sensation, tightness, tingling, flushing, and feelings of heaviness or pressure in areas such as the face, limbs, and chest [60,61]. These events have been designated "triptan sensations" because they appear to occur with all of the sumatriptanlike compounds that have been developed.…”

Section: Safety and Tolerabilitymentioning

confidence: 99%

Non-oral formulations of triptans and their use in acute migraine

Dahlöf¹

2005

Current Science Inc

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The introduction of triptans (5-HT (1B/1D) agonists) into clinical practice has expanded the therapeutic options for doctors treating migraine sufferers. The triptans are available in several different formulations such as conventional oral tablets, orally disintegrating wafers, subcutaneous injections, nasal sprays, and suppositories, which provide an excellent opportunity to tailor therapy to individual patients' needs. Although the oral formulations are the most popular with patients, they are not the most appropriate route of administration for drug delivery during the migraine attack. Due to gastrointestinal dysmotility, the intestinal absorption of any triptan administered orally may be impaired and treatment effects become inconsistent. For this reason, triptans preferably should be prescribed in a non-oral formulation (injection, nasal spray, or suppository). Parenteral administration of a triptan is more likely to provide relief of symptoms, even when it is used later in the course of the migraine attack.

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Cardiovascular Safety of 5Ht_1B/1D Agonists—Is There a Cause for Concern?

Cited by 53 publications

References 55 publications

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

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

Cutaneous allodynia and migraine: Another view

Non-oral formulations of triptans and their use in acute migraine

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

Cited by 53 publications

References 55 publications

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

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

Cutaneous allodynia and migraine: Another view

Non-oral formulations of triptans and their use in acute migraine

Contact Info

Product

Resources

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Cardiovascular Safety of 5Ht_1B/1D Agonists—Is There a Cause for Concern?