The Clinical Profile of Sumatriptan: Safety and Tolerability

Lloyd, Kate

doi:10.1159/000119531

Cited by 30 publications

(16 citation statements)

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“…As reported in previous studies (Ferrari 1996;Visser et al 1996), zolmitriptan was associated with mild and short-lived feelings of tightness or heaviness in the neck, jaw or throat which appear to be characteristic of this class of compound (Lloyd 1994). The frequency and duration, but not intensity, of these e¤ects was related to dose, and so could be expected to be reported not only as mild and transient, but as having a low incidence at clinically relevant doses (Ferrari 1996;Visser et al 1996).…”

Section: Discussionsupporting

confidence: 55%

Lack of an effect of zolmitriptan (Zomig, 311C90) on psychometric task performance: results of a placebo-controlled study in healthy volunteers

Mercer

Lamb

Rolan³

et al. 1998

Psychopharmacology

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The novel selective 5-hydroxytryptamine (5-HT)1B/1D agonist, zolmitriptan (Zomig, formerly known as 311C90), has shown good efficacy in the acute oral treatment of migraine. Zolmitriptan acts both centrally and peripherally, therefore it is important to assess central nervous system effects. At single doses of 25-50 mg (up to 8 times the likely therapeutic dose), zolmitriptan can cause sedation; therefore, a study was designed to examine the dose-response. A double-blind, randomized, placebo-controlled, six-limb crossover study in 13 healthy volunteers compared the effects of single oral doses of zolmitriptan (5, 10, 15 or 20 mg) and lorazepam (2 mg) on various psychometric tests. Zolmitriptan doses less than 20 mg had no statistically significant effects on choice reaction time, the Stroop test, visual analog scale (VAS) assessments of physical sedation, tranquilization and other types of feelings, the logical reasoning test or the adaptive tracking test. There was a mild transient increase in the subjective assessment on VAS of mental sedation which was dose related and occurred mainly with the highest zolmitriptan dose and were not reflected in objective measures of drug effects. In contrast, lorazepam (used as a positive control) was associated with statistically significant impairment in all tests (except tranquilization) for up to 10 h after dosing. The results demonstrate that therapeutic doses of zolmitriptan are unlikely to cause clinically significant impairment in psychometric performance.

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Section: Discussionsupporting

confidence: 55%

Lack of an effect of zolmitriptan (Zomig, 311C90) on psychometric task performance: results of a placebo-controlled study in healthy volunteers

Mercer

Lamb

Rolan³

et al. 1998

Psychopharmacology

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“…The adverse events reported were typical of this class of compound (22,23) and there was no trend for adverse events to be more frequent with any of the treatment combin a t' ions.…”

Section: Pharmacodynamic Interactionsmentioning

confidence: 83%

Potential drug interactions with the novel antimigraine compound zolmitriptan (Zomig™, 311C90)

Rolan

1997

Cephalalgia

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Seven randomized studies in healthy volunteers have investigated interactions between zolmitriptan (Zomig, formerly 311C90), a 5HT1B/1D agonist for acute migraine therapy, and selected drugs with which there was a possibility of interaction or a likelihood of concurrent use. Co-administration of oral dihydroergotamine, ergotamine, pizotifen, fluoxetine, paracetamol (acetaminophen)/metoclopramide or selegiline had no clinically significant effects on the pharmacokinetics of zolmitriptan or its metabolites, although small changes were observed in some cases. Co-administration of propranolol resulted in a 56% increase in the area under the plasma concentration-time curve (AUC) of zolmitriptan and a 11% decrease in the AUC of the active metabolite 183C91. However, these pharmacokinetic changes are unlikely to be relevant at lower clinical doses. Moclobemide, a monoamine oxidase A (MAO-A) inhibitor, decreased the clearance of zolmitriptan and, in particular, 183C91. This suggests that MAO-A is involved in the metabolism of 183C91 and it may be prudent to limit the daily zolmitriptan dose in migraine patients maintained on a MAO-A inhibitor. The clinically insignificant blood pressure increases produced by zolmitriptan, and the tolerability profile of this agent, were unaffected by any of the concomitant medications. Clinically significant interactions between zolmitriptan and commonly co-prescribed antimigraine therapies are unlikely.

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“…Sumatriptan, the first triptan to be approved and subsequently used to treat millions of attacks of migraine, is generally safe and well tolerated 2,3 . In placebo‐controlled, long‐term, and postmarketing surveillance studies, the most commonly reported adverse events (AEs) were nausea/vomiting, taste disturbances, dizziness/vertigo, and malaise/fatigue 2,3 . Chest symptoms (pressure, pain, and other unpleasant sensations) were another relatively common AE that many patients find disturbing.…”

mentioning

confidence: 99%

“…Chest symptoms are associated with both subcutaneous and oral sumatriptan, but are more common with subcutaneous sumatriptan 2,4 . These symptoms occurred at a rate of 3% to 5% in controlled clinical studies 2,3 . In a retrospective, postmarketing study that included nearly 28 000 attacks in outpatients attending the neurology clinic of a university hospital, chest symptoms, consisting mostly of tightness or pressure and a sensation of heavy arms, were experienced by 41% of patients following subcutaneous administration and by 24% following oral administration in all of at least five attacks 4 .…”

mentioning

confidence: 99%

Oral Almotriptan in the Treatment of Migraine: Safety and Tolerability

Dodick

2001

Headache

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Objective.—To summarize safety and tolerability data on orally administered almotriptan from premarketing clinical trials. Background.—Almotriptan is a new 5‐HT1B/1D receptor agonist similar to sumatriptan in mode of action and therapeutic efficacy. In addition, the safety and tolerability profile of almotriptan has been demonstrated in a number of controlled clinical trials. Sumatriptan is generally safe and well tolerated; however, in controlled clinical trials, it has been associated with chest symptoms (pressure, warmth, and other unpleasant sensations) with an incidence of 3% to 5%. Design.—Three phase 1 dose‐finding and pharmacokinetic studies in healthy men and women volunteers were reviewed to assess the safety and tolerability of oral almotriptan at single doses ranging from 2 to 200 mg. The objective of one study was to evaluate cardiovascular safety. Two phase 2 trials assessed the safety and tolerability of single doses of 2 to 150 mg in migraine (n=911). Two phase 3 trials assessed the safety and tolerability of a single 12.5‐mg oral dose after three attacks (n=910) and repeated doses of 12.5 mg for multiple attacks over the long term (n=747). All studies were conducted in Europe. Data from the United States is currently being analyzed and will be published at a later date. Results.—In phase 2 and 3 trials comprising more than 2500 patients with migraine and 15 000 attacks, adverse events were infrequent and mild. The most common events—dizziness, nausea and vomiting, headache, fatigue, paresthesia, and drowsiness—were reported in fewer than 3% of patients. At the recommended therapeutic dose of 12.5 mg, the adverse events profile was not statistically different from placebo. The incidence of chest symptoms was 0.2% in the phase 3 trials. The long‐term safety and tolerability profile after treatment of more than 10 000 attacks was similar to that following the single‐dose studies. In all clinical trials, almotriptan demonstrated a very favorable adverse event profile, particularly with respect to nonischemic‐related chest symptoms. Conclusions.—Almotriptan was safe and well tolerated in nearly all adult patients with migraine, with and without aura, enrolled in these studies. The incidence of chest symptoms in preclinical studies was substantially lower than that reported for sumatriptan in premarketing studies, indicating that almotriptan may be better tolerated than sumatriptan at clinically anticipated doses. However, any potential difference in cardiovascular safety between almotriptan and sumatriptan cannot be determined or inferred from this data. Cardiovascular risk profiles for all drugs within this class (triptans) should be considered similar. Only extensive postmarketing data, not currently available, can potentially change this recommendation.

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The Clinical Profile of Sumatriptan: Safety and Tolerability

Cited by 30 publications

References 0 publications

Lack of an effect of zolmitriptan (Zomig, 311C90) on psychometric task performance: results of a placebo-controlled study in healthy volunteers

Lack of an effect of zolmitriptan (Zomig, 311C90) on psychometric task performance: results of a placebo-controlled study in healthy volunteers

Potential drug interactions with the novel antimigraine compound zolmitriptan (Zomig™, 311C90)

Oral Almotriptan in the Treatment of Migraine: Safety and Tolerability

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