Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0018681 (headache)
 56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

In a double-blind, placebo-controlled study, the efficacy, safety and tolerability of 100 mg oral sumatriptan, given as a dispersible tablet, was compared with that of 900 mg oral aspirin plus 10 mg oral metoclopramide in the acute treatment of migraine. A total of 358 patients treated up to three migraine attacks within 3 months, recording clinical information on a diary card. In attack 1, headache relief after 2 h, defined as a reduction in severity from severe or moderate pain to mild or no pain, was recorded in 56% (74/133) of patients who took sumatriptan and 45% (62/138) of patients who took aspirin plus metoclopramide (p = 0.078). This analysis of the primary efficacy end point was not statistically significant. However, for attacks 2 and 3 (secondary end points), headache relief was achieved in 58 versus 36% of patients (p = 0.001) and 65 versus 34% of patients (p less than 0.001), respectively. Relief from nausea, vomiting, photophobia and phonophobia was similar in both treatment groups. Rescue medication was required by fewer patients treated with sumatriptan than by those who received aspirin plus metoclopramide (attack 1, 34 versus 56%, p less than 0.001; attack 2, 32 versus 51%, p = 0.001, and attack 3, 35 versus 54%, p = 0.001). Sumatriptan also produced a faster improvement and resolution of migraine attacks. Comparing the sumatriptan and aspirin plus metoclopramide treatment groups, complete resolution of the attack occurred within 6 h in 32 versus 19% (attack 1), 35 versus 23% (attack 2) and 32 versus 20% of patients (attack 3).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:A study to compare oral sumatriptan with oral aspirin plus oral metoclopramide in the acute treatment of migraine. The Oral Sumatriptan and Aspirin plus Metoclopramide Comparative Study Group. 131 94

Sumatriptan is a novel, highly effective drug against migraine and cluster headache attacks. It shows a remarkably selective pharmacological profile in animals. Determination of its mechanism of action in human should further the understanding of the pathophysiology of migraine and cluster headache. We, therefore, review current knowledge on the clinical and pharmacological effects of sumatriptan. Important pharmacological actions of sumatriptan are (i) poor penetration of the blood-brain barrier suggesting a peripheral point of action; (ii) 5-HT1-like/5-HT1d receptor-mediated vasoconstriction of large cerebral arteries and dural vessels; and (iii) blockade of neurogenic dural inflammation via 5-HT1d autoreceptor-mediated inhibition of vasoactive neuropeptides within the trigeminovascular system. Future research will tell which mechanism is involved in the pathophysiology of migraine and cluster headache.
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PMID:Clinical effects and mechanism of action of sumatriptan in migraine. 132 May 26

The efficacy of subcutaneous injection of sumatriptan in the acute treatment of migraine was assessed in a double-blind, randomized, placebo-controlled cross-over study of 27 migraine patients. In addition, the patients were asked to give information about their well-being and subjective symptoms by means of a self-administered standardized questionnaire. A total of 22 migraine sufferers received a subcutaneous (sc) injection of 8 mg of sumatriptan and 24 received placebo. Of these patients, 19 received both treatments and thus completed the study. The primary efficacy end-point was a reduction in headache severity from severe or moderate to mild or no headache at 30, 60, 90 and 120 min. An effective response to treatment was achieved within 30 min in 63% and within 60 min in 84% of patients when treated with 8 mg sumatriptan sc, compared with 11% for placebo (p less than 0.001). Sumatriptan also provided significant relief from nausea and photophobia as compared with placebo. The proportion of patients that needed rescue medication after 120 min was significantly lower (p less than 0.001) with active treatment when compared with placebo. Sumatriptan was well tolerated and the majority of adverse events were mild and transient. The most frequent symptoms were those of malaise/fatigue or numbness. No changes in blood pressure or ECG readings were observed during the treatment. Compared with placebo, subcutaneous 8 mg sumatriptan also caused a substantial improvement in general well-being as revealed by the Minor Symptoms Evaluation Profile-acute (MSEP-acute) questionnaire.(ABSTRACT TRUNCATED AT 250 WORDS)
Cephalalgia 1992 Aug
PMID:Sumatriptan injection is superior to placebo in the acute treatment of migraine--with regard to both efficacy and general well-being. 132 4

Sumatriptan and the ergot alkaloids are useful tools for deciphering drug mechanisms in migraine and related headaches. Both neuronal and vascular mechanisms have been proposed on the basis of actions of 5-HT at receptors resembling the 5-HT1D subtype. In this Viewpoint article, Michael A. Moskowitz argues that blockade of neural transmission and the neurogenic inflammatory response provides a mechanism by which sumatriptan and ergot alkaloids alleviate vascular headaches. He postulates, with similar arguments, that sumatriptan and ergot alkaloids may block headaches that develop from meningovascular inflammatory disorders such as from viral and bacterial meningitis and from the sequelae of head injury.
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PMID:Neurogenic versus vascular mechanisms of sumatriptan and ergot alkaloids in migraine. 132 94

Sumatriptan, a specific serotonin1-like receptor agonist, was studied in the acute treatment of migraine. Two hundred forty-two adult migraineurs participated in a randomized, double-blind study in which one dose of 1, 2, 3, 4, 6, or 8 mg of subcutaneous sumatriptan succinate was evaluated in sequential ascending fashion. At each dose level, a placebo group was included. Efficacy was defined as reduction of moderate or severe pain to mild or no pain, without the use of rescue medication. Headache relief rates showed an approximate dose-response relationship and at 1 hour were as follows: placebo, 24%; 1 mg, 43%; 2 mg, 57%; 3 mg, 57%; 4 mg, 50%; 6 mg, 73%; and 8 mg, 80%. Relief of nausea and improvement in clinical disability were also approximately dose related. Adverse events were dose related; the most common types were injection site reactions and tingling. The 6-mg dose was as effective as the 8-mg dose but was associated with fewer adverse effects and so is optimal.
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PMID:Dose ranging efficacy and safety of subcutaneous sumatriptan in the acute treatment of migraine. US Sumatriptan Research Group. 133 81

The role of serotonin in the pathogenesis of migraine is discussed, and the chemistry, pharmacology, pharmacokinetics, efficacy, adverse effects, and dosage and administration of sumatriptan are reviewed. Sumatriptan, which is structurally related to the neurotransmitter serotonin, is a serotonin type-1-like-receptor agonist that has a selective but heterogeneous effect on the carotid arterial system. Sumatriptan has a rapid onset of action and a large volume of distribution. Its subcutaneous bioavailability approaches 100%, and its mean terminal half-life is two hours. Studies have shown that both subcutaneous sumatriptan and oral sumatriptan are superior to placebo in relieving migraine and cluster headaches. Studies comparing oral sumatriptan with either ergotamine tartrate plus caffeine (Cafergot) or aspirin plus metoclopramide indicated that sumatriptan relieved headache more quickly and effectively; however, the dosages of these other agents may have been suboptimal. Sumatriptan is generally well tolerated by patients, and most dose-related effects are mild and transient. The most common adverse effect is pain at the injection site. No drug interactions have been identified so far. Subcutaneous sumatriptan 6 mg and oral sumatriptan 100 mg seem to offer the best benefit-to-risk ratio, although dosage and administration information is limited. Subcutaneous and oral sumatriptan are effective in aborting moderate to severe migraine and cluster headaches and their associated symtpoms. However, more studies are necessary to compare sumatriptan's efficacy with that of other treatments before it can be recommended as first-line therapy for migraine.
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PMID:Sumatriptan: a new drug for vascular headache. 838 41

Subcutaneous treatment of chronic tension-type headache with 2 mg and 4 mg sumatriptan, a selective 5-hydroxytryptamine1-like receptor agonist, was compared with placebo in a double-blind crossover study of 36 patients. The effect was evaluated using a 6-point verbal relief rating scale and by visual analog scale ratings of headache intensity before and for 2 h after treatment. Sumatriptan induced a modest but significantly greater headache relief than placebo, whereas no significant difference was found between the two doses of sumatriptan. Headache relief following sumatriptan was significant after 60 min and still seemed to be increasing after 120 min when the examination terminated. Three possible mechanisms of action of sumatriptan in tension-type headache are discussed.
Cephalalgia 1992 Dec
PMID:The 5-HT1-like agonist sumatriptan has a significant effect in chronic tension-type headache. 133 61

The methods used presently for abortion of the attacks of migraine and cluster headache are not fully satisfactory which causes that the search for new therapies is continuing. Although the mechanism of migraine attacks remains unexplained, it is thought that an important role in it is played by serotonin receptors, vasodilation in certain regions and opening of arteriovenous communications in the head. Sumatriptan is an agonist of 5-HT1 -like receptors and exerts a selective vasoconstricting effect on the arteries of the head, particularly in the rami of the carotid artery. In 1988 the first reports appeared on the effectiveness of the drug in migraine attacks. In the following years extensive, multicentre and international studies of the drug were carried out on over 600 healthy volunteers and nearly 6000 patients with migraine. The studies demonstrated that Sumatriptan was effective in abortion of migraine attacks. After oral administration of 100 mg or subcutaneous injection of 6 mg in nearly 70% of cases the attack regressed or was greatly alleviated, similarly as other symptoms accompanying the headache such as photophobia, nausea, vomiting. Studies were undertaken also on the effectiveness of Sumatriptan in emergency treatment of cluster headache, and good results were again achieved. The tolerance of the drug is good, although in some cases side effects develop, usually transient and mild, among them tingling, feeling of pressure, heat or heaviness of the head or chest, taste change and burning sensation at the site of injection. Sumatriptan, similarly as all novel drugs, requires caution in its use, particularly in patients with coronary heart disease and hypertension, and also in old patients. As yet, the use of the drug in paediatric migraine or in pregnancy is not recommended.
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PMID:[Sumatriptan and its use in treatment of migraine and cluster headaches]. 133 66

Sumatriptan is a highly selective 5 HT1 receptor subtype agonist. The efficacy and safety profiles of sumatriptan given by tablet or subcutaneous injection have been extensively investigated in the acute treatment of migraine attacks, where it has proved effective and well tolerated. A substantial proportion of patients with an acute attack of migraine suffer from once or more gastrointestinal symptom, including nausea, vomiting and occasionally diarrhoea. The presence of these symptoms may make the oral administration of acute treatments unsatisfactory. Subcutaneous administration is an alternative, but fear or dislike of injections or an inability to self inject makes subcutaneous treatment unacceptable to some patients. Alternative routes of administration are being investigated to overcome these difficulties including intranasal sprays and rectal suppositories. For those patients who experience difficulties swallowing whole tablets, an effervescent tablet is under development. Recent data have demonstrated that sumatriptan offers effective relief of cluster headache attacks, a condition where suffers experience repeated severe headache attacks, of short duration, during a cluster period. Further new indications are being investigated including the treatment of menstrual migraine, paediatric migraine and other headaches.
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PMID:[Sumatriptan--future development, alternative features and potential new indications]. 133 67

It is well established that cluster headache shows impaired functions at their neuroimmunomodulatory system level. Defect in receptor expression for 5-HT, IL-1 and IL-2 have been found in these patients. Sumatriptan, a molecule with agonistic activity for 5-HT1D receptor, truncates cluster headache attacks in 74% of patients. Flow cytometric analysis of monocytes expressing 5-HT receptor in cluster headache patients showed different trends clearly correlated with the clinical response to sumatriptan. Our findings strongly support the concept that cluster headache patients who are non responders to sumatriptan could present a block in their 5-HT receptor possibly due to specific autoantibodies for this receptor site.
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PMID:[The cluster headache: a clinical model of immunologic receptor pathology?]. 133 21


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