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)

Changes in tension were monitored isometrically on spiral strips of freshly obtained bovine basilar arteries. Ergotamine (E), dihydroergotamine (DHE), methysergide (M) and pizotifen (BC-105) displaced the concentration-response curve for 5-HT in a noncompetitive way and in similar concentration ranges as indicated by the pD' 2(60 min) values of the three ergot alkaloids (E: 9.2, M: 9.1, DHE: 8.8) and the pD' 2(30 min) value (8.9) of BC-105. The ergot alkaloids but not BC-105 also exhibited considerable stimulating activity. The calculated pD2 values were 8.8 for E, 8.6 for DHE and 6.6 for M. Relative to 5-HT (= 1) the intrinsic activities were 0.4, 0.2 and 0.1 for E, DHE and M, respectively. BC-105 was nearly equipotent in antagonizing responses to 5-HT, E and DHE suggesting that both ergot alkaloids act as noncompetitive dualists at the 5-HT receptor. The results suggest that the strong stimulant rather than the blocking activity at the 5-HT receptor of ergotamine may be an important property for its therapeutic efficacy in migrainous attacks.
Res Clin Stud Headache 1978
PMID:Studies on the 5-HT receptor in vascular smooth muscle. 72 57

The haemodynamic effects of sumatriptan, a 5-HT1-like receptor agonist, and ergotamine, an agonist at alpha-adrenergic, dopamine as well as 5-HT receptors, were compared using intracardiac injection of radioactive microspheres of different sizes in anaesthetized pigs. Ergotamine (0.02 mg.kg-1) and sumatriptan (0.3 mg.kg-1) decreased systemic vascular conductance and cardiac output. Only ergotamine raised arterial blood pressure. Both sumatriptan and ergotamine decreased arteriovenous anastomotic, but not capillary, blood flow in the head and body skin. Arteriovenous and capillary blood flow in the dura mater and nasal mucosa and capillary blood flow in the brain, kidneys, adrenals, intestine, heart, spleen and muscle remained unchanged. However, kidney conductance was decreased by both drugs, spleen conductance by sumatriptan and heart, liver and adrenal conductances were decreased by ergotamine. Thus, both sumatriptan and ergotamine constricted arteriovenous anastomoses in the skin, but not in the dura mater or nasal mucosa. Ergotamine constricted the vasculature more than sumatriptan, although both drugs may differentially decrease vascular conductances in some organs.
Cephalalgia 1992 Aug
PMID:Comparative effects of the antimigraine drugs sumatriptan and ergotamine on the distribution of cardiac output in anaesthetized pigs. 132

Changes in the diameter of extracranial and intracranial arteries resulting in changes in cerebral blood flow have previously been assumed to be the most important pathophysiological factor in migraine. To test this hypothesis 20 normal subjects, and three groups of patients (n = 29) with migraine were investigated by means of transcranial Doppler sonography. Blood flow velocities in the middle cerebral (MCA) and in basilar (BA) arteries were measured. Data from patients were obtained in the interval between migraine attacks, during migraine attacks and following treatment with either ergotamine (0.5 mg i.m.; n = 10); flunarizine, a calcium overload blocker (20 mg i.v.; n = 13); or a 5-HT1-like agonist (sumatriptan, 4 mg s.c.; n = 6). Ergotamine and sumatriptan are constrictors of cerebral arteries in animal experiments. The arithmetic mean of flow velocity in the BA was reduced in normal subjects (45 cm/s) as compared with patients with migraine measured in between attacks (53 cm/s). Mean flow velocity in MCA was not different in normals (72.5 cm/s) as compared with migraineurs (75 cm/s). Neither ergotamine nor the 5-HT1 agonist and flunarizine resulted in a significant change in blood flow velocity in MCA and BA. This was true irrespective of whether the drugs were given in the headache-free period, during a migraine attack or during the withdrawal phase of drug-induced headache. Ergotamine was effective in improving headache during migraine attacks and sumatriptan attenuated headache during drug withdrawal from chronic analgesic intake. These results indicate that the action of ergotamine and the 5-HT1-receptor agonist is probably not mediated by their vasoconstrictor action on cerebral arteries.
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PMID:Ergotamine, flunarizine and sumatriptan do not change cerebral blood flow velocity in normal subjects and migraneurs. 165 85

Headache induced by medications used for nonheadache conditions, and more importantly, headache perpetuated by symptomatic medications used for primary headache disorders are discussed in detail in this article. The clinical features and mechanisms of drug-induced headaches are reviewed. Ergotamine and analgesic rebound phenomena are described. Management strategies for drug-induced headaches are outlined.
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PMID:Drug-induced headache. 225 18

Many theories exist on the pathogenesis of migraine. However, the clinical picture of migraine is agreed on universally as a familial disorder characterized by recurrent attacks of headache that are variable in intensity, frequency, and duration. The attacks are usually unilateral and often associated with anorexia, nausea, and vomiting. Migraine therapy is complex and difficult, focusing on abortive and prophylactic regimens. General therapeutic measures, including diet and establishing schedules for meals and sleeping, may benefit many migraineurs. A variety of medications, including ergotamine, propranolol, the calcium channel blockers, antidepressants, and nonsteroidal anti-inflammatory drugs (NSAIDs) have been beneficial in the prophylactic treatment of migraine. Ergotamine is the drug of choice in the abortive treatment, although other agents, such as the NSAIDs, have been used successfully. Inpatient therapy in a specialized unit for headache patients may be indicated for the recidivist patient, the patient habituated to analgesics or ergotamine, or the patient with the mixed headache syndrome, i.e., migraine occurring with coexistent muscle contraction headaches.
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PMID:Migraine headache. Its diagnosis and treatment. 252 Mar 83

The action of ergotamine on the 5-hydroxytryptamine (5-HT) venous sensitivity was studied in ergotamine abuser and non-abuser migraine patients. Ergotamine abusers showed reduced 5-HT hand vein contraction during abuse, compared to seven days after ergotamine withdrawal. In non-ergotamine users, the 5-HT venoconstriction was not significantly modified 12 h after a single intramuscular ergotamine (0.25 mg) administration. Even the administration of ergotamine locally into the vein did not change the venospasm of 5-HT given acutely in the same vein. Therefore, it seems that the 5-HT antagonism does not contribute to the therapeutic effect of ergotamine during the migraine attack. Moreover, the reduced 5-HT responsiveness during ergotamine abuse may possibly be compatible with the chronic headache present in some abusers, the withdrawal headache attacks and the abuse itself.
Cephalalgia 1989 Dec
PMID:Reduced serotonin vascular sensitivity in ergotamine abusers. 261 83

The pathogenesis of migraine has not been completely understood. However, it is generally accepted that the prodromal symptoms encountered in classic migraine usually result from vasoconstriction of intracranial vessels, while the headache itself results from dilation of other cranial vessels, often branches of the external carotid artery. Despite of increasing refinement in angiographic technique, many authors demonstrate the difficulty of interpreting abnormal radiographic findings in patients of migraine. We experienced recently a rare case who complained of migraine with neurological disorder manifesting for dynamic changes of cerebral arteries on sequential angiography. This 39-year-old man was admitted to our hospital with complaint of classic migraine accompanied with transient hemiparesis of the left side. Curious dynamic changes were noted sequentially on the repeated angiograms sequentially during his hospitalization. The carotid angiogram on admission showed narrowing at the right M1 portion. The second angiogram obtained at the fourth hospital day showed reduction of the narrowing, and occlusion of the right angular artery. The patient was treated with Ergotamine. The third angiogram taken after admission for the period of 1 month showed increased stenosis at the right M1 portion. Isolated angiitis of central nervous system was suspected because of such sequential dynamic angiographic changes, and steroid therapy was started. However he began to suffer from hemiparesis of left side one week after the treatment. Therefore, EC-IC bypass was performed, and his symptoms were improved gradually. Migraine is one of the common neurologic disorders countered in clinical practice. This report suggests that careful observation is needed in patients of migraine.
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PMID:[A case of isolated cerebral angiitis with sequential angiographic changes]. 339 13

A double-blind controlled clinical trial of cross-over design for the treatment of headache was conducted in 88 women identified during a community survey as having headaches with the features of migraine. Of 79 subjects who completed the trial, 40 benefited from oral ergotamine tartrate and 46 benefited from the placebo. There was no evidence that ergotamine in doses of 2 or 3 mg. was more effective than the placebo. Ergotamine aggravated the attack significantly more often than the placebo. Neither the colour of the tablets nor the order of therapy significantly affected the results of the treatment.
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PMID:Controlled clinical trial of ergotamine tartrate. 491 61

Bioavailability and rate of absorption of ergotamine were studied in eight cluster headache patients outside attacks. In a cross-over design, approximately 2 mg ergotamine tartrate was administered as effervescent tablets, suppositories, and from an inhalation device, with 0.25 mg intravenously as the reference. Ergotamine in plasma was measured by high performance liquid chromatography with fluorescence detection from 5 to 420 min. For all three routes of administration, a similar low (0.5-4.2%) bioavailability of ergotamine was estimated. Only inhalation of ergotamine resulted in early (at 5 min) peak concentrations of ergotamine in plasma and is therefore most likely to relieve the short-lived attacks of cluster headache. The inhalation route for ergotamine poses problems, however, and we suggest ways of improving the inhalation device.
Cephalalgia 1983 Mar
PMID:Optimal routes of administration of ergotamine tartrate in cluster headache patients. A pharmacokinetic study. 640 71

Previous investigations from our laboratory have shown that ergotamine causes a selective vasoconstriction in the carotid vascular bed of the dog and that the drug constricts arteriovenous anastomoses (AVAs) in cats and pigs. Since ergotamine can act via alpha-adrenergic or D-serotonergic receptors in certain vascular and non-vascular tissues, we have attempted to ascertain here if these receptors mediate the constriction of AVAs. Using radioactive microspheres of 15 microns diameter we found in the dog that about 40% of the carotid arterial blood is shunted to the venous side via AVAs. Ergotamine (2-20 micrograms X kg-1, i.v.) reduced total carotid blood flow to a larger extent in the AVA part than in the extracerebral part (muscles, ears, skin and fat). The cerebral component of carotid blood did not change. These results, confirming that ergotamine decreases arteriovenous shunting, show that the drug has a more selective action on the AVAs than on the arterioles. Pretreatment with phentolamine (0.5 mg X kg-1), pizotifen (0.5 mg X kg-1) or their combination did not effectively modify the responses to ergotamine. It is concluded that the vasoconstriction of cranial AVAs (and arterioles) by ergotamine does not appear to be primarily mediated by either alpha-adrenergic or D-serotonergic receptors. However, the role of atypical serotonin receptors has yet to be determined.
Cephalalgia 1983 Jun
PMID:Ergotamine-induced constriction of cranial arteriovenous anastomoses in dogs pretreated with phentolamine and pizotifen. 640 16


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