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Query: UMLS:C0018681 (headache)
 56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The effects on the sexual tone of parachlorophenylalanine, a selective inhibtor of 5-hydroxytryptamine synthesis, testosterone and placebo were evaluated in patients complaining of migraine-headache and sexual deficiency. The combined treatment with parachlorophenylalanine and testosterone significantly increases the sexual stimulus more than parachlorophenylalanine, testosterone and placebo, when given on their own. Conversely subjects with normal or excessive sexual activity, reported a decrease of sexual tone, during chronic treatment with tryptophan. The hypothesis of an implication of brain 5-HT in the mechanism of psychogenic sexual deficiency and the possibility of a therapeutic approach with drugs able to interfere with 5-HT turnover are discussed.
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PMID:The influence of tryptophan and parachlorophenylalanine on the sexual activity in man. 14 11

Central panalgesia is a syndrome which includes systemic pains of a central nature, usually classified as hysteria, fibrositis and masked depression. Exploration of the peripheral neuromuscular junctions (in the iris by pupillometry, and in veins by computerized venotest) indicates an increased monoamine receptor sensitivity. 5-HT vein sensitivity is particularly impressive (up to 1,000 times). In the vein there appears to be a decentralization supersensitivity, as it is extended to different monoamines (5-HT, dopamine, noradrenaline, tyramine). This type of supersensitivity is compatible with the theory of a deficiency of neurotransmitters at the level of the anti-nociceptive and integrated systems, with subsequent central and peripheral supersensitivity. A similar condition limited to the rostral section of the anti-nociceptive system is valid for the mechanism of idiopathic headache including migraine: central and peripheral supersensitivity to monoamines and opiates is also episodically observed in headache sufferers.
Res Clin Stud Headache 1978
PMID:Decentralization supersensitivity in headache and central panalgesia. 72 53

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

Animal and clinical pharmacological studies show in certain vascular beds a biphasic action [potentiation and inhibition of serotonin (5-HT) responses] of some anti-migraine drugs, such as ergotamine, methysergide and more recently Org GC 94. Potentiation occurs at therapeutic drug concentrations. The present investigations seem to support the 5-HT theory of migraine and other essential headaches. In this theory, anti-migraine drugs, such as ergotamine, methysergide, pizotifen, and Org GC 94 could reduce the occurrence of pain in migraine and other esscutial headaches by acting as partial agonists tending to correct a deficiency of central 5-HT concentrations or turnover.
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PMID:Clinical and animal pharmacology of migraine: new perspectives. 97 97

By testing venomotor receptors (venous-constriction test), it was possible to show a potentiation of the venous constriction effect of serotonin by methysergide and ergotamine. This 5-HT potentiation was observed only when these drugs were sampled in concentrations similar to those in therapeutic use. When ergotamine and methysergide are sampled in concentrations higher than those used in clinical practice, the expected 5-HT antagonist effect is clearly evident. We could therefore conclude that methysergide and ergotamine can be considered pro-serotonin and not anti-serotonin drugs. The pro-serotonin effect of methysergide and ergotamine might take place peripherally on vasomotor or sensitive receptors and/or at a CNS level, making up for the lack of serotonin which, according to the central theory of essential headache, provokes the painful cephalic syndrome.
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PMID:[Progress of clinical pharmacology in essential headaches]. 108 98

In 14 migrainous patients during different clinical phases the urinary excretion of 5-hydroxy-tryptamine (5-HT) and its main metabolite, 5-hydroxyindoleacetic acid (5-HIAA) were followed. In the course of headache attack a significant increase in 5-HIAA excretion rate was found; at the same time the excretion of 5-HT was not significantly changed. After migraine attack a very pronounced lowering in excretion rate of both 5-hydroxy-indoles occured. The reserpine provocation test was followed by an intensive enhancement of urinary 5-hydroxyindole excretion, but the decrease thereafter was less expressed than after spontaneous attack. These findings lend support to the theory of an abrupt fall in total plasma 5-HT as a trigger mechanism for the painful phase of migraine.
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PMID:Fluctuation of 5-hydroxy-indole compounds in the urine of migrainous patients. 123 31

After thousands of painful long-lasting migraine or extremely violent cluster headache attacks no one has yet traced histological inflammatory or degenerative alterations of the interested tissues able to explain such dreadful pain. Therefore it has seemed logical to include these pains among the unjustified aimless, non finalized types of pain. Furthermore, clinical characteristics of automatism, explosiveness and the course of these pains resemble other aimless pains like those of organic deafferentation (phantom pain) which appear in a desensitized limb after denervation or even in amputated subjects. Intense and long lasting pains in opioid abstinence, mainly located in the chest and in the hip, also have all the characteristics of aimless pain. Idiopathic cephalic pain, together with deafferentation or opioid-abstinence pain, seems to be due to a dysafferentation which, through different channels, follows an analogous mechanism. This mechanism seems to be due to a deficit of autoanalgesia which in both organic deafferentation (phantom limb) and in opioid-abstinence can be related to the disuse of afferences' modulation. In idiopathic headache such a failure of autoanalgesia is likely to be due to a genetic, idiopathic mechanism. Headaches are characterized by a clear deficiency of autoanalgesia which may manifest itself not only at the level of the cephalic segment, which is so rich in afferences, but it may even involve the whole body. Even if pain is the compulsory phenomenon to diagnose headache, one must consider that migraine is a symptomatic triad in which vegetative and emotional phenomena also emerge. These phenomena are interindependent and not interdependent as each of them may appear as a first manifestation of an attack; one must therefore consider the possibility of a "unicum movens". Serotonin was taken into consideration because of its action which interests all or nearly all vegetative-emotional pain transmitting pathways. Today's identification of four types and various sub-types of 5-HT receptors has revealed the extraordinary eclecticism of this transmitter which within migraine's clinical expression underscores that migraine sufferers are characterized by a marked sensitivity to all the drugs capable of acutely or chronically interacting with serotonin metabolism and binding with many serotonin receptor types and sub-types. So even if the migraine sphinx still proposes its enigma, researchers--with their incurable curiosity--may not only find more and more accurate and effective medication for many human beings but also start penetrating a mystery, a great challenge to human imagination.
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PMID:[Noci-autonomic-affective automatism, the physiopathological essence of hemicrania. The serotonin theory as a guiding principle in the labyrinth of interpretations]. 129

The action of sumatriptan, putatively a selective 5-HT1D or 5-HT1-like receptor agonist which is effective in the treatment of migraine, has been studied on fresh human dural (middle meningeal) arteries. In low concentrations (10(-8)-10(-7) M) it was found to be a significantly stronger vasoconstrictor of dural arteries compared to cerebral and temporal arteries. However, its potency was less than that of 5-HT. The sumatriptan-induced vasoconstriction was antagonized by methiothepin (10(-9)-10(-8) M), but not by ketanserin (10(-7) M). The observations suggest that the sumatriptan-induced contraction of the dural artery is mediated via activation of 5-HT1D or 5-HT1-like receptors, whereas it does not appear to activate the 5-HT2 receptors.
Cephalalgia 1992 Aug
PMID:Sumatriptan is a potent vasoconstrictor of human dural arteries via a 5-HT1-like receptor. 132

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

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


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