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

The vasoconstrictor activity of sumatriptan and ergotamine were compared by injecting these drugs in the hand vein of migraine subjects. We used the "venotest method", which permits the evaluation of the venoconstrictor effect of small doses of drugs, acting locally in the hand vein. Sumatriptan injected at increasing doses in the hand vein provoked contraction only at high doses (500 micrograms): venoconstriction lasted 5-15 minutes and was similar in intensity and duration to that induced by 0.5-1 micrograms of 5-hydroxytryptamine (5-HT). Likewise, ergotamine induced contraction only at a dose of 50 micrograms: this venoconstrictor effect was long lasting (at least 1 hour). Ergotamine-induced hand vein contraction, almost completely inhibited by ketanserin, seems mediated at least in part by 5-HT2 receptors, like the one induced by 5-HT and sumatriptan, already observed in a previous study. Clinical doses of ergotamine (0.25 mg intramuscular) and of sumatriptan (6 mg subcutaneous) do not provoke hand vein contraction for at least 1 hour: this could be due to a low activity of these drugs on the 5-HT2 vein receptors or a technique that is unsuitable to detect the vasoconstrictor effect of drugs given by the systemic route. The long lasting venoconstrictor effect of ergotamine may be due to a slow dissociation from receptor sites. The short vasoconstriction induced by sumatriptan could account for the recurrence of headache in many sumatriptan-treated migraine subjects.
Headache 1994 Apr
PMID:Comparison between venoconstrictor effects of sumatriptan and ergotamine in migraine patients. 801 33

Gepirone, an azapirone, is a potent 5-hydroxytryptamine 1A (5-HT1A) agonist. We report an uncontrolled 6-week study in 21 patients (4 men, 17 women: mean age, 36.71 years) with a concurrent DSM-III-R diagnosis of generalized anxiety disorder and panic disorder with agoraphobia. After a 2-week medication-free period, patients were started on 2 mg of gepirone per day increasing over 3 weeks to 12 mg/day. Three patients dropped out in the first week, and one patient violated the protocol. They were therefore excluded from analysis. Two patients who dropped out at weeks 4 and 5 because they found the treatment ineffective were included. Twelve of the 17 patients (70.6%) had at least a 50% reduction in their panic attacks by week 6, and 9 of them had at least a 50% reduction by week 3. Ten patients had "0" panic attacks by week 6 (59%). On the Hamilton Anxiety Scale, 65% had a 50% or greater reduction in total score, mostly beginning in week 1. On Global Assessment, by week 6, 11 were much improved or better (65%). Adverse effects were rare and consisted of stomach upset, dizziness, or headaches. This preliminary study suggests the possible efficacy of gepirone in panic disorder.
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PMID:Gepirone and the treatment of panic disorder: an open study. 809 26

While headache is a documented side effect of electroconvulsive therapy (ECT), there is little information on this phenomenon. Studies of the mechanisms of ECT as a treatment for depression indicate that alterations in serotonergic neurotransmission appear to be related to its efficacy. While ECT and many of the antidepressant drugs have similar effects on serotonergic transmission, they are notably different in the changes they induce in type 2 receptors for 5-hydroxytryptamine (5-HT). ECT upregulates 5-HT2, and antidepressants down regulate the receptor's expression. 5-HT2 receptor sensitization has been associated previously with headache genesis, which may explain why ECT induces headache, and amitriptyline relieves headache. In our study we surveyed 98 patients retrospectively about their experiences with headache prior to and following ECT. Of the 54 patients who submitted properly completed questionnaires, five reported new onset of headaches following ECT, four reported exacerbation of a previous headache problem, and two reported their headaches improved. The patients experienced changes in the character or location of pain, with a tendency to progress from tension-type to migrainous headache. In all but two cases these developments persisted at least eight months after ECT. We discuss the possible reasons and significance of our findings.
Headache 1994 Mar
PMID:Headache and electroconvulsive therapy. 820 Jul 90

1. Sumatriptan, a 5-hydroxytryptamine (5-HT)1-like receptor agonist, is effective against the headache of migraine. The effects of sumatriptan injected via the carotid artery on the cerebral microcirculation were studied in 10 anaesthetized cats. 2. The local cerebral blood volume (CBV), mean transit time of blood (MTT) and cerebral blood flow (CBF) in the parieto-temporal cortex were measured by a photoelectric method. CBV represents the cumulative dimensions of the cerebral microvessels. 3. Sumatriptan at 5 and 50 micrograms kg-1 had no significant effects on the CBV, MTT, CBF, and mean arterial blood pressure (MABP); 500 micrograms kg-1 of sumatriptan reduced the CBV, prolonged the MTT, and decreased the CBF (approximately -20%) without affecting the MABP. Sumatriptan, 5 mg kg-1, elicited transient reductions in CBV and CBF, which were attributable to the rapid and marked falls of MABP seen with this dose. 4. Thus, while a high dose of sumatriptan (500 micrograms kg-1) exhibits direct vasoconstrictor actions on the cerebral vessels, low doses of sumatriptan, within the therapeutic range, elicit no vasoconstriction. The data do not support a vasoconstrictor action of sumatriptan playing a primary role in reversing the headache of migraine.
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PMID:Effects of sumatriptan on the cerebral intraparenchymal microcirculation in the cat. 830 85

Sumatriptan, a 5-hydroxytryptamine (5HT)1-like receptor agonist, is a new antimigraine drug which is also effective in cluster headache (CH), a disorder with marked ocular circulatory abnormalities. Sumatriptan could putatively exert a therapeutic effect in this vascular bed. The present study is an attempt to assess sumatriptan's vasoactivity in isolated porcine ophthalmic artery (POA) and to verify whether it has similar activity to 5HT, and whether it interferes with the vasodilation induced by calcitonin gene-related peptide (CGRP) and vasoactive intestinal peptide (VIP). In contrast to 5HT, sumatriptan induced only slight contraction in POA at high concentrations. However, in some artery segments pre-contracted with PGF2 alpha, sumatriptan induced a slight and short-lasting but marked relaxation. In addition, relaxations induced by VIP were inhibited significantly by sumatriptan, whereas CGRP effects were not influenced by the drug. Such reactions suggest that sumatriptan's effect in CH is probably unrelated to direct ocular arterial vasoconstriction.
Cephalalgia 1993 Dec
PMID:Sumatriptan relaxes isolated porcine ophthalmic artery, but inhibits VIP-induced relaxation. 831 50

The venoconstrictive activity of sumatriptan and its interaction with noradrenaline (NA)- and 5-hydroxytryptamine (5HT) venoconstriction was studied in vivo in the hand vein of migraineurs. Sumatriptan, injected at increasing doses into the vein, caused local venoconstriction after a 500 microgram dose, comparable to that induced by 0.5-1 micrograms of 5HT. This venoconstriction was completely inhibited by low doses of ketanserin (5 micrograms). Subcutaneous sumatriptan (6 mg) provoked a minor increase in vein tone, lasting less than 30 min. Non-venoconstrictive doses of sumatriptan (10-100 micrograms), injected in the hand vein, produced an amplification of NA-venoconstriction but not of 5HT-induced venoconstriction. A similar increased effect was displayed by subcutaneous sumatriptan (6 mg) for at least 1 h. Sumatriptan appears to cause peripheral venoconstriction only at high doses locally applied (in the hand vein), by acting on 5HT2 receptors. Clinical subcutaneous doses (6 mg) do not show significant venoconstrictive effects. The amplifying effect on NA venoconstriction, also caused by 5HT, ergotamine and dihydroergotamine in human cranial arteries, may be important in explaining the therapeutic action of sumatriptan in migraine attacks.
Cephalalgia 1993 Dec
PMID:Amplifying effect of sumatriptan on noradrenaline venoconstriction in migraine patients. 831 46

There is a considerable overlap in migraine and depression incidence, and both conditions may be associated with low levels of 5-hydroxytryptamine (5-HT). During a migraine attack there is evidence for low levels of platelet 5-HT and possibly also low Vmax for 5-HT uptake; both these findings are also associated with the depressed state. Both conditions can be treated by tricyclic and monoamine oxidase inhibiting antidepressants. However, there are also clear differences: migraine attacks are brief and self limiting. Part of the migraine cascade occurs outside the blood brain barrier, presumably involving blood vessels and, unlike depression, migraine attacks can be ameliorated by drugs which only act peripherally. In addition, migraine patients, especially males, often have permanently low levels of platelet monoamine oxidase activity, whereas patients with unipolar depression tend to have raised levels of this marker. This low enzyme activity may reflect part of the vulnerability to migraine, often associated in the prodromal phase with agitation or hyperactivity. Migraine may form part of a family of brief recurrent self-limiting disorders, which involve disturbances of both mood and monoamines; during the headache phase of the attack, the links with depression are most apparent.
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PMID:Migraine and depression: biological aspects. 836 71

Granisetron (BRL 43694A) is a novel, selective 5-hydroxytryptamine-3 (5-HT3) receptor antagonist developed for the prophylaxis and treatment of cytostatic drug-induced emesis. After a brief review of the preclinical evaluation of granisetron the clinical findings with this novel compound are summarised. From the data of large randomised trials one can conclude that granisetron is an active antiemetic, both as a prophylactic and an intervention agent, to an extent which is superior or at least equal to the best available antiemetic combination regimens, having a major efficacy ranging from 74 to 92%. Granisetron may be given as a single, 5-min infusion before chemotherapy and is thus more convenient to administer than many antiemetic regimens. The adverse event profile of granisetron is favourable with a wide therapeutic margin. The only consistent side-effects attributable to granisetron are headache in about 14% of the patients and constipation in about 4% of the patients. Headache induced by granisetron was generally mild and resolved spontaneously or was promptly relieved with standard analgesics. No extrapyramidal side-effects were observed with granisetron.
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PMID:Clinical studies with granisetron, a new 5-HT3 receptor antagonist for the treatment of cancer chemotherapy-induced emesis. The Granisetron Study Group. 838 Dec 93

The headache phase of the migraine attack is thought to be associated with a dilation of cranial blood vessels, particularly those in the dura mater, and an accompanying localized sterile inflammatory response. Serotonin, or 5-hydroxytryptamine (5-HT), is considered a possible mediator of this syndrome. Receptors for 5-hydroxytryptamine are present in cranial arteries and are widely distributed in the CNS. Studies indicate that sumatriptan, a 5-HT1 receptor agonist, is effective in treating acute migraine attacks. The mechanism of sumatriptan's therapeutic action is not completely understood. Evidence from animal and human studies suggests that sumatriptan constricts dural vessels and inhibits neuropeptide release from trigeminal nerve endings by activating 5-HT1 receptors. Clinically, sumatriptan is rapidly effective against all features of the headache phase in migraine in up to 80% of patients. The headache may recur, however, within 24 hours in about one third of patients, but this can be treated effectively with a subsequent dose of sumatriptan. Treatment with sumatriptan has been well tolerated with only minor, transient, acute side effects reported. At present, only limited information is available regarding long-term tolerability, safety, and efficacy. Sumatriptan should not be prescribed to patients with a cardiovascular history.
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PMID:Sumatriptan in the treatment of migraine. 838 11

The antiemetic efficacy and safety of granisetron (40 micrograms/kg), a selective and potent 5-hydroxytryptamine (serotonin) antagonist, was compared with that of metoclopramide (7 mg/kg) plus dexamethasone (12 mg) in patients receiving fractionated chemotherapy. Patients receiving cisplatin at doses of at least 15 mg/m2 or etoposide at least 120 mg/m2 or ifosfamide at least 1.2 g/m2 on each of 5 consecutive days were eligible. A total of 143 patients received granisetron and 141 received the comparator regimen. The 5-day complete response rate (no vomiting, no worse than mild nausea) for granisetron (46.8%) was equivalent to that for metoclopramide plus dexamethasone (43.9%). The overall 5-day response profile was superior for granisetron (P = 0.013) because of fewer failures in this group. The overall incidence of adverse experiences was significantly lower in the granisetron group (60.8% versus 77.3%, P = 0.003). Headache and constipation, more prevalent in the granisetron group, are recognized side-effects of serotonin antagonists. Extrapyramidal syndrome, not seen in any granisetron patients, occurred in 20.6% of comparator patients (P < 0.0001). The majority of granisetron patients only required a single prophylactic dose of the drug on each treatment day (at least 82%). In conclusion, granisetron showed at least equivalent efficacy to metoclopramide plus dexamethasone in patients receiving 5-day fractionated chemotherapy. In addition it offered a simple and convenient dosing regimen and a safer side-effect profile.
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PMID:The antiemetic efficacy and safety of granisetron compared with metoclopramide plus dexamethasone in patients receiving fractionated chemotherapy over 5 days. The Granisetron Study Group. 839 77


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