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PubMedDate not supplied

Comparison of the vasoconstrictor properties of the 5-HT1D-receptor agonists rizatriptan (MK-462) and sumatriptan in human isolated coronary artery: outcome of two independent studies using different experimental protocols.

Rizatriptan (MK-462) is a novel 5-HT1D-receptor agonist and is effective in the treatment of migraine headache. As angiographic studies have shown that the prototypic 5-HT1D/1B-receptor agonist sumatriptan can cause coronary artery constriction in patients with mild coronary artery disease, we have compared the contractile effects of rizatriptan on human isolated coronary artery with those of sumatriptan and 5-HT. Two different experimental protocols were used. In Study 1 (to avoid agonist desensitisation and interaction effects), arterial segments were exposed to a single agonist (either 5-HT, sumatriptan or rizatriptan) and in Study 2 each arterial segment was exposed to all three agonists with randomised first exposure to sumatriptan or rizatriptan. In both these studies the maximum contractions evoked by sumatriptan and rizatriptan were found to be smaller than those evoked by 5-HT, and the maximum contraction evoked by rizatriptan was significantly smaller than that for sumatriptan.

Adult↗

PubMedDate not supplied

Sumatriptan suppositories for the acute treatment of migraine. S2B351 Study Group.

A randomised, double-blind, parallel-group, placebo-controlled trial was undertaken to assess the efficacy and tolerability of the sumatriptan suppository in 184 patients with acute migraine. Patients used a sumatriptan suppository (12.5 mg or 25 mg) or placebo at home for the treatment of a moderate or severe migraine attack and those who experienced headache recurrence within 24 hours of dosing had the option to repeat the dose. By 2 hours post-dose, 68% of patients in the sumatriptan 25 mg group and 47% of patients in the sumatriptan 12.5 mg group compared with 25% of placebo patients achieved headache relief. Relief rates 2 hours post-dose for nausea, vomiting, photophobia and phonophobia were similar to those reported 2 hours post-dose for headache. Post hoc review of the recurrence data showed that administration of a second suppository was effective in alleviating recurrent headache in over 80% of the sumatriptan-treated patients experiencing recurrence. No serious or unusual adverse events were reported, and the pattern and incidence of adverse events did not vary as a function of dose. These data demonstrate that the sumatriptan suppository is a well-tolerated, effective treatment for the acute treatment of migraine pain and its associated symptoms.

Administration, Rectal↗

PubMed1998

Cardiac effects of sumatriptan: findings of Holter monitoring and review of the literature.

The aim of this study was to elucidate possible electrocardiographic effects of sumatriptan in a selected group of patients with severe headache requiring in-patient treatment. The patients (n = 21) were treated with sumatriptan in addition to various other compounds and were asked to record any symptoms following the administration of sumatriptan. In addition, Holter monitoring was performed in all subjects. In agreement with other studies, the adverse events reported by the patients were not related to ECG changes and, vice versa, ECG changes were not accompanied by clinical symptoms. The Holter findings before and after administration of sumatriptan were significantly different in three patients, i.e. recurrent episodes of ST depression and increase in extrasystoles. These changes occurred within a period of 1.45 to 18 hours and were not reproducible when Holter monitoring was repeated without sumatriptan. Even though the findings might be explained by spontaneous variability of Holter monitoring or other factors, this study does not definitely discount the possibility that sumatriptan may cause ST segment changes and increase pre-existing extrasystoles. Controlled studies are required to clarify this issue.

Adult↗

PubMed1998

Chromosomal localization of the 5-HT1F receptor gene: no evidence for involvement in response to sumatriptan in migraine patients.

The 5-HT1F receptor, which is present in both human vascular and neuronal tissue, may mediate the therapeutic effect and/or side-effects of sumatriptan. We investigated the chromosomal localization of the 5-HT1F receptor gene and the relation between eventually existing polymorphisms and the clinical response to sumatriptan in migraine patients. The 5-HT1F receptor gene was localized using a monochromosomal mapping panel, followed by a radiation-reduced hybrid mapping and fluorescent in situ hybridization. The results of these techniques show that the 5-HT1F receptor gene is localized at 3p12. We investigated the presence of polymorphisms by single strand conformation polymorphism analysis in 14 migraine patients who consistently responded well to sumatriptan, 12 patients who consistently experienced recurrence of the headache after initial relief, 12 patients with no response to sumatriptan, and in 13 patients who consistently experienced chest symptoms after use of sumatriptan. No polymorphisms were detected in any of the patients. We therefore conclude that genetic diversity of the 5-HT1F receptor gene is most probably not responsible for the variable clinical response to sumatriptan.

Adult↗

PubMed1998

Subcutaneous sumatriptan compared with usual acute treatments for migraine: clinical and pharmacoeconomic evaluation.

Cost-effectiveness and cost per successful treatment has been evaluated in 186 outpatients randomised to treat moderate to severe migraine attacks either with subcutaneous sumatriptan 6 mg (n = 97) or with their current therapy (n = 89) during an open, multicentre study of 3 months. Within 2 hours, headache severity decreased to none/mild in 86% of all attacks in the sumatriptan group (STG) compared to 25% in the customary group (CTG). Migraine was alleviated earlier in the STG than in the CTG (median 3.78 vs. 13.39 hours, p < 0.0001). The direct and total cost of treatment was 133 and 2012 BF, respectively, in the CTG and 1400 and 2522 BF, respectively, in the STG. Measuring the effectiveness of earlier pain relief with sumatriptan, the incremental cost-effective ratios for direct and total cost were 132 and 53 BF per hour of relieved pain, respectively. For this price, significantly more sumatriptan patients improved their quality of life by more than 20% (61.6 vs. 20.6% patients, p < 0.001) and less sumatriptan patient consulted a medical professional (11.3 vs. 29.2% patients, p < 0.01), used less medication for adverse events (6.2 vs. 22.5%, p < 0.001) and suffered less from associated migraine symptoms. The median number of hours of diminished work-efficiency (3 vs. 7 hours, p < 0.01) or of suspension of non-professional activity (10 vs. 24 hours, p < 0.001) was also significantly lower in the STG. The total cost per successfully treated patient was lower in the STG. Sumatriptan is more effective, provides a better quality of life, reduces health care resource utilisation, and improves work productivity as compared to the CTG, thereby resulting in a favourable cost-effectiveness ratio.

Absenteeism↗

PubMedDate not supplied

Multiple-attack efficacy and tolerability of sumatriptan nasal spray in the treatment of migraine.

OBJECTIVE: Sumatriptan hemisulfate nasal spray may provide a useful therapeutic option for patients with migraine who find injectable medications inconvenient or uncomfortable and for patients whose migraine-associated nausea and vomiting preclude the use of oral medication. This study was the first US trial to evaluate the effects of sumatriptan nasal spray administered for multiple migraine attacks. DESIGN/INTERVENTIONS: Sumatriptan nasal spray (5, 10, or 20 mg) was administered via a 1-shot nasal applicator into either nostril for up to 3 migraine attacks occurring over 6 months in a randomized, double-blind, parallel-group, placebo-controlled study. SETTING: Fifty-six outpatient clinical centers in the United States. PATIENTS: A total of 1086 men and women diagnosed with migraine with or without aura per International Headache Society criteria. MAIN OUTCOME MEASURES: Percentage of patients with headache relief (moderate or severe predose pain reduced to mild or none); percentage of patients with no or mild (vs moderate or severe) clinical disability; percentage of patients with nausea, vomiting, photophobia, or phonophobia; adverse events; clinical laboratory test results. RESULTS: Across attacks, headache relief in the 20-, 10-, and 5-mg drug and placebo groups was experienced 120 minutes postdose by 60%, 54%, 44%, and 32% of patients, respectively (P<.05 for each sumatriptan nasal spray group vs placebo, for the 10-mg vs 5-mg drug group, and for the 20-mg vs 5-mg drug group). Two thirds of the 20-mg patients treating 3 attacks experienced relief at 2 hours postdose for at least 2 of 3 attacks. Clinical disability scores at 120 minutes in the 20-, 10-, and 5-mg drug and placebo groups reflected no or mild impairment in 70%, 67%, 57%, and 50% of patients, respectively (P<.05 for the 10- or 20-mg drug group vs placebo group, and for the 20-mg vs 5- mg drug group). Similar efficacy rates were observed for nausea, photophobia, and phonophobia. For all parameters, individual-attack efficacy rates did not differ from across-attack rates. The incidence of adverse events was not dose related. The most frequently reported adverse event in the active treatment groups was taste disturbance (bad, bitter, or unpleasant). CONCLUSIONS: Sumatriptan hemisulfate nasal spray (5, 10, or 20 mg) is effective and well tolerated in the treatment of multiple migraine attacks. The 20-mg dose was associated with the highest efficacy rates across the greatest number of parameters.

Administration, Intranasal↗

PubMed1997

Clinical study of epidural analgesia with clonidine and sumatriptan in posthysterectomy.

A clinical study was conducted to compare the analgesic effect of clonidine with those of sumatriptan and their mixture and their effects on hemodynamics. 40 patients undergoing elective total hysterectomy were randomly divided into 4 groups in terms of the epidurally administered drugs with 10 patients in each group (group C1: clonidine 150 micrograms, group C2: clonidine 75 micrograms, group S: sumatriptan 6 mg and group S + C: clonidine 75 micrograms + sumatriptan 3 mg). MAP, HR, SpO2, VT VAS, VRS and ePDT were measured in the initial 4 h. The demographic data and the doses of intraoperative local anesthetics among the 4 groups were not statistically different. It was found that no significant difference in the pre- and postadministration values of HR, SpO2 and VT. A obvious reduction of MAP appeared in the groups of C1 and C2, but in the other groups the hemodynamical parameters were stable. The groups of C1, C2 and S + C showed significant increase in VAS and VRS, along with increase of ePDT when compared with the pre-drug level. There was no obvious alteration in group S after the drug administration. It was concluded that (1) single use of sumatriptan is ineffective in the dose given in this study; (2) small dose (150 micrograms and 75 micrograms) of clonidine has epidurally analgesic effects; (3) combined use of sumatriptan and clonidine is an acceptable way in epidural analgesia, in terms of its analgesic effect and hemodynamic changes.

Adult↗

PubMed1998

Sumatriptan (5-HT1D receptor agonist) does not exacerbate symptoms in obsessive compulsive disorder.

The non-selective serotonin (5-HT) receptor agonist meta-chlorophenylpiperazine (mCPP) has been reported to elicit symptoms in patients with obsessive compulsive disorder (OCD). MK-212, another non-selective 5-HT receptor agonist, does not seem to induce obsessive compulsive symptoms in OCD patients. The major pharmacological difference between mCPP and MK-212 is their affinity for the 5-HT(ID) receptor. The aim of this study was to explore the role of the 5-HT(ID) receptor in the pathophysiology of OCD, by using a challenge paradigm with the selective 5-HT(ID) receptor agonist sumatriptan (Imigran). A randomized, double-blind, placebo-controlled crossover challenge with sumatriptan (100 mg PO) was performed in 15 OCD patients. Neither the obsessive compulsive symptoms nor mood or anxiety symptoms changed significantly following sumatriptan administration as compared to placebo. Sumatriptan did induce a significant increase in plasma growth hormone (GH) levels. In the present study, no indication were found for the role of the 5-HT(ID) receptor in the pathophysiology of OCD. It should be noted, however, that sumatriptan does not readily pass the blood-brain barrier. Selective 5-HT(ID) receptors with better brain penetrating properties may shed more light on the role of this 5-HT receptor subtype in OCD.

Adolescent↗

PubMed2005

Managing migraine headaches experienced by patients who self-report with menstrually related migraine: a prospective, placebo-controlled study with oral sumatriptan.

The objective was to evaluate the efficacy and tolerability of oral sumatriptan (100 mg) in patients who self-reported with menstrually related migraine. A prospective, multicentre, randomised, double-blind, placebo-controlled, two-group crossover study was carried out in 20 UK primary and secondary care surgeries. Of 115 patients with a self-reported history of menstrually related migraine that entered the study, 93 patients completed it. Patients treated all migraine attacks for 2 months with sumatriptan (100 mg) and for 2 months with placebo. The primary endpoint was the proportion of patients reporting headache relief at 4 hours for the first treated attack. Only 11% of patients fulfilled the protocol definition of menstrually related migraine. Patients reported a variable pattern of migraine attacks occurring inside and outside the menstrual window. For the first attack, significantly more patients receiving sumatriptan than placebo reported headache relief for attacks occurring inside (67% vs. 33%, p=0.007) and outside (79% vs. 31%, p<0.001) the menstrual period. Sumatriptan was generally well tolerated. Oral sumatriptan (100 mg) is an effective and well tolerated acute treatment for patients who report menstrually related migraine.

Administration, Oral↗

PubMed1994

Characterization of the enzyme responsible for the metabolism of sumatriptan in human liver.

Studies have been undertaken to investigate the enzymes responsible for the metabolism of [14C]sumatriptan in man. Oxidative deamination of sumatriptan to form the indole acetic acid derivative is the only phase 1 pathway evident in man and both cytochrome P450 (P450) and monoamine oxidase (MAO) are capable of catalysing this type of reaction. The metabolism of [14C]sumatriptan was therefore investigated in vitro in a preparation derived from human liver, which was shown, by the use of the probe substrates [14C]testosterone (P450), [3H]5HT (MAO-A) and [14C]benzylamine (MAO-B) to be a rich source of both enzyme systems. Incubation with clorgyline and deprenyl, probe inhibitors of MAO-A and MAO-B, respectively, showed that [14C]sumatriptan was metabolized by MAO-A; there was no evidence of P450 involvement in its metabolism. The data in this study therefore indicate that the enzyme MAO-A is the major enzyme responsible for the metabolism of sumatriptan in human liver.

Clorgyline↗

PubMed1996

Changes in cerebral blood flow velocity after treatment with sumatriptan or placebo and implications for the pathophysiology of migraine.

Whether the primary mechanisms of migraine are vascular or neurogenic is, as yet, unresolved. In humans it is still unclear whether sumatriptan acts via constriction of dilated arteries or through other mechanisms. Doppler sonography is a non-invasive method for measuring blood flow velocities (BFV), an indirect marker of vessel diameter. This double-blind crossover placebo-controlled trial investigated changes in BFV in extra- and intracranial arteries in 132 migraine attacks (66 patients) before and after treatment with either 6 mg sumatriptan s.c. or placebo. Significant increases in BFV were observed only in the middle cerebral artery (MCA) and the basilar artery (BA) after administration of sumatriptan. However, the majority of the patients showed no change in BFV following sumatriptan. No difference in BFV could be detected between headache and non-headache side or between migraine and headache free periods. Despite a slight increase in BFV in intracerebral arteries, this study does not support the concept that vasoconstriction is sumatriptan's principal mechanism in pain relief.

Adult↗

PubMed1990

In vivo effects of sumatriptan (GR 43175) on extracellular levels of 5-HT in the guinea pig.

The effect of sumatriptan, a selective 5-HT1D receptor agent, on extracellular levels of 5-HT in the frontal cortex of the guinea pig was measured by intracerebral dialysis. A constant infusion of sumatriptan (10(-8)-10(-7) M) dose-dependently reduced extracellular levels of 5-HT (e.g. 80 +/- 2% decrease from control levels of 5-HT at 10(-7) M). Peripheral administration of sumatriptan (50 micrograms/kg i.p. and 500 micrograms/kg i.p.) had no effect on extracellular levels of 5-HT in the frontal cortex. These data suggest that sumatriptan, when infused into the brain, inhibits the release of 5-HT by stimulating 5-HT autoreceptors and that the putative acute anti-migraine effects of sumatriptan are likely to be mediated by peripheral mechanisms.

Animals↗

PubMed1994

The effects of sumatriptan on pituitary secretion in man.

Sumatriptan, a new antimigraine drug with high affinity and selectivity for certain 5-hydroxytryptamine (5-HT1D) receptor subtypes, was administered to 12 normal subjects, in order to investigate the effects of 5-HT receptor activation on anterior pituitary secretion. Sumatriptan increased plasma growth hormone (GH) levels from 2.5 +/- 0.5 mIU/l in basal conditions to 17.3 +/- 2.6 mIU/l 30 min after administration of the drug. After pre-treatment with cyproheptadine, an anti-serotoninergic drug known to inhibit GH secretion, the mean integrated sumatriptan-induced GH response decreased from 14.8 +/- 3.9 muI/l*hr to 3.7 +/- 1.7 mIU/l*hr. Sumatriptan administration did not have any effect on the secretion of the other anterior pituitary hormones. It is concluded that sumatriptan selectively increases GH secretion in man, but the exact nature of the receptors involved is not yet known.

Adult↗

PubMed2005

Effect of chemical enhancers on the in vitro percutaneous absorption of sumatriptan succinate.

The effects of percutaneous enhancers on the transdermal absorption of sumatriptan succinate were investigated by in vitro permeation studies. Pretreatment of porcine skin with ethanol (vehicle), polyethylene glycol 600, Span 20, oleic acid, R-(+)-limonene, alpha-bisabolol and 1,8-cineole (at 5% in ethanol, w/w) produced in all cases an increase in the flux of sumatriptan. The amount of sumatriptan retained in the skin was also determined. Ethanol has showed a low but significant increment on the drug transdermal flux. Treatment of the skin with alpha-bisabolol shows the same enhancer effect than ethanol. Span 20, oleic acid, and polyethylene glycol 600 have shown a moderate enhancing activity on transdermal flux of sumatriptan. R-(+)-limonene showed the greatest ability to enhance the flux of sumatriptan.

Administration, Cutaneous↗

PubMed1997

Effects of the 5-HT1 receptor agonists, sumatriptan and CP 93,129, on dural arterial flow in the rat.

The blood flow in and around the medial meningeal artery (dural arterial flow) was recorded in the exposed parietal dura mater encephali of the anesthetized rat using laser Doppler flowmetry. Local electrical stimulation of the dura mater (pulses of 0.5 ms delivered at 7.5-17.5 V and 5 or 10 Hz for 30 s) caused temporary increases in dural arterial flow. The effects of the 5-HT1 receptor agonists sumatriptan and CP 93,129 on the basal flow and the electrically evoked increases in flow were examined. Topical administration of undiluted sumatriptan (12 mg/ml) lowered the basal and the evoked flow by 20% on average. Systemic (i.v.) administration of sumatriptan (0.24, 0.72 and 3.6 mumol/kg) caused a short-lasting reduction of the evoked flow increases only at the higher doses while the basal flow was not significantly altered. Systemic administration of CP 93, 129 (0.46 and 4.6 mumol/kg) caused no significant changes of the basal and the evoked flow. At a dose of 23 mumol/kg CP 93,129 lowered the basal flow by 20% and the evoked flow by 30% for 20 min. The systemic arterial pressure was not significantly altered by sumatriptan and CP 93,129 within the whole range of doses. It is suggested that sumatriptan and CP 93,129 at high doses exert inhibitory effects on those fine afferent nerve fibers which release the calcitonin gene-related peptide, since this neuropeptide mediates the evoked increases in dural arterial flow.

Animals↗

PubMedDate not supplied

Differential distribution of [3H]sumatriptan binding sites (5-HT1B, 5-HT1D and 5-HT1F receptors) in human brain: focus on brainstem and spinal cord.

We report on the autoradiographic distribution of 5-HT1B, 5-HT1D and 5-HT1F receptor subtypes in human brain, focusing on the brainstem and cervical spinal cord. We have used [3H]sumatriptan as a radioligand in the presence of suitable concentrations of 5-CT (5-carboxamidotryptamine) to define 5-HT1F receptors, and ketanserin, to discriminate between 5-HT1B and 5-HT1D receptors. In the brainstem the highest concentrations of [3H]sumatriptan binding sites were seen in substantia nigra. The spinal trigeminal nucleus, substantia gelatinosa of the spinal cord, nucleus of the tractus solitarius and periaqueductal grey, also showed significant levels of [3H]sumatriptan binding sites. In the brainstem and spinal cord the total population of 5-CT-insensitive receptors, corresponding to 5-HT1F receptors, ranged from 9.8% in the periaqueductal grey to 53.4% in the substantia gelatinosa. This population represented 67.0% of binding in layer V of the frontal cortex. The decrease in [3H]sumatriptan binding in the presence of 200 nM ketanserin, indicative of the presence of 5-HT1D receptors, was very limited throughout the human brain, only reaching 20% of total specific binding over the periaqueductal grey. The proportion of [3H]sumatriptan binding sites displaced by 5-CT and insensitive to ketanserin, corresponding to 5-HT1B receptors, was, in general, the most abundant, ranging from 43.8% in substantia gelatinosa to 69.9% in the periaqueductal grey. Significant levels of 5-HT1B and 5-HT1D receptors found in migraine control pain areas suggest their involvement in antinociceptive mechanisms.

Aged↗

PubMed1994

Is chest pain after sumatriptan oesophageal in origin?

3-5% of patients taking the 5HT1D agonist sumatriptan for migraine have chest discomfort, suggesting a cardiac origin. We have investigated an alternative explanation of an oesophageal cause in 24 volunteers after the subcutaneous administration of a supratherapeutic dose of sumatriptan (16 mg) or placebo in a randomised, double-blind crossover study. Sumatriptan did not alter the electrocardiogram but increased the amplitude (p < 0.001) and duration (p < 0.001) of oesophageal contractions without affecting velocity of propagation. Clinically abnormal motility was also increased (p = 0.001), and was more common in the 5 subjects with chest pain after sumatriptan. The effect of sumatriptan on oesophageal function provides an alternative explanation for the chest symptoms.

Adult↗

PubMed1995

The effectiveness of combined oral lysine acetylsalicylate and metoclopramide compared with oral sumatriptan for migraine.

Aspirin is commonly used to treat migraine attacks, although sumatriptan, a much more expensive treatment, is also effective. We compared a combination of lysine acetylsalicylate (equivalent to 900 mg aspirin) and 10 mg metoclopramide (LAS+MTC) with oral sumatriptan (100 mg) and placebo in 421 patients with migraine. LAS+MTC was as effective as sumatriptan with a decrease of headache from severe or moderate to mild or none of 57% and 53%, respectively, for the first migraine attack treated. Both treatments were better than placebo (success rate 24%, p < 0.0001). LAS+MTC was significantly more effective in the treatment of nausea than sumatriptan (p < 0.0001) and was better tolerated (adverse events in 18% and 28%, respectively, p < 0.05). LAS+MTC is as effective as sumatriptan in the treatment of migraine attacks. It is also much cheaper.

Administration, Oral↗