Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Sumatriptan”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 217 records · Page 12Linked to original sources
PubMed1997

Stability of sumatriptan succinate in extemporaneously prepared oral liquids.

The stability of sumatriptan succinate in extemporaneously prepared oral liquids was studied. Suspensions of sumatriptan (as the succinate salt) in Ora-Sweet, Ora-Sweet SF, and Syrpalta syrups (Paddock Laboratories and Humco Laboratory) were extemporaneously compounded to produce a sumatriptan concentration of 5 mg/mL. Each suspension was prepared in triplicate. The suspensions were stored at 4 degrees C in amber glass bottles for 60 days. Two 1-mL samples were removed from each bottle initially and on days 2, 7, 14, 21, 28, 35, and 60. Sumatriptan concentrations were determined by high-performance liquid chromatography. The samples also underwent visual inspection and microbial testing. The mean concentration of sumatriptan in all suspensions remained above 90% of the initial concentration for up to 21 days. By day 28, the sumatriptan concentration of all suspensions had decreased to less than 90% of the initial concentration. None of the suspensions had microbial growth up to day 28, and there were no visible changes in the suspensions throughout the study period. Sumatriptan 5 mg/mL (as the succinate salt) in three oral suspensions was stable for up to 21 days when stored without light at 4 degrees C.

Administration, Oral↗
PubMed2000

Human isolated coronary artery contraction to sumatriptan characterised by the selective 5-HT1B/1D receptor antagonist GR55562.

The antimigraine drug, sumatriptan, contracts the human coronary artery both in vivo and in vitro. Because sumatriptan has been associated with cardiac side effects, it is important to characterise the receptor involved in sumatriptan-induced coronary artery contraction. Using the agonists sumatriptan and 5-carboxamidotryptamine and the selective 5-HT1B/1D receptor antagonist GR55562, we have investigated the involvement of 5-HT1B/1D receptors in the contraction of the human isolated coronary artery. Contractions to sumatriptan (pEC50: 6.1+/-0.2, maximal effect: 21+/-4% of 100 mM K+-induced contraction) were competitively antagonised by GR55562. The pA2 of GR55562 (7.40+/-0.16) was in accord with its reported affinity at the human 5-HT1B receptor. Since the contractions to 5-carboxamidotryptamine did not reach a maximum with the highest concentration used (10 microM), pEC50 values could not be calculated for Schild analysis. However, using the pEC10%/K+ values (negative logarithm of the concentration needed to induce 10% of the contraction to 100 mM K+), GR55562 proved a less potent antagonist against 5-carboxamidotryptamine than against sumatriptan. These results show that sumatriptan contracts the human isolated coronary artery via 5-HT1B/1D receptors, most probably the 5-HT1B subtype. 5-Carboxamidotryptamine may contract the human isolated coronary artery, at least partly, via a novel yet to be characterised, receptor.

Benzamides↗
PubMed1991

Lack of an interaction between propranolol and sumatriptan.

1. The effect of twice-daily dosing with propranolol on the pharmacokinetics and pharmacodynamics of a single oral dose of sumatriptan was investigated in 10 healthy male subjects. 2. Each subject received 7 days dosing with propranolol (80 mg twice daily) plus a single dose of sumatriptan (300 mg orally) on day 7; on another separate occasion, placebo was administered for 7 days plus a single dose of sumatriptan on day 7. There was at least a 7 day washout interval between the two periods of dosing. Pulse and blood pressure were measured up to 10 h after dosing with sumatriptan and blood samples were taken up to 26 h post-dose. 3. Propranolol had no significant effect on any of the derived pharmacokinetic parameters of sumatriptan. The appropriate average parameter values in the presence of propranolol were, respectively: Cmax (120 ng ml-1 vs 126 ng ml-1), tmax (4.5 h vs 3.0 h), AUC (580 ng ml-1 h vs 566 ng ml-1 h), t 1/2,z (1.9 h vs 1.8 h). 4. Propranolol had no significant effect on the pharmacodynamics of sumatriptan, as measured by pulse rate and blood pressure. 5. The results of this study would suggest that no alteration in the sumatriptan dosage will be necessary for migraine patients taking propranolol prophylactic therapy.

Adult↗
PubMed1993

Subcutaneous sumatriptan in the acute treatment of migraine in patients using dihydroergotamine as prophylaxis. French Migraine Network Bordeaux-Lyon-Grenoble.

The efficacy of sumatriptan, a 5-HT1 receptor agonist, in patients with migraine attacks occurring despite prophylactic treatment with oral dihydroergotamine, was assessed in a double-blind placebo-controlled study involving 76 patients. Thirty-seven patients were treated with a subcutaneous injection of 6 mg sumatriptan self-administered with an auto-injector and 39 with placebo given by the same route. Patients having inadequate relief were allowed to use a second injection of test medication 1 hour later and rescue treatment between 2 hours and 24 hours after the first dose. Headache relief was achieved within 2 hours after sumatriptan in 26 patients (70%) compared to 8 patients (21%) in the placebo group (P < 0.0001). Of these patients, 19 (51%) and 3 (8%) were, respectively, pain free at this time. A second injection of sumatriptan was used by 8 (22%) patients compared to 30 (77%) patients in the placebo group (P < 0.0001), whereas rescue medication was used respectively by 13 (35%) and 22 (58%) patients (P < 0.024). The adverse event profile of sumatriptan was not affected by the concomitant use of dihydroergotamine and side-effects were all minor and transient. Patient satisfaction was significantly higher in the sumatriptan group (75%) compared to patient satisfaction with placebo (16%). These results show that the high efficacy rate of subcutaneous sumatriptan and its safety profile remain unchanged in migraine patients receiving oral dihydroergotamine as prophylaxis.

Acute Disease↗
PubMedDate not supplied

Sumatriptan in acute migraine using a novel cartridge system self-injector. United Kingdom Study Group.

This double-blind, randomized, placebo-controlled, parallel-group, multicenter study assessed the efficacy, acceptability, safety, and tolerability of subcutaneous sumatriptan 6 mg administered using a novel cartridge system self-injector for the acute treatment of migraine. Eighty-six patients treated one migraine attack at home with sumatriptan or placebo. A second identical injection was available after 1 hour for inadequate relief or if the headache recurred. Rescue medication was available 1 hour later. The primary end point was headache relief (improvement in headache from moderate or severe to mild or no pain) within 60 minutes of the first injection. Secondary end points included the acceptability of the self-injector, requirement for and efficacy of a second dose, relief of nonheadache symptoms, use of rescue medication, and adverse events. Significantly more patients taking sumatriptan than placebo reported headache relief 1 hour after the first injection (88% vs 11%, P < 0.001). The device was well accepted by patients; about 90% found it easy to use and wanted to take further medication using it. Significantly fewer patients taking sumatriptan than placebo required a second injection (33% vs 92%, P < 0.001) or rescue medication after the second injection (35% vs 67% P < 0.05). Significantly more patients taking sumatriptan than placebo reported headache relief after the second injection (83% vs 32%, P < 0.01), and resolution of nonheadache migraine symptoms (54% vs 23%, P < 0.01). Sumatriptan was generally well tolerated. Subcutaneous sumatriptan 6 mg self-administered using the novel self-injector is an effective, well accepted, and well tolerated acute treatment of migraine.

Acute Disease↗
PubMedDate not supplied

Almotriptan in migraine patients who respond poorly to oral sumatriptan: a double-blind, randomized trial.

OBJECTIVE: To investigate the efficacy and tolerability of almotriptan 12.5 mg in migraine patients who respond poorly to sumatriptan 50 mg. BACKGROUND: Poor response to sumatriptan therapy for acute migraine attacks has been documented in the literature, but few controlled trials have investigated the efficacy of an alternative triptan in this subgroup of patients. METHODS: Patients with an International Headache Society diagnosis of migraine who self-described as experiencing at least two unsatisfactory responses to sumatriptan treated their first migraine attack with open-label sumatriptan 50 mg. Patients who did not achieve 2-hour pain relief (improvement of headache from moderate/severe to mild/no headache) were then randomized to treat their second attack with almotriptan 12.5 mg or placebo under double-blind conditions. RESULTS: In the first attack, 221 of 302 participants (73%) did not achieve 2-hour pain relief with sumatriptan and were randomized to treatment of their second attack with almotriptan 12.5 mg or placebo. Of the 198 sumatriptan nonresponders who treated their second attack (99 almotriptan; 99 placebo), 70% had severe headache pain at baseline. Two-hour pain-relief rates were significantly higher with almotriptan compared to placebo (47.5% vs 23.2%; P<.001). A significant treatment effect for almotriptan was also seen in pain-free rates at 2 hours (33.3% vs 14.1%; P<.005) and sustained freedom from pain (20.9% vs 9.0%; P<.05). In the second attack, 7.1% of patients in the almotriptan group experienced adverse events compared to 5.1% in the placebo group (P=.77). CONCLUSIONS: Almotriptan 12.5 mg is an effective and well-tolerated alternative for patients who respond poorly to sumatriptan 50 mg. A poor response to one triptan does not predict a poor response to other agents in that class.

Adult↗
PubMed2000

Influence of sumatriptan on gastric fundus tone and on the perception of gastric distension in man.

BACKGROUND: In animals, activation of 5-HT(1) like receptors causes a relaxation of the gastric fundus through the activation of intrinsic inhibitory neurones. AIMS: To investigate the effect of sumatriptan, an agonist at enteric neuronal 5-HT(1) receptors, on fasting fundus tone and sensitivity to gastric distension in man. METHODS: A gastric barostat was used to study the effect of placebo and sumatriptan, 6 mg subcutaneously, on basal fundic tone in healthy subjects. In addition, stepwise isobaric and isovolumetric gastric distensions were performed and perception was measured before and after the administration of placebo and sumatriptan. RESULTS: Placebo had no significant effects on gastric tone and on perception. Sumatriptan induced an immediate relaxation of the gastric fundus, reflected by an intragastric volume increase of 209 (39) ml (p<0.0005). After sumatriptan, intragastric pressures at the thresholds for perception or discomfort were not significantly altered. However, the intragastric volumes and the corresponding calculated wall tensions at perception and discomfort thresholds were significantly increased. CONCLUSIONS: Administration of the 5-HT(1) receptor agonist sumatriptan induces a relaxation of the gastric fundus in man, allowing larger intragastric volumes before thresholds for perception or discomfort are reached. The effects of sumatriptan on the gastric fundus may have therapeutic potential in the treatment of patients with functional dyspepsia.

Adult↗
PubMed2004

Efficacy of 1,000 mg effervescent acetylsalicylic acid and sumatriptan in treating associated migraine symptoms.

Recently a new effervescent acetylsalicylic acid (ASA) tablet with high buffering capacity has been developed. In this double-blind, 3-arm, multicenter, parallel-group study, 433 patients were treated either with 1,000 mg effervescent ASA or 50 mg encapsulated sumatriptan or placebo. The primary endpoint was the percentage of patients with complete remission of the 3 accompanying symptoms nausea, photophobia and phonophobia within 2 h after intake of the study drug. 43.8% of patients treated with ASA, 43.7% of patients treated with sumatriptan and 30.9% of patients treated with placebo showed complete remission of all 3 accompanying symptoms (p < 0.05 for ASA and sumatriptan vs. placebo). Both active treatments were superior to placebo regarding the individual symptoms photophobia and phonophobia, but not for nausea. The percentage of patients with reduction in headache severity from moderate or severe to mild or no pain (secondary objective) was 49.3% for ASA, 48.8% for sumatriptan and 32.9% for placebo. All active treatments were superior to placebo (p < 0.05). 25.3, 24.4 and 14.5% of patients treated with ASA, sumatriptan or placebo were pain free at 2 h. Drug-related adverse events were reported in 3.9, 4.7 and 6.7% of patients treated with placebo, ASA or sumatriptan. The study showed that administration of effervescent ASA leads to remission of the migraine symptoms nausea, photophobia and phonophobia, reduces migraine headache and is comparable to sumatriptan.

Adolescent↗
PubMed2005

Almotriptan in migraine patients who respond poorly to oral sumatriptan: a double-blind, randomized trial.

OBJECTIVE: To investigate the efficacy and tolerability of almotriptan 12.5 mg in migraine patients who respond poorly to sumatriptan 50 mg. BACKGROUND: Poor response to sumatriptan therapy for acute migraine attacks has been documented in the literature, but few controlled trials have investigated the efficacy of an alternative triptan in this subgroup of patients. METHODS: Patients with an International Headache Society diagnosis of migraine who self-described as experiencing at least two unsatisfactory responses to sumatriptan treated their first migraine attack with open-label sumatriptan 50 mg. Patients who did not achieve 2-hour pain relief (improvement of headache from moderate/severe to mild/no headache) were then randomized to treat their second attack with almotriptan 12.5 mg or placebo under double-blind conditions. RESULTS: In the first attack, 221 of 302 participants (73%) did not achieve 2-hour pain relief with sumatriptan and were randomized to treatment of their second attack with almotriptan 12.5 mg or placebo. Of the 198 sumatriptan nonresponders who treated their second attack (99 almotriptan; 99 placebo), 70% had severe headache pain at baseline. Two-hour pain-relief rates were significantly higher with almotriptan compared to placebo (47.5 vs. 23.2%; p < 0.001). A significant treatment effect for almotriptan was also seen in pain-free rates at 2 h (33.3 vs. 14.1%; p < 0.005) and sustained freedom from pain (20.9 vs. 9.0%; p < 0.05). In the second attack, 7.1% of patients in the almotriptan group experienced adverse events compared to 5.1% in the placebo group (p = 0.77). CONCLUSIONS: Almotriptan 12.5 mg is an effective and well-tolerated alternative for patients who respond poorly to sumatriptan 50 mg. A poor response to one triptan does not predict a poor response to other agents in that class.

Adolescent↗
PubMed1993

Efficacy of subcutaneous sumatriptan in repeated episodes of migraine.

This double-blind, placebo-controlled, multicenter, crossover study investigated the efficacy and tolerability of sumatriptan administered for up to three separate migraine attacks. One hundred twenty adults received sumatriptan (SC, 6 mg; three attacks) and placebo (one attack). Patients completed questionnaires assessing the impact of migraine on their lives and the performance of sumatriptan relative to their usual acute therapies. Sumatriptan statistically outperformed placebo on all efficacy measures, including pain severity; presence/absence of nausea, vomiting, phonophobia, and photophobia; rescue medication use; and clinical disability. Efficacy was consistently maintained with repeated administration. For all attacks, pain relief 90 minutes postdose occurred in 86% to 90% of sumatriptan-treated patients, compared with 9% to 38% of placebo-treated patients. Sumatriptan was well tolerated, and the frequency and severity of adverse events did not change with repeated administration. Patients' perceptions of sumatriptan were consistent with clinical data demonstrating the drug's high degree of efficacy and tolerability.

Adolescent↗
PubMed1997

A study of the effects of sumatriptan on myocardial perfusion in healthy female migraineurs using 13NH3 positron emission tomography.

Sumatriptan, a 5-HT1D receptor agonist, is believed to alleviate migraine attacks by extracerebral vasoconstriction. Chest pain associated with myocardial ischemia may occur after sumatriptan administration. We investigated the effect of a single 6-mg subcutaneous dose of sumatriptan on myocardial perfusion (MP) as measured by 13NH3 positron emission tomography (PET) in a randomized, double-blind, placebo-controlled, crossover trial at the Clinical PET Centre, Guy's and St. Thomas' Hospitals, London. Nineteen volunteer female migraineurs, age range 33 to 62 years, at low risk for ischemic heart disease were included. All bad undergone previous treatment with oral or intravenous sumatriptan. Patients were recruited by advertisement and referral from local neurology specialists. Each volunteer underwent two scanning sessions. On each occasion, a baseline dynamic 13NH3 PET scan was acquired followed by a 13NH3 PET scan 10 minutes after subcutaneous injection of placebo or 6 mg of sumatriptan. Regional MP was measured in five myocardial regions using the Patlak system of image analysis. The mean % change from baseline (+/-SD) in global MP after placebo was +9.5% +/- 18.0 and after sumatriptan was +6.6% +/- 18.8 (repeated measures ANOVA for treatment effect p = 0.56). There were no significant differences in MP changes from baseline observed in any of the five myocardial regions (treatment p = 0.32 to 0.84). These data suggest that in healthy female migraineurs, a single 6-mg subcutaneous dose of sumatriptan does not cause a significant change in regional or global myocardial perfusion.

Adult↗
PubMed2000

Eletriptan in acute migraine: a double-blind, placebo-controlled comparison to sumatriptan. Eletriptan Steering Committee.

OBJECTIVE: To compare the efficacy, safety, and tolerability of oral eletriptan (20 mg, 40 mg, and 80 mg) with that of oral sumatriptan (100 mg) and placebo for the acute treatment of migraine. BACKGROUND: Eletriptan is a potent and selective agonist at human recombinant 5HT1B/1D receptors, with efficacy in animal models that predict antimigraine activity. In healthy volunteers, the pharmacokinetics of eletriptan are characterized by linear and rapid oral absorption. METHODS: Randomized, double-blind, parallel-group study conducted in 857 outpatients with a diagnosis of migraine according to the International Headache Society (IHS) criteria. Of these, 692 took study medication for one acute migraine attack and provided on-drug efficacy data. Subjects received either placebo, 100 mg of sumatriptan or 20 mg, 40 mg, or 80 mg of eletriptan for the treatment of an acute migraine attack. The primary endpoint was the percentage of patients with a headache response (improvement in pain intensity from moderate or severe to mild or none) at 2 hours after treatment. RESULTS: At the primary endpoint (2 hours after dosing), headache response rates were 24% (30/126) for placebo; 55% (63/115) for sumatriptan, 100 mg; 54% (70/129) for eletriptan, 20 mg; 65% (76/117) for eletriptan, 40 mg; and 77% (91/118) for eletriptan, 80 mg. There was a difference compared with placebo (p<0.001) for all doses of eletriptan, and at 2 hours there was a difference between sumatriptan, 100 mg, and eletriptan, 80 mg (p<0.001). Headache-free rates at 2 hours were superior to placebo (6%; p<0.001) for both the 80-mg dose of eletriptan (37%) and the 40-mg dose (29%), with the 80-mg dose also being superior to 100 mg of sumatriptan (23%; p<0.05). Eletriptan and sumatriptan were well tolerated, and the majority of adverse events were mild or moderate in intensity and transient. CONCLUSION: In this placebo-controlled trial, eletriptan, at selected doses, demonstrated superior efficacy, onset of action and patient acceptability in the acute treatment of migraine when compared with oral sumatriptan and placebo.

Acute Disease↗
PubMed1998

Sumatriptan contraindications and the serotonin syndrome.

OBJECTIVE: To determine the risk for serotonin syndrome associated with the concomitant use of sumatriptan and the currently contraindicated therapies, that is, the monoamine oxidase inhibitors (MAOIs), serotonin selective-reuptake inhibitors (SSRIs), and lithium. METHODOLOGY: A comprehensive search for reports of serotonin syndrome associated with sumatriptan use was conducted by using tertiary drug interaction literature, MEDLINE, EmBASE, Biological Abstracts, Current Contents, Reactions, ClinAlert, and the International Pharmaceutical Abstracts. In addition, related reports from the proprietary manufacturers, the Health Protection Branch of Health Canada, and the World Health Organization Collaborative Centre for International Drug Monitoring were also solicited. RESULTS: The concurrent use of sumatriptan with an SSRI or lithium has been reported to cause symptoms suggestive of serotonin syndrome in 16 and 2 cases, respectively. There were no reports involving MAOIs. In general, the reports indicated a mild-to-moderate, self-limited course with some features consistent with the serotonin syndrome. We found published reports of sumatriptan use without adverse events involving 148 patients receiving SSRIs, 31 patients taking MAOIs, and a small number using lithium. CONCLUSIONS: Clinical evidence supporting the strict contraindication of MAOIs, SSRIs and lithium was not identified. The balance of documented clinical experience pertaining to the use of sumatriptan concurrently with SSRIs or lithium suggests that most patients tolerate this combination without incident. Because there is little reliable experience with sumatriptan in combination with MAOIs, we suggest that sumatriptan should continue to be avoided in patients taking these agents until further data demonstrating safety become available.

Contraindications↗
PubMed2000

Naproxen sodium decreases migraine recurrence when administered with sumatriptan.

Forty to 78% of the patients using sumatriptan for the acute treatment of migraine may present recurrence at least occasionally. The concomitant use of a NSAID (nonsteroidal anti-inflammatory drug) has been recommended to decrease the recurrence rate. Sixty seven patients that treated successfully 8 migraine attacks with 100 mg of sumatritpan PO and presented recurrence in at least 5 attacks were studied prospectively. The patients received 100 mg of sumatriptan and 550 mg of naproxen sodium PO to treat 4 consecutive moderate or severe migraine attacks. The recurrence rate, once at least 62.5% (5 out of 8 attacks), decreased to 14.2% (38 out of 268 attacks) with the combination of compounds (p<0.0001). We then studied two groups of 13 patients made randomicaly from the 67 initially evaluated, that were given sumatriptan 100 mg plus naproxen sodium 550 mg or placebo, in a double-blind design, to treat 3 other consecutive migraine attacks. Each group of patients treated 39 attacks. The recurrence among the patients taking sumatriptan plus placebo was 59% (23 out of 39 attacks) and the recurrence presented by the group taking sumatriptan plus naproxen was 25.5% (10 out of 39 attacks) (p<0.0003). We concluded that the combination of sumatriptan plus naproxen sodium decreases significantly migraine recurrence presented by patients taking sumatriptan alone.

Acute Disease↗
PubMedDate not supplied

A comparison of the cost-effectiveness of almotriptan and sumatriptan in the treatment of acute migraine using a composite efficacy/tolerability end point.

OBJECTIVE: To use a composite efficacy/tolerability end point to compare the cost-effectiveness, from the perspective of a U.S. health care payer, of almotriptan and sumatriptan in the treatment of an acute migraine attack. METHODS: The composite end point. Sustained pain free and No Adverse Events. (SNAE) was created from the sustained pain free and adverse event rates obtained in a meta-analysis of 53 placebo-controlled trials of oral triptans. The total direct cost of treating a single migraine attack was calculated from published sources. RESULTS: In the base-case analysis, the average cost-effectiveness ratios (CERs) were 82 US dollars , 133 US dollars , and 138 US dollars (per attack at which SNAE is achieved, 2004 prices) for almotriptan 12.5 mg, sumatriptan 50 mg, and sumatriptan 100 mg, respectively; the incremental CERs for almotriptan 12.5 mg were 12 US dollars and 16 US dollars (compared with sumatriptan 50 mg and sumatriptan 100 mg, respectively) per incremental attack at which SNAE is achieved. Sensitivity analyses were conducted to explore the impact of (1) relaxing the base-case assumptions (independence of efficacy and tolerability, uniform apportionment of health service use costs across attacks, number of tablets used to treat 1 attack); (2) varying input costs; and (3) uncertainty in the efficacy and tolerability estimates from the meta-analysis. In all of these sensitivity analyses, almotriptan 12.5 mg remained cost effective compared with sumatriptan 50 mg and 100 mg. CONCLUSION: Almotriptan was economically superior to sumatriptan in the treatment of a migraine attack.

Acute Disease↗
PubMed1997

A multinational investigation of the impact of subcutaneous sumatriptan. IV: Patient satisfaction.

This report describes the patient satisfaction results from a prospective, sequential, multinational study. The study was conducted to concurrently evaluate the effects of sumatriptan, compared with customary therapy, on clinical parameters, health-related quality of life, productivity and patient satisfaction in adult patients with moderate to severe migraine. Patients treated migraine attacks for 12 weeks with their customary therapy, followed by 24 weeks' treatment with subcutaneous sumatriptan 6 mg. A questionnaire was conducted at the end of each study phase, or retrospectively at the end of the study, to assess patient satisfaction with customary therapy and sumatriptan. Sumatriptan was considered by most patients (67 to 85%) to be dependable and fast-acting, and to have a long duration of effect, allowing a quick return to normal activities. By comparison, 15 to 32% of patients considered that their customary therapy possessed the same attributes. However, customary therapy was considered to be easy/very easy to use by 82% of patients compared with 62% for subcutaneous sumatriptan. 89% of patients indicated that they would use sumatriptan again in the future. This study demonstrates that treatment of migraine attacks with subcutaneous sumatriptan for 24 weeks is associated with greater patient satisfaction as regards specific drug attributes than customary therapy.

Adolescent↗
PubMed1998

Antinociceptive effect of sumatriptan in mice.

Antinociceptive effect of the antimigraine drug sumatriptan (5-HT1A agonist) was studied against acetic acid-induced writhing in mice. Sumatriptan produced the effect in a dose-dependent manner (1, 5, 10 and 20 mg/kg, s.c.). Naloxone (1 mg/kg i.p.) an opiate antagonist failed to reverse sumatriptan-induced antinociception. Cholinomimetic physostigmine (0.05 mg/kg, i.p.) potentiated and the muscarinic antagonist atropine (5 mg/kg, i.p.) blocked the antinociceptive effect of sumatriptan, respectively. The antinociceptive effect of sumatriptan was compared with an another 5-HT agonist (5-HT1A) buspirone which also produced antinociception. Like sumatriptan-analgesia, the buspirone response was also potentiated by physostigmine in atropine sensitive way. Further, buspirone potentiated the analgesic effect of sumatriptan. These observations suggest that 5-HT1A agonists produce antinociception possibly by modulating central cholinergic activity.

Animals↗
PubMed2000

Oral therapy for migraine: comparisons between rizatriptan and sumatriptan. A review of four randomized, double-blind clinical trials.

The introduction in 1991 of sumatriptan succinate, the first approved 5-HT1B/1D receptor agonist, represented a significant advance in the treatment of acute migraine. The approval of three additional 5-HT receptor agonists, including rizatriptan, has further expanded the options for migraine treatment. Four randomized clinical trials have compared the effects of oral sumatriptan with those of oral rizatriptan. Forty mg rizatriptan was more effective than 100 mg sumatriptan but was associated with a high incidence of adverse events. Five mg rizatriptan was comparable to 50 mg sumatriptan. In two trials, rizatriptan 10 mg, the recommended dose in most countries, had a more rapid onset of action than 50 mg (p<0.05) and 100 mg sumatriptan (p=0.075). In addition, 10 mg rizatriptan resulted in more patients being pain-free after 2 hours than 100 mg sumatriptan (p<0.05), and resulted in fewer drug-related adverse events than sumatriptan.

Administration, Oral↗