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PubMed2003

Parental satisfaction with sumatriptan nasal spray in childhood migraine.

Migraine headaches are a frequently encountered neurologic problem in children. The utility of the triptans has not been as clearly documented in this population, although it is well delineated in acute migraine attacks in adults. We conducted a retrospective chart review of our experience with using sumatriptan nasal spray in children aged 5 to 12 years from our headache clinic population with migraine headaches. The nasal spray formulation is used frequently in our clinic population with patients who have failed over-the-counter therapy with ibuprofen or acetaminophen. None of the triptans are approved by the US Food and Drug Administration for use in children or adolescents (12 years and older). One hundred of these patients were identified, and their parents or guardians completed a standardized questionnaire regarding their child's response to sumatriptan nasal spray in acute migraine. Fifty-seven of 100 families completed the questionnaire, and 44 of 57 families (77%) reported good to excellent relief of their child's migraine attacks with sumatriptan nasal spray. In our cohort of pediatric patients, sumatriptan nasal spray was effective and well tolerated when used for abortive therapy of acute migraine attacks.

Administration, Intranasal↗
PubMed2006

Preliminary brain-targeting studies on intranasal mucoadhesive microemulsions of sumatriptan.

The aim of this investigation was to prepare microemulsions containing sumatriptan (ST) and sumatriptan succinate (SS) to accomplish rapid delivery of drug to the brain in acute attacks of migraine and perform comparative in vivo evaluation in rats. Sumatriptan microemulsions (SME)/sumatriptan succinate microemulsions (SSME) were prepared using titration method and characterized for drug content, globule size and size distribution, and zeta potential. Biodistribution of SME, SSME, sumatriptan solution (SSS), and marketed product (SMP) in the brain and blood of Swiss albino rats following intranasal and intravenous (IV) administrations were examined using optimized technetium-labeled ((99m)Tc-labeled) ST formulations. The pharmacokinetic parameters, drug targeting efficiency (DTE), and direct drug transport (DTP) were derived. Gamma scintigraphy imaging of rat brain following IV and intranasal administrations were performed to ascertain the localization of drug. SME and SSME were transparent and stable with mean globule size 38 +/- 20 nm and zeta potential between -35 to -55 mV. Brain/blood uptake ratios at 0.5 hour following IV administration of SME and intranasal administrations of SME, SMME, and SSS were found to be 0.20, 0.50, 0.60, and 0.26, respectively, suggesting effective transport of drug following intranasal administration of microemulsions. Higher DTE and DTP for mucoadhesive microemulsions indicated more effective targeting following intranasal administration and best brain targeting of ST from mucoadhesive microemulsions. Rat brain scintigraphy endorsed higher uptake of ST into the brain. Studies conclusively demonstrated rapid and larger extent of transport of microemulsion of ST compared with microemulsion of SS, SMP, and SSS into the rat brain. Hence, intranasal delivery of ST microemulsion developed in this investigation can play a promising role in the treatment of acute attacks of migraine.

Administration, Intranasal↗
PubMed1996

Absorption, pharmacokinetics and metabolism of 14C-sumatriptan following intranasal administration to the rat.

1. Studies have been carried out to investigate the absorption of sumatriptan after intranasal administration to rats. The pharmacokinetics, metabolism and excretion of 14C-sumatriptan were compared following intranasal and intravenous dosing to male and female albino rats using an aqueous buffered formulation at pH 5.5. 2. Following intravenous administration sumatriptan was eliminated from plasma with a half-life of about 1.1 h. After intranasal administration there was rapid absorption of part of the dose and two peak plasma concentrations were observed, initially at 0.5 and then at 1.5-2 h. The elimination half-life after the second peak was estimated as being about 4 h. 3. Radioactivity was largely excreted in urine (up to 89% of dose in 168 h) after both intravenous and intranasal administration, with a faster rate of excretion after intravenous dosage (73% males, 64% females within 6 h) than after intranasal dosage (37% males, 40% females within 6 h). 4. 14C-sumatriptan was the major component in urine and in extracts of faeces after both intravenous and intranasal administration. The major metabolite excreted in urine and faeces was GR49336, the indole acetic acid analogue. 5. The results of this in vivo rat study suggest that absorption of the dose via the nasal mucosa is incomplete after intranasal administration and that there is a secondary absorption phase probably reflecting oral absorption of part of the dose. The bioavailability is estimated as about 30%, for the period 0-6 h.

Absorption↗
PubMed1995

Sumatriptan (Imitrex) transport by the human placenta.

Sumatriptan (Imitrex), a selective 5-hydroxytryptamine receptor agonist, has been found to be of therapeutic benefit in the acute management of migraine. There is no information on the transfer of this agent across the human placenta. Accordingly, the current study assessed the transport of this drug across the normal term human placenta, using the isolated perfused single cotyledon technique. We found that only about 15% of a single dose of the agent placed in the maternal reservoir crossed into the fetal compartment over 4 hr. Given the average elimination half-life of 2 hr for sumatriptan, it is evident that only very small amounts of the agent will cross from mother to fetus after single doses of Imitrex. Only the parent drug entered the fetal compartment. Metabolites were not detected in the perfusates, but there was evidence of some metabolism of sumatriptan in the placenta. The nature of the metabolites has not been determined. The mechanism of transfer of the drug across the placenta is passive (i.e., the clearance is similar to L-glucose which is passively transported), the rate of transfer is equal in both directions (maternal to fetal and in the reverse), and the drug does not cross into the fetus against a concentration gradient. This passive transport of sumatriptan across the placenta is consistent with its molecular weight, its water solubility, and its slow penetration across the blood-brain barrier in experimental animals.

Biological Transport↗
PubMed1999

[The efficacy of subcutaneous sumatriptan for the treatment of migraine attack].

Sumatriptan is a novel drug for the treatment of acute migraine attacks. The aim of this study was to assess the efficacy of a 6 mg s.c. Sumatriptan in the early acute treatment of migraine. Patients were recruited with a current history of migraine with and without aura. 58 patients treated 1 migraine attacks at home using an autoinjector with a dose 6 mg of sumatriptan. Patient assessed headache severity and other migraine symptoms 1 and 4 h after treatment. 55% patients reported headache relief after 1 h and 77% patients after 4 h. Adverse events were reported by 11% of patients. In conclusion, sumatriptan were effective and well tolerated in the acute treatment of migraine.

Acute Disease↗
PubMed2001

[Effect of sumatriptan on cerebral blood flow during migraine headache: measurement by sequential SPECT used 99mTc-ECD background subtraction method].

The present study was designed to examine the effect of sumatriptan on regional cerebral blood flow (CBF) during migraine headache. Nine cases were examined by 99mTc-ECD background subtraction method for the absolute value measurement of regional CBF before and after sumatriptan injection. rCBF except for occipital and perioccipital lobes, were increased 10-20% during migraine headache and significant decreases were observed by sumatriptan injection. Two cases of nine had transiently increased systemic blood pressure and cardiac pulse rate, however, all cases improved migraine headache after injection of sumatriptan.

Adolescent↗
PubMed2002

Almotriptan versus sumatriptan in migraine treatment: direct medical costs of managing adverse chest symptoms.

OBJECTIVE: Triptans, a popular class of drugs for treatment of migraine headaches, can cause adverse events including chest symptoms. This study estimated the direct medical costs of managing chest symptoms in patients treated for acute migraine with almotriptan or sumatriptan using an economic model. METHODS: The economic model of this study combined data from a randomized clinical trial that compared almotriptan with sumatriptan and data from a practice pattern survey of physicians. The pertinent clinical evaluation period was the time immediately after administration of the first medication dose. The model was developed from the perspective of a managed care payer. RESULTS: The average direct medical cost of managing chest symptoms that appeared after the first dose of an oral triptan was $0.22 for patients treated with almotriptan and $1.64 for patients treated with sumatriptan, a difference of $1.42 per patient. CONCLUSION: Relative to sumatriptan, treatment with almotriptan is likely to reduce patient care costs associated with chest symptom adverse events.

Chest Pain↗
PubMed2002

Lack of sumatriptan-induced aortic contraction or relaxation: 5-HT1B receptor protein detected in endothelium and smooth muscle of vasa vasorum but not aorta.

Since 5-HT1B receptor mRNA was reported in rat aorta, and 5-HT1B receptor activation has been linked to vascular contraction, we explored sumatriptan-induced contractility and immunohistochemical density of 5-HT1B receptor protein in rat aorta. Sumatriptan (up to 10(-4) M), a 5-HT1B/1D receptor agonist, did not contract the endothelial intact or denuded rat aorta, even in the presence of L-NAME or after induction of modest tone with PGF2 alpha (10(-6) M). Sumatriptan also did not relax aortic preparations precontract with PGF2 alpha (3 x 10(-6) M) or phenylephrine (3 x 10(-7) M). Using a polyclonal antibody directed against the 5-HT1B receptor, minimal 5-HT1B receptor protein was detected in either the endothelium or smooth muscle of the rat aorta. However, dense 5-HT1B receptor protein was found in the vascular smooth muscle of the vasa vasorum supplying the aorta. Thus, the 5-HT1B receptor mRNA detected in tissue extracts of the rat aorta most likely reflects 5-HT1B receptor expression in the arterioles of the vasa vasorum. These studies support the link between the 5-HT1B receptor and vascular contraction in that the aorta with low density of 5-HT1B receptors lacked responses to sumatriptan, an agonist thought to contract blood vessels via 5-HT1B/1D receptors. Furthermore, caution must be observed when using 5-HT1B receptor mRNA to suggest receptor protein in tissues since this RT-PCR product may be derived predominantly from small blood vessels.

Animals↗
PubMed1992

[Sumatriptan and its use in treatment of migraine and cluster headaches].

The methods used presently for abortion of the attacks of migraine and cluster headache are not fully satisfactory which causes that the search for new therapies is continuing. Although the mechanism of migraine attacks remains unexplained, it is thought that an important role in it is played by serotonin receptors, vasodilation in certain regions and opening of arteriovenous communications in the head. Sumatriptan is an agonist of 5-HT1 -like receptors and exerts a selective vasoconstricting effect on the arteries of the head, particularly in the rami of the carotid artery. In 1988 the first reports appeared on the effectiveness of the drug in migraine attacks. In the following years extensive, multicentre and international studies of the drug were carried out on over 600 healthy volunteers and nearly 6000 patients with migraine. The studies demonstrated that Sumatriptan was effective in abortion of migraine attacks. After oral administration of 100 mg or subcutaneous injection of 6 mg in nearly 70% of cases the attack regressed or was greatly alleviated, similarly as other symptoms accompanying the headache such as photophobia, nausea, vomiting. Studies were undertaken also on the effectiveness of Sumatriptan in emergency treatment of cluster headache, and good results were again achieved. The tolerance of the drug is good, although in some cases side effects develop, usually transient and mild, among them tingling, feeling of pressure, heat or heaviness of the head or chest, taste change and burning sensation at the site of injection. Sumatriptan, similarly as all novel drugs, requires caution in its use, particularly in patients with coronary heart disease and hypertension, and also in old patients. As yet, the use of the drug in paediatric migraine or in pregnancy is not recommended.

Cluster Headache↗
PubMedDate not supplied

[Effect of sumatriptan on facial temperature variations, blood pressure and electrocardiogram in healthy subjects and patients with migraine without aura].

40 patients were evaluated for skin temperature changes from baseline measurements and after 6 mg subcutaneous sumatriptan administration. During examination, skin temperature were recorded on a color picture at 10', 20', 30', 60', 90' and 120 minutes after sumatriptan administration. At the some time, heart rate (HR), systolic (SBP), diastolic (BDP) blood pressure and ECG-monitoring were automatically recorded. The patients were subgrouped as follow: 20 non migrainous control subjects (6 males and 14 females) aged 19 to 55 years (mean age 39.5 +/- 15.4); 20 headache free migrainous patients (6 males and 14 females) aged 25 to 46 years (mean age 37.8 +/- 8.4). Our data demonstrate a significant reduction in skin temperature (face) in all patients studied. 10 minutes after sumatriptan administration a significant increase (p > 0.001) both in SBP and BDP was observed. This findings suggest that sumatriptan show a vasoconstrictor effect as demonstrate by reduction in face temperature both in nonmigrainous and in migrainous patients. The unchange in HR and ECG and the transient increase in blood pressure, not associated with clinical symptoms, suggest that this drug may be used in migrainous patients.

Adult↗
PubMed1995

[Sumatriptan treatment of migraine in general practice. A randomized, double-blind, placebo-controlled cross-over study].

Two hundred and thirty migraineurs diagnosed by their general practitioners in accordance with their usual practice were included. The patients treated two migraine attacks at home by subcutaneous injection of sumatriptan or placebo and the alternative medication for the second attack (cross-over). When sumatriptan was compared to placebo, significantly more of the 209 evaluable patients reported headache relief at one hour (56% v 8%, p < 0.001) and two hours (62% v 15%, p < 0.001) after the first injection. Resolution of nausea, photophobia and phonophobia was significantly more common in patients on sumatriptan than on placebo (p < 0.001 for all comparisons). The adverse events were usually transient and of mild or moderate severity, although, three patients withdrew due to adverse events. Ninety-five percent of patients evaluated by a neurological research fellow met the International Headache Society's criteria for migraine. In general practice, sumatriptan taken subcutaneously using an autoinjector at home was an effective and well tolerated acute treatment for migraine.

Adolescent↗
PubMed1995

Effects of sumatriptan on isolated rabbit heart.

Sumatriptan provokes, in healthy subjects as well as in those who suffer from hemicrania, a slight increase in both systolic and diastolic arterial pressure. It has also been shown to increase the pressure of pulmonary circulation and to reduce the calibre of coronary arteries. The present investigation was undertaken to study the effects of sumatriptan (75 ng/l) on isolated rabbit hearts. Fifteen isolated rabbit hearts, perfused according to Langerdoff's procedure, were divided into two groups: Group I (5 hearts), perfused with Krebs-Henseleit solution, as a control, and Group II (10 hearts), perfused with Krebs-Henseleit mixed with sumatriptan succinate (75 ng/l). After 30 min of perfusion, the basal values of heart rate (HR) dp/dt, systolic ventricular pressure (SVP), diastolic ventricular pressure (DVP) and coronary flow (CF) were measured. The above values in either control or treated hearts were measured 5, 15, 30, 45, 60 min after recording the baseline values. HR, SVP, DVP, dp/dt and CF did not show significant differences in the two groups. The present data suggest that sumatriptan does not exert any action on isolated rabbit hearts.

Animals↗
PubMed1993

Sumatriptan: a new serotonin agonist for the treatment of migraine headache.

Sumatriptan is a new serotonin receptor agonist that is useful in the treatment of migraine headache. More than 70 percent of patients with migraine headaches respond to subcutaneous sumatriptan within two hours, although headaches recur in up to two-thirds of initial responders. Side effects include lightheadness, a sensation of tingling or warmth, and breathlessness. Compared with the combination of ergotamine and caffeine, sumatriptan appears to work earlier and more completely but is associated with a higher rate of recurrent headache. Sumatriptan may be a useful additional therapy for migraine headache.

Humans↗
PubMed1996

5-Carboxamido-tryptamine, CP-122,288 and dihydroergotamine but not sumatriptan, CP-93,129, and serotonin-5-O-carboxymethyl-glycyl -tyrosinamide block dural plasma protein extravasation in knockout mice that lack 5-hydroxytryptamine1B receptors.

We studied the dural plasma protein extravasation response after unilateral electrical stimulation of the trigeminal ganglion in mice lacking serotonin 5-HT1B (5-HT1D beta) receptors by modifying a technique previously described in rats or guinea pigs. We investigated the inhibitory effects of six 5-HT1 receptor agonists in this model: 3-(1,2,5,6-tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one (CP-93,129), sumatriptan, serotonin-5-O-carboxymethyl-glycyl -tyrosinamide (GTI), 5-methylaminosulfonylmethyl-3-(N-methylpyrrolidin-2R -ylmethyl)-1H-indole (CP-122,288), 5-carboxamido-tryptamine (5-CT), and dihydroergotamine. The plasma extravasation response did not differ between wild-type and mutant after vehicle injection. The potency of sumatriptan, CP-122,288, CP-93,129, and 5-CT in wild-type mice was similar to that previously reported for rats. CP-122,288 (1 nmol kg), 5-CT (1 nmol/kg), and dihydroergotamine (72 nmol/kg) inhibited plasma protein extravasation within dura mater after electrical trigeminal ganglion stimulation in both wild-type and knockout mice, which suggests that these agonists act predominantly via receptors other than 5-HT1B. Unlike the wild-type mice, CP-93,129 (1.4 mumol/kg), a specific 5-HT1B receptor agonist, had no effect in knockout mice. The same held true for sumatriptan (0.7 mumol/kg) and GTI (0.6 mumol/kg). These results suggest that CP-93,129, sumatriptan, and GTI exert their effects via 5-HT1B (5-HT1D beta) receptors in mice.

Animals↗
PubMed1996

[18 months long-term analysis of effectiveness, safety and tolerance of sumatriptan s.c. in acute therapy of migraine attacks].

The aim of the open prospective study was to investigate the efficacy, safety and tolerability of subcutaneous sumatriptan in acute migraine treatment. Patient self-treatment was monitored over a time period of 6-18 months with 6 mg of sumatriptan administered subcutaneously by an autoinjector. In total, 2,263 patients participated in the study. Headache intensity was documented by the patient in a headache diary before and 1 and 2 h after application. During the study period from October 1991 to June 1993, 43,691 migraine attacks were investigated. Treatment with sumatriptan was efficient in 89.5% of the attacks. Headache relief was achieved in 71%. Headache reoccurred in 22.7% of the attacks, and therefore a second injection was administered. An intraindividual treatment efficacy of 80-100% was achieved in 82.9% of the patients. During long-term treatment the ratio of effective treatment and headache frequency was constant; 4.9% of the patients withdrew from the study because of adverse events and because they felt the treatment was not effective. A total of 44.5% of the patients reported adverse events that were serious in 1.7%. Subcutaneous self-treatment with sumatriptan in the acute treatment of migraine is effective and well tolerated by the patients.

Adult↗
PubMed1993

Sumatriptan does not affect vasopressin secretion in humans.

The aim of the study was to investigate the effects of a new serotoninergic drug, sumatriptan, on arginine vasopressin secretion in humans. Plasma vasopressin concentrations were determined in eight healthy volunteers, before and after administration of 6 mg of sumatriptan, or placebo. No changes in hormone levels were found after sumatriptan or placebo administration. The results suggest that in humans serotoninergic mechanisms, which modulate vasopressin secretion, do not involve the serotonin receptor activated by sumatriptan.

Adult↗
PubMed1997

Involvement of central cholinergic system in antinociception induced by sumatriptan in mouse.

The antinociceptive effect of the antimigraine drug sumatriptan was assessed in mice (hot-plate and abdominal constriction tests). Antinociception induced by sumatriptan (10-30 mg kg-1 i.p.) was prevented by the muscarinic antagonist atropine (5 mg kg-1 i.p.), the ACh-depletor hemicolinium-3 (1 microgram per mouse i.c.v.) and the 5-HT1A antagonist NAN-190 (0.5 mg kg-1 i.p.). Naloxone, CGP-35348 and reserpine administered in doses suitable for blocking analgesia respectively induced by morphine, baclofen and clomipramine did not modify sumatriptan antinociception. On the basis of the above findings, we can deduce that sumatriptan was able to induce antinociception by increasing cholinergic neurotransmission through the stimulation of 5-HT1A receptors.

Analgesics↗
PubMed1997

[Treatment of acute attack of migraine with sumatriptan].

INTRODUCTION AND MATERIAL: In the Hospital Clínico Quirúrgico Hermanos Almeijeiras a randomized double blind clinical trial was carried out involving 52 patients who presented with painful migraine crises with or without prodromes. A group of 27 patients were given 6 mg of sumatriptan subcutaneously. Another group of 25 patients were given 1 mg of dihydroergotamine intramuscularly. It was seen that both drugs relieved the migrainous pain. However, sumatriptan did so in a greater percentage of patients. RESULTS AND CONCLUSIONS: There was earlier, and also more complete, relief of pain in those patients receiving sumatriptan. With regard to side-effects of sumatriptan were pain at the back of the site of injection, sensation of pressure at the back of the neck, facial flushing and asthenia.

Acute Disease↗