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PubMed1991

Migraine pain associated with middle cerebral artery dilatation: reversal by sumatriptan.

The combination of measurements of regional cerebral blood flow (rCBF) and blood velocity in the middle cerebral arteries (MCA) by transcranial doppler sonography was used to investigate cerebrovascular involvement in migraine. Ten migraine patients with unilateral headache were studied during an attack and when they had been free of attacks for 5 days (non-attack). On both occasions they were given as intravenous infusion of sumatriptan (2 mg), a 5-HT1-like receptor agonist, which relieved the symptoms within 30 min without affecting rCBF. The MCA velocity was normal on both sides on the non-attack day and on the unaffected side during the attack. However, during the attack the MCA velocity on the headache side was significantly lower than that on the non-headache side (45 vs 61 cm/s:mean difference 16.3 [95% confidence interval 10.3-22.3]; p = 0.02). The MCA velocity on the headache side returned to normal after treatment with sumatriptan and recovery. Since rCBF in the MCA supply territory was unaffected, the lower velocity can be explained only by dilatation of the MCA. The mean MCA diameter increase was estimated to be 20%. Thus, headache was associated with intracranial large arterial dilatation on the headache side. Sumatriptan predominantly had effects on the distended artery, which suggests that the 5-HT receptor system has a role in the pathogenesis of migraine.

Adult↗
PubMed1992

Neurogenic versus vascular mechanisms of sumatriptan and ergot alkaloids in migraine.

Sumatriptan and the ergot alkaloids are useful tools for deciphering drug mechanisms in migraine and related headaches. Both neuronal and vascular mechanisms have been proposed on the basis of actions of 5-HT at receptors resembling the 5-HT1D subtype. In this Viewpoint article, Michael A. Moskowitz argues that blockade of neural transmission and the neurogenic inflammatory response provides a mechanism by which sumatriptan and ergot alkaloids alleviate vascular headaches. He postulates, with similar arguments, that sumatriptan and ergot alkaloids may block headaches that develop from meningovascular inflammatory disorders such as from viral and bacterial meningitis and from the sequelae of head injury.

Ergot Alkaloids↗
PubMed1993

Clinical and experimental effects of sumatriptan in humans.

Recent reviews on the mode of action of the anti-migraine drug sumatriptan arrived at contrasting conclusions. Whereas some reviewers concluded that vasoconstriction is the most important action, others suggest that neuronal inhibition is essential. Both views were based predominantly on animal or in vitro experiments. In this comment, Michel Ferrari and Pramod Saxena review the experimental effects of sumatriptan in humans and discuss the clinical validity of both theories. In addition, they examine the initial efficacy of treatment and the mechanism of recurrence of headache within 24 hours, which is the most important drawback of sumatriptan in clinical practice, next to its possible cardiac side effects.

Animals↗
PubMed1992

Clinical effects and mechanism of action of sumatriptan in migraine.

Sumatriptan is a novel, highly effective drug against migraine and cluster headache attacks. It shows a remarkably selective pharmacological profile in animals. Determination of its mechanism of action in human should further the understanding of the pathophysiology of migraine and cluster headache. We, therefore, review current knowledge on the clinical and pharmacological effects of sumatriptan. Important pharmacological actions of sumatriptan are (i) poor penetration of the blood-brain barrier suggesting a peripheral point of action; (ii) 5-HT1-like/5-HT1d receptor-mediated vasoconstriction of large cerebral arteries and dural vessels; and (iii) blockade of neurogenic dural inflammation via 5-HT1d autoreceptor-mediated inhibition of vasoactive neuropeptides within the trigeminovascular system. Future research will tell which mechanism is involved in the pathophysiology of migraine and cluster headache.

Animals↗
PubMed1996

Determination of sumatriptan succinate in human plasma by high-performance liquid chromatography with coulometric detection and utilization of solid-phase extraction.

Sumatriptan succinate (the analyte) and naloxone (the internal standard) were extracted from plasma with a solid-phase extraction technique. Chromatography and detection were performed by isocratic reversed-phase high-performance liquid chromatography with coulometric end-point detection. The standard curve was linear over the range 0-100 ng/ml of sumatriptan succinate in plasma. The reproducibility (as defined by the coefficient of variation, C.V.) over the range of the standard curve was 4.9-7.3%. The recovery averaged 83%. The sensitivity was 0.25 ng of sumatriptan on column (allowing a concentration of 0.5 ng/ml to be determined from a 1-ml plasma sample volume). Plasma profiles of the analyte following subcutaneous (s.c.) administration in eight normal male volunteers, are presented.

Chromatography, High Pressure Liquid↗
PubMed1996

Fully automated assay for the determination of sumatriptan in human serum using solid-phase extraction and high-performance liquid chromatography with electrochemical detection.

A method is described for a fully automated, sensitive, accurate and precise assay for the determination of sumatriptan in human serum. The assay consists of solid-phase extraction followed by reversed-phase HPLC with electrochemical detection. The extraction procedure has been fully automated on a Zymate XP robot linked on-line to the HPLC system. The assay is linear over the analytical range 1-30 ng ml-1 and selective for sumatriptan with respect to endogenous plasma components and GR49336, the major circulating metabolite. The intra-assay data demonstrate a maximum bias and precision across the calibration range of 10% and 6.6% respectively. The inter-assay data demonstrate a maximum bias and precision across the calibration range of 6.7% and 8.8%, respectively. The extraction efficiency of the assay is approximately 90% and is constant across the calibration range. The assay was used for the determination of sumatriptan in serum clinical samples and was shown to be robust in sustained use over several months. The use of a Zymate XP robot allowed complete automation of the assay, which resulted in high-quality, high-throughput analyses.

Autoanalysis↗
PubMed2007

Sumatriptan for the treatment of undifferentiated primary headaches in the ED.

OBJECTIVE: In this study, we determine the effectiveness and adverse effects of sumatriptan when used in the emergency department (ED) as a first-line treatment for benign undifferentiated headaches, and determine if the International Headache Society (IHS) classification of migraine, probable migraine, or tension-type headache has any effect on the effectiveness of the treatment. We hypothesize that there is no difference in the effectiveness of pain relief or frequency and severity of adverse effects between patients with migraine, probable migraine, or tension-type headaches when treated with sumatriptan. METHODS: This was a prospective observational study of adult ED patients undergoing treatment for primary headaches (ie, patients in whom head trauma, vascular disorders, infection, or disorders of facial or cranial structures have been clinically excluded). Other exclusions were renal impairment, hepatic impairment, and risk factors for coronary artery disease. Consenting patients then were asked to complete a 100-mm visual analog scale (VAS) representing their perceived pain, after which they were interviewed by a research assistant who completed a headache diagnosis worksheet, which differentiates the headache by IHS criteria. The patient repeated the VAS score at 30 and 60 minutes. Data were analyzed using descriptive statistics and chi squared tests. RESULTS: One hundred forty-seven patients were enrolled: 84 (57.1%) patients with migraine headache, 45 (30.7%) with a probable migraine headache, and 18 (12.2%) with a tension headache. A 50% reduction in VAS scores 60 minutes postdose was seen in 87 (59%) of 147 patients; 50 (60%) of 84 of migraine patients, 25 (56%) of 45 of probable migraine patients, and 12 (67%) of 18 tension patients (P = .72). There were no serious adverse events reported. Forty-seven patients (32%) received rescue medications after the 60-minute VAS score: 29 (34.5%) patients in the migraine group, 15 (33.3%) patients in the probable migraine group, and 3 (15.8%) patients in the tension-type headache group (P = .26). CONCLUSIONS: Most of the patients presenting with primary headaches had migraine or probable migraine headaches. There was no difference in sumatriptan's effectiveness based on the classification of the headache using IHS criteria.

Adult↗
PubMed2004

High performance liquid chromatographic method for the determination of sumatriptan with fluorescence detection in human plasma.

A rapid and sensitive high performance liquid chromatography (HPLC) method with fluorescence detection has been developed for the determination of sumatriptan in human plasma. The procedure involved a liquid-liquid extraction of sumatriptan and terazosin (internal standard) from human plasma with ethyl acetate. Chromatography was performed by isocratic reverse phase separation on a C18 column. Fluorescence detection was achieved with an excitation wavelength of 225 nm and an emission wavelength of 350 nm. The standard curve was linear over a working range of 1-100 ng/ml and gave an average correlation coefficient of 0.9997 during validation. The limit of quantitation (LOQ) of this method was 1 ng/ml. The absolute recovery was 92.6% for sumatriptan and 95.6% for the internal standard. The inter-day and intra-day precision and accuracy were between 0.8-3.3 and 1.1-6.3%, respectively. This method is simple, sensitive and suitable for pharmacokinetics or bioequivalence studies.

Chromatography, High Pressure Liquid↗
PubMed2002

Serotonergic functioning in children with oppositional defiant disorder: a sumatriptan challenge study.

BACKGROUND: Several studies support the notion that disturbances in the central serotonergic function are related to impulsive aggression. There is recent evidence from studies on 5-HT(1B) knock-out mice that this specific receptor is involved in impulsive aggressive behavior. The aim of the present study was to investigate 5-HT(1B/1D) receptor functioning in normal intelligent hospitalized children with oppositional defiant disorder (ODD). METHODS: The growth hormone (GH) response to a challenge with the 5-HT(1B/1D) agonist sumatriptan was examined in 20 children with an ODD, of whom 13 had an attention-deficit/hyperactivity disorder comorbidity, and 15 normal control subjects (NC). Blood samples for growth hormone were collected repeatedly between 8:30 and 12:00 AM. Sumatriptan was administered at 10 AM. The effect of stress due to this procedure was assessed by measuring salivary cortisol. RESULTS: The GH response was significantly stronger in the children with ODD. After sumatriptan injection NC children showed a significant increase in cortisol; no such pattern was present in the ODD group. CONCLUSIONS: The results suggest that the postsynaptic 5-HT(1B/1D) receptor is functionally more sensitive in children with ODD.

Aggression↗
PubMed1999

Effects of sumatriptan on nitric oxide and superoxide balance during glyceryl trinitrate infusion in the rat. Implications for antimigraine mechanisms.

Infusion of glyceryl trinitrate (GTN) into patients with migraine precipitates the onset of a migraine attack several hours after completion of the infusion. Using an infusion of GTN into anaesthetised rats, this study investigates the relationship of regional cerebral blood flux rCBF(ldf), cortical nitric oxide (NO) and cortical superoxide concentrations and the effect of sumatriptan on each variable. In saline treated animals, a 30 min infusion of GTN (2 microgram kg(-1) min(-1), i.v.) was found to markedly increase cortical rCBF(ldf) (133+/-3% of baseline) and NO concentrations (141+/-13% of baseline). Superoxide levels exhibited an inverse relationship to NO levels, decreasing below basal to 48+/-14% of baseline. It is hypothesised that high NO levels during GTN infusion may decrease the detectable superoxide due to "leeching" of the superoxide into low level peroxynitrite formation. In the presence of sumatriptan, a decrease below baseline in cortical rCBF(ldf) (82+/-5% of baseline) and NO concentration (64+/-13% of baseline) was observed throughout GTN infusion, although superoxide levels significantly increased above baseline by 105+/-14 nM (p<0.05, ANOVA post hoc LSD test). The mechanism for this action of sumatriptan is unknown but may include; modulation of cell redox state, NO scavenging or direct manipulation of superoxide release.

Animals↗
PubMed2001

Modifications by sumatriptan and acetylcholine of nitric oxide-mediated neurogenic dilatation in dog cerebral arteries.

Canine cerebral arterial strips denuded of endothelium responded to nicotine and transmural electrical stimulation with relaxations, which were abolished by NG-nitro-L-arginine and methylene blue. Magnitudes of relaxation did not differ in the arteries contracted with prostaglandin F2alpha and sumatriptan, an effective therapeutic of migraine. Sumatriptan concentration-dependently contracted the arteries responding to 2 Hz stimulation with persistent relaxations, and the concentration of this 5-HT1B/1D/1F receptor agonist to overcome the relaxation averaged 1.06 x 10(-7) M. Acetylcholine inhibited the response to nerve stimulation due possibly to its action on prejunctional nitroxidergic nerves; the inhibition did not differ in the arteries contracted with prostaglandin F2alpha and K+. It appears that sumatriptan does not interfere with the release of nitric oxide from nerves but counteracts the neurogenic relaxation by functional antagonistic action on smooth muscle. Prejunctional inhibition by muscarinic receptor activation is unlikely associated with opening of neuronal K+ channels.

Acetylcholine↗
PubMed1996

Different effects of the serotonergic agonists buspirone and sumatriptan on the posterior pituitary hormonal responses to hypoglycemia in humans.

The responses of serum oxytocin (OT) and vasopressin (AVP) to the serotonergic HT1A agonist buspirone (15 mg p.o.) or the HTD1 agonist sumatriptan (6 mg injected subcutaneously) were evaluated in 7 normal men either in basal conditions or during an insulin (0.15 iu/kg as an i.v. bolus) tolerance test (ITT). Neither buspirone nor sumatriptan administration modified the basal secretion of AVP and OT. Stimulation of 5HT-1D receptors with sumatriptan was unable to change neither AVP nor OT response to insulin-induced hypoglycemia. On the other hand, the pretreatment with the 5HT1A agonist buspirone significantly enhanced the OT response during hypoglycemia, without modifying the AVP rise. The results of this study suggest that serotonergic 5HT1A receptors may interact with hypoglycemia in the stimulation of OT, but not AVP secretion.

Adult↗
PubMed2003

An open-label study to assess changes in efficacy and satisfaction with migraine care when patients have access to multiple sumatriptan succinate formulations.

BACKGROUND: Because a patient's migraines often differ in duration, intensity, and accompanying symptoms, as well as the conditions and circumstances at the time of the headache, the mode for treatment also may change. OBJECTIVE: The goal of this study was to determine whether migraine management is improved by providing 3 formulations of sumatriptan succinate to patients, together with education to assist them in selecting the most appropriate formulation for specific attacks. METHODS: This was an open-label study conducted in 3 family practice settings. Patients were recruited who had at least a 1-year history of migraine meeting International Headache Society criteria and experienced 2 to 6 attacks per month within the previous 3 months. Patients received instructions on oral, intranasal, and subcutaneous (SC) sumatriptan and were provided with all 3 formulations to treat 6 headaches. Migraine features, formulation used, reason for selecting specific formulation, migraine symptom relief, and use of follow-up doses were recorded in diaries. At follow-up, patients completed a questionnaire assessing satisfaction with access to multiple formulations. RESULTS: Of the 33 enrolled patients (26 women, 7 men; mean age, 38.5 years [range, 23-54 years]), 25 (75.8%) completed all visits. Of 149 headaches treated, 39 (26.2%) were mild at onset, 70 (47.0%) were moderate, and 40 (26.8%) were severe. Eighty (53.7%) headaches were treated with tablets, 35 (23.5%) with nasal spray, and 34 (22.8%) with SC injection. Primary reasons for selecting specific formulations included "fewer side effects" for tablets, "convenience" for nasal spray, and "quick onset of action" for SC injection. Twenty-one (84.0%) patients reported being either very satisfied or satisfied with their ability to manage their headaches. Physicians reported that 18 of 24 (75.0%) patients had an improved attitude toward managing their headaches. All formulations were well tolerated. Eight (32.0%) patients reported adverse events, the 2 most common being chest pressure and fatigue. CONCLUSION: The patients in this study reported greater satisfaction with migraine management when given access to multiple sumatriptan formulations and education regarding their appropriate use.

Administration, Intranasal↗
PubMed2000

Increased growth hormone response to sumatriptan challenge in adult autistic disorders.

Serotonergic (5-HT) abnormalities have been documented in autism. To assess sensitivity of the 5-HT1d receptor, growth hormone response to the 5-HT1d receptor agonist sumatriptan was studied in adult autistic patients and matched normal controls. In this study, 11 adult patients with autism or Asperger's disorder were compared with nine matched controls. All subjects were randomized to single dose sumatriptan (6 mg SQ) and placebo challenges, separated by a 1-week interval, and growth hormone was measured before and during the challenges. The results showed a highly significant diagnosisxdrugxtime interaction on repeated measure analysis covaried for baseline. This suggests that autistic patients had significantly greater growth hormone response to sumatriptan than normal controls, independent of placebo effects. Therefore, abnormalities in 5-HT regulation in autism may be related to increased sensitivity of the 5-HT1d inhibitory receptor in autism.

Adolescent↗
PubMed1997

Sumatriptan-induced growth hormone release in patients with major depression, mania, and normal controls.

The purpose of this study was to assess serotonergic function in patients with major depression or mania using sumatriptan, a novel 5-HT1D receptor agonist, as a pharmacological probe in a neuroendocrine challenge paradigm. We studied 18 drug free patients (10 with acute unipolar major depression and 8 with acute mania) who met DSM-IV criteria, and healthy controls. Subjects presented for testing after an overnight fast. After obtaining a blood sample for baseline growth hormone (GH) levels, sumatriptan (6 mg) was given subcutaneously, and further blood samples were collected at half hour intervals for 2 hours. The results showed that GH responses to sumatriptan were blunted in depressed patients but not in manics, compared to healthy controls. There were no differences in basal GH levels between the 3 groups. The results of this study provide further support for the role of serotonergic system in pathophysiology of major depression, but not in mania.

Adult↗
PubMed1997

Atypical facial pain: a double-blind placebo-controlled crossover pilot study of subcutaneous sumatriptan.

A double-blind placebo-controlled crossover pilot study involving 19 patients was undertaken to evaluate the efficacy of subcutaneous sumatriptan, a selective 5-hydroxytryptamine (5-HT)-like receptor agonist, in the treatment of atypical facial pain (AFP). A reduction in total pain was found 120 min post injection in the sumatriptan group. Most patients, however, described the medication as ineffective overall, despite significant pain score reduction. The temporary improvement of pain scores with the active drug was thought to be too small to be of any clinical benefit, but suggests that vascular or neurogenic mechanisms may be involved in the aetiology of AFP. Sumatriptan is not an appropriate therapeutic option for patients with AFP, but could prove a valuable drug in experimental clinical pharmacology.

Adolescent↗
PubMed1998

Treatment of severe, drug resistant obsessive compulsive disorder with the 5HT1D agonist sumatriptan.

The serotonergic system has been implicated in both the aetiology and pharmacological treatment of obsessive compulsive disorder. In pharmacological challenge tests, mCPP, a 5-HT agonist, with an affinity for 5HT2C as well as 5HT1A and 5HT1D receptors, was associated with a transient exacerbation of obsessive compulsive symptoms. Chronic administration of mCPP was found to bring about some relief of these symptoms. Sumatriptan is an antimigraine agent, which interacts most potently with 5HT1D receptors. In the cases to be presented, we report the effects of chronic administration of Sumatriptan to three severe, treatment resistant, OCD patients. Following chronic administration of sumatriptan, these patients, who have been resistant to any former pharmacological treatment, responded with an improvement in their depression and a modest reduction in their obsessive compulsive symptoms.

Adult↗
PubMed2001

Sumatriptan responsiveness and clinical, psychiatric and psychologic features in migraine patients.

OBJECTIVE: To compare sumatriptan responders and nonresponders in a migraine population with regard to a number of clinical, psychiatric and psychologic features. METHODS: Patients were drawn from a referral headache clinic population, and classified as responders or nonresponders. Clinical features were assessed by a written questionnaire. The lifetime prevalence of several psychiatric disorders was determined by the National Institute of Mental Health diagnostic interview schedule and personality factors were measured by the 16 Personality Factors (16PF) Questionnaire. RESULTS: Nonresponders indicated less influence on their migraine by menstrual factors, had a higher lifetime prevalence of generalized anxiety, and showed 16PF scores indicating greater shyness, self-sufficiency and perfectionism. Nonresponders were also more imaginative and less socially outgoing. CONCLUSION: Although they must be interpreted with caution due to small sample size and the multiple comparisons made, our results indicate that there may be differences between sumatriptan responders and nonresponders with regard to a number of clinical, psychiatric and psychologic factors. These results suggest that biological differences exist between the two patient groups which likely account for both the differences in their responses to sumatriptan and in the clinical features noted above.

Adult↗