Sumatriptan

Dechant, Kerry L.; Clissold, Stephen P.

doi:10.2165/00003495-199243050-00010

Cited by 138 publications

(16 citation statements)

References 70 publications

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“…This route is practical, non-invasive, and also circumvents the problem of dose wastage which may occur due to emesis during a migraine attack. Drug delivery via intranasal route helps in bypassing the blood-brain barrier (BBB), whereby direct brain targeting can be achieved with absorption through the olfactory mucosa [11]. In the present work, chitosan nanoparticles were formulated as the delivery vehicle for the antimigraine drug, sumatriptan succinate, and were proposed to be given through the nasal route.…”

Section: Introductionmentioning

confidence: 99%

Intranasal Delivery of Chitosan Nanoparticles for Migraine Therapy

Gulati¹,

Nagaich²,

Saraf³

2013

Sci. Pharm.

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ObjectiveThe objective of the research was to formulate and evaluate sumatriptan succinate-loaded chitosan nanoparticles for migraine therapy in order to improve its therapeutic effect and reduce dosing frequency.Material and MethodsThe Taguchi method design of experiments (L9 orthogonal array) was applied to obtain the optimized formulation. The sumatriptan succinate-loaded chitosan nanoparticles (CNPs) were prepared by ionic gelation of chitosan with tripolyphosphate anions (TPP) and Tween 80 as surfactant.ResultsThe CNPs had a mean size of 306.8 ± 3.9 nm, a zeta potential of +28.79 mV, and entrapment efficiency of 75.4 ± 1.1%. The in vitro drug release of chitosan nanoparticles was evaluated in phosphate buffer saline pH 5.5 using goat nasal mucosa and found to be 76.7 ± 1.3% within 28 hours.DiscussionThe release of the drug from the nanoparticles was anomalous, showing non-Fickian diffusion indicating that drug release is controlled by more than one process i.e. the superposition of both phenomena, a diffusion-controlled as well as a swelling-controlled release. This is clearly due to the characteristics of chitosan which easily dissolves at low pH, thus a nasal pH range of 5.5 ± 0.5 supports it very well. The mechanism of pH-sensitive swelling involves protonation of the amine groups of chitosan at low pH. This protonation leads to chain repulsion, diffusion of protons and counter ions together with water inside the gel, and the dissociation of secondary interactions.ConclusionThe results suggest that sumatriptan succinate-loaded chitosan nanoparticles are the most suitable mode of drug delivery for promising therapeutic action.

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Section: Introductionmentioning

confidence: 99%

Intranasal Delivery of Chitosan Nanoparticles for Migraine Therapy

Gulati¹,

Nagaich²,

Saraf³

2013

Sci. Pharm.

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“…MR77 couples to the inhibition of adenylate cyclase and has a binding profile similar to that for the 5-HT1D receptor with the marked exception in affinity for 5-CT. Interestingly, sumatriptan and ergotamine, both of which exhibit high affinity for MR77, have been shown to have clinical efficacy for the treatment of migraine headaches (for review, see ref. 27). This raises the possibility that the action of these drugs may be mediated by more than one subtype of 5-HT receptors.…”

Section: T P R H a G I T I T T V W V I S V F I Smentioning

confidence: 99%

Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes.

Lovenberg

Erlander

Baron

et al. 1993

Proc. Natl. Acad. Sci. U.S.A.

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Sequential polymerase chain reaction experiments were performed to amplify a unique sequence representing a guanine nucleotide-binding protein (G-protein)-coupled receptor from rat hypothalamic cDNA. Degenerate oligonucleotides corresponding to conserved amino acids from transmembrane domains III, V, and VI of known receptors[5-HT1A, 5-HT,c, and 5-HT2; 5-HT is serotonin (5-hydroxytryptamine)] were used as primers for the sequential reactions. The resulting product was subcloned and used to screen a rat genomic library to identify a full-length clone (MR77) containing an intronless open reading frame encoding a 366-amino acid seven-transmembrane domain protein. The human homolog was isolated, and its encoded protein had 93% overall amino acid identity with the rat sequence. Within the conserved transmembrane domains, the sequences exhibit approximately 52%, 59%, 65%, and 68% amino acid identity with the known rat 5-HT1A, rat 5-HTIB, rat 5-HT1D, and human 5-HT1E receptors, respectively. MR77 was subcloned into a eukaryotic expression vector system and expressed in CosM6 cells. Studies on broken cell preparations indicate that the expressed receptor exhibits 125I-labeled d-lysergic acid diethylamide (LSD) binding that can be displaced by serotonin but not by other biogenic amines. The specific binding is displaced by the selective 5-HT1D agonist sumatriptan but not by the mixed 5-HTIA/1D agonist 5-carboxyamidotryptamine. 125I-labeled LSD binding was competitively antagonized by the ergot alkaloids methysergide and ergotamine. HeLa cells transfected with the MR77 gene exhibited inhibition of adenylate cyclase in response to serotonin. MR77 is expressed at low levels throughout the brain, with the greatest expression in the cortex, hippocampus, and striatum. MR77 thus represents a 5-HT receptor of the 5-HT1 class, and we propose that, based on the pharmacological characterization, MR77 represents an additional 5-HTlE-like receptor.Serotonin (5- In an attempt to identify other receptors that belong to the family of 5-HT receptors, we used a strategy based upon similarities shared among known members of the family. We designed highly degenerate oligonucleotides corresponding to conserved amino acid sequences in putative transmembrane domains III, V, and VI of the 5-HT1A, 5-HT,c, and 5-HT2 receptors. These oligonucleotides were used in sequential polymerase chain reactions (PCR) with rat hypothalamus cDNA as the template to generate a series ofclones. Here we report that one of these clones and its human homolog ¶ correspond to a 5-HT receptor that is more closely related in sequence to the recently cloned human S31 receptor (5-HT1E) than any previously described 5-HT receptor but clearly is a new member of the 5-HT1 receptor family. Initial pharmacological characterization of this receptor, which is negatively coupled to adenylate cyclase, is similar to but distinct from that described previously for the 5-HTlE receptor (9,12,13), and therefore we propose that MR77 belongs to a new subgroup of 5-HTlE-like r...

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“…Sumatriptan was the first 5-HT 1 receptor agonist to be developed for migraine [9]. Problems associated with its use include headache recurrence, poor oral bioavailability and cardiovascular side effects [10], and other triptans with improved pharmacokinetic profiles have now been developed.…”

Section: Introductionmentioning

confidence: 99%

Tolerability and Efficacy of Almotriptan in the Long-Term Treatment of Migraine

Pascual¹,

Falk

Docekal³

et al. 2001

Eur Neurol

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Background: Almotriptan is a highly specific 5-HT_1B/1D receptor agonist, which acts selectively on blood vessels of the brain. Short-term studies have demonstrated that almotriptan provides rapid, effective and reliable relief of migraine attacks, while offering excellent tolerability. Purpose: To assess the long-term tolerability and efficacy of oral almotriptan 12.5 mg administered for every migraine attack over a 1-year period. Methods: A total of 762 patients treated 13,751 attacks (1–97 per patient); 61.5% of attacks were treated with one 12.5-mg dose, while for 38.5% of attacks, patients took a second dose within 24 h. Results: Three hundred and ninety-one patients (51.3%) experienced a total of 1,617 adverse events (AEs). The majority (88.6%) of AEs were of mild-to-moderate intensity, and only 28.8% of AEs were considered to be related to the study drug. Only 2 patients experienced serious AEs possibly related to almotriptan, syncope and chest pain; both recovered without any sequelae. Patients reported at least 1 AE in 11% of attacks treated. The incidence of AEs decreased during the study. Only 6 (0.8%) study withdrawals were due to AEs considered to be related to almotriptan. Tolerability was not compromised in patients taking 2 doses of almotriptan or in those using migraine prophylactics. Patient age or sex did not influence the incidence of AEs. There was no evidence of tachyphylaxis in those patients completing the study. Pain relief at 2 h after the initial dose was achieved in 84.2% of moderate/severe attacks. Patients were pain free at 2 h after dose in 58.2% of all attacks. Older patients (>40 years) tended to respond better than younger ones (<40 years). Efficacy was not modified by use of migraine prophylactics or hormonal contraceptives. Efficacy measurements were consistent on treating repeated moderate/severe migraine attacks. Conclusion: This large, open study indicates that the new, specific 5-HT_1B/1D agonist almotriptan, at a dose of 12.5 mg, is a well tolerated and effective treatment for migraine pain when used over a period of up to 1 year.

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Sumatriptan

Cited by 138 publications

References 70 publications

Intranasal Delivery of Chitosan Nanoparticles for Migraine Therapy

Intranasal Delivery of Chitosan Nanoparticles for Migraine Therapy

Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes.

Tolerability and Efficacy of Almotriptan in the Long-Term Treatment of Migraine

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