Our library of drug research abstracts drawn from the medical literature is updated on a regular schedule, and you can be assured that new imigran research articles will be listed here shortly after becoming available to us.
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Medical research on imigran
Production of Ultrafine Sumatriptan Succinate Particles for Pulmonary Delivery.
Pharm Res. 2008 Jun 26;
Yang ZY, Le Y, Hu TT, Shen Z, Chen JF, Yun J
PURPOSE: Drug particle physical properties are critical for the efficiency of a drug delivered to the lung. The purpose of this study was to produce ultrafine sumatriptan succinate particles for inhalation. METHODS: Sumatriptan succinate particles were produced via reactive precipitation without any surfactants. Several low toxic organic solvents such as acetone, isopropanol, and tetrahydrofuran were investigated as the reaction medium. And the dry powder was obtained via spray drying. FT-IR, HPLC, SEM and XRD were exploited to characterize the physicochemical properties of the ultrafine sumatriptan succinate dry powder. The aerosol performance of the powder was evaluated using an Aeroliser(R)connected to a multi stage liquid impinger operating at 60 l/min. RESULTS: The mean particle size of the ultrafine sumatriptan succinate particles obtained under optimum conditions was in the range of 630 approximately 679 nm and consequently they were in the respirable range. The spray-dried powder whose fine particle fraction was increased up to 50.6 +/- 8.2% showed good aerosol performance whereas the vacuum-dried powder was approximate 18.2 +/- 3.0%. CONCLUSIONS: Good aerosol performance ultrafine sumatriptan succinate particles could be produced by reactive precipitation without any additives followed by spray drying at the optimum parameters.
Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides.
Bioorg Med Chem. 2008 Jun 10;
Yang B, Zhang H, Verkman AS
Inhibitors of brain glial water channel aquaporin-4 (AQP4) are of potential clinical utility, as they are predicted to modulate brain edema, neuroexcitation and glial scarring. Recently, Huber et al. (Bioorg. Med. Chem.2007, 17, 1270-1273; in press) reported that a series of arylsulfonamides, antiepileptics, and related small molecules strongly inhibited AQP4 water transport with IC(50)s down to 1muM. We retested the compounds with greatest reported potencies, including acetylsulfanilamide, acetazolamide, 6-ethoxy-benzothiazole-2-sulfonamide, topiramate, zonisamide, phenytoin, lamotrigine, and sumatriptan, in AQP4-transfected mammalian cells and primary cultures of brain glial cells, using several sensitive assays of osmotic water permeability. Contrary to the findings of Huber et al., in our studies we found no significant inhibition of AQP4 water permeability by any of the compounds at concentrations up to 100muM.
Updated overview of the putative role of the serotoninergic system in obsessive-compulsive disorder.
Neuropsychiatr Dis Treat. 2005 Sep; 1(3): 231-43
Aouizerate B, Guehl D, Cuny E, Rougier A, Burbaud P, Tignol J, Bioulac B
The pathophysiology of obsessive-compulsive disorder (OCD) remains unknown. However, increasing attention has been paid to the putative role of the serotoninergic system, the strongest evidence being based on the widely demonstrated efficacy of serotonin (5HT) reuptake inhibitor antidepressants in the treatment of OCD. The therapeutic effects are correlated with changes in peripheral parameters of 5HT function, which have been found to be altered in OCD, suggesting the possibility of reduced 5HT reuptake capacity. This could reflect a compensatory mechanism presumably due to decreased availability of extracellular 5HT, as evidenced by data derived from direct assessment of central 5HT neurotransmission. The development of new neurochemical probes that explore the sensitivity of various 5HT receptor subtypes has provided precious information. m-Chlorophenylpyperazine (m-CPP), an agonist to 5HT1A, 5HT1D, and 5HT2C receptors, and which also blocks 5HT3 receptors, exacerbates OC symptoms. In contrast, neither MK-212 (6-chloro-2-[1-piperazinyl]-pyrazine), a 5HT1A and 5HT2C receptor agonist, nor ipsapirone or buspirone, which acts as an agonist to 5HT1A receptors, have any effect on OC symptom severity. This suggests the potential implication of the 5HT1D receptor, as shown by the aggravation of OC manifestations in response to sumatriptan, a selective 5HT1D receptor agonist. The 5HT3 plays no specific role, given the lack of influence of the 5HT3 antagonist ondansetron, on OC symptom intensity. Further studies are required to elucidate the pharmacological molecular determinants of the putative 5HT1D receptor dysfunction.
Comparison of rizatriptan and sumatriptan.
Headache. 1999 Jan; 39(1): 59-60
O'Quinn S, Mansbach H, Salonen R
A fixed-dose combination of sumatriptan and naproxen for migraine.
Med Lett Drugs Ther. 2008 Jun 16; 50(1288): 45-6
Subcutaneous Sumatriptan Relieved Migraine-Like Headache in Two Adolescents With Aseptic Meningitis.
Headache. 2008 Jun 10;
Prokhorov S, Khanna S, Alapati D, Pallimalli SL
Sumatriptan was developed as an agent for the treatment of acute migraine. However, sumatriptan may alleviate not only migraine headache, but also headache of subarachnoid hemorrhage and meningitis. We report 2 patients whose migraine-like headache on presentation was relieved by subcutaneous sumatriptan. Later, both patients were diagnosed with aseptic meningitis.
Cephalalgia. 2008 Jun 5;
Wienecke T, Hansen J, Petersen J, Olsen K, Ashina M, Tfelt-Hansen P
Arteriovenous anastomoses (AVAs) may open up during migraine attacks. In studies with anaesthetized and bilaterally vagosympatectomized pigs, triptans reduce AVA blood flow and increase the arteriovenous O(2) difference (AVDO(2)). To investigate whether subcutaneous sumatriptan 6 mg could induce changes in the AVDO(2), we measured the AVDO(2) in the external jugular vein in healthy subjects. We also measured the AVDO(2) in the internal jugular and cubital veins. There were no changes in AVDO(2) after subcutaneous sumatriptan, probably because AVA blood flow is limited in humans with an intact sympathetic nervous system.
Prediction of attack frequency in migraine treatment.
Cephalalgia. 2008 Jun 5;
Maas H, Snelder N, Danhof M, Pasqua OD
Usually limited information about the frequency of migraine episodes is derived from acute migraine trials. However, the design of some studies is such that they also provide relevant information about the attack frequency without the bias associated with patient expectations of treatment effect between attacks during prophylaxis trials. Using clinical data from repeated migraine attacks treated with placebo, naratriptan 2.5 mg or sumatriptan 100 mg, we show that attack and interictal periods can be described by a random probability distribution. Based on a gamma distribution, the mean interval between attacks was estimated to be 24 (17-34) days for placebo, 23 (18-29) days for naratriptan 2.5 mg and 22 (17-28) for sumatriptan 100 mg. These findings suggest that the interictal interval is not affected by abortive treatment with triptans. Interpretation of these results may be limited by the study type, yet the method represents a new tool for the evaluation of disease dynamics and treatment effect in the prophylaxis of migraine.
Posterior cerebral hypoperfusion in migraine without aura.
Cephalalgia. 2008 May 28;
Denuelle M, Fabre N, Payoux P, Chollet F, Geraud G
In cerebral blood flow studies, migraine aura is characterized by a posterior cortical hypoperfusion. In contrast, only rare and mild changes in brain perfusion have been demonstrated in migraine without aura, suggesting two different haemodynamic patterns in migraine with and without aura. Our aim was to study hypoperfusion with positron emission tomography (PET) as early as possible during spontaneous migraine without aura attacks. We used H(2) (15)O PET to investigate seven patients (six female, one male) with migraine without aura (International Classification of Headache Diseases-II code 1.1) in three situations: during the headache phase, after headache relief following sumatriptan injection, and during an attack-free interval. Statistical analysis was performed with SPM2. Within 4 h after the attack onset, significant relative bilateral posterior cortical hypoperfusion was found and persisted after headache relief following sumatriptan injection. A posterior cortical hypoperfusion demonstrated in migraine without aura could suggest a common pathogenesis in migraine with and without aura. The significance of relative posterior hypoperfusion in migraine without aura is discussed according to the current knowledge of migraine pathogenesis.
Cephalalgia. 2008 Jul; 28(7): 723-33
Martino G, Perkins MN
A pharmacological model of migraine is described using ultrasound vocalization (USV) of rats following central inflammation-induced sensitization to tactile stimulation. Central inflammation induced by intracerebroventricular injection of lipopolysaccharide (LPS) increased USV induced by an air current focused on the head and this was abolished by morphine and ketorolac, suggesting a nociceptive component. USV in naive rats were unaffected. Diazepam reduced USV in both inflamed and naive rats. The triptans, zolmitriptan and sumatriptan, both reduced USV in inflamed but not in naive rats, as did dihydroergotamine, and the calcitonin gene-related peptide (CGRP) antagonists alphaCGRP(8-37) and BIBN4096BS. The neurokinin-1 antagonist L-733-060 had no effect in either inflamed or naive rats when given after induction of inflammation, but when given with the LPS it prevented the augmentation of USV. This profile of activity of agents proven to be effective in the clinic suggests this model can be used to predict novel therapeutic agents for migraine.
