Eletriptan Research Articles

Synthesis of compounds related to the anti-migraine drug eletriptan hydrobromide

Eletriptan hydrobromide (1) is a selective serotonin (5-HT1) agonist, used for the acute treatment of the headache phase of migraine attacks. During the manufacture of eletriptan hydrobromide the formation of various impurities were observed and identified by LC–MS. To control the formation of these impurities during the preparation of active pharmaceutical ingredients, the structure of the impurities must be known. Major impurities of the eletriptan hydrobromide synthesis were prepared and characterized by using various spectroscopic techniques, i.e., mass spectroscopy, FTIR , 1H NMR, 13C NMR/DEPT, and further confirmed by co-injection in HPLC. The present study will be of great help in the synthesis of highly pure eletriptan hydrobromide related compounds.

Eletriptan provides consistent migraine relief: results of a within-patient multiple-dose study

Eletriptan provides consistent migraine relief: results of a within-patient multiple-dose study

Quantitative analysis of eletriptan in human plasma by HPLC-MS/MS and its application to pharmacokinetic study

Authors developed a simple, sensitive, selective, rapid, rugged, and reproducible liquid chromatography-tandem mass spectrometry method for the quantification of eletriptan (EP) in human plasma using naratriptan (NP) as an internal standard (IS). Chromatographic separation was performed on Ascentis Express C18, 50 × 4.6 mm, 2.7 μm column. Mobile phase was composed of 0.1% formic acid: methanol (40:60 v/v), with 0.5 mL/min flow rate. Drug and IS were extracted by liquid-liquid extraction. EP and NP were detected with proton adducts at m/z 383.2→84.3 and 336.2→97.8 in multiple reaction monitoring (MRM) positive mode, respectively. The method was validated with the correlation coefficients of (r(2)) ≥ 0.9963 over a linear concentration range of 0.5-250.0 ng/mL. This method demonstrated intra- and inter-day precision within 1.4-9.2% and 4.4-5.5% and accuracy within 96.8-103% and 98.5-99.8% for EP. This method is successfully applied in the bioequivalence study of 24 human volunteers.

Study of forced degradation behavior of Eletriptan hydrobromide by LC and LC–MS and development of stability-indicating method

The objective of the present study was to report the stability profile of novel antimigrain drug Eletriptan hydrobromide based on the information obtained from forced degradation studies. The drug was subjected to acid (0.1–1 mol L −1 HCl), neutral and base (0.1–1 mol L −1 NaOH) hydrolysis and to oxidative decomposition (3–15% (v/v) H 2O 2). Photolysis and thermo degradation at 75 °C were carried out in methanol solution and in solid state with both Eletriptan hydrobromide bulk drug and the tablet formulation. The products formed under different stress conditions were investigated by LC and LC–MS. The experimental conditions for LC were chosen by employing experimental design and multicriteria decision making methodology. These powerful tools enabled the accomplishment of satisfactory resolution with the shortest possible analysis time. Analytes were separated on a C 18 column ( XTerra™, 150 mm × 3.9 mm, 5 μm) with the mobile phase composed of methanol–water solution of TEA (pH 6.52, 1%, v/v) (30:70, v/v) pumped at 1 mL min −1 flow rate. The column temperature was set at 50 °C and the detection at 225 nm using DAD detector. The LC method was suitably modified for LC–MS analysis which was further used to characterize the arisen degradation products. The possible degradation pathway was outlined based on the results. The drug appeared to be instable towards every stress condition but oxidation. The stability was not jeopardized even under more exaggerated conditions such as increased temperature of the solutions to 75 °C, increased strength of acid/alkali solutions and prolonged testing period. Validation of the LC-DAD method was carried out in accordance with ICH guideline. The method met all required criteria and was applied when testing the commercially available tablets.

LC Assay of Eletriptan in Tablets and In Vitro Dissolution Studies

Eletriptan (ELT) is a new selective serotonin agonist approved for the treatment of acute migraine headaches. A simple and rapid liquid chromatographic method was developed and validated for the assay of ELT in tablets. Chromatography was carried out on a 250 mm × 4.6 mm C18 column at 30 °C. Acetonitrile–15 mM triethylamine solution (adjusted to pH 7.0 using concentrated o-phosphoric acid) (60:40, v/v) mixture was used as mobile phase at 1.0 mL min−1 flow rate and UV detector was set at 225 nm. A linear response (r2 = 0.9999) was observed in the range of 0.1–1.6 μg mL−1. The method showed good recoveries (100.08 %) and the RSD values for intra- and inter-day precision were 0.78–1.93 and 1.10–2.15%, respectively. The method can be used for quality control assays and in vitro dissolution studies of ELT in tablets.

Development of Triptans in Japan: Bridging Strategy Based on the ICH-E5 Guideline

In Japan, five new drug applications (NDAs) of triptans have been approved through a bridging strategy. They constituted the largest target disease field among 26 NDAs which had been approved through the strategy between 1999 and 2003. The bridging strategies of the drugs were classified into two major categories to be described below. One was to conduct a placebo-controlled dose-response study as a bridging study in an attempt to extrapolate the data from the pivotal foreign Phase III studies including a repeated dose study (i.e., zolmitriptan, sumatriptan succinate, and eletriptan hydrobromide). Another was to conduct a placebo-controlled Phase III study in Japan in an attempt to extrapolate the data for efficacy from a repeated dose study (i.e., sumatriptan and rizatriptan benzoate). The extrinsic ethnic factors relating to triptans did not interfere with the extrapolation of foreign clinical data in the five applications. A bridging strategy reduced the number of clinical trials and/or sample size. The accumulation of these bridging experiences indicated that foreign clinical data could be used to support the approval of triptans in Japan.

Validation of an HPLC method for the simultaneous determination of eletriptan and UK 120.413

Arapid and sensitive RPHPLCmethod was developed for the routine control analysis of eletriptan hydrobromide and its organic impurity UK 120.413 in Relpax? tablets. The chromatography was performed at 20?C using a C18 XTerra ? (5 ?m, 150 x 4,6 mm) column at a flow rate 1.0 ml/min. The drug and its impurity were detected at 225 nm. The mobile phase consisted of TEA (1 %) - methanol (67.2:32.8 v/v), the pH of which was adjusted to 6.8 with 85 % orthophosphoric acid. Quantification was accomplished by the internal standard method. The developed RP HPLC method was validated by testing: accuracy, precision, repeatability, specificity, detection limit, quantification limit, linearity, robustness and sensitivity. High linearity of the analytical procedure was confirmed over the concentration range of 0.05 - 1.00 mg/ml for eletriptan hydrobromide and from 0.10 - 1.50 ?g/ml for UK 120.413, with correlation coefficients greater than r = 0.995. The low value of the RSD expressed the good repeatability and precision of the method. Experimental design and a response surface method were used to test robustness of the analytical procedure and to evaluate the effect of variation of the method parameters, namely the mobile phase composition, pH and temperature. They showed small deviations from the method setting. The good recovery and low RSD confirm the suitability of the proposed RP HPLC method for the routine determination of eletriptan hydrobromide and its impurity UK 120.413 in Relpax? tables.

Switching from butalbital-caffeine combinations to eletriptan is effective in patients with resistant migraines,

Switching from butalbital-caffeine combinations to eletriptan is effective in patients with resistant migraines,

New drugs 04, part 1.

In this article, you'll learn about nine new drugs marketed in the first half ofr 2003, including: adalimumab, given once every other week for rheumatoid arthritis (RA) eletriptan hydrobromide, a new option for treating acute migraine and associated symptoms atomoxetine HCl, an important new type of medication for children and adults with attention deficit hyperactivity disorder (ADHD) alefacept, the first biologic therapy for moderate or severe psoriasis. Unless otherwise specified, the information in the following summaries applies to adults, not children. Consult the package insert for information about each drugs safety during pregnancy and breast-feeding. Also consult the package insert, a pharmacist, or a comprehensive drug reference for more details on precautions, drug interactions, and adverse reactions* for all these drugs.

Eletriptan economically superior to sumatriptan in migraine

Eletriptan economically superior to sumatriptan in migraine

Eletriptan economically superior to sumatriptan in migraine

Eletriptan economically superior to sumatriptan in migraine

Eletriptan worth it for migraine

Eletriptan worth it for migraine

Poster Presentations VI

Minneapolis Convention Center; Exhibit Hall 3; Thursday, April 30; 3:00 PM-7:00 PM Posters Displayed; 3:00 PM-7:00 PM Senior Authors Stand by Posters; 5:30 PM-7:00 PM P06.001 Effect of Rizatriptan versus Sumatriptan on Migraine Associated Symptoms W. Hester Visser, Kaihong Jiang P06.002 Measures of Rapid Resolution of Migraine Symptoms and Patient Acceptance to Treatment following Eletriptan, Sumatriptan and Placebo P. H. Poole on behalf of the Eletriptan Steering Committee, N. C. Jackson P06.003 Clinical Measures of Efficacy, Safety and Tolerability for the Acute Treatment of Migraine: A Comparison of Eletriptan (20-80 mg), Sumatriptan (100 mg) and Placebo N. C. Jackson on behalf of the Eletriptan Steering Committee P06.004 Successful Treatment of Menstrual Migraine with a Non-Prescription Combination of Aspirin, Acetaminophen, and Caffeine: Results from Three Randomized, Placebo-Controlled Studies Stephen D. Silberstein, Joseph J. Armellino, Howard D. Hoffman, Jean P. Battikha, Richard B. Lipton P06.005 Familial Migraine with Vertigo: No Mutations Found in CACNA1A Jisoo Kim, Qing Yue, Joanna C. Jen, Stanley F. Nelson, Robert W. Baloh P06.006 The Pharmacokinetics of Eletriptan-A New Oral Agent for the Acute Treatment of Migraine A. Shah, B. F. Johnson, K. A. Milton P06.007 Migraine during Menstruation and the Efficacy of Oral Eletriptan E. A. MacGregor P06.008 Successful Treatment of Severe, Disabling Migraine Headache with a Non-Prescription Combination of Acetaminophen, Aspirin, and Caffeine: Results from Three Randomized, Placebo-Controlled Studies Jerome Goldstein, Howard D. Hoffman, Joseph J. Armellino, Jean P. Battikha, James Couch, Jr., Harvey Blumenthal, Richard B. Lipton P06.009 Treatment of Tension-Type Headache with Bromfenac, BAC, and Placebo Merle L. Diamond, Seymour Diamond, Frederick G. Freitag, Ivan Vavra P06.010 Non-Invasive Monitoring of Cerebral Hemoglobin Oxygenation during Migraine Treatment with ASA or Sumatriptan Guy Arnold, Stephan Kinze, Hellmuth Obrig, Wolfram von Pannwitz, Hauke Heekeren, Arno Villringer, Karl M. Einhaup P06.011 Gabapentin (Neurontin®) for Pain Associated with Diabetic …