1,721,066 research outputs found
Rational Use of Lasmiditan for Acute Migraine Treatment in Adults: A Narrative Review
No full textPurpose: This narrative review provides an update on the research that led to the development of ditans and lasmiditan for the acute treatment of migraine in adults and discusses the potential advantages and disadvantages of lasmiditan in clinical use.
Methods: The electronic databases PubMed, Scopus, and ClinicalTrials.gov were searched from database inception through January 9, 2021, to identify relevant studies. Search results were assessed for their overall relevance to this review.
Findings: Because part of the effect of the triptans is mediated by the serotonin 1F receptors, which are not present in the smooth muscle, a pure agonist of these receptors, lasmiditan, was developed. Lasmiditan is hypothesized to act on antinociceptive pathways and inhibit the calcitonin gene-related peptide release. Lasmiditan was approved by the US Food and Drug Administration in 2019 based on the results of 2 pivotal trials that found a significant difference from placebo in the percentage of patients who achieved freedom from pain and most bothersome symptom at 2 h. The main concern of lasmiditan derives from its
central nervous systemerelated adverse effects, mainly dizziness and paraesthesia, probably attributable to its high blood brain barrier penetration. These central nervous system adverse effects impair driving performance for hours and might be suboptimal for individuals with migraine who want to quickly stop the migraine attack to resume their activities as soon as possible.
Implications: Despite the advantage of being beneficial in the acute treatment of migraine without vasocostrictive action, lasmiditan also presents limitations, in particular the central nervous system adverse effects. Moreover, head-to-head trials against triptans and gepants are indispensable to determine the better option for patients
Resolution of the enantiomers of verapamil and gallopamil by chiral liquid chromatography mass spectrometry
No full textAn HPLC-CSP method has been developed for the separation of enantiomers of verapamil and gallopamil using the improved version of the alpha(1)-acid glycoprotein, chiral stationary phase as selector with a volatile mobile phase. The results of the investigation provide the conditions which allow direct coupling to a mass spectrometer. In addition, the simultaneous enantioseparation of both the enantiomeric pairs of verapamil and gallopamil was achieved
Atogepant: an emerging treatment for migraine
No full textIntroduction: Until recently, only non-specific and not always well-tolerated medications were available for migraine prophylaxis. Currently, specific drugs such as calcitonin gene-related peptide (CGRP) monoclonal antibodies and second-generation gepants are marketed for migraine treatment. Atogepant, an orally active small molecule, is a potent, selective antagonist of the CGRP receptor and is the only gepant authorized exclusively for episodic migraine prophylaxis in adults. Areas covered: Using literature obtained from PubMed, Scopus, Web of Science, Cochrane, and ClinicalTrials.gov (up to February 13rd, 2022), the authors summarize and evaluate the available data on atogepant for the prophylaxis of episodic migraine. Expert opinion: From pivotal trials, the efficacy and tolerability of atogepant in episodic migraine prophylaxis seem comparable to those of CGRP monoclonal antibodies, even if comparative studies have not been conducted. To date, limited information is available on atogepant, including the optimal dose and duration of therapy; hence, it is difficult to establish whether it could be a first-line drug for migraine prophylaxis. Furthermore, it is important to evaluate if atogepant use is associated with the risk of cardiovascular and cerebrovascular events, which could result from potent and persistent blockade of vasodilation by CGRP
Determinazione dei contenuti di cannabinoidi in Cannabis Sativa L. mediante cromatografia liquida abbinata alla spettrometria di massa
No full textSono state approntate procedure di analisi cromatografica abbinata alla spetttrometria di massa per la determinazione quantitativa del contenuto di cannabinoidi in campioni di Cannabis. I risultati ottenuti si sono rivelati utili al fine di verificare le possibili relazioni tra il contenuto di Cannabonoidi (acidi e neutri) e la pianta in esame (cultivar, grado di maturazione, sesso)
Studio dei profili di purezza di alcuni narcotici mediante cromatografia liquida a fase inversa
No full textIl lavoro riguarda la messa a punto di un metodo HPLC per lo studio dei profili di purezza di morfina, codeina ed eroina e, per quanto riguarda l'eroina, per lo studio della stabilità mediante la determinazione delle costanti di velocità di idrolisi. La metodica si è rivelata idonea ed alternativa al metodo ufficiale FU IX
Derivatisation procedures for the chromatographic enantioseparation of fexofenadine hydrochloride
No full textThe paper describes two different pre-column derivatisation procedures for the chromatographic enantioseparation of fexofenadine hydrochlorid
Enantioselective analyses of antihistaminic drugs by high-performance liquid chromatography on chiral stationary phases
No full textThe present communication describes enantioselective analyses of terfenadine and fexofenadine by HPLC on Chiralcel OD and Chirobiotic V columns
Allopregnanolone and pregnanolone are reduced in the hippocampus of epileptic rats, but only allopregnanolone correlates with the seizure frequency
No full textBackground: Neurosteroids modulate epileptic activity by interacting with the γ-aminobutyric acid type A receptor, but their brain levels are still undetermined. Objectives: We aimed to establish levels of neurosteroids in the neocortex and hippocampus by liquid chromatography–mass spectrometry in epileptic rats. Methods: Kainic acid-treated rats were continuously monitored up to 9 weeks to determine the seizure frequency by video electrocorticography (n=23), and compared to age-matched controls monitored in the same manner (n=11). Results: A reduction in allopregnanolone (-50%; p<0.05, Mann-Whitney test) and pregnanolone levels (-64%; p<0.01) was found in the hippocampus, whereas pregnenolone sulfate, pregnenolone, progesterone, and 5α-dihydroprogesterone were nonsignificantly reduced. No changes were found in the neocortex. Moreover, allopregnanolone (but not pregnanolone) levels were positively correlated with the seizure frequency (r2=0.4606, p<0.01). Conclusions: These findings indicate a selective reduction in hippocampal levels of 3α-reduced neurosteroids. This reduction was partially mitigated by seizures in the case of allopregnanolone
DETERMINATION OF AZELAIC ACID IN PHARMACEUTICALS AND COSMETICS BY RP-HPLC AFTER PRECOLUMN DERIVATIZATION
No full textThis paper reports a RP-HPLC method for the determination in topics of azelaic acid, a keratolytic and anti-comedogenic agent widely used in the treatment of all types of acne. A derivatization step was needed prior to chromatographic analysis because the analyte is lacking in chromophore. A sample clean-up procedure by solid-phase extraction was also developed to analyse azelaic acid in complex matrices, such as pharmaceutical and cosmetic formulations
Enantioselective analyses of antihistaminic drugs by high performance liquid chromatography
No full textHigh-performance liquid chromatographic methods have been developed for stereoselective separations of terfenadine and its active metabolite fexofenadine.Satisfactory enantioseparations of racemic terfenadine were achieved on a Chiralcel column by normal phase elution. Analysis of racemic fexofenadine, as such, took a very long time and achieved poor enantioselectivity on this column; nevertheless, the analyte when derivatised with diazomethane was well resolved.Racemic fexofenadine was also derivatised using a chiral agent: R-(+)-1-phenylethylisocyanate and subjected to achiral LC on a reversed-phase analytical column. Complete enantioseparations were achieved in short analysis times; excess reagent eluted before the diastereoisomeric pair and did not interfere
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