scholarly journals Telcagepant: A New Therapeutic Option for Acute Migraine?

2011 ◽  
Vol 3 ◽  
pp. CMT.S7477 ◽  
Author(s):  
E. Anne MacGregor

Telcagepant (MK0974) is one of several calcitonin-gene-related peptide antagonists in development as a potential treatment for acute migraine attacks and is the first orally available drug in this class. Preclinical and clinical data are reviewed, which support the efficacy and tolerability of telcagepant for the treatment of migraine, particularly for patients unable to tolerate, or who have cardiovascular contraindications to, triptans.

2020 ◽  
pp. 106002802095480 ◽  
Author(s):  
Alicia Potter DeFalco ◽  
Rachel Lazim ◽  
Nathan E. Cope

Objective To review the pharmacology, pharmacokinetics, efficacy, safety, and place in therapy of rimegepant for treatment of migraine. Data Sources A comprehensive PubMed and Cochrane search (1985 to May 2020) was performed utilizing the keywords rimegepant, Nurtec, orally disintegrating tablet, migraine, migraine headache, migraine disorder, calcitonin gene-related peptide, and calcitonin gene-related peptide antagonist. Additional data were obtained from the references of identified articles, manufacturer’s product labeling and website, ClinicalTrials.gov, and governmental sources. Study Selection and Data Extraction All English-language trials evaluating oral rimegepant were included for this review. Data Synthesis Rimegepant orally disintegrating tablet (ODT) is Food and Drug Administration approved for the treatment of migraine. According to data from 3 phase 3 randomized controlled trials, rimegepant has been shown to significantly improve freedom from pain at 2 hours after the dose and freedom from the most bothersome symptom 2 hours postdose. Additional outcomes improved include freedom from photophobia and phonophobia at 2 hours postdose and pain relief 2 hours after the dose. Adverse effects of rimegepant include nausea, urinary tract infection, and dizziness. Relevance to Patient Care and Clinical Practice Orally disintegrating rimegepant provides a novel mechanism of action for the treatment of acute migraine. When patients experience inadequate relief from other therapies, have contraindications to triptans, or are unable to tolerate the adverse effects of triptans, rimegepant is a promising therapeutic option. Conclusion Rimegepant ODT is an efficacious migraine treatment option with a novel mechanism of action, convenient dosage form, and limited adverse effect profile.


Author(s):  
S. Padmaja ◽  
J. Mohan

Migraine is a mysterious disorder characterized by pulsating head ache, which is actually characterized to one side and comes in attacks which will be lasting for about 3-48 hours and can be associated with nausea,vomiting,sensitivity to sound,flashes of light,vertigoand diarrhoea [1]. Most of the drugs which are in current use for actue migraine like triptans, treats the disorder symptomatically. A novel group of drugs has been in research for the migraine which treats the disorder pathologically. Calcitonin gene – related peptide (CGRP) has a major role in the pathophysiology of the disorder and hence CGRP receptor antagonist, known as Gepants are in the research process [2]. Gepants are being studied for the efficacy of treating acute migraine [2]. This article will be a review article about the drug – Ubrogepant, which is approved for treatment of migraine with acute attacks in adults [3].


2021 ◽  
Author(s):  
Jiyoung Kim ◽  
Kyoungjune Pak ◽  
Gha-Hyun Lee ◽  
Jae Wook Cho ◽  
Hyun-Woo kim

Abstract Background: The pathophysiology of migraine has been researched incessantly, and it has been suggested that calcitonin gene-related peptide (CGRP) is associated with migraine attacks. CGRP receptor blockers are attracting attention for migraine prevention and treatment of acute episodes, and CGRP receptor antagonists have been shown to be effective in treating acute migraine headaches. This meta-analysis aimed to assess the effect of available CGRP receptor antagonists, focusing on their therapeutic doses for acute migraine treatment.Methods: We performed a systematic search of MEDLINE (from inception to March 2021) and EMBASE (from inception to March 2021) for English publications using the keywords “migraine” and “Calcitonin gene-related peptide,” limited to human studies.Results: Five studies that focused on examining the effects of CGRP receptor antagonists on acute migraine treatment met the eligibility criteria for this meta-analysis. The pooled analysis demonstrated that the CGRP receptor antagonist improved freedom from pain (OR=2.066, 95% confidence interval [CI] 1.766–2.418, I2=0%), absence of bothersome symptoms (OR=1.606, 95% CI=1.408–1.830, I2=0%), pain relief (OR=1.791, 95% CI=1.598–2.008, I2=0%), and freedom from nausea (OR=1.361, 95% CI=1.196–1.548, I2=0%), significantly more than the placebo. Conclusions: CGRP receptor antagonists are effective for acute migraine treatment and are expected to be used clinically as emerging therapeutic agents.


Author(s):  
Saravana Kumar Ramasubbu ◽  
Senkadhirdasan Dakshinamurthy ◽  
Sarika Palepu ◽  
Arkapal Bandyopadhyay ◽  
Sathish Kumar Rajendran

Migraine is a neurological condition characterized by intense, debilitating headaches. Symptoms may include nausea, vomiting, numbness or tingling, sensitivity to light and sound. There are multitude of drugs available to treat migraine like triptans, non-steroidal anti-inflammatory drugs, ergots and opioids. But these drugs are associated with adverse effects especially triptans causing cardiovascular effects limiting its use. During last decade, calcitonin gene-related peptide (CGRP) has emerged as a possible mechanism for management of migraine. CGRP has been shown to release during episode of migraine attack and it may play a causative role in induction of migraine. Rimegepant is a novel CGRP antagonist has been approved by FDA for treatment of acute migraine. Rimegepant is a first oral CGRP antagonist compared to other gepants. The oral bioavailability of Rimegepant is 64% and high fat meal can decrease the Cmax, Tmax and area under the curve. This drug is mainly metabolized by CYP3A4 and to lesser extent by CYP2C9. Most common adverse reactions associated with this drug were nausea and urinary tract infection. Clinical trials for Rimegepant have been positive, and results suggest that the drug may be a new safe and effective option for treatment of acute migraine.


2019 ◽  
Vol 53 (1) ◽  
Author(s):  
Kristina M. Canlas ◽  
Regina A. Macalintal-Canlas ◽  
Fumihiko Sakai

Objective. This study determined the efficacy of calcitonin gene-related peptide (CGRP) antagonists in the treatment of acute migraine. Methods. Seven randomized, controlled trials were included. Outcome measures used were pain freedom and pain relief two hours after treatment. Results. The difference in pain freedom 2 hours post-dose significantly favored gepants 140/150 mg (OR=2.39, 95% CI=1.93-2.96, P<0.00001) and 280/300 mg (OR=2.94, 95% CI=2.44-3.35, P<0.00001) over placebo, while the difference in pain freedom 2 hours post- dose did not significantly favor triptans over gepants 140/150 mg and vice versa (OR=0.62, 95% CI=0.32-1.21, P=0.16) and over gepants 280/300 mg (OR=0.86, 95% CI=0.64-1.15, P=0.34). The difference in pain relief 2 hours post-dose significantly favored gepants 140/150 mg (OR=2.49, 95% CI=2.13-2.91, P<0.00001) and 280/300 mg (OR=2.78, 95% CI=2.41-3.21, P<0.00001) over placebo. The difference in pain relief 2 hours post-dose significantly favored triptans over gepants 140/150 mg (OR=0.73, 95% CI=0.56-0.96, P=0.03), but not over gepants 280/300 mg and vice versa (OR=0.98, 95% CI=0.76-1.27, P=0.89). Conclusion. With regard to pain freedom and pain relief two hours post-dose, CGRP antagonists are more efficacious than placebo in the treatment of acute migraine but there is insufficient evidence to demonstrate superior efficacy of CGRP antagonists over triptans.


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