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CGRP Antagonists for Migraine Prophylaxis

Mark Percifield, PharmD: It’s nice to see that there are extra choices. Jennifer, may I ask you to come back in and speak about gepants? Gepants are an FDA-approved class of CGRP antagonists for the remedy of acute migraine. For those who may speak somewhat about ubrogepant and rimegepant, that might be nice.

Jennifer L. Mazan, PharmD: The CGRP protein is launched, or considered launched, throughout a migraine. These are CGRP antagonists, in order that they block the receptor. That’s how they work. Ubrogepant was the primary CGRP antagonist to be accepted for acute remedy of migraine. We had a few of them already accepted for power remedy or preventive remedy, however that’s simply the primary 1 accepted for acute remedy of migraine. It’s out there as 50-mg and 100-mg tablets, and sufferers have the choice to take a second dose after that 2-hour mark in the event that they want it.

It has been proven to be efficient in medical trials. There are 2 fundamental trials: the ACHIEVE I and the ACHIEVE II trials, each of which demonstrated the effectiveness of extra sufferers taking ubrogepant than placebo. About 60% of sufferers acquired aid after the 2-hour mark, about 20% have been pain-free on the 2-hour mark, and about 40% have been freed from their most bothersome signs on the 2-hour mark. It has a positive adverse-effect profile with nausea, somnolence, and dry mouth being essentially the most reported adversarial results, however the incidents of these are additionally very low. It does require dosage adjustment in sufferers with renal or hepatic dysfunction, however that dose ought to be not more than 50 mg. We don’t wish to transfer to the 100-mg dosing for individuals with hepatic or renal dysfunction. It ought to be prevented altogether for sufferers with extreme renal impairment.

It does have a number of drug interactions. It interacts with the CYP3A4 inducers. It’s contraindicated with concomitant use of itraconazole, ketoconazole, and clarithromycin. Rimegepant was the second CGRP antagonist accepted for the acute remedy of migraine. That drug is offered as a 75-mg pill. It’s a sublingual pill; it’s an ODT [orally disintegrating tablet] for single use solely. The benefit of that is the ODT, however you don’t have the choice of taking the second dose in the event you’re not getting sufficient aid. The efficacy may be very related. Once we have a look at the info, the chances are similar to ubrogepant, in order that they’re just about neck and neck so far as the efficacy goes. The protection profile additionally has a positive adverse-effect profile with nausea and abdomen ache or indigestion being essentially the most reported adversarial results. Once more, the incidence of those signs is low. The drug interactions of this are like that of ubrogepant. The CYP3A4 inhibitors and CYP3A4 inducers might be a difficulty and should be monitored. It additionally must be prevented when treating sufferers with hepatic and renal impairment.

Mark Percifield, PharmD: What suggestions have you ever gotten from sufferers concerning the ODT formulation? Is that one thing they appear to love?

Jennifer L. Mazan, PharmD: Many sufferers are drawn to the ODT formulation as a result of you do not want to have water. You may take it anytime, wherever. Individuals who expertise extreme nausea are extra seemingly to decide on the ODT formulation than an oral pill for the mere indisputable fact that they don’t must swallow utilizing water.

Mark Percifield, PharmD: It’s nice to listen to about these sufferers and the elevated proportion of them being pain-free after 2 hours with these new formulations. Sufferers have a greater choice than what we had, as Tim talked about, a number of many years in the past. Thanks very a lot.

Transcript edited for readability.

https://www.pharmacytimes.com/view/cgrp-antagonists-for-migraine-prophylaxis

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