CGRP Blockers & SRAs – The New Faces In Research For Migraine Management

CGRP stands for Calcitonin Gene-Related Peptide. It is a calcitonin group compound made up of polymers of amino acid monomers. CGRP is manufactured in the human body in the nerve cells (neurons) of the central nervous system and the peripheral nervous system.

Research – New Migraine drugs In The Pipeline (1)

So what is the function of CGRP? Of the many functions, CGRP is a powerful vasodilator and it contributes significantly in the transmission of pain message through the body. It is also believed to play a critical role in cardiovascular homeostasis as well as in processing noxious stimuli that has the potential to damage the tissues of the heart.

The development of drugs which are essentially CGRP receptor antagonist is in the pipeline aimed at helping migraineurs the world over cull the pain of their migraine episodes. How does the CGRP receptor antagonist do this? It has been observed that during the onset of a migraine attack, CGRP binds to CGRP receptors and activates these receptors which then transmit pain signals. CGRP receptor antagonist prevents the CGRP from binding on to CGRP receptors thus circumventing the transmission of pain signals causing migraine pain.

Telecagepant was such a CGRP receptor antagonist drug developed by Merck & Co. and was undergoing Phase III clinical trials but the trials were abandoned after identification of two patients with significant elevations in serum transaminases indicating liver damage. However, similar drugs without such side-effects are now being designed. CGRP receptor blockers also significantly reduce nausea and are more desirable in total benefit than triptans. As per Peter Goadsby, MD, PhD, director of UCSF’s Headache Center, “So this is a way for it to be effective and adds a safety bonus to the patients and it seems to be better tolerated.” (2)

There is another approach to drug design and development aimed at reducing the misery of migraineurs and it comes from the side of serotonin activity. In this class, one investigational drug of note is Lasmiditan thought of by Eli Lilly & Co and being designed to treat acute migraine by CoLucid Pharmaceuticals. These drugs are technically serotonin receptor agonists and selectively bind to the 5-HT1F receptor subtype. Unlike triptans these drugs do not constrict the heart vessels and have lesser side-effects. Trials have shown that administration of this drug reduced migraines to almost nothing within a two-hour period in almost 60% of the patients also tackling nausea and photophobia beautifully. The drug is expected to be ready by 2014. As per Dr. Goadsby, “Lasmiditan is now that finished its phase two studies and clearly works. It does not have the same sort of liver effects as its predecessors and will move on into phase three. That is again for acute migraine treatment. So it is a safe and totally different action than what we currently have.” (2)

 

SOURCES:

1. Image by Ponsulak; Freedigitalphotos.net; March 2012;
   http://www.freedigitalphotos.net/images/view_photog.php?photogid=1983
   
2. Cutting Edge Treatments For Migraines: More Than Just A Headache; Ivanhoe.com; March 2012;
   http://www.ivanhoe.com/channels/p_channelstory.cfm?storyid=29106&channelid=CHAN-100018
   

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New Rapid Relief Migraine Drug from MAPP Inc Issued U.S Patent

The US Patent and Trademark Office has issued MAP Pharmaceutical Inc’s new drug under the banner, “Method of Therapeutic Administration of DHE to Enable Rapid Relief of Migraine while Minimizing Side Effect Profile.”

Pulmonary Administration DHE from MAPP Issued Patent (1)

The drug’s primary ingredient DHE or Dihydroergotamine is MAPP’s proprietary formulation. The novelty of this new formulation is that it has proved to have rapid efficacy in curbing migraine pain but minimizes the adverse effects that other migraine formulations have.

To be able to achieve quick distribution, metabolization and excretion of the drug, the DHE drug involves pulmonary administration or inhalation of the drug. This is advantageous as the results are almost instantaneous because the drug does not undergo a ‘first-pass effect’ and is absorbed almost entirely into the general blood circulation through the lungs.

The drug has been named LEVADEX® is an orally inhaled investigational drug administered using the Company’s proprietary TEMPO® inhaler for the potential acute treatment of migraine in adults and targets the pharmacokinetic profiles described in this patent. DHE is a drug that is currently available in other dosage forms to treat migraine. (2)

SOURCES:

1. Image from Ambro; Freedigitalphotos.net; February 2012; 
   http://www.freedigitalphotos.net/images/view_photog.php?photogid=1499
   
2. MAP Pharmaceuticals, Inc. (MAPP) Issued Additional U.S. Patent for Methods of Achieving Rapid Treatment of Migraine Based Upon Pharmacokinetic Profile; BioSpace; Febraury 2012;
   http://www.biospace.com/news_story.aspx?StoryID=250731&full=1
   

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What the Migraineurs Should Know About The Triptan Drugs

(Source:
http://tinyurl.com/l332mz
)

Triptans are the relatively new weaponry in the scientists’ arsenal in migraine management and treatment. They work at the neurochemical (serotonin receptor) level. Triptans are not painkillers. All the Triptan drugs act at the wall of the blood vessels (especially cranial/dural blood vessels) and cause their constriction (or narrowing) called vasoconstriction, thus offsetting the swelling that causes the pain. It is also effective in alleviating some of the other symptoms of migraine attack such as sensitivity to light and sound. It acts towards stimulating the release of serotonin in the bloodstream.

Triptan range of medication includes chemicals Frovatriptan, Naratriptan, Eletriptan, Sumatriptan, Almotriptan and Rizatriptan. They should however, never be mixed with ergotamine drugs or any other drug stated in the drug literature or by the doctor. In addition, they are not to be taken in conjunction with any anti-depressant that is known to increase serotonin levels. Neither are they indicated for use by hemiplegic and basilar artery migraineurs.

All of these medications have similar possible side effects such as those of dizziness, fatigue, tingling sensations on skin, dryness of mouth, hot flashes, chest pain or tightness, sensitivity to temperatures, joint pains, coronary artery vasospasm, transient myocardial ischemia, myocardial infarction, ventricular tachycardia, and ventricular fibrillation, serotonin syndrome etc.

Triptan drugs are available at pharmacies on showing a doctor’s prescription due to the potential side effects, which may be serious in nature. Some Triptan drugs work faster than the others do. Some others work for longer hours, some have only one set of side effects, and the other Triptans may have another set. This makes it imperative for you to consult your doctor before taking these medications. The doctor will make a decision on a case-to-case basis depending on your migraine frequency, intensity, duration, medical history (especially those of heart, diabetes and hypertension etc).

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