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FarmaKology Newsletter - Issue #42

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FarmaKology

April 20 · Issue #42 · View online
FarmaKology is a newsletter that brings you the latest news, research, job opportunities in the Pharma world, and much more! If you would like to be featured in the newsletter, sponsor an issue, or need anything, please feel free to get in touch with me at "abdul@farmakology.com".

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A Look at Two Novel Treatment Options for Acute Migraine:
Ubrelvy & Nurtec ODT
I grew up seeing my mother go through the phases of migraine and sometimes for days not leaving her bedroom. She had tried almost everything to get a better control of her headaches.
Unfortunately, she was never able to find relief and continued to struggle. It affected not only her job but us as a family. My brother and I missed having a mother to play with, help with homework, get ready for high school graduation, and many more events. My mother eventually turned to Botox injections which finally helped her and she hardly has any more migraines.
Today, I not only understand the dept of her headaches and its debilitating effects, but also find myself having the casual migraines here and there. Having a child myself and not wanting to miss out on the same moments I missed with my own mother, I set out to find better alternatives for myself before it takes over my life. Not taking control of migraines can turn into chronic migraines which means more frequent episodes and more difficult to manage.
Migraines are not just severe headaches. It comes with nausea, photo and sound sensitivity and lethargy. Even when the symptoms are gone, the body is physically exhausted and needs rest, which can cause few days of bed rest and absence from work. For me, after the episodes are over, I feel extreme hunger and become hazy for the entire day. I was excited to learn about two new medications that recently came out for the treatment of acute migraine and I knew I had to dig deeper and do a side by side comparison of the two.
Ubrelvy (ubrogepant) was approved in December 2019, while Nurtec ODT (rimegepant) was approved just two months later in February 2020. They both have the same mechanism of action which is Calcitonin Gene-Related Peptide (CGRP) inhibitor.
CGRP, a protein that is highly prevalent in the head and the neck, increases and transmits pain during a migraine attack. Inhibiting CGRP is what these two drugs do to manage the symptoms of migraine. I found this to be a novel idea compared to other mechanisms for treatment of migraine, such as blood vessel constriction by triptans, which can itself induce a host of other problems for the patient.
Nurtec ODT is an Oral Disintegrating Tablet (ODT) which gives it its quick dissolving property for the times that is needed to work fast since the key to migraine management is time. Just one dose of Nurtec ODT can last for up to 48 hours, and studies show that more than 85% of the patients do not need another dose.
This is a huge advantage compared to Ubrelvy tablets, which needs to be ingested, preferably with plenty of water, to more quickly start the process of being broken down to have its effect. In addition to difficulty swallowing while nauseated, the time it takes to actually have an effect can be delayed. Anyone that has ever had any type of headache, especially migraines, know how critical timing can be.
Nurtec ODT seems to have 96% protein binding affinity with a half-life of about 11 hours while Ubrelvy has a half-life of about 5-7 hours. This is the reason with Nurtec ODT, only one dose is required but with Ubrelvy, you might need to take another dose two hours later. Ubrelvy also comes in 3 different doses which means the 1 st dose taken at onset of migraine might not have been enough and a higher dose was needed. Therefore, waiting 2 hours to find out can mean missing work, missing family events, or being ineffective at school.
As a pharmacist talking and counseling thousands of people, I have heard many of the same complaints over the years: Having to take alternative OTC or prescription medications to further supplement their regimen and needing other rescue treatments.
Most insurances pay for only about 9 triptans per month and many find themselves using other drugs to manage the episodes in between, such as Tylenol, NSAIDs such as Ibuprofen, or Fioricet which is combination of acetaminophen, butalbital, and caffeine. Many also have severe allergy to lactose which is a very common filler for drugs. I was delighted to know both these medications do not contain lactose, making its allergy profile very clean.
As a certified pharmacogenomics pharmacist, I also looked at the metabolism and the enzymes used for both Nurtec ODT and Ubrelvy. The two medications are both CYP3A4 substrates which means there will be interactions with common medications that are CYP3A4 inhibitors such as Prozac (fluoxetine) or Prilosec (omeprazole) and inducers such as Dilantin (phenytoin).
Fortunately, for a medication that is in the form of an ODT, that metabolism profile is almost insignificant as its dissolves very quickly on the tongue before it enters the gut to be metabolized. This is not the same for a tablet which uses the enzymes present in the gut to break it down to either induce its pharmacological effect, get deactivated, or produce toxicity. Therefore, it is important to consider drug-drug interactions especially when taking Ubrelvy and how the body might react.
For me, it became clear that I prefer one dose that would act fast and lasts a long time so I can attend to my family and better take control of my migraines rather than letting it control my life as it did with my mother.
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