Rimegepant (Nurtec ODT) is a new drug available as orally disintegrating tablets for the acute treatment of migraine headaches. Ubrelvy (Ubrogepant) is another drug from the same class used as an abortive migraine medicine.
Apart from triptans (Sumatriptan, Zolmitriptan, Almotriptan, etc), we only had NSAIDs and acetaminophen (paracetamol) for the acute treatment of migraine until now.
NSAIDs, like Naproxen and Adderall, are associated with severe gastrointestinal side effects. In addition, these drugs are contraindicated in patients who have kidney impairment.
Triptans use has been associated with hypertension and angina. In addition, these drugs can not be given to patients with heart diseases and with concomitant antidepressants.
Indications and Limitations of Rimegepant (Nurtec ODT) Use:
Nurtec ODT is used to treat patients with a severe acute attack of migraine headache. It can be used in patients with or without aura [Ref].
In clinical trials, 19.6% of the patients in the Rimegepant group noticed an improvement in their migraine headache compared to 12% in the placebo group after 2 hours [Ref]
The FDA has criticized the commercial of Nurtec ODT featuring Khloe Kardashian as it is misleading and falsely claims the drug’s efficacy and rapidity of onset [Ref]
The FDA has specifically highlighted the statement ” … as something that works within 15 to 30 minutes”. The statement is not scientifically backed by data from clinical trials.
An “Aura” is a symptom complex experienced by patients with migraine usually before the actual attack of migraine headache.
Patients with migraine Aura may have any of the following symptoms:
- Abnormal colors such as flashing lights, rainbows, and blurring of vision
- Abnormal sense of smell (usually not felt before and is unpleasant most of the time)
- Loss of vision on one or both sides
- Weakness or numbness of the head, arms, or legs
- Paralysis of one side of the body
Limitations to Nurtec ODT use:
It is not indicated for chronic use to prevent a migraine attack. It is not indicated to be used as a preventive migraine medicine.
For prevention of a migraine attack, commonly used medications include:
- Topiramate (Topamax)
- Valproic acid (Epival)
- Beta-blockers (Inderal)
- Calcium channel blockers (Verapamil, Diltiazem, and Flunarizine)
- Tricyclic antidepressants (Amitriptyline), and
- the Novel drugs Aimovig (Erenumab), Ajovy (Fremanezumab), and Emgality (Galcanezumab)
Nurtec ODT is not recommended to be used in children and individuals who are younger than 18 years of age.
Rimegepant (Nurtec ODT) Dose:
The usual dose of Nurtec ODT is 75 mg orally once a day. It is best taken within 1 minute of the onset of migraine headache.
For people with frequent migraine headaches, it is best to take preventive medicine. It is not advisable to use Nurtec ODT for more than 15 days per month (30 days).
Hence, it can be taken orally every other day. The maximum per month dose should not exceed 15 doses.
In case of overdosage, supportive treatment should be given to the patient. The drug is not dialyzable because of its strong binding affinity to plasma proteins.
Rimegepant Drug Interactions:
Nurtec ODT should not be taken simultaneously with another strong or moderate CYP3A4 inhibitor. If however, it is administered with a moderate CYP3A4 inhibitor, it should be taken at least 48 hours apart.
Significantly elevated blood levels of Nurtec ODT may occur resulting in toxicity if it is administered with a concomitant strong or moderate CYP3A4 inhibitor.
Some of the commonly used CYP3A4 inhibitors include:
- Clarithromycin and telithromycin
- Valproic acid
Nurtec ODT should also be avoided in patients who are on a concomitant strong or moderate CYP3A4 inducer. The concomitant use of a strong CYP3A4 inducer may decrease the efficacy of Rimepegant.
Some of the commonly used CYP3A4 inducers include:
Nurtec ODT should not be used in patients who are on concomitant drugs that inhibit P-gp and BCRP since Rimegepant is a substrate of these transporter proteins. This could result in significant systemic exposure to the drug.
Commonly used drugs that inhibit BCRP include:
Commonly used drugs that inhibit P-gp include:
- Omeprazole, and Lansoprazole
Rimegepant (Nurtec ODT) Use in Kidney and Liver impairment:
Use in Kidney disease:
In patients with mild, moderate, or severe renal impairment, the manufacturer has not recommended any dose adjustment.
The drug, however, has not been studied in patients with end-stage renal disease (CrCl of less than 13 ml/minute) and those on hemodialysis or peritoneal dialysis.
The manufacturer advises against its use in patients with end-stage renal disease.
Use in Liver disease:
The manufacturer recommends avoiding Nurtec ODT in patients with severe hepatic impairment (Child Class C). In these patients, the blood levels of the drug may exceed the normal levels and result in toxicity.
In those with Child Class A or B hepatic impairment, the drug can be used cautiously. Patients may be monitored for the development of any toxic effects of the drug. However, the manufacturer does not recommend any adjustments in the dose in these patients.
Rimegepant (Nurtec ODT) use in pregnancy and lactation:
Rimegepant (Nurtec ODT) has not been studied in human pregnancies. In animals, however, the drug was associated with significantly low birth weight and fetal variations when it was administered during the period of organogenesis.
This is the period correlating with the first trimester in human pregnancies. It is not recommended to be used during pregnancy since data is very limited.
In case of unintentional exposure to the drug during pregnancy, it should be reported.
Similarly, it is not known if the drug has any effect on the child if the nursing mother is taking the Nurtec ODT while breastfeeding.
It is also not known whether the drug is excreted in breastmilk or not. The effect of the drug on milk production is also not known.
The manufacturer recommends using Rimegepant during breastfeeding with caution taking the risk of exposure to the nursing child.
Rimegepant (Nurtec ODT) Side effects:
Nurtect ODT is considered a very safe oral medicine with minimal side effects. However, data is still being evaluated for side effects.
In clinical trials, and as per the manufacturer, the most common side effects of Nurtec ODT are:
- Nausea (2.7% of the patients developed nausea)
- Stomach pain and indigestion occurred in 2.4% of the patients.
Some patients reported:
“It gives me a weird feeling, mild general malaise. Like something is a little off”
Another patient reported:
“I feel like having a cold for about 30 minutes before it starts working”
Most patients reported that they did not notice any side effects.
Another most important side effects are allergic reactions that are mentioned in the “contraindications and warnings” section below.
Rimegepant (Nurtec ODT) Contraindications and Warnings:
Rimegepant (Nurtec ODT) is contraindicated in patients who are allergic to the drug or have had an allergic reaction to it in the past.
Serious allergic reactions manifesting as hypotension, shock, and angioedema have been reported with its use.
Individuals who develop a hypersensitivity reaction should immediately discontinue the treatment. Supportive measures such as oxygen inhalation, intravenous fluids, antiallergics, corticosteroids, and adrenaline may be administered.
Since delayed hypersensitivity reactions can occur, patients must be monitored for late-onset of hypersensitivity reactions.
Rimegepant (Nurtec ODT) Monitoring Parameters:
No specific monitoring parameters have been mentioned when using Nurtec ODT. However, the response to treatment should be assessed.
How to administer Rimegepant (Nurtec ODT)?
Nurtec ODT is administered via the oral route. The blister should be opened by peeling off the foil cover gently with dry hands. After removing the foil cover, the tablet should not be pushed to extract.
Once the tablet is removed from the blister pack, immediately put it over the tongue or under the tongue. The tablet should not be stored once it is removed from the blister.
The medicine will dissolve spontaneously inside the oral cavity and the liquid should be swallowed. There is no need for taking water or any liquid after the tablet is swallowed.
It is best to take the drug on an empty stomach immediately after the onset of pain.
Mechanism of action (MOA) of Rimegepant (Nurtec ODT):
Rimegepant belongs to the class of drugs called CGRPR antagonists (calcitonin gene-related peptide antagonists).
CGPR receptors are considered to play a significant role in the pathophysiology of migraine headaches.
However, unlike the triptans, Rimegepant has minimal vasoconstrictive properties and hence can be given to patients who have underlying cardiovascular disease or hypertension. Nurtec ODT also does not have any effect on cardiac electrophysiology and QT interval.
- The maximum concentration of the drug is found in the blood after 1.5 hours of sublingual administration. The absorption is delayed by about one hour if it is taken in a fed state, especially after a fatty meal.
- The absolute bioavailability of the drug is 64%
- About 96% of the drug is bound to plasma proteins.
- The drug is metabolized primarily by CYP3A4 and to a lesser extent by CYP2C9. Up to 77% of the drug is excreted as unchanged without any metabolites.
- The half-life elimination of the drug is about 11 hours
Brands of Rimegepant:
Cost of Rimegepant:
8 tablets of Nurtec ODT 75 mg sublingual disintegrating tablets cost USD $ 978.
One tablet of Nurtec ODT costs around $122.25 USD.