Ubrelvy is the brand name of Ubrogepant. It is a novel class of medicines, called the “gepants”. Ubrelvy got FDA approval in the US in 2019 for the acute treatment of migraine.
Ubrelvy (Ubrogepant) and drugs from the same class such as Rimegepant (Nurtec ODT) act by inhibiting the CGRPR (calcitonin gene-related peptide receptors).
Indications and Uses of Ubrelvy (Ubrogepant) [Ref]:
Ubrelvy is used to terminate the acute attack of migraine headache. It can be used in patients with migraine with or without aura.
Aura is a symptom complex that is perceived by patients with migraine a few moments before the onset of the headache. These symptoms include:
- Flashing lights
- abnormal sense of smell such as a sharp smell that is unpleasant
- enlarged blindspot or visual loss at one of the quadrants of the vision
- Photophobia or inability to tolerate light
- Weakness of one of the limbs or generalized weakness
The “gepants” including Ubrogepant and Rimegepant have the advantage of cardiac safety. So, unlike the triptans, they can be used in patients with hypertension, angina, and other cardiovascular diseases.
However, these drugs are not recommended to be used for the prevention of migraine headaches.
Ubrelvy Dose in the treatment of Acute Migraine headache:
Ubrelvy (Ubrogepant) is available in 50 mg and 100 mg tablets.
The usual recommended dose is 50 or 100 mg tablet immediately after the onset of headache. If the headache persists after two hours, another tablet of 100 mg may be taken.
The maximum recommended dose is 200 mg per 24 hours (per day). The safety of the drug to treat more than 8 migraine episodes per month has not been established.
The dose should be modified in patients who are on concomitant enzyme-inducers or enzyme-inhibitors and in patients with liver or renal impairment.
In such patients, the dose should be adjusted as mentioned below:
Dose Adjustment in specific situations
|Child Class C Liver disease||50 mg||50 mg|
|Severe renal impairment (CrCl of 15 to 30 ml/minute)||50 mg||50 mg|
|End-stage renal disease||Avoid Use|
|Moderate CYP3A4 inhibitors||50 mg||Avoid the next dose within 24 hours|
|Weak CYP3A4 inhibitors||50 mg||50 mg|
|Strong CYP3A4 Inducers||Avoid concomitant use|
|Weak or moderate CYP3A4 inducers||100 mg||100 mg|
|BCRP and/ or p-gp only inhibitors||50 mg||50 mg|
In case of drug overdosage, patients should be monitored for at least 24 hours since the drug has a half-life of about 7 hours.
How to take the Ubrelvy (Ubrogepant):
It has been observed that fatty food delays the absorption of the drug by as much as 2 hours. It is recommended to take the drug without meals or in a fasting state.
However, since it is recommended to take the drug immediately after the onset of the headache, one should not wait if he/ she has taken a meal.
Ubrelvy Dose in Liver and Renal Impairment:
Dose adjustment in Liver impairment:
The dosage adjustment has been mentioned in the table above. Although the drug exposure is slightly increased in patients with mild and moderate hepatic impairment, the manufacturer does not recommend any adjustments in the dose in these patients.
In severe hepatic impairment, the dose should be reduced to half as mentioned in the table above.
Dose Adjustment in Renal Impairment:
Although Ubrogepant does not undergo renal clearance, dose adjustment is recommended in severe renal impairment. The dose should be reduced by half as mentioned in the table above in patients with a CrCl of 15 to 30 ml/minute.
The manufacturer recommends avoiding the drug in end-stage renal disease (CrCl of less than 15 ml/minute).
In mild to moderate renal impairment, no dose adjustment is recommended.
Ubrelvy Use during Pregnancy and Lactation:
Ubrogepant has not been studied in human pregnant females. In animal studies, the drug has been associated with increased fetal deaths and low birth weight.
Migraine is also associated with an increased risk of preeclampsia and gestational hypertension. However, since the Ubrogepant has not been studied in pregnant females and animal studies have shown an increased risk of fetal deaths, it is not recommended to be used during pregnancy.
The excretion of the drug into breastmilk has also not been studied. Data is very limited. The manufacturer, therefore, recommends considering the health of the mother and the potential exposure of the nursing child before recommending treatment to lactating women.
Contraindications and Warnings:
Ubrogepant is contraindicated in patients who are allergic to the drug and in combination with strong CYP3A4 Inhibitors.
Strong CYP3A4 Inhibitors include:
- Clarithromycin (Klaricid)
- Itraconazole (Sporanox)
Side effects of Ubrelvy:
Ubrogepant, like Rimegepant, is considered a very safe medicine with minimal side effects.
The most common side effects that affect 2% or more of the individuals are nausea, dry mouth, and sleepiness (somnolence). These side effects compared to placebo treatment are tabulated below:
|Side effect||Ubrogepant 50 mg||Ubrogepant 100 mg||Placebo|
Mechanism of Action (MOA) of Ubrelvy (Ubrogepant):
Ubrogepant acts by inhibiting the calcitonin gene-related peptide receptors. These receptors have potent vasodilatory effects on the blood vessels.
The drug does not have any effect on the heart or QT intervals even when administered in supratherapeutic doses (twice the normally recommended doses).
After oral administration of the drug, the maximum plasma concentration is seen in about 1.5 hours. When administered with a fatty meal, the peak plasma concentrations is achieved in about 2 hours with a reduction in the Cmax by 22%.
87% of the drug is bound to plasma proteins.
The drug is primarily metabolized by the enzyme CYP3A4. The metabolites are not active. They bind to the CGRPR with 6000 times reduced affinity than the parent compound.
- The half-life elimination of the drug is about 5 to 7 hours
Brands of Ubrogepant:
Ubrelvy 50 mg and 100 mg tablets
Cost of Ubrelvy:
Ubrelvy 50 mg tablets cost USD $951 per ten tablets. The cost of ten tablets of 100 mg of Ubrelvy is approximately USD $996.
One tablet of 50 mg Ubrelvy costs USD 95.1.
One tablet of 100 mg costs USD 99.6