Eletriptan

Generic name: eletriptan
Brand name: Relpax
Dosage form: oral tablet (20 mg; 40 mg)
Drug class: Antimigraine agents

Medically reviewed by A Ras MD.

What is eletriptan?

Eletriptan is a prescription medicine that is used to treat migraine headaches.

Description

Eletriptan tablets contain eletriptan hydrobromide, which is a selective 5-hydroxytryptamine 1B/1D (5-HT1B/1D) receptor agonist. Eletriptan hydrobromide is chemically designated as (R)-3-[(1-Methyl-2-pyrrolidinyl)methyl]-5-[2-(phenylsulfonyl)ethyl]-1H-indole monohydrobromide, and it has the following chemical structure:

The empirical formula is C22H26N2O2S . HBr, representing a molecular weight of 463.43. Eletriptan hydrobromide is a white to light pale colored powder that is readily soluble in water.

Each eletriptan tablet for oral administration contains 24.2 or 48.5 mg of eletriptan hydrobromide equivalent to 20 mg or 40 mg of eletriptan, respectively. Each tablet also contains the inactive ingredients microcrystalline cellulose NF, lactose monohydrate NF, croscarmellose sodium NF, magnesium stearate NF, titanium dioxide USP, hypromellose, triacetin USP and FD&C Yellow No. 6 aluminum lake.

Mechanism of Action

Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors.

Migraines are likely due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of eletriptan for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.

Before taking eletriptan, tell your doctor:

If you are allergic to eletriptan; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
If you have any of these health problems: High blood pressure or some types of migraine headaches like hemiplegic or basilar migraine.
If you have ever had any of these health problems: Chest pain or pressure; diseased arteries going to the legs or arms; heart attack; heart disease; poor blood flow in the heart, brain, bowel, or kidney; stroke or transient ischemic attack (TIA); or a heartbeat that is not normal like Wolff-Parkinson-White syndrome.
If you have liver disease.
If you have taken almotriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan, or zolmitriptan in the last 24 hours.
If you have taken ergotamine, methysergide, dihydroergotamine, or any drug like them in the last 24 hours.
If you have taken clarithromycin, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, or troleandomycin in the last 72 hours.

This is not a list of all drugs or health problems that interact with eletriptan.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take eletriptan with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take eletriptan?

Tell all of your health care providers that you take eletriptan. This includes your doctors, nurses, pharmacists, and dentists.
Very bad and sometimes deadly allergic side effects have rarely happened. Talk with your doctor.
Avoid driving and doing other tasks or actions that call for you to be alert until you see how eletriptan affects you.
This medicine is not meant to prevent or lower the number of migraine headaches you get.
Taking more of eletriptan (a higher dose, more often) than your doctor told you to take may cause your headaches to become worse.
High blood pressure has happened with eletriptan. Have your blood pressure checked as you have been told by your doctor.
Very bad and sometimes deadly heart problems like heart attack and a heartbeat that is not normal have rarely happened within a few hours of taking eletriptan. Call your doctor right away if you have chest, throat, neck, or jaw tightness, pain, pressure, or heaviness; break out in a cold sweat; shortness of breath; a fast heartbeat; a heartbeat that does not feel normal; or very bad dizziness or passing out.
Use care if you have risks for heart disease (high blood pressure, high cholesterol, overweight, high blood sugar or diabetes, cigarette smoking, man older than 40 years of age, other family members with early heart disease, woman after change of life). Talk with your doctor.
If you are 65 or older, use eletriptan with care. You could have more side effects.
Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using eletriptan while you are pregnant.
Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

How is eletriptan best taken?

Use eletriptan as ordered by your doctor. Read all information given to you. Follow all instructions closely.

Take with or without food.
Take with liquids as early as you can after the attack has started.
If your headache comes back after the first dose, 1 more dose may be taken 2 hours after the first one.

What do I do if I miss a dose?

This medicine is taken on an as needed basis. Do not take more often than told by the doctor.

What are the side effects of eletriptan that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
Signs of high blood pressure like very bad headache or dizziness, passing out, or change in eyesight.
Very upset stomach or throwing up.
Very bad headache or if headache is not better after the first dose.
Constipation.
Diarrhea.
Severe stomach pain or bloody diarrhea.
Belly pain after meals.
A burning, numbness, or tingling feeling that is not normal.
Fever.
Weight loss.
Leg cramps.
Feeling of heaviness or tightness in the leg muscles.
Feeling cold.
Burning or aching pain in the feet or toes.
Change in color of skin to a bluish color like on the lips, nail beds, fingers, or toes.
A severe and sometimes deadly problem called serotonin syndrome may happen. The risk may be greater if you also take certain other drugs. Call your doctor right away if you have agitation; change in balance; confusion; hallucinations; fever; fast or abnormal heartbeat; flushing; muscle twitching or stiffness; seizures; shivering or shaking; sweating a lot; severe diarrhea, upset stomach, or throwing up; or very bad headache.
Very bad and sometimes deadly brain blood vessel problems like stroke have rarely happened with eletriptan. Call your doctor right away if you have weakness on 1 side of the body, trouble speaking or thinking, change in balance, drooping on 1 side of the face, or change in eyesight.

What are some other side effects of eletriptan?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

Dizziness.
Upset stomach.
Feeling tired or weak.
Feeling sleepy.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out eletriptan?

Store at room temperature.
Store in a dry place. Do not store in a bathroom.
Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.