Eletriptan

Eletriptan is used to treat the symptoms of migraine headaches (severe throbbing headaches that sometimes are accompanied by nausea and sensitivity to sound and light). Eletriptan is in a class of medications called selective serotonin receptor agonists. It works by narrowing blood vessels in the brain, stopping pain signals from being sent to the brain, and blocking the release of certain natural substances that cause pain, nausea, and other symptoms of migraine. Eletriptan does not prevent migraine attacks or reduce the number of headaches you have.

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom).

Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA's Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.

It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org

Eletriptan is an oral drug that is used for treating migraine headaches. It is in the "triptan" class of drugs that also includes sumatriptan (Imitrex), zolmitriptan (Zomig), naratriptan (Amerge), rizatriptan (Maxalt), almotriptan (Axert), and frovatriptan (Frova). Migraine headaches are believed to be the result of abnormal activity in the brain that leads to dilation of the blood vessels on the surface of the brain as well as the tissues that surround the brain. The dilation of the blood vessels is believed to be associated with inflammation. The triptan class of drugs, including eletriptan, constricts the blood vessels, thus preventing migraine headache. While it is very effective in relieving migraine, it does not prevent or reduce the number of attacks of migraine. In a large study, it was shown to be more effective than sumatriptan in relieving migraine headache pain within two hours. Eletriptan was approved by the FDA in December 2002.

Dosage Forms & Strengths

tablet

• 20mg
• 40mg

Migraine Headache

20-40 mg PO at onset of symptoms; repeat dose after 2 hr if necessary

Not to exceed 80 mg/day

Renal Impairment

Monitor for increase in blood pressure; dose adjustment not necessary

Hepatic Impairment

Mild to moderate impairment: Dose adjustment not necessary

Severe impairment: Do not administer

<18 years old: Not recommended

Migraine headache: See adult dosing

Mechanism of Action

Selective 5-HT1 receptor agonist in cranial arteries. Causes vasoconstriction and reduces inflammation associated with antidronic neuronal transmission associated with relief of migraine

Pharmacokinetics

Half-Life elimination: 4 hr

Peak Plasma Time: 1.5-2 hr

Bioavailability: 50%

Protein bound: 85%

Vd: 138 L

Metabolism: hepatic CYP3A4

Metabolites: N-demethylated eletriptan (10-20%)

Renal Clearance: 3.9 L/hr

Excretion: 90% Non-renal

Eletriptan is a prescription medication used to treat migraine headaches once they have started. Eletriptan belongs to a group of drugs called selective serotonin receptor agonists or "triptans", which reduce swelling of blood vessels surrounding the brain. This swelling is associated with the headache pain of a migraine attack. Eletriptan blocks the release of substances from nerve endings that cause more pain and other symptoms like nausea, and sensitivity to light and sound.

This medication comes in tablet form to be taken at the first sign of a migraine headache.  A second tablet can be taken after 2 hours if needed.

Common side effects of eletriptan include dizziness, nausea, and weakness. 

Tell your doctor if you are allergic to any ingredient in eletriptan.

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

Tell your doctor if you are pregnant or breastfeeding.

Tell your doctor if you are breastfeeding or plan to breastfeed. Eletriptan is excreted in human breast milk. It is not known if eletriptan will harm your nursing baby.

• Store eletriptan at room temperature 15–30°C (59–86°F).
• Keep eletriptan and all medicines out of the reach of children.

You should not take eletriptan if you have any history of heart disease, or if you have angina, blood circulation problems, lack of blood supply to the heart, uncontrolled high blood pressure, severe liver disease, ischemic bowel disease, a history of a heart attack or stroke, or if your headache seems to be different from your usual migraine headaches.

Do not take eletriptan within 24 hours before or after using another migraine headache medicine.

Do not use eletriptan within 72 hours before or after taking: clarithromycin, itraconazole, ketoconazole, nefazodone, ritonavir, or nelfinavir.

You should not use this medication if you are allergic to eletriptan, or if you have:

• coronary heart disease, angina (chest pain), blood circulation problems, lack of blood supply to the heart;

• a history of heart disease, heart attack, or stroke, including "mini-stroke";

• severe or uncontrolled high blood pressure;

• severe liver disease;

• ischemic bowel disease; or

• a headache that seems different from your usual migraine headaches.

To make sure you can safely take eletriptan, tell your doctor if you have any of these other conditions:

• liver disease;

• kidney disease;

• high blood pressure, a heart rhythm disorder; or

• risk factors for coronary artery disease (such as diabetes, menopause, smoking, being overweight, having high blood pressure or high cholesterol, having a family history of coronary artery disease, being older than 40 and a man, or being a woman who has had a hysterectomy).

It is not known whether this medicine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.

Eletriptan can pass into breast milk and may harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Do not give this medicine to anyone under 18 years old.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Usual Adult Dose for Migraine:

Use only after a clear diagnosis of migraine has been established

Initial dose: 20 mg or 40 mg orally, once
-Provided there has been some response to first dose, a second dose may be administered at least 2 hours later if migraine returns or symptoms recur.
Maximum dose: 80 mg in a 24-hour period

Comments:
-Doses should be individualized as responses vary; in clinical trials, benefit was observed with 20 mg, 40 mg, and 80 mg doses; however an increased incidence of side effects was observed at the 80 mg dose.
-This drug should not be used to treat basilar or hemiplegic migraines because these patients are at a greater risk of stroke.
-The safety of treating an average of 3 or more migraine attacks in a 30-day period has not been established.

Use: For the acute treatment of migraine with or without aura.

• If you have an allergy to eletriptan or any other part of eletriptan.
• If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
• 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 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 this medicine.

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.

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.

• If your symptoms or health problems do not get better or if they become worse, call your doctor.
• Do not share your drugs with others and do not take anyone else's drugs.
• Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
• Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
• Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about eletriptan, please talk with your doctor, nurse, pharmacist, or other health care provider.
• 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.

This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about eletriptan. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using eletriptan.

Review Date: October 4, 2017

The following adverse reactions are described elsewhere in other sections of the prescribing information:

• Myocardial ischemia and myocardial infarction, and Prinzmetal's angina [see Warnings and Precautions (5.2)]
• Arrhythmias [see Warnings and Precautions (5.3)]
• Chest, throat, neck, and/or jaw pain/tightness/pressure [see Warnings and Precautions (5.4)]
• Cerebrovascular events [see Warnings and Precautions (5.4)]
• Other vasospasm reactions [see Warnings and Precautions (5.5)]
• Medication overuse headache [see Warnings and Precautions (5.6)]
• Serotonin syndrome [see Warnings and Precautions (5.7)]
• Increase in blood pressure [see Warnings and Precautions (5.8)]
• Hypersensitivity reactions [see Contraindications (4) and Warnings and Precautions (5.9)]

Clinical Trials Experience

Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice.

Among 4,597 patients who treated the first migraine headache with Eletriptan in short-term placebo-controlled trials, the most common adverse reactions reported with treatment with Eletriptan were asthenia, nausea, dizziness, and somnolence. These reactions appear to be dose-related.

In long-term open-label studies where patients were allowed to treat multiple migraine attacks for up to 1 year, 128 (8.3%) out of 1,544 patients discontinued treatment due to adverse reactions.

Table 1 lists adverse reactions that occurred in the subset of 5,125 migraineurs who received Eletriptan doses of 20 mg, 40 mg and 80 mg or placebo in worldwide placebo-controlled clinical trials.

Only adverse reactions that were more frequent in an Eletriptan treatment group compared to the placebo group with an incidence greater than or equal to 2% are included in Table 1.

The frequency of adverse reactions in clinical trials did not increase when up to 2 doses of Eletriptan were taken within 24 hours. The incidence of adverse reactions in controlled clinical trials was not affected by gender, age, or race of the patients. Adverse reaction frequencies were also unchanged by concomitant use of drugs commonly taken for migraine prophylaxis (e.g., SSRIs, beta blockers, calcium channel blockers, tricyclic antidepressants), estrogen replacement therapy or oral contraceptives.

Postmarketing Experience

The following adverse reaction(s) have been identified during post approval use of Eletriptan. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Neurological: seizure

Digestive: vomiting

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.

Eletriptan hydrobromide tablets containing 20 mg or 40 mg Eletriptan (base) as the hydrobromide salt. Eletriptan hydrobromide tablets are orange, round, convex shaped, film-coated tablets with appropriate debossing.

They are supplied in the following strengths and package configurations:

Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].

Mild to moderate impairment: No dosage adjustment necessary.

Severe impairment: Use is not recommended.

Analgesics (Opioid): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

Antiemetics (5HT3 Antagonists): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

Anti-Parkinson Agents (Monoamine Oxidase Inhibitor): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity if selegiline, rasagiline, or safinamide is combined with a serotonin modulator. Use of transdermal selegiline with serotonin modulators is contraindicated. Consider therapy modification

Antipsychotic Agents: Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Eletriptan. Management: The use of eletriptan within 72 hours of a moderate CYP3A4 inhibitor should be avoided. Consider therapy modification

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Eletriptan. Avoid combination

Dapoxetine: May enhance the adverse/toxic effect of Serotonin Modulators. Avoid combination

Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Droxidopa: Serotonin 5-HT1D Receptor Agonists may enhance the hypertensive effect of Droxidopa. Monitor therapy

Ergot Derivatives: Serotonin 5-HT1D Receptor Agonists may enhance the vasoconstricting effect of Ergot Derivatives. Ergot Derivatives may enhance the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists. Exceptions: Nicergoline. Avoid combination

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Linezolid: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Management: Due to a risk of serotonin syndrome/serotonin toxicity, discontinue serotonin modulators 2 weeks prior to the administration of linezolid. If urgent initiation of linezolid is needed, discontinue serotonin modulators immediately and monitor closely. Consider therapy modification

Metaxalone: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

Methylene Blue: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Avoid combination

Methylphenidate: May enhance the adverse/toxic effect of Serotonin Modulators. Specifically, the risk of serotonin syndrome or serotonin toxicity may be increased. Monitor therapy

Metoclopramide: Serotonin Modulators may enhance the adverse/toxic effect of Metoclopramide. This may be manifest as symptoms consistent with serotonin syndrome or neuroleptic malignant syndrome. Monitor therapy

Palbociclib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Exceptions: Nicergoline; Tedizolid. Monitor therapy

Simeprevir: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Stiripentol: May increase the serum concentration of CYP3A4 Substrates. Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification

SUMAtriptan: Serotonin 5-HT1D Receptor Agonists may enhance the adverse/toxic effect of SUMAtriptan. Avoid combination

Tedizolid: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

TraMADol: Serotonin Modulators may enhance the adverse/toxic effect of TraMADol. The risk of seizures may be increased. TraMADol may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

1% to 10%:

Cardiovascular: Chest pain (2% to 4%; chest tightness, pain, and pressure), palpitations

Central nervous system: Dizziness (6% to 7%), drowsiness (6% to 7%), headache (4%), paresthesia (3% to 4%), chills, hypertonia, hypoesthesia, pain, vertigo

Dermatologic: Diaphoresis

Gastrointestinal: Nausea (8%), xerostomia (3% to 4%), abdominal pain (2%; pain, discomfort, stomach pain, cramps, and pressure), dyspepsia (2%), dysphagia (1% to 2%)

Neuromuscular & skeletal: Weakness (4% to 10%), back pain

Respiratory: Pharyngitis

<1% (Limited to important or life-threatening): Abnormal hepatic function tests, anaphylactoid reaction, anaphylaxis, angina pectoris, angioedema, cardiac arrhythmia, confusion, depersonalization, depression, edema, emotional lability, hyperesthesia, hyperkinesia, hypersensitivity reaction, hypertension, impotence, increased creatine phosphokinase, insomnia, ischemic colitis, lacrimation, myalgia, myasthenia, myocardial infarction, peripheral vascular disorder, photophobia, polyuria, Prinzmetal angina, seizure, skin rash, speech disturbance, stupor, tachycardia, thrombophlebitis, vasospasm, ventricular fibrillation, visual disturbance

Data not available