Drugs Details

Drugs Info of Relpax
Drugs Details
  • Drugs Type  : FDA
  • Date : 27th Jan 2015 03:20 am
  • Brand Name : Relpax
  • Generic Name : eletriptan (Pronunciation: EL e TRIP tan)
Descriptions

RELPAX (eletriptan hydrobromide) 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:

 

RELPAX® (eletriptan hydrobromide) Structural Formula Illustration

The empirical formula is C22H26N2O2S . HBr, representing a molecular weight of 462.43. Eletriptan hydrobromide is a white to light pale colored powder that is readily soluble in water.

Each RELPAX 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.

What are the possible side effects of eletriptan (Relpax)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop using eletriptan and call your doctor at once if you have a serious side effect such as:

  • feeling of pain or tightness in your jaw, neck, or throat;
  • chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, general ill feeling;
  • sudden numbness or weakness, especially on one side of the body;
  • sudden severe headache, confusion, problems with vision, speech, or...

Read All Potential Side Effects and See Pictures of Relpax »

What are the precautions when taking eletriptan hydrobromide (Relpax)?

Before taking eletriptan, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: blood circulation problems (for example, in your legs, arms/hands, or stomach), certain types of headaches (hemiplegic or basilar migraine), heart problems (such as chest pain, irregular heartbeat, previous heart attack), liver disease, seizure, stroke or "mini-stroke" (transient ischemic attack).

Certain conditions can increase your risk for heart problems. Tell your doctor if you have any of these conditions,...

Read All Potential Precautions of Relpax »

This monograph has been modified to include the generic and brand name in many instances.

Indications

RELPAX is indicated for the acute treatment of migraine with or without aura in adults.

Limitations of Use

  • Use only if a clear diagnosis of migraine has been established. If a patient has no response to the first migraine attack treated with RELPAX, reconsider the diagnosis of migraine before RELPAX is administered to treat any subsequent attacks.
  • RELPAX is not intended for the prevention of migraine attacks.
  • Safety and effectiveness of RELPAX have not been established for cluster headache.

Dosage Administration

The maximum recommended single dose is 40 mg.

In controlled clinical trials, single doses of 20 mg and 40 mg were effective for the acute treatment of migraine in adults. A greater proportion of patients had a response following a 40 mg dose than following a 20 mg dose [see Clinical Studies].

If the migraine has not resolved by 2 hours after taking RELPAX, or returns after transient improvement, a second dose may be administered at least 2 hours after the first dose. The maximum daily dose should not exceed 80 mg.

The safety of treating an average of more than 3 migraine attacks in a 30-day period has not been established.

How Supplied

Dosage Forms And Strengths

20 mg Tablets: Orange, round, convex shaped, film-coated, with “PFIZER” and “REP20” debossed.

40 mg Tablets: Orange, round, convex shaped, film-coated, with “PFIZER” and “REP40” debossed.

Storage And Handling

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

They are supplied in the following strengths and package configurations:

Relpax Tablets

Package Configuration Tablet Strength (mg) NDC Code Debossing
Carton of 12 tablets. Two blisters of 6 tablets in each carton. 40 mg 0049-2340-05 REP40 and Pfizer
Blister of 6 tablets 20 mg 0049-2330-45 REP20 and Pfizer
Blister of 6 tablets 40 mg 0049-2340-45 REP40 and Pfizer

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].

Distributed by: Roerig, Division of Pfizer Inc, Y, NY 10017. Revised September 2013

This monograph has been modified to include the generic and brand name in many instances.

Side Effects

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]
  • Arrhythmias [see WARNINGS AND PRECAUTIONS]
  • Chest, throat, neck, and/or jaw pain/tightness/pressure [see WARNINGS AND PRECAUTIONS]
  • Cerebrovascular events [see WARNINGS AND PRECAUTIONS]
  • Other vasospasm reactions [see WARNINGS AND PRECAUTIONS]
  • Medication overuse headache [see WARNINGS AND PRECAUTIONS]
  • Serotonin syndrome [see WARNINGS AND PRECAUTIONS]
  • Increase in blood pressure [see WARNINGS AND PRECAUTIONS]
  • Hypersensitivity reactions [see CONTRAINDICATIONS and WARNINGS AND PRECAUTIONS]

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 RELPAX in short-term placebo-controlled trials, the most common adverse reactions reported with treatment with RELPAX 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 a RELPAX treatment group compared to the placebo group with an incidence greater than or equal to 2% are included in Table 1.

Table 1: Adverse Reactions Incidence in Placebo-Controlled Migraine Clinical Trials: Reactions Reported by ≥ 2% Patients Treated with RELPAX and More Than Placebo

Adverse Reaction Type Placebo
(n=988)
RELPAX 20 mg
(n=431)
RELPAX 40 mg
(n=1774)
RELPAX 80 mg
(n=1932)
ATYPICAL SENSATIONS
Paresthesia 2% 3% 3% 4%
Flushing/feeling of warmth 2% 2% 2% 2%
PAIN AND PRESSURE SENSATIONS
Chest – tightness/pain/pressure 1% 1% 2% 4%
Abdominal – pain/discomfort/stomach pain/ cramps/pressure 1% 1% 2% 2%
DIGESTIVE
Dry mouth 2% 2% 3% 4%
Dyspepsia 1% 1% 2% 2%
Dysphagia – throat tightness/difficulty swallowing 0.20% 1% 2% 2%
Nausea 5% 4% 5% 8%
NEUROLOGICAL
Dizziness 3% 3% 6% 7%
Somnolence 4% 3% 6% 7%
Headache 3% 4% 3% 4%
OTHER
Asthenia 3% 4% 5% 10%

The frequency of adverse reactions in clinical trials did not increase when up to 2 doses of RELPAX 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 RELPAX. 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

Read the Relpax (eletriptan hydrobromide) Side Effects Center for a complete guide to possible side effects

Learn More »

Interactions

Ergot-Containing Drugs Including Other 5-HT1B/1D Agonists

Ergot-containing drugs have been reported to cause prolonged vasospastic reactions. Because these effects may be additive, use of ergotamine-containing or ergot-type medications (like dihydroergotamine [DHE] or methysergide) and RELPAX within 24 hours of each other is contraindicated. Concomitant use of other 5-HT1 agonists within 24 hours of RELPAX treatment is contraindicated [see CONTRAINDICATIONS

CYP3A4 Inhibitors

Potent CYP3A4 inhibitors significantly increase the exposure of RELPAX. Relpax should not be used within at least 72 hours of treatment with potent CYP3A4 inhibitors [see CONTRAINDICATIONS and CLINICAL PHARMACOLOGY].

Selective Serotonin Reuptake Inhibitors/Serotonin Norepinephrine Reuptake Inhibitors and Serotonin Syndrome

Cases of serotonin syndrome have been reported during co-administration of triptans and SSRIs, SNRIs, TCAs and MAO inhibitors [see WARNINGS AND PRECAUTIONS].

Read the Relpax Drug Interactions Center for a complete guide to possible interactions

Learn More »

This monograph has been modified to include the generic and brand name in many instances.

Warnings

Included as part of the PRECAUTIONS section.

Precautions

RELPAX should only be usedwhere a clear diagnosis of migraine has been established.

Myocardial Ischemia, Myocardial Infarction, and Prinzmetal's Angina

RELPAX is contraindicated in patients with ischemic or vasospastic CAD. There have been rare reports of serious cardiac adverse reactions, including acute myocardial infarction, occurring within a few hours following administration of RELPAX. Some of these reactions occurred in patients without known CAD. RELPAX may cause coronary artery vasospasm (Prinzmetal's angina), even in patients without a history of CAD.

Perform a cardiovascular evaluation in triptan-naïve patients who have multiple cardiovascular risk factors (e.g., increased age, diabetes, hypertension, smoking, obesity, strong family history of CAD) prior to receiving RELPAX. Do not use RELPAX if there is evidence of CAD or coronary artery vasospasm [see CONTRAINDICATIONS]. For patients with multiple cardiovascular risk factors who have a negative cardiovascular evaluation, consider administering the first RELPAX dose in a medically-supervised setting and performing an electrocardiogram (ECG) immediately following administration of RELPAX. For such patients, consider periodic cardiovascular evaluation in intermittent long-term users of RELPAX.

Arrhythmias

Life-threatening disturbances of cardiac rhythm including ventricular tachycardia and ventricular fibrillation leading to death have been reported within a few hours following the administration of 5-HT1 agonists. Discontinue RELPAX if these disturbances occur. RELPAX is contraindicated in patients with Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders [see CONTRAINDICATIONS].

Chest, Throat, Neck and/or Jaw Pain/Tightness/Pressure

Sensations of tightness, pain, and pressure in the chest, throat, neck, and jaw commonly occur after treatment with RELPAX and are usually non-cardiac in origin. However, perform a cardiac evaluation if these patients are at high cardiac risk. RELPAX is contraindicated in patients with CAD or Prinzmetal's variant angina [see CONTRAINDICATIONS].

Cerebrovascular Events

Cerebral hemorrhage, subarachnoid hemorrhage, and stroke have occurred in patients treated with 5-HT1 agonists, and some have resulted in fatalities. In a number of cases, it appears possible that the cerebrovascular events were primary, the 5-HT1 agonist having been administered in the incorrect belief that the symptoms experienced were a consequence of migraine, when they were not.

Before treating headaches in patients not previously diagnosed as migraineurs, and in migraineurs who present with symptoms atypical of migraine, other potentially serious neurological conditions need to be excluded. RELPAX is contraindicated in patients with a history of stroke or TIA [see CONTRAINDICATIONS].

Other Vasospasm Reactions

RELPAX may cause non-coronary vasospastic reactions, such as peripheral vascular ischemia, gastrointestinal vascular ischemia and infarction (presenting with abdominal pain and bloody diarrhea), and Raynaud's syndrome. In patients who experience symptoms or signs suggestive of a vasospastic reaction following the use of any 5-HT1 agonist, rule out a vasospastic reaction before receiving additional RELPAX doses [see CONTRAINDICATIONS].

Medication Overuse Headache

Overuse of acute migraine drugs (e.g. ergotamine, triptans, opioids, or combination of these drugs for 10 or more days per month) may lead to exacerbation of headache (medication overuse headache). Medication overuse headache may present as migraine-like daily headaches or as a marked increase in frequency of migraine attacks. Detoxification of patients, including withdrawal of the overused acute migraine drugs and treatment of withdrawal symptoms (which often includes a transient worsening of headache) may be necessary.

Serotonin Syndrome

Serotonin syndrome may occur with RELPAX, particularly during co-administration with selective serotonin reuptake inhibitors (SSRIs), serotonin norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), and monoamine oxidase (MAO) inhibitors [see DRUG INTERACTIONS]. Serotonin syndrome symptoms may include mental status changes (e.g., agitation, hallucinations, coma), autonomic instability (e.g., tachycardia, labile blood pressure, hyperthermia), neuromuscular aberrations (e.g., hyperreflexia, incoordination), and/or gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea). The onset of symptoms usually occurs within minutes to hours of receiving a new or a greater dose of a serotonergic medication. Discontinue RELPAX if serotonin syndrome is suspected.

Increase in Blood Pressure

Significant elevation in blood pressure, including hypertensive crisis with acute impairment of organ systems, has been reported on rare occasions in patients treated with 5-HT1 agonists, including patients without a history of hypertension. Monitor blood pressure in patients treated with RELPAX. RELPAX is contraindicated in patients with uncontrolled hypertension [see CONTRAINDICATIONS].

Anaphylactic/Anaphylactoid Reactions

There have been reports of anaphylaxis, anaphylactoid, and hypersensitivity reactions including angioedema in patients receiving RELPAX. Such reactions can be life threatening or fatal. In general, anaphylactic reactions to drugs are more likely to occur in individuals with a history of sensitivity to multiple allergens. RELPAX is contraindicated in patients with a history of hypersensitivity reaction to RELPAX [see CONTRAINDICATIONS].

Patient Counseling Information

See FDA Approved Patient Labeling (PATIENT INFORMATION)

Myocardial Ischemia and/or Infarction, Prinzmetal's Angina, Other Vasospastic Reactions, and Cerebrovascular Events

Inform patients that RELPAX may cause serious cardiovascular adverse reactions such as myocardial infarction or stroke, which may result in hospitalization and even death. Although serious cardiovascular reactions can occur without warning symptoms, instruct patients to be alert for the signs and symptoms of chest pain, shortness of breath, weakness, slurring of speech, and instruct them to ask for medical advice when observing any indicative sign or symptoms. Instruct patients to seek medical advice if they have symptoms of other vasospastic reactions [see WARNINGS AND PRECAUTIONS].

Anaphylactic/Anaphylactoid Reactions

Inform patients that anaphylactic/anaphylactoid reactions have occurred in patients receiving RELPAX. Such reactions can be life threatening or fatal. In genera l, anaphylactic reactions to drugs are more likely to occur in individuals with a history of sensitivity to multiple allergens [see CONTRAINDICATIONS].

Medication Overuse Headache

Inform patients that use of drugs to treat acute migraines for 10 or more days per month may lead to an exacerbation of headache, and encourage patients to record headache frequency and drug use (e.g., by keeping a headache diary) [see WARNINGS AND PRECAUTIONS].

Serotonin Syndrome

Inform patients about the risk of serotonin syndrome with the use of RELPAX or other triptans, particularly during combined use with selective serotonin reuptake inhibitors (SSRIs) or serotonin norepinephrine reuptake inhibitors (SNRIs) [see WARNINGS AND PRECAUTIONS and DRUG INTERACTIONS].

Pregnancy

Inform patients that RELPAX should not be used during pregnancy unless the potential benefit justifies the potential risk to the fetus [see Use In Specific Populations].

Nursing Mothers

Inform patients to notify their healthcare provider if they are breastfeeding or plan to breastfeed [see Use in Specific Populations].

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenesis

Eletriptan was administered to rats and mice in the diet for 104 weeks. In rats, the incidence of testicular interstitial cell adenomas was increased at the high dose of 75 mg/kg/day, but not at 15 mg/kg/day, a dose associated with plasma exposures (AUC) approximately 2 times that in humans at the MRHD of 80 mg/day. In mice, the incidence of hepatocellular adenomas was increased at the high dose of 400 mg/kg/day, but not a dose of 90 mg/kg/day, associated with plasma AUC approximately 7 times that in humans at the MRHD.

Mutagenesis

Eletriptan was negative in in vitro (bacteria reverse mutation (Ames), mammalian cell gene mutation (CHO/ HGPRT), chromosomal aberration assay in human lymphocytes) and in vivo (mouse micronucleus) assays.

Impairment of Fertility

In a fertility and early embryonic development study, eletriptan (50, 100, or 200 mg/kg/day) was orally administered to male and female rats prior to and throughout mating and continuing in females to implantation. Plasma exposures (AUC) were 4, 8 and 16 times in males and 7, 14 and 28 times in females, respectively, that in humans at the MRHD. Dose-related decreases in the number of corpora lutea, implants, and viable fetuses per dam were observed at all doses. Prolongation of the estrus cycle was observed at the highest dose tested. Male fertility parameters were not affected.

Use In Specific Populations

Pregnancy

Pregnancy Category C

There are no adequate and well-controlled studies in pregnant women. In reproductive toxicity studies in pregnant animals, oral administration of eletriptan was associated with developmental toxicity (decreased fetal and pup weights and an increased incidence of fetal structural abnormalities) at clinically relevant plasma exposures. RELPAX should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus

When pregnant rats were administered eletriptan during the period of organogenesis at doses of 10, 30 or 100 mg/kg/day, fetal weights were decreased and the incidences of vertebral and sternebral variations were increased at 100 mg/kg/day (approximately 12 times the maximum recommended human dose [MRHD] of 80 mg/day on a mg/m² basis). The 30 and 100 mg/kg/day doses were also maternally toxic, as evidenced by decreased maternal body weight gain during gestation. The no-effect dose for developmental toxicity in rats was 30 mg/kg/day, which is approximately 4 times the MRHD on a mg/m² basis.

When doses of 5, 10, or 50 mg/kg/day were given to pregnant rabbits throughout organogenesis, fetal weights were decreased at 50 mg/kg/day, which is approximately 12 times the MRHD on a mg/m² basis. The incidences of fused sternebrae and vena cava deviations were increased at all doses. Maternal toxicity was not evident at any dose. A no-effect dose for developmental toxicity in rabbits was not established; the lowest dose tested (5 mg/kg/day) is similar to the MRHD on a mg/m² basis.

Nursing Mothers

Eletriptan is excreted in human milk. Caution should be exercised when RELPAX is administered to a nursing woman.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

The efficacy of RELPAX Tablets (40 mg) in patients 11-17 was not established in a randomized, placebo-controlled trial of 274 adolescent migraineurs [see Clinical Studies]. Adverse reactions observed were similar in nature to those reported in clinical trials in adults. Postmarketing experience with other triptans includes a limited number of reports that describe pediatric patients who have experienced clinically serious adverse reactions that are similar in nature to those reported rarely in adults. Long-term safety of eletriptan was studied in 76 adolescent patients who received treatment for up to one year. A similar profile of adverse reactions to that of adults was observed. The long-term safety of eletriptan in pediatric patients has not been established.

Geriatric Use

Blood pressure was increased to a greater extent in elderly subjects than in young subjects. The pharmacokinetic disposition of eletriptan in the elderly is similar to that seen in younger adults [see CLINICAL PHARMACOLOGY]. In clinical trials, there were no apparent differences in efficacy or the incidence of adverse reactions between patients under 65 years of age and those 65 and above.

Hepatic Impairment

The effect of severe hepatic impairment on RELPAX metabolism has not been evaluated. RELPAX is not recommended for use in patients with severe hepatic impairment [see CLINICAL PHARMACOLOGY].

This monograph has been modified to include the generic and brand name in many instances.

OverDose

The elimination half-life of eletriptan is about 4 hours [see CLINICAL PHARMACOLOGY], therefore monitoring of patients after overdose with eletriptan should continue for at least 20 hours or longer while symptoms or signs persist.

There is no specific antidote to eletriptan.

It is unknown what effect hemodialysis or peritoneal dialysis has on the serum concentration of eletriptan.

 

ContrainDications

RELPAX is contraindicated in patients with:

  • Ischemic coronary artery disease (CAD) (angina pectoris, history of myocardial infarction, or documented silent ischemia) or coronary artery vasospasm, including Prinzmetal's angina [see WARNINGS AND PRECAUTIONS].
  • Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders [see WARNINGS AND PRECAUTIONS].
  • History of stroke, transient ischemic attack (TIA), or history or current evidence of hemiplegic or basilar migraine because these patients are at a higher risk of stroke [see WARNINGS AND PRECAUTIONS].
  • Peripheral vascular disease [see WARNINGS AND PRECAUTIONS].
  • Ischemic bowel disease [see WARNINGS AND PRECAUTIONS].
  • Uncontrolled hypertension [see WARNINGS AND PRECAUTIONS].
  • Recent use (i.e., within 24 hours) of another 5-hydroxytryptamine1 (5-HT1) agonist, ergotamine-containing medication, or ergot-type medication such as dihydroergotamine (DHE) or methysergide [see DRUG INTERACTIONS].
  • Hypersensitivity to RELPAX (angioedema and anaphylaxis seen) [see WARNINGS AND PRECAUTIONS].
  • Recent use (i.e., within at least 72 hours) of the following potent CYP3A4 inhibitors: ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, or nelfinavir [see DRUG INTERACTIONS and CLINICAL PHARMACOLOGY].

This monograph has been modified to include the generic and brand name in many instances.

Clinical Pharamacology

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 RELPAX 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.

Pharmacokinetics

Absorption

Eletriptan is well absorbed after oral administration with peak plasma levels occurring approximately 1.5 hours after dosing to healthy subjects. In patients with moderate to severe migraine the median Tmax is 2.0 hours. The mean absolute bioavailability of eletriptan is approximately 50%. The oral pharmacokinetics are slightly more than dose-proportional over the clinical dose range. The AUC and Cmax of eletriptan are increased by approximately 20 to 30% following oral administration with a high fat meal. RELPAX can be taken with or without food.

Distribution

The volume of distribution of eletriptan following IV administration is 138L. Plasma protein binding is moderate and approximately 85%.

Metabolism

The N-demethylated metabolite of eletriptan is the only known active metabolite. This metabolite causes vasoconstriction similar to eletriptan in animal models. Though the half-life of the metabolite is estimated to be about 13 hours, the plasma concentration of the N-demethylated metabolite is 10-20% of parent drug and is unlikely to contribute significantly to the overall effect of the parent compound.

In vitro studies indicate that eletriptan is primarily metabolized by cytochrome P-450 enzyme CYP3A4 [see CONTRAINDICATIONS and DRUG INTERACTIONS].

Elimination

The terminal elimination half-life of eletriptan is approximately 4 hours. Mean renal clearance (CLR) following oral administration is approximately 3.9 L/h. Non-renal clearance accounts for about 90% of the total clearance.

Special Populations

Age: The pharmacokinetics of eletriptan are generally unaffected by age. Blood pressure was increased to a greater extent in elderly subjects than in young subjects [see Use in Specific Populations ]. The pharmacokinetic disposition of eletriptan in the elderly is similar to that seen in younger adults.

There is a statistically significant increased half-life (from about 4.4 hours to 5.7 hours) between elderly (65 to 93 years of age) and younger adult subjects (18 to 45 years of age) [see Use In Specific Populations].

Gender: The pharmacokinetics of eletriptan are unaffected by gender.

Race: A comparison of pharmacokinetic studies run in western countries with those run in Japan has indicated an approximate 35% reduction in the exposure of eletriptan in Japanese male volunteers compared to western males. Population pharmacokinetic analysis of two clinical studies indicates no evidence of pharmacokinetic differences between Caucasians and non-Caucasian patients.

Menstrual Cycle: In a study of 16 healthy females, the pharmacokinetics of eletriptan remained consistent throughout the phases of the menstrual cycle.

Renal Impairment: There was no significant change in clearance observed in subjects with mild, moderate or severe renal impairment, though blood pressure elevations were observed in this population [see WARNINGS AND PRECAUTIONS].

Hepatic Impairment: Subjects with mild or moderate hepatic impairment demonstrated an increase in both AUC (34%) and half-life. The Cmax was increased by 18%. No dose adjustment is necessary in subjects with mild or moderate hepatic impairment. The effects of severe hepatic impairment on eletriptan metabolism have not been evaluated [see Use in Specific Populations].

Drug Interaction Studies

CYP3A4 inhibitors: In vitro studies have shown that eletriptan is metabolized by the CYP3A4 enzyme. A clinical study demonstrated about a 3-fold increase in Cmax and about a 6-fold increase in the AUC of eletriptan when combined with ketoconazole. The half-life increased from 5 hours to 8 hours and the Tmax increased from 2.8 hours to 5.4 hours. Another clinical study demonstrated about a 2-fold increase in Cmax and about a 4-fold increase in AUC when erythromycin was co-administered with eletriptan. It has also been shown that co-administration of verapamil and eletriptan yields about a 2-fold increase in Cmax and about a 3-fold increase in AUC of eletriptan, and that co-administration of fluconazole and eletriptan yields about a 1.4-fold increase in Cmax and about a 2-fold increase in AUC of eletriptan.

RELPAX is contraindicated within at least 72 hours of treatment with the following potent CYP3A4 inhibitors: ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir and nelfinavir. RELPAX should not be used within 72 hours with drugs that have demonstrated potent CYP3A4 inhibition [see CONTRAINDICATIONS].

Propranolol: The Cmax and AUC of eletriptan were increased by 10 and 33%, respectively, in the presence of propranolol. No interactive increases in blood pressure were observed. No dosage adjustment appears to be needed for patients taking propranolol.

The effect of eletriptan on other drugs: The effect of eletriptan on enzymes other than cytochrome P450 has not been investigated. In vitro human liver microsome studies suggest that eletriptan has little potential to inhibit CYP1A2, 2C9, 2E1 and 3A4 at concentrations up to 100 μM. While eletriptan has an effect on CYP2D6 at high concentration, this effect should not interfere with metabolism of other drugs when eletriptan is used at recommended doses. There is no in vitro or in vivo evidence that clinical doses of eletriptan will induce drug metabolizing enzymes. Therefore, eletriptan is unlikely to cause clinically important drug interactions mediated by these enzymes.

Clinical Studies

The efficacy of RELPAX in the acute treatment of migraines was evaluated in eight randomized, double-blind placebo-controlled studies. All eight studies used 40 mg. Seven studies evaluated an 80 mg dose and two studies included a 20 mg dose.

In all eight studies, randomized patients treated their headaches as outpatients. Seven studies enrolled adults and one study enrolled adolescents (age 11 to 17). Patients treated in the seven adult studies were predominantly female (85%) and Caucasian (94%) with a mean age of 40 years (range 18 to 78). In all studies, patients were instructed to treat a moderate to severe headache. Headache response, defined as a reduction in headache severity from moderate or severe pain to mild or no pain, was assessed up to 2 hours after dosing. Associated symptoms such as nausea, vomiting, photophobia and phonophobia were also assessed.

Maintenance of response was assessed for up to 24 hours post dose. In the adult studies, a second dose of RELPAX or other medication was allowed 2 to 24 hours after the initial treatment for both persistent and recurrent headaches. The incidence and time to use of these additional treatments were also recorded.

In the seven adult studies, the percentage of patients achieving headache response 2 hours after treatment was significantly greater among patients receiving RELPAX at all doses compared to those who received placebo. The two-hour response rates from these controlled clinical studies are summarized in Table 2.

Table 2: Percentage of Patients with Headache Response (Mild or No Headache) 2 Hours Following Treatment

  Placebo RELPAX 20 mg RELPAX 40 mg RELPAX 80 mg
Study 1 23.80% 54.3%* 65.0%* 77.1%*
  (n=126) (n=129) (n=117) (n=118)
Study 2 19.00% NA 61.6%* 64.6%*
  (n=232)   (n=430) (n=446)
Study 3 21.70% 47.3%* 61.9%* 58.6%*
  (n=276) (n=273) (n=281) (n=290)
Study 4 39.50% NA 62.3%* 70.0%*
  (n=86)   (n=175) (n=170)
Study 5 20.60% NA 53.9%* 67.9%*
  (n=102)   (n=206) (n=209)
Study 6 31.30% NA 63.9%* 66.9%*
  (n=80)   (n=169) (n=160)
Study 7 29.5% (n=122) NA 57.5%* (n=492) NA
* p value < 0.05 vs placebo
NA -Not Applicable

Comparisons of the performance of different drugs based upon results obtained in different clinical trials are never reliable. Because studies are generally conducted at different times, with different samples of patients, by different investigators, employing different criteria and/or different interpretations of the same criteria, under different conditions (dose, dosing regimen, etc.), quantitative estimates of treatment response and the timing of response may be expected to vary considerably from study to study.

The estimated probability of achieving an initial headache response within 2 hours following treatment is depicted in Figure 1.

Figure 1 : Estimated Probability of Initial Headache Response Within 2 Hours*

View Enlarged Table

*Figure 1 shows the Kaplan-Meier plot of probability over time of obtaining headache response (no or mild pain) following treatment with eletriptan. The plot is based on 7 placebo-controlled, outpatient trials in adults providing evidence of efficacy (Studies 1 through 7). Patients not achieving headache response or taking additional treatment prior to 2 hours were censored at 2 hours.

For patients with migraine-associated photophobia, phonophobia, and nausea at baseline, there was a decreased incidence of these symptoms following administration of RELPAX as compared to placebo.

Two to 24 hours following the initial dose of study treatment, patients were allowed to use additional treatment for pain relief in the form of a second dose of study treatment or other medication. The estimated probability of taking a second dose or other medications for migraine over the 24 hours following the initial dose of study treatment is summarized in Figure 2.

Figure 2 : Estimated Probability of Taking a Second Dose / Other Medication Over the 24 Hours Following the First Dose*

View Enlarged Table

*This Kaplan-Meier plot is based on data obtained in 7 placebo-controlled trials in adults (Studies 1 through 7). Patients were instructed to take a second dose of study medication as follows: a) in the event of no response at 2 hours (studies 2 and 4-7) or at 4 hours (study 3); b) in the event of headache recurrence within 24 hours (studies 2-7). Patients not using additional treatments were censored at 24 hours. The plot includes both patients who had headache response at 2 hours and those who had no response to the initial dose. It should be noted that the protocols did not allow re-medication within 2 hours post dose.

The efficacy of RELPAX was unaffected by the duration of attack, gender or age of the patient, relationship to menses, or concomitant use of estrogen replacement therapy/oral contraceptives or frequently used migraine prophylactic drugs.

In a single study in adolescents (n=274), there were no statistically significant differences between treatment groups. The headache response rate at 2 hours was 57% for both RELPAX 40 mg Tablets and placebo.

This monograph has been modified to include the generic and brand name in many instances.

 

Patient Information

RELPAX®
(REL -packs)
(eletriptan hydrobromide) Tablets

Please read this information before you start taking RELPAX and each time you get a refill. There may be new information. This information does not take the place of talking with your doctor about your medical condition or your treatment.

What is the most important information I should know about RELPAX?

RELPAX can cause serious side effects, including:

Heart attack and other heart problems. Heart problems may lead to death.

Stop taking REPLAX and get emergency medical help right away if you have any of the following symptoms of a heart attack:

  • discomfort in the center of your chest that lasts for more than a few minutes, or that goes away and comes back
  • chest pain or chest discomfort that feels like an uncomfortable heavy pressure, squeezing, fullness, or pain
  • pain or discomfort in your arms, back, neck, jaw, or stomach
  • shortness of breath with or without chest discomfort
  • breaking out in a cold sweat
  • nausea or vomiting
  • feeling lightheaded

REPLAX is not for people with risk factors for heart disease unless a heart exam is done and shows no problem. You have a higher risk for heart disease if you:

  • have high blood pressure
  • have high cholesterol levels
  • smoke
  • are overweight
  • have diabetes
  • have a family history of heart disease
  • are a female who has gone through menopause
  • are a male over age 40

Serotonin syndrome. Serotonin syndrome is a serious and life-threatening problem that can happen in people taking REPLAX, especially if REPLAX is taken with anti-depressant medicines called selective serotonin reuptake inhibitors (SSRIs) or selective norepinephrine reuptake inhibitors (SNRIs).

Ask your doctor or pharmacist for a list of these medicines if you are not sure.

Call your doctor right away if you have any of the following symptoms of serotonin syndrome:

  • mental changes such as seeing things that are not there (hallucinations), agitation, or coma
  • fast heartbeat
  • changes in blood pressure
  • high body temperature
  • tight muscles
  • trouble walking
  • nausea, vomiting, or diarrhea

What is RELPAX?

RELPAX is a prescription medicine used to treat acute migraine headaches with or without aura in adults.

RELPAX is for people who have been diagnosed with migraine headaches.

RELPAX is not used to prevent or decrease the number of migraine headaches you have.

It is not known if RELPAX is safe and effective to treat cluster headaches.

It is not known if RELPAX is safe and effective in children.

Who should not take RELPAX?

Do not take RELPAX if you:

  • have heart problems or a history of heart problems
  • have or have had a stroke or problems with your blood circulation
  • have hemiplegic or basilar migraines. If you are not sure if you have these types of migraines, ask your doctor
  • have narrowing of the blood vessels in your legs, arms, stomach, or kidney (peripheral vascular disease)
  • have ischemic bowel disease
  • have uncontrolled high blood pressure
  • have taken any of the following medicines in the last 24 hours:
  • other “triptans” or triptan combination products such as:
    • almotriptan (Axert® )
    • sumatriptan and naproxen sodium, (Treximet™)
    • frovatriptan (Frova™)
    • zolmitriptan (Zomig®)
    • naratriptan (Amerge®)
    • rizatriptan (Maxalt®)
    • sumatriptan (Imitrex®)
  • ergotamines such as:
    • Bellergal-S®
    • Ergomar®
    • Cafergot®
    • Wigraine®
  • dihydroergotamines such as:
    • D.H.E. 45® or Migranal® or methysergide (Sansert®)
  • have taken the following medicines within the last 72 hours:
    • ketoconazole (Nizoral®)
    • clarithromycin (Biaxin®)
    • itraconazole (Sporanox®)
    • ritonavir (Norvir®)
    • nefazodone (Serzone®)
    • nelfinavir (Viracept®)
    • troleandomycin (TAO®)
  • are allergic to eletriptan or any of the ingredients in RELPAX. See the end of this leaflet for a complete list of ingredients in RELPAX.

What should I tell my doctor before taking RELPAX?

Before you take RELPAX, tell your doctor if you:

  • have heart problems or family history of heart problems or stroke
  • have high blood pressure
  • have high cholesterol
  • have diabetes
  • smoke
  • are overweight
  • are a female who has gone through menopause
  • have kidney problems
  • have liver problems
  • are pregnant or plan to become pregnant. It is not known if RELPAX will harm your unborn baby.
  • are breastfeeding or plan to breastfeed. RELPAX passes into your breast milk and may harm your baby. Talk to your doctor about the best way to feed your baby if you take RELPAX.

Tell your doctor about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Your doctor will decide if you can take RELPAX with your other medicines. RELPAX and other medicines may affect each other causing side effects.

Especially tell your doctor if you take anti-depressant medicines called:

  • selective serotonin reuptake inhibitors (SSRIs)
  • serotonin norepinephrine reuptake inhibitors (SNRIs)

Ask your doctor or pharmacist for a list of these medicines if you are not sure. Know the medicines you take. Keep a list of them to show your doctor or pharmacist when you get a new medicine.

How should I take RELPAX?

  • Take RELPAX exactly as your doctor tell you to take it.
  • Your doctor will tell you how much RELPAX to take and when to take it.
  • Your doctor may change your dose if needed. Do not change your dose without first talking to your doctor.
  • Take 1 RELPAX tablet as soon as you feel a migraine coming on.
  • If you do not get any relief after your first RELPAX tablet, do not take a second tablet without first talking with your doctor.
  • If your headache comes back or you only get some relief from your headache, you can take a second tablet 2 hours after the first tablet.
  • Do not take more than a total of 80 mg of RELPAX tablets in a 24-hour period.
  • If you take too much RELPAX, call your doctor or go to the nearest hospital emergency room right away.
  • You should write down when you have headaches and when you take RELPAX so you can talk to your doctor about how well RELPAX is working for you.

What should I avoid while taking RELPAX?

RELPAX can cause dizziness, weakness, or drowsiness. If you have these symptoms, do not drive a car, use machinery, or do anything where you need to be alert.

What are the possible side effects of RELPAX?

RELPAX may cause serious side effects. See “What is the most important information I should know about RELPAX?”

These serious side effects include:

  • changes in color or sensation in your fingers and toes (Raynaud's syndrome)
  • stomach and intestinal problems (gastrointestinal and colonic ischemic events). Symptoms of gastrointestinal and colonic ischemic events include:
    • sudden or severe stomach pain
    • stomach pain after meals
    • weight loss
    • nausea or vomiting
    • constipation or diarrhea
    • bloody diarrhea
    • fever
  • problems with blood circulation to your legs and feet (peripheral vascular ischemia). Symptoms of peripheral vascular ischemia include:
    • cramping and pain in your legs or hips
    • feeling of heaviness or tightness in your leg muscles
    • burning or aching pain in your feet or toes while resting
    • numbness, tingling, or weakness in your legs
    • cold feeling or color changes in 1 or both legs or feet
  • medication overuse headaches. Some people who take too many RELPAX may have worse headaches (medication overuse headache). If your headaches get worse, your doctor may decide to stop your treatment with RELPAX.

The most common side effects of RELPAX include:

  • dizziness
  • nausea
  • weakness
  • tiredness
  • drowsiness

Tell your doctor if you have any side effect that bothers you or that does not go away. These are not all the possible side effects of RELPAX. For more information, ask your doctor or pharmacist. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800FDA-1088.

How should I store RELPAX?

  • Store RELPAX at room temperature between 68°F to 77°F (20°C to 25°C).

General information about the safe and effective use of RELPAX

Medicines are sometimes prescribed for conditions that are not mentioned in patient information leaflets. Do not use RELPAX for a condition for which it was not prescribed. Do not give RELPAX to other people, even if they have the same symptoms you have. It may harm them.

This Patient Information summarizes the most important information about RELPAX. If you would like more information about RELPAX, talk with your doctor. You can ask your doctor or pharmacist for information on RELPAX that is written for health professionals.

For more information, call 1-866-4RELPAX (1-866-473-5729) or go to www.RELPAX.com.

What are the ingredients in RELPAX?

Active ingredient: eletriptan hydrobromide

Inactive ingredients: microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate, titanium dioxide, hypromellose, triacetin, and FD&C Yellow No. 6 aluminum lake.

This product's label may have been updated. For current full prescribing information, please visit www.pfizer.com.

This monograph has been modified to include the generic and brand name in many instances.

 

Consumer Overview Uses

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

 

ELETRIPTAN - ORAL

 

(EL-e-TRIP-tan)

 

COMMON BRAND NAME(S): Relpax

 

USES: Eletriptan is used to treat migraines. It helps to relieve headache, pain, and other migraine symptoms (including nausea, vomiting, sensitivity to light/sound). Prompt treatment helps you return to your normal routine and may decrease your need for other pain medications. Eletriptan belongs to a class of drugs known as triptans. It affects a certain natural substance (serotonin) that causes narrowing of blood vessels in the brain. It may also relieve pain by affecting certain nerves in the brain.

Eletriptan does not prevent future migraines or lessen how often you get migraine attacks.

 

HOW TO USE: Read the Patient Information Leaflet available from your pharmacist before you start using eletriptan and each time you get a refill. If you have any questions, ask your doctor or pharmacist.

Take this medication by mouth with or without food as directed by your doctor, at the first sign of a migraine. The dosage is based on your medical condition and response to treatment. If there is no improvement in your symptoms, do not take more doses of this medication before talking to your doctor. If your symptoms are only partly relieved, or if your headache comes back, you may take another dose two hours after the first dose. For the US product, do not take more than 80 milligrams in a 24-hour period. For the Canadian product, the manufacturer recommends a maximum of 40 milligrams in a 24-hour period.

If you have a higher risk for heart problems (see Precautions), your doctor may perform a heart exam before you start taking eletriptan. He/she may also direct you to take your first dose of this medication in the office/clinic to monitor for serious side effects (such as chest pain). Talk to your doctor for details.

Overuse of drugs to treat sudden migraine attacks can sometimes lead to worsening of headache (medication overuse headache) or rebound headache. Therefore, do not use this medication more often or for longer than prescribed. Tell your doctor if you need to use this medication more often, if the medication is not working as well, or if you have more frequent or worse headaches. Your doctor may need to change your medication and/or add another medication to help prevent headaches.

Consumer Overview Side Effect

SIDE EFFECTS: Nausea, feelings of tingling/numbness, weakness, tiredness, drowsiness, or dizziness may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: blue fingers/toes/nails, cold hands/feet.

Chest/jaw/neck tightness can commonly occur soon after using eletriptan. Only rarely are these signs of a serious condition. However, you may not be able to tell it apart from a serious reaction due to a lack of blood flow to the heart, brain, or other parts of the body. Get medical help right away if you have any very serious side effects, including: chest pain, jaw/left arm pain, fainting, fast/irregular/pounding heartbeat, vision changes, weakness on one side of the body, confusion, slurred speech, sudden or severe stomach/abdominal pain, bloody diarrhea, change in the amount of urine.

This medication may increase serotonin and rarely cause a very serious condition called serotonin syndrome/toxicity. The risk increases if you are also taking other drugs that increase serotonin, so tell your doctor or pharmacist of all the drugs you take (see Drug Interactions section). Get medical help right away if you develop some of the following symptoms: fast heartbeat, hallucinations, loss of coordination, severe dizziness, severe nausea/vomiting/diarrhea, twitching muscles, unexplained fever, unusual agitation/restlessness.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

 

Read the Relpax (eletriptan hydrobromide) Side Effects Center for a complete guide to possible side effects

Learn More »

PRECAUTIONS: Before taking eletriptan, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: blood circulation problems (for example, in your legs, arms/hands, or stomach), certain types of headaches (hemiplegic or basilar migraine), heart problems (such as chest pain, irregular heartbeat, previous heart attack), liver disease, seizure, stroke or "mini-stroke" (transient ischemic attack).

Certain conditions can increase your risk for heart problems. Tell your doctor if you have any of these conditions, including: high blood pressure, high cholesterol, diabetes, family history of heart disease, overweight, smoker, postmenopausal (women), age more than 40 years (men).

This drug may make you dizzy or drowsy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Limit alcoholic beverages.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

The risk of heart disease and high blood pressure increases with age. Older adults may be more sensitive to the side effects of this drug, especially increased blood pressure and heart problems.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

This drug passes into breast milk. Consult your doctor before breast-feeding.

Consumer Overview Missed Dose

DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.

Avoid taking certain medications that can affect the removal of eletriptan from your body within 72 hours of taking eletriptan. Examples include cobicistat, nefazodone, azole antifungals such as ketoconazole/itraconazole, macrolide antibiotics such as clarithromycin/erythromycin, certain hepatitis C virus protease inhibitors such as boceprevir/telaprevir, HIV protease inhibitors such as nelfinavir/ritonavir, among others.

If you also take any ergotamine medication (such as dihydroergotamine or methysergide) or other "triptan" drugs (such as sumatriptan, rizatriptan), separate your eletriptan dose at least 24 hours apart from your dose of these other medications to lessen the chance of serious side effects.

The risk of serotonin syndrome/toxicity increases if you are also taking other drugs that increase serotonin. Examples include street drugs such as MDMA/"ecstasy," St. John's wort, certain antidepressants (including SSRIs such as fluoxetine/paroxetine, SNRIs such as duloxetine/venlafaxine), among others. The risk of serotonin syndrome/toxicity may be more likely when you start or increase the dose of these drugs.

 

OVERDOSE: If overdose is suspected, contact a poison control center or emergency room immediately. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

 

NOTES: Do not share this medication with others.

Certain foods, beverages, or food additives (such as red wine, cheese, chocolate, monosodium glutamate) as well as lifestyle patterns such as irregular eating/sleeping habits or stress may bring on a migraine headache. Avoiding these "triggers" may help lessen migraine attacks. Consult your doctor for more details.

Laboratory and/or medical tests (such as blood pressure) may be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

 

MISSED DOSE: Not applicable. (See How to Use section.)

 

STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

 

Information last revised January 2014. Copyright(c) 2014 First Databank, Inc.

Patient Detailed Side Effect

Brand Names: Relpax

Generic Name: eletriptan (Pronunciation: EL e TRIP tan)

  • What is eletriptan (Relpax)?
  • What are the possible side effects of eletriptan (Relpax)?
  • What is the most important information I should know about eletriptan (Relpax)?
  • What should I discuss with my healthcare provider before using eletriptan (Relpax)?
  • How should I use eletriptan (Relpax)?
  • What happens if I miss a dose (Relpax)?
  • What happens if I overdose (Relpax)?
  • What should I avoid while using eletriptan (Relpax)?
  • What other drugs will affect eletriptan (Relpax)?
  • Where can I get more information?

What is eletriptan (Relpax)?

Eletriptan is a headache medicine that narrows blood vessels around the brain. Eletriptan also reduces substances in the body that can trigger headache pain, nausea, sensitivity to light and sound, and other migraine symptoms.

Eletriptan is used to treat migraine headaches. Eletriptan will only treat a headache that has already begun. It will not prevent headaches or reduce the number of attacks.

Eletriptan should not be used to treat a common tension headache, a headache that causes loss of movement on one side of your body, or any headache that seems to be different from your usual migraine headaches. Use this medication only if your condition has been confirmed by a doctor as migraine headaches.

Eletriptan may also be used for purposes not listed in this medication guide.

What are the possible side effects of eletriptan (Relpax)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop using eletriptan and call your doctor at once if you have a serious side effect such as:

  • feeling of pain or tightness in your jaw, neck, or throat;
  • chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, general ill feeling;
  • sudden numbness or weakness, especially on one side of the body;
  • sudden severe headache, confusion, problems with vision, speech, or balance;
  • sudden and severe stomach pain and bloody diarrhea;
  • numbness or tingling and a pale or blue-colored appearance in your fingers or toes; or
  • (if you are also taking an antidepressant) - agitation, high fever, sweating, fast or pounding heartbeats, nausea, vomiting, diarrhea, loss of balance or coordination, overactive reflexes, hallucinations, fainting.

Less serious side effects may include:

  • mild headache (not a migraine);
  • pressure or heavy feeling in any part of your body;
  • dry mouth, upset stomach, stomach pain or cramps;
  • dizziness, drowsiness, weakness; or
  • warmth, redness, or mild tingling under your skin.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the Relpax (eletriptan hydrobromide) Side Effects Center for a complete guide to possible side effects

Learn More »

What is the most important information I should know about eletriptan (Relpax)?

You should not take this medication if you are allergic to eletriptan, if you have any history of heart disease, or if you have coronary heart disease, 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, including almotriptan (Axert), frovatriptan (Frova), naratriptan (Amerge), rizatriptan (Maxalt), sumatriptan (Imitrex, Treximet), zolmitriptan (Zomig), or ergot medicine such as ergotamine (Ergomar, Cafergot, Migergot), dihydroergotamine (D.H.E. 45, Migranal), or methylergonovine (Methergine).

Do not use eletriptan within 72 hours before or after taking ketoconazole (Extina, Ketozole, Nizoral, Xolegal), itraconazole (Sporanox), nefazodone, clarithromycin (Biaxin), ritonavir (Norvir, Kaletra), or nelfinavir (Viracept).

Before taking eletriptan, tell your doctor if you have liver or kidney disease, high blood pressure, a heart rhythm disorder, or coronary heart disease (or risk factors such as diabetes, menopause, smoking, being overweight, having 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).

Also tell your doctor if you are also taking an antidepressant such as citalopram (Celexa), desvenlafaxine (Pristiq), duloxetine (Cymbalta), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem), fluvoxamine (Luvox), paroxetine (Paxil), sertraline (Zoloft), or venlafaxine (Effexor).

Eletriptan will only treat a headache that has already begun. It will not prevent headaches or reduce the number of attacks.

After taking an eletriptan tablet, you must wait two (2) hours before taking a second tablet. Do not take more than 80 mg of eletriptan in 24 hours.

Side Effects Centers
  • Relpax

Patient Detailed How Take

What should I discuss with my healthcare provider before using eletriptan (Relpax)?

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
  • coronary heart disease (or risk factors such as diabetes, menopause, smoking, being overweight, having 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).

FDA pregnancy category C. It is not known whether eletriptan will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.

Eletriptan can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

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

How should I use eletriptan (Relpax)?

Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label. Overuse of migraine headache medicine can actually make your headaches worse.

Take eletriptan as soon as you notice headache symptoms, or after an attack has already begun.

Your doctor may want to give your first dose of this medicine in a hospital or clinic setting to see if you have any serious side effects.

Take one eletriptan tablet whole with a full glass of water.

After taking a tablet: If your headache does not completely go away, or goes away and comes back, take a second tablet two (2) hours after the first. Do not take more than 80 mg of eletriptan in 24 hours. If your symptoms have not improved, contact your doctor before taking any more tablets.

Contact your doctor if you have more than three headaches in one month (30 days).

If you use eletriptan long-term, your doctor may want to check your heart function using an electrocardiograph or ECG (sometimes called an EKG), a machine that measures electrical activity of the heart. This will help your doctor determine if it is still safe for you to use this medication. Visit your doctor regularly.

Store at room temperature away from moisture and heat.

Side Effects Centers
  • Relpax

Patient Detailed Avoid Taking

What happens if I miss a dose (Relpax)?

Since eletriptan is used as needed, it does not have a daily dosing schedule. Call your doctor promptly if your symptoms do not improve after using eletriptan.

After taking an eletriptan tablet, you must wait two (2) hours before taking a second tablet. Do not take more than 80 mg of eletriptan in 24 hours.

What happens if I overdose (Relpax)?

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

Overdose could cause high blood pressure (severe headache, blurred vision, buzzing in your ears, anxiety, confusion, chest pain, shortness of breath, uneven heartbeats, or seizure).

What should I avoid while using eletriptan (Relpax)?

Do not take eletriptan within 24 hours before or after using another migraine headache medicine, including:

  • almotriptan (Axert), frovatriptan (Frova), naratriptan (Amerge), rizatriptan (Maxalt, Maxalt-MLT), sumatriptan (Imitrex, Treximet), or zolmitriptan (Zomig); or
  • ergot medicine such as ergotamine (Ergomar, Cafergot, Migergot), dihydroergotamine (D.H.E. 45, Migranal), or methylergonovine (Methergine).

Do not use eletriptan within 72 hours before or after taking any of the following medicines:

  • ketoconazole (Extina, Ketozole, Nizoral, Xolegal), itraconazole (Sporanox);
  • nefazodone;
  • clarithromycin (Biaxin); or
  • ritonavir (Norvir, Kaletra), nelfinavir (Viracept).

Eletriptan may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

What other drugs will affect eletriptan (Relpax)?

Tell your doctor about all other medicines you use, especially:

  • conivaptan (Vaprisol);
  • imatinib (Gleevec);
  • isoniazid (for treating tuberculosis);
  • an antibiotic such as dalfopristin/quinupristin (Synercid), erythromycin (E.E.S., EryPed, Ery-Tab, Erythrocin, Pediazole), or telithromycin (Ketek);
  • an antidepressant such as citalopram (Celexa), desvenlafaxine (Pristiq), duloxetine (Cymbalta), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem), fluvoxamine (Luvox), nefazodone, paroxetine (Paxil), sertraline (Zoloft), or venlafaxine (Effexor);
  • antifungal medicine such as miconazole (Oravig) or voriconazole (Vfend);
  • heart or blood pressure medication such as diltiazem (Cartia, Cardizem), nicardipine (Cardene), quinidine (Quin-G), verapamil (Calan, Covera, Isoptin, Verelan), and others; or
  • HIV/AIDS medicine such as atazanavir (Reyataz), delavirdine (Rescriptor), fosamprenavir (Lexiva), indinavir (Crixivan), or saquinavir (Invirase).

This list is not complete and there may be other drugs that can interact with eletriptan. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.

Where can I get more information?

Your pharmacist can provide more information about eletriptan.


Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

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