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eletriptan hbr 40 mg tablet generic relpax

Out of Stock Manufacturer GREENSTONE LLC. 59762232201
Out of Stock

Uses

Vascular Headaches

Migraine

Eletriptan hydrobromide is used for the acute treatment of attacks of migraine with or without aura in adults. The manufacturer states that eletriptan should not be used for the management of hemiplegic or basilar migraine or for the prophylaxis of migraine. Safety and efficacy have not been established for the management of cluster headaches.

Efficacy of eletriptan administered at the recommended dosage of 20 or 40 mg has been evaluated for the acute treatment of migraine attacks in several randomized, placebo-controlled studies in adult outpatients with moderate to severe headaches. In these studies, 47-54 or 54-65% of patients receiving eletriptan 20 or 40 mg, respectively, achieved a response (mild to no pain) 2 hours after treatment, compared with 19-40% of patients receiving placebo. The drug also relieved manifestations of migraine other than headache (including nausea, photophobia, and phonophobia) and reduced the need for supplemental migraine therapy.

Eletriptan appears to be at least as effective as oral sumatriptan in alleviating the pain associated with migraine 2 hours after treatment. In several comparative studies, response rates 2 hours after treatment were substantially higher in patients receiving eletriptan 40 mg (64-67%) than in patients receiving sumatriptan 50 mg (50%) or 100 mg (53-59%). In another study, similar response rates were reported for eletriptan 20 or 40 mg (54 or 65%, respectively) and sumatriptan 100 mg (55%). In all comparative studies to date, sumatriptan tablets were encapsulated for the purpose of blinding, while eletriptan tablets were not. The encapsulated sumatriptan formulations were reportedly bioequivalent to conventional sumatriptan tablets; however, in another study, encapsulation of sumatriptan delayed absorption of the drug during the first 2 hours after dosing compared with conventional sumatriptan tablets. Results of a pooled analysis suggest that headache response rates 2 hours after treatment may be lower with eletriptan 20 mg than with sumatriptan 100 mg.

The US Headache Consortium considers 5-HT1B/1D receptor agonists (e.g., eletriptan) an appropriate treatment choice for the acute management of moderate to severe migraine headaches in patients without contraindications to these drugs and recommends use of 5H-T1B/1D receptor agonists, dihydroergotamine, or ergotamine in patients with more severe migraine attacks as well as in patients in whom previous therapy with nonsteroidal anti-inflammatory agents (NSAIAs) or fixed-combination preparations such as acetaminophen, aspirin, and caffeine has been ineffective.

Dosage and Administration

General

Eletriptan hydrobromide is administered orally without regard to meals. Dosage of eletriptan hydrobromide is expressed in terms of eletriptan.

Vascular Headaches

Migraine

For the acute treatment of migraine attacks with or without aura in adults, single oral eletriptan doses of 20 or 40 mg were effective in clinical studies, although the 40-mg dose was effective in a greater proportion of patients. Because individuals vary in their response to eletriptan, dosage selection should be individualized. In clinical studies, doses exceeding 40 mg were effective but were associated with an increased risk of adverse effects. The maximum single dose of eletriptan should not exceed 40 mg.

If headache recurs following an initial dose, additional doses of eletriptan may be administered at intervals of not less than 2 hours, up to a maximum adult dosage of 80 mg in any 24-hour period. However, additional doses of eletriptan are unlikely to provide benefit in patients who do not respond to the first dose of the drug for the same headache. The safety of treating an average of more than 3 headaches per 30-day period has not been established.

Special Populations

Use of eletriptan is contraindicated in patients with severe hepatic impairment. The manufacturer states that dosage adjustment is not necessary in mild to moderate hepatic impairment.

Cautions

Contraindications

Known or suspected ischemic heart disease (e.g., angina pectoris, myocardial infarction, silent ischemia), coronary vasospasm (e.g., Prinzmetal variant angina), uncontrolled hypertension, other serious underlying cardiovascular disease, cerebrovascular syndromes (e.g., stroke syndrome, transient ischemic attacks), peripheral vascular disease, or ischemic bowel disease. Basilar or hemiplegic migraine. Treatment within the previous 24 hours with another 5-HT1 receptor agonist or with an ergot alkaloid (e.g., ergotamine, dihydroergotamine, methysergide [no longer commercially available in the US]). Severe hepatic impairment (Child-Pugh grade C). Known hypersensitivity to eletriptan or any ingredient in the formulation.

Warnings/Precautions

Careful Diagnosis of Migraine

Eletriptan should be used only in patients in whom a clear diagnosis of migraine has been established. Care should be taken to exclude other potentially serious neurologic disorders before eletriptan is administered to patients not previously diagnosed with migraine or to patients who present with atypical symptoms.

Interactions with CYP3A4 Inhibitors

Eletriptan should not be used within at least 72 hours of treatment with potent inhibitors of the cytochrome P-450 (CYP) 3A4 isoenzyme (e.g., ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir). (See Drug Interactions: Drugs Affecting Hepatic Microsomal Enzymes.)

Cardiac Effects

Serious cardiac events, including acute myocardial infarction and fatal or life-threatening cardiac rhythm disturbances (e.g., ventricular tachycardia or fibrillation), have occurred within a few hours following administration of 5-HT1 receptor agonists. Myocardial ischemia/infarction or coronary vasospasm (e.g., Prinzmetal variant angina) may occur even in patients without a history of coronary artery disease. Use of eletriptan is contraindicated in patients with ischemic or vasospastic heart disease.(See Cautions: Contraindications.) Therapy with 5-HT1 receptor agonists should be discontinued if disturbances in cardiac rhythm occur.

Although sensations of tightness, pain, pressure, and heaviness in the precordium, throat, neck, and jaw occur frequently following administration of 5-HT1 receptor agonists, these sensations usually are noncardiac in origin. However, the manufacturer states that patients experiencing symptoms suggestive of angina after receiving eletriptan should be evaluated for the presence of coronary artery disease or predisposition to Prinzmetal variant angina before receiving additional doses of the drug. If administration of eletriptan is resumed and such symptoms recur, electrocardiographic evaluation should be performed.

Patients with multiple cardiovascular risk factors (e.g., postmenopausal women; men older than 40 years of age; patients with risk factors such as hypertension, hypercholesterolemia, smoking, obesity, diabetes, or family history of coronary artery disease) who have not previously received therapy with a 5-HT1 receptor agonist should undergo cardiovascular evaluation prior to initiation of 5-HT1 receptor agonist therapy. If the evaluation provides evidence of coronary artery disease or coronary artery vasospasm, the drug should not be administered. For patients with a satisfactory cardiovascular evaluation, the manufacturer states that consideration should be given to administration of the first dose in a medically supervised setting with electrocardiographic monitoring performed immediately following administration of the dose. Periodic cardiovascular evaluation is recommended for patients with risk factors for coronary artery disease who are receiving intermittent long-term therapy with 5-HT1 receptor agonists, including eletriptan.

For further information on the systematic approach to administering 5-HT1 receptor agonists in patients with risk factors for the development of coronary artery disease,

Cerebrovascular Effects

Cerebral or subarachnoid hemorrhage and stroke, sometimes fatal, have occurred in patients receiving 5-HT1 receptor agonists. In a number of cases, it appears possible that the cerebrovascular event was the primary event, and the 5-HT1 receptor agonist was administered in the mistaken belief that the patient's symptoms were caused by a migraine attack. Patients with migraine may be at increased risk for certain cerebrovascular events (e.g., stroke, hemorrhage, transient ischemic attack). Therapy with 5-HT1 receptor agonists should be discontinued in patients experiencing a cerebrovascular event.(See Cautions: Contraindications.)

Other Cardiovascular or Vasospastic Effects

Noncoronary vasospastic reactions, including peripheral vascular ischemia, GI ischemia and infarction (presenting with abdominal pain and bloody diarrhea), splenic infarction, and Raynaud's syndrome, have been reported in patients receiving 5-HT1 receptor agonists.(See Cautions: Contraindications.) Transient or permanent blindness and partial vision loss also have been reported in patients receiving 5-HT1 receptor agonists, although visual disorders may occur as manifestations of migraine attacks. Patients experiencing signs or symptoms suggestive of vasospastic reactions following administration of any 5-HT1 receptor agonist should be evaluated to rule out vasospastic reactions before receiving additional doses of eletriptan.

Substantial increases in blood pressure, including hypertensive crisis with acute impairment of organ systems, have been reported rarely following administration of 5-HT1 receptor agonists in patients with or without a history of hypertension.(See Cautions: Contraindications.) Transient increases in blood pressure have been observed following administration of eletriptan doses of 60 mg or greater and may be more pronounced in patients with renal impairment and geriatric patients.

Increases (18%) in mean pulmonary arterial pressure have been observed following administration of another 5-HT1 receptor agonist to patients with suspected coronary artery disease who were undergoing cardiac catheterization.

Serotonin Syndrome

Potentially life-threatening serotonin syndrome has been reported in patients receiving 5-HT1 receptor agonists, particularly in those receiving concomitant therapy with selective serotonin-reuptake inhibitors (SSRIs) or selective serotonin- and norepinephrine-reuptake inhibitors (SNRIs). Serotonin syndrome also may occur in patients receiving 5-HT1 receptor agonists concomitantly with monoamine oxidase (MAO) inhibitors or tricyclic antidepressants. Symptoms of serotonin syndrome 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 GI symptoms (e.g., nausea, vomiting, diarrhea). If concurrent therapy with a 5-HT1 receptor agonist and an SSRI or SNRI is clinically warranted, the patient should be observed carefully, particularly during initiation of therapy, when dosage is increased, or when another serotonergic agent is initiated. If manifestations of serotonin syndrome occur, treatment with eletriptan and any concurrently administered serotonergic agents should be discontinued and supportive and symptomatic treatment should be initiated.

Medication Overuse Headache

Excessive use of drugs indicated for the management of acute migraine attacks (e.g., use of 5-HT1 receptor agonists, ergotamine, opiates, or certain analgesic combinations on a regular basis for 10 or more days per month) may result in migraine-like daily headaches or a marked increase in the frequency of migraine attacks. Detoxification, including withdrawal of the overused drugs; treatment of withdrawal symptoms (which often include transient worsening of headaches); and consideration of prophylactic therapy for migraine attacks may be necessary.

Sensitivity Reactions

Serious allergic reactions, including angioedema, have been reported in patients receiving eletriptan.

Ocular Effects

Accumulation of eletriptan and/or its metabolites in melanin-rich tissues (such as the eye) may occur over time, resulting in potential toxicity in these tissues with extended use.

Specific Populations

Pregnancy

Category C.

Lactation

Eletriptan is distributed into human milk. Caution is advised if used in nursing women.

Pediatric Use

Safety and efficacy have not been established in children younger than 18 years of age. Eletriptan is not recommended for use in patients younger than 18 years of age.

Geriatric Use

Pharmacokinetic profile in patients 65 years of age and older is similar to that in younger adults, although half-life was increased in geriatric patients during clinical trials. No substantial differences in efficacy or safety relative to younger adults have been observed; however, there is limited clinical experience in patients 65 years of age or older. Increases in blood pressure may be more pronounced in geriatric patients.

Hepatic Impairment

Peak plasma concentrations and area under the plasma concentration-time curve (AUC) of eletriptan were increased 18 and 34%, respectively, in patients with mild to moderate hepatic impairment. Eletriptan has not been studied in patients with severe hepatic impairment; use in such patients is contraindicated.

Common Adverse Effects

Adverse effects occurring in 2% or more of patients receiving eletriptan include asthenia, headache, nausea, paresthesia, dizziness, somnolence, dry mouth, flushing or feeling of warmth, pain/pressure sensations (i.e., chest pain [tightness/pressure], abdominal pain/discomfort/stomach pain/cramps/pressure), dyspepsia, and dysphagia (i.e., throat tightness, difficulty swallowing).

Drug Interactions

Drugs Affecting Hepatic Microsomal Enzymes

Because in vitro studies have shown that eletriptan is metabolized via the cytochrome P-450 (CYP) isoenzyme 3A4, concomitant use with drugs that inhibit this enzyme (e.g., fluconazole, ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir) may increase peak plasma concentrations and area under the plasma concentration-time curve (AUC) of the drug. Administration of eletriptan within 72 hours of drugs with demonstrated potent CYP3A4 inhibition is not recommended.

In vitro studies of human liver microsomes indicate that eletriptan has little potential to inhibit or induce CYP isoenzymes 1A2, 2C9, 2E1, or 3A4; pharmacokinetic interaction is unlikely. The manufacturer states that while eletriptan has an effect on the isoenzyme CYP2D6 at high drug concentrations, such an effect should not interfere with metabolism of other drugs when eletriptan is used at recommended dosages.

Ergot Alkaloids and Other 5-HT1 Receptor Agonists

Potential pharmacologic interaction (additive vasospastic effects) when eletriptan is used concomitantly with ergot alkaloids (e.g., ergotamine, dihydroergotamine, methysergide [no longer commercially available in the US]) or other 5-HT1 receptor agonists. Use within 24 hours is contraindicated.

Monoamine Oxidase (MAO) Inhibitors

Pharmacokinetic interaction is unlikely.

Propranolol

Potential pharmacokinetic interaction (increases in the maximum plasma concentrations and AUC of eletriptan); no dosage adjustment is required.

Selective Serotonin-reuptake Inhibitors and Selective Serotonin- and Norepinephrine-reuptake Inhibitors

Potential pharmacologic interaction (potentially life-threatening serotonin syndrome). If concomitant use is clinically warranted, the patient should be observed carefully, particularly during treatment initiation, when dosage is increased, or when another serotonergic agent is initiated.(See Serotonin Syndrome under Cautions: Warnings/Precautions.)

Pharmacokinetics

Absorption

Bioavailability

Eletriptan is well absorbed after oral administration. Absolute bioavailability is approximately 50%.

Peak plasma concentrations are attained approximately 1.5 and 2 hours after oral administration in healthy adults and patients with moderate to severe migraine, respectively.

Food

High-fat meal increases AUC and peak plasma concentrations by approximately 20-30%.

Distribution

Extent

Distributed into human milk.

Plasma Protein Binding

Approximately 85%.

Elimination

Metabolism

Eletriptan is metabolized principally by CYP3A4. The N-demethylated metabolite (only known active metabolite) does not appear to contribute substantially to overall effect of parent drug.

Elimination Route

Renal clearance accounts for about 10% of total clearance.

Half-life

Approximately 4 hours.

Special Populations

In patients with mild to moderate hepatic impairment, peak plasma eletriptan concentrations and AUC are increased 18 and 34%, respectively. Eletriptan has not been studied in patients with severe hepatic impairment.

In patients with renal impairment, there are no substantial changes in clearance.

In geriatric patients, pharmacokinetic profile is similar to that in younger adults, although half-life may be increased.

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