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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Relpax
Generic Name
Eletriptan Hydrobromide
Active Ingredient
EletriptanCategory
Other
Salt Form
Hydrobromide
Variants
4
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Relpax, you must consult a qualified healthcare professional.
| 40 mg/1 | TABLET | ORAL | 58151-368 |
Detailed information about Relpax
Eletriptan is a second-generation selective serotonin (5-HT1B/1D) receptor agonist, commonly known as a 'triptan,' indicated for the acute treatment of migraine with or without aura in adults. It works by inducing cranial vasoconstriction and inhibiting neurogenic inflammation.
The standard recommended starting dose for Eletriptan in adults is either 20 mg or 40 mg, taken at the first sign of a migraine headache. Clinical data suggests that the 40 mg dose may provide a higher rate of response, but it also carries a slightly higher risk of transient side effects. If the migraine returns after an initial response, a second dose may be taken, but it must be at least two hours after the first dose.
If the first dose of Eletriptan does not provide any relief, a second dose should not be taken for the same attack, as it is unlikely to be effective. In such cases, patients should contact their healthcare provider to discuss alternative treatments.
Eletriptan is currently not approved for use in pediatric patients (children and adolescents under the age of 18). Clinical trials in adolescent populations (ages 12 to 17) failed to demonstrate a statistically significant difference between Eletriptan and placebo, likely due to a high placebo response rate common in pediatric migraine trials. Consequently, its safety and efficacy in this demographic have not been established.
No dosage adjustment is generally required for patients with mild to moderate renal impairment. However, because Eletriptan can increase blood pressure, caution is advised in patients with significant kidney disease. Eletriptan should be used with extreme caution, if at all, in patients with severe renal impairment.
For patients with mild to moderate hepatic impairment (Child-Pugh Categories A and B), the metabolism of Eletriptan may be slowed, but specific dose reductions are not always mandated. However, Eletriptan is contraindicated in patients with severe hepatic impairment (Child-Pugh Category C) because the drug is extensively metabolized by the liver, and blood levels could reach toxic concentrations.
Clinical studies of Eletriptan did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently than younger subjects. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range (20 mg), reflecting the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy.
Eletriptan should be taken as soon as the migraine symptoms begin. It can be taken with or without food. The tablet should be swallowed whole with a full glass of water or other liquid. Do not crush, chew, or split the tablet, as this may affect the rate of absorption and the efficacy of the medication.
Storage is also vital; Eletriptan should be kept at room temperature (20°C to 25°C or 68°F to 77°F) in its original blister pack or container to protect it from moisture. Keep the medication out of reach of children and pets.
Eletriptan is taken only as needed for acute migraine attacks. It is not a daily medication. If you have a migraine and forget to take your dose, take it as soon as you remember. However, if you do not have a migraine, do not take a dose to 'prevent' a future attack. Never take two doses at once to make up for a missed one.
Signs of an Eletriptan overdose may include severe hypertension (high blood pressure), tachycardia (rapid heartbeat), chest pain, or other cardiovascular disturbances. Because Eletriptan has a half-life of 4 hours, monitoring for at least 20 hours is generally required following a significant overdose. There is no specific antidote for Eletriptan. In the event of an overdose, seek emergency medical attention immediately or contact a poison control center. Treatment is supportive, often involving gastric lavage and cardiovascular monitoring.
> Important: Follow your healthcare provider's dosing instructions strictly. Do not adjust your dose or frequency of use without medical guidance, as overusing triptans can lead to medication overuse headaches.
While Eletriptan is generally well-tolerated, some patients may experience mild to moderate side effects. The most frequently reported adverse reactions include:
Eletriptan is a potent vasoconstrictor and must be used with extreme caution. It is not a medication for 'everyday' headaches and should only be used when a clear diagnosis of migraine has been established by a healthcare professional. Before starting Eletriptan, patients must undergo a thorough medical history screening, particularly regarding cardiovascular health.
There are no FDA black box warnings for Eletriptan. However, the clinical warnings regarding its use in patients with undiagnosed coronary artery disease (CAD) are of paramount importance.
Eletriptan has several critical drug-drug interactions that can lead to life-threatening complications:
Eletriptan must NEVER be used in patients with the following conditions:
Eletriptan is classified under the former FDA Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Animal studies have shown developmental toxicity (decreased fetal body weight and increased incidences of skeletal variations) at doses that were also maternally toxic. Eletriptan should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. If you are pregnant or planning to become pregnant, discuss alternative migraine management strategies with your obstetrician and neurologist.
Eletriptan is excreted in human breast milk. In a study of 8 women, the average total amount of drug excreted in milk over 24 hours was approximately 0.02% of the dose. While this is a small amount, the effects on the nursing infant are not fully known. To minimize exposure, some healthcare providers suggest waiting 24 hours after taking a dose before resuming breastfeeding, during which time milk can be expressed and discarded.
Safety and effectiveness in pediatric patients under 18 years of age have not been established. As previously mentioned, clinical trials in adolescents did not show a benefit over placebo. Use in children is generally discouraged unless specifically directed by a pediatric neurologist in a specialized setting.
Eletriptan is a selective agonist for the 5-HT1B, 5-HT1D, and 5-HT1F serotonin receptors. It has very little affinity for 5-HT2, 5-HT3, or alpha-adrenergic, dopaminergic, or muscarinic receptors. Its primary action is to bind to 5-HT1B receptors on intracranial blood vessels, causing them to constrict. Simultaneously, it binds to 5-HT1D receptors on the sensory nerve endings of the trigeminal system, which inhibits the release of pro-inflammatory neuropeptides. This dual action addresses both the vascular and neural components of a migraine attack.
The onset of action for Eletriptan is approximately 30 to 60 minutes, with peak effects occurring around 2 hours. The duration of effect is typically sufficient to cover the length of a standard migraine attack, though recurrence can occur in some patients within 24 hours. Eletriptan does not appear to cause significant tolerance when used occasionally, but frequent use can lead to the downregulation of serotonin receptors, contributing to medication overuse headache.
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Common questions about Relpax
Eletriptan is a prescription medication specifically used for the acute treatment of migraine headaches with or without aura in adults. It is not intended to prevent migraines or to treat other types of headaches, such as tension headaches or cluster headaches. As a member of the triptan class, it works by narrowing blood vessels around the brain and stopping pain signals from being sent. It should only be taken once a migraine attack has already started. Your doctor will determine if your headache patterns are appropriate for this specific type of therapy.
The most common side effects reported by patients taking Eletriptan include dizziness, drowsiness, nausea, and a feeling of weakness or tiredness (asthenia). Some people also experience a dry mouth or a sensation of tightness and pressure in the chest and throat. These side effects are usually mild and temporary, often resolving as the medication wears off. However, if you experience severe chest pain, shortness of breath, or signs of an allergic reaction, you must seek emergency medical help immediately. Always discuss any persistent side effects with your healthcare provider.
It is generally advised to avoid drinking alcohol while taking Eletriptan. Alcohol is a common trigger for migraines and can worsen the headache you are trying to treat. Additionally, both alcohol and Eletriptan can cause drowsiness and dizziness; combining them can significantly impair your coordination and judgment. This increases the risk of falls or accidents and can make the sedative side effects of the medication much more intense. For the best results in treating your migraine, it is safest to stay hydrated with water and avoid alcohol during and immediately after an attack.
The safety of Eletriptan during pregnancy has not been fully established, as there are no adequate clinical trials in pregnant women. Animal studies have suggested that high doses may cause some harm to the developing fetus, particularly when the mother also experiences toxicity. Therefore, Eletriptan is typically only prescribed during pregnancy if the potential benefits clearly outweigh the potential risks. If you are pregnant, think you might be pregnant, or are planning to conceive, you should consult your doctor to discuss the safest options for managing your migraines. Many doctors prefer using older, better-studied treatments during pregnancy.
Most patients begin to feel relief from their migraine symptoms within 30 to 60 minutes after taking Eletriptan. The medication reaches its peak concentration in the bloodstream approximately 1.5 to 2 hours after it is swallowed. Clinical trials have shown that a significant number of patients achieve 'headache response' (pain reducing to mild or none) by the two-hour mark. If your symptoms do not improve at all after the first dose, do not take a second dose for the same attack; instead, contact your doctor. If the headache initially goes away but then returns, you may take a second dose after at least two hours.
Since Eletriptan is taken only as needed for acute migraine attacks and not as a daily preventive medication, there is no risk of traditional withdrawal symptoms from stopping it. You can stop using it whenever you choose if you no longer have migraines. However, if you have been using Eletriptan very frequently (more than two days a week), stopping it might lead to a temporary increase in headaches known as 'rebound' or medication overuse headaches. In this situation, you should work with your doctor to gradually reduce your usage and start a preventive treatment plan to manage your migraines more effectively.
Because Eletriptan is an 'as-needed' medication for the treatment of an active migraine, you cannot 'miss' a dose in the way you would with a daily pill. If you have a migraine and forget to take your medication, you can take it as soon as you remember, provided the migraine is still occurring. However, you should never take a dose of Eletriptan if you do not have a migraine headache, as it will not prevent a future one from starting. Always ensure there is at least a two-hour gap between doses and never exceed 80 mg in a 24-hour period.
Weight gain is not a recognized or common side effect of Eletriptan. Clinical trials and post-marketing surveillance have not shown a link between the occasional use of triptans and changes in body weight. If you are experiencing weight gain while taking Eletriptan, it may be due to other factors, such as lifestyle changes caused by frequent migraines, or other medications you may be taking for migraine prevention (some of which, like certain antidepressants or anti-seizure meds, are known to cause weight changes). If you have concerns about your weight, you should discuss them with your healthcare provider to identify the underlying cause.
Eletriptan can interact with several other medications, some of which are very dangerous. It must not be taken within 72 hours of potent CYP3A4 inhibitors, such as certain antibiotics (clarithromycin), antifungals (ketoconazole), or HIV protease inhibitors. It also should not be used within 24 hours of other triptans or ergot-type medications. There is also a risk of serotonin syndrome if taken with SSRI or SNRI antidepressants. Because of these complex interactions, it is vital that you provide your doctor with a complete list of all prescription drugs, over-the-counter medicines, and herbal supplements you are currently taking.
Yes, Eletriptan is available as a generic medication (Eletriptan Hydrobromide). The generic version became available after the patent for the brand-name drug, Relpax, expired. Generic Eletriptan is required by the FDA to have the same active ingredient, strength, dosage form, and route of administration as the brand-name version. It must also prove bioequivalence, meaning it works in the body in the same way and over the same amount of time. Choosing the generic version can often be a more cost-effective way to manage migraine treatment while receiving the same clinical benefits as the brand-name drug.
Other drugs with the same active ingredient (Eletriptan)
These effects occur in a smaller percentage of the population but are still documented in clinical literature:
Rare but documented side effects include:
> Warning: Stop taking Eletriptan and call your doctor immediately or seek emergency care if you experience any of the following:
The primary concern with long-term, frequent use of Eletriptan is Medication Overuse Headache (MOH). If Eletriptan is used for 10 or more days per month, it can actually cause headaches to become more frequent and more severe. This creates a cycle of dependency and chronic daily headache. Patients should track their usage and report frequent migraine recurrence to their doctor to discuss preventative therapies.
No FDA black box warnings are currently issued for Eletriptan. However, the FDA mandates a 'Warnings and Precautions' section regarding serious cardiovascular, cerebrovascular, and vasospastic reactions. These warnings are considered 'class warnings' for all triptan medications.
Report any unusual symptoms to your healthcare provider. If you experience side effects, you may also report them to the FDA at 1-800-FDA-1088.
For most healthy patients, routine lab tests are not required specifically for Eletriptan use. However, for those with underlying conditions, the following may be monitored:
Eletriptan commonly causes somnolence (drowsiness) and dizziness. Migraine itself often causes cognitive impairment and light sensitivity. Therefore, patients are strongly advised not to drive, operate heavy machinery, or engage in hazardous activities until the migraine has resolved and the effects of the medication have worn off.
Alcohol is a known migraine trigger for many individuals. Furthermore, alcohol can increase the sedative effects of Eletriptan, leading to profound drowsiness or impaired coordination. It is generally recommended to avoid alcohol consumption during a migraine attack and while Eletriptan is in your system.
There is no physical 'withdrawal' syndrome associated with stopping Eletriptan if it is used occasionally as prescribed. However, if the drug has been overused (leading to Medication Overuse Headache), stopping the drug may cause a temporary 'rebound' increase in headache frequency. In such cases, a doctor-supervised tapering schedule or a 'bridge' therapy with other medications may be necessary.
> Important: Discuss all your medical conditions, especially heart, liver, or kidney problems, with your healthcare provider before starting Eletriptan.
Eletriptan is not known to interfere significantly with common clinical laboratory tests. However, always inform your laboratory technician and doctor about all medications you are taking.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking. The 72-hour rule for CYP3A4 inhibitors is a critical safety requirement.
These conditions require a careful risk-benefit analysis by a physician:
Patients who have had an anaphylactic or severe allergic reaction to other triptans (like sumatriptan or rizatriptan) may have a cross-sensitivity to Eletriptan. While the chemical structures differ slightly, the pharmacological class is the same, and caution is warranted.
> Important: Your healthcare provider will evaluate your complete medical history, including a possible 'stress test' for your heart, before prescribing Eletriptan.
Patients over the age of 65 are at a higher risk for cardiovascular events, including hypertension and ischemic heart disease. Pharmacokinetic studies have shown that the half-life of Eletriptan may be slightly longer in the elderly (about 5-6 hours vs. 4 hours in younger adults). Because of the increased risk of side effects and underlying health conditions, Eletriptan is often avoided in the geriatric population in favor of safer alternatives.
In patients with mild to moderate renal impairment, the AUC of Eletriptan is slightly increased, but not to a degree that requires routine dose adjustment. However, because the drug can increase blood pressure, patients with renal disease should have their blood pressure monitored closely. Eletriptan should be avoided in patients with severe renal failure requiring dialysis.
The liver is the primary site of Eletriptan metabolism. In subjects with moderate hepatic impairment, the AUC and half-life are increased. While no dose adjustment is strictly required for mild-to-moderate impairment, the drug is contraindicated in severe hepatic impairment (Child-Pugh C).
> Important: Special populations require individualized medical assessment. Always inform your doctor if you fall into any of these categories before taking your first dose.
| Bioavailability | ~50% |
| Protein Binding | ~85% |
| Half-life | ~4 hours |
| Tmax | 1.5 - 2 hours |
| Metabolism | Hepatic (CYP3A4) |
| Excretion | Fecal (~81%), Renal (~9%) |
Eletriptan belongs to the 'Triptan' class of medications (selective 5-HT1B/1D receptor agonists). Related medications include sumatriptan (Imitrex), rizatriptan (Maxalt), zolmitriptan (Zomig), naratriptan (Amerge), almotriptan (Axert), and frovatriptan (Frova). Among these, Eletriptan is noted for its high potency and relatively fast onset of action.