Eletriptan Hbr (eletriptan hydrobromide)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Eletriptan hydrobromide is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors (''triptan'').
Eletriptan hydrobromide is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors. Eletriptan is structurally and pharmacologically related to other selective 5-HT1B/1D receptor agonists (e.g., almotriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan, zolmitriptan). Because the mechanisms involved in the pathogenesis of migraine are not clearly understood, the precise mechanism of action of 5-HT1 receptor agonists in the management of migraine has yet to be established.
However, current data suggest that 5-HT1 receptor agonists, including eletriptan, may ameliorate migraine through selective constriction of certain intracranial blood vessels, inhibition of neuropeptide release, and/or reduced transmission in the trigeminal pain pathway.
Eletriptan is well absorbed following oral administration. Peak plasma concentrations are achieved in approximately 1.5 and 2 hours in healthy adults and patients with moderate to severe migraine, respectively. A high-fat meal increases AUC and peak plasma concentrations by approximately 20-30%.
Eletriptan is distributed into human milk. Plasma protein binding of the drug is approximately 85%.
In vitro, eletriptan is metabolized principally by cytochrome P-450 (CYP) isoenzyme 3A4. Since plasma concentrations of the N-demethylated metabolite, the only active metabolite identified for eletriptan, generally are only about 10-20% of the parent drug, the metabolite does not appear to contribute substantially to the overall effect of the parent drug. The elimination half-life of eletriptan is approximately 4 hours.
Renal clearance accounts for about 10% of total clearance of eletriptan.
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.
Generic name: eletriptan hydrobromide
Pronunciation: (EL-e-TRIP-tan)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Eletriptan Hbr
Indications
The following indications are listed for Eletriptan Hbr:
- Migraine
Dosing
Available as eletriptan hydrobromide; dosage is expressed in terms of eletriptan.
Eletriptan is available in a tablet formulation for oral administration. Eletriptan may be administered without regard to meals.
Tablets should be stored at 20-25degreesC with excursions permitted between 15-30degreesC.
No dosing information is available for this tab.
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Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Ischemic coronary artery disease (e.g., angina pectoris, history of myocardial infarction, documented silent ischemia), coronary artery vasospasm (e.g., Prinzmetal variant angina), or uncontrolled hypertension.
*Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders.
*Cerebrovascular syndromes (e.g., history of stroke, transient ischemic attack, or history or current evidence of hemiplegic or basilar migraine), peripheral vascular disease, or ischemic bowel disease.
*Recent (i.e., 24 hours or less) treatment with another 5-HT1 receptor agonist or an ergotamine-containing or ergot-type drug.
*Recent (i.e., 72 hours or less) use of the following strong CYP3A4 inhibitors: ketoconazole, itraconazole, nefazodone, clarithromycin, ritonavir, or nelfinavir.
*Known hypersensitivity to eletriptan; angioedema and anaphylaxis reported.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse reactions (incidence >=5% and greater than placebo) with eletriptan include asthenia, nausea, dizziness, and somnolence.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy have not been established in pediatric patients younger than 18 years of age. In a study involving 274 adolescents (11-17 years of age), the headache response rate at 2 hours for eletriptan 40 mg was not different from placebo (57% for both groups). Adverse reactions in the study were similar to those observed in adults.
There are insufficient human data on the use of eletriptan in pregnancy to determine a drug-associated risk for major birth defects and miscarriage. In animal reproductive studies, eletriptan was associated with developmental toxicity (e.g., reduced fetal and pup weights, increased fetal structural abnormalities, decreased pup viability) when administered during the period of pregnancy and lactation at clinically relevant doses.
Linked data from the Medical Birth Registry of Norway to the Norwegian Prescription Database revealed that of 189 women who redeemed an eletriptan prescription during the first trimester of pregnancy, 4 gave birth to infants with major congenital malformations while 11 infants with major congenital malformations were born to 174 women who redeemed an eletriptan prescription before, but not during, pregnancy.
Eletriptan is distributed into human milk; the effects of eletriptan on the breastfed infant or milk production are unknown. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for eletriptan and any adverse effects on the breastfed infant from the drug or from the underlying maternal condition. Infant exposure to eletriptan can be minimized by avoiding breastfeeding for 24 hours after treatment.
No specific dosage adjustment is recommended in geriatric patients.
Pharmacokinetic profile in patients 65 years of age and older is similar to that in younger adults. No apparent differences in efficacy or safety relative to younger adults have been observed in clinical trials. Increases in blood pressure are more pronounced in geriatric patients.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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