ELETRIPTAN HYDROBROMIDE
Clinical safety rating
avoidContraindicated (not allowed)
Selective 5-HT1B/1D receptor agonist; causes vasoconstriction of cranial arteries and inhibition of trigeminal nerve transmission.
| Metabolism | Primarily metabolized by CYP3A4; also minor contribution from CYP2C9, CYP2C19, and CYP2D6. |
| Excretion | Approximately 90% of the dose is eliminated in feces, with less than 10% recovered in urine. Renal excretion accounts for about 9% of total clearance, primarily as unchanged drug. Biliary/fecal elimination is the major route. |
| Half-life | Terminal elimination half-life is approximately 4-5 hours in healthy adults. In patients with hepatic impairment, half-life may be prolonged up to 8 hours. The half-life supports a clinical duration suitable for acute migraine treatment, with no accumulation with single doses. |
| Protein binding | Approximately 85% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is approximately 1.4 L/kg (range 1.0-2.0 L/kg), indicating extensive distribution into tissues beyond total body water. |
| Bioavailability | Oral bioavailability is approximately 50% (range 30-70% due to first-pass metabolism) for the tablet formulation. Absolute bioavailability is moderate due to presystemic clearance. |
| Onset of Action | Oral: Onset of clinical effect occurs within 30-60 minutes post-dose, with peak plasma concentrations reached at approximately 1.5-2 hours. Maximum clinical benefit may not be achieved until 2-4 hours. |
| Duration of Action | Duration of clinical effect is approximately 24 hours for headache relief, but the therapeutic effect can persist up to 48 hours in some patients. Recurrence within 24 hours may occur and requires re-dosing. |
| Molecular Weight | 382.48 |
40 mg orally once, may repeat after 2 hours if headache recurs; maximum 80 mg/day.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment; contraindicated in severe renal impairment (CrCl <10 mL/min). |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh C); no adjustment for mild to moderate impairment. |
| Pediatric use | Not established; safety and efficacy in patients <18 years not studied. |
| Geriatric use | Use with caution due to potential decreased hepatic/renal function; consider lower starting dose (20 mg). |
| 1st trimester | Insufficient human data; animal studies show reproductive toxicity. Avoid unless clearly needed. |
| 2nd trimester | Insufficient human data; potential for uterine vasoconstriction. Use only if benefit outweighs risk. |
| 3rd trimester | Insufficient human data; potential for uterine vasoconstriction and preterm labor. Avoid near term. |
Clinical note
Strong CYP3A4 inhibitors (eg ketoconazole) are contraindicated due to increased risk of coronary vasospasm Contraindicated in ischemic heart disease and uncontrolled hypertension.
| Placental transfer | Eletriptan crosses the placenta based on animal studies; human data limited. |
| Breastfeeding | Eletriptan is excreted into human breast milk in low amounts (relative infant dose <5%). No adverse effects reported in infants. Caution, especially in preterm or neonates. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | Limited human data; animal studies show no teratogenicity at clinically relevant doses. First trimester: risk cannot be excluded; second/third trimester: no known increased risk. Avoid in third trimester due to possible uterine atony or decreased placental perfusion. |
| Fetal Monitoring | Monitor blood pressure and heart rate in mother; fetal heart rate monitoring for signs of bradycardia or distress if used near term. Assess for signs of serotonin syndrome if combined with other serotonergic drugs. |
| Fertility Effects | No known adverse effects on fertility in animal studies; no human data. Theoretical risk of decreased uterine perfusion with vascular mechanism. |
■ FDA Black Box Warning
No FDA boxed warning.
| Common Effects | Chest pain |
| Serious Effects |
Hypersensitivity to eletriptan or any excipientIschemic heart disease (angina, history of MI, silent ischemia)Coronary artery vasospasm (Prinzmetal's angina)Uncontrolled hypertensionHemiplegic or basilar migraineWithin 24 hours of another triptan, ergotamine, or ergot-type medicationConcomitant use with MAO-A inhibitors or within 2 weeks of discontinuationSevere hepatic impairment (Child-Pugh C)
| Precautions | Coronary artery vasospasm and ischemic heart disease, Cerebrovascular events (stroke, transient ischemic attack), Life-threatening serotonin syndrome (especially with SSRIs/SNRIs), Hypertensive crisis in patients with uncontrolled hypertension, Risk of myocardial ischemia in patients with risk factors |
| Food/Dietary | Grapefruit and grapefruit juice should be avoided as they inhibit CYP3A4, increasing eletriptan exposure and risk of adverse effects. No other significant food interactions reported. |
| Clinical Pearls | Eletriptan has higher lipophilicity and longer half-life than sumatriptan, potentially offering better CNS penetration and sustained efficacy. Contraindicated within 24 hours of other triptans or ergotamines. Avoid in patients with severe hepatic impairment (Child-Pugh C) as metabolism is CYP3A4-dependent. Maximum single dose 40 mg; may repeat after 2 hours if no response, but do not exceed 80 mg/day. Onset typically within 30 minutes; if first dose fails, consider alternative therapy for subsequent attacks. |
| Patient Advice | Take at the first sign of migraine headache, not for prevention. · Do not take more than 80 mg in 24 hours; wait at least 2 hours between doses. · Avoid taking within 24 hours of other triptans or ergotamine medications. · Report chest pain, palpitations, or shortness of breath immediately. · Do not use if you have uncontrolled high blood pressure, coronary artery disease, or history of stroke. · Grapefruit juice may increase drug levels; avoid consumption during treatment. · Swallow tablet whole; do not crush or chew. |
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