Mechanism of effect
Selective agonist for serotonin (5-HT1B and 5-HT1D receptors) in cranial arteries; causes vasoconstriction and reduces sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine.
Pharmacokinetics
Half-life: 26 hr
Peak plasma time: 2-4 hr
Metabolism: CYP1A2
Distribution: 4.2 L/kg (male); 3 L/kg (female)
Protein binding: 15%
Bioavailability: 20% (male); 30% (female)
Excretion: Feces (62%); urine (32%)
Drug indications
Dosage
2.5 mg PO at onset; may repeat once after 2 hr
Not to exceed 7.5 mg/day
Drug contraindications
-Hypersensitivity, severe hepatic or renal impairment, migraine prophylaxis
-Ischemic heart disease, uncontrolled HTN, hemiplegic or basilar migraines, cluster headache, cerebrovascular syndromes, PVD
-Do not use within 24 hr of another 5-HT1 agonist or ergot derivative, or within 2 weeks of MAOIs
Side effects
Flushing , hot or cold flashes , chest pain , palpitations, Dizziness , fatigue ,headache , paresthesia , drowsiness , anxiety , dysesthesia , hypoesthesia , insomnia , pain, Diaphoresis ,Xerostomia , nausea , dyspepsia , abdominal pain , diarrhea , vomiting, Musculoskeletal pain, Visual disturbance, Tinnitus ,Rhinitis , sinusitis
Interactions
Ergotamine-C , Sibutramine , Tapentadol , Almotriptan , Dolasetron , Palonosetron , Lorcaserin , Desvenlafaxine , Dexfenfluramine , Levomilnacipran , 5-hydroxytryptophan , Droxidopa , NetupitantDroxidopa ,Ergot Derivatives ,Monoamine Oxidase Inhibitors ,Serotonergic Agents ,SUMAtriptan
Alerts
-Serious cardiac and cerebrovascular events, including cerebral hemorrhage, subarachnoid hemorrhage, stroke, acute MI, arrhythmias, and death reported within a few hours after administration
-Chest discomfort and jaw or neck tightness reported infrequently following intranasal administration
-Serotonin syndrome may occur, particularly when coadministered with SSRIs
-Not for use with unrecognized Coronary artery disease as predicted by risk factors (eg, hypertension, hypercholesterolemia, smoking, obesity, diabetes, strong family history of CAD, female with surgical or physiological menopause, male aged >40 yr)
-Use with caution in severe impairment
-Partial vision loss and blindness have been reported with use of 5-HT1 agonists
-Vasospasm-related events
Points of recommendation
-Clear diagnosis of migraine headache must be established
-Overuse of acute migraine drugs (eg, ergotamine, triptans, opioids, or combination of these drugs for ≥10 days/month) may lead to exacerbation of headache (medication overuse headache)
-May increased blood pressure, monitor
Pregnancy level
HAVE NOT BEEN ESTABLISHEDThere are no adequate data on developmental risk associated with use in pregnant women. Published data have suggested that women with migraines may be at increased risk of preeclampsia during pregnancy.
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