five ht1 agonists
Controlled Substance Schedule: V
Acute treatment of migraine with or without aura.
Acts as a selective agonist of 5-HT1F receptors, which decreases stimulation of the trigeminal system (without causing vasoconstriction).
Relief of pain associated with acute migraine attacks.
Absorption: Rapidly absorbed. Absorption delayed by high-fat food.
Metabolism and Excretion: Primarily metabolized by hepatic and non-hepatic pathways (by non-CYP enzymes) to inactive metabolites. Primarily excreted in urine as metabolites.
Half-life: 5.7 hr.
TIME/ACTION PROFILE (pain relief)
|PO||30–60 min||2 hr||up to 24 hr|
- Severe hepatic impairment.
Use Cautiously in:
- History of substance abuse;
- OB: Use during pregnancy only if potential maternal benefit outweighs potential fetal risk;
- Lactation: Use while breast feeding only if potential maternal benefit outweighs potential risk to infant;
- Pedi: Safety and effectiveness not established in children;
- Geri: Use lowest dose possible in older adults (↑ risk for sedation and BP elevation).
Adverse Reactions/Side Effects
CV: ↓ heart rate, ↑ BP
GI: nausea, vomiting
MS: muscle weakness
Neuro: paresthesia, dizziness, drowsiness
Misc: HYPERSENSITIVITY REACTIONS (including angioedema), SEROTONIN SYNDROME, fatigue
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
- Use with other CNS depressants, including benzodiazepines, sedative/hypnotics, anxiolytics, opioids, or alcohol may cause profound sedation; avoid concurrent use.
- ↑ risk of serotonin syndrome with SSRIs, SNRIs, TCAs, MAOIs, dextromethorphan, triptans, trazodone, meperidine, bupropion, or buspirone.
- Concurrent use with beta blockers, diltiazem, verapamil, digoxin, clonidine, or ivabradine may result in further ↓ in heart rate; use concomitantly with caution.
- May ↑ levels and risk of toxicity of P-glycoprotein substrates or breast cancer resistant protein (BCRP) substrates ; avoid concurrent use.
↑ risk of serotonin syndrome with St. John's wort or SAMe .
PO (Adults): 50 mg, 100 mg, or 200 mg as a single dose (not to exceed one dose/24 hr).
Tablets: 50 mg, 100 mg
- Assess pain location, intensity, duration, and associated symptoms (photophobia, phonophobia, nausea, vomiting) during migraine attack.
- Assess for occurrence of signs and symptoms of serotonin syndrome periodically during therapy.
- Acute pain (Indications)
- PO Administer without regard to food. Do not administer >1 dose/24 hr; a 2nd dose for same migraine is not effective.
- Instruct patient to take lasmiditan as directed and not take more than 1 dose in 24 hr. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
- Inform patient that lasmiditan should be used only during a migraine attack. It is meant to be used for relief of migraine attacks but not to prevent or reduce the number of attacks.
- Advise patient that lying down in a darkened room after lasmiditan administration may further help relieve headache.
- May cause dizziness and drowsiness. Caution patient to avoid driving or other activities requiring alertness for at least 8 hr after dose. Do not take lasmiditan if unable to follow this advice.
- Advise patient to notify health care professional if signs and symptoms of serotonin syndrome (mental status changes [agitation, hallucinations, coma], autonomic instability [tachycardia, labile blood pressure, hyperthermia], neuromuscular signs [hyperreflexia, incoordination], gastrointestinal [nausea, vomiting, diarrhea] occur. Discontinue lasmiditan if symptoms occur. Concurrent use of SSRIs, SNRIs, TCAs, MAO inhibitors, trazodone, triptans, cough syrups (dextromethorphan) or herbal products (St. John's Wort, SAMe) increase serotonin and may cause serotonin syndrome.
- Advise patient that overuse of acute migraine drugs (use more than 10 days/mo) may lead to exacerbation of headache (migraine-like daily headaches, or as a marked increase in frequency of migraine attacks). May require gradual withdrawal of lasmiditan and treatment of symptoms (transient worsening of headache).
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially St. John's Wort.
- Advise patient to avoid taking other CNS depressants and alcohol, which aggravates headaches and may cause profound sedation, during lasmiditan use.
- Advise patient that lasmiditan is a drug with known abuse potential. Protect it from theft, and never give to anyone other than the individual for whom it was prescribed. Store out of sight and reach of children, and in a location not accessible by others.
- Advise patient to notify health care professional if pregnancy is planned or suspected or if breast feeding.
Relief of migraine attack.
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