almotriptan (Rx)

1-10%

Somnolence (1-5%)

Dizziness (3-4%)

Nausea (1-3%)

Vomiting (2%)

Dry mouth (1-2%)

Headache (1-2%)

Nausea (1-2%)

Paresthesia (1-2%)

Paresthesia (1%)

Somnolence (>1%)

<1%

Infrequent (0.01-0.001%)

• Anxiety, asthenia, chills, CNS stimulation, fatigue, hypesthesia, tremor
• Pruitus, rash
• Diaphoresis, dysmenorrhea, hyperglycemia, increased thirst
• Abdominal cramp, gastroenteritis
• Back pain, myalgia, neck pain, rigid neck, Increased CPK
• Bronchitis, chest pain, dyspnea, pharyngitis, rhinitis, sinusitis
• Conjunctivitis, tinnitis, vertigo

Rare (<0.001%)

• Hypertension, syncope
• Fever, insomnia, nervousness, nightmares
• Erythema, photosensitivity
• Colitis, esophegeal reflux, gastritis
• Arthralgia, arthritis, muscle weakness, myopathy
• Laryngitis, sneezing
• Eye abnormalities, nystagmus
• Hypercholesteremia, hyperventilation, increased gamma glutamyl transpeptidase, increased salvation

Postmarketing Experience

Hypersensitivity reactions (including angioedema, anaphylactic reactions and eye disorders including visual impairment, vision blurred) reported

Contraindications

Hypersensitivity, severe hepatic or renal impairment, migraine prophylaxis

Ischemic heart disease, uncontrolled HTN, hemiplegic or basilar migraines, cluster HA, cerebrovascular syndromes, PVD

Do not use within 24 hr of another 5-HT1 agonist or ergot derivative, or within 2 weeks of MAOIs

Cautions

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); detoxification of patients, including withdrawal of overused drugs, and treatment of withdrawal symptoms (often includes a transient worsening of headache) may be necessary

After dose is administered, patients who experience angina symptoms or chest pain, pressure, and tightness, should be evaluated for coronary artery disease or Prinzmetal's angina before receiving additional doses

Hemorrhage and stroke have been reported with 5-HT1 agonist administration

Significant increase in blood pressure has been reported with 5-HT1 agonists

Transient and permanent blindness and partial vision loss have been reported with 5-HT-1 agonisits

Serotonin syndrome may develop if administered concomitantly with proserotonergic drugs

Pregnancy Category: C

Lactation: excretion in milk unknown; use with caution

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Selective 5-HT1 receptor agonist in cranial arteries. Causes vasoconstriction and reduces inflammation associated with antidronic neuronal transmission associated with relief of migraine

Pharmacokinetics

Half-Life: 3-4 hr

Peak Plasma Time: 1-3 hr

Bioavailability: 70%

Protein bound: 35%

Vd: 180-200 L

Absorption: Well absorbed

Metabolism: CYP3A4, CYP2D6

Excretion: Urine (75%)