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naratriptan (Amerge)

 

Classes: Serotonin 5-HT-Receptor Agonists; Antimigraine Agents

Dosing and uses of Amerge (naratriptan)

 

Adult dosage forms and strengths

tablet

  • 1mg
  • 2.5mg

 

Migraine

1-2.5 mg PO at onset; may repeat once after 4 hours

Not to exceed 5 mg/day

 

Renal Impairment

Mild-to-moderate: Not to exceed 2.5 mg/day

Severe (<15 mL/min); Do not administer

 

Pediatric dosage forms and strengths

Safety and efficacy not established

 

Geriatric dosage forms and strengths

Not recommended

 

Amerge (naratriptan) adverse (side) effects

1-10%

Dizziness

Drowsiness

Fatigue

Paresthesias

Pain/pressure sensation

Nausea (1-5%)

Throat/neck symptoms

 

<1%

Myocardial infarction

Coronary artery vasospasm in pts with CAD risk factors

 

Warnings

Contraindications

Hypersensitivity, including angioedema and anaphylaxis

Severe hepatic or renal impairment

Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders

Ischemic heart disease (angina pectoris, history of myocardial infarction, or documented silent ischemia) or coronary artery vasospasm, including Prinzmetal’s angina)

History of stroke or TIA, or history of hemiplegic or basilar migraine because such patients are at a higher risk of stroke

Peripheral vascular disease

Ischemic bowel disease

Uncontrolled hypertension

Do not use within 24 hr of another 5-HT1 agonist or ergot derivative

 

Cautions

Decrease dose with mild-moderate renal impairment

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)

Serotonin syndrome: Potentially life-threatening serotonin syndrome may occur, particularly during combined use with SSRIs (eg, fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram) or SNRIs (eg, venlafaxine, duloxetine)

Myocardial infarction, cardiac arrest, transient ischemia, coronary artery vasopasm reported

Significant increase in blood pressure including hypertensive crisis with acute impairment of organ systems reported

Anaphylaxis/anaphylactoid and hypersensitivity reactions, including angioedema reported (see Contraindications)

May cause dizziness, weakness, or drowsiness (infrequent)

 

Pregnancy and lactation

Pregnancy category: C

Lactation: unknown; use with caution in breastfeeding

 

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.

 

Pharmacology of Amerge (naratriptan)

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

 

Absorption

Bioavailability: 70%

Peak Plasma Time: 3-4 hr

Peak Plasma Concentration: 50-1,000 ng/ml; 50% higher in women

 

Distribution

Protein Bound: 28-31%

Vd: 170 L

 

Metabolism

Via hepatic CYP450 enzymes

 

Elimination

Half-Life: 6 hr

Excretion: Urine 50%