zolmitriptan (Zomig, Zomig Rapimelt, Zomig-ZMT)

Dosing and uses of Zomig, Zomig Rapimelt (zolmitriptan)

• Adult
• Pediatric

 

Adult dosage forms and strengths

tablet

• 2.5mg (scored)
• 5mg

oral disintegrating tablet

• 2.5mg
• 5mg

intranasal spray

• 2.5mg/single-use device
• 5mg/single-use device

 

Migraine

Indicated for acute treatment of migraine with or without aura

Initial dose: 2.5 mg PO/intranasally at onset of migraine

Individual response varies, may increase dose to 5 mg; do not exceed 5 mg per single dose

If migraine has not resolved, may repeat dose after 2 hr if needed; not to exceed 10 mg/24 hr

Safety not established in the treatment of an average of >3 migraines/30 days (tablets) or >4 migraines/30 days (intranasal)

 

Dosage modifications

Coadministration with cimetidine: Limit zolmitriptan to 2.5 mg/dose and 5 mg/day

Renal impairment: Not evaluated with nasal spray; with oral dosing, zolmitriptan clearance reduced by 25% in patients with severe renal clearance

Hepatic impairment

• Mild: No dosage adjustment required
• Moderate-to-severe: Not recommended; increased zolmitriptan blood levels may elevate blood pressure in some patients

 

Pediatric dosage forms and strengths

Intranasal spray

• 2.5mg/single-use device
• 5mg/single-use device

 

Migraine

Nasal spray dosage form indicated for acute treatment of migraine with or without aura in pediatric patients aged ≥12 yr

<12 years: Safety and efficacy not established

Initial dose: 2.5 mg intranasally at onset of migraine

Individual response varies, may increase dose to 5 mg; do not exceed 5 mg per single dose

If migraine has not resolved, may repeat dose after 2 hr if needed; not to exceed 10 mg/24 hr

Safety not established in the treatment of an average of >4 migraines/30 days

 

Dosage modifications

Coadministration with cimetidine: Limit zolmitriptan to 2.5 mg/dose and 5 mg/day

Renal impairment: Not evaluated with nasal spray; with oral dosing, zolmitriptan clearance reduced by 25% in patients with severe renal clearance

Hepatic impairment

• Mild: No dosage adjustment required
• Moderate-to-severe: Not recommended; increased zolmitriptan blood levels may elevate blood pressure in some patients

 

Zomig, Zomig Rapimelt (zolmitriptan) adverse (side) effects

1-10%

Dizziness (6-10%)

Neck/throat/jaw pain (4-10%)

Parasthesia (5-9%)

Nausea (4-9%)

Weakness (3-9%)

Somnolence (5-8%)

Warm/cold sensation (5-7%)

Xerostomia (3-5%)

Chest pain (2-4%)

Diaphoresis (3%)

Pain (2-3%)

Dyspepsia (1-3%)

Dysphagia (2%)

Myasthenia (2%)

Palpation (2%)

Vertigo (2%)

Hypoesthesia (1-2%)

Myalgia (1-2%)

 

<1%

QT prolongation

Bradycardia

Tachycardia

Thrombophlebitis

Postural hypotension

Hyperglycemia

Alk phos increased

Arthritis

Twitching

Myocardial infarction and artery vasospasm in patients with CAD risk factors

 

Warnings

Contraindications

Hypersensitivity

Ischemic or vasospastic artery disease

Uncontrolled HTn

Wolf-Parkinson-White syndrome

Peripheral vascular disease

Ischemic bowel disease

Not indicated for basilar or hemiplegic migraine

Do not use concurrently with or within 2 wk of using MAO Inhibitors

Do not use within 24 hr of other 5-HT agonist or ergotamine-containing or ergot-type medication

 

Cautions

Little added benefit with 5 mg PO dose compared with 2.5 mg

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)

As with other 5-HT1 agonists, sensations of tightness, pain, pressure, and heaviness in the precordium, throat, neck, and jaw commonly occur that are not cardiac in origin

Cerebral hemorrhage, subarachnoid hemorrhage, and stroke have occurred with 5-HT1 agonists, including some fatalities

May cause noncoronary vasospastic reactions (eg, peripheral vascular ischemia, GI vascular ischemia and infarction, splenic infarction, and Raynaud’s syndrome

Significant increases in blood pressure reported

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)

 

Pregnancy and lactation

Pregnancy category: C

Lactation: unknown, use 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.

 

Pharmacology of Zomig, Zomig Rapimelt (zolmitriptan)

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 elimination: 2.8-3.7 hr

Peak Plasma Time: 1.5 hr; 3 hr (ZMT)

Bioavailability: 40%

Onset of action: 0.5-1 hr

Protein Bound: 25%

Vd: 7.0 L/kg

Metabolism: liver

Metabolites: N-desmethyl zolmitriptan

Excretion: Urine (65%); Feces (30%)

Clearance

• Total Body: 31.5 mL/min/kg
• Renal: 5.25 mL/min/kg

 

Administration

Instructions

For 1.25 mg dose, manually break the scored 2.5 mg regular oral tablet in half

Do not break orally disintegrating tablets