zolmitriptan (Zomig, Zomig Rapimelt, Zomig-ZMT)
Classes: Serotonin 5-HT-Receptor Agonists; Antimigraine Agents
Dosing and uses of Zomig, Zomig Rapimelt (zolmitriptan)
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
