Zolmitriptan

Indications

Zolmitriptan is used for: Acute migraine attacks

Adult Dose

Oral Acute migraine attacks Adult: Initially, 2.5 mg. A 2nd dose may be taken at least 2 hr after the 1st dose if symptoms recur within 24 hr. Max dose: 10 mg in 24 hr. Safety of treating > three headaches in a 30-day period has not been established. Hepatic impairment: Dose reduction may be needed with BP monitoring. Moderate to severe: Max dose: 5 mg/24 hr

Child Dose

Renal Dose

After orally dosing zolmitriptan, renal clearance was Reduced by 25% in patients with severe renal impairment (Clcr ?5 ?25mL/min) compared to the normal group (Clcr ?70 mL/min); No significant change in renal clearance was observed in the moderately renally impaired group (Clcr ?26 ?50 mL/min).

Administration

May be taken with or without food.

Contra Indications

Patients at risk of coronary artery disease (post-menopausal women, men >40 yr, hypertension, hypercholesterolemia, smoking, obesity, DM, family history of coronary artery disease) unless evaluated. Wolff-Parkinson-White syndrome; arrhythmias associated with accessory cardiac conduction pathways; previous cerebrovascular accident; uncontrolled or severe hypertension; ischaemic heart disease, history of MI, coronary vasospasm, transient ischaemic attack. Basilar or hemiplegic migraine.

Precautions

Use only if there is a clear diagnosis of migraine; exclude other potentially serious neurological conditions. Monitor BP closely. May impair ability to drive or operate machinery. Pregnancy and lactation. Child. Moderate to severe hepatic impairment. Prior CV evaluation for patients with risk factors of coronary heart disease; admin of first dose under close supervision and ECG if satisfactory CV assessment in these patients. Periodic CV evaluation for patients with risk factors of coronary arteries on zolmitriptan. Avoid oral disintegrating formulation for patients with phenylketouria. Long term use may cause accumulation of zolmitriptan in melanin rich tissue (e.g. eye). Lactation: unknown, use caution

Pregnancy-Lactation

Pregnancy There are no adequate data on the developmental risk associated with the use in pregnant women; in reproductive toxicity studies in rats and rabbits, oral administration of zolmitriptan to pregnant animals resulted in embryolethality and fetal abnormalities (malformations and variations) at clinically relevant exposures Published data have suggested that women with migraine may be at increased risk of preeclampsia during pregnancy Lactation There are no data on presence of drug or metabolites in human milk, effects on the breastfed infant, or on milk production; in rats, oral dosing with zolmitriptan resulted in levels in milk up to 4 times that in maternal plasma Developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from drug or from underlying maternal condition

Interactions

Increased risk of serotonin syndrome with SSRI, selective serotonin- and norepinephrine-reuptake inhibitors (SNRI). Increased zolmitriptan concentrations with cimetidine, quinolone antibacterials and drugs that inhibit the cytochrome P450 isoenzyme CYP1A2. Potentially Fatal: Increased risk of fatal serotonin syndrome with sibutramine. Increased risk of serotonin syndrome with MAOI and reversible inhibitors of monoamine oxidase type-A (RIMA); do not use zolmitriptan during and for 2 wk after the use of MAOI and RIMAs Do not use within 24 hr of treatment with another 5-HT1 agonist. Increased risk of additive vasoconstriction with ergot alkaloids; zolmitriptan should not be taken within 24 hr of any ergotamine or ergot-type medication.

Side Effects

Side effects of Zolmitriptan : 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 Potentially Fatal: Cardiac arrhythmias, MI, subarachnoid haemorrhage.

Mode of Action

Zolmitriptan is a selective agonist for serotonin (5HT1 receptors). It relieves migraine by selective constriction of intracranial blood vessels, neuropeptide release inhibition and decreased transmission in the trigeminal pain pathway.