Zolmitriptan Nasal prep
Indications
Zolmitriptan Nasal prep is used for:
Acute migraine attacks
Adult Dose
Nasal
Acute migraine attacks
Adult: 5 mg (1 spray) into 1 nostril as soon as possible after onset of symptoms, repeated at least 2 hr after the 1st dose if symptoms recur w/in 24 hr. Max: 10 mg/day. Safety of treating >4 headaches in a 30 day period is not established.
Hepatic impairment: Avoid use.
Child Dose
Migraine
Nasal spray
<12 years: Safety and efficacy not established
>12 yr
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
Renal Dose
Administration
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 Nasal prep :
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.