Overview
11 DESCRIPTION ZOLMITRIPTAN NASAL SPRAY contains zolmitriptan, which is a selective 5-hydroxytryptamine 1B/1D (5-HT 1B/1D ) receptor agonist. Zolmitriptan is chemically designated as (S)-4-[[3-[2-(dimethylamino) ethyl]-1H-indol-5-yl]methyl]-2-oxazolidinone and has the following chemical structure: The empirical formula is C 16 H 21 N 3 O 2 , representing a molecular weight of 287.36.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Zolmitriptan binds with high affinity to human recombinant 5-HT 1D and 5-HT 1B receptors, and moderate affinity for 5-HT 1A receptors. The N-desmethyl metabolite also has high affinity for 5-HT 1B/1D and moderate affinity for 5-HT1A receptors. Current theories proposed to explain the etiology of migraine headache suggest that symptoms are due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system.
Indications
- 1 INDICATIONS AND USAGE ZOLMITRIPTAN NASAL SPRAY is indicated for the acute treatment of migraine with or without aura in adults and pediatric patients 12 years of age and older. Limitations of Use Only use ZOLMITRIPTAN NASAL SPRAY if a clear diagnosis of migraine has been established. If a patient has no response to ZOLMITRIPTAN NASAL SPRAY treatment for the first migraine attack, reconsider the diagnosis of migraine before ZOLMITRIPTAN NASAL SPRAY is administered to treat any subsequent attacks. ZOLMITRIPTAN NASAL SPRAY is not indicated for the prevention of migraine attacks.
Common Doses
- 2.5 mg
- 5 mg
- 10 mg
Dosage
2 DOSAGE AND ADMINISTRATION Recommended starting dose: 2.5 mg (2.1) Maximum single dose: 5 mg (2.1) May repeat dose after 2 hours if needed; not to exceed 10 mg in any 24-hour period (2.1) 2.1 Dosing Information The recommended starting dose for ZOLMITRIPTAN NASAL SPRAY in adult and pediatric patients 12 years of age and older is 2.5 mg. As the individual response to ZOLMITRIPTAN NASAL SPRAY may vary, the dose should be adjusted on an individual basis. The maximum recommended single dose of ZOLMITRIPTAN NASAL SPRAY is 5 mg.
Contraindications
- 4 CONTRAINDICATIONS Zolmitriptan is contraindicated in patients with: Ischemic coronary artery disease (angina pectoris, history of myocardial infarction, or documented silent ischemia), other significant underlying cardiovascular disease, or coronary artery vasospasm including Prinzmetal's angina [see Warnings and Precautions (5.1) ] Wolff-Parkinson-White Syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders [see Warnings and Precautions (5.
Side Effects
- 6 ADVERSE REACTIONS The following adverse reactions are discussed in more detail in other sections of labeling: Myocardial Ischemia, Myocardial Infarction, and Prinzmetal's Angina [see Warnings and Precautions (5.1) ] Arrhythmias [see Warnings and Precautions (5.2) ] Chest, Throat, Neck and/or Jaw Pain/Tightness/Pressure [see Warnings and Precautions (5.3)] Cerebrovascular Events [see Warnings and Precautions (5.4)] Other Vasospasm Reactions [see Warnings and Precautions (5.5)] Medication Overuse Headache [see Warnings and Precautions (5.
Interactions
- 7 DRUG INTERACTIONS If co-administered with cimetidine: Maximum single dose of 2.5 mg, not to exceed 5 mg in any 24-hour period. (2.3 , 7.4) 7.1 Ergot-containing drugs Ergot-containing drugs have been reported to cause prolonged vasospastic reactions. Because these effects may be additive, use of ergotamine-containing or ergot-type medications (like dihydroergotamine or methysergide) and zolmitriptan within 24 hours of each other is contraindicated [see Contraindications (4) ] . 7.2 MAO-A Inhibitors MAO-A inhibitors increase the systemic exposure of zolmitriptan.