Zomig
(Zolmitriptan)Zomig Prescribing Information
ZOMIG 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.
- Only use ZOMIG if a clear diagnosis of migraine has been established. If a patient has no response to ZOMIG treatment for the first migraine attack, reconsider the diagnosis of migraine before ZOMIG is administered to treat any subsequent attacks.
- ZOMIG is not indicated for the prevention of migraine attacks.
- Safety and effectiveness of ZOMIG have not been established for cluster headache.
- Not recommended in patients with moderate or severe hepatic impairment [see Dosage and Administration (2.2)].
Nasal Spray 2.5 mg and 5 mg.
ZOMIG 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 (5.2)]
- History of stroke, transient ischemic attack (TIA) or history of hemiplegic or basilar migraine because these patients are at higher risk of stroke [see Warnings and Precautions (5.4)]
- Peripheral vascular disease (PVD) [see Warnings and Precautions (5.5)]
- Ischemic bowel disease [see Warnings and Precautions (5.5)]
- Uncontrolled hypertension [see Warnings and Precautions (5.8)]
- Recent use (i.e., within 24 hours) of another 5-HT1 agonist, ergotamine-containing medication, or ergot-type medication (such as dihydroergotamine or methysergide) [see Drug Interactions (7.1, 7.3)]
- Concurrent administration of an MAO-A inhibitor or recent discontinuation of a MAO-A inhibitor (that is within 2 weeks) [see Drug Interactions (7.2) and Clinical Pharmacology (12.3)]
- Known hypersensitivity to ZOMIG (angioedema and anaphylaxis seen) [see Adverse Reactions (6.2)]
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 (5.6)]
- Serotonin Syndrome [see Warnings and Precautions (5.7)]
- Increase in Blood Pressure [see Warnings and Precautions (5.8)]
ZOMIG® (zolmitriptan) Nasal Spray contains zolmitriptan, which is a selective 5-hydroxytryptamine 1B/1D (5-HT1B/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 C16H21N3O2, representing a molecular weight of 287.36. Zolmitriptan is a white to almost white powder that is readily soluble in water. ZOMIG Nasal Spray is supplied as a clear to pale yellow solution of zolmitriptan, buffered to a pH 5.0. Each ZOMIG Nasal Spray contains 2.5 mg or 5 mg of zolmitriptan in a 100-μL unit dose aqueous buffered solution containing citric acid, anhydrous, USP, disodium phosphate dodecahydrate USP and purified water USP.
ZOMIG Nasal Spray is hypertonic. The osmolarity of ZOMIG Nasal Spray for 2.5 mg is 360 to 420 mOsmol, and for 5 mg is 420 to 470 mOsmol.
Zolmitriptan binds with high affinity to human recombinant 5-HT1D and 5-HT1B receptors, and moderate affinity for 5-HT1A receptors. The N-desmethyl metabolite also has high affinity for 5-HT1B/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. The therapeutic activity of ZOMIG for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.