Products
Zolmitriptan is commercially available as film-coated tablets, meltable tablets, and as a nasal spray (Zomig, generics). It has been approved in many countries since 1997. Generic versions entered the market in 2012.
Structure and properties
Zolmitriptan (C16H21N3O2, Mr = 287.4 g/mol) is an indole and oxazolidinone derivative structurally related to serotonin. It exists as a pure -enantiomer and as a white powder that is soluble in water. Zolmitriptan is more lipophilic than sumatriptan.
Effects
Zolmitriptan (ATC N02CC03) has intracranial vasoconstrictive and anti-inflammatory properties and causes a slight increase in blood pressure. The effects are due to selective binding to serotonin 5HT1D and -5HT1B receptors. Zolmitriptan has a short half-life of 2.5 to 3 hours. The active metabolite -desmethylzolmitriptan (183C91) is formed in the liver and is implicated in the effects.
Indications
For acute treatment of migraine attacks with or without aura and cluster headache.
Dosage
According to the SmPC. The drug should be administered as soon as possible at the onset of symptoms. During treatment, the low maximum daily dose (10 mg) and dosing interval must be observed. Absorption is hardly affected by food taken at the same time. The melting tablets can be taken without water and in case of nausea. The nasal spray has a faster onset of action compared with the tablets.
Contraindications
- Hypersensitivity
- Hemiplegic migraine
- Basiliaris migraine
- Ischemic heart disease
- Myocardial infarction
- Prinzmetal angina
- Inadequately controlled hypertension
Full details of precautions and interactions can be found in the drug label.
Interactionsn
Zolmitriptan is metabolized primarily by CYP1A2 and to a lesser extent by MAO-A. Plasma concentrations may be increased when CYP1A2 inhibitors are administered. Dose reduction is recommended. Two potent such inhibitors are fluvoxamine and ciprofloxacin. Another drug-drug interaction is possible with MAO inhibitors. Serotonin syndrome may occur with concomitant use of serotonergic drugs. Zolmitriptan should not be combined with ergot alkaloids because they have an additional vasoconstrictor effect.
Adverse effects
The most common possible adverse effects include abdominal pain, nausea, vomiting, dry mouth, palpitations, muscle weakness and muscle pain, dizziness, headache, drowsiness, feeling warm, numbness, and weakness. A and a feeling of heaviness, tightness, pain, or pressure may occur in the throat, neck, jaw, hands, feet, and chest. Zolmitriptan, like other triptans, has the potential for coronary artery narrowing. Very rarely, severe cardiovascular disease, such as myocardial infarction or angina, has been reported.
