Zolmitriptan
Mechanism :
Selective agonist for serotonin (5-HT1B and 5-HT1D receptors) in cranial arteries and sensory nerves of the trigeminal system; causes vasoconstriction and reduces inflammation associated with antidromic neuronal transmission correlating with relief of migraine
Indication :
- Acute treatment of migraine in children >12 years
Contraindications :
Hypersensitivity to zolmitriptan or any component of the formulation; ischemic coronary artery disease. Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders; peripheral vascular disease; ischemic bowel disease; uncontrolled hypertension; recent use (within 24 hours) of treatment with another 5-HT1 agonist, or an ergotamine-containing or ergot-type medication like dihydroergotamine or methysergide; history of stroke, transient ischemic attack, or history of hemiplegic or basilar migraine.
Dosing :
Nasal spray:
2.5 mg, Second dose: May repeat in 2 hours, may increase to 5 mg/dose. Maximum single dose: 5 mg.
Oral:
1.25 to 2.5 mg, Second dose: May repeat in 2 hours, may increase to 5 mg/dose. Maximum single dose: 5 mg.
Adverse Effect :
Unpleasant taste, chest pain, facial edema, palpitations, cardiac arrhythmia, dizziness, paresthesia, drowsiness, diaphoresis, nausea, hypersensitivity reaction, local pain, application site irritation, weakness, nasal discomfort.
Interaction :
Ergot Derivatives: May enhance the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists. Serotonin 5-HT1D Receptor Agonists may enhance the vasoconstricting effect of Ergot Derivatives. Exceptions: Nicergoline.
Methylene Blue: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
Monoamine Oxidase Inhibitors: May decrease the metabolism of Serotonin 5-HT1D Receptor Agonists. Management: If MAO inhibitor therapy is required, naratriptan, Eletriptan or frovatriptan may be a suitable 5-HT1D agonist to employ.
Sumatriptan: Serotonin 5-HT1D Receptor Agonists may enhance the adverse/toxic effect of Sumatriptan.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
20-50 | Dose as in normal renal function |
10-20 | Dose as in normal renal function |
<10 | Dose as in normal renal function |
Dose in Patients undergoing Renal Replacement Therapies
CAPD | Unknown dialysability. Dose as in normal renal function |
HD | Unknown dialysability. Dose as in normal renal function |
HDF/High flux | Unknown dialysability. Dose as in normal renal function |
CAV/VVHD | Unknown dialysability. Dose as in normal renal function |
Hepatic Dose :
Dose adjustment guidelines are not available. In patients with moderate and severe hepatic impairment: the orally disintegrating and nasal inhalational formulas of the drug are not recommended and dose reduction of oral formulation will be necessary.