Drug Index

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)
20-50Dose as in normal renal function
10-20Dose as in normal renal function
<10Dose as in normal renal function

Dose in Patients undergoing Renal Replacement Therapies
CAPDUnknown dialysability. Dose as in normal renal function
HDUnknown dialysability. Dose as in normal renal function
HDF/High fluxUnknown dialysability. Dose as in normal renal function
CAV/VVHDUnknown 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.
08/12/2024 18:33:31 Zolmitriptan
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