Sumatriptan
Mechanism :
Sumatriptan is an agonist for 5-hydroxytryptamine1 receptor subtype having only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7 receptors and no significant affinity for 5-HT2, 5-HT3 or 5-HT4 receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1; dopamine2; muscarinic, or benzodiazepine receptors.
Indication :
Contraindications :
Contraindicated in patients with history, symptoms, or signs of ischemic cardiac, cerebrovascular, or peripheral vascular syndromes, all forms of myocardial infarction, and silent myocardial ischemia, coronary vasospasm and uncontrolled hypertension.
Dosing :
Oral: As single dose.
6-10 years: 25 mg
10-12 years: 50 mg
12-18 years: 50-100 mg
Adverse Effect :
Rarely serious cardiac events, including some that have been fatal, have occurred following the use of sumatriptan including coronary artery vasospasm, transient myocardial ischemia, myocardial infarction, ventricular tachycardia, ventricular fibrillation, nausea, vomiting, seizures, transient tingling sensation, heaviness, flushing, dizziness, weakness and hypersensitivity reactions.
Interaction :
MAO-A Inhibitors: Reduce sumatriptan clearance, significantly increasing systemic exposure. Therefore, the use of sumatriptan tablets in patients receiving MAO-A inhibitors is contraindicated.
Selective Serotonin Reuptake Inhibitors Fluoxetine, Fluvoxamine, Paroxetine, Sertraline: Rarely cause weakness, hyperreflexia, and incoordination when coadministered with 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, use with caution |
| <10 | Dose as in normal renal function, use with caution |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Unknown dialysability. Dose as in GFR<10 mL/min |
| HD | Unknown dialysability. Dose as in GFR<10 mL/min |
| HDF/High flux | Unknown dialysability. Dose as in GFR<10 mL/min |
| CAV/VVHD | Unknown dialysability. Dose as in normal renal function. Use with caution |
Hepatic Dose :
Mild to Moderate hepatic Impairment:
Intranasal preparation: No dose adjustment recommended.
Oral preparation: Hepatic impairment increases bioavailability of the drug. Use is not recommended. However if required, the maximum dose that can be given is 50mg a dose in adults.
Subcutaneous preparation: No dose adjustment recommended.
Severe hepatic impairment: Do not use sumatriptan.