Sumigran

Each film-coated tablet contains Sumatriptan succinate eq. to sumatriptan 50 mg.

Pharmacology: Pharmacodynamics: Mechanism of action: Sumatriptan is a selective agonist of vascular serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors on intracranial blood vessels and sensory nerves of the trigeminal system; causes vasoconstriction and reduces neurogenic inflammation associated with antidromic neuronal transmission correlating with relief of migraine.
Pharmacokinetics: Sumatriptan is rapidly absorbed following oral administration; oral absorption appears to occur in the small intestine. The bioavailability of sumatriptan following oral administration averages only about 15%, principally because of presystemic metabolism of the drug and in part because of incomplete absorption. Sumatriptan is approximately 14-21% bound to plasma proteins over a concentration range of 10-1000 ng/mL. Sumatriptan is distributed into milk in humans and animals. The elimination half-life is 1.5-2.6 hours. Sumatriptan is metabolized in the liver and possibly in the GI tract and is eliminated in urine and feces. Sumatriptan is excreted in urine via glomerular filtration and tubular secretion, but renal plasma clearance accounts for only 22% of the systemic clearance of 1176-1200 mL/min.

Sumatriptan is indicated for the acute relief of migraine attacks with or without aura, including the treatment of migraine attacks associated with the menstrual period in women.

Recommended Dose: Adult: Initial dosage: Single dose of 50 mg tablet. If the headache returns or the patient has a partial response to the initial dose, the dose may be repeated after 2 hours, not to exceed a total daily dose of 200 mg.
Maximum dose: 200 mg/day.
Hepatic function impairment: Mild to moderate hepatic impairment: Bioavailability is increased with liver disease. If treatment is needed, do not exceed single doses of 50 mg.
Children and adolescents (under 18 years of age): The efficacy of sumatriptan tablets in this population has not been demonstrated.
Elderly (over 65 years of age): Experience of the use of sumatriptan tablets in patients aged over 65 years is limited. The pharmacokinetics do not differ significantly from a younger population, but until further clinical data are available, the use of sumatriptan tablets in patients aged over 65 years is not recommended.
Mode of Administration: Sumigran is administered orally. It is advisable that sumatriptan be given as early as possible after the onset of a migraine headache, although it is equally effective at whatever stage of the attack it is administered.

Overdose and Treatment: Since the elimination half-life of sumatriptan is about 2-2.5 hours, monitoring of patients after overdosage should continue while symptoms persist or for at least 10-12 hours.
The effect of hemodialysis or peritoneal dialysis on serum concentrations of sumatriptan is not known.

Sumatriptan is contraindicated in patients with a history of hypersensitivity to sumatriptan or any component of the formulation.
Sumatriptan is contraindicated in patients with uncontrolled hypertension.
Sumatriptan is contraindicated in patients with hemiplegic or basilar migraine.
Sumatriptan is contraindicated in patients with severe hepatic impairment.
Sumatriptan is contraindicated in patients with ischemic heart disease (angina pectoris, history of myocardial infarction, or documented silent ischemia).
Sumatriptan is contraindicated in patients with coronary artery vasospasm (e.g., Prinzmetal variant angina).
Sumatriptan is contraindicated in patients with a history of stroke or transient ischemic attack, peripheral vascular disease, or ischemic bowel disease.
The concomitant use of ergotamine or derivatives of ergotamine (including methysergide) is contraindicated.
Concurrent administration of monoamine oxidase inhibitors (MAOIs) and sumatriptan is contraindicated. Sumatriptan must not be used within 2 weeks of discontinuation of therapy with MAOIs.

Patients should be advised to avoid performing hazardous activities that require mental alertness (e.g., operating machinery, driving a motor vehicle).
Sumatriptan should be used with caution in patients with a history of seizure disorders or conditions associated with a lowered seizure threshold.
Sumatriptan should be used with caution in patients with diseases that may alter the absorption, metabolism, or excretion of the drug, such as impaired renal or hepatic function.
Sumatriptan should be avoided in patients with multiple cardiovascular risk factors (e.g., postmenopausal women; men older than 40 years of age; patients with risk factors such as hypertension, hypercholesterolemia, obesity, diabetes, smoking, or family history of coronary artery disease) who have not previously received therapy with a 5-HT₁ receptor agonist. These patients should undergo cardiovascular evaluation prior to initiation of sumatriptan therapy.
Sumatriptan should only be used where there is a clear diagnosis of migraine.
Sumatriptan is not indicated for use in the management of hemiplegic, basilar or ophthalmoplegic migraine.
Before treating with sumatriptan, care should be taken to exclude potentially serious neurological conditions (e.g. CVA, TIA) if the patient presents with atypical symptoms or if they have not received an appropriate diagnosis for sumatriptan use.

Pregnancy: There are no adequate and well-controlled studies evaluating the use of sumatriptan in pregnant women. Sumatriptan should be used during pregnancy only if the potential benefit justifies the risk to the fetus.
Lactation: Sumatriptan is distributed into breast milk following administration of the drug to lactating animals or nursing women. Infant exposure can be minimized by avoiding breast-feeding for 12 hours after receiving the drug.

Cardiovascular: Chest pain, chest pressure, chest tightness, hot and cold flashes.
Central nervous system: Fatigue, feeling of heaviness, heaviness of chest, malaise, pain, paresthesia, sensation of pressure, sensation of tightness, vertigo.
Gastrointestinal: Sore throat.
Local: Local pain.
Neuromuscular & skeletal: Jaw pain, jaw pressure, jaw tightness, neck pain.
Respiratory: Pharyngeal edema.

1) Concomitant use of sumatriptan and MAO-A inhibitors may decrease sumatriptan clearance and increase half-life and blood concentrations of the drug.
2) Ergot alkaloids (e.g. ergotamine, dihydroergotamine, methylsergide) have been reported to cause prolonged vasospastic reactions and the vasoconstrictor effects of these drugs may be additive to those of sumatriptan, therefore use of ergot alkaloids and sumatriptan within 24 hours of each other is contraindicated.
3) Serotonin syndrome has been reported during concurrent therapy with 5-HT₁ receptor agonists and selective serotonin-reuptake inhibitors (SSRIs) or selective serotonin- and norepinephrine-reuptake inhibitors (SNRIs).

Store below 30 °C.

Antimigraine Preparations

N02CC01 - sumatriptan ; Belongs to the class of selective serotonin (5HT1) agonists preparations. Used to relieve migraine.

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