Sutrip

Sumatriptan succinate.

Each film-tablet contains: Sumatriptan succinate, BP Equivalent to Sumatriptan 50 mg.
Excipients q.s.
Colour: Titanium Dioxide.
Sutrip 50 mg tablet contains sumatriptan as active ingredient. The empirical formula of sumatriptan succinate {1-[3-[2-dimethylamino)ethyl]-1H-indol-5yl]-N-methylmethanesulfonamide succinate} is C₁₈H₂₇N₃O₆S and its molecular weight is 413.5 g/mol.

Pharmacological Classification: Antimigraine (Selective Serotonin (5HT1) Agonist).
Pharmacology: Mechanism of Actions: Sumatriptan is a selective serotonin agonist that acts at 5-HT1 receptors and produces vasoconstriction of cranial arteries. Drugs like sumatriptan, which are commonly known as triptans, are believed to act mainly at 5-HT1B and 5-HT1D subtype receptors and are therefore sometimes referred to as 5HT1B/1D-receptor agonists.
Pharmacokinetics: Sumatriptan is rapidly but incompletely absorbed when given orally and undergoes first-pass metabolism, resulting in a low absolute bioavailability of about 14%.
Peak plasma concentrations after oral doses are achieved in about 2 hours. Bioavailability is much higher (96%) after subcutaneous doses with peak concentrations occurring within 25 minutes. Bioavailability after intranasal doses is 16% of that achieved subcutaneously, with peak concentrations occurring in about 1.5 hours. Plasma protein binding is low at about 14 to 21%. The elimination half-life of sumatriptan is about 2 hours. Sumatriptan is extensively metabolised in the liver predominantly by monoamine oxidase type A and is excreted mainly in the urine as the inactive indole acetic acid derivative and its glucuronide. Sumatriptan and its metabolites also appear in the faeces. Small amounts of sumatriptan are distributed into breastmilk.

Sumatriptan is used for the acute treatment of migraine attacks and of cluster headache. Sumatriptan should only be used where there is a clear diagnosis of migraine.

It may be given orally or subcutaneously as the succinate and intranasally as the base. Doses are expressed in terms of the base; sumatriptan succinate 70 mg is equivalent to about 50 mg of sumatriptan. For the acute treatment of migraine sumatriptan should be used as soon as possible after the onset of the headache phase, but efficacy is independent of the duration of the attack before starting treatment. If no response is obtained with the initial dose by any route, a second dose should not be given for the same attack.
It is given orally to adults aged 18 years and over, the clinical response can be expected after about 30 minutes. If symptoms recur after an initial response, further doses may be given provided that there is a minimum interval of 2 hours between doses and that not more than 300 mg is taken in any 24-hour period. A lower dose of 25 mg may be used, although some patients require 50 or 100 mg.
This may be followed by a second dose of up to 100 mg if the headache returns or the patient has a partial response provided that the total daily dose does not exceed the recommended maximum of 200 mg. A minimum interval of 2 hours is recommended between doses or as prescribed by the physician.
Administration in children: Sumatriptan may be given for the treatment of acute migraine in children and adolescents. Although not licensed for oral paediatric a single oral dose of 25 mg may be given to children aged 6 to10 years and 50 mg to those aged 10 to 12 years, repeated once after at least 2 hours if symptoms recur after an initial response; older children may be given the usual adult dose.
Administration in hepatic impairment: A dose of up to 50 mg by mouth is considered suitable. It should not be given to patients with severe impairment.
For High-altitude disorders, Sumatriptan has been tried with some success in a small study for the prevention of symptoms of acute mountain sickness.

Sumatriptan should not be used in patients who have: Hypersensitivity to any component of the preparation. A history of myocardial infarction Peripheral vascular disease or symptoms or signs consistent with ischaemic heart disease. Prinzmetal's angina/coronary vasospasm. Uncontrolled hypertension. Cerebrovascular accident or transient ischaemic attack. Severe hepatic impairment.

Sumatriptan and other serotonin (5-HT1) agonists should only be used where there is a clear diagnosis of migraine or cluster headache and care should be taken to exclude other potentially serious neurological conditions. They should not be used for prophylaxis and should not be given to patients with basilar, hemiplegic, or ophthalmoplegic migraine. Serotonin (5-HT1) agonists are contraindicated in patients with uncontrolled hypertension, ischaemic heart disease (coronary artery disease), a history of myocardial infarction, coronary vasospasm (Prinzmetal's angina), peripheral vascular disease, or a previous cerebrovascular accident or transient ischaemic attack. Unrecognised cardiovascular disease should be excluded before the use of serotonin (5-HT1) agonists in postmenopausal women, men over 40 years of age, and those with risk factors for ischaemic heart disease. If chest pain and tightness occur during use, appropriate investigations should be performed. Sumatriptan should not be used intravenously because of the increased risk of producing coronary vasospasm. Drowsiness may occur after treatment with serotonin (5-HT1) agonists and patients thus affected should not drive or operate machinery. Sumatriptan should be used with caution in patients with hepatic or renal impairment and should generally be avoided if impairment is severe. There have been rare reports of seizures after use of sumatriptan and it should therefore be used with caution in patients with a history of epilepsy or other conditions predisposing to seizures. Patients with hypersensitivity to sulfonamides may exhibit a similar reaction to sumatriptan.
Use in Lactation: Infant exposure can be minimised by avoiding breastfeeding for 12 hours after treatment. The distribution of sumatriptan into breast milk after a 6-mg subcutaneous dose has been studied in 5 lactating mothers. The mean total recovery of sumatriptan in breast milk was estimated to be 14.4 micrograms or 0.24% of the dose. It was calculated that on a weight-adjusted basis an infant could receive a maximum of 3.5% of the maternal dose.
Use in Pregnancy: Pregnancy. Sumatriptan crosses the placenta; however, only a very small quantity reaches the fetus. A literature review concluded that exposure to sumatriptan in pregnancy posed no additional risk of birth defects compared with that in the general population, but as for other drugs sumatriptan should only be used in pregnancy when the benefit justifies the potential risk to the fetus.

The most commonly adverse effects of serotonin (5-HT1) agonists such as sumatriptan include dizziness, flushing, weakness, drowsiness, and fatigue. Nausea and vomiting may occur. Dyspnoea and sensory disturbance including paraesthesia and hypoaesthesia have been reported. Pain or sensations of heaviness, heat or cold, pressure, or tightness have also been commonly reported, can affect any part of the body including the throat and chest, and may be intense. These symptoms may be due to vasospasm, which on rare occasions has resulted in severe cardiovascular events including cardiac arrhythmias, myocardial ischaemia, or myocardial infarction. There have been isolated reports of associated cerebrovascular events in patients receiving sumatriptan. Transient increases in blood pressure may occur soon after treatment. Hypotension, bradycardia or tachycardia, palpitations, Raynaud's syndrome, and ischaemic colitis have been reported. Visual disturbances have also occurred. Medication-overuse headache has been reported with sumatriptan and may necessitate withdrawal of the drug. Sumatriptan has occasionally been associated with minor disturbances in liver function. There have also been rare reports of seizures with sumatriptan. Hypersensitivity reactions ranging from skin rashes to, more rarely, anaphylaxis have occurred. Transient pain at the injection site is common after subcutaneous sumatriptan injections; stinging, burning, erythema, bruising, and bleeding have also been reported. Irritation of the nasal mucosa and throat and epistaxis have been reported after intranasal use.
Effects on the cardiovascular system.
Pain or tightness in the chest or anginal pain mostly associated with oral sumatriptan.
Patient with hypertrophic obstructive m developed ventricular fibrillation a few hours after the onset of chest pain and this led to fatal cardiac arrest.
Effects on the cerebrovascular system.
Cerebral vasospasm has also been reported with the use of oral sumatriptan.
Effects on the gastrointestinal tract.
Reaction to sumatriptan such as ischaemic colitis, mesenteric ischaemia and Oesophageal constriction or throat tightness have been reported in sumatriptan.
Effects on the respiratory system.
Hypersensitivity. Reactions to sumatriptan such as skin rashes and, more rarely, anaphylaxis, and urticaria.
Medication-overuse headache.
Sumatriptan may have a similar risk of misuse to that associated with analgesics and ergotamine compounds in patients with medication-overuse headache.
Sumatriptan is more likely to be associated with dysphoria and apathetic sedation.

Sumatriptan and other serotonin (5-HT1) agonists (such as naratriptan, rizatriptan, zolmitriptan) should not be given with ergotamine or related compounds (including methysergide) since there is an increased risk of vasospastic reactions. In addition, a delay is advised before starting a serotonin (5-HT1) agonist in patients who have been receiving ergotamine or related compounds: sumatriptan should not be given until at least 24 hours after stopping the use of preparations containing ergotamine. Serotonin (5-HT1) agonists should not be given together. Sumatriptan should not be used with, and for 2 weeks after stopping, an MAOI. Use with the selective monoamine oxidase type B inhibitor selegiline is thought unlikely to provoke an interaction. St John's Wort (Hypericum perforatum). Taking herbal remedies that contain St. John's Wort together with Sutrip may make side effects more likely. Oral sumatriptan appeared to delay gastric emptying and might affect the absorption of other drugs, as judged by its delaying effect on paracetamol absorption in migraine patients.

Store at temperatures not exceeding 30°C. Protect from light.
Shelf-life: 2 years from manufacturing date.

Antimigraine Preparations

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

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