Imigran 50 mg 6 tablets

Imigran Sumatriptan Tablets Qualitative and Quantitative Composition Tablets contain 50 or 100 mg of sumatriptan base as the succinate salt. Pharmaceutical Form Imigran 50 mg tablets are pink, film-coated tablets, engraved with "GXES3" on one side and plain on the other, or plain on one side and engraved with "50" on the other. Imigran 100 mg tablets are white or off-white, film-coated tablets, engraved with "GXET2" on one side and plain on the other, or plain on one side and engraved with "100" on the other. Clinical Features Indications Imigran tablets are indicated for the acute relief of migraine attacks with or without aura, including the treatment of acute migraine attacks associated with the menstrual period in women. Dosage and Administration Imigran is not for prophylactic use. Overdose of Imigran is not recommended. Sumatriptan should be taken as soon as possible after the onset of migraine headache. It is equally effective at any stage of the attack. Populations Adults The recommended dose of oral Imigran is a single 50 mg tablet. Some patients may require 100 mg. If a patient does not respond to the first dose of Imigran, a second dose should not be taken for the same attack. Imigran tablets may be taken for subsequent attacks. If a patient responds to the first dose but symptoms recur, a second dose may be taken, provided there is an interval of at least two hours between doses and the total dose does not exceed 300 mg in a 24-hour period. Tablets should be swallowed whole with water. Children and Adolescents (under 18 years of age) The efficacy of sumatriptan tablets in this population has not been demonstrated (see Clinical Studies). Elderly (over 65 years of age) Experience with the use of sumatriptan tablets in patients over 65 years of age is limited. Pharmacokinetic parameters do not differ significantly from younger populations, however, until further clinical data become available, the use of Imigran in patients over 65 years of age is not recommended. For the treatment of acute migraine attacks, also see: Migralgin - Migralgin 50 mg 10 tablets Contraindications - Hypersensitivity to the active substance or to any of the excipients; - Imigran should not be used in patients who have had myocardial infarction or have ischemic heart disease (IHD), Prinzmetal's angina/coronary vasospasm, peripheral arterial disease or in patients with symptoms and signs of IHD; - Imigran should not be used in patients who have a history of stroke (cerebrovascular accident (CVA) or transient ischemic attack (TIA); - Imigran is contraindicated in uncontrolled hypertension; - Imigran should not be administered to patients with severe hepatic impairment; - Concomitant use of ergotamine or its derivatives (including methysergide) is contraindicated (see Interactions); - Concomitant use of monoamine oxidase inhibitors (MAOIs) and Imigran is contraindicated. Imigran should not be used within two weeks of discontinuation of MAOI therapy. Warnings and Precautions Imigran should only be used when there is a clear diagnosis of migraine. Imigran is not indicated for hemiplegic, basilar or ophthalmoplegic migraine. Before initiating treatment with Imigran, attention should be paid to exclude potentially serious neurological conditions (e.g., CVA, TIA) when the patient has atypical symptoms or has not been diagnosed with a condition for which Imigran is indicated. Transient symptoms including pain and a feeling of tightness in the chest, which may be severe and involve the throat, may occur following the use of Imigran (see Side Effects). In cases where these symptoms are likely to indicate IHD, appropriate investigation should be undertaken. In patients in whom cardiac disease is suspected, Imigran should not be administered without a prior cardiovascular assessment. Such patients include women with risk factors for coronary artery disease in the post-menopausal period, men over 40 years of age. However, these assessments may not identify all patients with cardiac disease and, in very rare cases, severe cardiac events have occurred in patients without underlying cardiovascular disease. Imigran should be used with caution in patients with controlled hypertension, as a transient increase in blood pressure and peripheral vascular resistance has been observed in a small proportion of patients. Rare post-marketing cases of serotonin syndrome (including mental status changes, autonomic instability and neuromuscular abnormalities) have been reported following the administration of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. Serotonin syndrome has been reported following concomitant administration of triptans and serotonin-norepinephrine reuptake inhibitors (SNRIs). If concomitant use of Imigran and SSRIs/SNRIs is clinically warranted, the patient should be appropriately monitored (see Interactions). Concomitant administration of any other triptan/5-HT1 agonist with Imigran is not recommended. Imigran should be used with caution in patients with conditions that may significantly affect the absorption, metabolism or excretion of the drug, e.g. hepatic impairment (Child-Pugh grade A or B; see Pharmacokinetics – Special Populations) or renal impairment (see Pharmacokinetics). Imigran should be used with caution in patients with a history of epilepsy or with other risk factors that lower the seizure threshold. Patients who have established hypersensitivity to sulfonamides may have an allergic reaction following Imigran. Reactions can range from skin hypersensitivity to anaphylaxis. Evidence of cross-sensitivity is limited, however caution should be exercised when prescribing Imigran in such patients. Overuse of acute headache medication is associated with exacerbation of headache (medication overuse headache, MOH) in susceptible patients. Treatment may need to be discontinued. Interactions There is no evidence of interaction with propranolol, flunarizine, pizotifen or alcohol. Prolonged vasospastic reactions have been reported with concomitant use of ergotamine. As these effects are additive, 24 hours should elapse between the administration of any ergotamine-containing preparation and sumatriptan. Conversely, ergotamine-containing preparations should not be taken until six hours have passed after Imigran administration. Interactions may occur between Imigran and MAO inhibitors, therefore their concomitant use is contraindicated (see Contraindications). Rare post-marketing cases of serotonin syndrome have been reported (including mental status changes, autonomic instability and neuromuscular abnormalities) following the administration of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. Serotonin syndrome has been reported following concomitant administration of triptans and serotonin-norepinephrine reuptake inhibitors (SNRIs) (see Warnings and Precautions). Pregnancy and Lactation Pregnancy Caution is advised when assessing the possible benefit to the mother against the possible risk to the fetus. Post-marketing data from a large number of prospective pregnancy registries have confirmed pregnancy in 1,000 women exposed to sumatriptan. However, there is insufficient information to make a definitive conclusion, and the results did not show an increased frequency of congenital defects or a consistent pattern of congenital defects in women taking sumatriptan compared to the general population. Lactation Sumatriptan has been shown to be excreted in breast milk following subcutaneous administration. The exposure to the infant can be minimized if breastfeeding is avoided for 12 hours after taking the medication. Effects on Ability to Drive and Use Machines Drowsiness may occur as a result of migraine or sumatriptan treatment. Caution is advised in patients performing tasks that require alertness, e.g. driving or operating machinery. Side Effects Adverse events are listed by organ system class and frequency. Frequencies are defined as: very common (≥1/10), common (≥1/100 and <1/10), uncommon (≥1/1000 and <1/100), rare (≥1/10,000 and <1/1000) and very rare (<1/10,000) including isolated reports. Data from clinical trials were used for assessment. It should be noted that the background incidence was not taken into account in comparable groups. Post-marketing data indicate a higher reporting frequency than true frequency. Clinical Trial Data Nervous System Disorders Common: Dizziness, somnolence, sensory disturbances, including paraesthesia and hypoesthesia. Vascular Disorders Common: Transient increase in blood pressure occurring shortly after treatment, flushing. Respiratory, Thoracic and Mediastinal Disorders Common: Dyspnoea. Gastrointestinal Disorders Common: Nausea and vomiting occur in some patients, but the association with sumatriptan is not clear. Musculoskeletal and Connective Tissue Disorders The following symptom is usually transient and may be intense and occur in any part of the body, including the chest and throat: Common: Feeling of heaviness. General Disorders and Administration Site Conditions The following symptoms are usually transient and may be intense and occur in any part of the body, including the chest and throat: Common: Pain, sensations of heat or cold, sensations of pressure or tightness. The following symptoms are mostly mild to moderate and transient: Common: Feeling of weakness, fatigue. Investigations Very rare: Minor abnormalities in liver function tests have been reported. Post-Marketing Data Immune System Disorders Very rare: Hypersensitivity reactions ranging from skin hypersensitivity to anaphylaxis. Nervous System Disorders Very rare: Seizures, although some have been reported in patients with a history of seizures or predisposing concomitant conditions. They have also been reported in patients in whom no such predisposing factors were identified. Tremor, dystonia, nystagmus, scotoma. Eye Disorders Very rare: Squinting, diplopia, visual impairment, loss of vision (usually transient). However, visual disturbances may also develop during the migraine attack itself. Cardiac Disorders Very rare: Bradycardia, tachycardia, palpitations, cardiac arrhythmias, transient ischemic changes on ECG, coronary artery vasospasm, angina, myocardial infarction (see Contraindications, Warnings and Precautions). Vascular Disorders Very rare: Hypotension, Raynaud's phenomenon. Gastrointestinal Disorders Very rare: Ischemic colitis. Overdose Symptoms and Signs Doses above 400 mg were not associated with any other adverse effects than those listed above. Treatment In case of overdose, the patient should be monitored for at least 10 hours and standard supportive therapy should be administered if necessary. It is not known what effect hemodialysis or peritoneal dialysis has on sumatriptan plasma concentrations. Pharmacological Properties Pharmacodynamics ATC Code N02CC01 Mechanism of Action Pharmacotherapeutic group: Selective 5-HT1 receptor agonists. Sumatriptan is a selective vascular 5-hydroxytryptamine-1-(5-HT1D) receptor agonist which has no effect on other 5-HT receptor (5-HT2-7) subtypes. The vascular 5-HT1D receptor is predominantly found in the cranial blood vessels and causes vasoconstriction. In animals, sumatriptan selectively constricts the carotid arterial circulation but does not alter cerebral blood flow. The carotid arterial circulation supplies the extracranial and intracranial tissues such as the meningeal vasculature and the dilatation and/or oedema development in these vessels is thought to be the mechanism of migraine development in men. Furthermore, experimental data indicate that sumatriptan inhibits trigeminal nerve activation. Both these mechanisms contribute to the antimigraine action of sumatriptan in humans. Pharmacodynamic Effects Clinical response begins within 10-15 minutes following 6 mg subcutaneous injection, within 15 minutes following 20 mg intranasal administration and approximately 30 minutes following 100 mg oral dose or 25 mg rectal dose. Although the recommended dose of oral Imigran is 50 mg, migraine attacks vary in severity both within and between patients. Doses of 25-100 mg have shown greater efficacy than placebo in clinical trials, but 25 mg is statistically significantly less effective than 50 and 100 mg. Imigran is effective for the acute treatment of migraine, including migraine associated with menstruation. Pharmacokinetics The pharmacokinetics of sumatriptan are not significantly affected by migraine attacks. Absorption Following oral administration, sumatriptan is rapidly absorbed, with peak concentrations occurring at 45 minutes, with 70% of the maximum concentration. The mean peak plasma concentration following a 100 mg dose is 54 ng/ml. The mean absolute oral bioavailability is 14%, due in part to presystemic metabolism and in part to incomplete absorption. Distribution Plasma protein binding is low (14-21%); the mean total volume of distribution is 170 L. Metabolism The main metabolite, indole acetic acid, a sumatriptan analogue, is primarily excreted in the urine, where it is present as the free acid and as a glucuronide conjugate. It is not known to have 5-HT1 or 5-HT2 activity. Minor metabolites have not been identified. Elimination The elimination half-life is approximately 2 hours. The mean total plasma clearance is approximately 1,160 ml/min and the mean renal plasma clearance is approximately 260 ml/min. Non-renal clearance accounts for approximately 80% of total clearance. Sumatriptan is primarily eliminated by oxidative metabolism, which is mediated by monoamine oxidase A. Special Populations Hepatic Impairment Following oral administration, presystemic clearance is reduced in patients with hepatic impairment, leading to increased plasma levels of sumatriptan (see Warnings and Precautions). Clinical Studies The safety and efficacy of standard sumatriptan tablets were evaluated in placebo-controlled clinical trials in over 650 children and adolescents aged 10 to 17 years with migraine. These studies failed to demonstrate a statistically significant difference in headache relief between placebo and any dose of sumatriptan group within two hours. The profile of adverse events for oral sumatriptan in children and adolescents aged 10-17 years from the studies was similar to that observed in the adult population. Preclinical Safety Data Carcinogenesis/Mutagenesis Sumatriptan had no genotoxic or carcinogenic effects in in vitro systems and animal studies. Reproductive Toxicology In a rat fertility study, oral doses of sumatriptan caused plasma levels approximately 200 times those observed in humans following a 100 mg oral dose and were associated with a reduction in successful fertilization. This effect was not observed in a subcutaneous injection study where peak plasma levels were approximately 150 times those observed in humans following oral dosing. Pregnancy and Lactation Teratogenic effects were not observed in rats or rabbits and sumatriptan had no effect on postnatal development in rats. When administered to pregnant rabbits during organogenesis, sumatriptan caused embryolethality in some instances at doses high enough to cause maternal toxicity. Pharmaceutical Particulars List of Excipients 50 mg Lactose (monohydrate) Lactose (anhydrous) Microcrystalline cellulose Croscarmellose sodium Magnesium stearate Purified water 100 mg Lactose (monohydrate) Microcrystalline cellulose Croscarmellose sodium Magnesium stearate Purified water Incompatibilities None described. Shelf Life Shelf life is indicated on the packaging. Special Storage Conditions Imigran tablets should be stored at a temperature not exceeding 30°C. Container Form and Contents Imigran 50 mg tablets are packed in PVC/aluminium foil blisters or PVC-aluminium/paper child-resistant foil blisters. Imigran 100 mg tablets are packed in PVC/aluminium foil blisters or PVC-aluminium/paper child-resistant foil blisters. Instructions for Use/Consumption Not provided. Not all pack sizes may be marketed in all countries. Dispensing Category: Pharmaceutical Product Group II, dispensed with Form No. 3 prescription.