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| SUMATRIPTAN-HAKIM |
| :: Antimigraine :: |
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F.C. Tab. 50,100 mg |
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Pharmacologic category
Antimigraine agent ; Serotonin 5-HT 1D receptor agent
Mechanism of action
Although sumatriptan's mechanism of action has not been established , suppression of migraine headaches may result from sumatriptan –induced decreases in the firing of serotonergic (5-HT ) neurons. Specifically , it is thought that agonist activity at the 5- HT1D receptor subtype provides relief of acute headache . It has been proposed that constriction of cerebral blood vessels resulting from 5-HT1D receptor stimulation reduces the pulsation that may be responsible for the pain of vascular headaches . It has also been proposed that neurogenic inflammation in areas innervated by the trigeminal nerve may contribute to the development of migraine headaches ; there is some evidence that serotonergic mechanisms may be involved . Sumatriptan may also relieve migraines by decreasing release of neuropeptides and other mediators of inflammation and by reducing extravastion of plasma proteins.
Indications
Sumatriptan is indicated to relieve acute migraine headaches ( with or without aura ) in patients who do not obtain sufficient relief with analgesics . Sumatriptan also relieves the nausea , vomiting , photophobia , and phonophobia that frequently occur in association with migraine headaches . Sumatriptan is not recommended for long –term migraine prophylaxis and for treatment of basilar artery migraine or hemiplegic migraine.
Side/Adverse effects
Dizziness; Flushing ; Weakness ; Drowsiness ; Lightheadedness ; Fatigue ; Nausea; Vomiting ; Pain or sensations of tingling , heaviness , heat , pressure , or tightness in chest and/or neck ; Hypotension ; Bradycardia or tachycardia ; Palpitations ; Visual disturbances ; Minor disturbances in liver function ; Seizures ; Skin rashes ; Anaphylaxis ; Muscle aches , cramps , or stiffness ; Anxiety
Contraindications
Hypersensitivity to sumatriptan or any component of the formulation ; Patients with ischemic heart disease ; Cerebrovascular syndromes ; Peripheral vascular syndromes ( including ischemic bowel disease ) ; Uncontrolled hypertension ; Use within 24 hours of ergotamine derivatives ; Use within 24 hours of another 5-HT1 agonist ; Concurrent administration or within 2 weeks of discontinuing a MAO inhibitor , specifically MAO type A inhibitors ; Management of hemiplegic or basilar migraine ; Prophylactic treatment of migraine ; Severe hepatic impairment.
Warnings / Precautions
Sumatriptan is indicated only in patients > or = 18 years of age with a clear diagnosis of migraine . Safety and efficacy in pediatric patients have not been established . Do not give to patients with risk factors for CAD until a cardiovascular evaluation has been performed . Use with caution in patients with history of seizure disorder or in patients with a lowered seizure threshold.
Pregnancy
FDA pregnancy category C . Adequate and well –controlled studies have not been done in pregnant women . Use only if potential benefit to the mother outweighs the potential risk to the fetus.
Breast–Feeding
Sumatriptan enters breast milk . Use with caution.
Drug Interactions
Ergot –containing drugs (dihydroergotamine , ergotamine or methysergide) prolong vasospastic reactions ; do not use sumatriptan with them within 24 hours of each other . MAO inhibitors type A (furazolidone , isocarboxazid , meclobemide , phenelzine , toloxatone , and tranylcypromine ) reduce sumatriptan clearance ; concurrent use is contraindicated ; wait at least 2 weeks after discontinuing MAO inhibitor type A to start sumatriptan . While not specifically contraindicated , combination with selegiline ( a selective MAO inhibitor type B) may best be avoided until further study . Concurrent use of sumatriptan with SSRIs ( fluoxetin , fluvoxamine , paroxetine , sertraline ) can lead to symptoms of hyper –reflexia , weakness , and incoordination ; careful monitoring is recommended . Use sumatriptan cautiously in patients receiving concomitant medications that can lower the seizure threshold.
Administration and dosage
- Usual adult dose: Oral , 25,50 or 100 mg as a single dose . If necessary , additional doses up to 100 mg may be taken at intervals of at least two hours , up to 200 mg a day . For relief of migraine headache that returns after an initial treatment with sumatriptan tablets : the dose may be repeated after two hours , up to a maximum of 200 mg once a day.
- Usual adult prescribing limits: Oral , not more than 200 mg in 24 hours.
- Usual pediatric dose: Safety and efficacy in patients up to 18 years of age have not been established.
How Supplied
Tablet 50 mg, 100 mg
Storage
Store between 2 and 30°C (36° F and 86° F)
References
- USP DI, 2004
- Up To Date, Vol. 13.1 (2005)
- Martindale, The Complete Drug Reference, 33 rd edition 2002
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