Indications of Etopira 50 mg
Epilepsy: Etopira 50 mg is indicated as monotherapy in adults and children aged 6 years and above with newly diagnosed epilepsy who have generalised tonic-clonic seizures or partial seizures with or without secondarily generalised seizures. Etopira 50 mg is indicated as adjunctive therapy ... Read moreEpilepsy: Etopira 50 mg is indicated as monotherapy in adults and children aged 6 years and above with newly diagnosed epilepsy who have generalised tonic-clonic seizures or partial seizures with or without secondarily generalised seizures. Etopira 50 mg is indicated as adjunctive therapy for adults and children over 2 years of age who are inadequately controlled on conventional first line antiepileptic drugs for partial seizures with or without secondarily generalised seizures; seizures associated with Lennox Gastaut Syndrome and primary generalised tonic-clonic seizures.Migraine: Etopira 50 mg is indicated in adults for the prophylaxis of migraine headache. Prophylactic treatment of migraine may be considered in situations such as: adults experiencing three or more migraine attacks per month; frequent migraine attacks that significantly interfere with the patient's daily routine. Continuing therapy should be reviewed every six months.
Adjunct anti-epileptic drugs
Etopira 50 mg is a sulfamate-substituted monosaccharide, related to fructose. Etopira 50 mg is quickly absorbed after oral use. Etopira 50 mg enhances GABA-activated chloride channels. In addition, Etopira 50 mg inhibits excitatory neurotransmission, through actions on kainate and AMPA receptors. Etopira 50 mg has a specific effect on GluR5 kainate receptors. It is also an inhibitor of carbonic anhydrase, particularly subtypes II and IV, but this action is weak and unlikely to be related to its anticonvulsant actions, but may account for the bad taste and the development of renal stones seen during treatment. Its possible effect as a mood stabilizer seems to occur before anticonvulsant qualities at lower dosages.
Dosage of Etopira 50 mg
Adults and children over 16 years: Titration should begin at 25 mg nightly for 1 week. The dosage should then be increased at 1- or 2-week intervals by increments of 25 or 59 mg/day, administered in two divided doses. The recommended initial target dose for Etopira 50 mg monotherapy in adults with newly diagnosed epilepsy is 100 mg/day and the maximum recommended daily dose is 400 mg.
Children aged 6-16 years: Treatment of children aged 6 years and above should begin at 0.5 to 1 mg/kg nightly for the first week. The dosage should then be increased at 1- or 2-week intervals by increments of 0.5 to 1 mg/kg/day, administered in two divided doses. The recommended initial target dose range for Etopira 50 mg monotherapy in children with newly diagnosed epilepsy aged 6 years and above is 3 to 6 mg/kg/day. Higher doses have been tolerated and rarely doses up to 16 mg/kg/day have been given.
Epilepsy: Adjunctive therapy:
Adults and children over 16 years: The minimal effective dose as adjunctive therapy is 200 mg per day. The usual total daily dose is 200 mg to 400 mg in two divided doses. Some patients may require doses up to 800 mg per day, which is the maximum recommended dose.
Children aged 2-16 years: The recommended total daily dose of Etopira 50 mg as adjunctive therapy is approximately 5 to 9 mg/kg/day in two divided doses. Titration should begin at 25 mg nightly for the first week. The dosage should then be increased at 1- or 2-week intervals by increments of 1 to 3 mg/kg/day (administered in two divided doses), to achieve optimal clinical response. Dose titration should be guided by clinical outcome. Daily doses up to 30 mg/kg/day have been studied and were generally well tolerated.
Adults and children over 16 years: Titration should begin at 25 mg nightly for 1-week. The dosage should then be increased in increments of 25 mg/day administered at 1-week intervals. The recommended total daily dose of Etopira 50 mg as treatment for the prophylaxis of migraine headache is 100 mg/day administered in two divided doses. Some patients may experience a benefit at a total daily dose of 50 mg/day.
Children: Etopira 50 mg in migraine prophylaxis has not been studied in children under 16 years.
Administration of Etopira 50 mg
Etopira 50 mg tablets can be taken without regards to meals.
Interaction of Etopira 50 mg
The addition of Etopira 50 mg to other antiepileptic drugs (phenytoin, carbamazepine, valproic add, phenobarbitai, primidone) has no clinically significant effect on their steady-state plasma concentrations, except in some patients where the addition of Etopira 50 mg to phenytoin may result in an increase of plasma concentrations of phenytoin.CNS Depressants: Etopira 50 mg should be used with caution if used in combination with alcohol and other CNS depressants.Oral Contraceptives: In an interaction study with a combined oral contraceptive, Etopira 50 mg increased plasma clearance of the oestrogenic component significantly. Consequently, and bearing in mind the potential risk of teratogenicity, patients should receive a preparation containing not less than 50 μg of oestrogen or use some alternative non-hormonal method of contraception. Patients taking oral contraceptives should be asked to report any change in their bleeding patterns.Lithium: In patients with bipolar disorder, the pharmacokinetics of lithium were unaffected during treatment with Etopira 50 mg at doses of 200 mg/day; however, there was an observed increase in systemic exposure (26% for AUC) following Etopira 50 mg doses of up to 600 mg/day. Lithium levels should be monitored when co-administered with Etopira 50 mg.Hydrochlorothiazide (HCTZ): The steady-state pharmacokinetics of HCTZ were not significantly influenced by the concomitant administration of Etopira 50 mg. Clinical laboratory results indicated decreases in serum potassium after Etopira 50 mg or HCTZ administration, which were greater when HCTZ and Etopira 50 mg were administered in combination.Metformin: Etopira 50 mg did not affect metformin tmax. The clinical significance of the effect of Etopira 50 mg on metformin pharmacokinetics is unclear. Oral plasma clearance of Etopira 50 mg appears to be reduced when administered with metformin. The clinical significance of the effect of metformin on Etopira 50 mg pharmacokinetics is unclear. When Etopira 50 mg is added or withdrawn in patients on metformin therapy, careful attention should be given to the routine monitoring for adequate control of their diabetic disease state.Pioglitazone: When Etopira 50 mg is added to pioglitazone therapy or pioglitazone is added to Etopira 50 mg therapy, careful attention should be given to the routine monitoring of patients for adequate control of their diabetic disease state.Glibenclamide: The steady-state pharmacokinetics of Etopira 50 mg were unaffected by concomitant administration of glibenclamide. When Etopira 50 mg is added to glibenclamide therapy or glibenclamide is added to Etopira 50 mg therapy, careful attention should be given to the routine monitoring of patients for adequate control of their diabetic disease state.Others: Etopira 50 mg, when used concomitantly with other agents predisposing to nephrolithiasis, may increase the risk of nephrolithiasis. While using Etopira 50 mg, agents like these should be avoided since they may create a physiological environment that increases the risk of renal stone formation. The interaction with benzodiazepines has not been studied. Valproic Acid: Concomitant administration of Etopira 50 mg and valproic acid has been associated with hyperammonemia with or without encephalopathy in patients who have tolerated either drug alone. An association of hyperammonemia with Etopira 50 mg monotherapy or concomitant treatment with other anti epileptics has not been established.
Hypersensitivity to any component of this product.
Side Effects of Etopira 50 mg
Nausea, abdominal pain, dyspepsia, diarrhoea, dry mouth, taste disturbance, weight loss, anorexia, paraesthesia, hypoaesthesia, headache, fatigue, dizziness, speech disorder, drowsiness, insomnia, impaired memory & concentration, anxiety, depression, visual disturbance, lesscommonly: sucidal ideation, rarely: reduced sweetening mainly children, metabolic acidosis and alopecia, very rarely: Leucopenia, thrombocytopenia and serious skin reaction.
Pregnancy & Lactation
Etopira 50 mg is pregnancy category C. So it may be given only if clearly needed and after the assessment of risk benefit ratio. It is not known whether Etopira 50 mg is excreted through breast milk. So caution should be taken if it is prescribed to a breast feeding mother.
Precautions & Warnings
In patients with or without a history of seizures or epilepsy, antiepileptic drugs, including Etopira 50 mg, should be gradually withdrawn to minimize the potential for seizures or increased seizure frequency. Etopira 50 mg can produce central nervous system-related adverse events and may be more sedative than other antiepileptic drugs. Drowsiness is a likelihood. In addition, there have been reports of visual disturbances/blurred vision. Patients should be warned of these and advised that if affected, they should not drive, operate machinery and/or take part in activities where such reactions could put themselves or others at risk.
Overdose Effects of Etopira 50 mg
Etopira 50 mg overdose can result in severe metabolic acidosis. In acute Etopira 50 mg overdose, if the ingestion is recent, the stomach should be emptied immediately by lavage or by induction of emesis. Activated charcoal has been shown to adsorb Etopira 50 mg in vitro. Treatment should be appropriately supportive. Haemodialysis has been shown to be an effective means of removing Etopira 50 mg from the body. The patient should be well hydrated.
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Use In Special Populations
Patients with Renal Impairment: In renally impaired subjects (creatinine clearance less than 70 ml/min/1.73 m2), one-half of the usual adult dose is recommended. Such patients will require a longer time to reach steady-state at each dose.Patients Undergoing Hemodialysis: Etopira 50 mg is cleared by hemodialysis at a rate that is 4 to 6 times greater than a normal individual. Accordingly, a prolonged period of dialysis may cause Etopira 50 mg concentration to fall below that required to maintain an anti-seizure effect.To avoid rapid drops in Etopira 50 mg plasma concentration during hemodialysis, a supplemental dose of Etopira 50 mg may be required. The actual adjustment should take into account 1) the duration of dialysis period, 2) the clearance rate of the dialysis system being used, and 3) the effective renal clearance of Etopira 50 mg in the patient being dialyzed.
Adjunct anti-epileptic drugs
Mode Of Action
A seizure is an abnormal and unregulated electrical discharge occurring in the brain. This leads to a transient interruption in brain function, manifested by reduced alertness, abnormal sensations, and focal involuntary movements or convulsions. Several types of seizures exist, with common types including tonic-clonic seizures and partial onset seizures.The exact mechanisms by which Etopira 50 mg exerts pharmacological actions on seizures and migraines are currently not fully characterized. Several properties of this drug, however, are likely to contribute to its therapeutic effects. Etopira 50 mg has been observed to exert actions on voltage-dependent sodium channels, GABA receptors, and glutamate receptors.Etopira 50 mg stimulates GABA-A receptor activity at brain non-benzodiazepine receptor sites and reduces glutamate activity at both AMPA and kainate receptors. Normally, GABA-A receptors are inhibitory and glutaminergic receptors are stimulatory for neuronal activity. By increasing GABA activity and inhibiting glutamate activity, Etopira 50 mg blocks neuronal excitability, preventing seizures and migraines. Additionally, it blocks the voltage-dependent sodium channels, further blocking seizure activity. Etopira 50 mg has been shown to inhibit various carbonic anhydrase isozymes, but the clinical significance of this is unknown at this time.
Etopira 50 mg should not be used during pregnancy unless, in the opinion of the physician, the potential benefit outweighs the potential risk to the foetus. Etopira 50 mg should not be used during breastfeeding.