Topiramate

When ATH:
N03AX11

Characteristic.

The white crystalline powder bitter taste. It is soluble in acetone, xloroforme, dimethyl sulfoxide, ethanol.

Pharmacological action.
Antiepileptic.

Application.

The partial or generalized tonic-clonic seizures in monotherapy or in combination with other anticonvulsants; adjunctive therapy in the treatment of seizures, связанных с синдромом Леннокса — Гасто (in adults and children); newly diagnosed epilepsy (in adults and children older than 2 years).

Contraindications.

Hypersensitivity.

Restrictions apply.

Pregnancy, lactation, childhood (safety and efficacy in children under 2 years to be determined).

Pregnancy and breast-feeding.

Maybe, if the effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies on the use during pregnancy has not been). At the time of treatment should stop breastfeeding.

Side effects.

From the nervous system and sensory organs: fatigue, ataxia, impaired thinking and concentration, emotional lability, confusion, dizziness, paraesthesia, gipesteziya, drowsiness; редко — возбуждение, amnesia, afazija, depression, diplopia and other visual disturbances, conjunctivitis, nistagmo, speech disorder, perversion of taste sensations.

From the digestive tract: anorexia, gingivitis, nausea.

Other: weight loss, abdominal pain, chills, leukopenia, dyspnoea, edema, nose bleed, nephrolithiasis, hematuria, prurit, tynnyt, dysmenorrhoea, the weakening of the libido, impotence.

Cooperation.

Phenytoin and carbamazepine, topiramate lowers blood. Topiramate umenyshaet AUC digoxin (on 12%), phenytoin levels in plasma and the effectiveness of oral contraceptives. The simultaneous use of drugs, predisposing to nephrolithiasis, may increase the risk of kidney stones.

Overdose.

Symptoms: increased side effects.

Treatment: gastric lavage or induction of vomiting, maintenance therapy. In severe cases, hemodialysis may.

Dosing and Administration.

Inside (regardless of the meal). Adults with monotherapy: the initial dose - 25 mg 1 once a day (for the night) during 1 Sun, затем дозу увеличивают на 25–50 мг/сут (divided into 2 admission) every 1-2 weeks until clinical effect; the recommended dose - 100 mg / day, maximum daily - 500 mg (для некоторых пациентов с рефрактерными формами эпилепсии — до 1000 mg / day). Children over 2 years: в первую неделю лечения — 0,5–1 мг/кг на ночь, затем дозу увеличивают на 0,5–1 мг/кг/сут (divided into 2 admission) with an interval of 1-2 weeks; рекомендуемые дозы — 3–6 мг/кг/сут (для детей с недавно диагностированными парциальными припадками — до 500 mg / day).

In combination with other anticonvulsants: взрослым — 25–50 мг на ночь в течение 1 Sun, затем дозу увеличивают на 25–50 мг с интервалом 1–2 нед и принимают в 2 admission; минимальная эффективная доза — 200 mg / day, средняя суточная — 200–400 мг, maximum - 1600 mg. Children over 2 years: — 1–3 мг/кг/сут на ночь в течение 1 Sun, затем дозу увеличивают на 1–3 мг/кг с интервалом 1–2 нед и принимают в 2 admission; рекомендуемая суточная доза — 5–9 мг/кг.

Precautions.

Patients, hemodialysis, in the days of the meeting should be given an additional dose (about 1/2 daily dose) before and after treatment. The abolition of a gradually, уменьшая дозу на 100 mg weekly intervals.

In patients with an increased risk of nephrolithiasis recommended adequate increase fluid intake. To use caution in patients with impaired liver function (due to a possible decrease in clearance of topiramate). There are cases of secondary angle-closure glaucoma in children and adults. In the event of a significant loss of body weight in the treatment of topiramate the need to strengthen the power or the use of food additives.

Should not be used during the drivers of vehicles and people, skills relate to the high concentration of attention. Do not take with alcohol or drugs, CNS depressants.

Cooperation

Active substance	Description of interaction
Aцetazolamid	FMR. It increases the risk of kidney stones. Combined use not recommended.
Buspirone	FMR. Strengthens (mutually) CNS depression.
Haloperidol	FMR. May reduce the seizure threshold (require dose adjustment). Strengthens (mutually) CNS depression.
Gidroxlorotiazid	FKV. Increases (a third) maximum blood level (FROMmax) and area under the concentration curve (АUC).
Digoxin	FKV. Against the background of topiramate decreases AUC.
Dorzolamid	FMR. It increases the risk of kidney stones. Combined use not recommended.
Droperidol	FMR. Strengthens (mutually) CNS depression.
Zolpidem	FMR. Strengthens (mutually) CNS depression.
Carbamazepine	FKV. Decreases (on 40%) concentration in the blood.
Quetiapine	FMR. Strengthens (mutually) CNS depression.
Ketamine	FMR. Strengthens (mutually) CNS depression.
Klozapyn	FMR. Strengthens (mutually) CNS depression.
Codeine	FMR. Strengthens (mutually) CNS depression.
Lorazepam	FMR. Strengthens (mutually) CNS depression.
Metformin	FKV. Decreases (mutually) plasma clearance. On the background of topiramate increases the average value of the maximum concentration and the area under the concentration curve.
Midazolam	FMR. Strengthens (mutually) CNS depression.
Morphine sulfate	FMR. Strengthens (mutually) CNS depression.
Oxazepam	FMR. Strengthens (mutually) CNS depression.
Olanzapine	FMR. Strengthens (mutually) CNS depression.
Perfenazyn	FMR. Strengthens (mutually) CNS depression.
Risperidone	FMR. Strengthens (mutually) CNS depression.
Tioridazin	FMR. Strengthens (mutually) CNS depression.
Trifluoperazine	FMR. Strengthens (mutually) CNS depression.
Phenytoin	FKV. Decreases (twice) concentration in the blood. Against the background of topiramate (угнетает изоформу цитохрома Р450 — CYP2CMap) may increase plasma levels and develop toxicity.
Phenobarbital	FMR. Strengthens (mutually) CNS depression.
Flufenazin	FMR. Strengthens (mutually) CNS depression.
Xlordiazepoksid	FMR. Strengthens (mutually) CNS depression.
Chlorpromazine	FMR. Strengthens (mutually) CNS depression.
Chlorprothixene	FMR. Strengthens (mutually) CNS depression.
Ethinylestradiol	FKV. FMR. Against the background of topiramate may decrease the contraceptive effect and increases the risk of "breakthrough" bleeding.