Testosterone undecanoate is rapidly and well absorbed. Food intake has no clinically significant effect on its bioavailability, which is about 80%. Connection with the plasma protein-13-17%. Average distribution. This figure depends on the floor; in women, these values are 50% of the values observed in men, which is associated with a higher content of fat tissue in women.Metabolized about 20% of topiramate.
Up to 50% of topiramate is metabolized in patients concurrently taking other anti-epileptic drugs ) that induce metabolizing enzymes. From the plasma, urine and feces identified six human practically inactive metabolites topiramate. Unmodified topiramate and its metabolites are mainly excreted through the kidneys. Plasma clearance of about 20-30 ml / min. After a single dose, it is linear pharmacokinetics andriol testocaps, plasma clearance is constant, and the area under the curve “concentration / time” in doses ranging from 100 to 400 mg increases proportionally with dose. In normal kidney function, patients may require 4-8 days to reach equilibrium plasma concentrations. The average value of the maximum concentration after repeated oral administration of 100 mg twice a day topiramate is 6.76 g / ml.
In patients with impaired renal function (creatinine clearance <60 mL / min) reduced plasma and renal clearance of topiramate; in patients with end-stage renal failure, reduced plasma clearance of topiramate. Plasma testosterone undecanoate clearance of topiramate is unchanged in elderly patients, in the absence of violations of certain functions of the kidneys. Plasma clearance of topiramate is decreased in patients with moderate and severe hepatic impairment. The pharmacokinetics of topiramate in children, as is linear in adults.Clearance does not depend on the drug dose andriol tc, the equilibrium concentration in the plasma increases proportionally with dose. However, children have higher values of clearance and a shorter half-life.Consequently, the concentration of topiramate in plasma when receiving identical doses per kg body weight may be lower in children compared with adults. Topiramate is effectively cleared from the blood plasma by hemodialysis. Presumably it passes into breast milk.
- monotherapy of epilepsy in children of 7 years and adults (including patients with newly installed epilepsy);
- adjuvant therapy in children from 3 years and adults with lack of effectiveness of AEDs first choice for partial or generalized tonic-clonic seizures, as well as seizures in the background Lennox-Gastaut syndrome.Contraindications
- hypersensitivity to any component of the drug;
- Children under 3 years of age;
- pregnancy and lactation.Precautions: renal or hepatic impairment, nefrourolitiaz (including past or family history), hypercalciuria.
Dosing and Administration General Inside, swallowing the tablet whole without chewing, regardless of the meal. For optimal control of seizures, it is recommended to start treatment with low doses with a subsequent increase to the effective dose.
- In the complex therapy of adults: minimum effective dose of 200 mg / day. The usual daily dose of 200-400mg (2 receptions). The maximum daily dose of 1600 mg. Treatment starts with 25-50 mg daily at bedtime for one week. The dose was then increased to 25-50 mg per day for 1-2 weeks, with a multiplicity of receiving two times a day. At intolerance of such a dosing regimen, the dose is increased by a smaller amount, or over large intervals. The dose and dosing frequency is adjusted depending on the clinical effect. Children over 3 years: the recommended daily dose is 5-9 mg / kg body weight, divided into 2 doses. Treatment started with a dose of 25 mg at bedtime for one week. The dose was then increased by 1 -3 mg / kg / day for 1 to 2 weeks, with a multiplicity of receiving two times a day, to achieve optimal clinical effect.
- Monotherapy Adults: treatment is initiated testosterone undecanoate with 25 mg at bedtime for one week. The dose was then increased to 25-50 mg per day for 1-2 weeks, with a multiplicity of receiving two times a day. At intolerance of such a dosing regimen novorapid flexpen, the dose is increased by a smaller amount, or over large intervals. The dose and dosing frequency is selected depending on the clinical effect. The recommended starting dose of topiramate monotherapy in adults with newly diagnosed epilepsy is 100 mg / day, the maximum recommended dose – 500 mg / day. These doses are recommended for all adults, including the elderly with normal renal function. Children from 7 years: treatment begins with a dose of 0.5-1 mg / kg body weight per night for 1 week. The dose was then increased by 0.5-1 mg / kg / day for 1-2 weeks, the dosing frequency – 2 times a day. At intolerance of such a dosing regimen, the dose is increased by a smaller amount, or over large intervals. The dose and dosing frequency is selected depending on the clinical effect. The recommended dose range 6.3 mg / kg body weight. Children with recently established partial seizures can be assigned up to 500 mg per day.