Roliten tabs 2mg #30

Roliten instruction for use

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Composition

Each film-coated tablet contains:
Active ingredient: tolterodine tartrate - 2 mg
Excipients: Microcrystalline cellulose, calcium phosphate, sodium carboxymethyl starch (Type A), colloidal silicon dioxide, magnesium stearate.
Shell: Opadry white dye (OY-S-58910) *, purified water **.
* - hypromellose, titanium dioxide, macrogol 400, talc ** - evaporates during production

Description

Round, biconvex tablets of white to almost white color film-coated.
Pharmacotherapeutic group:
m-holinoblokator
ATX Code: G04BD07

pharmachologic effect

Antagonist of m-cholinergic receptors localized in the bladder and salivary glands. Reduces the contractile function of the bladder and reduces salivation. Causes incomplete emptying of the bladder, increases the amount of residual urine and reduces the pressure of the detrusor. The persistent therapeutic effect of tolterodine is achieved after 4 weeks. Tolterodine and its active metabolite 5-hydroxymethyl are highly specific for muscarinic receptors, have selectivity for bladder receptors (compared to receptors for the salivary glands).

Pharmacokinetics

Suction

After taking Roliten inside, tolterodine is rapidly absorbed from the gastrointestinal tract. The maximum concentration (Сmax) in serum is reached in 1-3 hours. The Cmax value increases in proportion to the dose of tolterodine in the range from 1 to 4 mg. The absolute bioavailability of tolterodine is 65% in persons with reduced metabolism (deprived of CYP2D6) and 17% in persons with increased metabolism (most patients).
Food does not affect the exposure of unbound tolterodine and the active 5-hydroxymethyl metabolite in individuals with increased metabolism, although the level of tolterodine increases when it is taken with meals.

Distribution

Equilibrium concentration is achieved within 2 days. The volume of distribution of tolterodine - 113 liters.

Metabolism

Tolterodine is mainly metabolized in the liver using the CYP2D6 polymorphic enzyme to form a pharmacologically active 5-hydroxymethyl metabolite. Further metabolism leads to the formation of 5-carboxylic acid and its N-dealkylated metabolites.
In persons with reduced metabolism (deprived of CYP2D6), tolterodine is not metabolized to the active 5-hydroxymethyl metabolite, but undergoes dealkylation by CYP2D6 isoenzymes With the formation of N-dealkylated tolterodine. not having pharmacological activity.
Tolterodine and 5-hydroxymethyl metabolite bind predominantly to orosomucoid; unbound fractions are 3.7% and 36%, respectively.

Excretion

The systemic clearance of tolterodine in individuals with increased metabolism is about 30 l / h, and the half-life (T1 / 2) is 2-3 hours. T1 / 2 5-hydroxystyrene metabolite is 3-4 hours. After 14C-tolterodine is injected, approximately 77% of the radioactive label is excreted in the urine and 17% in the feces, with less than 1% in an unchanged form and about 4% in the form of an active metabolite. The carboxylated metabolite and the corresponding dealkylated metabolite constitute about 51% and 29% of the amount that is excreted in the urine.

Pharmacokinetics in special clinical situations

Reduced clearance and T1 / 2 lengthening (up to 10 hours) of tolterodine in individuals with reduced metabolism leads to an increase in its concentration (approximately 7 times) against the background of non-detectable concentrations of 5-hydroxymethyl metabolite. As a result, the area under the concentration / time curve (AUC) of tolterodine in individuals with reduced metabolism is close to the sum of the AUC values ​​of tolterodine and its active 5-hydroxymethyl metabolite in patients with increased metabolism with the same dosing regimen. Consequently, the safety, tolerability and clinical effect of Roliten are the same, regardless of the phenotype.
The AUC value of tolterodine and its active 5-hydroxymethyl metabolite increases approximately 2 times in patients with cirrhosis of the liver.

Indications for use

Hyperreflexia (hyperactivity, instability) of the bladder, manifested by frequent, imperative urination and / or incontinence.

Contraindications

Hypersensitivity, urinary retention, angle-closure glaucoma (not amenable to treatment), myasthenia, ulcerative colitis, megacolon, pregnancy, lactation, childhood.

Carefully

Obstruction of the urinary tract, obstructive lesions of the gastrointestinal tract, neuropathy, irreducible hernia.

Dosage and administration

Roliten is administered orally 2 mg 2 times a day. With hepatic and / or renal failure, as well as in the case of side effects, the dose is reduced to 1 mg 2 times a day.
After 6 months, the need for further treatment should be assessed.

Side effect of Roliten

Side effects associated with anticholinergic action: often (more than 10%), dry mouth; not often (1 - 10%) - disturbance of accommodation, reduced tearing (xerophthalmia), dry skin; rarely (less than 1%) - urinary retention.
On the part of the digestive system: not often (1-10%) - dyspepsia, constipation, abdominal pain, flatulence, vomiting; rarely (less than 1%) - gastroesophageal RSflux.
From the side of the central nervous system and peripheral nervous system: not often (1-10%) - headache, dizziness, drowsiness, nervousness, paresthesias; rarely (less than 1%) - impaired consciousness.
Other: not often (1-10%) - weakness, fatigue, weight gain, rarely (less than 1%) - chest pain, allergic reactions, flushing to the skin of the face.

Overdose

The highest dose that volunteers received was 12.8 mg of tolterodine L-tartrate per dose.
The most important symptoms noted in this case were disturbances of accommodation and painful urge to urinate. Hallucinations, severe agitation, convulsions, respiratory failure, tachycardia, urinary retention, dilated pupils are possible.
Treatment: gastric lavage, the appointment of activated carbon, symptomatic therapy: with pronounced central anticholinergic effects (including hallucinations) - physostigmine: with convulsions or marked arousal - benzodiazepines; with tachycardias - beta-blockers; in respiratory failure - artificial respiration: during urinary retention - catheterization; with dilated pupils - pilocarpine in the form of eye drops and / or transfer of the patient into a dark room.

Drug interaction

With the combined use of Roliten with other drugs with anticholinergic properties, it is possible to enhance the therapeutic effect and undesirable effects.
With simultaneous use of Roliten with m-cholinomimetics, the therapeutic effect of the drug may be reduced.
With the combined use of Roliten with metoclopramide and cisapride, the effects of the latter can be weakened.
Perhaps the pharmacokinetic interaction with other drugs that are metabolized by the cytochrome P450 system (CYP2D6 or CYP3A4) or inhibit them. However, the combined use of rolithen with fluoxetine (a strong CYP2D6 inhibitor that is metabolized to norfluoxetine, which is a CYP3A4 inhibitor) only leads to a slight increase in the total AUC of tolterodine and its active 5-hydroxymethyl metabolite, which does not cause clinically significant interaction.
Simultaneous treatment with strong CYP3A4 inhibitors, such as macrolide antibiotics (erythromycin and clarithromycin) or antifungal agents (ketoconazole, itraconazole and miconazole) should be avoided.
When conducting clinical trials, it was established that Roliten does not interact with warfarin or combined oral contraceptives (containing ethinyl estradiol / levonorgestrel).
A clinical study using metabolic probes did not give any indication that tolterodine is able to inhibit the activity of CYP2D6, CYP2C19, CYP3A4 or CYP1A2.

special instructions

Before starting treatment, organic causes of frequent and imperative urination should be eliminated.
Roliten is not recommended to be prescribed to children, because at present the safety and efficacy of the use of Roliten in this category of patients has not been studied. Women of childbearing age should use reliable methods of contraception during Rolitten therapy.
Influence on ability to driving of the car and control of mechanisms
Since Roliten can cause accommodation disturbances and decrease the speed of psychomotor reactions, the question of the possibility of practicing potentially hazardous activities should be solved only after evaluating the patient's individual response to the drug.

Release form

On 10 tablets in the blister from aluminum foil / PVC / PVdH. 3 or 6 blisters with the application instruction in a cardboard pack.

Storage conditions

Store in a dry place at a temperature not higher than 25 ° C.
Keep out of the reach of children.
Shelf life - 4 years.
Do not use later than the date indicated on the package.

Pharmacy sales terms

You can buy Roliten without a prescription.