Included in the formulation
АТХ:G.04.B.D.11 Fesoterodine
Pharmacodynamics:Selectively and competitively blocks m-holinoretseptory subtype M3, located on the smooth muscle cells of the bladder, has an antispasmodic effect, reduces the number of urination and episodes of imperative urinary incontinence, increases the average volume with urination.
Pharmacokinetics:After oral administration, regardless of the time of ingestion, up to 52% is absorbed in the gastrointestinal tract, and then rapidly and extensively hydrolyzed by nonspecific esterases to the active metabolite, 5-hydroxymethyl-tolterodine, whose maximum plasma concentration is reached after 5 hours. The connection with plasma proteins is 50%.
Therapeutic effect develops 1 week after the beginning of admission and reaches a maximum after 4 hours. Does not penetrate the blood-brain barrier. Metabolism in the liver involving CYP3A4 before the formation of three metabolites, none of which shows no pharmacological activity.
The half-life is 7 hours. Elimination by the kidneys (69.2%, of which less than 15% in unchanged form) and with feces (about 22.5%) as 5-hydroxymethyl-tolterodine.
Indications:It is used for the treatment of imperative (urgent) urinary incontinence, with rapid urination in patients with the syndrome of hyperactivity of the bladder.
XIV.N30-N39.N31 Neuromuscular dysfunction of the bladder, not elsewhere classified
XVIII.R30-R39.R32 Urinary incontinence, unspecified
XVIII.R30-R39.R35 Polyuria
Contraindications:Delayed urination, renal and hepatic insufficiency, keratoconus, iris synechia, closed-angle and open-angle glaucoma, hemodialysis.
Individual intolerance, children under 18 years.
Carefully:Infravesical obstruction of the bladder outlet, moderate renal and hepatic insufficiency.
Pregnancy and lactation:Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.
Dosing and Administration:Inside, 4 mg once a day. If necessary, the dose may be doubled, up to 8 mg once a day.
The highest daily dose: 8 mg.
The highest single dose: 8 mg.
Side effects:Central and peripheral nervous system: fast fatigue, drowsiness.
Respiratory system: dryness of the nasal mucosa.
Digestive system: dyspeptic disorders, constipation, abdominal pain, gastritis, rarely - coprostasis.
Sense organs: violation of accommodation, dryness of the conjunctiva.
Allergic reactions.
Overdose:Dry mouth, blurred vision, confusion, delirium, hallucinations, difficulty breathing, palpitations, pain in the eyes.
Treatment. Administration of physostigmine intravenously from 0.5 to 2 mg at a speed of 1 mg per minute (not more than 5 mg per day) or neostigmine methylsulfate intramuscularly 1 mg every 2-3 hours, intravenously - up to 2 mg.
Interaction:Reduces effects stimulants of motility of the gastrointestinal tract: metoclopramide, cisapride.
Simultaneous use of cholinergic receptors with agonists reduces the effect of fesoterodine.
Simultaneous reception with m-holinoblokatorami increases the development of side effects.
With simultaneous application with inhibitors of CYP3A4 (fluconazole, cimetidine, ketoconazole) increases the concentration of the drug in the blood plasma.
Special instructions:The use of the drug may lead to disruption of accommodation and a decrease in the rate of psychomotor reactions. The intake of fesoterodine is contraindicated in individuals,the performance of professional duties which is connected with driving cars or working with moving machinery.