Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):VED
ONLS
АТХ:G.04.B.D Spasmolytics
G.04.B.D.08 Solifenacin
Pharmacodynamics:Selectively and competitively blocks m-holinoretseptory subtype M3located on the smooth muscle cells of the bladder, has an antispasmodic effect, stimulates the secretion of the salivary glands.
Pharmacokinetics:After oral administration, regardless of the time of ingestion, up to 90% is absorbed in the gastrointestinal tract. The maximum concentration in blood plasma is reached after 3-8 hours. The connection with plasma proteins is 98%.
Therapeutic effect develops 1 week after the beginning of admission and reaches a maximum after 4 hours. It does not penetrate the blood-brain barrier. Metabolism in the liver with the participation of CYP3A4 to the formation of 4 metabolites, one of which exhibits pharmacological activity - 4R-hydroxoliphenacin.
The half-life is 45-68 hours with constant intake. Elimination of the kidneys (69.2%, of which less than 15% - unchanged) and faeces (about 22.5%) in the form of 4R-hydroxoliphenacin.
Indications:
It is used for the treatment of imperative (urgent) urinary incontinence, with frequent 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:
Infravesical obstruction of the bladder outlet, moderate renal and hepatic insufficiency.
Carefully:
Delayed urination, renal and hepatic insufficiency, keratotonus, iris synechia, closed-angle and open-angle glaucoma, hemodialysis, individual intolerance.
Pregnancy and lactation:Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.
Dosing and Administration:Inside, regardless of the time of food intake, 5 mg 1 time / day, squeezed large amounts of liquid. In the absence of effect, the dose is doubled.
The highest daily dose: 10 mg.
The highest single dose: 10 mg.
Side effects:Central and peripheral nervous system: fast fatigue, drowsiness.
Respiratory system: dry nasal mucosa.
Digestive system: dyspeptic disorders, constipation, abdominal pain, gastritis, rarely - coprostasis.
Sense organs: disruption of accommodation, dryness of the conjunctiva.
Allergic reactions.
Overdose:Dry mouth, blurred vision, confusion, delirium, hallucination, difficulty breathing, palpitations, pain in the eyes.
Treatment. Introduction of physostigmine: intravenously from 0.5 to 2 mg at a speed of up to 1 mg / min, not more than 5 mg / 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: metoclopromide, cisapride.
Simultaneous use of cholinergic receptors with agonists reduces the effect of solifenacin.
Simultaneous reception with m-holinoblokatorami increases the development of side effects.
With simultaneous application with inhibitors of CYP3A4 (fluconazole, cimetidine, ketonazole) 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. Solifenacin is contraindicated in individuals whose professional duties are associated with driving cars or working with moving machinery.