Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
The blocker of m-holinoretseptorov, localized in the bladder and salivary glands. Tolterodin and its active 5-hydroxymethyl metabolite are highly specific for m-cholinergic receptors, have selectivity for these bladder receptors, as compared to salivary glands.
Reduces the contractile function of the bladder and reduces salivation. It causes incomplete emptying of the bladder, increases the amount of residual urine and reduces detrusor pressure.
Time to achieve a therapeutic effect - 4 weeks.
PHARMACOKINETICS
Absorption is fast, high. C max in the blood plasma increases in proportion to the dose in the range of 1-4 mg. Metabolized by the polymorphic enzyme CYP2D6 to form a pharmacologically active 5-hydroxymethyl metabolite, which is then metabolized to 5-carboxylic acid and N-dealkylated 5-carboxylic acid. Bioavailability in persons with reduced metabolism (deprived of CYP2D6) is 65%, in those with increased metabolism 17%. Food does not affect the exposure of unbound tolterodine and the active 5-hydroxymethyl metabolite in individuals with increased metabolism, although its concentration rises when taken with meals. Tolterodin and 5-hydroxymethyl metabolite bind mainly with orosomucoid. Unrelated fractions are 3.7 and 36%, respectively. V d Tolterodine - 113 liters. In individuals with elevated metabolism, T 1/2 and systemic clearance is higher than in individuals with reduced metabolism. It is excreted by the kidneys - 77% (51% in the form of 5-carboxylic acid, 29% - N-dealkylated 5-carboxylic acid), through the intestine - 17%, while less than 1% - unchanged and about 4% .
INDICATIONS
Hyperactivity of the bladder, manifested by frequent imperative urges to urinate or urinary incontinence.
DOSING MODE
Take inside at a dose of 4 mg / day. If necessary, incl. with kidney and / or liver failure, concomitant therapy with ketoconazole or other potent inhibitors of CYP3A4, the daily dose is reduced to 2 mg.
SIDE EFFECT
From the digestive system: dryness of the oral mucosa, constipation, abdominal pain, indigestion, flatulence, vomiting, gastroesophageal reflux.
From the side of the central nervous system: headache, dizziness, drowsiness, nervousness, confusion, hallucinations.
From the side of the organ of vision: dry sclera, visual impairment (including accommodation disorders).
On the part of the respiratory system: bronchitis, sinusitis.
From the urinary system: dysuria, urinary retention.
Allergic reactions: anaphylactic reactions, including angioedema.
Other: weakness, fatigue, chest pain, dry skin, weight gain, blood flushes to the skin of the face, tachycardia, palpitations, peripheral edema.
CONTRAINDICATIONS
Urine retention, angle-closure glaucoma (not treatable), myasthenia gravis, severe flow ulcerative colitis, megacolon, pregnancy, lactation period, hypersensitivity to the tolterin.
PREGNANCY AND LACTATION
Contraindicated in pregnancy, during lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Use with caution in renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Use with caution in liver failure.
APPLICATION FOR CHILDREN
At present, the safety and efficacy of the drug in children have not been studied.
SPECIAL INSTRUCTIONS
Use with caution in cases of severe obstruction of the lower parts of the urinary tract, obstructive lesions of the gastrointestinal tract (including pyloric stenosis), hepatic and / or renal failure, with neuropathy, hernia of the esophageal opening of the diaphragm, in children and adolescents under the age of 18.
Before the beginning of treatment it is necessary to exclude organic causes of frequent and imperative urge to urinate.
At present, the safety and efficacy of the drug in children have not been studied.
Impact on the ability to drive vehicles and manage mechanisms
During the period of treatment, patients should be careful when driving vehicles and other potentially dangerous activities that require increased concentration of attention, rapidity of psychomotor reactions and good vision (can cause discomfort and accommodation of psychomotor reactions).
DRUG INTERACTION
When used simultaneously with drugs with anticholinergic properties, the effect of tolterodine is increased and the risk of side effects increases.
M-cholinergic receptor agonists decrease the effectiveness of tolterodine.
Tolterodin reduces the effect of prokinetics.
Possible pharmacokinetic interaction with drugs metabolized by isoenzymes CYP2D6 or CYP3A4, which are inducers or inhibitors of these isoenzymes.Simultaneous application with strong inhibitors of CYP3A4, such as macrolide antibiotics (erythromycin and clarithromycin), or antifungal agents with azole derivatives (ketoconazole, itraconazole and miconazole) should be avoided.
