Detruzitol

Detruzitol – a competitive blocker of m-holinoretseptorov, the drug reducing a tone of smooth muscles of urinary tract.

Form of release and structure

• Capsules of the prolonged action: the size No. 4, firm gelatinous, with the case and kryshechny blue-green color, on the case white ink put figure "2", on a cover – a symbol in the form of the little man; contents – microspheres with a diameter about 1 mm of color, white with a yellowish shade (on 7 pieces in blisters, in a cardboard pack of 1, 4, 7, 12 or 40 blisters);
• Capsules of the prolonged action: the size No. 3, firm gelatinous, with the case and kryshechny blue color, on the case white ink put figure "4", on a cover – a symbol in the form of the little man; contents – microspheres with a diameter about 1 mm of color, white with a yellowish shade (on 7 pieces in blisters, in a cardboard pack of 1, 4, 7, 12 or 40 blisters);
• Tablets, coated: round, convex from two parties, white color, on one of the parties the letters "TO", over and under them – arches are engraved (on 14 pieces in blisters, in a cardboard pack 1, 2 or 4 blisters; on 60 pieces in bottles, in a cardboard pack 1 bottle);
• Tablets, coated: round, convex from two parties, white color, on one of the parties the letters "DT", over and under them – arches are engraved (on 14 pieces in blisters, in a cardboard pack 1, 2 or 4 blisters; on 60 pieces in bottles, in a cardboard pack 1 bottle).

Active ingredient – a tolterodina hydrotartrate:

• 1 capsule the size No. 4 – 2 mg that corresponds to the maintenance of a tolterodin – 1,37 mg;
• 1 capsule the size No. 3 – 4 mg that corresponds to the maintenance of a tolterodin – 2,74 mg;
• 1 tablet with an engraving "THEY" are 1 mg that corresponds to the maintenance of a tolterodin – 0,68 mg;
• 1 tablet with an engraving of "DT" – 2 mg that corresponds to the maintenance of a tolterodin – 1,37 mg.

Additional components of capsules:

• Excipients: gipromelloza, sugar granules (starch corn and sucrose), Surelease E-7-19010 transparent (oleic acid, triglycerides srednetsepochny, ethyl cellulose);
• Structure of a cover: indigo carmine, gelatin, titanium dioxide, blackened white Opacode White S-1-7085 (titanium dioxide, shellac, симетикон, propylene glycol), and also dye ferrous oxide yellow – in capsules No. 4.

Excipients of tablets: starch sodium glycollate, hydrophosphate calcium dihydrate, magnesium stearate, cellulose microcrystallic, stearic acid, gipromelloza, titanium dioxide, silicon dioxide colloid anhydrous.

Indications to use

Detruzitol – drug for treatment of the hyperactivity of a bladder which is shown increase of an urination, frequent and imperative desires to an urination and/or an urine incontience.

Contraindications

• The frequent and imperative desires to an urination caused by the organic reasons;
• Urination delay;
• Heavy ulcer colitis;
• Myasthenia gravis;
• Megacolon;
• Gastric emptying delay;
• Closed-angle glaucoma resistant to treatment;
• Glyukozo-galaktozny malabsorption, rare inherited disorders of portability of fructose, deficit of invertase-isomaltase (for capsules);
• Age up to 18 years (for capsules);
• Lactation;
• Hypersensitivity to drug.

With care Detruzitol appoint in the following cases:

• The expressed obstruction of lower parts of urinary tract;
• Risk of delay of gastric emptying, including obstructive diseases of digestive tract (for example, pyloric stenosis);
• Renal or liver failure (the daily dose of drug should not exceed 2 mg);
• Hernia of an esophageal opening of a diaphragm;
• Neuropathy;
• The inborn or acquired lengthening of an interval of QT;
• Concomitant use of antiarrhytmic drugs of the class IA (procaineamide, quinidine) or class III (соталол, Amiodaronum);
• Age up to 18 years (for tablets).

During pregnancy drug can be appointed only according to vital indications if the estimated advantage surpasses possible risks.

Route of administration and dosage

Detruzitol accept inside, without binding to meals.

The daily dose of drug makes 4 mg: capsules of the prolonged action – on 4 mg of 1 times a day, coated tablets – on 2 mg 2 times a day.

Depending on portability of drug the daily dose can be reduced to 2 mg.

The recommended daily dose for patients with renal failures and/or a liver, the patients receiving кетоконазол or other strong CYP3A4 inhibitors, makes 2 mg: capsules – on 2 mg of 1 times a day, tablets – on 1 mg 2 times a day.

Side effects

Classification of side effects: often – more than 10% of cases, sometimes – from 1 to 10%, are rare – less than 1%:

• Alimentary system: sometimes – abdominal pains, a lock, vomiting, a meteorism, dyspepsia; seldom – a gastroesophageal reflux;
• Central and peripheral nervous system: sometimes – вертиго, drowsiness, a headache, vision disorders, nervousness, weakness, fatigue; seldom – hallucinations, confusion of consciousness;
• Urinary system: sometimes – a dysuria;
• Cardiovascular system: seldom – rushes of blood to skin, feeling of strong heartbeat, tachycardia, peripheral hypostases;
• Allergic reactions: seldom – anaphylactic reactions, including a Quincke's disease;
• The side effects connected with anticholinergic action: often – dryness of a mucous membrane of an oral cavity; sometimes – a xerophthalmia (decrease in a slezootdeleniye), accommodation disturbances; seldom – an urination delay;
• The side effects caused by administration of drug in tablets: sometimes – increase in body weight, a xeroderma, a stethalgia, bronchitis;
• The side effects caused by administration of drug in capsules: sometimes – sinusitis.

Special instructions

Before Detruzitol's appointment it is necessary to conduct examination of the patient to exclude existence of the organic reasons of frequent and imperative desires to an urination.

The daily dose of drug should be lowered to 2 mg in need of simultaneous use of CYP3A4 inhibitors, such as antibiotics of group of macroleads (кларитромицин, erythromycin), antifungal means (итраконазол, Miconazolum, кетоконазол).

Detruzitol is not recommended to appoint to children as safety of its use for this age group of patients is not studied.

Drug can reduce the speed of psychophysical reactions and cause accommodation disturbances in this connection during treatment it is necessary to refrain from control of vehicles and performance of potentially dangerous types of the works requiring special attention and speed of reactions.

Women of childbearing age during treatment need to apply reliable methods of contraception.

Medicinal interaction

• Anticholinergic drugs: therapeutic action of Detruzitol and his undesirable effects amplifies;
• M-cholinomimetics: therapeutic effect of drug decreases;
• Metoclopramidum, цизаприд: their action is weakened;
• Fluoxetine: increase in the general concentration of a tolterodin and its active 5-hydroxymethyl metabolite is insignificant (clinically significant reactions is not followed).

Perhaps pharmacokinetic interaction with drugs, the metabolized isoenzymes 2D6 or 3A4 of system of P450 cytochrome or the being inductors or inhibitors of these isoenzymes.

Patients with insufficiency of CYP2D6 should avoid simultaneous use of Detruzitol with strong CYP3A4 inhibitors, such as antibiotics of group of macroleads (кларитромицин and erythromycin), antifungal means (Miconazolum, итраконазол, кетоконазол) since increase in concentration of a tolterodin in blood serum and increase in risk of overdose is possible.

Tolterodin does not interact with the combined oral contraceptives (containing levonorgestrel or ethinylestradiol) and warfarin.

Terms and storage conditions

To store at a temperature up to 25 ºС in the place protected from light and unavailable to children.

Period of validity of capsules – 2 years, tablets – 3 years.