Urotol
Urotol: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Urotol
ATX code: G04BD07
Active ingredient: tolterodine (tolterodine)
Manufacturer: Zentiva ks (Czech Republic)
Description and photo update: 2018-26-10
Prices in pharmacies: from 324 rubles.
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Urotol is a drug with anti-dysuric, m-anticholinergic action.
Release form and composition
Dosage form of Urotol release - film-coated tablets: round biconvex; 1 mg each - yellow; 2 mg - white (in a carton box 2 or 4 blisters of 14 tablets each).
Composition of 1 tablet:
- active substance: tolterodine hydrotartrate - 1 or 2 mg;
- auxiliary components (1 or 2 mg, respectively): sodium stearyl fumarate - 1.5 / 3 mg; microcrystalline cellulose - 73/146 mg; colloidal silicon dioxide - 1/2 mg; sodium carboxymethyl starch (type A) - 3.5 / 7 mg;
- shell (1 or 2 mg, respectively): hypromellose 2910/5 - 1.75 / 3.5 mg; macrogol 6000 - 0.3 / 0.6 mg; dye iron oxide yellow - 0.05 / 0 mg; talc - 0.25 / 0.5 mg; titanium dioxide - 0.15 / 0.4 mg.
Pharmacological properties
Pharmacodynamics
Urotol is one of the m-anticholinergics.
Tolterodine and its 5-hydroxymethyl derivative are highly specific for muscarinic receptors, they competitively block m-cholinergic receptors with the highest selectivity for bladder receptors (in comparison with salivary gland receptors).
Urotol reduces the contractile activity of the detrusor, the tone of smooth muscles of the urinary tract, and also reduces salivation.
When used in higher therapeutic doses, it increases the amount of residual urine and causes incomplete emptying of the bladder.
Does not inhibit CYP2D6, 2C19, 1A2 or 3A4.
The therapeutic effect of Urotol is achieved after 4 weeks of use.
Pharmacokinetics
After oral administration, tolterodine is rapidly absorbed from the gastrointestinal tract. Time to reach C max (maximum concentration) in serum is 1–2 hours.
In the range of therapeutic doses (from 1 to 4 mg), there is a linear relationship between the dose of the drug and the serum C max in the blood.
The absolute bioavailability of tolterodine is 17% (in most patients) and 65% (in individuals with CYP2D6 deficiency).
Food does not affect the bioavailability of the drug, although the concentration of tolterodine when taken with food increases.
The binding of tolterodine and 5-hydroxymethyl metabolite occurs mainly with orosomucoid, unbound fractions - 3.7% and 36%, respectively. V d (volume of distribution) of tolterodine is 113 liters.
The AUC (area under the concentration-time curve) of tolterodine in individuals with CYP2D6 deficiency approximately corresponds to the sum of the AUC values of tolterodine and the 5-hydroxymethyl metabolite in most patients with the same dosing regimen. Thus, the tolerability, safety and clinical effect of Urotol do not depend on the activity of CYP2D6.
Tolterodine is metabolized mainly in the liver by the polymorphic enzyme CYP2D6. As a result, a pharmacologically active 5-hydroxymethyl metabolite is formed, which is then metabolized to N-dealkylated 5-carboxylic acid and 5-carboxylic acid. The 5-hydroxymethyl metabolite has pharmacological properties close to tolterodine; in most cases, it significantly enhances the effect of the drug.
Tolterodine with reduced metabolism (with CYP2D6 deficiency) undergoes dealkylation by CYP3A4 isoenzymes to form N-dealkylated tolterodine, which has no pharmacological activity.
In most patients, the systemic serum clearance of tolterodine is approximately 30 L / h. T 1/2 (half-life) of tolterodine varies within 2-3 hours, 5-hydroxymethyl metabolite - from 3 to 4 hours. With a reduced metabolism, this figure is approximately 10 hours.
A decrease in the clearance of the parent compound in patients with CYP2D6 deficiency leads to an increase in the concentration of tolterodine (approximately 7 times) against the background of undetectable concentrations of the 5-hydroxymethyl metabolite.
About 17% of tolterodine is excreted in the feces, 77% in the urine. Less than 1% of the dose is excreted unchanged, approximately 4% as a 5-hydroxymethyl metabolite. N-dealkylated 5-carboxylic acid and 5-carboxylic acid make up, respectively, about 29% and 51% of the amount excreted in the urine.
In liver cirrhosis, the AUC value of tolterodine and its active 5-hydroxymethyl metabolite increases by about 2 times.
In patients with severe renal impairment (glomerular filtration rate ≤ 30 ml / min), the average AUC of tolterodine and 5-hydroxymethyl metabolite is 2 times higher. In these patients, the plasma content of other metabolites is significantly higher (clinical significance is unknown).
Indications for use
According to the instructions, Urotol is prescribed for the treatment of hyperreflexia (hyperactivity, instability) of the bladder, which manifests itself in the form of frequent, urgent urge to urinate, increased frequency of urination and / or urinary incontinence.
Contraindications
Absolute:
- angle-closure glaucoma, refractory to treatment;
- delay in urination;
- myasthenia gravis;
- megacolon;
- severe ulcerative colitis;
- age up to 18 years;
- lactation period;
- individual intolerance to any component of the drug.
Relative (Urotol is prescribed under medical supervision):
- severe obstruction of the lower urinary tract (associated with the risk of urinary retention);
- neuropathy;
- increased risk of decreased peristalsis of the gastrointestinal tract;
- renal / hepatic impairment;
- obstructive diseases of the gastrointestinal tract (in particular, pyloric stenosis);
- hernia of the esophageal opening of the diaphragm;
- pregnancy.
Instructions for the use of Urotol: method and dosage
Urotol tablets are taken orally, regardless of the meal.
The recommended dosage regimen: 2 mg 2 times a day.
Based on the individual tolerance of the drug, a single dose can be reduced to 1 mg. At the same dose, Urotol is prescribed for impaired renal / hepatic function, as well as against the background of simultaneous use with ketoconazole or other strong CYP3A4 inhibitors.
The effectiveness of therapy should be re-evaluated 2-3 months after starting the drug.
Side effects
- skin: dry skin;
- nervous system: paresthesia, dizziness, impaired consciousness, nervousness, hallucinations, drowsiness, headache;
- immune system: very rarely - Quincke's edema, allergic reactions;
- sense organs: violation of accommodation, dry eye syndrome;
- urinary system: urinary retention;
- digestive system: xerostomia, vomiting, dyspepsia, abdominal pain, constipation, flatulence; rarely - gastroesophageal reflux;
- cardiovascular system: rarely - increased heart rate, tachycardia, arrhythmia;
- others: weight gain, chest pain, fatigue, bronchitis, peripheral edema.
Overdose
The main symptoms are urinary retention, mydriasis, paresis of accommodation, painful urge to urinate, hallucinations, convulsions, severe agitation, tachycardia, respiratory failure, prolongation of the QT interval.
Therapy: the appointment of activated carbon, gastric lavage. Other measures depend on the symptoms of the overdose:
- convulsions or severe agitation: benzodiazepine anxiolytics;
- hallucinations, severe agitation: physostigmine;
- tachycardia: beta-blockers;
- respiratory failure: artificial lung ventilation;
- mydriasis: transferring the patient to a dark room and / or pilocarpine in eye drops;
- retention of urine: catheterization of the bladder.
special instructions
Before starting the course, organic causes of imperative and frequent urge to urinate should be excluded.
Influence on the ability to drive vehicles and complex mechanisms
During the period of therapy, when driving vehicles, care should be taken, which is associated with the likelihood of developing accommodation disorders.
Application during pregnancy and lactation
- pregnancy: therapy can be carried out under medical supervision after assessing the balance of benefits and risks;
- the period of breastfeeding: Urotol is contraindicated (data on whether the active substance is excreted in breast milk is not presented).
Women of childbearing age need to use reliable methods of contraception during therapy.
Pediatric use
Patients under 18 years of age are not prescribed Urotol tablets (safety profile has not been studied).
With impaired renal function
Urotol in patients with impaired renal function should be used under medical supervision in a daily dose of 2 mg.
For violations of liver function
Urotol in patients with impaired hepatic function should be used under medical supervision in a daily dose of 2 mg.
Drug interactions
Possible interactions:
- macrolide antibiotics (erythromycin, clarithromycin), protease inhibitors, antifungal agents (miconazole, ketoconazole, itraconazole) and other strong CYP3A4 inhibitors: an increase in the serum concentration of tolterodine in the blood, which leads to an increased risk of overdose of Urotol (the combination is not recommended);
- drugs with anticholinergic action: increasing the action of Urotol and increasing the likelihood of adverse reactions;
- muscarinic cholinergic receptor agonists: decreased efficacy of tolterodine;
- prokinetics (metoclopramide, cisapride): weakening of their action;
- drugs metabolized by isoenzymes CYP2D6 or CYP3A4 (inducers and inhibitors): the likelihood of a pharmacokinetic interaction.
Analogs
Urotol analogues are: Detrusitol, Uroflex, Roliten.
Terms and conditions of storage
Store at temperatures up to 25 ° C in original packaging. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Urotol
Reviews about Urotol are different. Its high efficiency and good tolerance are noted. In other cases, they indicate a lack of therapeutic effect and a high cost.
Price for Urotol in pharmacies
The approximate price for Urotol (56 pieces in a package of 1 or 2 mg) is 519-597 or 594-674 rubles.
Urotol: prices in online pharmacies
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Drug name Price Pharmacy |
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Urotol 2 mg film-coated tablets 56 pcs. 324 r Buy |
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Urotol 1 mg film-coated tablets 56 pcs. 549 r Buy |
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Urotol tablets p.p. 1mg 56 pcs. 578 r Buy |
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Urotol tablets p.p. 2mg 56 pcs. RUB 620 Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
