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Preparations
Urological agent Urotol is used as a medication that lowers smooth muscle tone in the urinary canals.
Release form
Urotol is produced in the form of tablets, coated with a film film. Active ingredient Urotol is tolterodine (in the form of tolterodine hydrogen-tartrate).
- Urotol 1 mg is a tablet preparation in a yellow film coating film.
- Urotol 2 mg is a tablet preparation in a white sheath film.
Urotol tablets are packed in blister plates of 14 pieces. A cardboard box contains two or four blister plates.
Pharmacodynamics
Urotol - or rather, its active ingredient tolterodine - refers to drugs that are competitive antagonists of cholinergic muscarinic receptors, with a predominantly selective activity towards urethral receptors. Derivatives of the active ingredient are also selectively specific to muscarinic receptors and do not significantly affect other receptors.
Urotol inhibits active detrusor reduction, while reducing the intensity of salivary fluid secretion. In high volumes, Urotol can cause incomplete urinary output from the bladder, and also increase the volume of residual urinary fluid.
Apparent therapeutic effect of Urotol is found about one month after the start of treatment.
Pharmacokinetics
Urotol in tablets is digested in the digestive system relatively quickly: the plasma concentration of Tolterodin reaches a limit after 1.5 hours.
There is evidence of a linear relationship between the plasma concentration limit and the amount of the drug taken.
After oral administration of Urotol, metabolic processes occur in the liver, involving the polymorphic enzyme CYP2D6 and the formation of the active 5-hydroxymethyl product, which is further transformed to 5-carboxylic acid and N-dealkylated 5-carboxylic acid.
Metabolite has the property of potentiating the action of the drug.
The total clearance in the plasma is usually about 30 liters per hour, and the final half-life after drinking Urotol can be 2-3 hours.
Complete bioavailability in the vast majority of patients is 17%. The food masses in the stomach do not affect the bioavailability, but the concentration content of tolterodine may increase if the drug is taken with food.
The main ingredient and metabolites bind mainly to the orosomucoid. Incoherent fractions are defined as 3.7% and 36%. The distribution volume of the active ingredient is equal to 113 liters. About 77% of the medication is excreted with urinary fluid, and 17% - with mucus masses. Up to 1% of the total is in unchanged form, and about 4% is a 5-hydroxymethyl metabolite.
Use of the urotola during pregnancy
There is no evidence that there is no risk of taking Urotol during pregnancy. Experiments on animals demonstrated the presence of toxic effects of Urotol on the reproductive system, however, testing of the drug with participation of pregnant women was not carried out. Given this, do not take Urotol pregnant women.
When breast feeding Urotol is highly undesirable.
Contraindications
The doctor does not prescribe Urotol in cases of increased likelihood of developing a hypersensitivity reaction in the patient, as well as in other cases, for example:
- with a delay in urinary excretion;
- with an enduring form of an angle-closure glaucoma;
- with classical autoimmune myasthenia gravis;
- with complicated ulcerative colitis;
- with toxic gigantism of the large intestine (the so-called megacolon);
- in childhood (up to 18 years).
Side effects of the urotola
Admission Urotol is able to cause mild or moderate specific manifestations - in the first place, such as thirst, indigestion and dry mucous membranes.
The most common symptoms are:
- pain in the head;
- dryness of mucous membranes.
Less common can be observed:
- dizziness, sleep disturbance, numbness of the limbs;
- bronchitis;
- visual impairment associated with dry mucous membranes;
- cardiopalmus;
- bloating, vomiting, diarrhea;
- retention of urination;
- a feeling of fatigue, pain in the chest;
- edema.
Very seldom were other symptoms fixed:
- allergic manifestations;
- impaired orientation, irritability;
- memory impairment;
- heart rhythm disturbances;
- hallucinations.
Dosing and administration
The standard valid dosage of Urotol for adults is 4 mg of medication daily (2 mg twice daily). The exception to the rule is patients with impaired functional capacity of the liver or kidneys: for them, the recommended amount of Urotol is 1 mg twice a day. If undesirable side effects are found during treatment, the dosage of Urotol should also be minimal - 1 mg twice daily.
The duration of the therapeutic course is usually six months. The advisability of longer therapy is determined by the doctor individually.
With the simultaneous administration of medication inhibitors CYP3A4, the optimal daily amount of Urotol should be 2 mg.
Overdose
Tests of a possible overdose were carried out using 12.8 mg of Urotol taken at a time. The most pronounced reactions were:
- accommodation disorders;
- pain when urinating.
First aid in taking a large dose of Urotol is to wash the stomach and use sorbent funds.
Symptomatic therapy is carried out as follows:
- In the state of overexcitation, hallucinations are prescribed by Physostigmine;
- with convulsions prescribe drugs benzodiazepine series;
- in respiratory function disorders, ventilators are connected;
- in cases of cardiac disorders, the appointment of blockers is appropriate;
- when urinary excretion is delayed, catheterization is performed;
- When dilating the pupils, eye drops are applied on the basis of pilocarpine (in mild cases, the patient is placed in a darkened room).
Interactions with other drugs
It is recommended to avoid the combination of Urotol with macrolides, antifungal azole preparations and antiprotein agents, since the listed medicines can cause an excessive concentration of Urotol in the blood serum.
Undesirable effects of Urotol can be exacerbated by the action of medications with anticholinergic activity.
The therapeutic effect of Urotol is reduced under the influence of muscarinic cholinergic receptor agonist preparations.
Urotol can weaken the effects of metoclopramide and cisapride.
Urotol does not interact with other drugs, including oral contraceptives.
Attention!
To simplify the perception of information, this instruction for use of the drug "Urotol" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.