Vesicare pills 10mg №30

Indications

- treatment of urgent (imperative) incontinence of urine, frequent urination and urgent (imperative) urge to urinate, typical of patients with hyperactive bladder syndrome.

Dosage and administration

Adults 18 years and older, incl. elderly patients the drug is administered orally at 5 mg 1 time / day, regardless of the meal. If necessary, the dose can be increased to 10 mg 1 time / day.

Tablets should be taken with enough liquid.

Adverse effects

Vesicare^® may cause side effects associated with the m-anticholinergic blocking effect of solifenacin, usually mild or moderate severity. The frequency of these adverse effects is dose dependent. The most frequently observed side effect of Vesicare is dry mouth (it was observed in 11% of patients who received the drug in a daily dose of 5 mg, in 22% of patients who received the drug in a daily dose of 10 mg, and in 4% of patients who received placebo). The severity of this side effect was usually weak and only in rare cases did it interrupt the treatment. Overall, adherence was very high.

Below are the other side effects registered in clinical studies on the use of Vesicare. The following criteria were used to assess the frequency of occurrence of side effects: frequent (> 1/100,<1/10); infrequent (> 1/1000, <1/100); rare (> 1/10 000, <1/1000), very rare (<1/10 000 and with an unknown frequency that cannot be estimated from the data presented).

Gastrointestinal: often - constipation, nausea, dyspepsia, abdominal pain; infrequently - gastroesophageal reflux disease, dry throat; rarely - intestinal obstruction, coprostasis; very rarely - vomiting *, loss of appetite *.

Urogenital: infrequently - urinary tract infections, difficulty urinating; rarely, acute urinary retention; very rarely - renal failure *.

From the side of the central nervous system: infrequently - drowsiness, dysgeusia (a violation of taste); very rarely - dizziness *, headache *.

Psychological: very rarely - hallucinations *, confusion *, drowsiness *, delusional state *.

Special senses: often - blurred vision (accommodation disturbance); infrequently - dry eyes.

Respiratory: infrequently - dry nasal cavity.

From the skin and subcutaneous tissue: infrequently - dry skin; very rarely - erythema multiforme *, pruritus *, rash *, urticaria *, angioedema *, exfoliative dermatitis *.

Other: infrequently - fatigue, swelling of the lower extremities.

* - observed after registration of the drug.

When using solifenacin after registration in various countries, a prolongation of the QT interval and pirouette tachycardia has been reported. It has also been reported abnormal liver function, characterized by increased levels of liver enzymes (ALT, ACT, GGT), cases of hyperkalemia.Due to the fact that the data were obtained by the method of spontaneous messages in the period after the registration, the determination of frequency and causal connection is difficult.

Allergic reactions were not observed during clinical studies. However, the possibility of allergic reactions should not be ruled out. Anaphylactic reaction was noted in some patients who received treatment with solifenacin after registering the drug. With the development of Anaphylactic reactions, treatment with solifenacin should be discontinued and appropriate treatment should be carried out.

Contraindications

- urinary retention;

- severe gastrointestinal diseases (including toxic megacolon);

- myasthenia gravis;

- angle-closure glaucoma;

- severe liver failure;

- severe renal insufficiency or moderate hepatic insufficiency with simultaneous treatment with CYP3A4 inhibitors (for example, ketoconazole);

- hemodialysis;

- children's age (lack of data on efficacy and safety);

- hypersensitivity to the drug.

Patients with rare hereditary disorders of the tolerance of galactose, lactase deficiency of lapps (Saami), glucose-galactose malabsorption should not take the drug.

WITH caution the drug should be prescribed to patients:

— with a clinically significant obstruction of the bladder outlet leading to the risk of urinary retention;

— with gastrointestinal obstructive diseases (including stagnation of food in the stomach);

— with the risk of reduced GI motility;

— with severe renal (CK ≤30 ml / min) and moderate hepatic (7-9
points on a scale Child-Pugh) failure (doses for these patients should not exceed 5 mg);

— at the same time taking a powerful inhibitor of the isoenzyme CYP3A4, for example, Ketoconazole;

— with hernia of the esophageal opening of the diaphragm, gastroesophageal reflux, and patients simultaneously taking drugs (for example, bisphosphonates) that can cause or strengthen esophagitis;

— with autonomic neuropathy;

— with such risk factors as the syndrome of lengthening the QT interval and hypokalemia (prolongation of the QT interval and tachycardia of the "pirouette" type were observed).

Use during pregnancy and lactation

There is no clinical data on women who become pregnant while taking solifenacin. Vezikar should be used with caution^® during pregnancy.

Data on the release of solifenacin in human breast milk are not available. Application Vesicare is not recommended during breastfeeding.

AT experimental studies no direct adverse effect on fertility, embryo / fetus development or childbirth was detected in animals.

Application for violations of the liver

Caution should be assigned Vesicare^® with moderate liver failure (from 7 to 9 points on the Child-Pugh scale); drug doses for these patients should not exceed 5 mg.

Application for violations of kidney function

Caution should be assigned Vesicare^® in case of severe renal failure (CK ≤ 30 ml / min), the doses of the drug for these patients should not exceed 5 mg.

Use in children

Use in children is contraindicated.

Use in elderly patients

Apply according to indications.

Special notes

Before starting treatment with Vesicare, it should be ascertained whether there are any other causes of urinary disturbances (heart failure or kidney disease). If urinary tract infection is detected, appropriate antimicrobial treatment should be initiated.

Influence on ability to drive motor transport and control of mechanisms

Solifenacin, like other m-holinoblokatoram, can cause blurred vision, as well as drowsiness (rarely) and a feeling of fatigue, which can adversely affect the ability to drive and work with mechanisms. It is necessary to observe precautions when driving and engaging in other potentially hazardous activities that require high concentration of attention and speed of psychomotor reactions.

Overdosage

An overdose of solifenacin may be accompanied by severe m-holinoblokiruyuschimi violations and requires appropriate treatment. A case of erroneous administration of solifenacin in a dose of 280 mg over a 5-hour period is described, as a result of which the patient developed a change in mental state that did not result in hospitalization.

Symptoms: When using the drug in volunteers at a dose of 100 mg, the following side effects were observed most often: headache (mild), dry mouth (moderate), dizziness (moderate), drowsiness (mild) and blurred vision (moderate). No cases of acute overdose have been reported.

Treatment: in case of overdose, activated charcoal should be prescribed, gastric lavage should be performed, but vomiting should not be induced. If necessary, conduct symptomatic therapy:

- with severe anticholinergic effects of central action (hallucinations, pronounced excitability), physostigmine or carbachol is prescribed;

- for convulsions or marked irritability - benzodiazepines;

- in respiratory failure - artificial respiration;

- with tachycardia - beta-blockers;

- in acute urinary retention - catheterization;

- in case of mydriasis, pilocarpine is instilled into the eyes and / or the patient is placed in a dark room.

As in the case of overdose of other m-cholinoblockers, special attention should be paid to patients with an established risk of lengthening the QT interval (ie, with hypokalemia, bradycardia and at the same time taking drugs that prolong the QT interval) and patients with heart disease (myocardial ischemia, arrhythmias, chronic heart failure).

Drug interaction

Pharmacological interaction

With concomitant treatment with drugs with m-holinoblokiruyuschim properties may have a more pronounced therapeutic effect and the development of undesirable effects.After discontinuation of solifenacin, a week break should be taken before starting treatment with another m-holinoblokatorom. The therapeutic effect can be reduced while taking m-cholinomimetics.

Solifenacin can reduce the effect of drugs that stimulate GI motility, such as Metoclopramide and cisapride.

Pharmacokinetic interaction

In vitro studies have shown that solifenacin does not inhibit CYP1A 1/2, 2C9, 2C19, 2D6 or 3A4 isoenzymes at therapeutic concentrations. Therefore, it is unlikely that solifenacin will change the clearance of drugs metabolized by these isoenzymes.

Effects of other drugs on solifenacin pharmacokinetics

Solifenacin is metabolized by CYP3A4. The simultaneous administration of ketoconazole at a dose of 200 mg / day, a CYP3A4 inhibitor, caused a twofold increase in the AUC of solifenacin, and at a dose of 400 mg / day, a threefold increase. Therefore, the maximum dose of Vesicare should not exceed 5 mg if the patient simultaneously takes ketoconazole or therapeutic doses of other CYP3A4 inhibitors (such as ritonavir, nelfinavir, itraconazole). The simultaneous administration of solifenacin and a CYP3A4 inhibitor is contraindicated in patients with severe renal insufficiency or with moderate hepatic insufficiency. Since solifenacin is metabolized by CYP3A4, pharmacokinetic interactions with other CYP3A4 substrates with higher affinity (verapamil, diltiazem) and with CYP3A4 inducers (rifampicin, phenytoin, carbamazepine) are possible.

Effect of solifenacin on the pharmacokinetics of other drugs

No pharmacokinetic interaction of solifenacin and combined oral contraceptives (ethinyl estradiol / levonorgestrel) was detected.

Simultaneous administration of solifenacin did not cause changes in the pharmacokinetics of R-warfarin or S-warfarin or their effect on prothrombin time.

Simultaneous administration of solifenacin had no effect on the pharmacokinetics of Digoxin .

Terms and conditions of storage

The drug should be stored out of the reach of children at a temperature not higher than 25 ° C.