Vesicare - instructions for use, analogs, reviews and release forms (5 mg and 10 mg tablets) of a drug for the treatment of urinary incontinence or rapid urination in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Vesicar. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Vesikar in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Vesikar in the presence of existing structural analogues. Use for the treatment of urinary incontinence or increased urination in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Vesicar - antispasmodic.Solifenacin (the active substance of the drug Vesicar) is a specific competitive inhibitor of muscarinic cholinergic receptors, mainly M3-subtype. It has also been found that solifenacin has a low affinity or lack of affinity for various other receptors and ion channels.

The effectiveness of the drug Vesicare when used in doses of 5 mg and 10 mg with hyperactive bladder syndrome is observed already during the first week of treatment and stabilized during the next 12 weeks of treatment. The maximum Vesicare effect can be detected after 4 weeks. The effectiveness is maintained for a long time (at least 12 months).

Composition

Solifenacin succinate + excipients.

Pharmacokinetics

After ingestion, Cmax in the blood plasma is reached after 3-8 hours. Absolute bioavailability is 90%. Food intake does not affect Cmax and AUC solifenacin. The pharmacokinetics of solifenacin is linear in the therapeutic dose range. Solifenacin is actively metabolized in the liver, mainly by the isoenzyme CYP3A4. However, there are alternative ways of solifenacin metabolism.The systemic clearance of solifenacin is about 9.5 l / h, and the final T1 / 2 is 45-68 hours. After taking the drug inside the plasma, in addition to solifenacin, the following metabolites were identified: one pharmacologically active (4R-hydroxysolifenacin) and three inactive (N-glucuronide, N-oxide and 4R-hydroxy-N-solifenacin). After a single administration of 10 mg of 14C-labeled solifenacin at 26 days, about 70% of the radioactivity was detected in urine and 23% in feces. In the urine, approximately 11% of the radioactivity was detected as an unchanged active substance, about 18% as an N-oxide metabolite, 9% in the form of 4R-hydroxy-N-solifenacin oxide, and 8% as a 4R-hydroxy metabolite (active metabolite) .

There is no need to adjust the dose depending on the age of the patients.

The pharmacokinetics of solifenacin in children and adolescents has not been studied.

The pharmacokinetics of solifenacin does not depend on the sex of the patient and race.

In patients with mild to moderate renal failure, Cmax and AUC solifenacin slightly differ from those in healthy volunteers.

The pharmacokinetics in patients undergoing hemodialysis have not been studied.

Indications

• treatment of urgent (mandatory) urinary incontinence, rapid urination and urgent (imperative) urinary urges, characteristic of patients with the syndrome of hyperactive bladder.

Forms of release

Tablets, film-coated 5 mg and 10 mg.

Instructions for use and dosing regimen

Adults 18 years and older, incl. elderly patients, the drug is administered orally 5 mg once a day, regardless of food intake. If necessary, the dose can be increased to 10 mg once a day.

Tablets should be washed down with a sufficient amount of liquid.

Side effect

• dry mouth;
• constipation;
• nausea, vomiting;
• dyspepsia;
• abdominal pain;
• gastroesophageal reflux disease (GERD);
• dryness of pharynx;
• intestinal obstruction;
• coprostasis;
• decreased appetite;
• urinary tract infections;
• difficulty urinating;
• acute retention of urination;
• kidney failure;
• drowsiness;
• dysgeusia (a taste disorder);
• dizziness;
• headache;
• hallucinations;
• confusion of consciousness;
• delirium;
• dry eyes;
• dryness of the nasal cavity;
• dry skin;
• erythema multiforme;
• itching;
• rash;
• hives;
• angioedema;
• exfoliative dermatitis;
• fatigue;
• swelling of the lower extremities.

Contraindications

• retention of urination;
• severe gastrointestinal diseases (including toxic megacolon);
• myasthenia gravis;
• angle-closure glaucoma;
• severe hepatic impairment;
• severe renal failure or moderate hepatic impairment with simultaneous treatment with CYP3A4 inhibitors (eg, ketoconazole);
• conducting hemodialysis;
• children's age (lack of data on effectiveness and safety);
• hypersensitivity to the components of the drug.

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

Caution should be given to patients:

• with clinically significant bladder outlet obstruction leading to a risk of developing urinary retention;
• with gastrointestinal obstructive diseases (including stagnation of food in the stomach);
• with the risk of decreased GI motility;
• with severe renal (KK less than 30 ml / min) and moderate hepatic (7-9 points on the Child-Pugh scale) insufficiency (doses for these patients should notexceed 5 mg);
• simultaneously taking a potent inhibitor of the isoenzyme CYP3A4, for example, ketoconazole;
• with hernia of the esophagus of the diaphragm, gastroesophageal reflux and patients taking medications simultaneously (for example, bisphosphonates), which can cause or intensify esophagitis;
• with autonomic neuropathy;
• with such risk factors as QT interval prolongation syndrome and hypokalemia (prolongation of QT interval and pirouette tachycardia was observed).

Application in pregnancy and lactation

There are no clinical data on women who have had a pregnancy with solifenacin. Caution should be given to Vesicare during pregnancy.

Data on the isolation of solifenacin with human milk are absent. The use of Vesicare is not recommended during breastfeeding.

In experimental animal studies, no direct adverse effects on fertility, development of the embryo / fetus, or delivery have been identified.

Use in children

Contraindicated in children and adolescents under the age of 18 years.

Application in elderly patients

Possible application for indications.

special instructions

Before starting treatment with Vesicare, you should determine whether there are other causes of urinary disorders (heart failure or kidney disease). If an infection of the urinary tract is detected, appropriate antimicrobial treatment should be initiated.

Influence on ability to driving by motor transport and management of mechanisms

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

Drug Interactions

Pharmacological interaction

With concomitant treatment with preparations with m-cholinoblocking properties, a more pronounced therapeutic effect and development of undesirable effects can be noted. After discontinuing taking solifenacin, you should take a one-week break before starting treatment with another m-holinoblokatorom.The therapeutic effect can be reduced by simultaneous administration of m-cholinomimetics.

Vesicare can reduce the effect of drugs that stimulate the motility of the gastrointestinal tract, for example, Metoclopramide and cisapride.

Pharmacokinetic interaction

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

The effect of other drugs on the pharmacokinetics of Vesicare

Solifenacin is metabolized by CYP3A4. Simultaneous administration of Ketoconazole at a dose of 200 mg per day, an inhibitor of CYP3A4, caused a twofold increase in AUC solifenacin, and at a dose of 400 mg per 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 an inhibitor of CYP3A4 is contraindicated in patients with severe renal insufficiency or with moderate hepatic insufficiency.Since solifenacin is metabolized by CYP3A4, pharmacokinetic interactions with other substrates of CYP3A4 with higher affinity (verapamil, diltiazem) and with CYP3A4 inducers (rifampicin, phenytoin, carbamazepine) are possible.

The influence of Vesicar on the pharmacokinetics of other drugs

There was no pharmacokinetic interaction between solifenacin and combined oral contraceptives (ethinyl estradiol / levonorgestrel).

The simultaneous use of solifenacin did not cause a change in the pharmacokinetics of R-warfarin or S-warfarin or their effect on prothrombin time.

Simultaneous reception of solifenacin had no effect on the pharmacokinetics of digoxin.

Analogues of the drug Vesicare

Vesicar does not have structural analogs for the active substance.

Analogues on the curative effect (agents for the treatment of neurogenic weakness of the bladder):

• Vitaprost forte;
• Gentos;
• Detruzitol;
• Nivalin;
• Novitropane;
• Pantogam;
• Proserin;
• Spazmeks;
• Spasmocystenal;
• Ubretid;
• Urotol;
• Cystrin.

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