Vesicare, 10 mg, film-coated tablets, 30 pcs.

Pharmacological properties of the drug Vesicare

In vitro and in vivo studies have shown that solifenacin is a competitive specific antagonist of cholinergic receptors, predominantly of the M3 subtype. Solifenacin has low affinity for other receptors and ion channels. The therapeutic effect of the drug, which was studied in several double-blind randomized controlled clinical trials in men and women with overactive bladder syndrome, was observed as early as 1 week of treatment and stabilized over the next 12 weeks of treatment. The maximum effect of the drug can be observed after 4 weeks. The effectiveness of the drug is maintained with long-term use. After oral administration, the maximum concentration of solifenacin in the blood plasma is achieved after 3–8 hours. The time to reach the maximum concentration in the blood plasma does not depend on the dose of the drug. The maximum concentration and AUC increase proportionally to the dose in the range of 5–40 mg. Absolute bioavailability is about 90%. Food intake does not affect the values ​​of maximum concentration and AUC. The volume of distribution of solifenacin after intravenous administration is about 600 l. Solifenacin is highly (almost 98%) bound to plasma proteins, mainly to α1-acid glycoprotein. Solifenacin is extensively metabolized in the liver, mainly by cytochrome P450 3A4 (CYP 3A4). The systemic clearance of solifenacin is about 9.5 l/h, its terminal half-life is 45–68 hours. After oral administration of the drug in the blood plasma, in addition to solifenacin, one pharmacologically active (4R-hydroxysolifenacin) and three inactive metabolites (N-glucuronide) were identified , N-oxide and 4R-hydroxy-N-oxide of solifenacin). After a single administration of 10 mg of 14C-labeled solifenacin after 26 days, approximately 70% of the radiolabel is detected in the urine and 23% in the feces. Approximately 11% of the radioactive tracer is excreted in the urine as unchanged active substance; approximately 18% as the N-oxide metabolite, 9% as the 4R-hydroxy-N-oxide metabolite, and 8% as the 4R-hydroxy metabolite (active metabolite). In the range of therapeutic doses, the pharmacokinetics of the drug is linear. There is no need to adjust the dose depending on the age of the patients. It was found that the exposure of solifenacin (when taken at a dose of 5 and 10 mg), expressed as AUC, was similar in healthy elderly individuals (65–80 years) and in young and mature individuals (younger than 55 years). The mean rate of absorption, expressed as time to peak concentration, was slightly lower and the terminal half-life approximately 20% longer in elderly subjects. These minor differences are not clinically significant. The pharmacokinetics of solifenacin does not depend on the gender or race of the patient. The AUC and maximum concentration of solifenacin in patients with mild to moderate renal impairment are not significantly different from the corresponding values ​​in healthy volunteers. In patients with severe renal impairment (creatinine clearance ≤30 mL/min), solifenacin exposure is significantly higher, with an increase in maximum concentration of approximately 30%, AUC greater than 100%, and elimination half-life greater than 60%. A statistically significant relationship was noted between the clearance of creatinine and solifenacin. In patients with moderate hepatic impairment (7–9 points on the Child-Pugh scale), the maximum concentration does not change, the AUC increases by 60%, and the half-life doubles. Pharmacokinetics in patients with severe hepatic impairment have not been studied.

Reviews about Vesicare (patients' opinions)

Reviews about Vesicare on medical forums indicate that the drug has not been able to establish itself as the most highly effective remedy in the fight against the problem of urinary incontinence. Most patient stories do not report any relief after taking the drug. In addition, many users report frequent side effects.

However, there is evidence of cases where the best result among analogues was observed precisely after taking Vesicare; when other medications did not help. It is important to remember that the treatment of overactive bladder syndrome is complex and largely depends on the individuality of each individual organism.

Side effects of Vesicare

When using Vesicare, side effects associated with the anticholinergic effect of solifenacin are possible, which, as a rule, are mild or moderate and dose-dependent. The most common side effect is dry mouth, which is usually mild and only in isolated cases requires discontinuation of the drug. The frequency of side effects is classified: very often (≤1/10, ≥1/100); uncommon (≤1/100, ≥1/1000); rare or isolated cases (≤1/1000, ≥1/10,000). From the gastrointestinal tract: often - nausea, dyspepsia, constipation, abdominal pain; infrequently - dryness of the pharyngeal mucosa, gastroesophageal reflux; rarely, in isolated cases - obstruction of the large intestine, coprostasis. From the side of the central nervous system: infrequently - drowsiness, taste disturbance. From the senses: often - blurred vision (impaired accommodation), infrequently - dry eyes. Infections and infestations: uncommon - urinary tract infections. General disorders: infrequently - increased fatigue, swelling of the lower extremities. From the respiratory system: not often - dryness of the nasal mucosa. From the skin: infrequently - dry skin. From the urinary system: infrequently - difficulty urinating, in isolated cases - urinary retention.

pharmachologic effect

Solifenacin is a specific inhibitor of membrane proteins responsible for signal transmission at neuromuscular synapses, acetylcholine muscarinic receptors (m-cholinergic receptors). The medication has an antispasmodic and anticholinergic effect (reduces the tone of the smooth muscle tissue of the urinary tract). Solifenacin is characterized by an almost complete lack of affinity for ion channels and other receptors.

When using Vesicare, a cumulative effect is observed - the maximum effect is recorded after a month of use and persists in case of long-term use (at least 1 year).

Special instructions for the use of Vesicare

Before starting treatment with the drug, it is necessary to establish the likelihood of other causes of frequent urination (kidney disease, heart failure, etc.). If a urinary tract infection is detected, appropriate antibiotic therapy should be started. The drug should be prescribed with caution to patients with clinically significant obstruction of the bladder outlet, obstructive gastrointestinal diseases, gastrointestinal motility disorders, severe renal (creatinine clearance ≤30 ml/min) and moderately severe liver failure (7-9 points on the Child-Pugh scale; dose for these patients should not exceed 5 mg), autonomic neuropathy, hiatal hernia and gastroesophageal reflux and/or concomitant use of drugs that can cause or worsen esophagitis (e.g. bisphosphonates), while using an active CYP3A4 inhibitor (e.g. ketoconazole) . The drug should not be prescribed to patients with congenital galactose sensitivity disorder, lactase deficiency or glucose-galactose malabsorption. The effect of using the drug is noted already in the 1st week of treatment, but the maximum effect is achieved after 4 weeks of therapy. There are no data on the use of the drug in children. Since the drug, like other anticholinergic drugs, can cause disturbances in accommodation and a decrease in the speed of psychomotor reactions, the question of the possibility of performing potentially hazardous activities should be decided only after assessing the patient’s individual response to the drug. There are no clinical data on the use of solifenacin during pregnancy, however, experimental studies have not revealed any direct adverse effects on fertility, fetal development or the course of labor. In this regard, caution should be exercised when using the drug in pregnant women. There is no data on the excretion of solifenacin in breast milk, therefore the use of Vesicare during breastfeeding is not recommended.

Contraindications

• severe gastrointestinal diseases ;
• liver failure in severe and terminal forms;
• renal failure (including when taking CYP3A4 inhibitors);
• hemodialysis;
• myasthenia gravis;
• urinary retention;
• angle-closure form of glaucoma ;
• hypersensitivity or intolerance to the components of the drug;
• childhood and adolescence;
• galactosemia and lactose deficiency.

There is no data on the effect of this drug on the body under 18 years of age. There are no contraindications for the elderly. Use with caution during pregnancy and lactation .

Vesicare drug interactions

Concomitant use of other drugs with anticholinergic properties may have a more pronounced therapeutic effect, as well as more pronounced side effects. After stopping taking Vesicare, an interval of about 1 week should be maintained before prescribing other drugs with anticholinergic effects. The therapeutic effect of solifenacin may be reduced by concomitant use of cholinergic receptor agonists. Solifenacin may reduce the effectiveness of gastrointestinal motility stimulants (metoclopramide, cisapride). When taking ketoconazole or other active inhibitors of the CYP3A4 enzyme (for example, ritonavir, nelfinavir, itraconazole), the dose of Vesicare should be reduced to 5 mg. Concomitant administration of solifenacin and an active CYP3A4 enzyme inhibitor is contraindicated in patients with severe renal or moderate hepatic impairment. Since solifenacin is metabolized by the CYP3A4 enzyme, pharmacokinetic interactions with other substrates of this enzyme (eg verapamil, diltiazem) and inducers of the CYP3A4 enzyme (eg rifampicin, phenytoin, carbamazepine) are possible. There was no pharmacokinetic interaction of solifenacin with combined oral contraceptives (ethinyl estradiol/levonorgestrel). Vesicare does not affect the pharmacokinetics of warfarin and digoxin.

Instructions for Vesicare (Method and dosage)

The drug is administered orally with plenty of liquid, 1 tablet with a solifenacin concentration of 5 mg once a day. According to indications, the dose can reach 10 mg. The medication can be taken regardless of the time of day or meal.

Instructions for use of Vesicare indicate the possible effect of the active substance on the quality of visual perception and the functioning of the central nervous system. You should not take the drug when working with complex mechanisms or driving vehicles.

Vesicare drug overdose, symptoms and treatment

The maximum dose of the drug used was 100 mg once. Side effects such as mild headache, moderate dry mouth, dizziness, drowsiness, and blurred vision were noted. In case of overdose, it is necessary to rinse the stomach and prescribe activated charcoal. As with an overdose of other anticholinergic drugs, the following measures are taken: for pronounced central effects (hallucinations, agitation) - physostigmine or carbachol; for seizures - benzodiazepines; in case of respiratory failure - mechanical ventilation; for urinary retention - catheterization of the bladder; for mydriasis - instilling pilocarpine into the eyes or placing the patient in a darkened room; for tachycardia - β-adrenergic receptor blockers. Particular attention should be paid to patients at risk of prolongation of the QT on the ECG (with hypokalemia, bradycardia, simultaneous use of drugs that can cause prolongation of the QT ) and patients with heart disease (coronary artery disease, arrhythmia, chronic heart failure).

Vesicare price, where to buy

The cost of the drug in Russian pharmacies varies from 1200 to 1550 rubles for 30 tablets. The price of Vesicare depends on the region of sale and pharmacy chain.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

ZdravCity

• Vesicare tab.
  p/o captivity. 0.005g 30pcs Astellas Pharma Europe B.V. RUR 746 order
• Vesicare tab. p/o captivity. 0.01g 30pcs Astellas Pharma Europe B.V.

  RUB 1,064 order

Pharmacy Dialogue

• Vesicare (tab.pl/vol.5mg No. 30)Astellas Pharma

  RUR 722 order

• Vesicare (tab.pl/vol. 10 mg No. 30)Astellas Pharma

  RUB 1,044 order

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Pharmacy24

• Vesicare 5 mg No. 30 tablets Astellas Pharma Europe B.V., Netherlands
  346 UAH.order

PaniPharmacy

• Vesicare tablets Vesicare tablets. p/o 5 mg No. 30 Netherlands, Astellas Pharma Europe

  369 UAH. order

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Composition and release form

in a blister pack 10 pcs.; in a cardboard pack 1 or 3 packs.

in a blister pack 10 pcs.; in a cardboard pack 1 or 3 packs.