Vesicar tabs 5mg #30

Vesicar instruction

You can buy Vesicar on this page

Vesicar is a drug that reduces the tone of smooth muscles of the urinary tract, used to treat urological diseases.

Release form and composition

Dosage form - film-coated tablets: round, convex on both sides, light yellow (5 mg tablets) or light pink (10 mg tablets) color, with the company logo and marking “150” (5 mg tablets) or “ 151 "(tablets 10 mg) on ​​one side (10 pcs. In a blister, in a cardboard box 1 or 3 blisters).
The active ingredient of Vesicar: solifenacin succinate, in 1 tablet - 5 or 10 mg.
Excipients: hypromellose 3 mPa × s, corn starch, magnesium stearate, lactose monohydrate.
The composition of the film coating of tablets 5 mg: opadry yellow 03F12967 (macrogol 8000, talc, hypromellose 6 mPa × s, titanium dioxide and iron oxide yellow).
The composition of the film coating of tablets 10 mg: pink opadry 03F14895 (macrogol 8000, talc, hypromellose 6 mPa × s, titanium dioxide and iron oxide red).

Pharmacological properties

Solifenacin is a specific competitive antagonist of muscarinic receptors. The bladder is innervated by parasympathetic cholinergic nerves. Due to the action of acetylcholine on muscarinic receptors (mainly M3), detrusor contraction occurs.
Studies have shown that solifenacin is a specific competitive inhibitor of muscarinic receptors of the M3 subtype. In addition, it was found that solifenacin lacks or has a low affinity for various other receptors and ion channels.

Pharmacodynamics

As a result of the conducted controlled clinical trials, it was found that in patients of both sexes with overactive bladder syndrome, improvement is observed already within the first seven days of therapy, stabilization - after 12 weeks of using Vesicar.
Treatment of overactive bladder symptoms leads to significant improvements in quality of life. The maximum effect is usually detected after 4 weeks of taking Vesicar.

Pharmacokinetics

Cmax (maximum concentration of a substance) in plasma is reached in 3–8 hours, regardless of the dose. Cmax and AUC (area under the concentration-time curve) are dose-dependent and increase in proportion to the dose increase from 5 to 40 mg. The absolute bioavailability is 90%. Food intake has no effect on Cmax and AUC.
After intravenous administration, the volume of distribution of solifenacin is about 600 liters. Solifenacin is associated with plasma proteins (approximately 98%), mainly with α1-acid glycoprotein.
The substance is actively metabolized by the liver, mainly by the CYP3A4 isoenzyme, while there are alternative metabolic pathways. The systemic clearance of solifenacin is approximately 9.5 l / h, the terminal half-life is in the range of 45 to 68 hours. After oral administration of Vesicar in plasma, in addition to solifenacin, the following metabolites are identified: 4R-hydroxysolifenacin, N-glucuronide, N-oxide and 4R-hydroxy-N-oxide of solifenacin (the first of them exhibits pharmacological activity, the other three are inactive).
The elimination route was investigated using 14C-labeled solifenacin. After a single injection of 10 mg after 26 days, approximately 23% of radioactivity is found in feces, 70% in urine. In urine, about 11% of radioactivity is found as an unchanged active substance, 18%, 9% and 8% are metabolites N-oxide, 4R-hydroxy-N-oxide and 4R-hydroxysolifenacin (respectively).
The pharmacokinetics of solifenacin in the therapeutic dose range is linear.
The AUC and Cmax indices of solifenacin in mild and moderate renal failure differ insignificantly from the corresponding indices in healthy volunteers. In severe renal failure (with creatinine clearance ≤ 30 ml / min), the exposure of solifenacin increases significantly (Cmax - by 30%, AUC - more than 100%, half-life - more than 60%). There is a statistically significant relationship between solifenacin clearance and creatinine clearance. Pharmacokinetic parameters in patients undergoing hemodialysis have not been studied.
With moderate hepatic impairment (according to the Child-Pugh classification - stage B), the Cmax value does not change, the AUC increases by 60%, the half-life is doubled. Pharmacokinetic parameters in severe hepatic impairment have not been studied.

Indications for use

According to the instructions, Vesicar is used to treat imperative (urgent) urinary incontinence, imperative (urgent) urge to urinate and frequent urination - signs characteristic of overactive bladder syndrome.

Contraindications

Absolute:
    Severe liver failure;
    Moderate hepatic impairment with the need for concomitant use of CYP3A4 inhibitors (eg, ketoconazole);
    Severe gastrointestinal diseases (including toxic megacolon);
    Delay in urination;
    Closed-angle glaucoma;
    Hemodialysis;
    Myasthenia gravis;
    Rare hereditary disorders of galactose tolerance, lactase deficiency of Lapps (Sami), glucose-galactose malabsorption;
    Age under 18;
    Lactation;
    Hypersensitivity to the components of the drug.
Relative (the use of Vesicar is possible, but with extreme caution, since there is a risk of complications):
    Clinically significant obstruction of the bladder outlet, fraught with the development of urinary retention;
    Gastrointestinal obstructive diseases (including stagnation of food in the stomach);
    The risk of decreased motility of the gastrointestinal tract;
    Severe renal (creatinine clearance ≤30 ml / minute) and moderate hepatic (7-9 points on the Child-Pugh scale) failure (for such patients, the dose of Vesicar should not exceed 5 mg);
    Concomitant use of a potent inhibitor of the CYP3A4 isoenzyme (for example, ketoconazole);
    Hernia of the esophageal opening of the diaphragm, gastroesophageal reflux;
    Concomitant use of drugs that can cause or intensify esophagitis (for example, bisphosphonates);
    Autonomic neuropathy;
    The presence of risk factors such as hypokalemia or long QT syndrome;
    Pregnancy.

Instructions for the use of Vesicar: method and dosage

Vesicar should be taken orally, swallowing the tablets whole and drinking plenty of fluids, regardless of meals.
At the beginning of treatment, adult patients are prescribed 5 mg 1 time per day. If necessary, the dose is increased to 10 mg once a day.

Side effects

    Digestive system: often (> 1/100, <1/10) - dyspepsia, nausea, abdominal pain, constipation; infrequently (> 1/1000, <1/100) - dryness of the pharynx, gastroesophageal reflux disease; rarely (> 1/10 000, <1/1000) - coprostasis, intestinal obstruction; very rarely (<1/10 000, including isolated cases) - decreased appetite *, vomiting *, increased liver enzymes *, hyperkalemia *;
    Urinary system: infrequently - difficulty urinating, urinary tract infections; rarely - acute urinary retention; very rarely - renal failure *;
    Central nervous system: infrequently - taste disturbance (dysgeusia), drowsiness, very rarely - headache * and dizziness *;
    Mental disorders: very rarely - drowsiness *, confusion *, delusional state *, hallucinations *;
    Organ of vision: often - violation of accommodation (blurred visual perception); infrequently - dry eyes;
    Respiratory system: infrequently - dryness of the nasal mucosa;
    Cardiovascular system: prolongation of the QT interval *, pirouette-type tachycardia *;
    Skin and subcutaneous tissue: infrequently - dry skin; very rarely - rash *, itching *, urticaria *, exfoliative dermatitis *, erythema multiforme *, angioedema *;
    Allergic reactions: anaphylactic reactions *;
    Others: infrequently - edema of the lower extremities, fatigue.
* - these side effects were observed in the post-registration period of the use of Vesicar. Data about them were obtained by the method of spontaneous messages, therefore, it is difficult to determine the frequency and cause-and-effect relationship of these reactions with the reception of Vesicar.

Overdose

In an overdose study, the maximum dose used was 100 mg solifenacin once. The most typical symptoms: moderate severity - dry mouth, dizziness, blurred vision; mild severity - headache, drowsiness.
There have been no reports of acute overdose.
Therapy: activated carbon, gastric lavage; vomiting is not recommended.
Therapeutic measures are determined by the indications:
    convulsions or severe irritability: benzodiazepines;
    severe central anticholinergic effects (severe excitability, hallucinations): carbachol or physostigmine;
    tachycardia: beta-blockers;
    urinary retention: catheterization;
    respiratory failure: artificial respiration;
    mydriasis: pilocarpine (instillation in the eyes) and / or darkening of the room where the patient is.
Patients with an established risk of prolongation of the QT interval (i.e., with bradycardia, hypokalemia, against the background of combined therapy with drugs that cause prolongation of the QT interval) and heart disease (congestive heart failure, arrhythmia, myocardial ischemia) need special attention.

Special instructions

Before the appointment of Vesicar, the patient should undergo a complete medical examination to determine if there are any other causes of urinary disorders, such as kidney disease or heart failure. If a urinary tract infection is diagnosed, appropriate antimicrobial therapy is prescribed.
Solifenacin, like other m-anticholinergics, can cause blurred vision, fatigue and drowsiness. For this reason, during the period of treatment, special care should be taken when driving vehicles and engaging in potentially hazardous activities that require the speed of psychophysical reactions and high concentration of attention.

Influence on the ability to drive vehicles and complex mechanisms

During the period of therapy, it is necessary to take into account the likelihood of developing blurred visual perception, drowsiness and feelings of fatigue, which can negatively affect the ability to drive vehicles.

Application during pregnancy and lactation

    pregnancy: the drug can be used under medical supervision after assessing the ratio of the expected benefit with the possible risk; animal studies of a direct negative effect on fertility, embryo / fetal development or childbirth have not been identified;
    lactation period: therapy with Vesicar is contraindicated.

Childhood use

Vesicar therapy is contraindicated in patients under 18 years of age.

With impaired renal function

    severe renal failure when combined with strong inhibitors of the isoenzyme CYP3A4, in particular with ketoconazole: therapy is contraindicated;
    severe renal failure (with creatinine clearance <30 ml / min): Vesicar should be used under medical supervision at a maximum daily dose of 5 mg.

For violations of liver function

    severe hepatic impairment: therapy is contraindicated;
    moderate hepatic failure when combined with strong inhibitors of the isoenzyme CYP3A4, in particular with ketoconazole: therapy is contraindicated;
    moderate hepatic impairment (according to the Child-Pugh classification - stage B): Vesicar should be used under medical supervision at a maximum daily dose of 5 mg.

Drug interactions

Vesicar reduces the effectiveness of drugs that stimulate gastrointestinal motility (for example, cisapride and metoclopramide).
In the case of the simultaneous use of ketoconazole in a daily dose of 200 mg, the total concentration of solifenacin in the blood plasma increases 2 times, when taking ketoconazole in a daily dose of 400 mg - 3 times. If it is necessary to use Vesicar simultaneously with ketoconazole or other CYP3A4 inhibitors (such as nelfinavir, ritonavir, itraconazole), its dose should not exceed 5 mg / day. This combination is contraindicated in patients with moderate hepatic impairment and severe renal impairment. Given that solifenacin is metabolized by CYP3A4, pharmacokinetic interactions with other substrates of CYP3A4 with a higher affinity (diltiazem, verapamil), as well as with inducers of CYP3A4 (phenytoin, rifampicin, carbamazepine) are not excluded.
It should be borne in mind that Vesicar, like all drugs with m-anticholinergic properties, can affect the action of any simultaneously used drugs, including the severity of their side effects. Before starting treatment with another m-anticholinergic antagonist, after taking solifenacin, you must take a week break.
The therapeutic effect of Vesicar can be reduced by m-cholinomimetics.

Terms and conditions of storage

Store at temperatures up to 25 ºС out of reach of children.
Shelf life is 3 years.

Reviews about Vesicar

According to reviews, Vesicar does not have the claimed therapeutic effect in all cases. In addition, many report the development of severe adverse reactions. The cost of the drug is generally estimated to be overpriced.

Terms of sell

A prescription is not required to buy Vesicar.