Vesicare pills 5 mg 30 pcs
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Active ingredients
Solifenacin
Release form
Pills
Composition
1 tablet contains: Active substances: solifenacin succinate - 5 mg. Auxiliary substances: lactose monohydrate - 107.5 mg, corn starch - 30 mg, hypromellose 3 MPa · s - 6 mg, magnesium stearate - 1.5 mg, purified water * - 54 mg. The composition of the film shell: opadry yellow 03F12967 (hypromellose 6 MPa · s - 61.83%, talc - 18.54%, macrogol 8000 - 11.6%, titanium dioxide - 7.88%, iron yellow oxide - 0.15%) - 4 mg, purified water * - 36 mg.
Pharmacological effect
Antispasmodic. Solifenacin is a specific competitive inhibitor of muscarinic cholinergic receptors, primarily the M3 subtype. It was also found that solifenacin has a low affinity or lack of affinity for various other receptors and ion channels. The effectiveness of the Vesicare preparation; when used in doses of 5 mg and 10 mg in overactive bladder syndrome, it is observed already during the first week of treatment and stabilizes over the next 12 weeks of treatment. The maximum Vesicare effect can be detected after 4 weeks. Effectiveness persists for prolonged use (at least 12 months).
Pharmacokinetics
Absorption After ingestion, C max in plasma is reached after 3–8 hours. Tmax is not dose dependent. Cmax and AUC increase in proportion to the dose increase from 5 to 40 mg. Absolute bioavailability - 90%. Food intake does not affect the Cmax and AUC of solifenacin. The pharmacokinetics of solifenacin are linear in the therapeutic dose range. Distribution After IV administration of Vd solifenacin is about 600 liters. The binding of solifenacin to plasma proteins, predominantly with the α1-acidic glycoprotein, is about 98%. MetabolismSolifenacin is extensively metabolized in the liver, predominantly by the CYP3A4 isoenzyme. However, there are alternative metabolic pathways for solifenacin. The systemic clearance of solifenacin is about 9.5 l / h, and the final T1 / 2 is 45-68 h. 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 oxide). Exit After a single injection of 10 mg of 14C-labeled solifenacin after 26 days, about 70% of radioactivity was detected in urine and 23% in feces.In urine, approximately 11% of radioactivity was detected as unchanged active substance, about 18% as N-oxide metabolite, 9% as 4R-hydroxy-N-solifenacin oxide, and 8% as 4R-hydroxy metabolite (active metabolite) . Pharmacokinetics in special clinical situations. There is no need to adjust the dose depending on the age of patients. Studies have shown that exposure to solifenacin (5 and 10 mg), expressed as AUC, was similar in healthy elderly people (65 to 80 years old) and in healthy young people (55 years old). In the elderly, the average absorption rate, expressed as TCmax, was slightly lower, and the final T1 / 2 increased by about 20%. These minor differences are not clinically significant. The pharmacokinetics of solifenacin in children and adolescents has not been studied. The pharmacokinetics of solifenacin do not depend on the patient’s gender and race. In patients with mild to moderate renal insufficiency, the maxifenacin differs slightly from those in healthy volunteers. In patients with severe renal failure (CK ≤ 30 ml / min), the exposure of solifenacin is much higher - the increase in Cmax is about 30%, the AUC is more than 100% and T1 / 2 - more than 60%. There was a statistically significant relationship between QC and clearance of solifenacin. The pharmacokinetics in patients undergoing hemodialysis has not been studied. In patients with moderate hepatic insufficiency (from 7 to 9 points on the Child-Pugh scale), Cmax does not change, AUC increases by 60%, T1 / 2 increases 2 times. Pharmacokinetics in patients with severe hepatic insufficiency has not been studied.
Indications
- treatment of urgent (imperative) incontinence of urine, frequent urination and urgent (imperative) urge to urinate, typical of patients with hyperactive bladder syndrome.
Contraindications
- urinary retention; - severe gastrointestinal diseases (including toxic megacolon); - myasthenia gravis; - angle-closure glaucoma; - severe hepatic insufficiency; - severe renal failure or moderate hepatic insufficiency with simultaneous treatment with CYP3A4 inhibitors (eg, ketoconazole); - conduction hemodialysis; - children's age (lack of data on efficacy and safety); - hypersensitivity to the components of the drug.Patients with rare inherited impairment of tolerance galactose, lactase deficiency Lapp (Sami)Glucose-galactose malabsorption should not take the drug. Patients should be prescribed with caution 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 motility of the gastrointestinal tract; - with severe renal (CK ≤ 30 ml / min) and moderate hepatic (7–9 points on the Child-Pugh scale) insufficiency (doses for these patients should not exceed 5 mg); powerful in CYP3A4 isoenzyme ibitor, for example, ketoconazole; with esophageal hernia, gastroesophageal reflux, and patients simultaneously taking medications (such as bisphosphonates) that can cause or increase esophagitis; with autonomous neuropathy; prolongation of the QT interval and hypokalemia (prolongation of the QT interval and pirouette tachycardia was observed).
Use during pregnancy and lactation
There is no clinical data on women who become pregnant while taking solifenacin. Caution should be given to Vesicare; during pregnancy. There are no data on the isolation of solifenacin in human breast milk. The use of Vesicare is not recommended during the breastfeeding period. In experimental studies on animals, no direct adverse effect on fertility, embryo / fetus development or childbirth was detected.
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 washed down with a sufficient amount of liquid.
Side effects
Vesicard; may cause side effects associated with m-anticholinergic blocking action of solifenacin, more often with 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 to treatment was very high. The rest of the side effects recorded in clinical studies on the use of Vesicare are listed below.The following criteria were used to assess the frequency of occurrence of side effects: frequent (more than 1/100, less than 1/10); infrequent (more than 1/1000, less than 1/100); rare (more than 1/10 000, less than 1/1000), very rare (less than 1/10 000 and with an unknown frequency that cannot be estimated from the data presented). From the digestive system: often - constipation, nausea, dyspepsia, abdominal pain ; infrequently - gastroesophageal reflux disease, dry throat; rarely - intestinal obstruction, coprostasis; very rarely - vomiting *, loss of appetite *. From the urinary system: rarely - urinary tract infections, difficulty urinating; rarely, acute urinary retention; very rarely - renal failure *. On the CNS side: infrequently - drowsiness, dysgeusia (taste disorder); very rarely - dizziness *, headache *. Mental disorders: very rarely - hallucinations *, confusion *, drowsiness *, delusional state *. On the part of the organ of vision: often - blurred visual perception (accommodation disturbance); infrequently - dry eyes. From the respiratory system: infrequently - dry nasal cavity. From the skin and subcutaneous tissue: infrequently - dry skin; very rarely - erythema multiforme *, pruritus *, rash *, urticaria *, angioedema *, exfoliative dermatitis *. Others: infrequently - fatigue, edema of the lower extremities. * - were observed after registration of the drug. lengthening of the QT interval and pirouette type 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 registration, determining the frequency and cause-effect relationship is difficult. Allergic reactions during clinical studies were not observed. 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.
Overdose
An overdose of solifenacin may be accompanied by severe m-holinoblokiruyuschimi violations and requires appropriate treatment. A case of erroneous administration of solifenacin at a dose of 280 mg over a 5-hour period was 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 noted 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 done, but vomiting should not be induced. If necessary, symptomatic therapy is carried out: - for severe anticholinergic effects of the central action (hallucinations, severe excitability), physostigmine or carbachol is prescribed; - for convulsions or severe irritability - benzodiazepines; - for respiratory failure - artificial respiration; - for tachycardia - beta-blockers; in case of acute urinary retention - catheterization; - in mydriasis - pilocarpine is instilled into the eyes and / or the patient is placed in a dark room. As in the case of an overdose of other m-cholinoblocato s, particular attention should be given to patients with established risk for QT interval elongation (ie, hypokalemia, bradycardia, and while taking drugs that cause QT interval elongation) and patients with heart disease (myocardial ischemia, arrhythmia, congestive heart failure).
Interaction with other drugs
Pharmacological interaction. With the concomitant treatment with drugs with m-anticholinergic properties, a more pronounced therapeutic effect and the development of undesirable effects may be noted. 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 the motility of the gastrointestinal tract, such as metoclopramide and cisapride. , 2D6 or 3A4.Therefore, it is unlikely that solifenacin will change the clearance of drugs metabolized by these isoenzymes. Effects of other drugs on the pharmacokinetics of solifenacin 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 solifenacs are metabolized by the CYP3A4 / levonorgestrel). Simultaneous administration of solifenacin did not cause changes in the pharmacokinetics of R-warfarin or S-warfarin or their iyaniya on prothrombin vremya.Odnovremenny receiving solifenacin had no effect on the pharmacokinetics of digoxin.
special instructions
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. Impact on ability to drive vehicles and control mechanismsSolifenacin, like other m-holinoblokatoram, can cause blurred visual perception, as well as drowsiness (rarely) and feeling tired drive a car 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.