Solixa Xanthis, 10 mg 60 pcs

Indications

Symptomatic treatment of urinary incontinence, frequent urination and urgent urge to urinate in patients with overactive bladder syndrome.

Active ingredient

Solifenacin

Composition

1 film-coated tablet, 10 mg contains:

the active ingredient:

solifenacin succinate – 10.00 mg;

auxiliary substances:

lactose monohydrate – 110.50 mg,

corn starch – 30.00 mg,

talcum powder – 3.00 mg,

magnesium stearate – 1.50 mg;

film coating: Opadray white 03B28796 – 3.60 mg, (hypromellose 6cP E464 – 2.2500 mg, titanium dioxide E171 – 1.1250 mg, macrogol 400 – 0.2250 mg), Opadray brown 02F 23883 – 0.40 mg (hypromellose 5 cP E464 – 0,2374 mg, titanium dioxide E171 – 0.0895 mg, macrogol 6000 – 0.0475 mg, iron oxide yellow dye E172 – 0.0128 mg, iron oxide red dye E172 – 0.0128 mg).

How to take, the dosage

Adults, including the elderly

5 mg once daily orally, whole, with liquids, regardless of the time of meals. If necessary, the dose may be increased to 10 mg once daily.

Children

The safety and effectiveness of solifenacin in children have not been studied; therefore, the use of Solix-Xantis in children is contraindicated.

Patients with renal impairment

Dose adjustment is not required in patients with mild to moderate renal impairment (creatinine clearance > 30 ml/min). In patients with severe renal impairment (creatinine clearance < 30 ml/min), Solixa-Xantis should be used under close medical supervision and at a dose not exceeding 5 mg daily.

Patients with hepatic impairment

Dose adjustment is not required in patients with mild hepatic impairment. In patients with moderate hepatic impairment (Child-Pugh stage B), Solixa-Xantis should be used under close medical supervision and at a dose of no more than 5 mg daily.

Patients receiving strong CYP3A4 isoenzyme inhibitors

. When solifenacin is coadministered with ketoconazole or a therapeutic dose of another strong CYP3A4 isoenzyme inhibitor, such as nelfinavir itraconazole, the maximum daily dose of Solix-Xantis should not exceed 5 mg.

Interaction

Pharmacological interaction

Continuous treatment with drugs with anticholinergic properties may lead to more pronounced pharmacological effects and adverse reactions. After stopping solifenacin, a break of approximately one week should be taken before starting treatment with another anticholinergic drug. Pharmacological effects may be reduced by concomitant administration of cholinergic receptor agonists. Solifenacin may decrease the effects of drugs that stimulate gastrointestinal motility, such as metoclopramide.

Pharmacokinetic interaction

The studies in vitro have shown that at therapeutic concentrations, solifenacin does not inhibit the CYP1A1/2, 2C9, 2C19, 2D6 or ZA4 isoenzymes isolated from human liver microsomes. Therefore, it is unlikely that solifenacin will alter the clearance of drugs metabolized by these CYP enzymes.

Effects of other drugs on the pharmacokinetics of solifenacin

Solifenacin is metabolized by the CYP3A4 isoenzyme. Concomitant administration of ketoconazole (200 mg daily), a strong inhibitor of the CYP3A4 isoenzyme, caused a twofold increase in the AUC time-dependent concentration of solifenacin, and a threefold increase in the dose of 400 mg/day. Therefore, the maximum dose of solifenacin should not exceed 5 mg if the patient simultaneously takes ketoconazole or therapeutic doses of other strong CYP3A4 isoenzyme inhibitors (such as ritonavir, nelfinavir, itraconazole). Co-administration of solifenacin and strong CYP3A4 isoenzyme inhibitors is contraindicated in patients with severe renal insufficiency or moderate hepatic insufficiency. The phenomena of enzyme induction on the pharmacokinetics of solifenacin and its metabolites have not been studied, nor have the effects of high-affinity CYP3A4 isoenzyme substrates on the action of solifenacin.

As solifenacin is metabolized by the CYP3A4 isoenzyme, pharmacokinetic interactions are possible with other higher affinity CYP3A4 isoenzyme substrates (verapamil, diltiazem) and with CYP3A4 isoenzyme inducers (rifampicin, phenytoin, carbamazepine).

Influence of solifenacin on the pharmacokinetics of other drugs

Orral contraceptives: No pharmacokinetic interaction between solifenacin and combined oral contraceptives (ethinylestradiol + levonorgestrel) has been identified.

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

Digoxin: Taking solifenacin had no effect on the pharmacokinetics of digoxin.

Special Instructions

In patients with such risk factors as existing QT interval prolongation and hypokalemia, QT interval prolongation and pirouette-type ventricular tachycardia have been observed. Efficacy and safety have not been studied in patients with neurogenic bladder dysfunction. Several cases of angioedema with airway obstruction have been identified in patients taking solifenacin. Therefore, if angioedema occurs, solifenacin should be discontinued and appropriate measures taken.

Particular cases of anaphylactic reactions have been identified in patients taking solifenacin. Therefore, if an anaphylactic reaction occurs, solifenacin should be discontinued and appropriate measures taken.

Influence on ability to drive, operate machinery

Solifenacin, like other anticholinergic drugs, may cause blurred vision and (rarely) drowsiness and fatigue, which may adversely affect the ability to drive and operate machinery.

Synopsis

Penetaled tablets, 10 mg

Circular, biconvex, film-coated tablets with a pink color.

Contraindications

• painful urinary retention;
• severe gastrointestinal disease (including toxic megacolon);
• myasthenia gravis;
• closed-angle glaucoma;
• hypersensitivity to solifenacin or any of the excipients;
• Hemodialysis;
• Severe hepatic impairment;
• Severe renal impairment or moderate hepatic impairment when concurrently treated with strong CYP3A4 isoenzyme inhibitors such as ketoconazole (see
• lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome;
• breastfeeding period (see sect.
• pregnancy and breastfeeding
• children under 18 years of age.

Cautions

Before starting therapy with solifenacin, other causes of frequent urination (chronic heart failure or kidney disease) should be excluded. If a urinary tract infection is detected, appropriate antibiotic therapy should be carried out. Observance of precautions when using solifenacin is required in patients:

• with clinically significant bladder outlet obstruction leading to risk of urinary retention;
• with gastrointestinal disease with obstruction;
• with severe renal impairment (creatinine clearance < 30 ml per minute) and moderate hepatic impairment (Child-Pugh stage B); doses for these patients should not exceed 5 mg;
• simultaneously taking a strong CYP3A4 isoenzyme inhibitor such as ketoconazole;
with esophageal hernia, gastroesophageal reflux, or patients taking concomitant medications (e.g., bisphosphonates) that may cause or aggravate esophagitis;
• with autonomic neuropathy;

in women during pregnancy (see

Pregnant women during pregnancy (see “Use in pregnancy and during breastfeeding”).

Side effects

The use of solifenacin may cause adverse reactions associated with its anticholinergic effect, often of mild to moderate severity. The frequency of these adverse reactions depends on the dose of solifenacin. The most frequently reported adverse reaction of solifenacin is dry mouth. It was observed in 11% of patients receiving a dose of 5 mg daily, in 22% of patients receiving a dose of 10 mg daily, and in 4% of patients receiving placebo. The severity of dry mouth was usually mild and only rarely resulted in treatment interruption.

Immune system disorders: anaphylactic reactions

Metabolic and nutritional disorders: decreased appetite, hyperkalemia

Mental disorders: hallucinations, confusion, delirium

Gastrointestinal disorders: dry mouth, constipation, nausea, dyspepsia, abdominal pain, gastroesophageal reflux disease, dry throat, colonic obstruction, coprostasis, vomiting, ileus, abdominal discomfort

Liver and biliary tract disorders: Liver disorders, changes in liver function test scores

Infectious and parasitic diseases: urinary tract infection, cystitis

Nervous system disorders: drowsiness, dysgeusia (taste disorder), dizziness, headache

Visual disturbances: blurred vision (impaired accommodation), dry eye mucosa, glaucoma

Cardiac disorders: pirouette-type ventricular tachycardia, prolonged QT interval (ECG), atrial fibrillation, tachycardia, palpitations

General disorders and disorders in the injection site: fatigue, peripheral edema

Respiratory, chest and mediastinal organ disorders: nasal dryness, dysphonia

Skin and subcutaneous tissue disorders: dry skin, rash, itching, erythema multiforme, urticaria, angioedema, exfoliative dermatitis

Muscular and connective tissue disorders: muscle weakness

Renal and urinary tract disorders: difficulty in urination, urinary retention, renal failure

Overdose

Solifenacin overdose has the potential to cause severe anticholinergic effects. The highest dose of solifenacin that was accidentally taken by one patient was 280 mg over 5 hours. This dose resulted in a change in the patient’s mental state, but did not require hospitalization. In cases of overdose, activated charcoal should be administered, gastric lavage is effective within an hour, but vomiting should not be induced. As in cases of overdose of other anticholinergic agents, symptoms should be treated as follows:

• for severe central anticholinergic effects (hallucinations, marked excitability), carbachol;
• for seizures or marked excitability, benzodiazepines;
• in tachycardia – beta-blockers;
• in acute urinary retention – catheterization;
• in mydriasis – eye drops pilocarpine and/or placing the patient in a dark room.

As in overdose with other anticholinergic drugs, special attention should be given to patients with an established risk of QT interval prolongation (i.e. hypokalemia, bradycardia, and concomitant administration of drugs that cause QT interval prolongation) and patients with previously identified cardiac conditions (myocardial ischemia, arrhythmias, chronic heart failure).

Pregnancy use

There are no clinical data on women who have become pregnant while taking solifenacin. Animal studies have shown no direct adverse effects on fertility, embryo/fetal development, or childbirth. Solifenacin should only be used during pregnancy if the benefit to the mother exceeds the potential risk to the fetus.

There are no data on the penetration of solifenacin into human breast milk. In animal studies it was found that solifenacin and/or its metabolites penetrated into the milk of lactating mice. The use of solifenacin is contraindicated during breastfeeding.

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