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Description of the drug VEZOMNI

Solifenacin

After multiple doses, Tmax for solifenacin varied between 4.27 hours and 4.76 hours in different studies, for tamsulosin - between 3.47 hours and 5.65 hours, respectively. Cmax in plasma for solifenacin varied between 26.5 ng/ml and 32.0 ng/ml, for tamsulosin - between 6.56 ng/ml and 13.3 ng/ml. The AUC value for solifenacin varied from 528 ng×h/ml to 601 ng×h/ml, for tamsulosin - between 97.1 ng×h/ml and 222 ng×h/ml. The absolute bioavailability for solifenacin is about 90%, while tamsulosin is absorbed by 70-79%.

After a single dose, T1/2 for solifenacin varies from 49.5 hours to 53 hours, for tamsulosin - from 12.8 hours to 14 hours.

Cmax is reached after 3-8 hours. Tmax is independent of dose. Cmax and AUC increase proportionally with increasing doses from 5 to 40 mg. Absolute bioavailability - 90%. Vd of solifenacin after intravenous administration is approximately 600 l. Solifenacin is largely (about 98%) bound to plasma proteins, predominantly to α1-acid glycoprotein.

Solifenacin is actively metabolized in the liver, mainly by the CYP3A4 isoenzyme. However, there are alternative metabolic pathways through which solifenacin can be metabolized. The systemic clearance of solifenacin is about 9.5 l/h, and the final T1/2 is 45-68 hours. After taking the drug orally, the following metabolites were identified in the plasma past solifenacin:

one pharmacologically active (4R-hydroxysolifenacin) and three inactive solifenacin N-glucuronide, N-oxide and 4R-hydroxy-N-oxide).

After a single dose of 10 mg 14C-labeled solifenacin administered after 26 days, approximately 70% of the radioactivity was detected in urine and 23% in feces. In urine, approximately 11% of the radioactivity was found as unchanged active substance, about 18% as the N-oxide metabolite, 9% as the 4R-hydroxy-N-oxide metabolite, and 8% as the 4R-hydroxy metabolite (the active metabolite).

Tamsulosin

Tamsulosin is characterized by linear pharmacokinetics. At steady state, Cmax of tamsulosin in plasma is achieved after 4-6 hours. Plasma protein binding is about 99%, Vd is small (about 0.2 l/kg).

Tamsulosin is slowly metabolized in the liver to form less active metabolites. Most of tamsulosin is present in the blood plasma unchanged. Tamsulosin is mainly metabolized in the liver, mainly with the participation of isoenzymes CYP3A4 and CYP2D6.

After a single dose of 0.2 mg 14C-labeled tamsulosin after 1 week, about 76% of radioactivity was detected in urine and 21% in feces. In urine, about 9% of the radioactivity was found as unchanged active substance; about 16% as o-deethylated tamsulosin sulfate, and 8% as o-ethoxyphenoxyacetic acid.

In clinical pharmacology and bioavailability studies, patient ages ranged from 19 to 79 years. After administration, the highest concentrations were found in elderly patients, although there was almost complete agreement with individual values in younger patients. Can be used in elderly patients.

The AUC and Cmax of solifenacin in patients with mild to moderate renal impairment do not differ significantly from the corresponding values in healthy volunteers. In patients with severe renal failure (creatinine clearance ≤30 ml/min), the exposure to solifenacin is significantly higher - the increase in Cmax is about 30%, AUC is more than 100% and T1/2 is more than 60%. A statistically significant relationship was noted between creatinine clearance and clearance of solifenacin.

Vesomni PPO tablets with modif release 6mg+0.4mg No. 10

Compound

Tablets
Active ingredients: solifenacin succinate 6.0 mg, tamsulosin hydrochloride 0.4 mg, Excipients: mannitol 83.0 mg, maltose 10.0 mg, magnesium stearate 2.2 mg, macrogol 7,000,000,200.0 mg, macrogol 8,000 40.0 mg.

Contraindications

- hypersensitivity to the active components of the drug or to excipients - hemodialysis - severe liver failure - severe renal failure or moderate liver failure with simultaneous treatment with strong inhibitors of the CYP3A4 isoenzyme, for example, ketoconazole - the presence of severe gastrointestinal diseases (including toxic megacolon), myasthenia gravis and angle-closure glaucoma, as well as the risks of developing these diseases. - orthostatic hypotension - children and adolescents under 18 years of age With caution. Vesomni should be prescribed with caution to patients with: - severe renal failure, - risk of urinary retention, - gastrointestinal obstructive diseases, - risk of reduced gastrointestinal motility, - hiatal hernia, gastroesophageal reflux and patients taking concomitant drugs (eg, bisphosphonates) that may cause or worsen esophagitis, with peripheral neuropathy, QT prolongation and torsade de pointes (TdP) have been observed in patients with risk factors such as long QT syndrome and hypokalemia.

Directions for use and doses

Adult men, including older men.

Take 1 tablet of Vesomni (6 mg / 0.4 mg) orally 1 time per day, regardless of meals. The maximum daily dose of Vesomni is 1 tablet (6 mg / 0.4 mg). The tablets are taken whole, without chewing, but do not crush.

Patients with renal failure. The effect of renal failure on the pharmacokinetics of Vesomni has not been studied. However, the effect on the pharmacokinetics of individual active ingredients of the drug has been well studied (see Section Pharmacokinetic properties). The drug Vesomni can be prescribed to patients with mild to moderate renal failure (creatinine clearance > 30 ml/min). For patients with severe renal failure (creatinine clearance &le, 30 ml/min), use the drug with caution and do not exceed the maximum daily dose.

Patients with impaired liver function. The effect of liver failure on the pharmacokinetics of Vesomni has not been studied. However, the effect on the pharmacokinetics of individual active ingredients of the drug has been well studied (see Section Pharmacokinetic properties). Vesomni can be prescribed to patients with mild hepatic impairment (Child-Pugh score ≤ 7). Patients with moderate liver failure (Child-Pugh score 7-9) should use the drug with caution and not exceed the maximum daily dose. For patients with severe liver failure (Child-Pugh score > 9), the use of Vesomni is contraindicated.

Moderate and potent inhibitors of cytochrome P450 ZA4. Vesomni should be used with caution in patients receiving concomitant treatment with moderate or strong CYP3A4 inhibitors (such as verapamil, ketoconazole, ritonavir, nelfinavir, itraconazole).

Children.

The drug is not intended for use in children (under 18 years of age).

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 30 C.

Best before date

3 years

special instructions

Other causes of frequent urination (heart failure or kidney disease) should be assessed before starting Vesomni. If a urinary tract infection is present, appropriate antibiotic therapy should be initiated. An anaphylactic reaction has been reported in some patients treated with solifenacin after drug approval. If anaphylactic reactions develop, treatment with Vesomni should be discontinued and should not be resumed. As with the use of other 1-blockers, when treated with tamsulosin, in some cases a decrease in blood pressure may be observed, which in rare cases can lead to fainting. Patients starting to take Vesomni should be warned to sit or lie down at the first signs of orthostatic hypotension (dizziness, weakness) and remain in this position until the signs disappear. Some patients taking or previously taking tamsulosin hydrochloride during surgery for cataracts and glaucoma have developed intraoperative iris instability syndrome (small pupil syndrome), which can lead to complications during surgery or in the postoperative period. It is not recommended to initiate Vesomni therapy in patients scheduled for cataract or glaucoma surgery. The advisability of discontinuing Vesomni therapy 1-2 weeks before surgery for cataracts or glaucoma has not yet been proven. During the preoperative examination of patients, the surgeon and ophthalmologist should consider whether the patient is taking or has taken Vesomni. This is necessary to prepare for the possibility of developing intraoperative iris instability syndrome during surgery. Vesomni should be used with caution in combination with strong and moderate CYP3A4 inhibitors, for example, verapamil, ketoconazole, ritonavir, nelfinavir, itraconazole. The drug should not be used in patients with impaired metabolism of the CYP2D6 isoenzyme in combination with strong CYP3A4 inhibitors or strong CYP2D6 inhibitors, for example, paroxetine. Patients with renal insufficiency: Vesomni can be used by patients with mild to moderate renal insufficiency (creatinine clearance>30 ml/min), but should be used with caution in patients with severe renal failure (creatinine clearance, 30 ml/min), for whom the maximum daily dose is one tablet Vesomni (6 mg/0.4 mg). Patients with hepatic insufficiency: Vesomni can be used in patients with mild hepatic insufficiency (Child-Pugh score < 7). Patients with moderate liver failure (7-9 points on the Child-Pugh scale) should take the drug with caution (maximum daily dose of one Vesomni tablet (6 mg/0.4 mg)). In patients with severe liver failure (Child-Pugh score above 9), the use of Vesomni is contraindicated. Pregnancy and lactation: Vesomni is used only in men. Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous machinery: Studies of the effect of the drug Vesomni on the ability to drive vehicles and engage in potentially hazardous activities have not been conducted. However, the patient should be informed about the possible occurrence of dizziness, blurred vision, fatigue and, less commonly, drowsiness, which may adversely affect the ability to drive a car and operate machinery.

Conditions for dispensing from pharmacies

Available with prescription

Side effects

Vesomni may cause side effects associated with the m-anticholinergic effect of solifenacin, often of mild or moderate severity. The most commonly reported side effects during clinical trials with Vesomni were dry mouth (9.5%), constipation (3.2%) and dyspepsia (including abdominal pain 2.4%). Other common adverse reactions include dizziness (1.4%), blurred vision (1.2%), fatigue (1.2%), and ejaculation disorders (including retrograde ejaculation 1.5%). Acute urinary retention (0.3%, rare) is the most serious side effect observed during treatment with Vesomni in clinical trials. In the table below, the column Frequency of Adverse Reactions with Vesomni reflects the adverse reactions recorded during the clinical trial of Vesomni. The solifenacin and tamsulosin adverse reaction incidence columns reflect adverse reactions that have been reported for the individual components (data from the product labels for solifenacin 5 and 10 mg and tamsulosin 0.4 mg, respectively) and that could potentially occur while taking Vesomni. The frequency of adverse reactions is determined as follows: very often (&ge.1/10), often (&ge.1/100 to * observed after registration of the drug. Due to the fact that the data were obtained by spontaneous reports in the period after registration, frequency determination and a causal relationship with tamsulosin and solifenacin appears to be difficult.Long-term safety data for Vesomni: The types and frequency of adverse reactions observed during 1 year of treatment with Vesomni were consistent with those observed during the 12-week study. The drug was well tolerated, and there were no specific adverse reactions associated with long-term use of the drug.Elderly: Adverse effects occurring in the elderly were similar in effect to those occurring in younger patients.

Interaction

Interactions with inhibitors of CYP3A4 and CYP2D6.

Co-administration of solifenacin with ketoconazole (a strong CYP3A4 inhibitor) at a dose of 200 mg/day resulted in a 1.4- and 2.0-fold increase in the Cmax and AUC of solifenacin, while administration of ketoconazole at a dose of 400 mg/day resulted in a 1.5- and 2.0-fold increase. 2.8-fold increase in Cmax and AUC of solifenacin.

With simultaneous use of tamsulosin with ketoconazole at a dose of 400 mg/day, a 2.2- and 2.8-fold increase in tamsulosin Cmax and AUC was observed, respectively.

When tamsulosin was co-administered with cimetidine, a weak CYP3A4 inhibitor (400 mg every 6:00), a 1.44-fold increase in tamsulosin AUC was observed, while Cmax did not change significantly. Vesomni can be used concomitantly with weak CYP3A4 inhibitors.

Concomitant use of tamsulosin with paroxetine, a strong CYP2D6 inhibitor (20 mg per day) led to a 1.3 and 1.6 fold increase in tamsulosin Cmax and AUC, respectively. Vesomni can be used concomitantly with CYP2D6 inhibitors.

The effect of induction enzymes on the pharmacokinetic properties of solifenacin and tamsulosin has not been studied. Since solifenacin and tamsulosin are metabolized by CYP3A4, pharmacokinetic interactions with CYP3A4 inducers (eg rifampicin) are possible, which may reduce the plasma concentrations of solifenacin and tamsulosin.

Other interactions.

Solifenacin.

Solifenacin may reduce the effect of drugs that stimulate gastrointestinal motility such as metoclopramide and cisapride. In vitro studies of solifenacin noted that solifenacin at therapeutic concentrations does not inhibit CYP1A1/2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 or 3A4, therefore no interactions are expected between solifenacin and drugs that are metabolized by these CYP enzymes . Taking solifenacin does not change the pharmacokinetics of R-warfarin or S-warfarin or their effect on prothrombin time. It has been shown that taking solifenacin has virtually no effect on the pharmacokinetics of digoxin.

Tamsulosin.

Concomitant use of tamsulosin with other alpha 1 adrenergic receptor blockers can lead to hypotensive effects. In in vitro studies, the amount of free fraction of tamsulosin in human plasma did not change with the simultaneous use of drugs such as diazepam, propranolol, trichlormethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin or warfarin. Tamsulosin does not change the amount of free fraction of diazepam, propranolol, trichlormethiazide or chlormadinone. Although diclofenac and warfarin may increase the elimination rate of tamsulosin. Concomitant use with furosemide results in a decrease in plasma levels of tamsulosin, but since tamsulosin levels remain within the therapeutic range, simultaneous use of tamsulosin and furosemide is acceptable. In vitro studies of tamsulosin have shown that, at therapeutic concentrations, tamsulosin has virtually no inhibition of CYP1A2, 2C9, 2C19, 2D6, 2E1 or 3A4. Therefore, no interactions are expected between tamsulosin and drugs that are metabolized by these CYP enzymes. There are no cases of interaction of tamsulosin when used simultaneously with atenolol, enalapril or theophylline.

Overdose

Symptoms Overdose when using a combination of solifenacin and tamsulosin can potentially lead to severe anticholinergic effects with the development of acute arterial hypotension. The highest doses taken incidentally during clinical trials were 126 mg of solifenacin succinate and 5.6 mg of tamsulosin hydrochloride. These doses were well tolerated, with mild dry mouth reported after 16 days of treatment.

Treatment.

In case of overdose of solifenacin and tamsulosin, the patient should take activated charcoal. Gastric lavage may be helpful during the first hour after taking the drug, but do not induce vomiting.

Symptoms of solifenacin overdose, like other anticholinergic drugs, can be treated as follows:

severe anticholinergic effect on the central nervous system, hallucinations or other severe disorders: treatment with physostigmine or Carbachol,
convulsions or severe excitability: treatment with benzodiazepines,
respiratory failure: treatment with artificial respiration,
tachycardia symptomatic treatment if necessary. Beta blockers should be used with caution as concomitant tamsulosin overdose can potentially cause severe hypotension.
urinary retention: catheterization.

As with other antimuscarinics, in case of overdose, special attention should be paid to patients with an established risk of developing QT prolongation (eg, hypokalemia, bradycardia, and concomitant use of drugs that can prolong the QT interval) and relevant pre-existing cardiac disease ( e.g. myocardial ischemia, arrhythmia, heart failure).

Acute hypotension, which is possible with an overdose of tamsulosin, should be treated symptomatically. Since tamsulosin binds very well to plasma proteins, hemodialysis is unlikely.