Toviaz sustained release pills 8mg, 28pcs

Composition

of 1 tab. fesoterodine 8 mg

Pharmacological action

Competitive inhibitor of m-cholinergic receptors.

After oral use, fesoterodine is rapidly and intensively hydrolyzed with the participation of non-specific esterases to form the active metabolite 5-hydroxymethyl tolterodine, which determines the m-cholinolytic activity of fesoterodine.

Activation of postganglionic parasympathetic m-cholinergic receptors in the bladder smooth muscle induces detrusor contraction. Fesoterodine inhibits these receptors in the bladder, which is assumed to lead to the development of appropriate pharmacological effects.

Clinical use of fesoterodyne has been shown to increase bladder volume by the time of the first detrusor contraction and increase bladder capacity.

These effects increase in proportion to the dose increase.

Indications

Treatment of an overactive bladder in the presence of symptoms of acute urinary incontinence with the need for urgent and frequent urination.

Contraindications

Urinary retention, delayed evacuation of food from the stomach, uncontrolled angle-closure glaucoma, hypersensitivity to fesoterodine.

Side effects

From the digestive system:  dry mouth, constipation, dyspepsia, nausea, vomiting, abdominal pain, increased ALT and AST activity; in some cases – irritable bowel syndrome.

From the urinary system:  urinary tract infections, dysuria, urinary retention.

Respiratory system disorders:  cough, dry throat.

From the side of the visual organ:  dry eyes, blurred vision.

Musculoskeletal disorders:  back pain.

Skin and subcutaneous fat disorders:  skin rash, itching.

Allergic reactions:  angioedema with airway obstruction, facial edema, urticaria.

From the central nervous system: dizziness, headache, drowsiness.

From the cardiovascular system:  palpitation; in some cases – prolongation of the QTc interval on the ECG.

General reactions:  peripheral edema.

Interaction

Concomitant use of Fesoterodinee with other m-holinoblockers that cause dry mouth, constipation, urinary retention, and other anticholinergic effects may increase the frequency and / or severity of such effects. Anticholinergic agents may interfere with absorption when used concomitantly with certain medications due to their anticholinergic effect on gastrointestinal motility.

Fesoterodinee in doses greater than 4 mg is not recommended for use in patients receiving strong inhibitors of the CYP3A4 isoenzyme, such as ketoconazole, itraconazole and clarithromycin. When ketoconazole and fesoterodine are co-administered, the_cmax and AUC of 5-hydroxymethyl tolterodine, the active metabolite of fesoterodine, increase by almost 2-fold.

Moderate CYP3A4 inhibitors do not have a clinically significant effect on the pharmacokinetics of fesoterodine. When used concomitantly with moderate CYP3A4 inhibitors (for example, erythromycin, fluconazole, diltiazem, verapamil and grapefruit juice), no dose adjustment is required.

Concomitant use of Fesoterodinee 8 mg and the CYP3A4 inducer rifampin 600 mg 1 time/day reduces the_cmax and AUC of the active metabolite of Fesoterodinee by approximately 70% and 75%, respectively, while T_1/2 of the active metabolite does not change.

In individuals with reduced CYP2D6 metabolism, the maximum inhibition of CYP2D6increases the cmax and AUC of the active metabolite of fesoterodine by 1.7 and 2 times, respectively. When used concomitantly with CYP2D6 inhibitors, no dose adjustment is required.

How to take, course of use and dosage

They are taken orally.

The recommended starting dose is 4 mg 1 time / day. Depending on the efficacy and tolerability, the dose can be increased to 8 mg 1 time / day.

Do not exceed the dose of 460 mg / day in patients with impaired renal function with creatinine clearance

It is not recommended to use fesoterodine in patients with impaired liver function (Child-Pugh class C).

Special instructions

If angioedema develops, fesoterodine should be discontinued and appropriate therapy should be initiated immediately. In some cases, angioedema develops after the first dose.

Fesoterodinee should be used with caution in patients with clinically significant narrowing of the bladder outlet, since there is a risk of urinary retention; in patients with reduced gastrointestinal motility (for example, with severe constipation); in patients receiving treatment for angle-closure glaucoma, and only in cases where the expected benefit of therapy exceeds the possible risk; in patients with myasthenia gravis.

Patients should be monitored for symptoms of anticholinergic effects from the central nervous system, especially at the beginning of treatment and after increasing the dose. With the development of such effects, you can reduce the dose or cancel fesoterodine.

It is not recommended to use fesoterodine in patients with severe hepatic impairment, as fesoterodine has not been studied in this category of patients.

It is not recommended to use fesoterodine at a dose of more than 4 mg in patients receiving strong CYP3A4 inhibitors (including ketoconazole, itraconazole, clarithromycin).

When used concomitantly with moderate inhibitors of the CYP3A4 isoenzyme (for example, with erythromycin, fluconazole, diltiazem, verapamil and grapefruit juice), dose adjustment of fesoterodine is not required.

The effect of weak inhibitors of the CYP3A4 isoenzyme (for example, cimetidine) has not been studied in clinical studies, but some pharmacokinetic interactions should be expected, although less pronounced than when used with moderate CYP3A4 inhibitors.

Influence on the ability to drive motor vehicles and manage mechanisms

Patients who experience headache, dizziness or drowsiness after taking Fesoterodinee should refrain from driving vehicles and other potentially dangerous activities.

Active ingredient

Fesoterodyne

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

Adult Doctor’s prescription