Imidafenacin (Tablets) Instructions for Use

Marketing Authorization Holder

R-Pharm JSC (Russia)

Manufactured By

Kyorin Pharmaceutical Group Facilities, Co. Ltd. (Japan)

ATC Code

G04BD14 (Imidafenacin)

Active Substance

Imidafenacin (Rec.INN registered by WHO)

Dosage Form

Imidafenacin

Film-coated tablets, 0.1 mg: 100 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets from light red to light reddish-brown or reddish-violet in color, round, flat-cylindrical, with the inscription “UT 0.1” printed in blue ink on one side.

Excipients: microcrystalline cellulose (PH-301), partially pregelatinized starch, povidone (Kollidon 90F), magnesium stearate.

Film coating composition Opadry 03A45009 (red) [hypromellose, titanium dioxide, red ferric oxide, carnauba wax].
Composition of the printing ink for the tablet (Blue Ink No.4 for tablet printing) white shellac, red ferric oxide, FD&C Blue No.1 Aluminum Lake, FD&C Blue No.2 Aluminum Lake, FD&C Red No.3 Aluminum Lake, carnauba wax, fatty acid glycerol ester, anhydrous ethanol, 1-butanol.

10 pcs. – blisters (10) – cartons.

Clinical-Pharmacological Group

Drug reducing the tone of the smooth muscles of the urinary tract

Pharmacotherapeutic Group

Drugs used in urology; drugs for the treatment of frequent urination and urinary incontinence

Pharmacological Action

A specific competitive inhibitor of muscarinic receptors, predominantly of the M3 and M1 subtypes.

Pharmacokinetics

The absorption of imidafenacin from the gastrointestinal tract is almost 100% with an absolute bioavailability of 57.8%. Plasma protein binding is 87.1-88.8%, mainly with albumin and α1-acid glycoprotein. After oral administration, about 40% of imidafenacin undergoes first-pass metabolism in the liver.

Imidafenacin is metabolized mainly in the liver by the enzymes CYP3A4 and UGT1A4. The main metabolites in plasma are M2 (oxidized metabolite on the imidazole ring of imidafenacin), M4 (M2 metabolite with a cleaved ring), and M9 (N-glucuronide of imidafenacin).

After a single oral administration of ¹⁴C-imidafenacin to healthy adult males at a dose of 0.25 mg on an empty stomach, 95% of the dose was excreted as radioactive substance in urine and feces within 192 hours after administration (65.6% in urine and 29.4% in feces). Less than 10% of the dose was excreted unchanged in urine.

Indications

Symptomatic treatment of overactive bladder syndrome (frequent urination, urgent need to urinate, urge urinary incontinence) in adult patients.

ICD codes

Dosage Regimen

Administer orally at a dose of 0.1 mg (100 mcg)twice daily.

Swallow the tablet whole with a sufficient amount of water.

The maximum daily dose must not exceed 0.2 mg (200 mcg).

Adhere strictly to the twice-daily schedule to maintain consistent plasma concentrations.

Do not exceed the prescribed dose or frequency of administration.

If a dose is missed, take it as soon as remembered unless it is nearly time for the next dose. Do not double the dose to catch up.

The duration of therapy is determined by the prescribing physician based on therapeutic response and tolerability.

Discontinuation should be considered if satisfactory symptomatic control is not achieved after an appropriate treatment period.

Adverse Reactions

Nervous system disorders common – drowsiness; uncommon – dysgeusia, dizziness, headache; frequency unknown – lack of sensation.

Psychiatric disorders frequency unknown – hallucinations, delirium.

Eye disorders common – photophobia, blurred vision; uncommon – unnatural eye sensation, xerophthalmia, asthenopia, eyelid edema, diplopia, acute glaucoma.

Cardiac disorders uncommon – extrasystole, palpitations, increased blood pressure.

Respiratory, thoracic and mediastinal disorders uncommon – sore throat, dry throat, hoarseness, cough.

Gastrointestinal disorders very common – dry mouth; common – abdominal discomfort, constipation; uncommon – dry lips, stomatitis, anorexia, nausea, abdominal pain, bloating, diarrhea, dyspepsia, gastritis, vomiting, abnormal stool character, impaired liver function.

Renal and urinary disorders common – dysuria; uncommon – urinary tract infections, urinary retention.

Skin and subcutaneous tissue disorders uncommon – pruritus, rash, dry skin.

General disorders and administration site conditions uncommon – back pain, edema, malaise, chest pain, weakness, asthenia, thirst.

Investigations common – residual urine; uncommon – erythropenia, leukopenia, thrombocytopenia, increased triglycerides, increased cholesterol, increased AST, ALT, GGT, ALP, LDH activity, increased bilirubin level, increased blood uric acid concentration, positive urine test for leukocytes and erythrocytes, positive urine test for protein, increased creatinine concentration.

Contraindications

Hypersensitivity to imidafenacin; urinary retention; severe heart disease; angle-closure glaucoma; myasthenia gravis; gastrointestinal obstruction, paralytic ileus, decreased gastrointestinal motility and muscle tone, megacolon; pregnancy, breastfeeding period; age under 18 years.

Use in Pregnancy and Lactation

Imidafenacin should not be used during pregnancy and while breastfeeding.

Use in Hepatic Impairment

Imidafenacin should be used with caution in patients with impaired liver function.

Use in Renal Impairment

Imidafenacin should be used with caution in patients with impaired renal function.

Pediatric Use

Contraindicated for use under 18 years of age.

Special Precautions

Imidafenacin should be used with caution in patients with dysuria, arrhythmia, impaired liver function, impaired renal function, parkinsonism, cerebrovascular disorders, ulcerative colitis (toxic megacolon may develop), hyperthyroidism.

The drug is not indicated for use in patients with dementia or confusion who cannot clearly recognize the symptoms of an overactive bladder.

In patients with obstructive diseases of the lower urinary tract, including benign prostatic hyperplasia, residual urine volume should be measured before treatment. Patients should be carefully monitored during treatment, paying attention to an increase in residual urine volume.

In the absence of satisfactory treatment efficacy, the drug should not be used for a long time; alternative rational therapy should be considered.

Effect on ability to drive vehicles and operate machinery

Caution should be exercised when engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions during the period of drug use.

Since m-cholinolytics can cause accommodation disturbances, including photophobia, blurred vision, and eye pathology, patients should be instructed to exercise caution when handling potentially dangerous machinery.

Drug Interactions

M-cholinolytics, antihistamines, tricyclic antidepressants, phenothiazine derivatives, MAO inhibitors may enhance the anticholinergic effect of imidafenacin. Symptoms such as thirst, dry mouth, constipation, and dysuria may develop.

When imidafenacin was co-administered with itraconazole in healthy adult males, the C_max and AUC values of imidafenacin increased approximately 1.3-fold and 1.8-fold, respectively, compared with monotherapy.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.