Generic

Mirabegron

Indications

Mirabegron is a beta-3 adrenergic agonist indicated for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency.

Pharmacology

Mirabegron is the first agonist for the beta-3 adrenoceptor. Mirabegron works in two ways: it increases the levels of cyclic adenosine monophosphate (cyclic AMP) and leads to relaxation of the detrusor smooth muscle during the storage phase of the urine bladder fill-void cycle by activating beta-3 adrenoceptors, which increases bladder capacity.

Dosage & Administration

Adults including elderly: The recommended starting dose is Mirabegron 25 mg tablet once daily with or without food. Based on individual patient efficacy and tolerability the dose may be increased to Mirabegron 50 mg tablet once daily.

Renal or hepatic impairment:

Patients with severe renal impairment (ClCr 15 to 29 mL/min or eGFR 15 to 29 mL/min/1.73 m2) or moderate hepatic impairment (Child-Pugh Class B), the daily dose of Mirabegron should not exceed 25 mg tablet once daily.

Mirabegron has not been studied in patients with end stage renal disease (GFR <15 mL/min/1.73 m2 or patients requiring haemodialysis) or severe hepatic impairment (Child Pugh Class C) and it is therefore not recommended for use in these patient populations.

Gender: No dose adjustment is necessary according to gender.

Paediatric population: The safety and efficacy of Mirabegron in children below 18 years of age have not yet been established.

Interactions

Effect of enzyme inhibitors: In healthy volunteers, mirabegron exposure (AUC) was enhanced 1.8-fold in the presence of the powerful CYP3A/P-gp inhibitor ketoconazole. When Mirabegron is taken with CYP3A and/or P-gp inhibitors, there is no need to change the dose. The suggested dose is 25 mg once day with or without meals in patients with mild to moderate renal impairment or mild hepatic impairment who are also taking strong CYP3A inhibitors such itraconazole, ketoconazole, ritonavir, and clarithromycin. Patients with severe renal impairment or moderate hepatic impairment who are also taking powerful CYP3A inhibitors should not take mirabegron.

Inducers of CYP3A or P-gp reduce Mirabegron plasma concentrations. When Mirabegron is given with therapeutic amounts of rifampicin or other CYP3A or P-gp inducers, there is no need to alter the dosage.

Mirabegron’s effect on transporters: Mirabegron is a mild P-gp inhibitor. In healthy volunteers, mirabegron enhanced the Cmax and AUC of the P-gp substrate digoxin by 29% and 27%, respectively. When starting a patient on a combination of Mirabegron and digoxin, the lowest digoxin dose should be provided first. To achieve the intended therapeutic effect, serum digoxin concentrations should be monitored and utilized to titrate the digoxin dose.

Contraindications

Patients with hypersensitivity to the active component or any of the excipients, as well as severe uncontrolled hypertension (systolic blood pressure 180 mm Hg and/or diastolic blood pressure 110 mm Hg), should not take Mirabegron.

Side-Effects

The foremost common side impacts detailed for patients treated with Mirabegron 50 mg amid the three 12-week stage 3 twofold dazzle, fake treatment controlled considers are tachycardia and urinary tract diseases. The recurrence of tachycardia was 1.2% in patients getting Mirabegron 50 mg. Tachycardia driven to cessation in 0.1% patients getting Mirabegron 50 mg. The recurrence of urinary tract contaminations was 2.9% in patients getting Mirabegron 50 mg. Urinary tract contaminations driven to cessation in none of the patients accepting Mirabegron 50 mg. Genuine unfavorable responses included atrial fibrillation (0.2%).

Pregnancy & Lactation

There are constrained sum of information from the utilize of Mirabegron in pregnant ladies. Thinks about in creatures have appeared regenerative harmfulness. Mirabegron isn’t prescribed amid pregnancy and in ladies is arranging to be pregnant. Mirabegron is excreted within the drain of rodents and thus is anticipated to be display in human drain. No thinks about have been conducted to survey the affect of Mirabegron on drain generation in people, its nearness in human breast drain, or its impacts on the breast-fed child. Mirabegron ought to not be managed amid breast-feeding. There were no treatment-related impacts of Mirabegron on ripeness in creatures. The impact of Mirabegron on human ripeness has not been set up.

Precautions & Warnings

End-stage renal disease (GFR 15 mL/min/1.73 m2 or patients requiring haemodialysis): Mirabegron has not been tested in patients with end-stage renal disease (GFR 15 mL/min/1.73 m2 or patients requiring haemodialysis), hence it is not indicated for use in this patient population. Patients with severe renal impairment (GFR 15 to 29 mL/min/1.73 m2) have limited data; a dose reduction to 25 mg is indicated in this population based on a pharmacokinetic study. Mirabegron is not indicated for people who are using powerful CYP3A inhibitors and have severe renal impairment (GFR 15 to 29 mL/min/1.73 m2).

Mirabegron has not been investigated in individuals with severe hepatic impairment (Child-Pugh Class C), hence it is not indicated for usage in this patient group. Mirabegron is not indicated for people who are using powerful CYP3A inhibitors and have moderate hepatic impairment (Child-Pugh Class B).

Mirabegron has the potential to raise blood pressure. Blood pressure should be checked at the start of treatment and at regular intervals while taking Mirabegron, especially in hypertensive individuals. In patients with stage 2 hypertension, there is a scarcity of information (systolic blood pressure 160 mm Hg or diastolic blood pressure 100 mm Hg).

Therapeutic Class

Urinary incontinence/BPH/ Urinary retention.

Storage Conditions

Store in a cold, dry, and light-protected location.

Pharmaceutical Name

General Pharmaceuticals Ltd.