Product Information
Registration Status: ActiveSIN14623P
BETMIGA PROLONGED-RELEASE TABLET 50MG is approved to be sold in Singapore with effective from 2014-09-15. It is marketed by ASTELLAS PHARMA SINGAPORE PTE LTD, with the registration number of SIN14623P.
This product contains Mirabegron 50mg in the form of TABLET, FILM-COATED, EXTENDED-RELEASE. It is approved for ORAL use.
This product is manufactured by Avara Pharmaceutical Technologies in UNITED STATES, and Inc. in NETHERLANDS.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
Mirabegron is a beta-3 adrenergic receptor agonist for the management of overactive bladder. It is an alternative to antimuscarinic drugs for this indication. FDA approved on June 28, 2012.
Indication
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.
Mechanism of Action
Mirabegron is a potent and selective agonist for beta-3 adrenergic receptors. Once beta-3 receptors are activated, the detrusor smooth muscle relaxes to allow for a larger bladder capacity. At higher doses (200 mg), there is a potential for mirabegron to activate beta-1 and beta-2 adrenergic receptors.
Pharmacokinetics
- Absorption
- The absolute bioavailability increases from 29% at a dose of 25 mg to 35% at a dose of 50 mg. Mean Cmax and AUC increase more than dose proportionally. This relationship is more apparent at doses above 50 mg. Females generally have a lower magnitude of increase of Cmax and AUCtau compared to males when doses of mirabegron doubles or quadruples. Steady state concentrations are achieved within 7 days of once daily dosing with mirabegron. After once daily administration, plasma exposure of mirabegron at steady state is approximately double that seen after a single dose. Tmax, oral dose, healthy subjects= 3.5 hours;
- Distribution
- Vd, steady state, IV dose = 1670 L. This high value suggests that mirabegron is extensively distributed in the body.
- Metabolism
- Mirabegron is metabolized via multiple pathways involving dealkylation, oxidation, (direct) glucuronidation, and amide hydrolysis. The major circulating entity is mirabegron. Two major and inactive metabolites (phase 2 glucuronides) are produced. Although mirabegron is a substrate for CYP2D6 and CYP3A4, its role in the elimination of the drug is limited. Studies also suggest that CYP3A4 is the main enzyme that facilitates the oxidative metabolism of the drug. Furthermore, butylcholinesterase, uridine diphospho-glucuronosyltransferases (UGT), and possibly alcohol dehydrogenase may be involved with the metabolism of mirabegron.
- Elimination
Clearance
Total body clearance (CLtot), IV dose = 57 L/h; Renal clearance (CLR) = 13 L/h
Toxicity
Most commonly reported adverse reactions (> 2% and > placebo) were hypertension, nasopharyngitis, urinary tract infection and headache
Active Ingredient/Synonyms
Mirabegron | Mirabegron |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.