Drug Interaction:
Drugs Metabolized by CYP2D6 (e.g. Metoprolol and Desipramine):
Mirabegron is CYP2D6 inhibitor and when used concomitantly with
drugs metabolized by CYP2D6, especially narrow therapeutic index drugs,
appropriate monitoring and possible dose adjustment of those drugs may
be necessary
Digoxin:
When initiating a combination of Myrbetriq and digoxin,prescribe the lowest
dose of digoxin; monitor serum digoxin concentrations to titrate digoxin
dose to desired clinical effect
Indication:
MYRBETRIQ (mirabegron) extended-release tablets, for oral use
Initial U.S. Approval: 2012
Drug Name- Myrbetriq
Active Ingredient - Mirebegron
To treat adults with overactive bladder
Indication-
To treat adults with overactive bladder
Approved by FDA on 28-6-2012 (Ref- FDA Approved List- 2012)
Adverse Reaction:
Most commonly reported adverse reactions (> 2% and > placebo) were
hypertension, nasopharyngitis, urinary tract infection and headache
Contra-Indications:
CONTRAINDICATIONS
None
WARNINGS AND PRECAUTIONS
Increases in Blood Pressure:
Myrbetriq can increase blood pressure.
Periodic blood pressure determinations are recommended, especially in
hypertensive patients. Myrbetriq is not recommended for use in severe
uncontrolled hypertensive patients
Urinary Retention in Patients With Bladder Outlet Obstruction and in
Patients Taking Antimuscarinic Drugs for Overactive Bladder:
Administer with caution in these patients because of risk of urinary retention
Patients Taking Drugs Metabolized by CYP2D6:
Myrbetriq is a moderate inhibitor of CYP2D6.
Appropriate monitoring is recommended and dose adjustment may be necessary
for narrow therapeutic index CYP2D6 substrates
Dosages/ Overdosage Etc:
r
Indication-
To treat adults with overactive bladder
INDICATIONS AND USAGE
Myrbetriq is a beta-3 adrenergic agonist indicated for the treatment of
overactive bladder (OAB) with symptoms of urge urinary incontinence,
urgency, and urinary frequency (1)
DOSAGE AND ADMINISTRATION
Recommended starting dose is 25 mg once daily, with or without food
25 mg is effective within 8 weeks. Based on individual efficacy and
tolerability, may increase dose to 50 mg once daily
Swallow whole with water, do not chew, divide or crush
Patients with Severe Renal Impairment or Patients with Moderate Hepatic
Impairment:
Maximum dose is 25 mg once daily
Patients with End Stage Renal Disease (ESRD) or Patients with Severe
Hepatic Impairment:
Not recommended
DOSAGE FORMS AND STRENGTHS
Extended-release tablets: 25 mg and 50 mg
Patient Information:
PATIENT COUNSELING INFORMATION
See FDA-approved patient labeling (Patient Information)
Inform patients that Myrbetriq may increase blood pressure.
Periodic blood pressure determinations are recommended, especially in patients
with hypertension.
Myrbetriq has also been associated with infrequent urinary tract infections,
rapid heart beat, rash, and pruritis.
Inform patients that urinary retention has been reported when taking mirabegron
in combination with antimuscarinic drugs used in the treatment of overactive bladder.
Instruct patients to contact their physician if they experience these effects while
taking Myrbetriq.
Patients should read the patient leaflet entitled -Patient Information- before starting
therapy with Myrbetriq
Pharmacology/ Pharmacokinetics:
1. Mechanism of Action
Mirabegron is an agonist of the human beta-3 adrenergic receptor (AR) as demonstrated
by in vitro laboratory experiments using the cloned human beta-3 AR.
Mirabegron relaxes the detrusor smooth muscle during the storage phase of the
urinary bladder fill-void cycle by activation of beta-3 AR which increases
bladder capacity.
2. Pharmacokinetics
Absorption
After oral administration of mirabegron in healthy volunteers, mirabegron is absorbed
to reach maximum plasma concentrations (Cmax) at approximately 3.5 hours.
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. In the overall population
of males and females, a 2-fold increase in dose from 50 mg to 100 mg mirabegron
increased Cmax and AUCtau by approximately 2.9- and 2.6-fold, respectively,
whereas a 4-fold increase in dose from 50 to 200 mg mirabegron increased
Cmax and AUCtau by approximately 8.4- and 6.5-fold.
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.
Pregnancy and lactation:
USE IN SPECIFIC POPULATIONS
Pregnancy:
Use only if the benefit to the mother outweighs the potential
risk to the fetus
Nursing mothers:
Myrbetriq is predicted to be excreted in human milk and is not recommended
for use by nursing mothers
Pediatric use:
The safety and effectiveness of Myrbetriq in pediatric patients have not been
established
Geriatric use:
No dose adjustment is recommended for elderly patients
Manufacturer Details