Mirabegron (3 brand names, 2 dosage forms, 1 route)
Available dosage forms: TABLET, EXTENDED RELEASE, FOR SUSPENSION, EXTENDED RELEASE.
Routes of administration: ORAL.
Brand Names
- MIRABEGRON
- MYRBETRIQ
- MYRBETRIQ GRANULES
Contraindications
Mirabegron for extended-release oral suspension is contraindicated in patients with known hypersensitivity reactions to mirabegron or any inactive ingredients of the oral suspension [see Adverse Reactions (6.1, 6.2)].
Adverse Reactions
The following adverse reactions are discussed in more detail in other sections of the labeling. Hypertension [see Warnings and Precautions (5.1)] Urinary Retention [see Warnings and Precautions (5.2)] Angioedema [see Warnings and Precautions (5.3)]
Drug Interactions
Drug interaction studies were conducted in adult patients to investigate the effect of coadministered drugs on the pharmacokinetics of mirabegron and the effect of mirabegron on the pharmacokinetics of coadministered drugs (e.g., ketoconazole, rifampin, solifenacin succinate, tamsulosin, and oral contraceptives) [see Clinical Pharmacology ( 12.3 )]. No dose adjustment is recommended when these drugs are coadministered with mirabegron. The following are drug interactions for which monitoring is recommended:
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. Although mirabegron showed very low intrinsic activity for cloned human beta-1 AR and beta-2 AR, results in humans indicate that beta-1 AR stimulation occurred at a mirabegron dose of 200 mg.
Overdosage
Mirabegron has been administered to healthy volunteers at single doses up to 400 mg. At this dose, adverse events reported included palpitations (1 of 6 subjects) and increased pulse rate exceeding 100 beats per minute (bpm) (3 of 6 subjects). Multiple doses of mirabegron up to 300 mg daily for 10 days showed increases in pulse rate and systolic blood pressure when administered to healthy volunteers. Treatment for overdosage should be symptomatic and supportive. In the event of overdosage, pulse rate, blood pressure and ECG monitoring is recommended.