High Purity Mirabegron CAS 223673-61-8 99% Purity

Mirabegron More Info

Mirabegron is a medication belonging to a class of drugs known as beta-3 adrenergic receptor agonists, with the CAS Registry Number 223673-61-8. It is the first agent of its kind approved for the treatment of overactive bladder and represents a significant therapeutic advancement over traditional anticholinergic medications. As an extended-release formulation, it is designed for once-daily oral administration, providing consistent symptom control throughout the day and night. The compound is commercially available under the brand name Myrbetriq among others, and has expanded treatment options for patients with bladder control disorders.

The mechanism of action of mirabegron involves selective activation of beta-3 adrenergic receptors located primarily on the detrusor smooth muscle of the urinary bladder. During the urine storage phase, sympathetic nerve stimulation predominates, and activation of these receptors promotes relaxation of the bladder muscle, allowing the bladder to accommodate increasing volumes of urine without inappropriate contractions. This contrasts with anticholinergic medications that work by blocking muscarinic receptors responsible for bladder contractions. By directly relaxing the detrusor muscle during filling, mirabegron effectively increases bladder capacity and reduces the frequency of involuntary contractions without impairing the ability to void normally. Importantly, beta-3 receptor stimulation does not interfere with the parasympathetic-mediated voiding process, preserving normal urinary function.

The primary clinical application of mirabegron is the treatment of overactive bladder syndrome in adults, characterized by symptoms of urinary urgency, increased daytime frequency, and urgency incontinence. It is indicated for use either as monotherapy or in combination with solifenacin, another bladder medication, for patients who have not achieved adequate symptom control with single-agent therapy. Additionally, mirabegron has received approval for the treatment of neurogenic detrusor overactivity in pediatric patients aged three years and older, a condition resulting from neurological disorders affecting bladder control such as spinal cord injury or multiple sclerosis. Beyond its approved indications, emerging research suggests potential utility in other urological conditions, including medical expulsive therapy for distal ureteral stones.

From a pharmacokinetic perspective, mirabegron exhibits unique properties that influence its clinical use. Following oral administration, peak plasma concentrations are achieved within approximately three to five hours. The drug undergoes extensive distribution in the body, with a volume of distribution of approximately sixteen hundred liters, and is about seventy-one percent bound to plasma proteins. Metabolism occurs through multiple pathways including dealkylation, oxidation, direct glucuronidation, and amide hydrolysis, with the parent compound being the major circulating component. The terminal elimination half-life is approximately fifty hours in adults, supporting once-daily dosing. For pediatric patients receiving the extended-release suspension, administration with food is essential as fasting significantly increases drug exposure.

The safety profile of mirabegron is distinguished by its cardiovascular effects, which require monitoring during treatment. Common adverse effects include increases in blood pressure and heart rate, which are dose-dependent and reversible upon treatment discontinuation. The thorough QT studies demonstrated that at the maximum recommended dose of fifty milligrams, the mean increase in systolic blood pressure was approximately four millimeters of mercury greater than placebo, with corresponding increases in heart rate up to seven beats per minute. Other frequently reported adverse events include urinary tract infection, tachycardia, atrial fibrillation, headache, and nasopharyngitis. Importantly, real-world pharmacovigilance data from the FDA Adverse Event Reporting System has identified additional signals including hypertension, urinary retention, dry mouth, and, rarely, more serious events such as angioedema and anti-neutrophil cytoplasmic antibody positive vasculitis. Due to these effects, mirabegron is contraindicated in patients with severe uncontrolled hypertension, and blood pressure should be measured before initiating treatment and monitored regularly during therapy, with particular attention to individuals with pre-existing cardiovascular conditions.