Mirabegron; Uses, Dosage, Side Effects, Drug Interactions

Mirabegron; Uses, Dosage, Side Effects, Drug Interactions

Mirabegron is an orally bioavailable agonist of the human beta-3 adrenergic receptor (ADRB3), with muscle relaxing, neuroprotective and potential antineoplastic activities. Upon oral administration, mirabegron binds to and activates ADRB3, which leads to smooth muscle relaxation. Mirabegron also restores sympathetic stimulation in mesenchymal stem cell (MSC) niches, inhibits JAK2-mutated hematopoietic stem cell (HSC) expansion and blocks the progression of myeloproliferative neoplasms (MPNs). Lack of sympathetic stimulation of the MSC and HSC niche is associated with the development of MPNs.

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. Mirabegron activates the β3 adrenergic receptor in the detrusor muscle in the bladder, which leads to muscle relaxation and an increase in bladder capacity.

Mechanism of action of mirabegron

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.

Indications of mirabegron

Contra-Indications of mirabegron

  • Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.
  • Severe uncontrolled hypertension defined as systolic blood pressure ≥ 180 mm Hg and/or diastolic blood pressure ≥ 110 mm Hg.
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Dosages of mirabegron

  • Strengths: 25 mg; 50 mg

Urinary Incontinence

  • Initial dose: 25 mg orally once a day
  • Maintenance dose: 25 to 50 mg orally once a day based on individual patient efficacy and tolerability

Urinary Frequency

  • Initial dose: 25 mg orally once a day
  • Maintenance dose: 25 to 50 mg orally once a day based on individual patient efficacy and tolerability

Side effects of mirabegron

The most common

More common

Less common

Drug interactions of Mirabegron

Mirabegron may interact with following drugs,suppliment & may change the efficasy of drugs

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Pregnancy & Lactation

FDA Pregnancy Category C

Pregnancy 

Mirabegron falls into category C. In animal studies, pregnant animals were given this medication and had some babies born with problems. No well-controlled studies have been done in humans. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.

Lactation

Although mirabegron was found in the milk of rats in animal studies, it is not known if mirabegron is excreted in human milk. As many drugs are excreted into human milk and have the potential of causing harm to nurse infant, mirabegron should only be used during nursing if it is clearly needed.

References

 

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