Vibegron is a selective β3-adrenergic receptor agonist. It was first approved in the United States in 2020 for the treatment of overactive bladder (OAB) in adults. As a novel drug for OAB treatment, Vibegron increases bladder capacity by activating β3 receptors to relax the detrusor muscle.

Precautions for Vibegron Administration

Renal Impairment

For patients with mild to moderate renal impairment (eGFR 15 to < 90 mL/min/1.73m²), no dose adjustment is required.

Use of Vibegron is not recommended in patients with severe renal impairment (eGFR < 15 mL/min/1.73m²) or those requiring hemodialysis.

Hepatic Impairment

For patients with mild to moderate hepatic impairment (Child-Pugh Class A and B), no dose adjustment is required.

Use of Vibegron is not recommended in patients with severe hepatic impairment (Child-Pugh Class C).

Urinary Retention

Vibegron may cause urinary retention, and the risk is higher in patients with bladder outlet obstruction or those concurrently using antimuscarinic drugs for OAB treatment.

During medication administration, symptoms such as dysuria and weak urine flow should be monitored. If urinary retention occurs, the drug should be discontinued immediately.

Drug Interactions

Digoxin: Vibegron can increase the Cmax (maximum plasma concentration) and AUC (area under the plasma concentration-time curve) of digoxin by 21% and 11%, respectively. The plasma concentration of digoxin should be monitored before and during Vibegron treatment.

CYP3A4 Inhibitors/Inducers: Ketoconazole (a strong CYP3A4 inhibitor), diltiazem (a moderate CYP3A4 inhibitor), and rifampicin (a strong CYP3A4 inducer) have no significant effects on the pharmacokinetics of Vibegron.

Medication Monitoring for Vibegron

Pre-Treatment Assessment

Baseline Examination: Complete blood count, liver function, renal function, and electrolyte levels.

Urination Status Assessment: Obtain a medical history of symptoms such as dysuria and weak urine flow.

Concomitant Medication Assessment: Pay special attention to the use of digoxin.

Allergy History Assessment: Confirm that there is no history of allergy to Vibegron or any components of its formulation.

Routine Monitoring

Urinary Function Monitoring: Regularly assess urination status and monitor for symptoms of urinary retention.

Adverse Reaction Monitoring: Focus on common adverse reactions including headache (4.0%), urinary tract infection (6.6%), nasopharyngitis (2.8%), diarrhea (2.2%), nausea (2.2%), and upper respiratory tract infection (2.0%).

Laboratory Monitoring: Regularly recheck liver and renal function, especially in patients with pre-existing liver or renal impairment.

Special Monitoring

Digoxin Plasma Concentration Monitoring: Measure the baseline concentration before starting Vibegron treatment, and conduct regular monitoring during treatment to adjust the digoxin dose.

Long-Term Medication Monitoring: Extended studies have shown that during long-term use (52 weeks), new adverse reactions with an incidence of ≥ 2% are urinary tract infection (6.6%) and bronchitis (2.9%).