Vibegron

Vibegron is a Beta-3 adrenergic agonist belonging to Drug for overactive bladder.

Vibegron is a beta-3 adrenergic agonist the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency in adults.

Vibegron is having Tmax of approximately 1-3 hours. The mean apparent volume of distribution of vibegron is 6304 L. Vibegron is 49.6–51.3% bound to human plasma proteins. CYP3A4 is the main enzyme responsible for the metabolism of vibegron, which plays a minor role in the elimination of vibegron. Two predominant metabolic pathways are oxidation and glucuronidation to form two oxidative metabolites and three glucuronide metabolites. Approximately 59% of the radiolabeled dose was recovered in feces, in which 54% of that amount was in the unchanged parent drug form. About 20% of the radioactivity was recovered in urine, in which 19% of the amount was in the unchanged form.

Vibegron shows side effects like Headache, diarrhea, nausea, fever, runny or stuffy nose, sore throat, or other signs of infection.

Vibegron is available in the form of Oral tablets.

Vibegron is available in India, US, Spain, Canada, China, UK, France, Italy, and Russia.

Vibegron belongs to the Drug for overactive bladder acts as a Beta-3 adrenergic agonist.

Vibegron, a selective human beta-3 adrenergic receptor agonist, activates beta-3 adrenergic receptors in the bladder resulting in relaxation of the detrusor smooth muscle during the urine storage phase, thus increasing bladder capacity.

The Data of Onset and duration of action of Vibegron is not clinically established.

The Tmax of Vibegron is approximately 1-3 hours.

Vibegron is available in the form of Oral tablets.

Vibegron tablets is taken orally, usually once daily.

Vibegron is a beta-3 adrenergic agonist the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency in adults.

Vibegron is a Beta-3 adrenergic agonist belonging to Drug for overactive bladder.

Vibegron, a selective human beta-3 adrenergic receptor agonist, activates beta-3 adrenergic receptors in the bladder resulting in relaxation of the detrusor smooth muscle during the urine storage phase, thus increasing bladder capacity.

Vibegron is approved for use in the following clinical indications

• Overactive Bladder Syndrome

Vibegron is a beta-3 adrenergic agonist the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency in adults.

• Overactive Bladder Syndrome

Oral: 75 mg once daily.

Vibegron is available in various strengths as 75 mg.

Vibegron is contraindicated in patients with

• Patients with known hypersensitivity to vibegron or any components of the product.

• Bladder flow obstruction

Use with caution in patients with bladder outlet obstruction and in patients using concomitant muscarinic antagonists; may increase the risk of urinary retention. Monitor for signs and symptoms of urinary retention; discontinue use if urinary retention occurs.

• Hepatic impairment

Use is not recommended in patients with severe impairment; has not been studied.

• Renal impairment

Use is not recommended in patients with end-stage kidney disease (eGFR <15 mL/minute/1.73 m² with or without hemodialysis); has not been studied.

There are no data on the presence of vibegron in human milk, the effects of the drug on the breastfed infant, or the effects on milk production. When a single oral dose of radiolabeled vibegron was administered to postnatal nursing rats, radioactivity was observed in milk. When a drug is present in animal milk, it is likely that the drug will be present in human milk.

There are no available data on vibegron use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.

• Common

Constipation, diarrhea, nausea, xerostomia, Increased post-void residual urine volume, urinary retention, Headache, Nasopharyngitis, upper respiratory tract infection.

• Rare

Eczema, pruritus, skin rash, Fixed drug eruption.

Digoxin: Vibegron may increase the serum concentration of Digoxin.

The common side effects of Vibegron include the following

• Common side effects

Headache, diarrhea, nausea, fever, runny or stuffy nose, sore throat, or other signs of infection.

• Rare side effects

Difficulty emptying the bladder or weak urine stream, fever or painful, urgent, or frequent urination.

• Pregnancy

There are no available data on vibegron use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.

• Nursing Mothers

There are no data on the presence of vibegron in human milk, the effects of the drug on the breastfed infant, or the effects on milk production. When a single oral dose of radiolabeled vibegron was administered to postnatal nursing rats, radioactivity was observed in milk. When a drug is present in animal milk, it is likely that the drug will be present in human milk.

• Pediatric Use

The safety and effectiveness of vibegron in pediatric patients have not been established.

• Geriatric Use

Of 526 patients who received vibegron in the clinical studies for OAB with symptoms of urge urinary incontinence, urgency, and urinary frequency, 242 (46%) were 65 years of age or older, and 75 (14%) were 75 years of age or older. No overall differences in safety or effectiveness of vibegron have been observed between patients 65 years of age and older and younger adult patients.

There is no experience with inadvertent GEMTESA over dosage. In case of suspected overdose, treatment should be symptomatic and supportive.

Pharmacodynamic

Vibegron selectivity for beta-3 adrenergic receptors is >9000 times higher than for β1AR or β2AR. Vibegron improves clinical symptoms of overactive bladder by increasing bladder capacity without affecting bladder contraction. It significantly increases the functional bladder volume in a dose-dependent manner, which results in prolongation of the interval between voids. In clinical studies, vibegron inhibited detrusor bladder contractions in a concentration-dependent manner, reduced voiding pressure, and increased bladder compliance.

Pharmacokinetics

• Absorption

Vibegron is having Tmax of approximately 1-3 hours.

• Distribution

The mean apparent volume of distribution of vibegron is 6304 L. Vibegron is 49.6–51.3% bound to human plasma proteins.

• Metabolism and Excretion

CYP3A4 is the main enzyme responsible for the metabolism of vibegron, which plays a minor role in the elimination of vibegron. Two predominant metabolic pathways are oxidation and glucuronidation to form two oxidative metabolites and three glucuronide metabolites. Approximately 59% of the radiolabeled dose was recovered in feces, in which 54% of that amount was in the unchanged parent drug form. About 20% of the radioactivity was recovered in urine, in which 19% of the amount was in the unchanged form.

• https://www.drugs.com/vibegron.html
• https://go.drugbank.com/drugs/DB14895
• https://medlineplus.gov/druginfo/meds/a621015.html
• https://reference.medscape.com/drug/gemtesa-vibegron-4000077
• https://www.rxlist.com/gemtesa-drug.htm#warnings
• https://www.uptodate.com/contents/vibegron-drug-information?search=vibegron&source=panel_search_result&selectedTitle=1~8&usage_type=panel&kp_tab=drug_general&display_rank=1