vibegron

Action and Spectrum

Actions and Spectrum: 

vibegron is a medication used to treat overactive bladder (OAB) in adults. It works by selectively activating beta-3 adrenergic receptors in the bladder, leading to muscle relaxation, increased bladder capacity, and decreased urgency and frequency of urination. 

The spectrum of activity of vibegron is limited to the treatment of OAB, characterized by urinary urgency, frequency, and incontinence. It is impractical for other urinary tract conditions such as infections or urinary retention. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Headache (4%) 

Nasopharyngitis (2.8%) 

Nausea (2.2%) 

Dry mouth (<2%) 

Residual urine volume increased (<2%) 

Hot flush (<2%) 

Urinary tract infection (6.6%) 

Bronchitis (2.9%) 

Diarrhea (2.2%) 

Upper respiratory tract infection (2%) 

Constipation (<2%) 

Urinary retention (<2%) 

Post-marketing reports 

Rash 

Pruritus 

Urinary retention 

Eczema 

Constipation 

Black Box Warning

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

The contraindications of vibegron include: 

• Hypersensitivity: vibegron should not be used in patients with a known hypersensitivity to vibegron or any of its components. 

• Severe hepatic impairment: vibegron is contraindicated in patients with severe hepatic impairment (Child-Pugh C). 

• Severe renal impairment: vibegron is contraindicated in patients with severe renal impairmt (estimated glomerular filtration rate (eGFR) less than 30 mL/min/1.73m2). 

• Severe hypertension: vibegron should be used cautiously in patients with uncontrolled hypertension. 

• Concomitant use with potent CYP3A4 inhibitors: vibegron should not be used concomitantly with potent CYP3A4 inhibitors, such as ketoconazole, itraconazole, clarithromycin, and ritonavir, as this may increase the exposure of vibegron. 

• Concomitant use with potent CYP2C8 inhibitors: vibegron should not be used concomitantly with potent CYP2C8 inhibitors, such as gemfibrozil, as this may increase the exposure of vibegron. 

Caution: 

• Moderate hepatic impairment: vibegron should be used cautiously in patients with moderate hepatic impairment (Child-Pugh B). 

• Moderate renal impairment: vibegron should be used cautiously in patients with moderate renal impairment (eGFR 30 to less than 60 mL/min/1.73m2). 

• Cardiovascular disease: vibegron should be used cautiously in patients with cardiovascular disease, as it may increase heart rate and blood pressure. 

• Urinary retention: vibegron should be used cautiously in patients with urinary retention or obstruction. 

• Pregnancy and breast-feeding: The safety of vibegron during pregnancy and breastfeeding is unknown. Therefore, it should be used with caution in these populations.

• Interactions with other medications: vibegron may interact with other medications, such as CYP3A4 inducers and inhibitors, and caution should be taken when co-administering these medications. 

• Alcohol consumption: Caution should be taken when consuming alcohol with vibegron, as it may increase the risk of adverse effects, such as dizziness and drowsiness. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.   

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

vibegron is a medication used to treat overactive bladder, and it works by activating beta-3 adrenergic receptors in the bladder. This leads to the relaxation of the detrusor muscle, which controls the bladder and reduces urination urgency. 

vibegron is a selective beta-3 adrenergic receptor agonist, which selectively binds to and activates beta-3 adrenergic receptors in the bladder while avoiding other beta receptors in other body parts. This helps to reduce the risk of adverse effects such as increased heart rate and blood pressure. 

Pharmacodynamics: 

vibegron is a selective beta-3 adrenergic receptor agonist which targets explicitly and activates beta-3 adrenergic receptors in the bladder. These receptors are located in the detrusor muscle, which controls bladder function. 

Activating beta-3 adrenergic receptors in the bladder by vibegron leads to the relaxation of the detrusor muscle, which reduces the urgency to urinate and increases the bladder capacity. vibegron also decreases the number of contractions of the detrusor muscle, which further reduces the urgency to urinate. 

The activation of beta-3 adrenergic receptors by vibegron also leads to an increase in cyclic adenosine monophosphate (cAMP) levels, which plays a role in the relaxation of the detrusor muscle. cAMP activates protein kinase A, which then phosphorylates specific proteins that relax the detrusor muscle. 

Pharmacokinetics: 

Absorption 

vibegron is well absorbed after oral administration, with a bioavailability of approximately 60%. The time to reach maximum plasma concentration (Tmax) is approximately 1 to 2 hours after oral administration. 

Distribution 

vibegron is highly protein-bound (greater than 99%) and has a volume of distribution of approximately 383 L. It crosses the blood-brain barrier and the placenta, but its distribution into breast milk is unknown. 

Metabolism 

vibegron is primarily metabolized in the liver by the cytochrome P450 (CYP) system, mainly by CYP2C9 and CYP3A4 enzymes, into several metabolites. The active metabolite, M18, has approximately 10% of the pharmacological activity of the parent compound. 

Elimination and Excretion 

vibegron and its metabolites are excreted in both urine and feces, with approximately 59% of the dose excreted in urine and 38% in feces. The elimination half-life of vibegron is approximately 24 hours. 

Adminstartion

Administration: 

vibegron is an oral medication that is usually taken once daily. The recommended dose of vibegron is 75 mg, which can be taken with or without food. It is essential to follow the instructions of your healthcare provider or pharmacist regarding the dosage and administration of vibegron. 

The tablet should be swallowed whole with water and not crushed, chewed, or broken. If you miss a dose of vibegron, you should take it as soon as you remember, but if it is close to your next dose, you should skip it and continue with your regular dosing schedule.

It is essential not to take a double dose to compensate for a missed dose. vibegron should be stored at room temperature, away from heat, moisture, and light. Keeping vibegron out of the reach of children and pets is essential. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: vibegron 

Why do we use vibegron? 

vibegron is a medication used to treat overactive bladder (OAB) syndrome in adults. OAB is characterized by urinary urgency, frequency, and sometimes incontinence, which can significantly impact a person’s quality of life. vibegron works by activating beta-3 adrenergic receptors in the bladder, which leads to the relaxation of the detrusor muscle, reduced urinary urgency and frequency, and increased bladder capacity. 

The use of vibegron is appropriate for individuals who experience symptoms of OAB and have not responded well to lifestyle changes, such as fluid management and pelvic floor exercises. vibegron is often prescribed as part of a comprehensive treatment plan, including behavioral therapy and other medications.