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Vibegron for overactive bladder

by egpat         06 May 2024

Vibegron is one of the beta-3 adrenergic receptor agonists. The suffix -begron indicates that this is one of the drugs indicated for the treatment of an overactive bladder. This condition is commonly known as OAB, where the overactivity of the bladder results in an increased frequency of urination, which results in severe lifestyle complications. Normally, the bladder empties the urine when its volume reaches void potential. However, in people with overactive bladders, the urination frequency is increased.

What causes an overactive bladder?

This overactivity of the bladder may be due to many reasons. Any risk of infection may increase its activity. The use of a few of the medicines that produce bladder constriction can also increase urinary frequency. Sometimes damage to the bladder may cause inflammation that leads to overactivity. All these conditions result in enhanced emptying and lead to urinary incontinence. In such a group of people, we can observe a few of the symptoms, like increased urinary urgency and increased urinary frequency.

Normally, the daily urinary frequency may be variable from person to person, but when this urinary frequency is greater than eight times per day, it may indicate an overactive bladder. Even in such people, we can observe nocturia, a condition of urination during bedtime that disturbs sleep.

Vibegron can be given to relieve the symptoms. It acts as a beta-3 agonist; therefore, it stimulates the beta-3 adrenergic receptors located on the bladder neck, which produce bladder relaxation. In other words, Vibegron is a bladder relaxant, and this drug is available as a tablet under the brand name GEMTESA.

How it works in an overactive bladder?

The contraction of the bladder can be controlled by many of the neurotransmitters, so many of the neurons can control bladder activity; among them, norepinephrine is one of the important mediators. Norepinephrine is a mediator of the sympathetic system, and acetylcholine is of the parasympathetic system. Both of these mediators can control bladder activity; norepinephrine produces bladder relaxation, whereas acetylcholine produces bladder contraction.

Vibegron increases the activity of norepinephrine. On the bladder neck, beta-3 receptors are located. Normally, norepinephrine can act on these beta-3 receptors, which produce relaxation of the bladder. However, in people with overactive bladders, urinary frequency is increased, resulting in urinary incontinence. In such people, norepinephrine is not sufficient to activate these beta-3 receptors.

That's why Vibegron can be used externally. It is a selective beta-3 receptor agonist that causes relaxation of the bladder. Because of bladder relaxation, the bladder volume is increased, leading to increased bladder capacity. Therefore, more urine can be accommodated within the bladder, which reduces urinary incontinence and urinary frequency. So for such people, Vibegron can reduce the urinary urgency as well as the frequency, which improves the lifestyle, and even the urination during bedtime can be reduced.

Important precautions

Vibegron produces bladder relaxation, which may result in urinary retention. As more urine can be accommodated within the bladder, more urine is retained. At the same time, the bladder is not contracted but instead relaxed. With the use of vibegron, many people can observe urinary retention, which is quite opposite to urinary incontinence. This situation may be more pronounced when this vibegron is combined with other bladder relaxants. Muscarinic antagonists like darifenacin and solifenacin can act as bladder relaxants, so when these muscarinic antagonists are combined with vibegron the urinary retention is more pronounced, which is fatal to the patient.

For people with any obstruction in the bladder outlet, vibegron should be carefully given because it can also increase urinary retention. So urinary retention is one of the important precautions with this vibegron.

Similarly, few of the drugs, like digoxin, are mainly excreted within the urine, so their excretion through the urine is very important because this medication is cardiotonic with a narrow therapeutic window. This drug can be used in the treatment of heart failure, but any small change in the levels of digoxin may produce toxic effects from this medication. Now, with the use of vibegron urine is retained, and the excretion of digoxin is reduced, which may increase the serum levels of digoxin. This increases digoxin toxicity. So with the use of vibegron, the dose of digoxin should be reduced in order to avoid any digoxin toxicity.

Possible side effects

Vibegron produces various side effects, like headaches and diarrhea. It can also produce some nausea. It can even produce nasopharyngitis and cold-like symptoms. Urinary retention is one of the important side effects that can be observed with prolonged use, along with muscarinic antagonists.

Apart from these side effects, it can also produce pruritus and some itching sensations. Dry mouth and hot flushes are also observed because of the increased vasodilatory response. It can even produce some upper respiratory tract infections as well as urinary tract infections in people with urinary retention.

How is it given?

This drug is available as a tablet at a strength of 75 mg, and the dose of this vibegron is 75 mg given once daily. This tablet can be taken either with or without food, but the same time should be maintained each day. If it is required, the tablet can be crushed, and it can even be combined with apple sauce in order to mask the bitter taste of this tablet as well as to reduce the nausea with this medication.

Conclusion

Vibegron is a beta-3 agonist that acts as a bladder relaxant. It stimulates the beta-3 receptors located on the bladder neck, which produce bladder relaxation, so bladder capacity and bladder volume are increased, which reduces the urinary frequency as well as urinary urgency. But at the same time, vibegron may increase the risk of urinary retention, particularly when this drug is combined with muscarinic antagonists like darifenacin and solifenacin.

Even in people with any obstruction in the bladder outlet, this drug should be carefully given as it may increase urinary retention. Common side effects mainly include headaches, diarrhea, nasopharyngitis, urinary retention, and urinary tract infections. This drug is given as a tablet at a 75 mg dose given once daily. It can be either crushed or combined with apple sauce. It can be taken to mask the bitter taste and reduce the nausea with this medication.



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