Miracle Tablets For Overactive Bladder

Definition

Overactive bladder is a common chronic lower urinary tract dysfunction, defined by the International Anti-Incontinence Society as a clinical syndrome characterized by urinary urgency. Overactive bladder may or may not be accompanied by incontinence; frequent urination and nocturia are often present, but similar symptoms due to infection, local disease, or metabolic factors are not present.

Pathogenic factors

Overactive bladder is caused by overactive detrusor muscle, that is, involuntary contraction of the detrusor muscle during bladder filling, resulting in increased intravesical pressure and a sudden strong urge to urinate. May be related to the stimulation of the muscarinic receptor M3 on the smooth muscle cell membrane. There are many pathogenic factors of overactive bladder, some are spontaneous, while others are caused by old age, peripheral and central nervous system diseases, or due to bladder reconstruction and abnormal detrusor function.

Commonly used drugs

With the deepening of the understanding of the etiology, the development of new tablets for overactive bladder has been very active in recent years. The tablets for overactive bladder are mainly muscarinic receptor antagonists. If the drugs lack specificity to the bladder, they can cause adverse reactions of central anticholinergics, and their clinical application will be limited. Trospium chloride is an orally available quaternary ammonium compound with muscarinic antagonism, which is an effective class of tablets for overactive bladder. This product can inhibit esophagus and gastrointestinal motility, inhibit gallbladder emptying and gastric acid secretion, but it is currently only used for the treatment of overactive bladder with symptoms of urinary frequency, urgency and urge incontinence. This product is hydrophilic, and the conventional therapeutic dose is not easy to pass through the normal blood-brain barrier, so its adverse reactions to the nervous system are less than other muscarinic antagonists.

Pharmacodynamic properties

Effects on peripheral muscarinic cholinergic receptors

Trospium chloride is a competitive acetylcholine antagonist that can specifically bind to M1, M2, and M3 receptors with high affinity. This product does not bind to nicotinic acetylcholine receptors, and has a stronger affinity for muscarinic receptors than other anticholinergic drugs such as oxybutynin, tolterodine, darifenacin and solifenacin.

Effects on central muscarinic cholinergic receptors

Like all quaternary ammonium compounds, trospium chloride is hydrophilic, and its molecules have difficulty penetrating the lipid layer. Therefore, the drug is not easy to pass through the normal blood-brain barrier, and the central permeability is very weak. Healthy volunteers took trospium chloride 45mg a day, and EEG test confirmed that its central anticholinergic effect was very weak. Results of another study in healthy volunteers showed that trospium chloride had a better effect than oxybutynin, propiverine, and tolterodine, with less effect on sensory accuracy and alertness . It is suggested that trospium chloride may have good curative effect on the elderly patients with overactive bladder and urinary incontinence, as well as patients with neuropathy such as Alzheimer's disease.

Compared with oxybutynin, this product has potential clinical application advantages in terms of the effect on sleep. A randomized, double-blind study of young healthy volunteers showed that, compared with tolterodine and trospium chloride, the oxybutynin group had no significant difference in sleep questionnaire and psychological test data, but the rapid eye movement sleep was relatively suppressed, and has a mild sedative effect.

Adverse reactions

According to US prescribing information, the most common adverse reactions (incidence <1%) of trospium chloride are dry mouth, constipation, headache, fatigue, epigastric pain, dyspepsia, urinary retention, flatulence, and dry eyes. Rare adverse reactions (incidence <0.5%) were tachycardia, blurred vision, abdominal distension, vomiting, dysgeusia, dry throat and skin. Clinical reports of 1 case of angioedema, urinary retention, tachyarrhythmia, and mild to moderate elevation of serum liver enzymes have also been reported, with an incidence of <1%.

Position in the treatment

Overactive bladder has a high incidence and can affect HR-QOL. It places a heavy financial burden on patients, families, healthcare providers, and society as a whole.

Muscarinic antagonists have long been the main tablets for overactive bladder, but many drugs lack bladder selectivity and anticholinergic adverse reactions are common. Compared with the commonly used oxybutynin, trospium chloride not only has the same efficacy but also is better tolerated, and pharmacokinetic studies have shown that its drug interactions are less. Post-marketing drug surveillance studies have confirmed that trospium chloride can substantially improve the HR-QOL of patients, and is effective for elderly patients, while reducing treatment costs. Preliminary studies have shown that this product is also effective in children, but it is not recommended for children at this time. Intravesical administration of this product, especially in patients with bladder spasm caused by indwelling catheterization, also requires further evaluation of efficacy. In addition, the clinical efficacy of this product in combination with other drugs should also be studied. In conclusion, the products is  effective and well-tolerated tablets for overactive bladder treatment.