Silodosin

Details:

Silodosin is an α-adrenergic receptor antagonist invented by Japan's Kissei Pharmaceutical Company. It has a very good therapeutic effect on urination disorders related to benign prostatic hyperplasia. The selective effect on the urethra is 12 and 7.5 times higher than that of prazosin and tamsulosin, respectively. It can significantly inhibit the contraction of the human prostate caused by norepinephrine; it has a dose-dependent effect on the hyperactivity of the bladder in the rat model of benign prostatic hypertrophy The inhibitory effect and can increase the pressure threshold of bladder contraction. These data suggest that in addition to improving bladder function, silodosin is also effective in relieving symptoms related to benign Chemicalbook prostatic hypertrophy. Compared with similar drugs prazosin and tamsulosin, silodosin is highly selective for α1A-receptors located in the prostate and bladder neck, but has no obvious affinity for α1B- and α1D-receptors. It blocks the α1A-receptors in this area, relaxes smooth muscles, and leads to improved urine flow and alleviation of BPH symptoms. Silodosin's selective binding to α1A-receptors is greater than that of cardiovascular-related α1B-receptors, thereby maximizing the activity of target organs and minimizing the potential impact on blood pressure.

Benign prostatic hyperplasia (BPH for short) is one of the most common diseases among middle-aged and elderly men. It is characterized by non-malignant enlargement of the prostate. The obstructive and irritating symptoms caused by it have brought great influence to the life of the elderly. Big impact. In recent years, with the increasing level of industrialization in my country, the gradual increase in animal protein intake and the extension of life expectancy, the incidence of benign prostatic hyperplasia has increased year by year. More than 50% of elderly people aged 60 years or older suffer from this disease, and more than 90% of elderly people aged 85 years or older suffer from this disease. The cause of the disease has not yet been clarified, but it is generally believed to be related to the secretion and metabolic disorders of sex hormones and cholesterol. Some people believe that due to the weakening of the pituitary-gonadotropin-testis pathway of action in the elderly, or due to endogenous changes, the testis degenerates, decreases in sexual function, decreases in testosterone values, and increases in the prostate due to the increase in connective tissue, resulting in glandular epithelial changes and prostate enlargement. Big. Enlargement of the prostate will compress the urethra, causing poor urine flow in the bladder and even blocking the bladder outlet. There are α1A-adrenergic receptors in the human prostate. The activation of this receptor can aggravate urethral obstruction and dysuria. Therefore, by blocking the binding of α1A-adrenergic receptors, the obstructed prostate smooth muscle can be relaxed, thereby improving symptoms. In recent years, 5α-reductase inhibitors and α1-adrenergic receptor (α1-AR) blockers (silodosin) have been used clinically, and they have achieved good results. They are considered to be a major factor in the treatment of benign prostatic hyperplasia. Achievement.