What Is Tamsulosin Hydrochloride?

Tamsulosin hydrochloride sustained-release tablets are used to treat symptoms such as dysuria caused by benign prostatic hyperplasia, such as frequent urination, increased nocturia, and dysuria.

Foreign name: Tamsulosin Hydrochloride Sustained Release Tablets
Whether prescription drugs: prescription

Dosage form: Sustained-release tablets
Drug type: chemical
Specifications: 0.2mg

Ingredients of Tamsulosin Hydrochloride Sustained-release Tablets :

Tamsulosin hydrochloride chemical name: 5-[(2R) -2- [2- [2- [2- (2-ethoxyphenoxy) ethyl] amino] propyl] -2-methoxybenzenesulfonamide mono The chemical structure of hydrochloride is:

Molecular formula: C ₂₀ H ₂₈ N ₂ O ₅ S · HCl
Molecular weight: 444.98

Properties of Tamsulosin Hydrochloride Sustained-release Tablets :

This product is a white tablet

Indications for Tamsulosin Sustained-release Tablets

It is mainly used for symptoms such as dysuria caused by prostatic hyperplasia, such as frequent urination, increased nocturia, and difficulty urinating. Since this product is used to improve the smooth muscle function of the urethra, bladder neck, and prostate, it does not shrink the proliferative glands, so it is suitable for mild and moderate patients and those who do not cause severe dysuria. If severe urinary retention has occurred This product should not be taken alone.

Dosage and dosage of tamsulosin hydrochloride sustained-release tablets

The recommended oral dosage is 0.2 mg / d (one tablet / day) for adults, taken once after a meal; the dosage can be increased or decreased as appropriate according to age and symptoms.

Adverse reactions of tamsulosin hydrochloride sustained-release tablets

Common side effects include nausea, vomiting, loss of appetite, and occasional rashes. And there are different degrees of dizziness, staggering or orthostatic hypotension and tachycardia during treatment. Individual cases may not be able to adhere to medication due to dizziness and hypotension. Long-term use shows elevated AST, ALT and LDH values.

Taboxin hydrochloride sustained-release tablets contraindications

Patients with a history of allergies to this product and patients with renal dysfunction are disabled.

Precautions for tamsulosin hydrochloride sustained-release tablets

1. Allergic reactions such as rash should be discontinued. 2. Orthostatic hypotension should be used with caution. Patients with a history of orthostatic hypotension or when taking antihypertensive drugs should pay attention to changes in blood pressure. 3. Liver function should be checked regularly for long-term medication. 4. Don't increase in elderly patients with renal insufficiency.

Tamsulosin hydrochloride sustained-release tablets for children

Children are not recommended to use this product.

Drug Interactions of Tamsulosin Sustained-release Tablets

1. Nifedipine, atenolol, and phenylproterate: Patients should take nifedipine, atenolol, and phenylproteril together without adjusting the dose of tamsulosin hydrochloride. 2. Warfarin: There is no test result for the combination of tamsulosin hydrochloride and warfarin, so caution should be exercised in combination with warfarin. 3. Digoxin and theophylline: Do not adjust the dosage when tamsulosin hydrochloride is used with digoxin or theophylline. 4. Fasting urine: Do not adjust the dose in combination with fasting urine. 5. Cimetidine: Cimetidine significantly reduces the clearance of tamsulosin hydrochloride and significantly increases the AUC, so it should be used with caution in combination with cimetidine, especially when the dose is greater than 0.4 mg.

Pharmacology and Toxicology of Tamsulosin Sustained-release Tablets

Pharmacological effect This product is tamsulosin hydrochloride, which is a blocker of adrenergic 1 receptor subtype 1A. Its affinity for 1 receptor is 5400-24000 times stronger than 2 receptor. Because the 1 receptor in the urethra, bladder neck and prostate is mainly the receptor 1A, this product has a highly selective blocking effect on the urethra, bladder neck and prostate smooth muscle. The ability of this product to suppress the rise in internal urethral pressure is 13 times the ability to suppress the rise of vasodilation pressure, so this product can reduce the chance of orthostatic hypotension after taking the drug. This product can improve urination disorders, and it has been proven that this product can reduce the pressure of the prostate in the urethral pressure curve, but it has no effect on the rhythmic bladder contraction and the bladder pressure curve. Toxicology studies Carcinogenic male rats were administered at a dose of 43 mg / kg / day, and female rats were administered at a dose of 52 mg / kg / day. There was no increase in tumor incidence. Breast fibroma increased when female rats received 5.4 mg / kg (P <0.015). The highest dose of systemic indication (AUC) of tamsulosin hydrochloride in the rat carcinogenicity test was 3 times the maximum human dose (0.8 mg per day). Male mice were given a dose of 127 mg / kg / day and female mice were given a dose of 1.58 mg / kg / day. Male mice did not have obvious tumorigenesis. Female mice were given 2 highest doses of 45 and 158 mg / kg / day for 2 years. P <0.0001), and the incidence of breast cancer (P <0.0075) increased significantly. In the carcinogenicity test of mice, the indication of maximum dose generation system (AUC) of tamsulosin hydrochloride is 8 times that of the maximum therapeutic dose of 0.8 mg / day in humans. The increased incidence of mammary gland hyperplasia in mice and rats is secondary to excessive plasma prolactin caused by tamsulosin hydrochloride. Whether tamsulosin hydrochloride increases human prolactin is unclear. The regulation of prolactinous endocrine adenomas found in rodents in humans is unclear. Mutagenicity of mutagenic tamsulosin hydrochloride has not been confirmed in the inverse Amer test in vitro, mouse lymphoma thymidine kinase analysis, non-listed DNA repair junction analysis and Chinese Eastern European rat ovary cells and humans Analysis of lymphocyte chromosomal abnormalities, in vivo sister chromosome analysis exchange and mouse micronucleus analysis did not reveal mutation effects. Reproductive toxicity was given to male rats tamsulosin hydrochloride capsules in a single dose or 300 mg / kg / day multiple doses, which significantly reduced fertility. The mechanism of male fertility decline may be the change of semen composition trapped in the vagina and damage to ejaculation. The effect on fertility will improve 3 days after a single dose or 4 weeks after multiple doses. Full recovery will be achieved within 9 weeks after withdrawal of multiple doses. 10 and 100 mg / kg / day tamsulosin hydrochloride multiple doses do not change the fertility of male mice. The effects of tamsulosin hydrochloride capsules on semen composition and function have not been demonstrated. Studies on female rats have shown that single-dose or 300 mg / kg / day multiple-dose dextrose or racemic hydrochloride tamsulosin capsules significantly reduce fertility. The decline in fertility after single-dose administration in female rats is associated with impaired fertilization. Administration of 10 or 100 mg / kg / day multiple doses of racemate did not significantly impair fertility in female rats.

Pharmacological effects of tamsulosin hydrochloride sustained-release tablets

This product is a drug for the treatment of benign prostatic hyperplasia (BPH) and is a selective ₁ adrenergic receptor blocker. Its main mechanism of action is to selectively block _1A adrenergic receptors in the prostate, relax the smooth muscles of the prostate, and thereby improve symptoms such as dysuria caused by benign prostatic hyperplasia.

Pharmacokinetics of Tamsulosin Sustained-release Tablets :

Experiments show that tamsulosin hydrochloride is well absorbed, mainly distributed in the liver and kidneys, rats, and dogs. There is no accumulation in oral administration for 21 consecutive days. Rottanox hydrochloride sustained-release preparations in healthy adults took 0.1-0.6 mg of oral sustained-release preparation 7 to 8 hours later, and the blood concentration reached a peak, with a C _max of 5.9 ± 1.0 ng / ml. Both C _max and AUC increased in proportion to the administered dose. The drug is mainly metabolized in the liver. The excretion rate of the prototype drug in the urine within 30 hours after administration is 12% -24%, and the urine excretion rate after continuous administration is unchanged.