What Is Nebivolol?

Nebivolol, commonly known as "nebivolol hydrochloride", is a selective 1 adrenergic receptor antagonist with vasodilating activity and no endogenous sensory nerve activity. It is used for the treatment of patients with mild to moderate hypertension and can also be used for the treatment of angina pectoris and congestive heart failure.

Nebivolol

English name: nebivolol

Product Name: Nebilet Bystolic

Phonetic name: naibiluoer

Categories: Nebivolol hydrochloride raw materials, Nebivolol hydrochloride tablets are chemical drugs 3.1

Chemical name: 2,2 '-[iminobis (methylene)] bis [6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] di [2-hydroxy- 2- (6-fluoro-3,4-dihydro-2H-1-benzopyran-2-)] ethylamine

Formulation: tablet, 5mg / tablet.

Dosage: once a day, one tablet at a time, liver and kidney dysfunction and the elderly can be appropriately reduced.

Adverse reactions: This product has fewer adverse reactions. The most common are headache, dizziness, fatigue, paresthesia, constipation, and diarrhea. These adverse reactions are usually transient and rarely discontinued. This product does not cause orthostatic hypotension, rarely induces heart failure or causes severe bradycardia.

Former research and development company (person): Johnson & Johnson developed (US) Italian Menarim company was granted marketing authorization; it was first listed in Germany in May 1997, and successively listed in Britain and other countries in May 1999. MYLAN BERTEK was approved for listing in the United States on December 17, 2007.

Transfer unit: Shandong Taitian New Drug Development Co., Ltd., research and development, nebivolol hydrochloride raw materials, nebivolol hydrochloride tablets have been submitted for clinical approval, in the state of review, transfer of clinical approval.

1. Nebivolol is a potent and selective third-generation beta receptor blocker, which blocks the beta1 receptor 290 times more strongly than the beta2 receptor, and

Use case

A 4-week, multicenter, double-blind, randomized, placebo-controlled, parallel grouped dose study of 509 hypertensive patients showed that the effect of 0.5-10 mg to reduce systolic and diastolic blood pressure was dose-dependent. A dose of more than 2.5 mg once a day can achieve a significant antihypertensive effect. The antihypertensive effect of 5 mg once a day is significantly better than 2.5 mg or placebo. The antihypertensive effect of 10 mg once a day is not better than 5 mg.

In a multicenter, double-blind, placebo-controlled trial of 114 patients with essential hypertension, it was found that this product, 5 mg a day for 8 weeks, can reduce supine and orthostatic blood pressure, and slow heart rate and diastolic blood pressure to normal. Or decrease by more than 10% to 65%.

A number of multicenter randomized double-blind controlled studies in patients with mild to moderate hypertension showed that 5 mg or 10 mg of antihypertensive effect of this product is equivalent to 50 mg of atenolol and 100 mg of metoprolol. Sustained-release preparation of nifedipine 20 mg, twice a day or lisinopril 10 mg a day; significantly better than enalapril 10 mg a day, hydrochlorothiazide 25 mg a day and placebo.

In a randomized double-blind parallel grouped controlled study involving 30 patients with non-insulin-dependent diabetes mellitus and hypertension, this product has a blood pressure lowering effect similar to atenolol at 5 mg / day for 6 months, and does not affect insulin sensitivity. Sex.

Ten patients with mild to moderate hypertension and renal arteriosclerosis received 5 mg of this product for 1 day for 4 weeks. As a result, the patient's diastolic blood pressure and plasma renin were significantly reduced, and renal function was not significantly changed.

In a randomized double-blind placebo-controlled crossover study in 16 patients with stable angina pectoris, this product was given 5 mg once a day for two weeks and had antianginal and anti-myocardial ischemic effects. This product can significantly slow down the heart rate during rest and exercise, lower blood pressure, also improve the left ventricular dilatability, reduce the load before and after the heart, and thus have a protective effect on left ventricular function.

A number of studies have shown that 5 mg of this product, once a day, can improve cardiac function in patients with stable congestive heart failure.

-blockers are used for the treatment of hypertension and myocardial ischemia. Currently, -blockers used in the market (referring to the treatment of cardiovascular system diseases, excluding ophthalmic indications and other diseases) are mainly as follows Several types: metoprolol, bisoprolol, esmolol, labelol, arolol, sotalol, propranolol and atenolol.

Although the number of beta-blocker medications has fluctuated within the past five years, the amount of medications used has remained a steady upward trend. The total market size of beta-blockers in 1999 was approximately 150 million yuan, and in 2003 it rose to 3-350 million yuan, with an average annual growth rate of 20%. The difference in the number of medications and the amount of medication reflects the relatively large price fluctuations of these products, because the proportion of near-mouth products in this category of products is quite large, and the impact of price on the number of medications is relatively large.

summary

Of the above 8 products, between 1999 and 2003, in terms of sales amount, except for atenolol, which gradually decreased, the other 7 products showed an upward trend, or at least remained stable (Punamir). Metoprolol, bisoprolol, and esmolol consistently occupy the top three sales shares, and their sales are significantly higher than the other five products. Metoprolol's share of sales has decreased year by year, while bisoprolol and esmolol's share has increased year by year. In 2003, the annual sales of the three products mentioned above reached 150 million, 120 million and 50 million, respectively. In terms of sales volume, Metoprolol, Bisorolol and Punelol are among the top three. The general feature of beta blockers is that there are few new products and competition is not fierce. The appearance of nebivolol has added new highlights to beta blockers.

Nebivolol is different from other -receptor antagonists as a third-generation -receptor antagonist. It combines highly selective -receptor antagonists with nitric oxide-mediated vasodilation and is beneficial to endothelial function. Role. Can be well tolerated for patients with hypertension and heart failure. This product is approved for the treatment of essential hypertension in Europe. It is also used in combination with standard treatment for mild to moderate chronic heart failure (CHF) in patients over 70 years of age, which can effectively reduce mortality and cardiovascular disease in elderly CHF patients. Inpatient combination evaluation endpoint. By virtue of its protective effect on the heart, good antihypertensive effect, good tolerability and few adverse reactions, this product will surely grab a large share in the antihypertensive drug market and bring huge social benefits to enterprises And economic benefits. This product has a bright market prospect and huge potential.

Analysis of Intellectual Property Status:

There are no compound patents or indication patents for this project in China. Therefore, there is no core patent for this product, and the synthetic process patent can be bypassed, so there is no intellectual property problem.

Nebivolol Hydrochloride Tablets Instructions

No

Domestic declarations

(Domestic applications are in accordance with Class 3.1 of Chemicals)

Acceptance No.Drug manufacturer's review date

CXHL0700321 Nebivolol Hydrochloride Tablets Shandong Taitian New Drug Development Co., Ltd. 2007-11-26

CXHL0700320 Nebivolol Hydrochloride Shandong Taitian New Drug Development Co., Ltd. 2007-11-26

CXHL0700105 Nebivolol Hydrochloride Beijing Furuizheng Medical Technology Institute 2007-06-22

CXHL0700104 Nebivolol Hydrochloride Tablets Beijing Furui Kangzheng Medical Technology Institute 2007-06-22