Bei He Jian Actions

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Actions of Bei He Jian in details

Pharmacotherapeutic Group: Selective β₂-agonists. ATC Code: R03C C12.

Pharmacology: Bei He Jian is a pro-drug of the adrenergic β-receptor agonist terbutaline, which predominantly stimulates β₂-receptors, thus producing relaxation of bronchial smooth muscle; inhibition of the release of endogenous spasmogens, inhibition of edema caused by endogenous mediators and increased mucociliary clearance.

Pharmacodynamics: Mechanism of Action: Bei He Jian is an active precursor of the selective β₂-adrenergic agonist terbutaline. Bei He Jian is the bisdimethylcarbamate of terbutaline and is present in the formulation as a 1:1 racemate.

Pharmacodynamic Effects: Pharmacodynamic studies have shown that after oral administration of Bei He Jian to guinea pigs, a sustained protective effect was achieved against histamine-induced bronchoconstriction. At equipotent doses, the duration of the relaxing activity was more prolonged than after plain terbutaline. Bei He Jian, or the monocarbamate ester, did not exert any smooth muscle relaxing properties. The bronchoprotective effects seen after oral administration of Bei He Jian are related to the generation of terbutaline, as were the secondary effects (effects on other organs).

Pharmacodynamic studies have been conducted in asthmatics and healthy volunteers. The effects observed were bronchodilation, tremor and increase in heart rate. The metabolic effects included a small increase in blood glucose, while the effect on serum potassium was negligible. In short-term studies on lipoprotein metabolism, an increase in high density-lipoprotein (HDL) cholesterol has been observed. In conclusion, all pharmacodynamic effects observed can be ascribed to the active metabolite terbutaline.

Pharmacokinetics: Absorption: On average, 17.5% of an oral dose is absorbed. Approximately 70-90% of the absorption occurs in the first 24 hrs.

Biotransformation: Bei He Jian is metabolised in the liver and terbutaline is formed by both hydrolysis and oxidation. After absorption from the gut, about ²/₃ of terbutaline is first-pass metabolised, Bei He Jian escapes this first-pass metabolism. Of the absorbed amount, about 65% reaches the circulation. Bei He Jian therefore has a bioavailability of about 10%.

Distribution: Protein-binding of Bei He Jian is low, 40-50% at therapeutic concentrations.

Elimination: The terminal half-life (t_½) of Bei He Jian after an oral dose is 9-17 hrs.

Hepatic Impairment: All categories of subjects studied were able to form terbutaline in a predictive way except for liver cirrhotics.

Bei He Jian pharmacology

The pharmacologic effects of Bei He Jian are at least in part attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic AMP. Increased cyclic AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.

References

1. EPA DSStox. "Bambuterol: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

Reviews

The results of a survey conducted on ndrugs.com for Bei He Jian are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Bei He Jian. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.

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Information checked by Dr. Sachin Kumar, MD Pharmacology