Etafedrine API Manufacturers

General Description:

Etafedrine, identified by CAS number 48141-64-6, is a notable compound with significant therapeutic applications. Etafedrine (INN) or ethylephedrine is a long-acting bronchodilator and has been an ingredient combined with other drugs in the brand names Nethaprin and Dalmacol . It was previously available as both the free base and as the hydrochloride salt manufactured by Sanofi-Aventis (now Sanofi) has been discontinued . Ethylephedrine is be formed by alkylating ephedrine with ethyl iodide. The hydrochloride is be prepared by passing hydrogen chloride through a solution of ethylephedrine in diethyl ether . This belongs to the family of medications called _decongestants_. It acts by narrowing blood vessels in the nasal passages, helping to relieve nasal congestion .

Indications:

This drug is primarily indicated for: Conditions characterized by bronchial congestion and bronchospasm when an expectorant or bronchodilator action is required, such as acute bronchitis, acute episodes of chronic bronchitis and bronchial asthma , . Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Absorption:

The absorption characteristics of Etafedrine are crucial for its therapeutic efficacy: Similar to its parent drug, ephedrine, it is readily and completely absorbed from the gastrointestinal tract; plasma peak concentrations are reached an hour after ingestion . A single oral dose of 24 mg produced an average peak plasma concentration of 0.10 mg/L . The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Etafedrine is an important consideration for its dosing schedule: It has a plasma half-life ranging from 3 to 6 hours depending on urinary pH . This determines the duration of action and helps in formulating effective dosing regimens.

Route of Elimination:

The elimination of Etafedrine from the body primarily occurs through: Excreted mainly in the urine . Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Etafedrine is distributed throughout the body with a volume of distribution of: Similar to ephedrine, at about 3L/kg . This metric indicates how extensively the drug permeates into body tissues.

Pharmacodynamics:

Etafedrine exerts its therapeutic effects through: Etafedrine helps to control the cough which is associated with irritation of the mouth and throat that is not alleviated by cough medications that are less strong . The results of one study in 48 individuals showed that lung FEV1 (forced expiratory volume) and lung VC (vital capacity) were significantly improved with etafedrine, sleep improved, and patients showed improved appetite in addition to the suppression of cough . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Etafedrine functions by: A sympathomimetic agent, etafedrine acts on the sympathetic receptors of the bronchial tree, relieving spasm in a manner similar to that of ephedrine . Etafedrine acts as a selective β adrenoreceptor agonist, thereby mediating its bronchodilator effects without increasing norepinephrine release . This is distinctly different from ephedrine and tyramine which trigger the release of epinephrine or norepinephrine. N-ethylation of ephedrine suppresses the indirect sympathomimetic activity and markedly enhances the efficacy on beta 2- adrenoceptors . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Etafedrine belongs to the class of organic compounds known as phenylpropanes. These are organic compounds containing a phenylpropane moiety, classified under the direct parent group Phenylpropanes. This compound is a part of the Organic compounds, falling under the Benzenoids superclass, and categorized within the Benzene and substituted derivatives class, specifically within the Phenylpropanes subclass.

Categories:

Etafedrine is categorized under the following therapeutic classes: Adrenergic Agonists, Adrenergic beta-2 Receptor Agonists, Adrenergic beta-Agonists, Agents producing tachycardia, Agents that produce hypertension, Alcohols, Amines, Amino Alcohols, Drugs that are Mainly Renally Excreted, Ethylamines, Phenethylamines, Propanolamines, Propanols. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Etafedrine include:

• Melting Point: 108-110