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DL-Methylephedrine API Manufacturers & Suppliers

General Description:

DL-Methylephedrine, identified by CAS number 1201-56-5, is a notable compound with significant therapeutic applications. Methylephedrine is a sympathomimetic amine that appears in various over-the-counter cough and cold medications throughout the world , , . The abuse of methylephedrine-containing medications has been reported in Japan. Methylephedrine is not legally available in the United States, but has been identified in cases of drug abuse .

Indications:

This drug is primarily indicated for: Used as an antitussive and decongestant . Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

DL-Methylephedrine undergoes metabolic processing primarily in: Methylephedrine is metabolized to give ephedrine and norephedrine . This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of DL-Methylephedrine are crucial for its therapeutic efficacy: Methylephedrine is rapidly absorbed following oral administration . Peak plasma concentrations of ephedrine (from which methylephedrine is derived) occur 2-3h after administration . Due to the fact that methylephedrine is a derivative of ephedrine , peak plasma concentrations are likely similar. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of DL-Methylephedrine is an important consideration for its dosing schedule: 3-6 hours (Ephedrine) . This determines the duration of action and helps in formulating effective dosing regimens.

Route of Elimination:

The elimination of DL-Methylephedrine from the body primarily occurs through: The primary compound excreted in urine is unchanged methylephedrine (33-40% of dose), followed by the metabolite _methylephedrine-N-oxide_ (15% of dose), and approximately 8% of the dose excreted as ephedrine after 24 hours. About 70% of the dose is excreted in the urine as metabolites over 72 hours . Alkaline urine reduces elimination to 20-35% of the dose . Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

DL-Methylephedrine is distributed throughout the body with a volume of distribution of: Ephedrine: 2.5-3.0 L/kg . Methylephedrine is a derivative of ephedrine and quickly distributed throughout the body . This metric indicates how extensively the drug permeates into body tissues.

Pharmacodynamics:

DL-Methylephedrine exerts its therapeutic effects through: This drugs acts as an antitussive, bronchodilator, and adrenergic receptor agonist . It stimulates the alpha and beta adrenergic receptors, relieving cough and congestion . As with other adrenomimetic amines, the drugs in this class are much less potent than norepinephrine itself. Members of this class of drugs increase both systolic and diastolic blood pressure, cardiac contractility, and cardiac output; in general, however, they do not increase heart rate. Bronchial smooth muscle relaxation of prolonged duration occurs, and pupils dilate . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

DL-Methylephedrine functions by: The pharmacology of methylephedrine is similar to that of other members of the ephedra alkaloid class of drugs. These compounds are sympathomimetic amines because they mimic the effects of the catecholamines on the sympathetic nervous system. These alkaloids permeate the blood-brain barrier and have a direct central nervous system stimulant effect with peripheral effects; the peripheral effects are indirect and primarily mediated by norepinephrine release . Methylephedrine expands the bronchia by relaxing the bronchial muscles . The decrease in urination with sympathomimetic use is increased through activation of the alpha-adrenoceptors of the smooth muscles of the bladder . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

DL-Methylephedrine 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:

DL-Methylephedrine is categorized under the following therapeutic classes: Adrenergic Agonists, Adrenergic alpha-2 Receptor Agonists, Adrenergic alpha-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 DL-Methylephedrine include:

• Melting Point: 208
• Boiling Point: 251.3
• logP: 2.47