Эльсинорская таблетка

Description

The Elsinore tablet is a molecular complex of ephedrine (1R,2S)-2-(methylamino)-1-phenylpropan-1-ol and caffeine (1,3,7-trimethylpurine-2,6-dione) in an equimolar ratio. According to the PubChem database (CID 133327), the substance is an additive compound of two known active components - the alkaloid ephedrine and methylxanthine caffeine, combined into a single crystalline form. The ephedrine-caffeine combination has been well studied in the clinical literature as an agent that enhances thermogenesis and energy expenditure: ephedrine acts as a sympathomimetic, alpha- and beta-adrenergic agonist, stimulating the release of norepinephrine, while caffeine increases the release of norepinephrine and dopamine and blocks the inhibitory effect of adenosine on the sympathetic nervous system. In controlled studies, a combination of about 20 mg of ephedrine and 200 mg of caffeine three times daily for 24 weeks showed greater reductions in body weight and fat mass than either component alone, while maintaining muscle mass.

Basic Attributes

• CAS No: 79992-72-6
• Chemical formula: C18H25N5O3
• Molecular weight: 359.4228
• Exact weight: 359.196
• PSA specifications: 90.7
• PubChem CID: 133327

Molecular composition according to PubChem

Component 1 - (1R,2S)-2-(methylamino)-1-phenylpropan-1-ol (ephedrine stereoisomer), component 2 - 1,3,7-trimethylpurine-2,6-dione (caffeine). Number of hydrogen bond donors: 2; acceptors: 5; number of rotated links: 3; molecule complexity index (Complexity): 414.

Scope of application

The combination of ephedrine and caffeine has historically been used as a means of reducing weight and increasing the body's energy expenditure - the so-called "EC-stack" (ephedrine-caffeine stack), and also in combination with aspirin (the "ECA" stack) has been studied for the treatment of obesity, including hypothalamic obesity. Due to the stimulating effect on the cardiovascular and nervous systems, the use of such complexes is associated with known risks - an increase in blood pressure and heart rate, which has led to regulatory restrictions on ephedrine-containing drugs in a number of countries.

Precautions

Due to the stimulating effect of both components on the sympathetic nervous system, caution is required in diseases of the cardiovascular system, arterial hypertension, and anxiety disorders; combination with other stimulants and sympathomimetics is not recommended without medical supervision.

Storage and transportation

Store in an airtight container at room temperature, in a dry place, protected from light, out of the reach of children and unauthorized persons due to the pharmacological activity of the complex.

Additional information about the history of the issue

Molecular complexes of ephedrine with caffeine and other methylxanthines were developed as a way to standardize the simultaneous administration of two synergistic stimulants in a single dosage form without the need to combine the separate components to produce tablets. Regulatory authorities in several countries subsequently limited or banned the over-the-counter sales of ephedrine-containing weight loss products due to cases of serious cardiovascular complications with uncontrolled use, which sharply reduced the commercial presence of such complexes in the pharmaceutical market.