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General Description:

Docusate, identified by CAS number 10041-19-7, is a notable compound with significant therapeutic applications. Docusate, or dioctyl sulfosuccinate, is a stool softener indicated for the treatment of constipation. Docusate acts by increasing the amount of water the stool absorbs in the gut, making the stool softer and easier to pass . Docusate can be orally or rectally administered. Docusate is on the World Health Organization's List of Essential Medicines. However the effectiveness of docusate in treating constipation remains unclear, as several studies report docusate to be no more effective than placebo for increasing the frequency of stool or stool softening . Recently there has been pressure to stop prescribing docusate as it has been identified as an ineffective medicine. Additionally, it does not appear to lessen symptoms associated with constipation such as abdominal cramps. Still docusate is available in over-the-counter products as a common laxative.

Indications:

This drug is primarily indicated for: Indicated for the treatment of constipation associated with dry, hard stools or opioid induced constipation. Though recently, pressure has been building to end the use of docusate over concerns of efficacy. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Absorption:

The absorption characteristics of Docusate are crucial for its therapeutic efficacy: Docusate is not absorbed systemically. As the actions of docusate are local and it is not absorbed, the pharmacokinetic parameters are not available. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Route of Elimination:

The elimination of Docusate from the body primarily occurs through: If docusate is systemically absorbed, it undergoes biliary excretion . Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Pharmacodynamics:

Docusate exerts its therapeutic effects through: Docusate sodium is a laxative and an anionic detergent that supposedly promotes incorporation of water and fats into stool through a reduction in surface tension, resulting in softer fecal mass . Docusate's onset of action is 6-72 hours orally and 2-15 minutes rectally . The effects of docusate are thought to be exerted locally in the jejunum. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Docusate functions by: Recent studies suggest that docusate's mechanism of action is due largely to it's surfactant effect in the intestines, which allow fat and water into the feces to soften the stool. Docusate’s mechanism of action was investigated in 1985 on healthy patients. Docusate was added directly to the jejunum based on calculated concentrations of docusate in the jejunum. At this concentration, there was an increase in secretion of water, sodium, chloride, and potassium as well as a decrease in absorption of glucose and bicarbonate. Based on in vitro data, the authors suggested this effect was due to an increase in intracellular cyclic AMP either directly through docusate or E series prostaglandins. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Docusate belongs to the class of organic compounds known as fatty acid esters. These are carboxylic ester derivatives of a fatty acid, classified under the direct parent group Fatty acid esters. This compound is a part of the Organic compounds, falling under the Lipids and lipid-like molecules superclass, and categorized within the Fatty Acyls class, specifically within the Fatty acid esters subclass.

Categories:

Docusate is categorized under the following therapeutic classes: Alimentary Tract and Metabolism, Drugs for Constipation, Enemas, Laxatives, Softener and Emollient Laxatives, Softeners, Emollients, Succinates, Surface-Active Agents. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Docusate include:

• Water Solubility: Soluble
• Melting Point: 153-157
• logP: 3.95