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Information about Docusate

Docusate is an orally available, over-the-counter laxative and stool softener used to treat or prevent constipation.

Liver safety of Docusate

Docusate has not been linked to serum enzyme elevations during therapy or to clinically apparent liver injury with jaundice.

Mechanism of action of Docusate

Docusate (dok’ ue sate) is a stool softener and surfactant previously known as dioctyl sodium [or calcium] sulfosuccinate (DSS).

Clinical use of Docusate

Docusate is commonly used to treat or prevent constipation and to promote bowel regularity in hospitalized, bed-bound or immobilized persons. Docusate salts are thought to act as detergents, reducing surface tension of liquids and fatty substances in the intestine, thereby softening stool consistency. The efficacy of docusate in treatment and prevention of constipation has not been well documented. However, extensive experience with its use has documented its safety and tolerability.

FDA approval information for Docusate

Docusate has been in use in the U.S. since the 1950s and current indications are for treatment and prevention of constipation.

Dosage and administration for Docusate

Docusate is available without prescription in capsules of 50, 100, 240 and 250 mg generically and under various brand names such as Colace, Doxidan, Regulex, Silace and Surfak. A liquid formulation for oral use is also available.

The typical oral dose is 50 to 300 mg daily until bowel movements are normal.

Side effects of Docusate

Common side effects include diarrhea, abdominal cramping, nausea, bitter taste and dizziness.

Antidiarrheal agents

Antidiarrheal agents include bulk forming agents, hydroscopic agents, bile acid resins, bismuth, inhibitors of intestinal motility, non-absorbed antibiotics and hormones. Bulk forming agents include methylcellulose; hydroscopic agents include pectin and kaolin; bile acid resins are cholestyramine, colestipol and colesevalam; inhibitors of intestinal motility include opioids such as diphenoxylate and loperamide. Antibiotics include rifamycin and rifaximin which are non-absorbed and are used for travelers' diarrhea. Hormones with antidiarrheal activity include octretide and somatostatin. Most antidiarrheal agents are active locally in the small intestine and colon and are largely not absorbed. Some, however, have been implicated in rare causes of liver injury (senna, cascara, cholestyramine). Telotristat is a relatively new agent that inhibits the synthesis of serotonin and is used specifically for the diarrhea of carcinoid syndrome.

Antiemetics are a diverse group of medications that act at different points in the pathways that regulate nausea and vomiting. These include antihistamines, anticholinergic agents, phenothiazines, serotonin type 3 receptor blockers, centrally acting benzamides, cannabinoid receptor agonists, substance P antagonists and miscellaneous.

Anticholinergic Agents


Cannabinoid Receptor Agonists

Serotonin 5-HT3 Receptor Antagonists

Substance P/Neurokinin 1 Receptor Antagonists


Acid peptic disease/antiulcer agents that include antacids, the histamine type 2 receptor blockers (H2 blockers), and the proton pump inhibitors (PPIs). These agents are some of the most commonly taken medications and are very well tolerated, most being available both by prescription and over-the-counter. While many of these drugs are approved for use in duodenal and gastric ulcer disease, their major use is for acid reflux and indigestion.

Histamine H2 Receptor Antagonists (H2 Blockers) Cimetidine, Famotidine, Nizatidine, Ranitidine

Proton Pump Inhibitors

Cathartics, laxatives or agents for constipation include bulk forming agents, osmotic agents, stool wetting agents, nonspecific stimulants, prokinetic agents and agents that increase fluid secretion. Many of these therapies are not systemically absorbed and none are considered particularly hepatotoxic. Naldemedine and naloxegol are opioid antagonists and are used to treat the constipation associated with opioid use.

Inflammatory bowel disease encompasses several disorders, most commonly ulcerative colitis and Crohn colitis. Agents can be classified as 5-aminosalicyclic acid (5-ASA) based agents, immunosuppressive drugs, antitumor necrosis factor agents, corticosteroids, antibiotics and miscellaneous.

5-Aminosalicyclic Acid (5-ASA) Derivatives

Immunosuppressive Agents

Tumor Necrosis Factor Antagonists


Irritable Bowel Syndrome Agents Antimuscarinics/Antispasmodics [See Anticholinergic agents

Prokinetic Agents - See Serotonin 5-ht4 receptor agonists Alosetron, Cisapride, Domperidone, Linaclotide, Lubiprostone, Metoclopramide, Plecanatide, Prucalopride, Tegaserod


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