Oxyphenisatin is a stimulant laxative that has been used by mouth and as an enema. Oxyphenisatin was introduced as Lavema by Winthrop in US in 1959. Oxyphenisatin was used as a cleansing enema apart from x-ray studies and prior to urinary, gastro-intestinal and cholecystography x-ray examination. Oxyphenisatin was also used for preoperative preparation of the large intestine and colon. May be mixed with barium for x-ray examination of the large intestine. Oxyphenisatin may cause jaundice. Oxyphenisatin-induced liver damage usually occurs when the drug has been taken for at least six months and usually two years. Oxyphenisatin was withdrawn in most countries in the early 1970s.

Bisacodyl is typically prescribed for relief of constipation and for the management of neurogenic bowel dysfunction as well as part of bowel preparation before medical examinations, such as for a colonoscopy. Some drugs (e.g., diuretics, angiotensin converting enzyme inhibitors, angiotensin receptor blockers, or non-steroidal anti-inflammatory drugs) increase risk due to fluid and electrolyte changes. Most common adverse reactions (> 3%) are overall discomfort, abdominal fullness, abdominal cramping, nausea, and vomiting.

Danthron, a natural product, was originally extracted from the roots and rhizome of Polygonaceae plant. Danthron is an anthraquinone. Danthron has been widely administrated as a laxative since the 1900s. In the United States, danthron has been forbidden to continual use as laxative because it is considered to be a carcinogen. In the UK, it is not marketed alone but in combination with poloxamer 188 as co-danthramer and with docusate as co-danthrusate; in the UK, its use is strictly restricted to the elderly and to the terminally ill of all ages because of concerns about carcinogenicity and hepatotoxicity. It has only a limited role in the treatment of constipation.

Pentaerythritol is an inactive metabolite of pentaerythritol tetranitrate, a drug that is used for the treatment of angina pectoris.

Bisoxatin (Laxonalin, Wylaxine) acetate is a stimulant laxative that has been used in the treatment of constipation. The drug showed good effects to habitual constipation and dolichocolon but was not sufficient acting in megacolon. It seems that the drug is effective to constipation due to functional disorders but the effect is not sufficient to constipation caused chiefly by organic colonic changes. No side effect was observed even in long term administration.

Linaclotide (marketed under the trade name Linzess and Constella) is a peptide agonist of the guanylate cyclase 2C (GC-C). Once linaclotide and its active metabolite binds to GC-C, it has local effect on the luminal surface of the intestinal epithelium. Activation of GC-C by linaclotide results in the intra- and extracellular increase of cyclic guanosine monophosphate concentrations (cGMP). This elevation of cGMP levels stimulates the secretion of chloride and bicarbonate into the intestinal lumen via activation of cystic fibrosis transmembrane conductance regulator (CFTR) ion channel. The metabolite of linaclotide MM-419447 (CCEYCCNPACTGC) contributes to the pharmacologic effects of linaclotide. Ultimately, linaclotide helps patients with IBS (especially with constipation) as GI transit is accelerated and the release of intestinal fluid is increased. In animal models, a decrease in visceral pain after administration of linaclotide may be observed. A decrease in the activity of pain-sensing nerves occurs as a result of an increase in extracellular cGMP. It was approved by the FDA in August 2012 for the treatment of chronic idiopathic constipation and irritable bowel syndrome with constipation (IBS-C) in adults.