Anatomical Therapeutic Chemical Classification System
Bisacodyl is a locally acting laxative from the diphenylmethane derivatives group having a dual action. As a contact laxative, for which also antiresorptive hydragogue effects have been described, bisacodyl stimulates after hydrolysis in the large intestine, the mucosa of both the large intestine and of the rectum. Stimulation of the mucosa of the large intestine results in colonic peristalsis with promotion of accumulation of water, and consequently electrolytes, in the colonic lumen. This results in a stimulation of defecation, reduction of transit time and softening of the stool. Stimulation of the rectum causes increased motility and a feeling of rectal fullness. The rectal effect may help to restore the “call to stool” although its clinical relevance remains to be established.
Docusate sodium is an anionic wetting agent, which acts as a faecal softener by lowering the surface tension and allowing penetration of accumulated hard dry faeces by water and salts. Docusate sodium also possesses stimulant activity.
Lactitol is a sugar alcohol used as a replacement bulk sweetener for low calorie foods with approximately 40% of the sweetness of sugar. Lactitol also promotes colon health as a prebiotic. Lactitol is a laxative and is used to prevent or treat constipation.
Lactulose is a synthetic disaccharide which is metabolised by gastro-intestinal bacterial flora to low molecular weight acids (chiefly lactic and acetic acids). There is no endogenous metabolising enzyme in the human gut. Its mode of action in constipation is as an osmotic agent producing soft stools.
Linaclotide is a Guanylate Cyclase-C receptor agonist (GCCA) with visceral analgesic and secretory activities. Through its action at GC-C, linaclotide has been shown to reduce visceral pain and increase GI transit in animal models and increase colonic transit in humans.
High molecular weight (4000) macrogols are long linear polymers which retain water molecules by means of hydrogen bonds. When administered by the oral route, they lead to an increase in volume of intestinal fluids.
Magnesium carbonate, MgCO3 (archaic name magnesia alba), is an inorganic salt. The most common magnesium carbonate forms are the anhydrous salt called magnesite (MgCO3) and the di, tri, and pentahydrates known as barringtonite (MgCO3·2 H2O), nesquehonite (MgCO3·3 H2O), and lansfordite (MgCO3·5 H2O), respectively. The primary use of magnesium carbonate is the production of magnesium oxide by calcining.
Magnesium oxide (MgO), or magnesia, is an empirical formula of MgO and consists of a lattice of Mg2+ ions and O2− ions held together by ionic bonding.
Magnesium sulfate is a saline purgative. It can be employed locally in various inflammatory conditions, due to its osmotic action.
Mannitol is a naturally occurring sugar alcohol used clinically primarily for its osmotic diuretic properties.
Methylcellulose is a simple bulking agent.
Methylnaltrexone bromide is a selective antagonist of opioid binding at the mu-receptor. As a quaternary amine, the ability of methylnaltrexone bromide to cross the blood-brain barrier is restricted. This allows methylnaltrexone bromide to function as a peripherally acting mu-opioid antagonist in tissues such as the gastrointestinal tract, without impacting opioid-mediated analgesic effects on the central nervous system.
Naldemedine is an antagonist of opioid binding at the mu-, delta-, and kappa-opioid receptors. Naldemedine functions as a peripherally-acting mu-opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids without reversing the central nervous system (CNS)-mediated opioid effects.
Naloxegol is a PEGylated derivative of the mu-opioid receptor antagonist naloxone. PEGylation reduces naloxegol’s passive permeability and also renders the compound a substrate for the P-glycoprotein transporter. Naloxegol functions as a peripherally-acting mu-opioid receptor antagonist in the gastrointestinal tract, thereby decreasing the constipating effects of opioids without impacting opioid-mediated analgesic effects on the central nervous system.
The sugar moiety of the sennosides is removed by bacteria in the large intestine releasing the active anthrone fraction. This stimulates peristalsis via the submucosal and myenteric nerve plexuses.
Sodium picosulfate is a locally acting laxative from the triarylmethane group, which after bacterial cleavage in the colon, has a dual-action with stimulation of the mucosa of both the large intestine and of the rectum.