Classification by Mechanism of Action
Globally, all cholagogues are divided into two major categories depending on the stage of bile dynamics they affect:
- Choleretics — stimulate the bile-forming function of the liver.
- Bile-expelling agents — affect the tone and motility of the biliary tract. This group is further subdivided into cholekinetics (increase gallbladder tone) and cholespasmolytics (decrease biliary tract tone).
Choleretics: Stimulators of Bile Formation
The primary mechanism of choleretics is the direct stimulation of hepatocyte secretory function. In addition to increasing bile volume, they provide a kinetic "washing" effect, preventing ascending infection, and a litholytic effect by increasing the concentration of bile acid salts (cholates) to prevent cholesterol precipitation.
There are four subgroups:
- True choleretics (contain bile acids): Animal-derived preparations. Holenzyme contains dry bile combined with pancreatic and intestinal mucosal enzymes. Allochol is supplemented with garlic and nettle extracts, as well as activated charcoal (to suppress fermentation). Liobil features a high concentration of bile acids (5 times greater than analogues). Combined enzyme preparations (Festal, Panzinorm) are also included here.
- Synthetic choleretics: Chemical compounds that often possess additional antimicrobial and anti-inflammatory properties (Hydroxymethylnicotinamide). Some agents, such as Osmalide, provide a hypolipidemic effect by lowering blood cholesterol and bilirubin levels.
- Herbal choleretics: Extracts of Helichrysum arenarium (Flamin), rose hips (Holosas), corn silk, and the multi-herb complex Liv-52. They act via essential oils and flavonoids, exerting a complex secretory, anti-inflammatory, and antimicrobial effect.
- Hydrocholeretics: Mineral waters (containing sulfate anions) and valerian root rhizomes. They increase bile volume through the water component by limiting water reabsorption, thus making the bile more fluid.
Agents Regulating Bile Elimination
These agents act at the level of the gallbladder and biliary sphincters.
Cholekinetics irritate the mucosal receptors of the duodenum, triggering the release of endogenous cholecystokinin. As a result, the gallbladder actively contracts while the sphincters relax, leading to substantial gallbladder evacuation. These include:
- Polyhydric alcohols: xylitol and sorbitol (administered as 10% solutions).
- Saline agents: magnesium sulfate (hypertonic 20–25% solution on an empty stomach) and artificial Carlsbad salt.
- Herbal components: the alkaloid berberine, tansy flowers, and vegetable oils (olive, sunflower, sea buckthorn).
- Chole-spasmolytics (cholelithics), conversely, relax the smooth muscle of the biliary system. They are necessary to relieve spasm, facilitate bile outflow, and eliminate hyperkinetic dyskinesias. This effect is produced by antimuscarinics (anticholinergics), nitrates (nitroglycerin), methylxanthines, and combination medications (e.g., Olimetin, containing a complex of essential oils and purified sulfur).
Contraindications and Safety
When prescribing cholagogues, contraindications must be strictly considered. An absolute contraindication for all bile-containing and secretion-stimulating preparations is mechanical obstruction to bile outflow (obstructive jaundice).
Furthermore, many preparations (e.g., Allochol, Olimetin) are contraindicated in peptic ulcer disease of the stomach and duodenum, acute hepatitis, and active hepatic dystrophy.