Classification by Mechanism of Action
Globally, all choleretic drugs are divided into two large categories depending on which stage 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 divided into cholekinetics (increase gallbladder tone) and cholespasmolytics (decrease biliary tract tone).
Choleretics: stimulants of bile formation
The main mechanism of action of choleretics is the direct stimulation of the secretory function of hepatocytes. In addition to increasing the volume of bile, they exert a kinetic "washing" effect, preventing ascending infection, and a litholytic effect—increasing the concentration of bile acid salts (cholates) to prevent cholesterol from precipitating.
There are four subgroups:
- True choleretics (containing bile acids): animal-derived drugs. Holenzim contains dry bile with pancreatic and intestinal mucosal enzymes. Allochol is supplemented with garlic and nettle extracts, as well as charcoal (suppresses fermentation). Liobil is characterized by a high concentration of bile acids (5 times more than analogs). This group also includes combined enzymes (Festal, Panzinorm).
- Synthetic: chemical compounds that often have additional antimicrobial and anti-inflammatory effects (Hydroxymethylnicotinamide). Some, like Osalmid, produce a hypolipidemic effect, lowering blood cholesterol and bilirubin levels.
- Herbal: extracts of dwarf everlast (Flamin), rose hips (Holosas), corn silk, and the Liv-52 complex. They act through essential oils and flavones, providing a comprehensive secretory, anti-inflammatory, and antimicrobial effect.
- Hydrocholeretics: mineral waters (containing sulfate anions) and valerian rhizomes. They increase bile volume via the water component by limiting water reabsorption and making bile more fluid.
Drugs regulating bile excretion
These agents work at the level of the gallbladder and sphincters.
Cholekinetics irritate the receptors of the duodenal mucosa, triggering the release of endogenous cholecystokinin. As a result, the gallbladder actively contracts while the sphincters relax, leading to powerful gallbladder evacuation. These include:
- Polyhydric alcohols: xylitol and sorbitol (used as 10% solutions).
- Saline preparations: 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).
Cholespasmolytics (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 (M-cholinoblockers), nitrates (nitroglycerin), methylxanthines, and combination drugs (e.g., Olimetin, which contains a complex of essential oils and purified sulfur).
Contraindications and safety
When prescribing choleretic drugs, contraindications must be strictly considered. An absolute contraindication for all bile-containing and bile-stimulating drugs is a mechanical barrier to bile outflow (obstructive jaundice).
In addition, many drugs (e.g., Allochol, Olimetin) are contraindicated in gastric ulcer and duodenal ulcer, acute hepatitis, and active liver dystrophy.
Briefly: answers to topical questions
Which specific drugs from the group of M-anticholinergics are used as cholecysto-spasmolytics?
The provided methodological materials do not contain specific trade names or international nonproprietary names of drugs from the group of M-anticholinergics used as cholecysto-spasmolytics. Only the pharmacological group of atropine-like substances is mentioned without specifying particular drugs.
Which drugs belong to synthetic choleretics?
The group of synthetic choleretics includes drugs with a chemical structure that stimulates bile secretion. The main representatives of this subgroup are hydroxymethylnicotinamide (Nicodin), cyclovalone, and osalmid (oxaphenamide). In addition to their choleretic effect, these medicinal products often exert anti-inflammatory and antimicrobial effects.
Which bile acid preparations are used for medical dissolution of gallstones (cholelitholytics)?
Bile acid preparations are used for the medical dissolution of cholesterol stones in the gallbladder. This group includes chenodeoxycholic acid (Chenofalk) and ursodeoxycholic acid (Ursofalk). These cholelitholytic agents help dissolve existing stones by impairing intestinal cholesterol absorption, inhibiting its hepatic synthesis, and forming liquid crystals.
Which GI hormones are involved in the regulation of bile secretion and excretion?
Gastrointestinal hormones and peptides are involved in the regulation of bile formation and excretion. Humoral factors stimulating bile secretion include secretin, glucagon, gastrin, and cholecystokinin-pancreozymin. Bile excretion and gallbladder motility are regulated by cholecystokinin, which is secreted by endocrine cells of the small intestine.
For quick memorization: CholeRETICS — REproduce (form) bile in the liver. CholeKINETICS — provide KINETics (movement), pushing bile out of the gallbladder. CholeSPASMOLYTICS — relieve SPASM of the ducts.
Class and exam questions
What is the difference between true choleretics and hydrocholeretics?
True choleretics stimulate the production of bile acids by hepatocytes. Hydrocholeretics (e.g., mineral waters) increase bile volume exclusively via water, reducing its viscosity and increasing fluidity.
Why are preparations containing bile contraindicated in mechanical jaundice?
If there is an outflow obstruction (e.g., a stone in the duct), additional secretion stimulation will lead to a sharp increase in pressure within the biliary tract, causing severe colic and liver damage.
What is the mechanism of action of cholekinetics?
They irritate the receptors of the duodenum, causing the release of the hormone cholecystokinin. This leads to the simultaneous contraction of the gallbladder and relaxation of the sphincters, ensuring the release of bile.
What else to study on this topic
- Features of the use of enzyme preparations containing bile components (Panzinorm, Festal, Enzistal).
- Synthetic choleretics with a pronounced anti-inflammatory effect (Hydroxymethylnicotinamide, Cyclovalone).
- Pharmacodynamics of complex herbal preparations (Liv-52, Cholagogum).
- Polyhydric alcohols and saline solutions: regimens for course administration of cholekinetics.
- Combined cholecysto-spasmolytics: composition and homeopathic action of the drug Olimetin.
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