Choleretic drugs - drugs that enhance bile formation or promote the secretion of bile into duodenum.
Bile ( bilis- lat., fel- English) - a secret produced by hepatocytes. Bile production occurs in the body continuously. Bile produced in the liver is secreted into the extrahepatic bile ducts, which collect it into the common bile duct. Excess bile accumulates in gallbladder, where it is concentrated 4-10 times as a result of water absorption by the mucous membrane of the gallbladder. In the process of digestion, bile from the gallbladder is released into the duodenum, where it is involved in the processes of digestion and absorption of lipids. The flow of bile into the intestine is regulated by neuro-reflex mechanisms. Of the humoral factors in the process of bile secretion, the most important is cholecystokinin (pancreozymin), which is produced by the mucous membrane of the duodenum when gastric contents enter it and stimulates the contraction and emptying of the gallbladder. As it moves through the intestine, the bulk of the bile is absorbed through its walls along with nutrients, the rest (about a third) is removed with feces.
The main components of bile are bile acids (FA) - 67%, about 50% are primary FAs: cholic, chenodeoxycholic (1: 1), the remaining 50% are secondary and tertiary FAs: deoxycholic, lithocholic, ursodeoxycholic, sulfolithocholic. Bile also contains phospholipids (22%), proteins (immunoglobulins - 4.5%), cholesterol (4%), bilirubin (0.3%).
In terms of their chemical structure, FAs are derivatives of cholanic acid and represent the main end product of cholesterol metabolism. Most of FAs are conjugated with glycine and taurine, which makes them stable at low pH values. Bile acids facilitate emulsification and absorption of fats, inhibit cholesterol synthesis by the mechanism feedback, absorption of fat-soluble vitamins (A, D, E, K) depends on their presence. In addition, bile acids increase the activity of pancreatic enzymes.
Disturbances in the formation or outflow of bile into the duodenum can be of a different nature: liver disease, biliary dyskinesia, increased lithogenicity of bile, etc. When choosing a rational choleretic agent, it is necessary to take into account the pharmacodynamics of choleretic drugs.
Depending on the leading mechanism of action, choleretic agents are divided into two subgroups: agents that enhance the formation of bile and bile acids (Choleretica, Cholesecretica), and means promoting its release from the gallbladder into the duodenum ( Cholagoga, or Cholekinetica). This division is rather arbitrary, since most choleretic agents simultaneously increase the secretion of bile and facilitate its entry into the intestines.
The mechanism of action of choleretics is due to reflexes from the intestinal mucosa (especially when using drugs containing bile, bile acids, essential oils), as well as their effect on exosecretion of the liver. They increase the amount of secreted bile and the content of cholates in it, increase the osmotic gradient between bile and blood, which enhances the filtration of water and electrolytes into the bile capillaries, accelerates the flow of bile through the biliary tract, reduces the possibility of cholesterol precipitation, that is, prevents the formation of gallstones, enhance digestion and motor activity small intestine.
Bile-promoting drugs can act by stimulating contraction of the gallbladder (cholekinetic) or by relaxing the muscles biliary tract and the sphincter of Oddi (cholespasmolytics).
Clinical classification of choleretic agents
(see Belousov Y.B., Moiseev V.S., Lepakhin V.K., 1997)
[* - marked with drugs or DV, drugs which currently do not have valid registration in the Russian Federation.]
I. Drugs that stimulate bile formation - choleretics
A. Increasing the secretion of bile and the formation of bile acids (true choleretics):
1) preparations containing bile acids: Allochol, Cholenzym, Vigeratin, dehydrocholic acid (Hologon *) and sodium salt dehydrocholic acid (Decholin *), Liobil * and others;
2) synthetic drugs: hydroxymethylnicotinamide (Nikodin), osalmide (Oxafenamide), cyclovalon (Tsikvalon), hymecromone (Odeston, Holonerton *, Cholestil *);
3) herbal preparations: flowers of the immortelle sandy, corn stigmas, common tansy (Tanacehol), rose hips (Holosas), Berberine bisulfate, birch buds, blue cornflower flowers, oregano herb, calamus oil, turpentine oil, peppermint oil, scumpia leaves (Flakumin), Far Eastern lily of the valley herb (Konvaflavin), turmeric root (Febichol *), buckthorn, etc.
B. Drugs that increase the secretion of bile due to the water component (hydrocholeresis): mineral water, sodium salicylate, valerian preparations.
II. Drugs that stimulate bile secretion
A. Cholekinetics - increase the tone of the gallbladder and reduce the tone of the biliary tract: cholecystokinin *, magnesium sulfate, pituitrin *, choleritin *, barberry preparations, sorbitol, mannitol, xylitol.
B. Cholespasmolytics - cause relaxation of the biliary tract: atropine, platifillin, methocinia iodide (Metacin), belladonna extract, papaverine, drotaverine (No-shpa), mebeverin (Duspatalin), aminophylline (Euphyllin), olimetin.
I.A.1) Preparations containing bile acids and bile- these are drugs that contain either bile acids themselves, or combined drugs, which, in addition to lyophilized bile of animals, may include extracts medicinal plants, extract of liver tissue, pancreatic tissue and mucous membranes of the small intestine of large cattle, activated carbon.
Bile acids, being absorbed into the blood, stimulate the bile-forming function of hepatocytes, the unabsorbed part performs a substitution function. In this group, preparations that are bile acids increase the volume of bile to a greater extent, and preparations containing animal bile increase the content of cholates (bile salts) to a greater extent.
I.A.2) Synthetic choleretics have a pronounced choleretic effect, but do not significantly change the excretion of cholates and phospholipids into bile. After entering hepatocytes from the blood, these drugs are secreted into bile and dissociate, forming organic anions. The high concentration of anions creates an osmotic gradient between bile and blood and causes osmotic filtration of water and electrolytes into the bile capillaries. In addition to choleretic, synthetic choleretics have a number of other effects: antispasmodic (oxafenamide, gimecromone), hypolipidemic (oxaphenamide), antibacterial (hydroxymethylnicotinamide), anti-inflammatory (cyclovalon), and also suppress the processes of putrefaction and fermentation in the intestine (especially hydroxymethyl).
I.A.3) Effect herbal preparations associated with the influence of a complex of components that make up their composition, incl. such as essential oils, resins, flavones, phytosterols, phytoncides, some vitamins and other substances. Drugs in this group increase functional ability liver, increase the secretion of bile, increase the content of cholates in bile (for example, immortelle, rose hips, Holagol), reduce the viscosity of bile. Along with increased secretion of bile, most herbal remedies in this group increase the tone of the gallbladder with simultaneous relaxation of the smooth muscles of the biliary tract and the sphincters of Oddi and Lutkens. Choleretic phytopreparations also have a significant effect on other functions of the body - they normalize and stimulate the secretion of the glands of the stomach, pancreas, increase enzymatic activity gastric juice, increase intestinal peristalsis with its atony. They also have antimicrobial (for example, immortelle, tansy, mint), anti-inflammatory (olimetin, Holagol, rosehip), diuretic, antimicrobial action.
As medicinal preparations from plants, in addition to extracts and tinctures, infusions and decoctions from herbal collections are prepared. Usually, phytopreparations are taken 30 minutes before meals, 3 times a day.
I.B. Hydrocholeretics. This group includes mineral waters - "Essentuki" No. 17 (highly mineralized) and No. 4 (slightly mineralized), "Jermuk", "Izhevskaya", "Naftusya", "Smirnovskaya", "Slavyanovskaya" and others.
Mineral waters increase the amount of secreted bile, making it less viscous. The mechanism of action of the choleretic agents of this group is due to the fact that, being absorbed in the gastrointestinal tract, they are secreted by hepatocytes into the primary bile, creating an increased osmotic pressure in the bile capillaries and contributing to an increase in the water phase. In addition, the reabsorption of water and electrolytes in the gallbladder and bile ducts is reduced, which significantly reduces the viscosity of bile.
The effect of mineral waters depends on the content of sulfate anions (SO 4 2-) associated with magnesium (Mg 2+) and sodium (Na +) cations, which have a choleretic effect. Mineral salts also contribute to an increase in the colloidal stability of bile and its fluidity. For example, Ca 2+ ions, forming a complex with bile acids, reduce the likelihood of a difficult-to-dissolve sediment.
Mineral waters are usually consumed warm 20-30 minutes before meals.
Salicylates (sodium salicylate) and valerian preparations are also referred to hydrocholeretics.
II.A. TO cholekinetics include funds that increase tone and motor function gallbladder, reduce the tone of the common bile duct.
Cholekinetic action is associated with irritation of the receptors of the intestinal mucosa. This leads to a reflex increase in the release of endogenous cholecystokinin. Cholecystokinin is a polypeptide produced by cells of the duodenal mucosa. The main physiological functions cholecystokinin - stimulates the contraction of the gallbladder and the secretion of digestive enzymes by the pancreas. Cholecystokinin enters the bloodstream, is captured by hepatic cells and secreted into the bile capillaries, while exerting a direct activating effect on the smooth muscles of the gallbladder and relaxing the sphincter of Oddi. As a result, bile flows into the duodenum and its stagnation is eliminated.
Magnesium sulfate has a choleretic effect when oral administration... A solution of magnesium sulfate (20-25%) is administered orally on an empty stomach, and is also administered through a tube (with duodenal intubation). In addition, magnesium sulfate also has a cholespasmolytic effect.
Polyhydric alcohols (sorbitol, mannitol, xylitol) have both cholekinetic and choleretic effects. They have a beneficial effect on liver function, contribute to the normalization of carbohydrate, lipid and other types of metabolism, stimulate the secretion of bile, cause the release of cholecystokinin, and relax the sphincter of Oddi. Polyhydric alcohols are used during duodenal intubation.
Olive and sunflower oil, plants containing bitterness (including dandelion, yarrow, wormwood, etc.), essential oils (juniper, cumin, coriander, etc.), extract and juice of cranberries, lingonberries and dr.
II.B. TO cholespasmolytics include drugs with a different mechanism of action. The main effect of their use is the weakening of spastic phenomena in the biliary tract. m-cholinolytics (atropine, platifillin), blocking m-cholinergic receptors, have a non-selective antispasmodic effect in relation to various parts of the gastrointestinal tract, incl. in relation to the biliary tract.
Papaverine, drotaverine, aminophylline - have a direct (myotropic) effect on smooth muscle tone.
Other drugs also have a cholespasmolytic effect. However, they are rarely used as choleretic agents. So, nitrates relax the sphincter of Oddi, the lower esophageal sphincter, reduce the tone of the biliary tract and esophagus. For long-term therapy, nitrates are unsuitable, because have pronounced systemic side effects. Glucagon can temporarily reduce the tone of the sphincter of Oddi. But both nitrates and glucagon have short-term effects.
Indications to the appointment of choleretics are chronic inflammatory diseases liver and biliary tract, incl. chronic cholecystitis and cholangitis, they are used for biliary dyskinesia, in the treatment of constipation. If necessary, choleretics are combined with antibiotics, analgesics and antispasmodics, with laxatives.
Unlike other choleretic drugs, drugs containing bile acids and bile are agents of replacement therapy for endogenous bile acid deficiency.
Cholekinetics cause an increase in the tone of the gallbladder and relaxation of the sphincter of Oddi, therefore they are prescribed mainly for hypotonic form of biliary dyskinesia. Indications for their use are atony of the gallbladder with stagnation of bile with dyskinesia, chronic cholecystitis, chronic hepatitis, with anacid and severe hypoacid conditions. They are also used for duodenal intubation.
Cholespasmolytics are prescribed for hyperkinetic form of biliary dyskinesia and for gallstone disease... They are used for cupping pain syndrome moderate intensity, often accompanying the pathology of the biliary tract.
Choleretics contraindicated at acute hepatitis, cholangitis, cholecystitis, pancreatitis, peptic ulcer stomach and duodenum in the acute stage, with cholelithiasis with blockage of the excretory ducts, with obstructive jaundice, as well as with dystrophic lesions of the liver parenchyma.
Cholekinetics are contraindicated in acute diseases liver, in the presence of stones in the gallbladder, with exacerbation of hyperacid gastritis and gastric ulcer and duodenal ulcer.
Criteria for evaluating the effectiveness and safety of the use of drugs used in violation of bile secretion:
- Laboratory: determination of bile acids in the blood and gallbladder bile (with pathology, the amount of fatty acids in the blood increases, and in bile it decreases, the ratio between their three main forms - cholic, chenodeoxycholic, deoxycholic - and glycine and taurine conjugates), blood test (increased fatty acids in blood leads to hemolysis, leukopenia, disrupts the processes of blood coagulation), determination of indirect and direct bilirubin, ALT, AST, bile pigments, etc.
- Paraclinic, incl. duodenal intubation, contrast cholecystography, ultrasound.
- Clinical: high concentrations of cholates in the blood cause bradycardia, arterial hypertension, itchy skin, jaundice; symptoms of neurosis appear; pain in the right hypochondrium or epigastrium, an increase in the size of the liver.
TO drugs used for increased lithogenicity of bile(in the absence of calculi), include Allochol, Cholenzym, hydroxymethylnicotinamide (Nikodin), sorbitol, Olimetin. Means of this group have different mechanisms of action, since the lithogenicity of bile depends on many factors.
Cholelitholytic drugs(cm. ). A number of deoxycholic acid derivatives, in particular ursodeoxycholic, isomeric chenodeoxycholic, are able not only to prevent the formation of cholesterol stones in the gallbladder, but also to dissolve the existing ones.
Cholesterol, which forms the basis of most gallstones, is normally dissolved in the center of micelles, outer layer which form bile acids (cholic, deoxycholic, chenodeoxycholic). Phospholipids, concentrated in the center of the micelle, increase its ability to inhibit the crystallization of cholesterol. A decrease in the content of bile acids in bile or an imbalance between the concentration of phospholipids and cholesterol and a supersaturation of bile with cholesterol can lead to the fact that bile becomes lithogenic, i.e. capable of forming cholesterol stones. The change physical and chemical properties bile leads to precipitation of cholesterol crystals, which then form a nucleus with the formation of cholesterol gallstones.
Both ursodeoxycholic and chenodeoxycholic acids change the ratio of bile acids, reduce the secretion of lipids in bile and lower cholesterol in bile, reduce the cholate-cholesterol index (the ratio between the content of acids and cholesterol in bile), thereby reducing the lithogenicity of bile. They are prescribed as cholelitholytic agents in the presence of small cholesterol stones as an adjunct to surgical or shock wave treatments for cholelithiasis.
Drugs
Preparations - 1216 ; Trade names - 62 ; Active ingredients - 19
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Bile plays an essential role in the functioning of the gastrointestinal tract. Bile acids are stimulants of intestinal motility, production of pancreatic juice, emulsification and absorption of fats and fat-soluble vitamins. In addition, they are stimulants of dense and liquid bile fractions in the liver.
Lack of bile can be associated with:
1) violation of its formation in liver cells;
2) with difficulty in entering the duodenum from the bile ducts and bladder.
In accordance with this, choleretic agents are divided into two groups:
1. Means that enhance the secretion or production of bile (choleretics, cholesecretics).
2. Means that facilitate, facilitate the passage, separation of bile (holagog or cholekinetics):
The latter group, in turn, is divided into drugs that have an antispasmodic effect, used for hypertensive form of biliary dyskinesia, and drugs used for hypomotor dyskinesia, causing contraction of the gallbladder and opening of the sphincter of Oddi.
The first group of drugs (cholesecretics) includes, first of all, choleretics of animal origin, dehydrocholic acid (HOLAGOL; in tab. 0, 2). Mainly stimulates the formation of a liquid fraction of bile, increases blood flow in the liver, increases urine output.
Assign one tablet three times a day after meals. Choleretics of animal origin, firstly, make up for the lack of bile in the intestine, and secondly, they stimulate the secretory function of the liver, and also facilitate the passage of bile through the ducts, coordinate the duration of contraction of the muscles of the gallbladder and the sphincter of Oddi.
Other drugs of this group are now used. ALLOHOL (Allocholum) - official tablets, contain dry bile, extracts of garlic, nettle, as well as activated charcoal and other excipients. In addition to the effects usual for cholesecretics, allochol reduces the processes of putrefaction and fermentation in the intestines, flatulence.
Apply the drug at the end or after meals, two tablets three times a day for 3-4 weeks. The course of treatment is repeated after 3 months.
Indications for use. Allochol is used for chronic hepatitis, cholangitis, cholecystitis, and habitual constipation. Side effects: in some patients it is possible allergic reactions, diarrhea. In these cases, the drug should be canceled.
CHOLENSIM (Cholensimum) - contains, in addition to dry bile, a dried portion of the pancreas and a dried portion of the mucous membrane of the small intestines of slaughter cattle. In addition to the effects of choleretics, cholenzyme improves intestinal digestion due to the content of trypsin and amylase.
Assign inside after meals, one tablet 1 to 3 times a day. There are practically no side effects described.
> Drugs that stimulate bile formation - choleretics (cholesecretics):
- true (hologon, liobil);
- vegetable: flowers of immortelle (flamin), corn stigmas, tansy flowers (tanacehol), rose hips (holosas), scumpia leaves (flacumin), black radish juice;
- synthetic (odeston, tsikvalone, oxafenamide, nicodine);
- combined (allochol, cholenzyme, hepatofalk plant);
- hydrocholeretics (alkaline mineral waters, salicylates, valerian root).
- Cholekinetics:
- synthetic (magnesium sulfate, sorbitol, xylitol, berberine sulfate);
- vegetable (lingonberry leaf, cornflower flowers, rhubarb root, calendula flowers - kaleflon);
- combined (olimetin, cholagol).
- Cholespasmolytics:
- anticholinergics (atropine, metacin, belladonna preparations);
- myospasmolytics (drotaverine, papaverine, mebeverin, otylonium bromide, pinaverium bromide);
- vegetable (lemon balm herb, peppermint leaf, dried crushed grass, St. John's wort herb);
- combined (nikoshpan, papazol).
General indications for appointment: cholecystitis, cholangitis. Choleretics are often combined with laxative drugs to eliminate constipation and reduce the absorption of toxic substances from the intestines.
General contraindications: acute hepatitis, acute and subacute liver dystrophies, obstructive jaundice.
True choleretics. Allochol - combination drug containing dry animal bile (0.08 g), dry garlic extract (0.04 g), nettle extract (0.005 g), activated carbon (0.025 g) and filler (0.3 g). Dry bile contained in the preparation causes an increase in the secretion of its own bile, while the content of bile acids in it increases. The effect of the drug is due to the enhancement of not only the secretory function of the liver, but also the secretory and motor activity digestive tract, a decrease in the processes of putrefaction and fermentation in the intestine, an increase in the peristalsis of the large intestine. It is prescribed 1-2 tablets 3-4 times a day after meals. The course of treatment is 2-3 weeks, a second course - no earlier than 3 months later.
Cholenzym is a combined preparation containing dry animal bile (0.1 g), enzymes of the pancreas and intestines of animals (0.1 g each). The drug has choleretic activity and, due to the content of enzymes (trypsin and amylase) and bile, improves the digestion of proteins, fats, carbohydrates, which contributes to their more complete absorption in the small intestine. Cholenzyme also has an antispasmodic effect, while its choleretic effect is low. 1-2 tablets are prescribed 3 times a day after meals. The course of treatment is up to 4 weeks.
Chologon (dehydrocholic acid) is the least toxic of all bile acids. The action begins after 1020 minutes, the maximum effect is observed after 2 hours, the duration of the course is up to 8 weeks. It is prescribed 1-2 tablets 3-4 times a day after meals.
Liobil is freeze-dried bovine bile. The composition of the tablets includes acetylphthalyl cellulose, which ensures the stability of the tablet in the acidic environment of the stomach and its solubility in the alkaline environment of the intestine. The bile contained in the tablets promotes the formation and outflow of its own bile, increased secretion of the pancreas, the breakdown and absorption of fats in the intestine, and increased intestinal motility. In addition to traditional indications, it is also used for chronic pancreatitis with reduced secretory function of the pancreas. 1-2 tablets are prescribed 3 times a day after meals.
Synthetic choleretics. Hydroxymethylnicotinamide (nicodine) is a derivative of niacin amide and formaldehyde. It has a choleretic effect, as well as a bactericidal effect, which is due to the fact that in the process of metabolism, the formaldehyde part of the drug molecule is split off. Another part of the molecule (nicotinamide) has the properties of vitamin PP, increases the secretory function of the liver parenchyma, increasing the secretion of bile and facilitating its entry into the intestines. It is effective in the treatment of infections caused by E. coli, therefore it is advisable to use the drug in the combination of inflammatory diseases of the biliary tract with gastritis and colitis. It is prescribed orally 1-2 tablets 3-4 times a day before meals with 1/2 glass of water.
Osalmide (oxafenamide) enhances the formation (choleretic effect) and secretion (cholekinetic effect) of bile, has an antispasmodic effect, reducing the tone of the biliary tract. Has the ability to lower blood cholesterol levels. It is prescribed orally in tablets of 0.25-0.5 g (1-2 tablets) 3 times a day before meals. The average course of treatment is 14-21 days. Oxafenamide rarely causes side effects. In some cases, with prolonged use, a laxative effect is observed.
Cyclovalon (Cycvalon) stimulates bile formation and has an anti-inflammatory effect. It is prescribed orally in tablets of 0.1-0.2 g (1-2 tablets) 3 times a day before meals. The average course of treatment is 14-21 days. The drug is usually well tolerated. In some cases, at the beginning of treatment, there is sometimes a feeling of pressure in the liver, the appearance or increased bitterness in the mouth. These phenomena go away on their own and do not require discontinuation of the drug.
Gimecromone (odeston) excites the receptors of the intestinal mucosa and reflexively enhances the secretion and separation of bile, increases the osmotic gradient between bile and blood, which leads to an increase in the filtration of electrolytes and water into the bile ducts, a decrease in the content of cholates, prevents the crystallization of cholesterol and the development of cholelithiasis. It also has a selective myotropic antispasmodic effect on the biliary tract and their sphincters, but does not affect the motility of the gallbladder, the smooth muscles of the intestines and blood vessels. The drug is prescribed inside 30 minutes before meals, 200-600 mg (1-3 tablets) per day for 2-3 doses. Of the side reactions, allergic reactions are noted, with prolonged use - diarrhea, flatulence, headache, abdominal pain. The drug is contraindicated in case of hypersensitivity to it, pregnancy, lactation, with obstruction of the biliary tract, renal / liver failure, nonspecific ulcerative colitis, Crohn's disease, gastric ulcer and duodenal ulcer, hemophilia.
N.B.!
When combining odestone with metoclopramide, bilateral antagonism may develop. Joint appointment with indirect anticoagulants leads to an increase in their effect.
CHILDREN DRUGS. UTERINE REMEDIES.
Human bile is a secretion that is produced by the liver cells. This secret contains:
bilirubin (end product of hemoglobin metabolism)
bile acids (end products of cholesterol metabolism)
hormones, vitamins and other physiologically active substances
phospholipids (lecithin)
Bile acids (cholic, deoxycholic, chenodeoxycholic) play an important role in the digestion and absorption of lipids.
In some diseases of the gastrointestinal tract, bile formation and bile secretion can be disturbed.
This is observed in acute and chronic cholecystitis, cholangitis, chronic hepatitis, biliary dyskinesia. In these cases, the appointment of choleretic agents is indicated.
Choleretic drugs are drugs that increase the secretion of bile or promote its movement along the biliary tract into the duodenum.
CLASSIFICATION OF CHILDRONS according to their effect on the secretion and excretion of bile:
Choleretics are agents that stimulate bile formation.
a) True choleretics (contain bile and bile acids)
cholenzyme
b) Synthetic choleretics
tsikvalon
c) Choleretics of plant origin
immortelle (flowers)
peppermint
rosehip (fruit)
parsley
flacumin
corn silk
barberry amur
flamin (dry immortelle concentrate containing flavones)
oxaphenamine
d) hydrocholeretics
mineral water
valerian preparations
Biliary stimulants
a) True choleretics:
olive oil
berberine sulfate
b) Cholespasmolytics:
M-anticholinergics
Theophylline
Nitroglycerine
Papaverine hydrochloride
magnesium sulfate
Means that increase the hydrophilicity of bile and prevent the formation of gallstones: henofalk (hendol).
The presented classification is somewhat arbitrary, since in most cases drugs have a complex effect.
Consider choleretics. These drugs stimulate the biliary function of the liver. The mechanism of action of choleretics consists of several points:
direct stimulation of the secretory function of the hepatic parenchyma;
increased osmotic filtration of water and electrolytes into bile capillaries;
stimulation of receptors in the mucous membrane of the small intestine, which enhances bile formation.
Typical true choleretics are allochol and cholenzi. These are multicomponent preparations, the common component is animal bile (dry bile).
Synthetic choleretics All synthetic drugs increase bile production, increase bile volume, and have anti-inflammatory effects.
Choleretics of plant origin contain a large number of essential oils, resins, flavones and other biologically active substances... Decoctions and infusions from this group of plants or tablets, getting into the small intestine, stimulate the receptors of the intestinal mucosa, which increases bile production. In addition, each plant has its own traits of action. For example, the antispasmodic effect inherent in plants such as immortelle, corn silk, peppermint; antimicrobial action - tansy, immortelle, peppermint; tone up the gallbladder - tansy, Amur barberry, parsley.
HYDROCHOLERETICS
They increase the amount of bile due to the water component:
the secretion of bile increases;
the reabsorption of water and electrolytes in the gallbladder is limited. This leads to an increase in the colloidal stability of bile. The main representatives of hydrocholeretics are mineral waters (Jermuk, Naftusya, Arzni, Smirnovskaya, Slavyanovskaya). Sulfates have a choleretic effect in these waters, and magnesium helps to increase the tone of the gallbladder.
CHOLEKINETICS
True cholekinetics Cholespasmolytics
(MO 4, sorbide, xylitol) (M-anticholinergics, antispasmodics)
True cholekinetics increase the tone, increase the tone of the gallbladder and at the same time reduce the tone of the biliary tract.
Mechanism of action. They irritate the mucous membrane of the duodenum - cholecystokinin is released, which invokes contraction of the muscular wall of the gallbladder and relaxation of the sphincter of Oddi.
HOLESPASMOLITICS.
They are drugs of different pharmacological groups, and their mechanism of action is different. They are used not only as cholespasmolytics, but ultimately they relieve spasm of the biliary tract, increasing the passage of bile. They are used most often for biliary dyskinesia, which is accompanied by painful attacks (M-anticholinergics, no-shpa, papaverine).
Uterine products
Uterine funds are drugs that affect the tone and contractile activity of the myometrium (skein muscles).
Classification of uterine funds
Means that stimulate the muscles of the uterus.
Strengthening rhythmic contractions of the myometrium:
a) preparations of the oxytonin group:
oxytonin
deaminooxytocin
pituitrin
hyphalotocin
b) preparations of prostaglandins:
dinoprost
dinoprostone
Enhancing tonic contraction of the myometrium:
a) ergot and alkaloids:
ergometrine
methylergometrine
ergotamine
b) cotarnine chlorine.
Means that stimulate tonic and rhythmic contractions of the uterus:
spherophysin
pachicarpina hydroiodide
"Small" uterine products:
water pepper extract
tincture of Amur barberry leaves
shepherd's purse herb extract
extract of chitosebaceous epithelium
Means that relax the muscles of the uterus (tocolytics)
partusistin
rithodrin
Uterine remedies are used to enhance or weaken the contraction of the uterus during childbirth, to stop uterine bleeding.
Oxytocin - a hormonal drug from the posterior lobe of the pituitary gland.
Mechanism of action: excitation of adrenergic receptors of the cell membranes of the myometrium. When the receptors are excited, the polarization of the membrane of the muscle cells of the mass decreases. This leads to:
increased membrane permeability for K + (increased excitability);
increased release of calcium from the sarcoplasmic reticulum, and calcium is necessary for the binding of troponin and enhance the interaction of actin and myosin. The result is a contraction of the myometrium;
the formation of c-AMP, which binds calcium, is suppressed, which leads to a weakening, reduction of the actomyosin complex.
It should be borne in mind that small doses of oxytocin cause a rhythmic contraction of the uterus, and large doses can cause tetanic contraction of the uterus (fetal asphyxia, uterine rupture may occur).
Oxytocin increases milk production by the mammary glands.
Pituitrin- a hormonal preparation from the posterior lobe of the pituitary gland of cattle and pigs.
It contains 2 active ingredients:
oxytocin (shortens the uterine muscles);
vasopressin (reduces blood vessels and increases blood pressure).
Pituitrin is not prescribed for women with hypertension because of the vasopressin it contains.
Recently, to stimulate labor, they increasingly use prostaglandins... The uterus is influenced by the prostaglandins of the group. They cause an increase in the tone and motility of the uterus, and they act on both the pregnant and non-pregnant uterus.
The mechanism of action of prostaglandins on the uterus is associated with the excitation of specific receptors embedded in the membranes of muscle cells. Excitation of these receptors activates the contractile mechanism of the myometrium - rhythmic contractions of the uterus begin.
Pharmacokinetics prostaglandins:
Prostaglandins are quickly inactivated in the body, so they are usually injected intravenously. Childbirth occurs in 1-4 hours. Metabolism occurs in the liver, lungs, kidneys. The metabolists of prostaglandins are excreted by the kidneys.
Indications for use:
stimulation of labor
stopping severe postpartum hemorrhage
termination of pregnancy up to 15 weeks
Way of introduction: into the vein, into the uterus (for abortion)
Side effects: dyspepsia (nausea, vomiting, diarrhea), tachycardia, bronchospasm, phlebitis (with intravenous administration).
Contraindications: bronchial asthma, epilepsy.
Ergot preparations have been used for a long time to stop postpartum hemorrhage.
V obstetric practice use preparations of two ergot alkaloids: ergometrine and ergotamine. The mechanism of action of these drugs is associated with the selective excitation of the alpha-adrenergic receptors of the uterus. As a result, the powerful layer of the muscle of the uterus and the muscles of the cervix are contracted. This leads to mechanical compression of the blood vessels that are obliquely located in the myometrium. The bleeding stops.
Ergometrine vs Ergotamine Comparison Chart
|
A drug |
Action on the myometrium |
Action on alpha-adrenergic receptors |
|
Ergometrine |
Rapid contraction of the uterine muscles. When administered intravenously, the effect after 1 minute. Significant latency period. After intravenous administration, contraction of the uterine muscles develops slowly. |
There is no alpha blocking effect. It is a partial antagonist, partial antagonist of alpha-adrenergic receptors. With prolonged administration, the alpha-adrenomimetic effect predominates - spasm of the perapherical vessels and damage to the endothelium. |
|
Ergotamine |
Acute ergot poisoning often occurs in connection with an attempt to induce an abortion. Symptoms associated with the effect on the central nervous system prevail: motor agitation, convulsions, vomiting (excitation of the trigger zone), lowering blood pressure as an orthostatic collapse (inhibition of the vasomotor center).
Long-term use of ergot preparations leads to chronic poisoning (ergotism). Currently, it practically does not occur. Two forms of ergotism:
"Fire of St. Anthony "- gangrenous form;
"Evil writhing" - convulsive form
"Small" uterine products are herbal preparations obtained from water pepper, shepherd's purse, barberry. They are used in gynecology to treat various uterine bleeding in pathologies not related to pregnancy.
Tocolytic drugs- this is medications, weakening the contraction of the pregnant uterus with its excessive activity.
Tocolytic agents can be divided into 3 groups:
beta 2 - adrenergic agonists (partusisten, ritodrin).
Drugs that inhibit the synthesis of prostaglandins (acetylsalicic acid, indomethacin).
Means leading to a change in the content and movement of calcium ions (magnesium sulfate).
Beta-adrenomimetics. The mechanism of tocolytic action of beta 2 -adrenergic agonists is that beta 2 -adrenergic receptors are embedded in the uterus and when they are excited, the smooth muscles of the uterus relax. That is why these drugs are prescribed as a means of reducing the contraction of the uterus during premature contractions.
Drugs that inhibit the synthesis of prostaglandins(acetylsalicic acid, indomethacin).
The mechanism of the tocolytic action of these drugs is that they block the activity of the enzyme cyclooxygenase, and the synthesis of prostagladins decreases. And prostagladins stimulate the uterine muscles.
Acetylsalicic acid is used, 0.5 g, 4-6 times a day.
The third group of tocolytic agents is magnesium preparations (MO 4). The mechanism of tocolytic action of magnesium preparations: magnesium of competitors displace calcium ions from the sarcoplasmic reticulum, deplete calcium reserves. This leads to a decrease in the excitability of the uterine muscles.
As a tocolytic agent, magnesium sulfate is administered intramuscularly in a dose of 10 ml. solution 2-4 times a day.
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Currently choleretic drugs at complex treatment and the prevention of various diseases of the liver and gallbladder are used in clinical practice therapist-gastroenterologist is quite wide. This is due to the effects of choleretic drugs, which relieve pain attacks, facilitate the course of the disease, and also prevent the deterioration of the condition or the appearance new pathology, provoked by the decompensation of an existing disorder.
To understand why choleretic drugs are needed, you should know what bile is, what are its physiological functions and how it moves in digestive system... Bile is biological fluid produced by liver cells and accumulates in the gallbladder. The liquid has a bitter taste, a specific odor and, depending on the age of production, can be colored yellow, brown or greenish. Bile performs the following physiological functions in the human body:
- Emulsification and digestion of fats from food;
- Activation of enzymes in the small intestine and pancreas necessary for complete digestion of food;
- Provides full absorption of fat-soluble vitamins, calcium and cholesterol.
Emulsification of fats is carried out by bile acids contained in bile, which, in addition, improve intestinal motility, stimulate the formation of protective mucus and prevent the attachment of bacteria and proteins to the mucous membrane. Thanks to these effects, bile prevents constipation and intestinal infections. In addition, bile is necessary for the elimination of substances such as cholesterol, bilirubin, glutathione and steroid hormones from the human body along with feces.
Bile is synthesized by liver cells and enters the gallbladder through special ducts. Then, from the gallbladder, also through the duct system, it enters the duodenum, where it performs its physiological functions. That is, the gallbladder is a kind of reservoir for temporary storage of bile from the moment it is produced until the food lump enters the duodenum.
Classification of choleretic drugs
Currently, an anatomical-therapeutic-chemical classification of choleretic agents is used, which takes into account both the chemical structure of the drug used and its therapeutic effects, and the anatomical structures affected by the drug. Such A complex approach allows you to create the most complete classification reflecting various aspects of application, therapeutic effects and characteristics of absorption, distribution and excretion of drugs from the human body.So, today choleretic drugs are classified into the following groups and subgroups:
1. Choleretics(drugs that increase the production of bile by liver cells):
True choleretics that increase the production of bile due to the active synthesis of bile acids:
- Choleretics containing bile acids and made on the basis of plant or animal raw materials (for example, animal bile, plant extracts, etc.);
- Synthetic choleretics, which are chemical substances obtained by organic synthesis and having the property of increasing the production of bile;
- Medicinal herbs with choleretic effect (used in the form of infusions, decoctions, etc.).
2. Cholekinetics(means that improve the outflow of bile by increasing the tone of the gallbladder and simultaneously relaxing the bile ducts).
3. Cholespasmolytics (means that improve the outflow of bile by relaxing the muscles of the gallbladder and biliary tract):
- Anticholinergics;
- Synthetic antispasmodics;
- Plant-based antispasmodics.
- Preparations containing bile acids - ursodeoxycholic or chenodeoxycholic;
- Preparations containing highly active solvents organic compounds lipid nature, for example, methyl tertiary butyl ether.
Synthetic choleretics are preparations which contain only compounds obtained in the course of organic synthesis as active substances. Drugs of this group, in addition to choleretic action, also have the following therapeutic effects: antispasmodic (reduce pain in diseases of the biliary tract and gallbladder), hypolipidemic (reduce the concentration of cholesterol in the blood), antibacterial (destroy pathogenic bacteria, provoking inflammatory diseases of the biliary tract) and anti-inflammatory (suppress the inflammation present in the biliary tract). In addition, synthetic choleretics suppress the processes of putrefaction and fermentation in the intestines, thereby eliminating bloating, stool instability and other phenomena of dyspepsia.
Medicinal herbs with choleretic action improve liver function, increase the secretion of bile, while reducing its viscosity. Also herbs increase the concentration of cholates in bile. Along with choleretic action, medicinal herbs they also have a cholekinetic effect, that is, on the one hand, they increase the secretion of bile, and on the other, they improve its excretion, thereby achieving a complex therapeutic effect on the human body. Herbal preparations are also capable of anti-inflammatory, antimicrobial and diuretic effects. Due to the content of only various herbs as active substances, the preparations of this group are often called herbal choleretic agents.
Hydrocholeretics increase the volume of bile due to its dilution and decrease in viscosity, achieved by increasing the content of the fraction of water in it. In such a situation, the excretion of bile is facilitated and the formation of stones is prevented.
Cholekinetics are agents that increase the tone of the gallbladder and at the same time relax the muscles of the bile duct. To understand the significance of the effect of cholekinetics, you need to know that the gallbladder is connected to the duodenum precisely bile duct, through which bile flows from one organ to another. Accordingly, at increased tone it narrows in the bile duct, which interferes with the movement of bile. And with a low tone of the gallbladder, it simply does not "push" bile into the duct. Thus, an increase in the tone of the gallbladder and relaxation of the duct create ideal conditions for the outflow of bile, since the former is intensely contracted, pushing the contents out of itself and preventing it from stagnating, and the latter has a sufficiently wide lumen to allow the entire volume to pass through for a short period of time. The resulting effect of cholekinetics is the release of the gallbladder and the flow of bile into the duodenum, as a result of which digestion is improved and stagnation is eliminated.
Cholespasmolytics are subdivided into several groups depending on the characteristics of their pharmacological action however, the resulting effects are the same for everyone. Cholespasmolytics eliminate spasm and dilate the biliary tract, facilitating the excretion of bile into the intestine. These drugs are usually used in short courses to relieve pain in various diseases gallbladder and biliary tract.
Preparations to reduce the lithogenicity of bile, strictly speaking, are intended to dissolve existing stones in the gallbladder and prevent the formation of new ones. Since these drugs have a choleretic effect, they are, with some degree of convention, classified as choleretic.
Each group and subgroup includes certain drugs that have a number of properties and clinical effects used in different options pathology of the biliary tract and liver. In the next section, we provide a list of choleretic drugs belonging to each group and subgroup.
Choleretic drugs - lists
Below, for the convenience of orientation and selection, we present a list of choleretic drugs by classification groups. In this case, we will first indicate international name active substance, and next to or in brackets a number of commercial names under which the drug may be produced.True choleretics
True choleretics containing bile components include the following drugs: - Preparations containing components of natural animal bile - Allochol, Cholenzym, Vigeratin, Liobil;
- Dehydrocholic acid - Hologon;
- Sodium salt of dehydrocholic acid - Decholin, Biliton, Suprakol, Cholamin, Holomin.
Synthetic choleretics
The following drugs are synthetic choleretics:- Hydroxymethylnicotinamide (Nicodine, Bilamid, Bilizarin, Bilocid, Cholamid, Coloton, Felosan, Isochol, Niciform);
- Gimecromon (Odeston, Holonerton, Cholestil);
- Osalmid (Oxafenamide, Osalmid, Auxobil, Drenamid, Driol, Enidran, Salmidochol);
- Tsikvalon (Tsiklovalon, Benevo, Cyclovalone, Divanil, Divanone, Flavugal, Vanilone).
Choleretics based on medicinal herbs
Herbal choleretics are as follows:- Helichrysum flower extract (Flamin);
- Corn silk extract (Peridol, Insadol);
- Tansy extract (Tanacehol, Tanaflon, Sibektan, Solar);
- Turmeric extract (Konvaflavin, Febichol);
- Scumpia leaf extract (Flacumin);
- Barberry leaf and root extract (Berberine sulfate, Berberis-Gomaccord, Berberis plus);
- Rosehip fruit extract (Holosas, Holemax, Holos);
- Datiska hemp extract (Datiskan);
- Bupleus extract (Pequokrin);
- Artichoke extract (Hofitol, Holebil);
- Preparations containing a complex of herbs with a choleretic effect (Holagol, Holagogum, Travohol, choleretic fees No. 2 and 3, Urolesan, Phytohepatol No. 2 and 3).
Hydrocholeretics
The following drugs are hydrocholeretic:- Alkaline mineral waters (Naftusya, Borjomi, Narzan, Essentuki 17, Essentuki 4, Arzni, Smirnovskaya, Slavyanovskaya, Izhevskaya, Jermuk, etc.);
- Salicylates (sodium salicylate);
- Valerian preparations ( alcoholic infusion valerian, valerian tablets, Valerianachel, etc.).
Cholekinetics
The following drugs are cholekinetic: - Magnesium sulfate (Magnesia, Kormagnesin);
- Sorbitol (Sorbitol);
- Mannitol (Mannitol, Mannitol);
- Xylitol;
- Barberry leaf and root extract (Berberine sulfate, Berberis-Gomaccord, Berberis plus);
- Helichrysum flower extract (Flamin);
- Rosehip fruit extract (Holosas, Holemax, Holos).
Cholespasmolytics
Cholespasmolytics are the following choleretic drugs:1. Anticholinergics:
- Bellalgin;
- Belloid;
- Besalol;
- Metacin;
- Platyphyllin;
- Spasmolitin;
- Fubromegan.
- Papaverine (Papaverine, Papaverine Buffus, Papazol);
- Drotaverin (Bioshpa, Nora-Drotaverin, Droverin, No-Shpa, Nosh-Bra, Ple-Spa, Spazmol, Spazmonet, Spazoverin, Spakovin);
- Aminophylline (Aminophyllin-Eskom, Euphyllin);
- Mebeverin (Duspatalin).
- Arnica tincture;
- Valerian tincture;
- Elecampane tincture;
- Tincture of St. John's wort;
- Mint tincture;
- Lemon balm tincture;
- Tincture of calendula flowers;
- Convaflavin (turmeric root);
- Holagol (extracts of various herbs).
Choleretic with litholytic action
Choleretic with litholytic action are as follows:1. Ursodeoxycholic or chenodeoxycholic acids - Livodex, Urdoksa, Urso 100, Ursodez, Ursodex, Uroliv, Ursolit, Ursorom S, Ursosan, Ursofalk, Choludexan, Exhol;
2. Methyl tert-butyl ether.
Choleretic herbal preparations
Choleretic herbal preparations are represented by finished dosage forms (tablets, tinctures or powders for preparing a solution for oral administration) or dried crushed parts of plants with the necessary properties.
Currently in the domestic pharmaceutical market there are the following choleretic herbal preparations in ready-made forms:
- Berberis-Homaccord;
- Berberis plus;
- Berberine sulfate;
- Datiscan;
- Insadol;
- Peridol;
- Convaflavin;
- Pequokrin;
- Sibektan;
- Solar;
- Tanaflon;
- Tanacehol;
- Travohol;
- Urolesan;
- Febichol;
- Phytohepatol No. 2 and 3;
- Flacumin;
- Flamin;
- Holagogum;
- Holagol;
- Hollebil;
- Holemax;
- Holos;
- Holosas;
- Hofitol.
In addition, the following medicinal herbs have a choleretic effect (choleretic):
- Birch buds;
- Turmeric root;
- Calamus rhizome;
- Roots and leaves of barberry;
- Burdock roots;
- Dandelion roots;
- Chicory root;
- Corn silk;
- Artichoke leaves;
- Bupleur leaves;
- Nettle leaves;
- Peppermint leaves and oil;
- Orthosiphon leaves;
- Parsley leaves;
- Scumpia leaves;
- Leaves and flowers of tansy;
- Fir oil;
- Terpene oil Rosehip;
- Coriander fruit;
- Rowan fruits;
- Carrot seeds;
- Horseradish root juice;
- Highlander's grass;
- Datiski grass;
- Oregano herb;
- Centaury grass;
- Lily of the valley herb;
- Wormwood herb;
- Immortelle flowers;
- Cornflower flowers;
- Tatar flowers.
Have a cholekinetic effect following products and medicinal herbs:
- Calamus rhizomes;
- Dandelion roots;
- Rhubarb roots;
- Barberry leaves;
- Lingonberry leaves;
- Watch leaves;
- Coriander oil;
- Juniper oil;
- Cumin oil;
- Olive oil;
- Coriander fruit;
- Juniper fruits;
- Caraway fruits;
- Fennel fruit;
- Dog-rose fruit;
- Sunflower oil;
- Lingonberry juice;
- Highlander's grass;
- Oregano herb;
- Shepherd's purse herb;
- Thyme herb;
- Yarrow herb;
- Immortelle flowers;
- Cornflower flowers;
- Calendula flowers;
- Chamomile flowers.
Modern choleretic drugs
Modern choleretic drugs are represented by a group of synthetic choleretics and combined herbal and animal remedies. Synthetic choleretics include drugs containing nicodine, gimecromone, osalmide or tsikvalone as active substances. Compared to natural choleretics (for example, Allochol, Cholenzym, Lyobil, etc.), they are better tolerated, do not cause unstable stools, and also have a number of additional positive therapeutic effects, such as antispasmodic, hypolipidemic, antibacterial and anti-inflammatory.In addition, the modern choleretic drugs include dehydrocholic acid (Hologon, Decholin) and ursodeoxycholic acid (Livodexa, Urdoksa, Urso 100, Ursodez, Ursodex, Uroliv, Ursorom, Ursorom S, Ursosan, Ursofalk, Ekholudexan). Also modern drug is the cholespasmolytic Duspatalin.
Among the choleretic herbal and animal preparations, modern ones include the following:
- Berberis-Homaccord;
- Vigeratin;
- Insadol;
- Convaflavin;
- Pequokrin;
- Peridol;
- Sibektan;
- Solar;
- Tanacehol;
- Tanaflon;
- Urolesan N;
- Febichol;
- Holagogum;
- Holagol;
- Holaflux;
- Holosas.
Choleretic drugs - indications for use
A common indication for the use of choleretic drugs is pathology of the gallbladder, biliary tract or liver. However, for the selection of the optimal drug, it is necessary to know the indications for the use of each group of choleretic agents. Within the groups, there are slight differences between drugs, which, however, do not affect their indications for use, which remain the same. Thus, for clinical orientation in choleretic drugs, it is necessary to know the indications for the use of each classification group, which we will consider below.Choleretics
Indications for the use of choleretics are the same for all three subgroups of this group of choleretic drugs. This means that synthetic choleretics (for example, Tsikvalon, Nikodin, Oxafenamide, etc.), and preparations containing components of natural bile (for example, Allochol, Lyobil, Decholin, Cholenzim, Hologon, etc.), and remedies based on medicinal herbs (for example, Konvaflavin, Holosas, Flakumin, etc.) have the same indications for use. So, choleretics are indicated for use in the following conditions or diseases: - Chronic inflammatory liver diseases (for example, hepatitis, steatosis, etc.);
- Chronic inflammatory diseases of the biliary tract (cholangitis, cholecystitis, etc.);
- Habitual constipation provoked by a violation of the outflow of bile.
In addition, with insufficient bile secretion, choleretics containing components of natural bile of animals can be used as substitution therapy drugs.
Among choleretics, the most "harsh" are preparations containing bile components, so they are the worst tolerated and often provoke stool disorders. Synthetic choleretics have a milder effect, but in terms of the spectrum of positive therapeutic effects, they are significantly inferior to drugs containing bile components. In addition, synthetic choleretics do not improve the properties of bile, like natural preparations and products containing medicinal herbs. But synthetic choleretics, in addition to choleretic, have the following therapeutic effects:
- Antispasmodic effect (eliminate spasm and pain in the biliary tract) is expressed in osalmide and hymecromone;
- Lipid-lowering effect (reduce the concentration of cholesterol in the blood due to its excretion from the body) expressed in osalmide;
- Antibacterial effect expressed in Nikodin;
- Anti-inflammatory effect expressed in tsikvalon;
- Suppression of decay and fermentation in the intestine - the effect is expressed in nicodine.
Plant choleretics have a milder effect compared to synthetic and natural preparations containing bile components. In addition, they have a complex positive effect on the organs of the gallbladder, ducts and liver, due to which their very high efficiency is achieved. That is why, at the present time, in the absence of allergies or intolerance to the components of herbs, it is recommended to use preparations containing herbal components as choleretics.
Hydrocholeretics
Indications for the use of hydrocholeretics, in principle, do not differ from those for choleretics. However, the drugs of this group are almost never used independently. Usually they are used in combination with other choleretic agents, mainly choleretics and cholekinetics, to enhance the therapeutic effect.Cholekinetics
Indications for the use of cholekinetics are as follows:- Hypotonic biliary dyskinesia;
- Atony of the gallbladder with congestion of bile with dyskinesia;
- Chronic cholecystitis;
- Chronic hepatitis;
- Gastritis with low or zero acidity (hypoacid or anacid) of gastric juice;
- Preparation for duodenal intubation.
Cholespasmolytics
Indications for the use of cholespasmolytics are as follows: - Dyskinesia of the biliary tract of the hyperkinetic form;
- Moderate pain syndrome accompanying diseases of the biliary tract and gallbladder.
Indications for the use of choleretic drugs with litholytic action
Indications for the use of choleretic drugs with litholytic action are as follows:- Dissolving small stones in the gallbladder and preventing the formation of new ones;
- Dissolution of stone fragments formed after the ultrasonic crushing procedure;
- Complex treatment of gallstone disease;
- Reflux gastritis or reflux esophagitis, provoked by the reflux of bile acids into the stomach or esophagus;
- Acute hepatitis;
- Toxic liver damage from poisons, alcohol, drugs, etc.;
- Compensated biliary cirrhosis of the liver;
- Primary cholangitis;
- Intrahepatic biliary tract atresia;
- Stagnation of bile against the background of parenteral nutrition;
- Biliary dyskinesia;
- Complex treatment of chronic opisthorchiasis;
- Prevention of liver damage while using cytostatics or oral contraceptives.
Taking choleretic drugs - short instructions
All choleretic drugs, regardless of the form of release, must be taken 20-30 minutes before meals. Moreover, the overall daily dosage split equally into 3 - 5 receptions, depending on how many times a day a person eats. It is recommended to take choleretic drugs before every meal. Preparations must be taken with a drink enough water and be sure to eat something half an hour after taking it. If a person does not eat anything after taking a choleretic drug, then he will experience nausea, diarrhea and overall health will worsen.Usually, choleretic drugs are taken for long (up to 3 - 8 weeks) courses 2 - 4 times a year, making intervals between them at least 1 - 2 months. Such courses of the use of choleretic drugs are prophylactic and should be carried out during the entire period of time while the disease persists. With exacerbation of diseases of the biliary tract, liver and gallbladder, choleretic drugs are used as part of complex therapy in high dosages.
Ursodeoxycholic acid preparations for the treatment of reflux gastritis and reflux esophagitis, as well as dissolution of gallstones, must be taken continuously for 6 to 8 months.
Choleretic drugs for children
The following choleretic drugs can be used in children:- Choleretics containing components of natural bile - Allochol;
- Synthetic choleretics - Nikodin, Oxafenamid, Osalmid;
- Choleretics containing medicinal herbs - Flamin, Febichol, Holosas, Holemax, Holos, Hofitol;
- Cholekinetics - Valerian, Valerianachel, Magnesia, Kormagnesin, magnesium sulfate;
- Anticholinergics (cholespasmolytics) - Atropine, Metacin, Platyphyllin, Papaverine, Papazol, Drotaverin, No-Shpa, Bioshpa, Nora-Drotaverin, Nosh-Bra, Ple-Spa, Spazmol, Spazmonet, Spazoverin, Spakovin Euphyllin.
In addition, children can drink alkaline mineral waters (Borjomi, Essentuki 17, Essentuki 4, Jermuk, Slavyanovskaya, etc.) as natural hydrocholeretics. It is recommended not to use medicinal herbs with a choleretic effect in children under 12 years old, since the prepared infusions and decoctions contain a wide range of active substances and it is simply impossible to predict the child's body reaction to all of them.
Choleretic drugs during pregnancy
Pregnant women can take only those choleretic drugs that do not provoke uterine contractile activity and do not penetrate the placenta to the fetus, and also do not cause a pronounced deterioration of the condition. The following choleretic drugs are completely safe during pregnancy: - Cholenzyme;
- Holosas;
- Holemax;
- Holos;
- Valerian;
- Magnesia (magnesium sulfate);
- Feed magnesin;
- Atropine;
- Metacin;
- Papaverine (Papazol);
- Drotaverin (No-Shpa, Bioshpa, Nora-Drotaverin, Nosh-Bra, Ple-Spa, Spazmol, Spazmonet, Spazoverin, Spakovin).
- Odeston;
- Holonerton;
- Cholestil;
- Flamin;
- Febichol;
- Berberis-Gommacord;
- Hofitol;
- Euphyllin.
Dosages, rules of admission and duration of therapy with choleretic drugs in pregnant women are exactly the same as usual.
The use of choleretic drugs for certain diseases
Biliary dyskinesia (BDT)
The selection of drugs depends on the form of biliary dyskinesia. So, for hypertensive type biliary dyskinesia
(ZhVP) the following choleretic drugs are shown: - Cholespasmolytics of any type (for example, No-Shpa, Papaverin, Platifillin, Metacin, Duspatalin, Odeston, etc.), which reduce pain;
- Cholekinetics (for example, Magnesia, Kormagnesin, Berberine-Gommacord, Cholosas, Cholemax, Cholos, Sorbitol, Mannitol, Flamin, etc.).
With dyskinesia of the hypotonic type of gastrointestinal tract the following choleretic drugs are shown:
- Any choleretics (for example, Allohol, Liobil, Nikodin, Tsikvalon, Holagogum, Holagol, Flakumin, Konvaflavin, Febichol, Sibektan, Tanacehol, etc.);
- Hydrocholeretics (alkaline mineral waters, etc.);
- Myotropic antispasmodics (Duspatalin, Odeston).
Choleretic drugs for bile stagnation
In this case, to eliminate stagnation, the most effective and optimal are their choleretic groups of cholekinetics, for example, Kormagnesin, Berberine-Gommacord, Holosas, Mannitol, Flamin, etc.Cholecystitis
Choleretic drugs for cholecystitis are used at any stage of the disease. In the presence of stones in the gallbladder with cholecystitis, only agents containing ursodeoxycholic acid as an active substance can be used as choleretic drugs (for example, Livodex, Urdoksa, Urso 100, Ursodez, Ursodex, Uroliv, Ursolit, Ursorom S, Ursosan, Ursanofalk, , Exhol). With non-calculous cholecystitis, it is necessary to take choleretics from any group. Among synthetic choleretics, choleretic drugs containing oxafenamide and gimecromone or cyclovalon are optimal. When using oxafenamide or gimecromone, you do not need to additionally take cholespasmolytics (No-Shpa, Papaverine, etc.), since these synthetic choleretics have an antispasmodic effect. And against the background of the use of Cyclovalon, you do not need to additionally take antibacterial drugs, since this choleretic has a pronounced antimicrobial effect. When using choleretics containing bile components or medicinal herbs (for example, Allochol, Liobil, Sibektan, Tanacekhol, etc.), it is necessary to additionally take cholespasmolytics or antibacterial drugs.
In addition to any choleretics with non-stone cholecystitis, it is necessary to take cholekinetics (Magnesia, Kormagnesin, Berberine-Gommacord, Holosas, Cholemax, Holos, Sorbitol, Mannitol, Flamin, etc.), which will facilitate the secretion of bile into the duodenum from the gallbladder.
There are very few negative reviews about choleretic drugs and they are usually due to the ineffectiveness of a particular drug in this particular case. The lack of a clinical effect causes disappointment in a person, from which he concludes that the drug is ineffective, and leaves a negative review about it.
However, choleretic drugs are very effective if taken correctly and as directed, taking into account the properties of each drug. Therefore, a negative review of a drug is not a reflection of its ineffectiveness, but of the wrong choice of medicine.
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