Pituitrin pharmacological group. Pharmacological group - Cholagogues and bile preparations

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Indications for the use of the drug:

It is used to excite and enhance the contractile activity of the uterus during its primary and secondary weakness and distortion of pregnancy; hypotonic bleeding (bleeding caused by a decrease in the tone of the muscles of the uterus) in the early postpartum period; to normalize the involution of the uterus (reduction of the volume of the body of the uterus) in the post-natal and post-abortion periods. Diabetes insipidus (a disease caused by the absence or decrease in the secretion of antidiuretic / reducing urination / hormone). Bed-wetting.

The effect of the drug on the human body:

The main active ingredients of pituitrin are oxytocin and vasopressin (pitressin). The first causes contraction of the muscles of the uterus, the second - narrowing of the capillaries (the smallest vessels) and an increase in blood pressure, is involved in regulating the constancy of the osmotic pressure of the blood (hydrostatic pressure), causing an increase in water reabsorption (reabsorption) in the convoluted canal kidneys and a decrease in the reabsorption of chlorides.
Pituitrin activity is standardized by biological methods; 1 ml of the product must contain 5 units.

Pituitrin dosage and methods of application:

The drug is administered under the skin or intramuscularly in 0.2-0.25 ml (1.0-1.25 IU) every 15-30 minutes 4-6 times. To enhance the effect, pituitrin can be combined with intramuscular injection of estrogens (female sex hormones).
A single dose of pituitrin 0.5-1.0 ml (2.5-5 IU) can be used in the second stage of labor in the absence of obstacles to the advancement of the fetal head and rapid delivery.
To prevent and stop hypotonic bleeding in the early postpartum period, pituitrin is sometimes administered intravenously (1 ml - 5 IU - in 500 ml of 5% glucose solution) or very slowly (0.5-1 ml in 40 ml of 40% glucose solution).
In connection with the antidiuretic (reducing urination) effect of the product, it is also used for bedwetting and diabetes insipidus. Injected under the skin and into the muscles of adults, 1 ml (5 units), children under 1 year old - 0.1-0.15 ml, 2-5 years old - 0.2-0.4 ml, 6-12 years old - 0.4-0.6 ml 1-2 times every day.
Higher doses for adults: single - 10 IU, daily - 20 IU.

Pituitrin is contraindicated in:

Severe atherosclerosis, myocarditis (inflammation of the heart muscle), hypertension (persistent rise in blood pressure), thrombophlebitis (inflammation of the vein wall with their blockage), sepsis (infection of the blood with microbes from the focus of purulent inflammation), nephropathy (kidney disease) of pregnant women. The drug can not be prescribed in the presence of scars on the uterus, the threat of uterine rupture, the wrong position of the fetus.

Pituitrin possible side effects:

Large doses of pituitrin, especially with rapid administration, can cause spasms (a sharp narrowing of the lumen) of cerebral vessels, circulatory disorders, and collapse (a sharp drop in blood pressure).

Options for the form of release of the drug:

In 1 ml ampoules containing 5 units.

Pituitrin composition:

A hormonal product derived from the posterior pituitary gland of cattle and pigs.
Transparent colorless liquid of acid reaction (pH 3.0 - 4.0).
Preserved with 0.25 - 0.3% phenol solution.
The main active ingredients of pituitrin are oxytocin and vasopressin (pitressin).
Pituitrin activity is standardized by biological methods; 1 ml of the product should contain 5 U. List B. In a place protected from light at a temperature of +1 to +10 °C.

Be careful, before using the drug Pituitrin, you need to consult a doctor, since Pituitrin has various side effects and contraindications.

Pituitrin (Pituitrinum)

Pharmacological action of the drug.

The main active ingredients of pituitrin are oxytocin and vasopressin (pitressin). The first causes contraction of the muscles of the uterus, the second - narrowing of the capillaries (the smallest vessels) and an increase in blood pressure, is involved in regulating the constancy of the osmotic pressure of the blood (hydrostatic pressure), causing an increase in water reabsorption (reabsorption) in the convoluted canal kidneys and a decrease in the reabsorption of chlorides.

What is used for. Indications for the use of the drug.

It is used to excite and enhance the contractile activity of the uterus during its primary and secondary weakness and distortion of pregnancy; hypotonic bleeding (bleeding caused by a decrease in the tone of the muscles of the uterus) in the early postpartum period; to normalize the involution of the uterus (reduction of the volume of the body of the uterus) in the postpartum and post-abortion periods. Diabetes insipidus (a disease caused by the absence or decrease in the secretion of antidiuretic / reducing urination / hormone). Bed-wetting.

Dosage and method of application.

The drug is administered under the skin or intramuscularly at 0.2-0.25 ml (1.0-1.25 IU) every 15-30 minutes 4-6 times. To enhance the effect, pituitrin can be combined with intramuscular injection of estrogens (female sex hormones).
A single dose of pituitrin 0.5-1.0 ml (2.5-5 IU) can be used in the second stage of labor in the absence of obstacles to the advancement of the fetal head and rapid delivery.
To prevent and stop hypotonic bleeding in the early postpartum period, pituitrin is sometimes administered intravenously (1 ml - 5 IU - in 500 ml of 5% glucose solution) or very slowly (0.5-1 ml in 40 ml of 40% glucose solution).
In connection with the antidiuretic (reducing urination) effect of the drug, it is also used for bedwetting and diabetes insipidus. Injected under the skin and into the muscles of adults 1 ml (5 units), children under 1 year - 0.1-0.15 ml, 2-5 years - 0.2-0.4 ml, 6-12 years - 0.4-0.6 ml 1-2 times a day.
Higher doses for adults: single - 10 IU, daily - 20 IU.

Side effects and actions of the drug.

Large doses of pituitrin, especially with rapid administration, can cause spasms (a sharp narrowing of the lumen) of cerebral vessels, circulatory disorders, and collapse (a sharp drop in blood pressure).

Contraindications and negative properties.

Severe atherosclerosis, myocarditis (inflammation of the heart muscle), hypertension (persistent rise in blood pressure), thrombophlebitis (inflammation of the vein wall with their blockage), sepsis (infection of the blood with microbes from the focus of purulent inflammation), nephropathy (kidney disease) of pregnant women. The drug can not be prescribed in the presence of scars on the uterus, the threat of uterine rupture, the wrong position of the fetus.

Release form. Package.

In 1 ml ampoules containing 5 units.

Terms and conditions of storage.

List B. In a place protected from light at a temperature of +1 to +10 ° C.

Composition and content.

A hormonal preparation derived from the posterior pituitary gland of cattle and pigs.
Transparent colorless liquid of acid reaction (pH 3.0 - 4.0).
Preserved with 0.25 - 0.3% phenol solution.
The main active ingredients of pituitrin are oxytocin and vasopressin (pitressin).
Pituitrin activity is standardized by biological methods; 1 ml of the drug should contain 5 units.

Active ingredients: Oxytocin, vasopressin

Important!

Description of the drug Pituitrin» on this page is a simplified and supplemented version of the official instructions for use. Before purchasing or using the drug, you should consult your doctor and read the annotation approved by the manufacturer.
Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide on the appointment of the drug, as well as determine the dose and methods of its use.

Solution in 1 ml ampoules (5 IU).

pharmachologic effect

Stimulation of labor activity.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Pituitrin is a hormonal drug that is obtained from the pituitary gland of cattle. It contains hormones oxytocin and vasopressin . Biological activity is determined by the content oxytocin . Stimulates labor by causing uterine contractions. It has a vasoconstrictive effect and increases due to the presence vasopressin . The antidiuretic effect is manifested in an increase in the reabsorption of water in the kidneys.

Pharmacokinetics

Data not presented.

Indications for use

  • metrorrhagia ;
  • weakness of labor activity;
  • postpartum hemorrhage;
  • urinary incontinence;
  • diabetes insipidus .

Contraindications

  • hypersensitivity;
  • hypertonic disease ;
  • myocarditis ;
  • pronounced;
  • sepsis ;
  • pregnant women;
  • scars on the uterus and the threat of its rupture.

Pituitrin is used with caution when.

Side effects

Pituitrin can cause:

  • fetus;
  • uterine hypertonicity;
  • boost ;
  • bronchospasm .

Pituitrin, instructions for use (Method and dosage)

Pituitrin in the form of a solution is administered subcutaneously or intramuscularly. The highest single dose is 10 IU.

With uterine bleeding and for contraction of the uterus after childbirth - 0.25 ml every 30 minutes, bringing up to a total dose of 1 ml.

For rapid delivery, 0.5-1.0 ml is used once in the second stage of labor.

At diabetes insipidus - 1 ml intramuscularly 1-2 times a day.

Overdose

Cases of overdose are not known.

Interaction

Data not provided.

Terms of sale

Pituitrin is available by prescription.

Storage conditions

Temperature 1-8°C.

Best before date

Analogues

, Hyphotocin .

Reviews

Strengthen the contractility of the uterus - a synthetic drug oxytocin and natural organ preparations Hyphotocin and Pituitrin, which contains oxytocin and vasopressin , therefore, in addition to the effects inherent in oxytocin, it also increases blood pressure. In gynecological practice, it was used for the same indications as oxytocin: to stimulate labor, with uterine atony, and bleeding. The non-pregnant uterus is more sensitive to vasopressin , and with pregnancy increases sensitivity to oxytocin .

The drug Pituitrin is maximally freed from vasopressin , it is administered intravenously. Hyphotocin has less content vasopressin . Currently, these drugs are not found in the pharmacy network and are not used. There is an explanation for this. Synthetic oxytocin has the advantage that it has a more selective effect on the uterus, since it does not contain impurities of other hormones and does not significantly affect HELL . In addition, it is free of proteins and is used intravenously, without fear of pyrogenic effects, so for many years it has been widely used in gynecological practice.

PITUITRIN- a hormonal preparation, which is an aqueous extract of the posterior pituitary gland of cattle and pigs.

Pituitrin contains oxytocin (see) and vasopressin (see), to-rye are its active ingredients, providing the oxytocytic (uterine) action of Pituitrin (see. Uterine drugs), as well as its vasopressor and antidiuretic action. It is widely used as a drug to excite and enhance the contractile activity of the muscles of the uterus, with hypotonic bleeding in the early postpartum period, as well as to normalize the involution of the uterus in the postpartum and post-abortion periods. Pituitrin is also used in some surgical operations and in the early postoperative period, especially in patients with portal hypertension. Due to its anti-diuretic action, Pituitrin is used in the treatment of diabetes insipidus (if adiurecrin cannot be used) and bedwetting. Sometimes Pituitrin is also used as a choleretic agent.

The biological activity of P. is determined by the degree of contraction of the isolated horn of the uterus of the guinea pig caused by it and is expressed in the so-called. units of action - ED.

Pituitrin(Pituitrinum, Pituitrinum liquidum, Pituitrinum pro injectionibus, sp. B; synonym: Glanduitrin, Hypophen, Hypophysin, Piton, Pituglandol, Pituigan, etc.) is a colorless liquid with a pH of 3.0-4.0. Liquid P. is preserved by adding 0.3% phenol solution.

P. is administered subcutaneously or intramuscularly, and in some cases (for example, in the prevention and stopping of hypotonic bleeding in the early postpartum period) intravenously. Duration of action P. 4-5 hours. Higher doses for adults: single 10 IU, daily 20 IU. Children under the age of 1 year P. administered 0.1-0.15 ml, 2-5 years 0.2-0.4 ml, 6-12 years 0.4-0.6 ml 1-2 times in a day. When P. is used, especially in large doses, as a result of a spasm of cerebral vessels, a headache may occur, sometimes abdominal pain, diarrhea, an allergic reaction, hemodynamic disturbances, edema occur, in some cases pituitrin shock occurs (headache, vomiting , a feeling of constriction in the chest, increased heart rate and respiration, a drop in blood pressure, collapse).

P. contraindicated with hypertension, thrombophlebitis, severe atherosclerosis, angina pectoris, nephropathy of pregnant women, eclampsia, sepsis, myocarditis, the threat of uterine rupture, the presence of scars on the uterus, the wrong position of the fetus.

Release form: 1 ml ampoules containing 5 or 10 IU P.

Storage: cool (1.-10°). place protected from light.

Hyphotocin(syn. pituitrin M), as well as P., is a purified extract of the posterior pituitary gland of cattle and pigs, but differs from it in a higher degree of purification and a higher content of m oxytocin than vasopressin. It is used in obstetric and gynecological practice with weakness of labor activity. The drug is a colorless transparent liquid with a slight smell of phenol, which is used as a preservative; pH 3.0-4.0. Activity ("uterine") is expressed, as in P., in units of action - UNITS: 1 ml of the drug contains 5 UNITS. Hyfotocin is injected at 0.2-0.4 ml (1-2 IU) every 30 minutes. before the onset of rhythmic uterine contractions. If it is necessary to induce labor artificially, hyphotocin is administered after 2-4-6 hours. after opening the fetal bladder (total dose should not exceed 5-10 IU).

Bibliography: Anosova L. N., Zefirova G. S. and Krakov V. A. Brief endocrinology, p. 264, M., 1971; Arnaudov G. D. Drug therapy, trans. from Bulgarian, p. 205, Sofia, 1975; Mashkovsky M. D. Medicines, part 1, p. 544, 548, M., 1977; Drugs used in endocrinology, ed. H. T. Starkova, p. 68, Moscow, 1969; Tsatsanidi K. N., Novik M. G. and Scherzinger A. G. The use of pituitrin for bleeding from the veins of the esophagus and during operations in patients with portal hypertension, Vestn, hir., t. 104, No. 5, p. 29, 1970.

V. V. POTEMKIN.

Choleretic drugs are drugs that increase bile formation or promote the release of bile into the duodenum.

bile ( bilis- lat., fel- English) - a secret produced by hepatocytes. Bile production occurs continuously in the body. Bile produced in the liver is secreted into the extrahepatic bile ducts, which collect it into the common bile duct. Excess bile accumulates in the gallbladder, where it is concentrated 4-10 times as a result of absorption of water by the mucous membrane of the gallbladder. In the process of digestion, bile from the gallbladder is released into the duodenum, where it is included 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, cholecystokinin (pancreozymin) is of the greatest importance, 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 you move through the intestines, the main part 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. The composition of bile also includes phospholipids (22%), proteins (immunoglobulins - 4.5%), cholesterol (4%), bilirubin (0.3%).

According to the chemical structure, fatty acids are derivatives of cholanic acid and are the main end product of cholesterol metabolism. Most FAs are conjugated with glycine and taurine, making them stable at low pH. Bile acids facilitate the emulsification and absorption of fats, inhibit the synthesis of cholesterol by a feedback mechanism, and the absorption of fat-soluble vitamins (A, D, E, K) depends on their presence. In addition, bile acids increase the activity of pancreatic enzymes.

Violations of 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 that promote its release from the gallbladder into the duodenum ( Cholagoga, or Cholekinetica). This division is rather conditional, because most choleretic agents simultaneously enhance 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 liver exosecretion. 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, accelerate the flow of bile through the biliary tract, reduce the possibility of cholesterol precipitation, that is, prevent the formation of gallstones, enhance the digestive and motor activity of the small intestine.

Bile-promoting drugs can act by stimulating gallbladder contractions (cholekinetics) or by relaxing the muscles of the bile ducts and the sphincter of Oddi (cholespasmolytics).

Clinical classification of choleretic agents

(see Belousov Yu.B., Moiseev V.S., Lepakhin V.K., 1997)

[* - drugs or active ingredients are marked, the drugs of which do not currently have a 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: Allohol, Cholenzym, Vigeratin, dehydrocholic acid (Hologon *) and sodium salt of dehydrocholic acid (Decholine *), Liobil *, etc.;

2) synthetic drugs: hydroxymethylnicotinamide (Nicodin), osalmid (Oxafenamide), cyclovalone (Cyqualon), hymecromon (Odeston, Holonerton*, Cholestil*);

3) herbal preparations: flowers of immortelle sandy, corn stigmas, common tansy (Tanacechol), rose hips (Holosas), Berberine bisulfate, birch buds, blue cornflower flowers, oregano herb, calamus oil, turpentine oil, peppermint oil, skumpia leaves (Flacumin), Far Eastern lily of the valley herb (Konvaflavin), turmeric root (Febihol*), buckthorn, etc.

B. Drugs that increase the secretion of bile due to the water component (hydrocholeretics): mineral waters, 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, metocinium iodide (Metacin), belladonna extract, papaverine, drotaverine (No-shpa), mebeverine (Duspatalin), aminophylline (Eufillin), Olimetin.

I.A.1) Preparations containing bile acids and bile- these are drugs containing either bile acids themselves or combined drugs, which, in addition to lyophilized bile of animals, may include extracts of medicinal plants, an extract of liver tissue, pancreatic tissues and mucous membranes of the small intestine of cattle, activated carbon.

Bile acids, being absorbed into the blood, stimulate the bile-forming function of hepatocytes, the non-absorbed 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 the bile. After entering the hepatocytes from the blood, these drugs are secreted into the bile and dissociated, forming organic anions. A 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, gimecromon), hypolipidemic (oxafenamide), antibacterial (hydroxymethylnicotinamide), anti-inflammatory (cyclovalone), and also suppress the processes of putrefaction and fermentation in the intestine (especially hydroxymethylnicotinamide).

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. The drugs of this group increase the functional ability of the liver, increase the secretion of bile, increase the content of cholates in bile (for example, immortelle, wild rose, Cholagol), reduce the viscosity of bile. Along with increased bile secretion, most herbal remedies of this group increase the tone of the gallbladder while relaxing 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 the enzymatic activity of gastric juice, and increase intestinal motility during its atony. They also have antimicrobial (for example, immortelle, tansy, mint), anti-inflammatory (Olimetin, Cholagol, wild rose), diuretic, antimicrobial action.

As medicines from plants, in addition to extracts and tinctures, infusions and decoctions are prepared from herbal preparations. Usually take herbal remedies 30 minutes before meals, 3 times a day.

I.B. Hydrocholeretics. This group includes mineral waters - Essentuki No. 17 (highly mineralized) and No. 4 (weakly mineralized), Jermuk, Izhevskaya, Naftusya, Smirnovskaya, Slavyanovskaya, etc.

Mineral waters increase the amount of secreted bile, making it less viscous. The mechanism of action of 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 aqueous phase. In addition, the reabsorption of water and electrolytes in the gallbladder and biliary tract 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 sparingly soluble precipitate.

Mineral waters are usually consumed warm 20-30 minutes before meals.

Hydrocholeretics also include salicylates (sodium salicylate) and valerian preparations.

II.A. To cholekinetics include drugs that increase the tone and motor function of the 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 of cholecystokinin are to stimulate the contraction of the gallbladder and the secretion of digestive enzymes by the pancreas. Cholecystokinin enters the bloodstream, is captured by the liver 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 enters the duodenum and its stagnation is eliminated.

Magnesium sulfate has a choleretic effect when taken orally. A solution of magnesium sulfate (20-25%) is administered orally on an empty stomach, and also administered through a probe (with duodenal sounding). In addition, magnesium sulfate also has a cholespasmolytic effect.

Polyhydric alcohols (sorbitol, mannitol, xylitol) have both cholekinetic and choleretic effects. They have a positive 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 sounding.

Olive and sunflower oils, plants containing bitterness (including dandelion, yarrow, wormwood, etc.), essential oils (juniper, cumin, coriander, etc.), extract and juice of cranberries, lingonberries, etc., also have a cholekinetic effect. others

II.B. To cholespasmolytics include drugs with different mechanisms of action. The main effect of their application is the weakening of spastic phenomena in the biliary tract. m-Cholinolytics (atropine, platifillin), blocking m-cholinergic receptors, have a non-selective antispasmodic effect on various parts of the gastrointestinal tract, incl. regarding the bile ducts.

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 severe systemic side effects. Glucagon can temporarily reduce the tone of the sphincter of Oddi. But both nitrates and glucagon have a short-term effect.

Testimony choleretics are prescribed for chronic inflammatory diseases of the 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, preparations containing bile acids and bile are means 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, so they are prescribed mainly for the hypotonic form of biliary dyskinesia. Indications for their use are atony of the gallbladder with bile stasis in dyskinesia, chronic cholecystitis, chronic hepatitis, in anacid and severe hypoacid conditions. They are also used during duodenal sounding.

Cholespasmolytics are prescribed for hyperkinetic form of biliary dyskinesia and for cholelithiasis. They are used to relieve pain of moderate intensity, often accompanying the pathology of the biliary tract.

Choleretics contraindicated at acute hepatitis, cholangitis, cholecystitis, pancreatitis, peptic ulcer of the stomach and duodenum in the acute stage, with cholelithiasis with blockage of the excretory ducts, with obstructive jaundice, as well as with degenerative lesions of the liver parenchyma.

Cholekinetics are contraindicated in acute liver diseases, in the presence of gallstones, with exacerbation of hyperacid gastritis and peptic ulcer of the stomach and duodenum.

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 (in 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) changes, a 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 in the blood, etc.

- paraclinical, including duodenal sounding, contrast cholecystography, ultrasound.

- Clinical: high concentrations of cholates in the blood cause bradycardia, arterial hypertension, pruritus, 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 (Nicodin), sorbitol, Olimetin. Means of this group have different mechanisms of action, since the lithogenicity of bile depends on many factors.

Cholelitholytic agents(cm. ). A number of deoxycholic acid derivatives, in particular ursodeoxycholic acid, isomeric chenodeoxycholic acid, can not only prevent the formation of cholesterol stones in the gallbladder, but also dissolve existing ones.

Cholesterol, which forms the basis of most gallstones, is normally in a dissolved state in the center of micelles, the outer layer of which is formed by bile acids (cholic, deoxycholic, chenodeoxycholic). Phospholipids concentrated in the center of the micelle increase its ability to prevent cholesterol crystallization. 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 bile becoming lithogenic, i.e. capable of forming cholesterol stones. A change in the physicochemical properties of bile leads to the 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 into bile and lower the content of 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 addition to surgical or shock wave methods for the treatment of cholelithiasis.

Preparations

Preparations - 1670 ; Trade names - 80 ; Active ingredients - 21

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