Pituitrin instructions for use. Pharmacological group - Choleretic agents and bile preparations. How would you rate Pituitrin?

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

Pituitrin contains oxytocin (see) and vasopressin (see), which are its active ingredients, providing the oxytotic (uterine) effect of Pituitrin (see Uterine products), as well as its vasopressor and antidiuretic effect. It is widely used as a medicine to stimulate and enhance the contractile activity of the uterine muscles, 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 effect, Pituitrin is used in the treatment of diabetes insipidus (if it is impossible to use adiurecrin) and bedwetting. Sometimes Pituitrin is also used as a choleretic agent.

P.'s biological activity is determined by the degree of contraction of the isolated guinea pig uterine horn caused by it and is expressed in the so-called. units of action - UNITS.

Pituitrin(Pituitrinum, Pituitrinum liquidum, Pituitrinum pro injectionibus, sp. B; syn.: 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, when preventing and stopping hypotonic bleeding in the early postpartum period) intravenously. The duration of action of P. is 4-5 hours. Higher doses for adults: single 10 units, daily 20 units. Children under 1 year of age are administered P. 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 in a day. When using P., especially in large doses, as a result of spasm of cerebral vessels, a headache may occur, sometimes abdominal pain, diarrhea, an allergic reaction, hemodynamic disturbances, swelling, and in some cases “pituitrin shock” occurs (headache, vomiting , feeling of compression in the chest, increased heart rate and breathing, drop in blood pressure, collapse).

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

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

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

Hyfotocin(syn. pituitrin M), like P., is a purified extract of the posterior lobe of the pituitary gland of cattle and pigs, but differs from it in a higher degree of purification and a higher content of oxytocin than vasopressin. It is used in obstetric and gynecological practice when labor is weak. The drug is a colorless transparent liquid with a faint odor 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 administered at 0.2-0.4 ml (1-2 units) every 30 minutes. until rhythmic contractions of the uterus appear. If it is necessary to artificially induce labor, hyfotocin is administered after 2-4-6 hours. after opening of the amniotic sac (the total dose should not exceed 5-10 units).

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, M., 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.

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Indications for use of the drug:

Effect of the drug on the human body:

Pituitrin dosage and methods of application:

Pituitrin is contraindicated in:

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Options for the release form of the drug:

Pituitrin composition:

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

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pharmachologic effect

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Authors

Links

• Official instructions for the drug Pituitrin.
• Modern drugs: a complete practical guide. Moscow, 2000. S. A. Kryzhanovsky, M. B. Vititnova.

Name: Pituitrinum

Pharmacological effects:
The main active ingredients of pituitrin are oxytocin and vasopressin (pitressin). The first causes a contraction of the muscles of the uterus, the second causes a narrowing of the capillaries (the smallest vessels) and an increase in blood pressure, participates in regulating the constancy of the osmotic pressure of the blood (hydrostatic pressure), causing an increase in water reabsorption (reverse absorption) in the convoluted ducts of the kidneys and a decrease in the reabsorption of chlorides.

Pituitrin - indications for use:

Pituitrin - method of application:

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Important!
Before using the medicine Pituitrin you should consult your doctor. This instruction is intended for informational purposes only.

Choleretic drugs are drugs that enhance 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 the absorption of water by the mucous membrane of the gallbladder. During the digestion process, 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 intestines 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 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 (BAs) - 67%, about 50% are primary FAs: cholic, chenodeoxycholic (1:1), the remaining 50% are secondary and tertiary FAs: deoxycholic, lithocholic, ursodeoxycholic, sulfolitocholic. The composition of bile also includes phospholipids (22%), proteins (immunoglobulins - 4.5%), cholesterol (4%), bilirubin (0.3%).

According to their chemical structure, FAs are derivatives of cholanic acid and represent the main end product of cholesterol metabolism. Most of the FAs are conjugated to glycine and taurine, which makes them stable at low pH values. Bile acids facilitate the emulsification and absorption of fats, inhibit cholesterol synthesis via 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.

Disturbances in the formation or outflow of bile into the duodenum can be of 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 quite arbitrary, because Most choleretic drugs 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 exocretion. 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 bile ducts, reduce the possibility of cholesterol precipitation, that is, they prevent the formation of gallstones, enhance the digestive and motor activity of the small intestine.

Drugs that promote bile secretion may act by stimulating contractions of the gallbladder (cholekinetics) or by relaxing the muscles of the biliary tract and sphincter of Oddi (cholespasmolytics).

Clinical classification of choleretic agents

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

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

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

3) preparations of plant origin: sandy immortelle flowers, corn silk, tansy (Tanacehol), rose hips (Holosas), Berberine bisulfate, birch buds, blue cornflower flowers, oregano herb, calamus oil, turpentine oil, peppermint oil, mackerel leaves (Flacumin), Far Eastern lily of the valley herb (Convaflavin), turmeric root (Phebihol*), 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 bile ducts: cholecystokinin*, magnesium sulfate, pituitrin*, choleritin*, barberry preparations, sorbitol, mannitol, xylitol.

B. Cholespasmolytics - cause relaxation of the biliary tract: atropine, platiphylline, methocinium iodide (Metacin), belladonna extract, papaverine, drotaverine (No-shpa), mebeverine (Duspatalin), aminophylline (Eufillin), Olimethine.

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 animal bile, may include extracts of medicinal plants, extract of liver tissue, pancreatic tissue and mucous membranes of the small intestine of cattle, activated carbon.

Bile acids, absorbed into the blood, stimulate the bile-forming function of hepatocytes, the unabsorbed part performs a replacement function. In this group, drugs that are bile acids increase the volume of bile to a greater extent, and drugs 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 (oxaphenamide, hymecromone), hypolipidemic (oxaphenamide), antibacterial (hydroxymethylnicotinamide), anti-inflammatory (cyclovalone), and also suppress the processes of putrefaction and fermentation in the intestines (especially hydroxymethylnicotinamide).

I.A.3) Effect herbal preparations associated with the influence of a complex of components included in their composition, incl. such as essential oils, resins, flavones, phytosterols, phytoncides, some vitamins and other substances. Drugs in this group increase the functional capacity of the liver, increase the secretion of bile, increase the content of cholates in bile (for example, immortelle, rose hips, Cholagol), and reduce the viscosity of bile. Along with increasing bile secretion, most herbal remedies in this group increase the tone of the gallbladder while simultaneously relaxing the smooth muscles of the biliary tract and sphincters of Oddi and Lutkens. Choleretic herbal remedies also have a significant effect on other functions of the body - they normalize and stimulate the secretion of the glands of the stomach and pancreas, increase the enzymatic activity of gastric juice, and enhance intestinal motility during atony. They also have antimicrobial (for example, immortelle, tansy, mint), anti-inflammatory (Olimethin, Cholagol, rosehip), diuretic, antimicrobial effects.

As medicinal preparations from plants, in addition to extracts and tinctures, infusions and decoctions from herbal collections are prepared. Usually take herbal medicines 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 and make it less viscous. The mechanism of action of choleretic drugs of this group is due to the fact that, being absorbed into the gastrointestinal tract, they are secreted by hepatocytes into primary bile, creating 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 bile ducts decreases, 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 help to increase 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 and reduce the tone of the common bile duct.

The cholekinetic effect 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 the cells of the duodenal mucosa. The main physiological functions of cholecystokinin are to stimulate contraction of the gallbladder and the secretion of digestive enzymes by the pancreas. Cholecystokinin enters the blood, is captured by 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 prescribed orally on an empty stomach, and is also administered through a probe (for 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, help normalize carbohydrate, lipid and other types of metabolism, stimulate bile secretion, cause the release of cholecystokinin, and relax the sphincter of Oddi. Polyhydric alcohols are used when performing duodenal intubation.

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

II.B. TO cholespasmolytics include drugs with different mechanisms of action. The main effect of their use is the weakening of spastic phenomena in the biliary tract. m-Cholinolytics (atropine, platyphylline), by blocking m-cholinergic receptors, have a non-selective antispasmodic effect on 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. Thus, nitrates relax the sphincter of Oddi, the lower esophageal sphincter, and reduce the tone of the biliary tract and esophagus. Nitrates are not suitable for long-term therapy, because have pronounced systemic side effects. Glucagon may temporarily decrease the tone of the sphincter of Oddi. But both nitrates and glucagon have a short-term effect.

Indications 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, and laxatives.

Unlike other choleretic drugs, drugs 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 stagnation of bile in dyskinesia, chronic cholecystitis, chronic hepatitis, in anacid and severe hypoacid conditions. They are also used during duodenal intubation.

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

Choleretics contraindicated at acute hepatitis, cholangitis, cholecystitis, pancreatitis, gastric and duodenal ulcers in the acute stage, cholelithiasis with obstruction of the excretory ducts, obstructive jaundice, as well as dystrophic lesions of the liver parenchyma.

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

Criteria for assessing the effectiveness and safety of the use of drugs used for impaired bile secretion:

- Laboratory: determination of bile acids in the blood and gallbladder bile (with pathology, the amount of bile acids in the blood increases, and in bile - decreases, the ratio between their three main forms - cholic, chenodeoxycholic, deoxycholic - and glycine and taurine conjugates changes), blood test (increased bile acids in blood leads to hemolysis, leukopenia, disrupts blood coagulation processes), determination in the blood of indirect and direct bilirubin, ALT, AST, bile pigments, etc.

- Paraclinical, incl. duodenal intubation, contrast cholecystography, ultrasound.

- Clinical: high concentrations of cholates in the blood cause bradycardia, arterial hypertension, skin itching, jaundice; symptoms of neurosis appear; pain in the right hypochondrium or epigastrium, enlarged liver.

TO drugs used for increased lithogenicity of bile(in the absence of stones), include Allohol, Cholenzym, hydroxymethylnicotinamide (Nicodin), sorbitol, Olimethine. The drugs in this group have different mechanisms of action, since the lithogenicity of bile depends on many factors.

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

Cholesterol, which forms the basis of most gallstones, is normally found 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 concentrations of phospholipids and cholesterol and a supersaturation of bile with cholesterol can lead to the fact that the bile becomes lithogenic, i.e. capable of forming cholesterol stones. Changes in the physicochemical properties of bile lead to the precipitation of cholesterol crystals, which then form a nucleus to form cholesterol gallstones.

Both ursodeoxycholic and chenodeoxycholic acids change the ratio of bile acids, reduce the secretion of lipids into bile and lower the cholesterol content 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 treatments for cholelithiasis.

Drugs

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