Clinical pharmacology of choleretic agents

Choleretki(stimulate the formation of bile). True (increase the secretion of bile and bile acids): containing bile acids: cholenzym, cholagod, holosas, decholine; synthetic: iqualon, oxafenamide.

Plant origin: peppermint, tansy, rosehip. Hydrocholeretics (increase the water component of bile): valerian, sodium salicylate, mineral water.

Diseases of the liver, pancreas and biliary tract ♦ 395

cholekinetics(increase the tone of the gallbladder and reduce the tone of the biliary tract): magnesium sulfate, sorbitol, xylitol, berberine, cholecystokinin, sea buckthorn and olive oils, m-cholinolytics, nitrosorbitol, aminophylline.

Choleretics are contraindicated in severe inflammation of the gallbladder and bile ducts and in hepatitis.

Cholekinetics are contraindicated in duodenal and biliary hypertension.

Choleretics are best used in the remission phase and in combination with enzyme preparations, and with hypokinetic lyskinesia, it is better to use in combination with cholekinetics.

Holenzim

Pharmacodynamics. Combined drug, has a choleretic effect. Digestive enzymes (trypsin, amylase, lipase) and bile facilitate the digestion of proteins, fats, carbohydrates, which contributes to their more complete absorption in the small intestine. Improves the functional state of the gastrointestinal tract, normalizes the process of digestion.

Indications. IN as a choleretic and digestive enzyme in diseases and functional disorders of the gastrointestinal tract: chronic hepatitis, chronic cholecystitis, chronic pancreatitis, flatulence, diarrhea of non-infectious origin. To improve digestion, write in persons with normal function of the gastrointestinal tract in case of nutritional errors (eating fatty foods, overeating, irregular meals) and in case of chewing disorders, sedentary lifestyle, prolonged immobilization.

Contraindications. Hypersensitivity, acute pancreatitis, exacerbation of chronic pancreatitis, obstructive jaundice.

NLR. Allergic reactions (sneezing, lacrimation, skin redness, skin rash).

Osalmid(oxafenamide)

Pharmacodynamics. Choleretic agent. It has a choleretic and cholekinetic effect. It enhances the formation and secretion of bile, relieves spasm of the smooth muscles of the biliary tract and the sphincter of the common bile duct, reduces the content of cholesterol and bilirubin in the blood.

Indications. Chronic cholecystitis, cholangitis, cholelithiasis, cholecystohepatitis, to enhance bile secretion before duodenal sounding.

Contraindications. Acute hepatitis, cirrhosis of the liver, peptic ulcer of the stomach and duodenum, obstructive jaundice.

NLR. Diarrhea, allergic reactions.

Special instructions. It is recommended to combine with antibacterial drugs for acute inflammatory processes in the biliary tract and gallbladder; with severe spasms and accompanying pain, it is advisable to simultaneously prescribe anticholinergics and other antispasmodics.

Chenodeoxycholic acid(chenofalk)

Pharmacodynamics. Physiological bile acid of the system of hepatic-intestinal regulation; has a hypolipidemic, choleretic, choleretic effect. Reduces the synthesis and adsorption of cholesterol, dissolves cholesterol gallstones. Chenodeoxycholic acid is the primary bile acid, accounting for 20-30% of the total pool of bile acids. Brake-

396 ♦ Clinical pharmacology and pharmacotherapy ♦ Chapter 22

zit enzymatic synthesis of cholesterol in the liver, reducing the activity of hydroxy-3-methyl-glutaryl-CoA reductase, which leads to a decrease in cholesterol in bile. Changes the ratio of bile acids and cholesterol towards the predominance of chenodeoxychodic kyelosh in the general pool of bile acids. Changes bile quantitatively and qualitatively: the volume of secreted bile increases with an increase in the level of conjugated bile acids "] .

Pharmacokinetics. Rapidly and well absorbed after oral administration in the small intestine. In the course of s-interhepatic circulation, it is metabolized with the formation of lithocholic acid. Metabolites are excreted in feces.

Indications. Cholesterol gallstones (no more than 15-20 mm in size) in the gallbladder (no more than half filled with stones) if they cannot be removed surgically or endoscopically.

Contraindications. Hypersensitivity, calcification of stones, acute cholecystitis, cholangitis, hepatitis, Crohn's disease, liver irrosis, peptic ulcer of the stomach and duodenum (in (time of exacerbation), ulcerative catitis, inflammatory diseases of the esophagus, stomach, intestines, malabsorption syndrome, hepatic and / or kidney failure, pregnancy.

HJIP. Diarrhea, biliary colic, transient increase in liver transaminases, allergic reactions (pruritus, skin rash).

Interaction with others LS. Colestyramine. cholestipol. aluminium-containing antanides reduce the effectiveness of chenodeoxychodic acid. Henofalk enhances the effect of antidiabetic agents.

22.8. Chronic pancreatitis

Chronic pancreatitis is a progressive disease of the pancreas with signs of an acute inflammatory process during exacerbation, gradual replacement of the parenchyma with connective tissue and the development of insufficiency. ju- and endocrine functions of the organ.

There are 3 types of chronic pancreatitis:

Chronic kalyshfshruyushy pancreatitis (occurring against the background of chronic alcoholism):

Chronic obstructive pancreatitis (occurring against the background of obstruction of the pancreatic duct by a tumor or stone);

Chronic inflammatory pancreatitis (: * thiolo! I am not completely clear).

Ethnology and iatogenesis. One of the main etiological factors are alcohol (drinking alcoholic beverages daily, more than 20 g in terms of pure ethanol), taking drugs (azathioprine, hypohyazid, furosemide, sulfonamides, tetraiclines, eulfasalazine, asparaginase, glucocorticosteroids, mstronidazole, nitrofurans, non-steroidal anti-inflammatory drugs ), hereditary predisposition, malnutrition (consumption of less than 30 g of fat and 50 g of protein per day).

Chronic pancreatitis may be the result of acute pancreatitis and damage to other organs of the gastrointestinal tract: cholecystitis, peptic ulcer, bowel disease, liver.

Diseases of the liver, pancreas and biliary tract ♦ 397

Symptom complex of chronic pancreatitis. The main symptom is paroxysmal or constant girdle pain in the upper abdomen, accompanied by nausea, vomiting, loss of appetite, flatulence, unstable stools or diarrhea. The pain often radiates to the left half of the chest, the region of the heart, the left shoulder, is aggravated or provoked by a violation of the diet, eating fatty food, overeating, and especially drinking alcohol.

The course and severity of the disease. In the early stages of development, chronic pancreatitis is manifested by exacerbations or acute pancreatitis is complicated by the development of chronic. Pain syndrome is determined by acute attacks.

With the progression of chronic pancreatitis, the development of maldigestion syndrome 1 with steatorrhea 2 and weight loss, diabetes mellitus, vitamin B 12 deficiency anemia, and the formation of cholestasis as a result of compression of the common bile duct 3 are possible.

Methods of examination and diagnosis. Ultrasound is considered the most informative, its sensitivity in chronic pancreatitis reaches 85%. Another sensitive method for detecting changes in the pancreas is computed tomography.

If ductal obstruction is suspected, endoscopic retrograde cholangiopancreatography is used. The main purpose of this study is to clarify the state of the pancreatic ducts and bile ducts.

To confirm the diagnosis of chronic pancreatitis and its exacerbation, the content of amylase and lipase in the blood is usually determined. These enzymes are released into the blood in large quantities during acute inflammation of the gland. The level of amylase decreases rapidly with the weakening of the severity of the process, and the elevated level of lipase in the blood persists much longer. The content of acid phosphatase (a marker of lysosomal enzymes) increases in the blood, and the level of amylase in the urine increases.

Of particular practical interest is the determination of elastase in feces. This method is based on the use of highly specific monoclonal antibodies to pancreatic elastase. The method has high specificity and sensitivity and does not change in other diseases.

Clinical and pharmacological approaches to the choice of drugs for the treatment of chronic pancreatitis. Treatment of patients with chronic pancreatitis can be conservative or surgical. At the onset of the disease, with mild clinical manifestations, conservative treatment is indicated. In advanced cases with excruciating pains that are not amenable to conservative treatment, with the development of obstructive jaundice due to obstruction of the common bile duct, and complications (cyst, abscess), surgical treatment is recommended.

1 Maldigestion syndrome - a syndrome of indigestion. Occurs due to violation
digestion with a deficiency of enzymes on the membranes and in the cavity of the small intestine.

2 Steatorrhea - excretion of a large amount of fat with feces (more than 7-9 g with a diet containing
rub 100 g of fat).

3 The common bile duct passes through the thickness of the pancreas, where it can expose
pressure.

398 f Clinical pharmacology and pharmacotherapy -> Chapter 22

The treatment of chronic pancreatitis is based on 3 principles:

Dieting (restriction of products that stimulate the activity of the pancreas), avoidance of alcohol;

Relief of pain syndrome and prevention of complications;

Correction of exocrine and endocrine pancreatic insufficiency.

In chronic pancreatitis, frequent, fractional meals with a low fat content (30-40 g / day) and a sufficient amount of protein (80-120 r / day) are shown. In the acute phase, in the first 1-3 days, hunger is prescribed (according to indications, parenteral nutrition is possible), taking antacids, H is administered parenterally; - histamine blockers, provide detoxification therapy,

Treatment of exacerbations of chronic pancreatitis. To relieve pain, baralgin or a synthetic analogue of somatostatin, sandostatin, is administered parenterally. With insufficient effectiveness, you can use narcotic analgesics - promedol (but not morphine).

In severe exacerbation of chronic pancreatitis and high hyperenzymemia, protease inhibitors are traditionally used. However, their use is justified and effective only in the first 4-5 days, until the external secretion of the pancreas is suppressed. Anti-enzyme preparations contrykal, gordox, trasylol neutralize fermentemia, reduce the activity of the kallik-rhein-kinin system, inhibit proteases, normalize the rheological properties of blood and improve microcirculation. However, these drugs are ineffective in destructive forms of pancreatitis and do not prevent their development, the expediency of their use in has been questioned lately.

From the first day of exacerbation of chronic pancreatitis to prevent septic complications, it is recommended to administer antibiotics (semi-synthetic peniiillins or cephalosporins in usual daily doses).

Supportive care(outside of exacerbations of chronic pancreatitis) includes enzyme replacement therapy.

Monitoring the effectiveness of treatment. At Evaluation of effectiveness must take into account the dynamics of pain, body weight, dyspeptic disorders (diarrhea, flatulence, vomiting stop), and the absence of complications.

The effectiveness of the therapy is evidenced by the normalization of the level of pancreatic enzymes in the blood and urine, the disappearance of steatorrhea and creatorrhea.

Treatment safety control is aimed at predicting, preventing and stopping NLR, which includes a subjective assessment of the patient's condition, the dynamics of the results of objective, functional and laboratory research methods.

106. Means that promote the formation of bile and its secretion. Classification. Pharmacological characteristics of drugs.

Cholagogues are drugs that increase the secretion of bile or promote its progress through the biliary tract into the duodenum.

Drugs that stimulate bile production function liver (choleretics):

Preparations containing bile acids(tablets "Holenzim", "Allohol", "Liobil")

Synthetic choleretics ( Hydroxymethylnicotinamide (Nicodin), cyclovalone, osalmide)

Choleretics of plant origin(immortelle flowers, flamin, corn stigmas, holosas, liv-52)

Drugs that increase the secretion of the water component of bile (hydrocholeretics) (to ornevisca with valerian roots)

This group includes preparations containing bovine bile components (allohol, cholenzym, lyobil, etc.) and / or plant sterols that are part of choleretic herbs (immortelle flowers, corn stigmas, Liv -52, Holosas or rose hip extract) increasing concentration of organic anions (tanacechol, etc.). Synthetic drugs (choleretics) include: hydroxymethylnicotinamide (Nicodin), cyclovalone, osalmide (Oxaphenamide).

Bile-containing choleretics increase bile secretion by stimulating the secretory function of the liver parenchyma. In addition, they stimulate the receptors of the mucous membrane of the small intestine, which enhances the formation of bile; increase osmotic filtration of water and electrolytes into the bile ducts; increase the flow of bile through the biliary tract, which prevents the ascent of the infection and leads to a decrease in the inflammatory process; increase the content of cholates in bile, which reduces the possibility of the formation of cholesterol stones.

All drugs in this group are contraindicated in cases of biliary tract obstruction (obstructive jaundice).

Absolute contraindications to the use of choleretics are all variants of cholestasis: intrahepatic (hepatocellular, canalicular, ductular) and extrahepatic with and without jaundice (an exception is the use of ursodeoxycholic acid in intrahepatic cholestasis).

All choleretic preparations containing bile salts, as well as synthetic and vegetable origin, significantly increase the functional load on hepatocytes, reduce their content of detoxifying substances and antioxidants (glutathione, sulfates, etc.). This is especially true of multicomponent formulations of medicinal herbs (cholagogue, laxatives, sedatives), as well as herbal remedies of Chinese and Tibetan origin. When prescribing choleretic drugs, it is necessary to make sure that there is no blockade of bile flow at the stages of "liver cell - intra- and extrahepatic biliary system".

Holenzim is produced in tablets containing dry bile 0.1 g, dried tissue of the pancreas and mucous membrane of the small intestines of slaughter cattle. It is used for chronic diseases of the liver and biliary tract.

Allochol - 1 tablet contains dry animal bile 80 mg, dry garlic extract 40 mg, dry nettle extract 5 mg and activated charcoal 25 mg. It has a choleretic effect, inhibits the processes of fermentation in the intestines.

Liobil - a preparation of lyophilized bovine bile, contains 5 times more bile acids than Cholenzym and Allochol. It is taken 1-3 tablets 3 times a day at the end of meals for 3-4 weeks.

Panzinorm, Festal, Enzistal contain bile extract, improve digestion in the gastrointestinal tract.

Synthetic choleretic agents can also have anti-inflammatory and antimicrobial (hydroxymethylnicotinamide) effects.

Hydroxymethylnicotinamide - a derivative of nicotinic acid amide and formaldehyde. It has a choleretic, anti-inflammatory and antimicrobial effect. It is prescribed 1-2 tablets 3 times a day before meals for 2-3 weeks.

cyclovalon is a derivative of cyclohexanone. It is taken 1 tablet 3-4 times a day before meals for 3-4 weeks.

Osalmid - a derivative of salicylic acid. It has the ability to significantly increase the volume of bile, reduces the viscosity of bile, reduces the level of cholesterol and bilirubin in the blood. It is prescribed 1-2 tablets 3 times a day before meals for 1-2 weeks.

The choleretic effect of plant choleretics is due to the presence in their composition of essential oils, resins, flavones, phytosterols, vitamins and other substances.

Drugs that stimulate breeding bile:

Cholekinetics - drugs that increase the tone of the gallbladder and reduce the tone of the biliary tract (Xylitol, sorbitol, magnesium sulfate, Karlovy Vary salt, berberine, tansy flowers)

Cholespasmolytics (Cholelitics)- drugs that cause relaxation of the tone of the biliary tract (Olimetin)

Cholekinetics irritate the receptors of the mucous membrane of the duodenum, which causes the release of cholecystokinin, which contributes to the contraction of the gallbladder and relaxation of the biliary tract (the sphincter of Oddi relaxes).

Choleretic effect is also possessed by hepatoprotective agents of plant origin from milk thistle, fumes officinalis, celandine, turmeric and artichoke-based. They normalize the motor-evacuation function of the biliary tract and the tone of the sphincter of Oddi (gepabene, hofitol, galstena, hepatofalk-plant, etc.).

Xylitol obtained from cotton husks, produced in the form of tiles of 100-200 g. Used as a 10% solution of 50-100 ml 2-3 times a day 30 minutes before meals for 1-3 months.

Sorbitol formed during the hydrogenation of glucose. It is used in the form of a 10% solution of 50-100 ml 2-3 times 30 minutes before meals for 1-3 months.

Carlsbad salt Take 1 teaspoon per glass of water 30 minutes before meals.

Berberine - alkaloid of barberry leaves. It is taken 1-2 tablets 3 times a day before meals for 3-4 weeks.

tansy flowers taken as an infusion (10 g per 200 ml of water), 1 tablespoon 3 times a day before meals for 2-3 weeks.

Vegetable oils also have a cholekinetic effect: sunflower, olive, sea buckthorn, which are used 1 tablespoon 3 times a day before meals.

Cholespasmolytics- These are drugs that cause a decrease in the tone of the biliary tract. Cholespasmolytic effect can have M-cholinergic blockers, nitroglycerin, methylxanthines. Having an antispasmodic effect, the drugs facilitate the outflow of bile and eliminate hyperkinetic biliary dyskinesia.

Olimetin - capsules containing calamus oil, olive oil, peppermint oil, turpentine oil and purified sulfur. Essential oils, which are part of the drug, have an antispasmodic, choleretic, anti-inflammatory effect. Purified sulfur is a homeopathic component that reduces bile stasis.

Indications: for the prevention of gallstone disease, 2 capsules are used 3 times a day before meals for 1-2 months.

Contraindications: peptic ulcer of the stomach and duodenum, hepatitis.

As statistics show, today almost every second person suffers from liver dysfunction, which often provokes problems with the gallbladder. Correctly selected choleretic drugs in the shortest possible time will help you get rid of the ailments caused by this pathology, as well as reduce the manifestation of painful sensations. But before you buy a particular drug, you need to find out what they are and how they differ, and, of course, make sure that you have no contraindications to taking them.

Admission rules

Immediately note for yourself, if you decide to clean the gallbladder, then the first thing you will need to do is go for an ultrasound scan, because such procedures are strictly contraindicated in the presence of stones. As for the choice of the drug, then, of course, it would be much more reasonable to select it not on your own, but together with the doctor. So you protect yourself from all sorts of side effects and reduce the risk of complications.
In addition, no matter what medication you choose, remember the following rules for taking them:

Such drugs (regardless of the form of release) should be taken 40-50 minutes before eating. They drink plain water;
the daily dose of the drug is recommended to be divided into 3 doses;
keep in mind that such drugs often provoke nausea, so after taking them you will definitely need to eat;
the course of treatment usually lasts from 20 days to 2 months (after 60 days, it is necessary to take a break for at least a month).

Classification

Currently, in pharmacies you can find a huge selection of choleretic agents, which differ not only in their effect on the body, but also in their chemical composition. As for the cost of such medicines, it also varies greatly, so anyone can find something based on their financial capabilities. Here are the groups that such funds are divided into:

Choleretics. Their main function is to increase the production of bile. By their origin, they can be both natural (produced from extracts of plant and animal origin) and synthetic. The action of the second group is slightly different from the first, since synthetic drugs not only increase the amount of bile, but also have anti-inflammatory and antibacterial properties. In addition, they are able to speed up many metabolic processes and improve digestion;
cholekinetics. They increase the tone of the gallbladder and relax its walls, as a result of which bile begins to be released much faster. Here examples the most popular medicines of this group: Sorbitol and Magnesia;
cholespasmolytics. Their main function is to expand the bile excretion pathways and eliminate pain. As a result of this effect, bile is excreted much faster and the body. In addition, the undoubted advantage of such drugs is that they help to overcome spasms;
hydrocholeretics. Reduce the viscosity of bile, as a result of which its amount increases. As it becomes thinner and more watery, this makes it easier for it to enter the intestines and promote faster elimination from the body. The main means of this group are mineral waters.

Keep in mind that it is much wiser and safer to buy such drugs after examining and consulting a doctor. But if you still decide to self-medicate and don’t know what to choose, then here are the most popular remedies: Allohol, Nicodin, Tsikvalon, Hofitol, Papaverine, Besalol and Xylitol.

Choleretics(stimulate the formation of bile). True (increase the secretion of bile and bile acids): containing bile acids: cholenzyme, cholagol, holosas, decholine; synthetic: tsikvalon, oxafenamide.

Plant origin: peppermint, tansy, rosehip. Hydrocholeretics (increase the water component of bile): valerian, sodium salicylate, mineral water.

Indications. Liver dysfunction. Chronic hepatitis, chronic cholecystitis, chronic pancreatitis, flatulence, non-infectious diarrhea.

Contraindications. Choleretics are contraindicated in severe inflammation of the gallbladder and bile ducts and in hepatitis.

Cholekinetics are contraindicated in duodenal and biliary hypertension. Application features. Choleretics are best used in the remission phase and in combination with enzyme preparations, and with hypokinetic dyskinesia it is better to use in combination with cholekinetics.

Holenzim

Indications. As a choleretic and digestive enzyme in diseases and functional disorders of the gastrointestinal tract: chronic hepatitis, chronic cholecystitis, chronic pancreatitis, flatulence, diarrhea of non-infectious origin. To improve the digestion of food in persons with normal function of the gastrointestinal tract in case of nutritional errors (fatty foods, overeating, irregular meals) and chewing disorders, sedentary lifestyle, prolonged immobilization.

Contraindications. Hypersensitivity, acute pancreatitis, exacerbation of chronic pancreatitis, obstructive jaundice.

NLR. Allergic reactions (sneezing, lacrimation, skin redness, skin rash).

Osalmid(oxafenamide)

Pharmacodynamics. Choleretic agent. It has a choleretic and cho-lekinetic effect. It enhances the formation and secretion of bile, relieves spasm of the smooth muscles of the biliary tract and the sphincter of the common bile duct, reduces the content of cholesterol and bilirubin in the blood.

Indications. Chronic cholecystitis, cholangitis, cholelithiasis, cholecystohepatitis, to enhance bile secretion before duodenal sounding.

Contraindications. Acute hepatitis, cirrhosis of the liver, peptic ulcer of the stomach and duodenum, obstructive jaundice.

NLR. Diarrhea, allergic reactions.

18. Clinical and pharmacological characteristics of organic nitrates. Indications and contraindications for use. individual representatives. Features of the use of organic nitrates. Side effects and measures for their prevention. Interaction of organic nitrates with drugs of other groups.

Sample response

For the treatment of coronary artery disease, a group of antianginal drugs is used, which includes:

nitrates and nitrites

β-blockers

calcium channel blockers

disaggregants

anticoagulants

fibrinolytics

lipid-lowering agents.

Clinical pharmacology of nitrates

Nitrates include organic compounds containing groups - O-NO2.

Classification. Taking into account the peculiarities of the chemical structure, nitropreparations are divided into the following groups:

Nitroglycerin and its derivatives

Preparations of isosorbide dinitrate (nitrosorbide, isoket, isomak, cardiquet, cardix)

Preparations of isosorbide-5-mononitrate;

Derivatives of nitrosopeptone (erinite).

Depending on the duration of action, nitrates are divided into short-acting preparations (nitroglycerin) and long-acting preparations (sustak, nitrong, nitromac, trinitrolong, nitrosorbide, erinite, kardiket, kardiks).

Pharmacodynamics and mechanism of action. Nitrates cause peripheral vasodilation and reduce venous tone. The decrease in vascular tone is associated with a direct relaxing effect on vascular smooth muscle and with a central effect on the sympathetic parts of the central nervous system. Nitrates have a negative inotropic effect on cardiomyocytes, which also provides an anti-ischemic effect. Nitrates reduce preload, dilate coronary arteries (mostly small-caliber, especially in places of their spasm), improve collateral blood flow, and very moderately reduce afterload.

Nitrates have antiplatelet and antithrombotic activity. They also have a slight fibrinolytic effect as a result of the release of tissue plasminogen activator from the vascular wall.

Pharmacokinetics nitrates depends on the form of release, on the characteristics of the active substance and is considered in relation to each drug.

Criteria for the effectiveness of treatment- a decrease in the intensity and number of angina attacks per day, increased exercise tolerance, decreased shortness of breath in left ventricular heart failure.

Adverse Drug Reactions (ADRs) nitrates are more often represented by a pressing, bursting headache, which is accompanied by dizziness, tinnitus, flushing of the face. This is usually observed at the beginning of treatment and is associated with vasodilatation of the skin of the face and head, a decrease in blood supply to the brain, an increase in intracranial pressure due to varicose veins. An increase in intracranial pressure can worsen glaucoma. Taking drugs containing menthol (in particular, validol) leads to vasoconstriction and a decrease in headache (Vochal drops). Taking a β-blocker 30 minutes before nitroglycerin also reduces headache.

Long-term use of nitrates can lead to methemoglobinemia. However, the listed NLRs disappear when the dose is reduced or the drug is discontinued. With the appointment of nitrates, a sharp decrease in blood pressure, tachycardia are possible.

Tolerance. Nitrates can become addictive. To prevent tolerance to nitrates, an increase in the dose of drugs is used to restore the effect, the abolition of nitrates, which leads to the restoration of sensitivity after 3-5 days, intermittent intake of nitrates during the day with a break of at least 10-12 hours

Interaction with other drugs. β- Adrenoblockers, verapamil, cordarone enhance the antianginal effect of nitrates, these are rational combinations. On the contrary, under the influence of dihydroergotamine, a decrease in the antianginal effect of nitrates is possible. When combined with novocaine-mid, quinidine or alcohol intake, hypotension and collapse are possible. When taking acetylsalicylic acid, the level of nitroglycerin in plasma increases. Nitrates reduce the pressor effect of adrenomimetic agents.

Contraindications to the appointment of nitrates. TO absolute contraindications include hypersensitivity and allergic reactions, arterial hypotension, hypovolemia, low end-diastolic pressure in the left ventricle in patients with acute myocardial infarction and left ventricular failure, right ventricular myocardial infarction, constrictive pericarditis, cardiac tamponade, severe cerebrovascular insufficiency, hemorrhagic stroke.

Relative contraindications: increased intracranial pressure, angle-closure glaucoma, orthostatic arterial hypotension, hypertrophic cardiomyopathy with outflow tract obstruction, marked stenosis of the aorta or left atrioventricular orifice.

Nitroglycerine- the most famous drug from this group of antianginal drugs

Pharmacokinetics. When taking 0.5 mg under the tongue, the drug is determined in the blood after 15 seconds, the maximum concentration is reached after 5 minutes. Nitroglycerin undergoes a pronounced presystemic elimination: it is rapidly metabolized in the liver by denitration by glutathione reductase, located in the liver and erythrocytes. Bioavailability when taken orally is no more than 10% compared to nitroglycerin taken under the tongue, so it can only be taken orally in the form of special dosage forms that ensure its slow release. As a result of biotransformation, glyceryl dinitrate, which has vasodilatory activity, and mononitrate are formed, which are further degraded to glycerol and eliminated in the urine as glucuronides. Nitroglycerin has a very large volume of distribution. The half-life of nitroglycerin is 4-5 minutes. Action time up to 20 min. Usually, to stop an attack of angina pectoris, nitroglycerin is prescribed 1 tablet under the tongue. If necessary (insufficient efficacy, recurrence of pain), nitroglycerin can be repeated, increasing the dose to 30 tablets per day.

The visceral function of the liver consists in the continuous formation and secretion of bile into the lumen of the duodenum. Part of the bile is stored in the gallbladder and, if necessary (for example, when eating fatty foods), is released into the intestines. In just a day, a person excretes about 1 liter of bile. It plays an important role in the digestion of fats (emulsifies them) and stimulates intestinal motility, promotes the absorption of fat-soluble vitamins.

The formation and secretion of bile can be disturbed in diseases of the liver, gallbladder and bile ducts. The most common causes that impede the flow of bile into the intestines are inflammatory diseases of the gallbladder (cholecystitis), bile ducts (cholangitis), spasms of the bile duct or blockage of its stone. In this case, bile lingers in the gallbladder, liver, is absorbed into the blood and jaundice occurs, and a lack of bile in the intestine leads to indigestion, especially fats. With spasms of the bile duct or blockage with a stone (cholelithiasis), an attack of sharp pain occurs in the region of the right hypochondrium - hepatic colic.

The appointment of choleretic agents helps to cleanse the bile excretory system from mucus, microorganisms, stones, etc. and improves digestion in the intestines. According to the mechanism of action, choleretic agents are divided into two groups: 1) agents that enhance bile production - cholesecretics (choleretics); 2) means that promote the excretion of bile - cholagol.

Facilities cholesecretic groups increase the production of bile by the liver cells. These include bile acid preparations (dehydrocholic acid), Allohol and Cholenzim tablets containing dry bile; herbal preparations - holosas. corn silk. immortelle flowers and others. Recently, synthetic substances have been proposed as cholesecretics: oxafenamide. tsik-valon, nikodin and etc.

Some of them also have anti-inflammatory and antimicrobial effects.

TO cholagol group refer magnesium sulfate. m-anticholinergics and antispasmodics. Magnesium sulfate (20-30% solution) is administered orally or injected through a duodenal probe directly into the duodenum. In this case, a reflex contraction of the gallbladder occurs, relaxation of the sphincter of Oddi and bile from the bladder is released into the intestine. Some have a similar effect

vegetable oils (olive, sunflower) and specially prepared preparations ematin, olimetin, cholagol and etc.

With spasms of the bile ducts or their blockage with a stone, myotropic antispasmodics (papaverine, no-shpa, etc.) or m-anticholinergics (atropine, platifillin, etc.) are prescribed. Eliminating spasm, they facilitate the outflow of bile into the intestines. During an attack of hepatic colic, antispasmodics are prescribed together with analgesics: morphine, iromedol, or omnopon.