For the normal functioning of the organs included in the gastrointestinal tract, all organs and digestive mechanisms are necessary. The violation of the function of one of the organs leads to the disharmony of the work of the entire system. Therefore, it is impossible to treat only an intestinal ulcer and stomach, and you need to take measures to normalize the entire digestion system, use complex pharmacotherapy with means regulating the digestive system.

Pharmacomarketing

Classification and preparations

mechanism of action

Blockers H. 2-gestaiinovy \u200b\u200breceptors and M. 1 -cholypolica Blocked H 2-gestamine receptors (Famotidine, Cimetidine, Ranitidine) and M 1 -HolinoreseGtgore (Pyrenspine) of the gastric mucosa.

Inhibitors H. + -K. + -Atphase (Proton pump Parietal Eczocrivocifyment of the stomach) Block the enzyme H + -k + -at phase, which is responsible for the production of hydrochloric acid (omeprazole).

Antacid - neutralize hydrochloric acid in the stomach (aluminum phosphate (phosphapegel), alumag, carbaldrat).

Enveloping funds Create a film from a colloid that protects sensitive nerve endings from the action of irritant substances and hydrochloric acid, the stomach mucosa.

Binding They cause dehydration or partial coagulation of tissue proteins or wound exudate and form albuminates (which protect the mucous membrane) acts bactericidal on Helicobacter pylory (colloidal (de nol) subcratitis).

Maoprostol , methyluracyl Stimulate regeneration processes.

Antichelicobactert funds Bactericidal act on Helicobacter pylory.

Pharmacological

Blockers N. 2 -gistamine receptors, μ 1 -Holinolitica and inhibitors H. + -K. + -Atphase Reduce the secretion of hydrochloric acid and pepsin.

Pyrenspin Has an antispasmodic effect.

Antacid and enveloping funds endowed with an enveloping and antacid effect (Table 20).

Table 20.

Comparative characteristics of antacid

Binding We are endowed with gastroprotecture, antimicrobial astringent effect (bismuth subcitrate colloid (de nol), sucralfat).

Reparants , combined and other anti-sized means have gastroprotective; Antacid, binder (Vicair, Gastropharm, Liquimiton) SPRISMOLITIC (DROTAVERINE (but-shpa, but-shpa forte, no-cro-me), Liquimiton, planAglucid), anti-inflammatory effects (methyluracyl, Liquoriton, bismuth subcitrate, planaglucid).

Antichelicobacter equipment endowed with antibacterial effect (Table 21).

Table 21.

Pharmacological effects of anti-rich agents

Notes: +++ - a very pronounced effect, ++ - a moderately pronounced effect, + - the presence of effect, 0 - no effect, * - preparations that are neutralized by hydrochloric acid.

Indications for use and interchangeability

1. Ulcerative disease of the stomach and 12-rosewood, hyperacid gastritis (all anti-sized means, except for planaglucide).

2. Reflux Ezophagitis, Zollinger-Ellison syndrome (blockagora H 2 -Gistamine receptors, M 1 -cholinolitics, NMS-ATF-AZA inhibitors, beziclan).

3. Hypotic gastritis, ulcerative ulcer of the stomach and 12-repulitory intestine with normal or reduced acidity (planaglucide, housgrofit).

4. Spasm of peripheral vessels, hepatic and renal colic, cholecystitis, spastic and hypersion dyskinesia gastrointestinal tract, to reduce matters during pregnancy (DROTAVERIN (but-shpa, but-shpa forte, but Cro-I), beziclan).

Side effect

Suppressing the secretion of hydrogen ions and pepsin, blocker H. 2 -Gistamine receptors It is stimulated by the increase in gastrin products G of the cells of the anthral stomach, which can lead to the recurrences of ulcers after the sudden cancellation of the drug.

With rapid administration cimetidine and ranitidine Sometimes heart arrhythmias are observed.

When applied cimetidine Such side effects may be observed: diarrhea, muscle pain, allergic reactions, impotence is possible with prolonged use.

When applied Pyrenspin There are dryness in the mouth, light violations of near view; omeprazole , bismuth subcitrate and antacid - possible dyspeptic phenomena; sukralfat preparations aluminum - Possible constipation.

When applied methyluracila , maoprostol, Metronidazole, Helicozina Possible dyspeptic phenomena, headache, allergic reactions. In treating metronidazol Possible leukopenia.

Contraindications

H. 2 histamine blocators and omeprazop It should not be prescribed to go pregnancy and lactation, patients with impaired liver and kidney function. Cimetidine - Children under 14 years old.

Pyrenspin It should not be used in the first 3 months of pregnancy.

With pronounced renal function aluminum preparations , bismuth subcitrate , sukralfat contraindicated.

Sukralfat. and mizoprostol. Also contraindicated during pregnancy.

Methyluracyl It is impossible to use during acute and chronic forms of leukemia, lymphogranulomatosis, malignant bone marrow diseases.

Planagluocide It should not be used in hyperacid gastritis and ulcerative gastric ulcer with increased acidity.

Metroidazole and heliccin Contraindicated during pregnancy, lactation, bloodstream disorders, active diseases of the CNS.

Heliccin It should not be applied to patients under 18 years of age, as well as for diseases of the gastrointestinal tract with long-term diarrhea or vomiting.

Pharmacobespeck

Antacids Reduce the absorption of iron, NSAIDs, tetracycline, NG receptor blockers.

Antacids It is necessary to take 1.5-2 hours or 1.5-2 hours after the reception of other drugs.

Cimetidine It is impossible to use simultaneously with benzodiazepines, extractors with anticoagulants, propranolol, verapamil, cytostatics and preparations that depress blood formation.

Long reception bismuth subcitrate leads to scar stomach deformations and a 12-rosewoman.

Alumag. We must warm up and keep in your mouth until complete dissolution.

Before meal, ng receptor alocators, Mi-cholinolics and inhibitors N + -K + -ATPhase, carbaldrat, alumag, almagel, binders, plantaglulyucid, bismuth preparations (de nop) are prescribed.

After eating, you need to appoint Simaldrat, Maalox, Reni, Methyluracyl, Vicair.

During the meal - Mizoprostol, methyluracil, all antihelicobacter agents, except bismuth drugs.

Comparative characteristics of drugs

H 2 histamine blocators

Cimetidine It was the first drug of the Blocators H 2 -Gistamine receptors. Its use is accompanied by numerous side effects. In the liver, cimetidine blocks the cytochrome R-450 system, which is necessary for the metabolism of many drugs.

Ranitidine It is more active (4-5 times) inhibitor of the secretion of hydrochloric acid than cimetidine. Combines the inhibitory effect on NG receptors with activation of histamine-methyl-transferase and intensive violation of the synthesis of histamine. No increase in the concentration of gastrin. In contrast to cimetidine, the metabolism of drugs does not affect in the liver. Assigns 2 times a day.

Side effects are weaker than in cimetidine (rarely nausea, blunder, headache, rash).

Famotidin - Specific Blocator H 2 receptors of the third generation of histamine. Taking into account the Ekvimolari dose of Famotidine is 10 times more efficient than Ranitidine and 50 times - cimetidine. Famotidin has a longer action on gastric secretion. Due to this, there is enough one-time reception of 40 mg for the treatment of ulcerative disease every night with duration of therapy 6-8 weeks. To prevent recurrences, 20 mg of Famotidine is prescribed once in the evening.

Mi-Khalinalitika and proton pump inhibitors

Omeprazole Effective with peptic ulcers that cannot be treated with other anti-groomed drugs. In the treatment with the drug, the cellar special selection of doses of elderly people and patients with impaired liver and kidney function.

Pyrenspin - A representative of a new generation of anticholinergic agents, selectively suppresses the secretion by iron stomach hydrochloric acid and pepsinogen, and not the masses of a significant effect on the M-cholinoreceptors of the salivary glands, hearts and other organs. The drug is well tolerated.

antacids

The antacids are treated when the hypersecretion of the gastric glands is not eliminated in cholino and gisgamine-blocks by means.

The antacids are fast, but short-term action belongs carbaldritis (Dihydroxyalum Sodium Carbonate). Interacting with hydrochloric acid of gastric juice, it forms CO 2, which annoys the receptors of the gastric mucosa. Therefore, it is recommended as a means of symptomatic pharmacotherapy.

Aluminum phosphate (phosfalugel) Assign in the form of a colloidal gel is 30 minutes before meals. Has binding properties, effective in ingression. It can be used during pregnancy and lactation.

Alumag. - a balanced preparation with the same amounts of magnesium and aluminum hydroxide (0.2) - to prevent diarrhea and constipation. The gastric juice is quickly neutralized, and due to the formation of the gel in the stomach, it shows an adsorbing, obscaling and analgesic effect. Alumag can be used in therapeutic and prophylactic purposes for ulcerative disease and hyperacid gastritis, as well as episodically - if necessary, get rid of belching, bows and stomach pain. Almost does not produce systemic exposure due to minimal suction in the gastrointestinal tract.

Almagel - Combined antacid, adsorbing, enveloping properties. The presence of D-sorbitol contributes to the enhancement of bortoid and laxative action. The dosage form in the form of gel enhances the duration of the effect and creates conditions for a more equilibrium distribution of the drug on the gastric mucosa.

Nye Acts quickly, and the effect lasts for 60-90 minutes. You can apply several times a day.

binding

Sukralfat. Forms a sticky substance, which is especially identical and firmly covers the ulcerative surface of the stomach and the 12rred intestine at about 6:00.

Bismuth subcitrate colloidal (de Nol.) it has An antacid and citridotector Action is a colloid suspension, which, under the influence of the stomach hydrochloric acid, forms a white precipitate in the form of a polymergicoprotein complex, has a high affinity with glycoproteins of the mucous membrane, especially necrotic tissues of the peptic surface. Where-NOL stimulates the synthesis of PGE 2, which increases the formation of mucus and bicarbonates. It also has an antiseptic effect and bactericidal on Helicobacter Pylori.

Reparants, combined and other means

Mioprostol. - synthetic analog of prostaglandin E 1. Exhibits cytoprotective effects associated with an increase in the formation of mucus in the stomach and an increase in the secretion of the bicarbonate of the gastric mucosa. Showing a direct effect on stomach parietal cells, Mizoprostol suppresses basal, night and stimulated (food, histamine, peniagriam) secretion.

Methyluracyl It has an anti-inflammatory effect, accelerates cell regeneration processes, stimulates leukeopoese.

Vikair Contains bismuth, magnesium carbonate main, sodium hydrocarbonate, cavalry powder AIR and cortex crust.

Gastropharm. - Combined drug. Exhibits analgesic and antacid operation due to the buffer properties of protein contained in large quantities (25-35%) in the preparation. Stimulates regeneration processes in the mucous membrane of the stomach and a 12-rosewoman.

Gastrophit. - Drug collection of 15 medicinal plants, stimulates reparative processes, has a choleretic, laxative, anti-inflammatory effect. It is used to prevent and optimize the treatment of gastritis (including hypoacidal), duodenitis, enterocolitis, preventing the recurrences of the peptic ulcer of the stomach and 12-risen intestine, colitis, cholecystitis, cholangitis, dyskinesia of the urinary tract, for regulating the engine function of the stomach and intestines, the normalization of the chair.

DROTAVERINA (but-shpa, but-shpa forte, but Cro-I) According to pharmacological properties, Papaverin is close, but has a more pronounced and long-term myotropic antispasmodic effect. It also has a vasodilative action. After the intake, inside is quickly absorbed from the gastrointestinal tract. Biodimine - 100%. Does not penetrate the BC. Does not affect the vegetative nervous system.

Bencyclan. Next to the antispasmodic action has a moderate vasodilator. It has a local perscoming activity, causes a moderate sedative effect.

Anticcessobacterni means

Metronidazole. - An antiprotozoic agent, which also has a wide range of antibacterial action and is endowed with high bactericidal activity with respect to Helicobacger. Used in the treatment of ulcerative disease in the scheme of the so-called "triple therapy", where Mainydazole is combined with bismuth and tetracycline drug or amoxicillin. Standard "Triple therapy" is usually carried out for more than two weeks and allows you to achieve the destruction of Helicobacher in 90-95% of cases. Current "Triple therapy" is carried out against the background of receiving antagonists NG of histamine receptors within 2-4 weeks after the end of antibacterial treatment.

Heliccin by itself a combination of amoxicillin and metronidazole. The course of treatment includes a three-time reception of both drugs within 12 days.

Sodium oxyfferbone, retabolil, vitamin preparations A, B, B 2, pp, in 6, B. 12, C, R Also accelerate the healing of ulcers.

list of drugs

Drug therapy of ulcerative ulcer of the stomach and duodenum includes the use of several groups of drugs. The part is prescribed in a tablet form, others - in the form of injections or drip injections. The purpose of the appointment of these groups of drugs will be the return of the disease in the steady remission stage.

If you treat the disease, affecting the gastric and intestinal tract, using exclusively funds of folk or alternative medicine, this will not bring the desired effect, and can worsen the patient's condition. It is known that folk remedies are largely inferior to drug preparations for efficiency. Often in alternative medicine for the treatment of stomach ulcers use hydrogen peroxide.

For drug treatment, it is used not one specific cure for the stomach ulcers (for example, festal), and a number of pharmacological groups. Some are called to affect the cause of the disease, others - on individual pathogenetic links.

A competent combination of drugs will give a sustainable improvement, the doctor should select options.

The attending physician will make a full-fledged examination, recommends which pills to take from the ulcer of the stomach.

In order for drug treatment with a positive result and safely, prescribes such a therapist or a gastroenterologist. Attempts of self-treatment will show the depreciation of the patient. An endoscopic examination is performed periodically, tissue biopsy is taken to the macro-treatment.

A number of drugs can cause aggravation itself. This includes aspirin, paracetamol. With uncontrolled use of aspirin on an empty stomach, the stomach ulcer is formed in the shortest possible time.

Indications and contraindications

Medicinal preparations demonstrate a number of states when applying the specified is categorically not recommended. Consider more.

Medical therapy testimony

1. Pronounced aggravation of the ulcer process.
2. Lack of improvement in prolonged and strict observance of a special anti-rich diet, receiving funds like Festal.
3. Explicit progression of clinical symptoms with a stomach ulcer.
4. If the cause of peptic disease is an infectious agent. Antimicrobial drugs, for example, trichopol under the ulcer of the stomach, are considered to be selection preparations.
5. The emergence of intensive pain syndrome that does not disappear using home recipes. Maalox, Ranitidine or Omez taken overnight will help to take acute pain.
6. In the presence of clinical signs of ulcerative bleeding.
7. When the remission period is reached, the prevention of ulcers by drugs is carried out.

Contraindications to medication treatment

In addition to direct indications, most drugs have contraindications to use.

1. Abundant bleeding in the acute period of the ulcer process.
2. A pronounced allergic reaction or the presence of anamnestic information about allergies to the proposed drug-based drug.
3. Individual intolerance to a separate preparation or component. In the appearance of signs of intolerance, the reception of the drug immediately stop and accepted activated carbon. Often allergic reactions occur on antibiotics - clarithromycin, amoxiclav, Maalox.
4. A number of drugs are contraindicated during pregnancy and breastfeeding.
5. The presence of a number of heavy concomitant diseases - diabetes, renal, liver failure, HIV infection.
6. Recently conducted vaccination against a number of infectious diseases.
7. Childhood.
8. System infections - abscesses, phlegmon, sepsis.

Main groups

Preparations for the treatment of stomach ulcers are divided into several extensive groups. They differ in the mechanism of action and the final effect. In practical gastroenterology, it is customary to use these groups of drugs for treating ulcers.

1. Antibacterial drugs - clarithromycin, amoxiclav with stomach ulcers, trichopol, metronidazole.
2. Antacid substances - reduced acidity of gastric juice, protecting the walls of the stomach - Maalox. Partially this feature has activated carbon and polysorb.
3. Tools blocking the endings of histamine receptors.
4. Tools, the overwhelming functions of the proton pump - omeprazole with a stomach ulcer.
5. Medicinal substances contributing to the regeneration of tissues - for example, actovegin, solkossyril.
6. Medicines that buy inflammation and pain in the stomach - gastroprotectors.
7. Motropic antispasmodics used to eliminate pain syndrome, true analgesic substances.
8. Substances that reduce the secretion in the stomach - cholinoblocators and gangliplocators.
9. Antiwest means.
10. Triple scheme and quad diagram.
11. Other medication drugs - polysorb, activated carbon, hydrogen peroxide, festal.

Antimicrobial means

Antibacterial drugs are aimed at the destruction in the stomach of the microbe Helicobacter pylori - causative agent of ulcerative disease, gastritis. In the overwhelming majority of bacteria is responsible for the development of ulcerative disease.

A diagram is usually assigned to a range of antibiotics. Preparations are prescribed in a tablet form for oral administration and injecting. These include clarithromycin, erythromycin, amoxicillin, amoxiclave, tetracycline.

In addition to these drugs, the dosage scheme includes trichopol preparation with a stomach ulcer. The substance has an antibacterial and antiprotozoic effect.

Antibiotics, for example, clarithromycin are prescribed for ulcer therapy and for prevention. It should be careful to the appointment of antibiotics, it is fraught with the development of dysbacteriosis and diarrhea. The appointment of drugs is carried out under the control of the attending physician with regular surrender of laboratory tests.

Antacid funds

The drug group is used as antiseptic, enveloping and absorbent agents. They protect the gastric mucosa from aggressive factors, remove toxins, reduce the activity of hydrochloric acid and enzymes that cause corrosion of the gastric mucosa and supporting the inflammatory reaction. Means are much preferable than activated carbon or polysorb.

The drug preparations include tablets from the stomach ulcers - gastal or sodium bicarbonate in oral form. In the form of suspension, Phosfalsugel is appointed, Maaloks, Almagel. These funds complement therapeutic schemes for duodenal and stomach ulcers. The complex assign festal to improve the learning processes

Blockers of histamine receptors

A group of substances applies to block excessive secretory activity of glasses in the walls of the stomach. Preparations turn off parietal cells that are responsible for the production of hydrochloric acid and gastric juice enzymes. There is a decrease in the aggressive effect of the gastric juice on the walls of the stomach, the inflammatory process is reduced.

Gistamine receptor blockers numbered several generations. By the first generation belongs to the drug Cimetidine. Now the specified means against ulcers is practically not applied. The second generation of histamine receptor blockers is represented in the pharmaceutical market of Ranitidine, Nizatidine, Famotidin and other tablets for the treatment of peptic processes. When receiving paracetamol and aspirin of the stomach ulcer becomes frequent complication. Therefore, ranitidine is often prescribed with a prophylactic goal.

Gastroprotectors

Means for the treatment of ulcers of the 12-risen and stomach contains in the composition of bismuth and a number of chemicals. Preparations have a pronounced anti-inflammatory effect, reducing pain of duodenal ulcers. It is not recommended to take an anesthetic or paracetamol with a similar purpose, it can only worsen the situation.

Gastroprotectors have a small antimicrobial effect, albeit less than, for example, clarithromycin. A group of medicinal substances is applied not only for therapy of the acute period of the stomach ulcer or intestines, but also with a preventive purpose when the treatment of gastritis is carried out.

Prevention of stomach ulcers with the help of these drugs are carried out during acute or chronic gastritis. The most famous in the group of funds from the ulcer of the stomach and duodenum preparations VENTER, de NOL with a stomach ulcer, sukralfat, solkosryl, misoprostol. The drug de Nol is a means of choice, when with an ulcer of the stomach, treatment with other drugs is ineffective.

Proton pump inhibitors

The famous representative is. The international title of the drug is omeprazole. Another indication for the use of this medicine was the treatment of a 12-rosisse ulcers.

Other groups of drugs

Atropine for ulcerative stomach diseases is used as a spasmolytic agent and to reduce the secretory activity of the stomach parietal cells. The medication together with sodium bicarbonate is part of the Bekarbon tablets for the treatment of stomach ulcers. The effect of medication is similar to Ranitidine. To improve the processes of digestion in a subacute period, enzymes are prescribed - festal, mezim, polysorb, Maalox.

Activated carbon or polysorb is used to treat the ulcer disease of the stomach and removal of toxins from the stomach and intestines in some cases. After receiving coal, a full-fledged course of treatment is carried out with one of the schemes.

Signs of cure becomes the disappearance of clinical symptoms and the macro-treatment, which revealed healing processes.

Basic groups of anti-rich drugs

Since the basic disease is based on the balance between aggression and protection factors, drug treatment should be aimed at eliminating the aggression of gastric juice and stimulating the protection of the mucous membrane.

To reduce the aggressiveness of the gastric juice, preparations of two groups are used: reducing the secretion of hydrochloric acid insulating it.

Antisecretory tools

(I.) Cholinolitical means:

1.M-cholinolics:

· non-selective

Atropine Sulfat.

Hyoscin Hydrobromide (Skopolamine)

Hydrobromid homatropine

Platifillain hydrotatcht

Hyoscyamine

Radobellyn (Beauty Tapes)

Metacinia

Chlorosyl

· selective

Pyrenspine Dihydrochloride (Gastretepin)

Telenzpin

2.m-n-cholinolics

Aproofen \u003d hydrochloride \u003d

Arpelin \u003d hydrochloride \u003d

Safaszzolitin \u003d hydrochloride \u003d (Difazil)

Gastrikson

Ganglefin Hydrochloride (Gangleron)

Fubromeghan \u003d iodmethylate \u003d

(II.) H2-histamine Blockers:

Cimetidine (Belomet, Gistodyl, Tagamet, Cinamet)

Ranitidine (Zantak, Ranisan)

Famotidin (Pepadul, Gastrosidin)

Nizatidin (Axide)

(III.) Proton Pump Inhibitors:

Omeprazole (losek)

Lanzoprazole

Picoprazole

Timoprazole

(Iv.) Synthetic analogues of prostaglandinov:

Mizoprostol (siteotek)

Arbaprostil

Rioprostil

(V.) Other groups:

Protloumid

Acetazolamide (diakarb)

Sandostatin

Dalargin

KVIFENADIN \u003d hydrochloride \u003d (phencarol)

· calcium antagonists

Verapamil Hydrochloride (Isopin, Finoptin)

Nifedipine (Corinthar, Cordafen, Fenigidine)

Antacid drugs

(I.) Suction:

Sodium bicarbonate

Calcium carbonate

(Ii.) Insessant:

Aluminum hydroxide

Almagel (aluminum hydroxide + magnesium oxide)

Phosphhalugel (alfogel) - aluminum phosphate + pectin + agar-agar

Gastal (aluminum hydroxide + magnesium carbonate)

Sukral Fat (VENTER)

Sodium aluminum dihydroxycarbonate (alugastrine)

(II.) Mixed:

Vicalin
Vikair

Means that enhance the protection of the mucous

(I.) Preparations of colloid bismuth:

Bismuth subcitrate colloidal (de nol, tribimol)

(II.) Opioid peptides:

Dalargin

(III.) Synthetic analogues of prostaglandins:

Mizoprostol (siteotek)

(Iv.) Other groups:

Carbenoksolon

Sukral Fat.

Now for each group:

M-cholinoreceptor blockers

Indiscriminate antagonists

Atropine Sulfat. It causes the blockade of M-cholinoreceptors, makes them insensitive to acetylcholine formed in the end of the postganglyonary parasympathetic (cholinergic) nerves. Atropine reduces the secretion of saliva, gastric, bronchial, sweat glands, pancreas, causes tachycardia and reduces the tone of smooth muscle organs. T1 / 2 Atropine is from 1 to 1.5 hours, so frequent (every 2-3 hours) is required.

Atropine It is shown at ulcerative duel of duodenal, pylorosphazm, cholecystitis, bile sickness, intestinal spa and urinary tract, bronchospasm.

Atropin doses are individual. It is usually used in the form of a tablet or powder of 0.0005 g 1-2 times a day, or 5-10 drops of 0.1% solution before eating 2-3 times a day, or 0.5-1.0 ml 0.1% of the solution subcutaneously, intramuscularly, less often intravenously 2-3 times a day during the exacerbation of the duodenal ulceneous disease and pronounced pain syndrome.

The drug cannot be prescribed when glauer.

Close in its properties to Atropin Platifillain, which is often used as a spasmolytic agent for pharmacotherapy in the form of tablets of 5 mg or 0.2% solution.

Metacin Refers to M-cholinoblockers, an atropine is inferior in efficiency. It is shown in ulcerative ulcer of the stomach and duodenum, spasms smooth intestinal musculatory.

It is used by 0.2 mg 1-3 times a day or 0.5-1.0 ml of 0.1% of the solution 2 times a day. Metacin is contraindicated in glaucoma.

Chlorosyl It is a domestic drug that exceeds the effect of atropine through an anesthetic effect and the percentage of healing of an ulcer. His doses are: 1 ml 0.1% 2 times a day subcutaneously 6-8 days, then? In Tablets 0.002 g 2 tablets (0.004) 3-4 times 2-3 weeks. In combination with antacids, the drug is more efficient.

Propantelin Bromide (Slytin) refers to the cholinolics of prolonged action. Saltin is used for 15 mg 3 times a day before meals.

Propantelin Bromide is prescribed with ulcerative disease, acute pancreatitis, during endoscopy.

The drug is contraindicated in glaucoma, obstructive diseases of the gastrointestinal tract and urinary tract, heavy nonspecific ulcerative colitis, reflux-esophagite and diaphragmal hernia, myasthenia.

M-cholinoreceptor blockers (atropine group) Although have a dose-dependent antisecretory effect, but in conventional therapeutic doses, basal secretion is capable of only 30-50% and, in addition, reduce pancreatic secretion, which makes them irrational appointments with ulcer monotherapy. In addition, due to the lack of selectivity, they often cause systemic side effects (dry mouth, accommodation violations, tachycardia, urination disorders). It should be remembered that M-cholinoreceptor blockers normalize the motor-evacuation function of the stomach and duodenum, with which they are probably associated with their analgesic effect. An indication of their use is pronounced, especially night, pain. They can also be used in Zolinger-Ellison syndrome, in combination with histamine-receptor Blochetors, more pronounced braking of the secretory function of the stomach than using single H 2-receptor-receptor plants.

Election antagonists M-cholinoreceptors

Selective M 1 -Holinoblocator has significant advantages over atropine - Pyrenspine (gastrocepin). It has a selective effect on m 2-receptors of parietal cells, blocking the secretion of hydrochloric acid, and does not cause side effects. It is weaker than atropine, suppresses the secretion of hydrochloric acid (basal and stimulated). The effectiveness of suppressing the basal secretion of pyrenspine is 50-60%, which is not enough in pronounced hyperacidity. Pyrenspine does not block the products of protective mucus and enzymes, improves microcirculation into the gastric mucosa and duodenum, suppresses intragastric proteolysis, i.e. It acts as a cytoprotector and does not have those side effects as atropine (with the exception of dryness in the mouth, chairs in some cases).

By the chemical structure, Gastretepin is a tricyclic compound of benzodiazepine. From typical tricyclic benzodiazepines with neurotropic activity, it differs relatively low lipophilicity, good hydrophilicity, which increases the polarity of the molecule and determines the features of its pharmacokinetics: relatively low bioavailability, insignificant penetration through the hematorecephalic barrier, Metabolism in the liver. It is allocated mainly with bile. Gastrocepin does not oppress the cytochrome system P-450, which allows it to be used in chronic liver lesions. It can be used in patients with glaucoma, prostate adenoma.

The interval between therapeutic and toxic doses is wide (side effects appear in the form of vestibular disorders when peaking a concentration of 200 mg / ml and higher).

In patients with peptic ulcer and Zollinger-Ellison syndrome, the drug is first better to introduce intramuscularly or intravenously at 10 mg 2 times (in the morning, in the evening) 7-8 days and 1 tablet for lunch; Then 1 tablet 2 times a day.

If the drug is appointed in tablets, then 1-2 tablets in the morning and 2 tablets in the evening, and the sickness of pain - 1 tablet 2 times before the eterno 4-5 weeks. Sometimes they use the drug and for a longer time - 3-4 months.

Protonic pump inhibitors

Omeprazole Blocks up to 100% secretion of hydrochloric acid, and due to the irreversibility of interaction with the enzyme, the effect is stored for several days. Such pronounced ahlorogyrhydrium may, with long-term reception of the drug, lead to hypertrophy and hyperplasia of cells producing gastrin, which contributes to the formation of the tumor of the stomach. This limits the duration of the destination of omeprazole to 2-4 weeks and makes it impossible to use it during the remission.

Indications for the appointment of omeprazole:ulcers with Zollinger-Ellison syndrome, stomach and duodenal ulcers.

Comparison of the main groups of anti-rich drugs, the identification of their shortcomings and advantages make it possible to substantiate the choice of antihistamine H 2-receptor blockers as leading pathogenetic agents.

Treatment schemes containing omeprazole

Preparations -% Eradication

2-component schemes:

omeprazole + amoxicillin - 40-70

omeprazole + clarithromycin - 60-75

3 component schemes:

omeprazole + amoxicillin + + metronidazole - 88-91

omeprazole + amoxicillin + + clarithromycin - 85-90

omeprazole + clarithromycin + + metronidazole - 86

omeprazole + Clarithromycin + + Tinidazole - 87-95

It was noted that omeprazole, although it does not have antibacterial properties, but is capable of decreasing the number of bacteria (especially vegetative forms) in the antral stomach department. At the same time in the body and the day of the stomach, their number may increase.

Such an omeprazole effect is associated with its influence on the pH of the medium: a significant increase in its anthral department leads to a violation of ammonium metabolism produced by a helicobacter, which leads to the death of the microorganism. In the acidoproducting zone of the pH, the pH cannot be increased dramatically, there are favorable conditions for the persistence of Helicobacter.

In the phenomenon of its "movement" from the anthral department in the body and the bottom of the stomach, the role of omeprazole is great. In the foundal departure, bacteria are moving to vegetative forms and begin to multiply, which makes it possible to effect antibiotics. In addition, omeprazole, changing the pH of the stomach to 5.0 and higher, increases the bactericidal properties of these drugs.

De NOL requires an acidic environment for dissolution, and the effect of antibiotics in such a medium is reduced. All this forced to replace in antichhelicobacter combined therapy De Nol omeprazole.

Gistamine Blockers H 2 -receptors
Histamine (H) Receptors were open in 1937, after this, the first antihistamines appeared. They rendered an anti-allergic effect, but did not reduce the gastric secretion. Only in 1972 two types of n-receptors were revealed - H 1 and H 2 and the first H 2-block was created - Cimetidine, and then Ranitidine, Famotidin other.

The main differences between generations H 2-blocks

The 1st generation includes cimetidine, 2-MU - Ranitidine, to the 3rd - Famotidine, Nizatidin, Roxatidine.

Ranitidine and Famotidine have greater selectivity than cimetidine.

When used in high doses, cimetidine can influence on H 1 -receptors, since the selectivity is the phenomenon relative and dose-dependent.

Famotidine is 40 times more powerful than cimetidine and 8th anniotidine. In the clinic, the differences in the strength of the action are determined by the data on the equivalence of doses of different H 2-blocks acting on the decrease in the secretion of hydrochloric acid.

The binding force with receptors is determined by the duration of action. The drug that is strongly binding to the receptor, slowly dissociates, which causes the continuous effect.

Famotidine is mostly affected by basal secretion. Research intragastric pH shows that an effective decrease in basal secretion is maintained after taking cimetidine for 2-5 hours, ranitidine - 7-8 hours, Famotidine -10 and even 12 hours.

All H 2-blocks belong to hydrophilic medicinal substances. Cimetidine is the least hydrophilic and moderately lipophil among all H 2-blocks. This determines its ability to penetrate into different organs and, affecting the Localized H 2-receptors localized in them, cause side effects. Ranitidine and Famotidine High Hydrofils and have a preferential effect on H 2 receptors of parietal cells.

H 2-blocks differ in portability, especially in cases of long-term use.

Ranitidine and Famotidin due to a changed chemical structure (cimetidine contains a imidazole group, the Ranitidine - Furana, Famotidine - thiazole group) gives fewer side effects than cimetidine and do not affect the activity of hepatic metabolizing enzymes.

Basic action These drugs are aimed at reducing the aggressiveness of the gastric juice due to the suppression of the secretion of hydrochloric acid and pepsin. Mainly reduced basal and night secretion of acid. In addition, H 2-blocks have additional operational mechanisms:

* activate the bloodstream in the gastric mucosa

* Enhance the synthesis of bicarbonates

* Enhance the synthesis of prostaglandins in the gastric mucosa

* restore the cells of the epithelium

* Perhaps stimulates the products of mucus (in particular, ranitidine) Thus, H 2-blocks can enhance the protective properties of the mucous membrane, which makes them versatile preparations and allows for the monotherapy of ulcerative disease.

Famotidine is a powerful antisecretory drug, causing dose-dependent suppression of acid products. It reduces night secretion by more than 80%, and this is the optimal condition for the scarring of peptic ulcers. The greatest effect of Famotidin gives 20-40 mg doses - reduced night secretionHCl is 92 and 94%, respectively.

H 2-blocks cause a number of side effects, various development mechanisms. They may be associated with the relative selectivity of the action on histamine receptors and the effects of N 2-receptors localized in different organs; with impaired metabolism androgen; with antisecretoric effect and influence on the gastrointestinal tract; with hepatic metabolism.

Different drugs of this group determine side effects with different frequency. When using cimetidine, it is 3.2%, ranitidine - 2.7%, Famotidine - 1.3%.

Famotidin has a side effect mainly on the gastrointestinal tract - develop or diarrhea, or (less often) constipation.

Diarrhea arising from the reception of Famotidine is the result of antisecretory action. Reducing HCI products increases pH in the stomach, which prevents the transformation of pepsinogen in pepsin, involved in the splitting of food proteins. In addition, the decrease in the products of the gastric juice, as well as the blockade of H2-receptors of the pancreas become the reason for reducing the release of digestive enzymes of the pancreas and bile. All this leads to a violation of the digestive process and the development of diarrhea.

However, the frequency of these complications is small - 0.03-0.4% and usually does not require cessation of treatment. Such effects are characteristic of all H 2-blocks. They are dose-dependent and can weaken them, reducing the dose of the drug.

H 2-blocks can cause hematological side effects associated with idiosynczese. They usually arise in the first 30 days of treatment, they are reversible and the most often manifested by thrombocytopenia and granulocyteneenia. When using Famotidine, they are observed in 0.06-0.32% of patients.

Violation of the activities of the endocrine system is due to the ability of H 2-blocks to displace endogenous testosterone from receptors, as well as drug preparations containing this hormone, leading to sexual disorders (impotence, gynecomastia). These side effects are also dose-dependent. Famotidine causes them much less frequently than Cimetidine and Ranitidine.

H 2-blocks can disrupt the function of the cardiovascular system, blocking H 2 myocardial receptors, vascular wall. In suffering from cardiovascular diseases and older patients, they are able to cause arrhythmia, strengthen heart failure, provoke coronarrospasm. Hypotension is sometimes observed with intravenous administration of cimetidine.

Hepatotoxicity H 2-blocks manifested by hyperransaminsemia, hepatitis, violation of cytochrome P450 activity, is associated with metabolism H 2-blocks in the liver, which is most characteristic of cimetidine. When using Famotidine due to its minor metabolism, the frequency of such complications is minimal.

Neurological side effects - the result of penetration of H 2-blocks through the BCB. The degree of penetration into the central nervous system of cimetidine is 0.24, ranitidine - 0.17, Famotidine -0.12%. Similar adverse reactions arise in the elderly and with violations of the liver and kidney function. The frequency is 0.05-0.1%.

H 2-blocks may worsen the course of bronchological diseases, leading to bronchospasm. Allergic reactions are possible by the type of urticaria. The frequency of the appearance of the skin rash after receiving Famotidine is 0.1-0.2%.

The side effect, which is peculiar to all H 2-blocks, regardless of their pharmacokinetic properties - the development of cancellation syndrome. Therefore, the dose is recommended to reduce gradually.

Pharmacodynamic interactions H 2-blocks with other antisecretory preparations (for example, cholinoblockers) can enhance therapeutic efficacy. The combination of H 2-blocks with drugs acting on Helicobacter (de nolnom, metronidazole) accelerates healing of peptic ulcers.

Applied at:

1. A duodenal ulcer disease (recurrence treatment and prevention)

2. Ulcerativeness of the stomach (treatment and prevention of relapses)

3. Symptomatic ulcers: stress ulcers, yathedral ulcers, ulcer Zolinger Ellison (treatment and prevention)

4. Reflux Ezophagitis (Treatment)

Means that have a protective effect on the mucous membrane of the stomach and duodenum (Gastrocytoprotectors)

This group includes drugs that contribute to the preservation of the integrity of the mucous barrier and preventing the occurrence of ulcers. They do not affect the production of hydrochloric acid and pepsin.

The mucosal barrier includes at least four cytoschloric factor:

• mucous layer supporting the pH gradient between the cavity of the stomach and the cell surface, which preventsuu diffusion of hydrogen ions and pepsin, providing their unidirectional movement from the cells of the mucous membrane to the cavity of the stomach;
• secretion of bicarbonate by epithelial cells supporting the neutral pH value on the surface of mukoid cells;
• would be a jet cell regeneration that preserves the integrity of the mucous barrier;
• adequate blood flow in the mucous membrane, necessary to maintain the production of mucus and bicarbonate and for intracellular regeneration.

The cytoprotection mechanism is to prevent damage to the microShosuds, in protecting the zone of media profiling cells, increasing protective cellular mechanisms, secretion of bicarbonate and mucosia, stimulation of synthesis and inhibition of inactivation of gastric prostaglandins.

Sukral Fat. (VENTER) - the main aluminum salt of sucrose octasulfate. It comes into reacting with proteins of necrotic tissue of ulcers and forms a protective film on the site defect, which prevents further destruction of tissues with hydrochloric acid, pepsin and bile acids. Sukralfat locally neutralizes gastric juice, without affecting the pH of the entire stomach, slows the effect of pepsin and absorbs bile acids.

Pepsin activity is inhibited by 30%. At the site of ulceration, the drug is fixed for 6 hours. Systemic effect does not stand up 90% with feces.

The drug is absorbed by 3-5% of the administered dose, and more than 90% unchanged is released from the feces. At the site of the ulcers, the drug is fixed for 6 hours. By efficiency, the drug is comparable with cimetidine and carbenoxolone.

It is used for peptic ulcer of the stomach and duodenum and mostly "fresh" surface lesions, reflux-esophagite.

De Nol. (Colloid subcitrate of bismuth) refers to the VENTER, to gastrocytoprotectors with bactericidal properties, which are manifested in antihelicobacter activity: monotherapy De NNOL leads in 30% of cases to the destruction of these bacteria. De Nol enters all treatment schemes of helicobacteriosis; pH of the solution of the drug - about 10, with a decrease to 4-4,5 Or lower due to the effects of hydrochloric acid, the insoluble oxychloride and bismuth citrate occurs. The maximum precipitation is observed at pH 2.5-3.5, and the bottom of the ulcers is covered with a white hoist. With endoscopic observation, it is saved for several hours.

De Nol forms with mucus in the stomach complex, which is more effective against hydrogen ions, contributes to an increase in the level of prostaglandins, changes the qualitative characteristics of the gastric mucus, strengthening the barrier against hydrochloric acid. It has been discovered its ability to reduce the level of pepsin. The oppression of activity is especially effective at pH \u003d 1.6, characteristic of the aggravation of ulcerative disease. At this level, the drug de Nol is deposited completely.

The combination of de-nol with metroindazole or ampicillin (amoxicillin) leads to an increase in efficiency up to 80-90%.

The bismuth subcitrate is not absorbed into the blood, although its long-term use may lead to the cleavage of a small amount of bismuth and its suction. At the concentration of the drug in the blood plasma, reversible encephalopathy may occur, so long (more than 2 months) cannot be applied to it. The bismuth subcitrate is distinguished with feces, which is why the color of the feces becomes black. De-NOL is used for the stomach and duodenal ulcer and during gastroduodenites. The liquid form of de-nolas is used to treat gastritis, eosophagitis.

Prescribe on a tablet (capsule) 30 minutes before meals and at night4 times a dayIn the overwhelming majority of cases within 4 weeks there is a scarring of ulcers. . When detecting helicobacter is used in combination with antibacterial drugs.

Side effects Raren: nausea, vomiting, allergic reactions. With caution should be prescribed by the patients of senile age.

It is characteristic that such drugs like de nol and sucralfat do not lead to the scarring of the ulcers caused by the reception of the NSAIDs. Alternative to H 2-blocks in the treatment of ulcers caused by NSAIDs - Prostaglandins.

Synthetic analogues of prostaglandins

Universal stimulants protective factors. Among them, Mizoprostol occupies the main place. His most clearly, its effectiveness is proved in ulcers that have arisen in connection with the reception of the NSAID. Take 200 mg 4 times a day.

Advantages in front of the histamine H 2-receptors and omeprazole in the treatment of ulcerative disease, Mizoprostol has no.

By-effect: Diarrhea may appear during the treatment.

Anti-sized drugs.

According to modern ideas, the leading link of the pathogenesis of ulcerative disease is a violation of equilibrium between the factors of the acid-peptic aggression of gastric content and elements of the protection of the stomach mucosa.

Aggressive ulcerative formation includes:

a) hypersection of hydrochloric acid due to an increase in the mass of the shepherd cells, gastrogen hyperfunctions, nervous and humoral regulation;

b) improving the production of pepsinogen and pepsin;

c) violation of the motor function of the stomach and duodenum (delay or, on the contrary, acceleration of the evacuation from the stomach).

In recent years, the most important aggressive factor in ulcerative formation is recognized as a pyloric Helicobacter ( Helicobacter pylori.) - microorganism capable of sealing the mucous membrane of the stomach and metaplazized mucous membrane of the duodenum.

To weaken the protective properties of the gastric mucosa and duodenum can be conducted various factors:

a) decrease in the production and / or violation of the qualitative composition of the gastric mucus (for example, in alcohol abuse);

b) reducing the secretion of bicarbonates (in chronic pancreatitis);

c) reducing the regenerator activity of epithelial cells;

d) deterioration in the blood supply of the gastric mucosa;

e) reducing the content of prostaglandins in the wall of the stomach (for example, when taking non-steroidal anti-inflammatory drugs).

The diversity of various pathogenetic factors of ulcerative disease led to the appearance of a large number of drugs, selectively impact, as intended initially, for certain pathogenetic mechanisms of the disease.

The ulcers of the stomach and duodenal guts are 100% of cases, if during the day it is possible to maintain the level of intragastric pH\u003e 3 around 18 hours. Therefore, the list of anti-sized drugs used in the treatment of exacerbations of the disease to relieve clinical symptoms and achieving the scarring of a ulcer defect has decreased and currently includes 4 groups of drugs: antacids, selective cholinolities, histamine-receptor blockers, proton pump inhibitors. A separate "niche" occupied cytoprotectors, bismuth, antibiotics and some other drugs, for the application of which special testimony formulated.

Clinical classification of modern
Anti-sized drugs

Taking into account that the severity of the antisecretory effect of drugs used for the purpose base therapy Nazis Diseases (that is, for the treatment of exacerbations of diseases and supportive admission), non-etinakov, they are from the standpoint of practical use - can be divided into preparations of the first and second stage. In the first group it is advisable to include antacid and selective M-cholinolities, and inhibitors of the proton pump inhibitors.

An independent group is preparations used by special testimony: cytoprotective agents (sukralphal, synthetic analogs of prostaglandins), prescribed, mainly for the treatment and prevention of lesions of the gastric mucosa and duodenal integration caused by intracogenic drugs; drugs that normalize the motor function of the stomach and duodenum (spasmolytic, prokineetics); Antigelicobachantics (antibiotics, bismuth preparations)

Classification of anti-sized drugs

Preparations of basic therapy of the 1st stage are capable of maintaining the level of intragastric pH at the level\u003e 3 within 24 hours, only a relatively short time - up to 8-10 hours. Therefore, it is advisable to appoint them with a favorable course of ulcerative disease: rare and short exacerbations, small sizes of a peptic defect, a moderate increase in acid products, the absence of complications.

Preparations of basic therapy of the 2nd stage maintain the level of intragastric pH significantly longer time - up to 12-18 hours. They are shown, first of all, with frequent and long exacerbations of the disease, large (over 2 cm in diameter) sizes of a ulcerative defect, expressed hypersection of hydrochloric acid, the presence of complications (including anamnestic) concomitant erosive esophagite.