Has astringent and anti-inflammatory properties. Therapeutic effect. Inorganic astringent

By astringent action we mean the reversible reaction of drugs of this group with proteins of tissues and mucous membranes, as a result of which a temporary dense protective film is formed on their surface. Both internally and externally, this film (seal) protects affected (inflamed) tissues from microorganisms and poisons, helps stop bleeding, heal wounds, burns, cracks, reduces pain and inflammation and protects receptors from irritation .

Astringents are usually divided into two groups:

• astringents of organic nature;
• astringents of inorganic nature.

The first group of astringents includes plant preparations, for example, oak bark, blueberries, bird cherry, cinquefoil rhizome, St. John's wort, etc. The active ingredients of these plants are the special chemicals they contain - tanaglycosides. It is they who, when reacting with the proteins of the mucous membranes, cause their deposition and form a protective film. So, the mechanism of action of astringents can be presented as follows:

Tanaglycosides + Protein<-» Плотная защитная (временная) пленка.

Infusions and decoctions are prepared from these plants, which are used as gargles for bleeding from the gums and for sore throats; in the form of lotions for healing wounds, ulcers, burns; orally for peptic ulcers, intestinal disorders, inflammation (colitis, enterocolitis), etc.

The second group of astringents includes salts of heavy metals, such as bismuth, zinc, silver, etc., which, in addition to the astringent, have a cauterizing and antimicrobial effect, but this depends on the concentration of the drug.

The active principle of this group of drugs is a metal cation, which, when reacting with proteins of mucous membranes and affected tissues, forms a dense protective film - albuminate.

Cation + Protein<->Thick protective film (albuminate).

Inorganic astringents are often used in the form of ointments, suppositories, and powders as antimicrobial, wound-healing, and hemostatic agents. Less commonly, their solutions are used as part of solid dosage forms (tablets) for the treatment of ulcers and inflammatory diseases of the gastrointestinal tract.

The drugs in this group are basic bismuth nitrate, xeroform, dermatol, zinc oxide, silver nitrate, etc.

TANIN (Taninum) is a light brown powder, highly soluble in water. Use a 1-2% aqueous solution, 5-10% water-glycerin solution for rinsing or lubricating for inflammatory diseases of the oral cavity, pharynx, larynx and pharynx; 3, 5, 10% solutions and ointments are for the treatment of wounds, burns and cracks, and 0.5-2% solutions are used for gastric lavage in case of poisoning with salts of heavy metals and alkaloids, with which the drug forms an insoluble compound and precipitates.

Release form: powder.

OAK BARK (Cortex Quercus) in the form of a decoction (1: 10) is used for rinsing for gingivitis, stomatitis, bleeding gums and as a 20% decoction for lotions in the treatment of burns.

BLUEBERRY FRUITS (Fructus Myrthilli) are used in children's practice as an astringent for intestinal disorders in the form of infusion or jelly.

BISMUTH NITRATE (Bismuthi subnitras) as an astringent and weak antiseptic is prescribed orally for inflammatory diseases of the gastrointestinal tract (colitis, enteritis), and for peptic ulcers of the stomach and duodenum. Prescribed in powders and tablets of 0.25 and 0.5 g per dose up to 3 times a day; externally in the form of powder and 5 and 10% ointment for the treatment of dermatitis, eczema, etc. Bismuth nitrate is the main component of complex Vikalin tablets used to treat stomach ulcers.

The drug is produced in tablets of 0.25 and 0.5 g and in the form of an ointment of 10%.

Bismuth preparations are Xeroform, Dermatol and De-Nol.

Xeroformium - yellow powder with a characteristic odor, contains more than 50% bismuth oxide. Used as an astringent, drying and antiseptic agent in the form of powder, 3% eye ointment and 10% ointment for the treatment of skin lesions. Xeroform is part of the known liniment according to A.V. Vishnevsky and a number of other drugs.

Release form: powder.

DERMATOL (Dermatolum) - an analogue of Xeroform. Used in the form of powder, 10% ointment and as part of suppositories of 0.2 g.

Available in the form of powder, 10% ointment and suppositories of 0.2 g.

DE-NOL (De-Nol) - colloidal bismuth subcitrate, has an astringent, enveloping, antacid and cytoprotective (protective) effect on the cells of the gastric and intestinal mucosa. When taken orally, it forms a colloidal mass, which, evenly distributed over the surface of the gastric mucosa, protects it from destruction. The drug is indicated for peptic ulcers of the stomach and duodenum.

Prescribe De-Nol 1-2 tablets 4 times a day 30-60 minutes before meals.

The drug is produced in tablets of 0.12 g.

Pharmacology: lecture notes Valeria Nikolaevna Malevannaya

3. Astringents

3. Astringents

Astringents, when applied to the mucous membranes, cause coagulation of proteins, the resulting film protects the mucous membrane from irritating factors, pain is reduced and inflammatory processes are weakened.

This effect is exerted by many substances of plant origin, as well as weak solutions of salts of some metals.

Tannin(T a n i n u m).

Gallodinic acid. Has an astringent and anti-inflammatory effect.

Application: stomatitis, gingivitis, pharyngitis (1–2% solution for rinsing (3–5 times a day), externally for burns, ulcers, cracks, bedsores (3–10% solutions and ointments), poisoning with alkaloids, heavy salts metals (0.5% aqueous solution for gastric lavage).

Release form: powder.

Tansal(Tansal).

Composition: tanalbine – 0.3 g, phenyl salicylate – 0.3 g. Astringent and disinfectant.

Application: acute and subacute enteritis and colitis (1 tablet 3-4 times a day).

Release form: tablets No. 6.

St. John's wort herb(Herba Hyperici).

Contains tannins such as catechins, hyperoside, azulene, essential oil and other substances.

Application: as an astringent and antiseptic for colitis in the form of a decoction (10.0-200.0 g) 0.3 cups 3 times a day 30 minutes before meals, for rinsing the mouth in the form of a tincture (30–40 drops per glass of water) .

Release form: cut grass 100.0 g each, briquettes 75 g each, tincture ( Tinctura Hyperici) in bottles of 25 ml.

Oak bark(Cortex Quecus).

Application: as an astringent in the form of an aqueous decoction (1: 10) for rinsing with gingivitis, stomatitis and other inflammatory processes in the oral cavity, pharynx, larynx, externally for the treatment of burns (20% solution).

In medicinal practice, infusions and decoctions of plants such as: serpentine rhizome ( Rhizoma Bistortae), rhizome and burnet root ( Rhizoma cum radicibus Sanguisorbae), alder fruit ( Fructus Alni), sage leaves ( Folium Salviae), the drug from it is salvin ( Salvinum), chamomile flowers ( Flores Chamomillae), chamomile preparation; romazulan ( Romasulon), blueberries ( Baccae Murtilli), bird cherry fruits ( Baccae Pruni racemosae), cinquefoil rhizome ( Rhizoma Tormentillae), succession grass ( Herba Bidentis).

Metal salts. Bismuth preparations.

Bismuth nitrate basic(Bismuthi subnitras).

Application: as an astringent, weak antiseptic, fixative for gastrointestinal diseases, 0.25-1 g is prescribed orally (for children 0.1-0.5 g) per dose 4-6 times a day, 15-30 minutes before meals.

Side effects: with long-term use in large doses, methemoglobinemia is possible.

Release form: powder, which is part of the Vikair tablets, used for stomach and duodenal ulcers, and the Neo-Anuzol suppositories, which are used for hemorrhoids.

Xeroform(Xeroformium).

Used externally as an astringent, drying and antiseptic agent in powders, powders, ointments (3-10%). Included in balsamic liniment (Vishnevsky ointment)

Dermatol(Dermatolum).

Synonym: Bismuthi subgallas. Used externally as an astringent, antiseptic and drying agent for inflammatory diseases of the skin and mucous membranes in the form of powders, ointments, suppositories.

Release form: powder.

Lead preparations: lead acetate ( Plumbi acetas) – lead lotion – 0.25% solution.

Aluminum preparations: Alum ( Alumen). Used as an astringent and hemostatic agent (0.5–1% solution).

Burnt alum(Alumen ustum).

As an astringent and drying agent in the form of a powder included in the powder.

LECTURE No. 11. Medicines acting on peripheral neurotransmitter systems. Drugs acting on peripheral cholinergic processes 1. Drugs acting primarily on peripheral neurotransmitter systems B

LECTURE No. 15. Drugs acting in the area of ​​sensory nerve endings. Drugs that reduce the sensitivity of nerve endings 1. Local anesthetics Drugs in this group selectively block the process of transmission of excitation in the efferent nerves and

4. Enveloping agents and adsorbing agents Enveloping agents. Enveloping agents form colloidal solutions in water - mucus, covering the mucous membranes and protecting them from the action of irritating substances. They are used to treat inflammatory diseases

2. Products containing essential oils. Bitterness. Products containing ammonia Products containing essential oils. Eucalyptus leaf (Folium Eucalypti). Application: decoction and infusion of eucalyptus as an antiseptic for rinsing and inhalation for ENT diseases, as well as for treatment

46. ​​Astringents When applied to mucous membranes, astringents cause coagulation of proteins, the resulting film protects the mucous membrane from irritating factors, pain is reduced and inflammatory processes are weakened. This effect is exerted

47. Enveloping agents and adsorbent agents Enveloping agents. Enveloping agents form colloidal solutions in water - mucus, covering the mucous membranes and protecting them from the action of irritating substances. They are used for treatment

48. Products containing essential oils. Bitterness. Products containing ammonia Products containing essential oils. Eucalyptus leaf (Folium Eucalypti). Application: decoction and infusion of eucalyptus as an antiseptic for rinsing and inhalation for ENT diseases, as well as for treatment

MOISTURIZING AND Astringent EYE PREPARATIONS Used for dry eye syndrome. Substances that increase viscosity include cellulose derivatives (0.5–0.1% polyvinyl glycol, polyvinylporrolidone, derivatives of 0.9% polyacrylic acid. Substitutes

X. Household products X. Household products (supporting items). Saucer. Medicines are prepared in it. Bottles. Some “compositions” and other medicines are prepared and preserved in them. Ordinary water is used for preparing decoctions, infusions,

Astringent and tanning plants If your hand skin is of the oily type and you are tired of fighting it, using various kinds of cosmetics to cleanse the skin of the abundant secretion of fatty lubricant, which clogs the pores, causing painful acne to appear

COUGH DRUGS When coughing, the following expectorants are used to thin and remove mucus better. Breast elixir. The drugs are taken orally; children under 1 year of age are prescribed 1–2 drops 2–3 times a day, children over one year of age are prescribed the number of drops per dose,

General strengthening agents. Means that regulate metabolism - Take a pinch of thorn flowers and dandelion inflorescences, pour 1 glass of boiling water, let it brew, strain, add 1 tbsp. a spoonful of apple cider vinegar. Drink warm before bed. - For a restorative bath

Hand products For cracked skin Boil 5 potatoes, grind into a paste, add 5 tbsp. l. milk. Apply the warm paste to the skin and hold for 10 minutes, giving an energetic massage. Wash your hands with cold water and apply cream. You can simply immerse your hands in this paste until

Astringents- these are drugs that, when applied to the skin, mucous membranes or wound surface, cause compaction of colloids of extracellular fluid, mucus, exudate, and cell surfaces. In this case, a film is formed that protects the endings of the sensory nerves from irritation. As a result, local narrowing of blood vessels occurs, their permeability decreases and exudation decreases. In this regard, astringents have a local anti-inflammatory and mild anesthetic effect.

Astringents are used externally in the form of lotions, lubrication, rinsing, douching, powders for inflammatory lesions of the skin and mucous membranes, as well as internally for certain diseases of the gastrointestinal tract (peptic ulcer of the stomach and duodenum, enteritis, colitis).

There are astringents of plant origin and synthetic ones.

Astringents of plant origin. Oak bark, St. John's wort, blueberries and some other medicinal plants, as well as drugs obtained from them, for example, tannin, tanalbin, etc., are used as astringents of plant origin.

Oak bark (Cortex Quercus) is used in the form of a decoction (1: 10) for rinsing for gingivitis, stomatitis and other inflammatory lesions of the oral cavity, pharynx, pharynx, and larynx.

St. John's wort herb (Herba Hyperici) is used internally as an astringent and antiseptic for colitis, and topically for lubricating gums and as a mouth rinse in the treatment of gingivitis and stomatitis. Prescribed as an infusion (1:20) or tincture. For preparing an infusion at home, briquettes of St. John's wort weighing 75 g, divided into 10 equal slices, are convenient. One slice is poured into a glass of boiling water and boiled for 10 minutes, after which the infusion is cooled and filtered. Take 1/3 cup orally 3 times a day or as a mouth rinse.

St. John's wort tincture is prescribed orally, 40-50 drops 3-4 times a day, and for rinsing - 30-40 drops per 1/2 glass of water. Release form: in bottles of 25 and 100 ml.

Chamomile flowers (Flores Chamomillae) are used as a medicinal tea or infusion, 1-5 tablespoons 2-3 times a day, or in enemas for intestinal spasms, diarrhea, and flatulence. Externally prescribed for rinsing, lotions and baths. At home, tea is prepared at the rate of 1 tablespoon of chamomile flowers per glass of boiling water. Before use, the tea is cooled and filtered.

Romasulon is a liquid containing chamomile extract and essential oil. Used for rinsing, washing and compresses for stomatitis, gingivitis, vaginitis, urethritis, cystitis, trophic ulcers, inflammation of the external ear. For external use, the drug is diluted at the rate of 1.5 tablespoons per 1 liter of water. The drug is prescribed internally for gastritis, colitis, flatulence, 0.5 teaspoons per 1 glass of hot water. Release form: in bottles of 100 ml.

Tannin (Tanninum) is gallotannic acid obtained from growths on young shoots of Asia Minor oak or from domestic plants - sumac and scum. Used for inflammatory processes in the oral cavity, pharynx, larynx in the form of rinses (1-2% aqueous or glycerin solutions) and lubrication (5-10% solutions), as well as for burns, ulcers, bedsores, cracks (in the form of 3-10% ointments, solutions). Release form: powder.

Tannalbin (Tannalbinum) is a product of the interaction of tannins from sumac and mackerel leaves with protein. When taken orally, tannalbin is broken down in the intestines with the release of free tannin, which has an astringent effect on the intestines. Therefore, tanalbin is used for acute and chronic intestinal diseases accompanied by diarrhea. Adults are prescribed 0.3-1 g per dose 3-4 times a day; children - 0.1-0.5 g, depending on age. Release form: tablets of 0.5 g.

The herb (Herba Bidentis) is used as an infusion (at the rate of 7.5 g of herb per glass of boiling water) for baths for diathesis in children. They produce briquettes from succession grass weighing 75 g, divided into 10 slices of 7.5 g or in the form of round briquettes of 7.5 g.

Bird cherry fruit (Bassae Pruni racemosae) is indicated for diarrhea in the form of an infusion or decoction (1:20) 1/4-1/2 cup 2-3 times a day.

Blueberry fruit (Fructus Myrtilli) is used in the form of an infusion or decoction (1-2 teaspoons per 1 cup of boiling water), as well as in the form of blueberry jelly for diarrhea.

Sage leaf (Folium Salviae) is used as an infusion to rinse the mouth and throat. At home, an infusion is prepared at the rate of 1 tablespoon of leaves per glass of boiling water. After infusion for 20 minutes, the infusion is cooled and filtered.

Synthetic binders. Synthetic astringents include some inorganic (basic bismuth nitrate, alum, etc.) and organic (dermatol, xeroform) compounds of a number of metals and metalloids.

Medicinal plants:

Astringents are applied topically. They compact inflamed tissues due to a reversible coagulating effect on proteins and the formation of a protective film on the surface of the skin, mucous membranes, wounds, and ulcers. The compaction of inflammatory tissue contributes to the narrowing of blood vessels, reducing secretion, reducing swelling and pain. All this leads to limiting the area of ​​inflammation. The following means are distinguished:

Organic origin (tannin, decoction of oak bark, infusions and decoctions of sage leaves, St. John's wort, chamomile flowers, blueberries, bird cherry, serpentine root);

Inorganic origin (lead acetate, basic bismuth nitrate, aluminum alum, zinc oxide, copper sulfate, silver nitrate, collargol)

For oral use (for stomach ulcers, gastritis, enteritis), astringents of plant origin are used.

Externally used herbal products and salts of heavy metals (for burns, frostbite, dermatitis, erosion).

TANNIN

Gallodinic acid. Obtained from sumac and mackerel plants. Easily soluble in water and alcohol. Aqueous solutions form precipitates with alkaloids, protein solutions and heavy metal salts. Used as an astringent and anti-inflammatory agent for inflammatory processes in the oral cavity, nose, pharynx, larynx in the form of rinsing with a 1-2% aqueous or glycerin-water solution or for lubrication (5-10%) for burns, ulcers, cracks, bedsores. Prescribed orally for poisoning with salts of heavy metals and alkaloids - the stomach is washed with a 0.5% aqueous solution of tannin. Available in powder form.

BISMUTH NITRATE BASIC

It is a mixture of bismuth compounds: BiNO 3 (OH) 2; ВiONO 3; ViUN. Practically insoluble in water and alcohol, easily soluble in hydrochloric acid. Used as an astringent and antiseptic for gastrointestinal diseases (peptic ulcer of the stomach and duodenum, enteritis, colitis). Release form: powder, tablets of 0.25 and 0.5 g; ointment 10%; is part of the Vikalin Vikair tablets.

SILVER NITRATE (lapis, silver nitrate)

In small concentrations (0.05-0.25% solution) it has an astringent and anti-inflammatory effect, in higher concentrations (1%-2% solution) a cauterizing effect. Used externally for erosions, ulcers, excessive granulations, hyperplastic laryngitis. Release forms: 0.05-2% solutions and in the form of lapis pencils.

Enveloping and absorbent agents

Enveloping the products form colloidal systems with water, which, when applied topically, can form a protective layer and protect sensitive nerve endings from the effects of irritants and to slow down the absorption of drugs. Enveloping agents include starch mucus, mucus from flax seeds, milk, egg white solution, oatmeal decoction, aluminum hydroxide. Used for inflammatory and ulcerative lesions of the gastric and duodenal mucosa, enteritis, colitis, when prescribing medications that have an irritating effect on the mucous membranes, in case of poisoning with acids, alkalis and other aggressive substances.

Adsorbents - have a large contact surface with substances and, therefore, are able to adsorb gases, alkaloids, and toxins. Activated carbon, kaolin (white clay), talc, magnesium carbonate, zinc oxide, calcium carbonate have adsorbing properties.

ACTIVATED CHARCOAL

Coal of animal or vegetable origin, specially processed. Used for dyspepsia, flatulence, food intoxication, poisoning with alkaloids, salts of heavy metals. Release form: tablets of 0.25 g, powder.

ALMAGEL

A combined preparation containing aluminum hydroxide (gel), magnesium oxide, D-sorbitol, has adsorbent, enveloping and antacid properties. Used for gastric and duodenal ulcers, acute and chronic hyperacid gastritis. Prescribe 1-2 teaspoons orally 4 times a day, half an hour before meals and at night. Release form – bottles of 170 or 200 ml

Sucralfate (Venter, Sukrat)

The drug has an adsorbent, enveloping and antacid effect. When entering the stomach, it forms a polymer protective film on the surface of the affected mucous membrane and has a cytoprotective effect. Prescribed for adults with gastric and duodenal ulcers and hyperacid gastritis 0.5-1 hour before meals, 1-2 tablets before breakfast, lunch and dinner. The tablets are swallowed without chewing, washed down with a small amount of water. Release form: tablets of 0.5 in a package of 100 pieces.

Irritants

Irritants are used to reduce pain emanating from organs or muscles. To do this, they stimulate nerve endings in those areas of intact skin that are innervated by fibers that are part of the same nerve roots. These drugs cause redness of the skin and elements of inflammation (the release of large amounts of histamine, prostaglandins). Vasodilation at the site of application of irritating agents leads to improved blood circulation and tissue trophism, the release of small amounts of inflammatory mediators and has a distracting effect, since the entry of afferent impulses into the central nervous system from the skin can change the action of signals coming from other peripheral zones innervated by fibers from the same the nerve root itself.

Irritants include: capsin, Finalgon ointment, Capsicam ointment, camphor ointment, camphor alcohol and many others.

MENTHOL

The main component of peppermint essential oil. Stimulates cold receptors, reduces reflex vascular tone. It is the main component of validol. Unfortunately, validol is popular among the population as a means of relieving cardiac pain. It has no therapeutic effect and should not be used in coronary patients. It has a mild local anesthetic effect and has weak antiseptic properties. Used externally as a distraction and analgesic for myalgia, neuralgia, arthralgia, migraine. For inflammatory diseases of the upper respiratory tract (runny nose, laryngitis, pharyngitis, etc.) it is used in the form of inhalations and for lubricating mucous membranes, in nasal drops. Menthol is included in many combination medications. Available in the form of powder, menthol oil 1% and 2%, alcohol solution 1% and 2%.

AMMONIA

Ammonia solution 10%. When inhaling vapors, it reflexively excites the respiratory center, acting through the receptors of the upper respiratory tract. Used as an ambulance to induce breathing and bring patients out of fainting. Externally in the form of lotions for insect bites. Included in drops of ammonia-anise, ammonia liniment.

FINALGON

The ointment contains vanillylnonamide and butoxyethyl ether, which cause prolonged expansion of capillaries and skin hyperemia, providing a distracting, analgesic and anti-inflammatory effect. Prescribed for muscle and joint pain of various origins, tendovaginitis, neuritis, sciatica, and sports injuries. Using an applicator, rub the ointment into the skin of the affected area and cover it with a woolen cloth. The ointment is used 2-3 times a day. Avoid getting the ointment on the mucous membranes. Release form: 20 g tubes complete with applicator.

EXPERIMENTAL WORK

Astringents- these are chemical compounds that have the ability, when interacting with the protein of cells, tissues, tissue fluids of the body, to cause surface coagulation of proteins and form dense albuminates that protect nerve endings from irritation and further pain.

Organic astringents:

• tannin;
• oak bark (contains tannin);
• tanalbin;
• St. John's wort herb;
• sage leaves;
• fruits;
• bird cherry fruits, etc.

Inorganic binders (heavy metal salts):

• bismuth nitrate basic;
• bismuth citrate;
• dermatol;
• xeroform;
• potassium alum;
• Burov's liquid (aluminum acetate);
• zinc sulfate;
• copper sulfate;
• silver nitrate;
• protargol;
• lead acetate.

Application of astringents

Organic astringents are used for inflammation of the intestines, gastrointestinal bleeding, and catarrh of the mucous membranes of the mouth, throat and pharynx. They are prescribed externally for the treatment of burns, for rinsing the mouth and throat for stomatitis, pharyngitis, laryngitis, etc.

Tanalbin deserves special attention in this series. It is a product of the interaction of tannins from the leaves of mackerel (Cotinus coggygria Scop.) and sumac (Rhus coriaria L.) family. cy-flyweeds (Anacardiaceae) with protein (casein).

The fundamental idea of ​​​​creating such a complex is to “protect” the active principle of the drug from contact with the surface tissues of the oral cavity, pharynx, esophagus and stomach.

After administration, it enters the stomach, where, under the action of hydrochloric acid and digestive enzymes, the protein part of the complex is split off, and the active tannin molecules reach the intestines, where they exert their astringent effect. Therefore, tanalbin is used only orally for the treatment of inflammatory bowel diseases.

Salts of heavy metals, in addition to their astringent effect, also have other types of pharmacological activity, which directly depend on the active concentration of the substance (Table 1).

In addition, it should be noted that the strength of the pharmacological activity of heavy metal salts directly depends on the degree of ionization of the molecule and on the type of anion with which the salt is formed. This dependence is clearly seen in the example of zinc preparations: zinc sulfate and zinc oxide.

Zinc sulfate easily dissociates into ions:

ZnSO, -> Zn2+ + SO,2

As a result, free zinc ions actively contact proteins and exert their pharmacological effects. In addition, the resulting anion of sulfuric acid, which belongs to the class of strong acids, makes an additional contribution to the overall effect of the drug.

Therefore, zinc sulfate has all the types of action listed in Table 1, and its concentration ranges from 0.5% to 2%.

At the same time, zinc oxide does not undergo ionization, and therefore it has only an astringent effect in a concentration of 25-50%.

Table 1

Spectrum of pharmacological activity of heavy metal salts