A group of sulfonamides and co-trimoxazole. Sulfonamides What are the sulfonamide preparations?

The sulfonamides familiar to people have long established themselves, as they appeared even before the history of the discovery of penicillin. To date, these drugs in pharmacology have partially lost their significance, since they are inferior to modern medicines in terms of efficiency. However, in the treatment of certain pathologies, they are indispensable.

Sulfonamides (sulfonamides) are synthetic antimicrobial drugs that are derivatives of sulfanilic acid (aminobenzenesulfamide). Sulfanilamide sodium inhibits the vital activity of cocci and rods, affects nocardia, malaria, plasmodia, proteus, chlamydia, toxoplasma, has a bacteriostatic effect. Sulfanilamide preparations are drugs that are prescribed for the treatment of diseases caused by pathogens resistant to antibiotics.

Classification of sulfa drugs

In their activity, sulfa drugs are inferior to antibiotics (not to be confused with sulfonanilide). These drugs have a high toxicity, so they have a limited range of indications. The classification of sulfa drugs is divided into 4 groups, depending on the pharmacokinetics and properties:

  1. Sulfonamides, rapidly absorbed from the gastrointestinal tract. They are prescribed for systemic treatment of infections caused by susceptible microorganisms: Etazol, Sulfadimetoksin, Sulfametizol, Sulfadimidine (Sulfadimezin), Sulfacarbamide.
  2. Sulfonamides, incompletely or slowly absorbed. They create in thick and small intestine high concentration: Sulgin, Ftalazol, Phtazin. Etazol sodium
  3. Sulfonamides local application. Well proven in eye therapy: Sulfacyl sodium (Albucid, Sulfacetamide), Silver sulfadiazine (Dermazin), Mafenide acetate ointment 10%, Streptocide ointment 10%.
  4. Salazosulfanamides. This classification of compounds of sulfonamides with salicylic acid: Sulfasalazine, Salazomethoxin.

The mechanism of action of sulfa drugs

The choice of a drug for treating a patient depends on the properties of the pathogen, because the mechanism of action of sulfonamides is reduced to blocking sensitive microorganisms in synthesis cells. folic acid. For this reason, some drugs, for example, Novocaine or Methionomixin, are incompatible with them, as they weaken their effect. The key principle of action of sulfonamides is a violation of the metabolism of microorganisms, the suppression of their reproduction and growth.

Indications for the use of sulfonamides

Depending on the structure, sulfide preparations have a common formula, but unequal pharmacokinetics. There are dosage forms for intravenous administration: Sodium sulfacetamide, Streptocid. Some drugs are administered intramuscularly: Sulfalen, Sulfadoxin. Combination drugs are used in both ways. For children, sulfonamides are used topically or in tablets: Co-trimoxazole-Rivofarm, Cotrifarm. Indications for the use of sulfonamides:

  • folliculitis, acne vulgaris, erysipelas;
  • impetigo;
  • burns 1 and 2 degrees;
  • pyoderma, carbuncles, boils;
  • purulent-inflammatory processes on the skin;
  • infected wounds of various origins;
  • tonsillitis;
  • bronchitis;
  • eye diseases.

List of sulfa drugs

According to the circulation period, antibiotics sulfonamides are divided into: short, medium, long-term and extra-long exposure. It is not possible to list all drugs, so this table presents long-acting sulfonamides used to treat many bacteria:

Name

Indications

silver sulfadiazine

infected burns and superficial wounds

Argosulfan

silver sulfadiazine

burns of any etiology, minor injuries, trophic ulcers

norsulfazol

norsulfazole

pathologies caused by cocci, including gonorrhea, pneumonia, dysentery

sulfamethoxazole

urinary tract infections, respiratory tract, soft tissue, skin

Pyrimethamine

pyrimethamine

toxoplasmosis, malaria, primary polycythemia

Prontosil (Red streptocide)

sulfanilamide

streptococcal pneumonia, puerperal sepsis, erysipelas

Combined sulfa drug

Time does not stand still, and many strains of microbes have mutated and adapted. Doctors found new way fight bacteria - they created a combined sulfanilamide drug, in which antibiotics are combined with trimethoprim. The list of such sulfo drugs:

Titles

Indications

sulfamethoxazole, trimethoprim

gastrointestinal infections, uncomplicated gonorrhea and other infectious pathologies.

Berlocid

sulfamethoxazole, trimethoprim

chronic or acute bronchitis lung abscess, cystitis bacterial diarrhea and others

Duo-Septol

sulfamethoxazole, trimethoprim

broad spectrum antibacterial, antiprotozoal, bactericidal agent

sulfamethoxazole, trimethoprim

typhoid fever, acute brucellosis, brain abscess, inguinal granuloma, prostatitis and others

Sulfanilamide preparations for children

Since these drugs are broad-spectrum drugs, they are also used in pediatrics. Sulfanilamide preparations for children are available in tablets, granules, ointments and injection solutions. List of medicines:

Name

Application

sulfamethoxazole, trimethoprim

from 6 years: gastroenteritis, pneumonia, wound infections, acne

Etazola tablets

sulfaetidol

from 1 year: pneumonia, bronchitis, tonsillitis, peritonitis, erysipelas

Sulfargin

silver sulfadiazine

from 1 year: non-healing wounds, bedsores, burns, ulcers

trimezol

co-trimoxazole

from 6 years: infections of the respiratory tract, genitourinary system, skin pathologies

Instructions for use of sulfonamides

Antibacterial agents are prescribed, both inside and locally. Instructions for the use of sulfonamides states that children will use the drug: up to a year, 0.05 g, from 2 to 5 years - 0.3 g, from 6 to 12 years - 0.6 g for the entire intake. Adults take 5-6 times / day for 0.6-1.2 g. The duration of treatment depends on the severity of the pathology and is prescribed by a doctor. According to the annotation, the course is no more than 7 days. Any sulfa drug should be taken with an alkaline liquid and foods that contain sulfur to maintain the urine reaction and prevent crystallization.

Side effects of sulfa drugs

With prolonged or uncontrolled use, there may be side effects sulfonamides. These are allergic reactions, nausea, dizziness, headaches, vomiting. With systemic absorption, sulfo drugs can pass through the placenta and then be found in the blood of the fetus, causing toxic effects. For this reason, the safety of the use of drugs during pregnancy is questionable. The doctor should take into account such a chemotherapeutic effect when prescribing them to pregnant women and during lactation. A contraindication to the use of sulfonamides is:

  • hypersensitivity to the main component;
  • anemia;
  • porphyria;
  • liver or kidney failure;
  • pathology of the hematopoietic system;
  • azotemia.

The price of sulfa drugs

Medicines of this group are not a problem to buy in an online store or pharmacy. The difference in cost will be noticeable if you order several drugs from the catalog on the Internet at once. If you buy a medicine in a single version, you will have to pay extra for delivery. Domestically produced sulfonamides will be inexpensive, while imported drugs are much more expensive. Approximate price for sulfa drugs:

Video: what are sulfonamides

Sulfanilamide drugs - a list. The mechanism of action of sulfonamides, use and contraindications - all about medicines and health on the site

In this article, you can read the instructions for using the drug Sulfanilamide. Reviews of site visitors - consumers of this medicine, as well as opinions of doctors of specialists on the use of Sulfanilamide in their practice are presented. A big request to actively add your reviews about the drug: did the medicine help or not help get rid of the disease, what complications were observed and side effects, possibly not declared by the manufacturer in the annotation. Sulfanilamide analogues in the presence of existing structural analogues. Use for the treatment of tonsillitis, erysipelas, cystitis and other infectious diseases in adults, children, as well as during pregnancy and lactation. The composition of the drug.

Sulfanilamide- a broad-spectrum antibacterial agent. Sulfanilamide (streptocide) is one of the first representatives of chemotherapeutic agents of the sulfonamide group. It has a bacteriostatic effect. The mechanism of action is due to competitive antagonism with PABA and competitive inhibition of the enzyme dihydropteroate synthetase. This leads to a disruption in the synthesis of dihydrofolic and then tetrahydrofolic acid and, as a result, to a disruption in the synthesis of nucleic acids.

Sulfanilamide is active against gram-positive and gram-negative cocci, Escherichia coli (E. coli), Shigella spp. (shigella), Vibrio cholerae, Haemophilus influenzae, Clostridium spp., Bacillus anthracis, Corynebacterium diphtheriae, Yersinia pestis, as well as against Chlamydia spp. (chlamydia), Actinomyces spp., Toxoplasma gondii (toxoplasma).

When applied topically, it promotes rapid healing of wounds.

Previously, sulfanilamide was used orally for the treatment of tonsillitis, erysipelas, cystitis, pyelitis, enterocolitis, prevention and treatment of wound infection. Sulfanilamide (Streptocid soluble) used in the past as 5% aqueous solutions for intravenous administration.

It is not an antibiotic.

Compound

Sulfanilamide + excipients.

Pharmacokinetics

When taken orally, it is rapidly absorbed from the gastrointestinal tract. Cmax in the blood is created after 1-2 hours and decreases by 50%, usually in less than 8 hours. It passes through the histohematic, including the blood-brain (BBB), placental barriers. It is distributed in tissues, after 4 hours it is found in the cerebrospinal fluid. It is acetylated in the liver with loss of antibacterial properties. It is excreted mainly (90-95%) by the kidneys.

There is no information on carcinogenic, mutagenic and fertility effects during long-term use in animals and humans.

Indications

  • tonsillitis (tonsillitis);
  • sinusitis (sinusitis);
  • bronchitis;
  • pneumonia;
  • purulent-inflammatory skin lesions (skin abscess);
  • infected wounds of various etiologies (including ulcers, cracks);
  • furuncle;
  • carbuncle;
  • pyoderma;
  • folliculitis;
  • erysipelas;
  • acne vulgaris;
  • impetigo;
  • acute and chronic cholecystitis;
  • cholangitis;
  • cystitis;
  • urethritis and urethral syndrome;
  • inflammatory diseases of the prostate gland (prostatitis);
  • salpingitis and oophoritis;
  • burns (1 and 2 degrees).

Release forms

Tablets 0.3 g and 0.5 g.

Powder for external use 2 g and 5 g.

Liniment 5%.

Instructions for use and method of use

Inside - 0.5 g 5-6 times a day; children under 1 year old - 0.05-0.1 g per reception, 2-5 years old - 0.2-0.3 g, 6-12 years old - 0.3-0.5 g.

For deep wounds, it is injected into the wound cavity in the form of a carefully ground sterilized powder (5-15 g), while prescribing antibacterial drugs inside.

When applied externally, it is applied to the affected areas of the skin and mucous membranes.

Maximum doses for adults when taken orally: single 2 g, daily - 7 g.

Side effect

  • nausea, vomiting;
  • diarrhea;
  • eosinophilia, thrombocytopenia, leukopenia, hypoprothrombinemia, agranulocytosis;
  • visual impairment;
  • headache;
  • dizziness;
  • peripheral neuropathy;
  • cyanosis;
  • ataxia;
  • skin allergic reactions;
  • nephrotoxic reactions (most likely in patients with impaired renal function);
  • hypothyroidism.

Contraindications

  • severe renal failure;
  • blood diseases;
  • deficiency of glucose-6-phosphate dehydrogenase;
  • nephrosis, nephritis;
  • acute porphyria;
  • thyrotoxicosis;
  • 1st and 2nd trimesters of pregnancy;
  • lactation;
  • hypersensitivity to sulfonamides.

Use during pregnancy and lactation

Sulfanilamide is contraindicated for use in the 1st and 2nd trimesters of pregnancy and lactation.

Use in children

Use in children is possible according to the dosing regimen.

special instructions

Use with caution in patients with impaired renal function. During the treatment period, it is necessary to increase the amount of fluid consumed.

If hypersensitivity reactions occur, treatment should be discontinued.

drug interaction

Not marked.

Analogues of the drug Sulfanilamide

Structural analogues for the active substance:

  • Streptocid;
  • Streptocide soluble;
  • Streptocide tablets;
  • Streptocid ointment 10%.

Analogues by pharmacological group (sulfonamides):

  • Argedin;
  • Argosulfan;
  • Bactrim;
  • Bactrim forte;
  • Biseptol;
  • Groseptol;
  • Dvaseptol;
  • Dermazin;
  • Ingalipt;
  • Co-trimoxazole;
  • Cotrifarm 480;
  • Lidaprim;
  • Mafenide acetate ointment 10%;
  • Methosulfabol;
  • Oriprim;
  • Septrin;
  • Sinersul;
  • Streptonitol;
  • Streptocid;
  • Sulothrim;
  • Sulgin;
  • Sulfadimezin;
  • Sulfadimethoxine;
  • Sulfalen;
  • Sulfamethoxazole;
  • Sulfargin;
  • Sulfasalazine;
  • Sulfathiazole sodium;
  • Sulfacetamide;
  • Sulfacyl sodium;
  • Sumetrolim;
  • Trimezol;
  • Ftalazol;
  • Phthalylsulfathiazole;
  • Ziplin;
  • Etazol.

In the absence of analogues of the drug for the active substance, you can follow the links below to the diseases that the corresponding drug helps with and see the available analogues for the therapeutic effect.

Sulfanilamide preparations(synonymous with sulfonamides) - synthetic broad-spectrum chemotherapeutic agents from the group of derivatives of sulfanilic acid amide (sulfanilamide).

Streptococci, and diplococci (gonococci, meningococci, pneumococci), intestinal, dysentery, diphtheria and anthrax, brucella, vibrio cholerae, actinomycetes, chlamydia (causative agents of trachoma, ornithosis, etc.), as well as pathogens of anaerobic infection ( clostridia), some protozoal infections (malaria, a). Besides, separate activators of deep ov (nocardin, actinomycetes) are sensitive to S. of the item. Some S. items (sulfadimethoxine, sulfapyridazine, sulfalene) are active against mycobacteria leprosy (see. Anti-leprosy drugs ). Salmonella, Pseudomonas aeruginosa, mycobacterium tuberculosis, spirochetes, leptospira, and viruses are among the items resistant to S.. S.'s microorganisms, sensitive to them, in concentrations in which they accumulate in the body in therapeutic doses, act bacteriostatically.

The mechanism of the antimicrobial action of S. p. is due to the fact that they block the synthesis of dihydrofolic acid at the stage of formation of dihydropteroic acid from dihydropteridine and para-aminobenzoic acid (PABA) with the participation of the enzyme dihydropteroate synthetase (dihydrofolate synthetase). It is believed that the violation of the synthesis of dihydropteroic acid occurs primarily as a result of the inclusion of S. p. instead of PABA as a substrate for dihydropteroate synthetase, tk. according to the chemical structure of S. p., they are similar to PABA. As a result, the formation of analogues of dihydrofolic acid, which do not have its inherent biological activity, occurs. In addition, when S. p. interacts with dihydropteridine in the presence of ATP and magnesium ions, an intermediate metabolite is formed that inhibits dihydropteroate synthetase, which leads to inhibition of the formation of dihydrofolic acid. It is also possible that S. p. prevent the inclusion of dihydropteridine in the synthesis of dihydrofolic acid. Ultimately, the violation of the formation of dihydrofolic acid under the influence of S. p. leads to a decrease in the formation of tetrahydrofolic acid and the resulting inhibition of nucleotide biosynthesis and a delay in the development and reproduction of microorganisms. These features of the mechanism of action explain the fact that only those microorganisms in which the process of dihydrofolic acid synthesis occurs are sensitive to S. p. Microorganisms and macroorganism cells that utilize ready-made dihydrofolic acid from the external environment are not sensitive to the action of S. p.

With an excess of PABA and its derivatives in the environment, for example, novocaine, anestezin, etc., as well as methionine, folic acid, purine and pyrimidine bases, the antimicrobial activity of S. p. decreases. A decrease in the activity of S. p. in the presence of pus and wound discharge is associated with a high content of PABA and other antagonists of sulfanilamide preparations in these substrates.

The antimicrobial effect of S. p. is enhanced by drugs (for example, trimethoprim) that inhibit the conversion of dihydrofolic acid to folic (tetrahydrofolic) acid by inhibiting the enzyme dihydrofolate reductase. With the simultaneous use of S. p. with trimethoprim, the synthesis of tetrahydrofolic acid is disturbed at two successive stages - at the stage of formation of dihydrofolic acid (under the influence of S. p.) and at the stage of conversion of the latter into tetrahydrofolic acid (under the influence of trimethoprim), as a result of which a bactericidal effect develops .

After absorption into the blood, S. p. reversibly, but to a different extent, binds to plasma proteins. In a bound form, they do not have an antimicrobial effect and show it only as the drugs are released from this connection. The degree of their binding to blood plasma proteins does not affect the rate of S.'s release from the body. Metabolized by S. p. in the liver mainly by acetylation. The resulting acetylated metabolites of S. p. have no antimicrobial activity and are excreted from the body through the kidneys. In the urine, these metabolites can precipitate in the form of crystals, causing the appearance of crystalluria. The severity of crystalluria is determined not only by the degree of conversion of individual S. p. into acetylated metabolites and the magnitude of the doses of drugs, but also by the reaction of urine, tk. these metabolites are poorly soluble in an acidic environment.

According to features of pharmacokinetics and application among S. of the item distinguish the corresponding subgroups. For example, allocate a subgroup of S. items well absorbed from the gastrointestinal tract. Such S. items are used for systemic treatment of infections and for this purpose are prescribed orally and parenterally. Depending on the rate of their release among S. p. of this subgroup, there are: short-acting drugs (half-life less than 10 h) - streptocide, sulfacyl sodium, etazol, sulfadimezin, urosulfan, etc .; intermediate-acting drugs (half-life 10-24 h) - sulfazine, sulfamethoxazole, etc.; long-acting drugs (half-life from 24 to 48 h) - ulfapiridazine, sulfadimethoxine, sulfayunomethoxine, etc.; long-acting drugs (half-life more than 48 h) - sulfalene.

Long-acting sulfonamides differ from short-acting S. p. in higher lipophilicity and, therefore, they are reabsorbed in significant quantities (up to 50-90%) in the renal tubules and are more slowly excreted from the body.

Sulgin, ftalazol, and ftazin belong to the subgroup of S.'s poorly absorbed from the gastrointestinal tract. These drugs are used to treat intestinal infections (colitis and enterocolitis of bacterial etiology, including bacillary dysentery).

The subgroup of S. items intended for topical use usually include soluble sodium salts of drugs that are well absorbed from the gastrointestinal tract, for example, etazol sodium, sulfapyridazine sodium, soluble streptocide, etc., as well as silver sulfadiazine. Preparations of this subgroup in the appropriate dosage forms (solutions, ointments, etc.) are used topically for the treatment of purulent infections of the skin and mucous membranes, infected wounds, etc.

In addition, among S. p., the so-called salazosulfanilamides are distinguished - azo compounds synthesized on the basis of some S. p. of systemic action and salicylic acid. These include salazopyridazine, salazodimethoxine, and salazosulfapyridine, which are used primarily for the treatment of non-specific ulcerative a. The effectiveness of salazosulfanamides in this disease is associated with the presence of not only antimicrobial activity, but also pronounced anti-inflammatory properties, which are due to the formation of aminosalicylic acid in the intestine during the biotransformation of drugs of this group, which has an anti-inflammatory effect.

In modern clinical practice Combination preparations containing sulfonamides and trimethoprim are also widely used. Such combined preparations include biseptol containing sulfamstoxazole and trimethoprim (5:1 ratio) and sulfatone containing sulfomonomethoxine and trimethoprim (2.5:1 ratio). Unlike S. p. biseptol and sulfatone act bactericidal, have a broader spectrum of antimicrobial activity and are effective against strains resistant to sulfanilamide drugs.

In practice, other combinations of S. p. with diaminopyrimidine derivatives are also used. For example, combinations of sulfalene with chloridine are used to treat drug-resistant forms of malaria, and combinations of sulfazine with chloridine are used to treat a.

Sulfonamides are used to treat infections caused by microorganisms sensitive to these drugs. The choice of drugs is made taking into account the peculiarities of their pharmacokinetics. So, with systemic infections (bacterial infections of the respiratory tract, lungs, bile and urinary tract etc.) are used by S. p., well absorbed from the gastrointestinal tract. For the treatment of intestinal infections, S.

items that are poorly absorbed from the gastrointestinal tract (sometimes in combination with well-absorbed S. p.).

Single and course doses of S. p., as well as the schemes for their appointment, are established in accordance with the duration of action of the drugs. So, short-acting S. p. is used in daily doses of 4-6 G, appointing them in 4-6 doses (course doses 20-30 G); drugs of medium duration of action - in daily doses 1-3 G, appointing them in 2 doses (course doses 10-15 G); long-acting drugs are prescribed in one dose at a daily dose of 0.5-2 G(course doses up to 8 G). Ultra-long-acting sulfonamides are prescribed according to two schemes: daily at the initial dose (on the first day) 0.8-1 G and further in maintenance doses of 0.2 G 1 time per day; 1 time per week at a dose of 1.5-2 G. For children, doses are reduced according to age.

Side effects of S. p. (headache, dizziness, etc.), leukopenia, methemoglobinemia, etc. Due to poor solubility in water, S. p. and their acetylation products in the body can precipitate in the kidneys in the form of crystals and cause crystalluria (especially when urine is acidified). For the prevention of this complication when taking S. p., it is advisable to recommend a plentiful alkaline drink.

S. items are contraindicated if there is a history of data on toxic-allergic reactions to any drugs in this group. In diseases of the liver and kidneys, S. p. should be prescribed in reduced doses under the control of the functional state of these organs.

Methods of application, doses, forms of release and storage conditions of the main S. items are given below.

Biseptol(Biseptol; a synonym for Bactrim, Septrin, etc.) is prescribed orally (after meals) for adults and children over 12 years old, 1-2 tablets (for adults) 2 times a day, in severe cases - 3 tablets 2 times a day; children aged 2 to 5 years, 2 tablets (for children); from 5 to 12 years, 4 tablets (for children) 2 times a day. Release form: tablets for adults containing 0.4 G sulfamethoxazole and 0.08 G trimethoprim; tablets for children containing 0.1 G sulfamethoxazole and 0.02 G trimethoprim. Storage: list B.

Salazodimethoxine(Salazodimethoxinum) is used orally (after meals). Adults are prescribed 0.5 G 4 times a day or 1 G 2 times a day for 3-4 weeks. Upon the onset of a therapeutic effect, the daily dose is reduced to 1-1.5 G(by 0.5 G 2-3 times a day). Children aged 3 to 5 years are initially prescribed 0.5 G per day (in 2-3 doses). At the onset of a therapeutic effect, the dose is reduced by 2 times. Children aged 5 to 7 years are initially prescribed 0.75-1 G, from 7 to 15 years, 1-1.5 G per day. Release form: powder, tablets of 0.5 G. Storage: list B; in a place protected from light.

Salazopyridazine(Salazopyridazinum). Methods of application, doses. release forms and storage conditions are the same as for salazodimethoxine.

streptocide(Streptocidum, a synonym for white streptocide) is administered orally to adults at 0.5-1 G at the reception 5-6 times a day; children under the age of 1 year at 0.05-0.1 G, from 2 to 5 years by 0.2-0.3 G, from 6 to 12 years 0.3-0.5 G appointment. Higher doses for adults orally single 2 G, daily 7 G. Topically applied in the form of powders, ointments (10%) or liniments (5%). Release form: powder, tablets of 0.3 and 0.5 G; 10% ointment; 5% liniment. Storage: list B: in a well-closed container.

Streptocid soluble(Streptocidum solubile) is administered intramuscularly and subcutaneously in the form of 1-1,

5% solutions prepared with water for injection or isotonic sodium chloride solution, up to 100 ml(2-3 times a day). Intravenously administered in the form of 2-5-10% solutions prepared in the same solvents or 1% glucose solution, up to 20-30 ml. Release form: powder. Storage: List B in well-closed jars.

Sulgin(Sulginum) is prescribed inside for adults 1-2 times a day. G at the reception: on the 1st day 6 times a day, on the 2nd and 3rd days 5 times, on the 4th day 4 times, on the 5th day 3 times a day. The course of treatment is 5-7 days. Other schemes are used to treat acute dysentery. Higher doses for adults single 2 G, daily 7 G. release forms: powder; tablets 0.5 G

Silver sulfadiazine(Sulfadiazini argenti) is applied topically. Included in the composition of the ointment "Dermazin", which is applied to the oval surface with a layer of 2-4 mm 2 times a day, followed by the imposition of a sterile dressing. Ointment is not prescribed to premature and newborn children; in pregnant women, they are used according to health indications (with an area of ​​\u200b\u200bmore than 20% of the body surface). Release form: tubes of 50 G, cans of 250 G.

Sulfadimezin(Sulfadimezinum; synonymous with sulfadimidine, etc.) is administered orally to adults at the first dose 2 G, then 1 G every 4-6 h(until the body temperature drops), then 1 G after 6-8 h. Children inside at the rate of 0.1 g/kg at the first appointment, then 0.025 g/kg every 4-6-8 h. For the treatment of dysentery, adults are prescribed according to the following scheme: on the 1st and 2nd days, 1 G every 4 h(6 G per day), on the 3rd and 4th days 1 G every 6 h(4 G per day), on the 5th and 6th days 1 G every 8 h(3 G per day). After a break (within 5-6 days), a second cycle is carried out, appointing on the 1st and 2nd days 5 G per day, on the 3rd and 4th days 4 G per day, on the 5th day 3 G per day. For the same purpose, children under 3 years of age are prescribed at the rate of 0.2 g/kg per day (in 4 divided doses) for 7 days, children over 3 years old 0.4-0.75 G(depending on age) 4 times a day. Release form: powder; tablets of 0.25 and 0.5 G

Sulfadimethoxine(Sulfadimethoxinum; synonymous with madribon, etc.) is used orally. Adults are prescribed on the 1st day 1-2 G, in the following days, 0.5-1 G per day (in one dose); children at the rate of 0.025 g/kg on the 1st day and at 0.0125 g/kg in the following days. Release form: powder; tablets of 0.2 and 0.5 G. Storage: list B; in a place protected from light.

Sulfazin(Sulfazinum) is used internally. Adults are prescribed for the 1st appointment 2-4 G, within 1-2 days 1 G every 4 h, in the following days 1 G every 6-8 h; children at the rate of 0.1 g/kg at the first appointment, then 0.025 g/kg every 4-6 h. Release form: powder; tablets 0.5 G. Storage: list B; in a place protected from light.

Sulfalen(Sulfalenum; synonymous with kelfisin, etc.) is prescribed by mouth for adults, 2 G once every 7-10 days or on the first day 1 G, then by 0.2 G daily. Release form: tablets of 0.2 G. Storage: list B.

Sulfamonomethoxine(Sulfamonomethoxin). The method of administration and doses are the same as those of sulfadimethoxine. Release form: powder; tablets 0.5 G

Sulfapyridazine(Sulfapyridazinum; synonym: spofazadin, sulamine, etc.). The method of administration and doses are the same as those of sulfadimethoxine. Release form: powder; tablets 0.5 G. Storage: list B; in a place protected from light.

Sulfatone(Sulfatonum) is prescribed by mouth for adults, 1 tablet 2 times a day. Higher doses for adults: single - 4 tablets, daily - 8 tablets. Release form: tablets containing 0.25 G sulfamonomethoxine and 0.1 G trimethoprim. Storage: list B; in a dry, dark place.

Sulfacyl sodium(Sulfacylum-natrium; synonym: soluble sulfacyl, sulfacetamide-sodium, etc.) is administered orally to adults at 0.5-1 G, children 0.1-0.5 G 3-5 times a day. Intravenously (slowly) 3-5 ml 30% solution 2 times a day. In eye practice, they are used in the form of 10-20-30% solutions and ointments. Higher doses for adults orally single 2 G, daily 7 G. Release form: powder; 30% solution for injection in ampoules of 5 ml; 30% solution in vials of 5 and 10 ml; 20% and 30% solutions (eye drops) in dropper tubes of 1.5 ml; 30% ointment 10 G. Storage: list B; in a cool, dark place.

Urosulfan(Urosulfanum) is used internally. Adults are prescribed in the same doses as sodium sulfacyl, children 1-2.5 G per day (in 4-5 doses). The higher daily doses for adults are the same as sodium sulfacyl. Release form: powder, tablets of 0.5 G

Phtazin(Phthazinum) is administered orally to adults on the first day, 1 G 1-2 times, in the following days, 0.5 G 2 times a day. For children, the dose is reduced according to age. Release form: powder; tablets 0.5 G. Storage: list B: in a place well protected from light.

Ftalazol(Phthalazolum; synonymous with phthalyl-sulfathiazole, etc.) is used orally for dysentery. Adults are prescribed on the 1-2nd day 1 G every 4 h(6 G per day), on the 3rd-4th days, 1 G every 6 h(4 G per day), on the 5-6th day, 1 G every 8 h(3 G per day). After 5-6 days, the treatment is repeated: on the 1st-2nd days - 5 G per day, on the 3rd-4th days - 4 G per day, on the 5th day - 3 G per day. For other intestinal infections, adults are prescribed in the first 2-3 days 1-2 G, in the following days, 0.5-1 G every 4-6 h. Children under 3 years old with dysentery are prescribed at the rate of 0.2 g/kg per day (in 3 divided doses), children over 3 years old 0.4-0.75 G at the reception 4 times a day. The highest oral doses for adults are the same as for sulfacyl sodium. Release form: powder; tablets 0.5 G. Storage: list B; in a well sealed container.

Etazol(Aethazolum; synonymous with sulfaetidol, etc.) is administered orally to adults, 1 G 4-6 times a day: children under 2 years old 0.1-0.3 G every 4 h, from 2 to 5 years - 0.3-0.4 G every 4 h, from 5 to 12 years old - 0.5 each G every 4 h. Locally prescribed in the form of a powder (powder) or ointment (5%). The highest oral doses for adults are the same as for sulfacyl sodium. Release form: powder; tablets of 0.25 and 0.5 G. Storage: list B; in a well sealed container.

Etazol sodium(Aethazolum-natrium; synonymous with etazol soluble) is administered intravenously (slowly) 5-10 ml 10% or 20% solution. In pediatric practice, the drug is used orally in granules, which are dissolved in water before use and prescribed to children at the age of 1 year - 5 ml (0,1 G), 2 years - 10 ml (0,2 G), 3-4 years - 15 ml (0,3 G), 5-6 years - 20 ml every 4 h. Release form: powder; ampoules of 5 and 10 ml 10% and 20% solutions; granules in bags of 60 G. Storage: list B; in a well-closed container, protected from light.

(sulfonamides) are broad-spectrum bacteriostatic drugs from the group of sulfanilic acid amide derivatives.

Given the bacteriostatic effect of sulfonamides, the therapeutic effect is not always observed, which is why they are often used. together with other chemotherapy drugs.

Who discovered sulfa drugs?

In 1935, G. Domag showed the chemotherapeutic properties of the first of them - prontosil- with streptococcal infections. The effect of this drug was also noted in pneumococcal, gonococcal and some other infections.

In the same year, prontosil was synthesized in the USSR under the name of red streptocide by O. Yu. Magidson and M. V. Rubtsov. It was soon established that therapeutic effect prontosil is exerted not by its entire molecule, but by the metabolite split off from it - sulfanilic acid amide(sulfanilamide), used independently and synthesized in the USSR under the name white streptocide, now known as streptocide and its sodium salt.

What are sulfonamides?

On the basis of this drug synthesized more than 10,000 sulfa drugs, of which about 40 have found application in medical practice as antibacterial agents, often differing significantly from the original drug in many ways.

The sulfonamides used in medical practice are white, odorless, finely crystalline powders, usually slightly soluble in water (their sodium salts are much more soluble).

Action (indications) of sulfanilic acid amide derivatives

Sulfonamides have antimicrobial action on the:

  • many Gram-positive and Gram-negative bacteria
  • some protozoa (plasmodia malaria, toxoplasma),
  • chlamydia(in particular, pathogens of trachoma),
  • actinomycetes of mycobacterium leprosy.

With the introduction of sulfanilamide at an underestimated dose or with an incomplete course of treatment, it may develop resistance to sulfanilamide-susceptible pathogens to its action, which has a cross character in relation to most of the drugs in this group. But resistance usually develops rather slowly. Determination of bacterial resistance to these drugs should be carried out only on special nutrient media without peptone, which weakens their action.

Distinguish a subgroup of sulfa drugs intended primarily for chemotherapy with intestinal infections, in particular in various forms of bacterial colitis, for example dysentery. These are ftalazol, sulgin and some others. Due to poor absorption in the intestines, sulfonamides create very high concentrations in them. Usually they are prescribed 1 g per reception, the first day 6 times, then gradually reducing the number of doses to 3-4, the course of treatment is usually 5-7 days.

Known sulfanilamide preparations for topical use. These are mainly drugs of the I group - short-acting.

Mechanism of antibacterial action of sulfonamides

The mechanism of the antibacterial action of sulfonamides is reduced to blocking sensitive microorganisms in the cells. folic acid synthesis, necessary for the subsequent formation of para-aminobenzoic acid, necessary for their development and reproduction. Therefore, derivatives of para-aminobenzoic acid, for example novocaine, anestezin, incompatible with sulfonamides, as well as methionomyxin and some other substances are incompatible with sulfonamides, as they weaken their action.

Classification of sulfa drugs

The choice of sulfonamides for the treatment of a patient is associated with the properties of the pathogen, as well as individual drugs, in particular, the rate of their release from the body, which is associated with the degree of lipophilicity of sulfonamides. Based on this, sulfa drugs are divided into several subgroups.

Short acting sulfonamides

These drugs have an elimination half-life in the body of less than 10 hours:

  • streptocide;
  • sulfadiazine;
  • etazol;
  • sulfazol;
  • urosulfan;
  • sulfacyl;
  • some others, as well as their sodium salts.

Dosage

The dose for adults is usually about 1 g per dose 4-6 times a day. The course dose is up to 20-30 g. The course of treatment is up to 6-10 days.

In case of insufficient effectiveness of treatment sometimes 2-3 such courses are carried out, but in such cases it is better to use other chemotherapeutic drugs with a different spectrum and mechanism of action. The sodium salts of these sulfonamides, due to their greater solubility, are administered parenterally in the same doses.

Long acting sulfonamides

These drugs have a half-life of 24 to 48 hours:

  • sulfanylpyridazine and its sodium salt;
  • sulfadimethoxine;
  • sulfamonomethoxin, etc.

Dosage

Assign adults to 0.5-1 g 1 time per day.

Ultra long acting sulfonamides

These drugs have a half-life greater than 48 hours, often 60-120 hours:

  • sulfalene, etc.

Dosage

Assign according to two schemes: 1 time per day (the first day 0.8-1 g, the next 0.2 g) or 1 time per week at a dose of 2 g (more often in chronic diseases).

All drugs of these groups are rapidly absorbed in the intestines, which is why there is usually no need for their parenteral use, for which their sodium salts are prescribed. Sulfonamides are prescribed 30 minutes before a meal. Excreted mainly by the kidneys. For children, the dose is reduced accordingly.

Side effects of sulfa drugs

The most frequently observed side effects are dyspeptic and allergic.

Allergy

For allergic reactions prescribed antihistamines and calcium preparations especially gluconate and lactate. With minor allergic phenomena, sulfonamides are often not even canceled, which is necessary with more pronounced symptoms or more persistent complications.

Impact on the Central Nervous System

Possible phenomena from the central nervous system:

  • headache;
  • dizziness, etc.

Blood disorders

Sometimes there are changes in the blood:

  • agranulocytosis;
  • leukopenia, etc.

crystalluria

Everything side effects may be more persistent with the introduction of long-acting drugs that are more slowly excreted from the body. Because these poorly soluble drugs are excreted in the urine, they may form crystals in the urine. With an acid reaction of urine, it is possible crystalluria. To prevent this phenomenon, sulfa drugs should be taken with a significant amount of alkaline drink.

Sulfonamides contraindications

The main contraindications to the use of sulfa drugs are:

  • increased individual sensitivity individuals to sulfonamides (as a rule, to the whole group).

This may be indicated by anamnestic data on previous intolerance and other medicines different groups.

Toxic effect on the blood with other drugs

Do not take sulfonamides with other medicines providing toxic effect on the blood:

  • griseofulvin;
  • amphotericin preparations;
  • arsenic compounds, etc.

Pregnancy and sulfonamides

Due to easy cross-placental barrier sulfonamides undesirable for pregnant women especially in the first three and last months of pregnancy.

What can not be consumed with sulfonamides?

Prohibited drugs

Sulfonamides are incompatible with such drugs, due to the fact that they increase their toxicity:

  • amidopyrine;
  • phenacetin;
  • salicylates.

Forbidden foods

Sulfonamides are incompatible with certain foods containing the following chemicals:

  • sulfur:
    • eggs.
  • folic acid:
    • tomatoes;
    • beans;
    • beans;
    • liver.

ANTRIMA (Antrima)

Pharmachologic effect. Combined sulfanilamide drug. Sulfadiazine and trimethoprim have a bacteriostatic (preventing the growth of bacteria) and bactericidal (destroying bacteria) action, in combination their antimicrobial effect is enhanced. Highly sensitive to the drug: E. coli, Klebsiella, Enterobacter, Proteus, Citrobacter, Salmonella, Shigella, Haemophilus, Vibriocholerae, Listeria, Pneumocystiscarinii.

Indications for use. Bacterial infections caused by susceptible microorganisms, including respiratory tract infections, urinary tract infections, infections of the gastrointestinal tract (especially typhoid fever).

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Adults are prescribed 1 tablet 2 times a day with meals. For children, the drug is usually prescribed in the form of a suspension (suspension of solid particles of the drug in a liquid) - 1 attached measuring spoon (2.5 ml) per 5 kg of body weight 2 times a day with meals. The maximum daily dose is 8 scoops. Patients with creatinine clearance (the rate of blood clearance from final product nitrogen metabolism - creatinine) from 30 to 15 ml / min, the drug is prescribed only in case of hemodialysis (blood purification method), 1 time per day.

In the case of prolonged treatment with the drug, systematic monitoring of the picture of peripheral blood, kidney and liver function is necessary. When used in patients with diabetes it should be borne in mind that 2.5 ml of the drug contains 1 g of sucrose.

Side effect. Nausea, abdominal pain, thrombocytopenia (a decrease in the number of platelets in the blood),

neutropenia (decrease in the number of neutrophils in the blood), allergic reactions.

Contraindications. Deficiency of the enzyme glucose-6-phosphate dehydrogenase in erythrocytes (risk of increased hemolysis /destruction of erythrocytes/); pregnancy, breastfeeding; hypersensitivity to the components of the drug. The drug is not prescribed to premature and newborn children.

Release form. Tablets containing 0.4 g of sulfadiazine and 0.08 g of trimethoprim; oral suspension for children (2.5 ml - 0.1 g sulfadiazine and 0.02 g trimethoprim) in 50 ml vials.

Storage conditions. List B. In a dry, cool, dark place.

BISEPTOL (Biseptol)

Synonyms: Bactrim, Septrin, Abacin, Abactrim, Andoprim, Bacterial, Bacticel, Bactifer, Bactramin, Bactramel, Bactrizol, Berlocid, Hemitrin, Doctonil, Ectapprim, Ekspektrin, Falprin, Gantrin, Infectrim, Metomid, Microcetim, Nola "ps, Oradin, Oribact, Potecept, Primazol, Resprim, Septocid, Sumetrolim, Trimexazole, Trixazole, Uroxen, Vanadil, Aposulfatrin, Bactecod, Bactreduct, Blackson, Groseptol, Cotribene, Cotrim, Cotrimol, Eriprim, Primotren, Rancotrim, Sulfatrim, Trimezol, Expazole, Novotrimed, Oriprim, Sinersul, Cotrimaxol, Cotrimaxazole, Sulotrim, Trimosul, etc.

Combined drug containing two active ingredients: sulfanilamide drug sulfamethoxazole and diaminopyrimidine derivative - trimethoprim.

Pharmachologic effect. The combination of these two drugs, each of which has a bacteriostatic (preventing the reproduction of bacteria) effect, provides a high bactericidal (destroying

bacteria) activity against gram-positive and gram-negative microorganisms, including bacteria resistant to sulfanilamide preparations.

The bactericidal effect is associated with a double blocking effect of bactrim on the metabolism (metabolism) of bacteria. Sulfamethoxazole disrupts the biosynthesis of dihydrofolic acid, and trimethoprim blocks the next stage of metabolism - the restoration of dihydrofolic acid to tetrahydrofolic acid, which is necessary for the development of microorganisms. The choice of sulfamethoxazole as a component of bactrim is due to the fact that it has the same elimination rate (removal rate) with trimethoprim.

The drug is effective against streptococci, staphylococci, pneumococci, dysentery bacillus, typhoid fever, Escherichia coli, Proteus; ineffective against Mycobacterium tuberculosis, spirochetes, Pseudomonas aeruginosa.

The drug is rapidly absorbed when taken orally. The maximum concentration in the blood is observed 1-3 hours after ingestion and persists for 7 hours. High concentrations are created in the lungs and kidneys. It is excreted in a significant amount in the urine (within 24 hours, 40-50% of trimethoprim and about 60% of sulfamethoxazole are excreted, mainly in acetylated form).

Indications for use. Biseptol is used for respiratory tract infections: acute and chronic bronchitis (inflammation of the bronchi), pleural empyema (accumulation of pus between the membranes of the lungs), bronchiectasis (bronchial disease associated with the expansion of their lumen), abscess (abscess) of the lung, pneumonia (pneumonia) ; urinary tract: urethritis (inflammation of the urethra), cystitis (inflammation Bladder), pyelitis (inflammation of the renal pelvis), chronic pyelonephritis (inflammation of the tissue of the kidney and renal pelvis), prostatitis (inflammation of the prostate gland), gonococcal urethritis. It is also used for infections of the gastrointestinal tract, surgical infection and other infectious diseases. The drug is also effective in septicemia (a form of blood infection by microorganisms) caused by bacteria sensitive to the drug. The high efficacy of the drug in uncomplicated gonorrhea has been established.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Adults and children over 12 years of age are usually prescribed 4 tablets (or 2 forte tablets, or 8 measuring spoons of syrup) in a daily dose. The minimum daily dose for long-term therapy (more than 14 days) is 2 tablets (or 1 forte tablet, or 4 measuring spoons of syrup). The maximum daily dose (for the treatment of particularly severe cases) is 6 tablets (or 3 forte tablets, or 12 measuring spoons of syrup). The daily dose is divided into 2 doses (morning and evening). The drug is taken after meals with a sufficient amount of liquid. In acute infections, treatment with the drug is carried out for 5 days or until the patient has no symptoms of an infectious disease for 2 days.

For gonorrhea, the drug is prescribed for one day in a daily dose of 10 tablets (5 forte tablets, or 20 measuring beds of syrup), divided into 2 doses (morning and evening). In acute uncomplicated urinary tract infections in women, it is recommended to prescribe 2-3 forte tablets once. It is advisable to take the tablets in the evening after meals or before going to bed.

In pneumocystosis (an acute form of pneumonia; observed more often in weakened children of the first months of life) caused by Pneumocystiscarinii, sulfamethoxazole is prescribed in a daily dose of up to 0.1 g / kg of body weight and

trimethoprim up to 0.02 g/kg. Assign every 6 hours. The course of treatment is 14 days.

For children under 12 years of age, the drug is prescribed as a syrup in a daily dose of 0.03 g of sulfamethoxazole and 0.006 g of trimethoprim. The syrup is taken 2 times a day (morning and evening). In severe infections, the daily dose can be increased by about 50%.

For patients with impaired renal function, the dose is set depending on the amount of creatinine clearance (the rate of blood purification from the end product of nitrogen metabolism - creatinine). With a creatinine clearance greater than 30 ml / min, dose adjustment is not required; at 15-30 ml / min, half the usual dose is used; with a creatinine clearance of less than 15 ml / min, the drug is not recommended. Elderly patients may also require dose adjustment.

The drug should be used under close medical supervision.

Side effect. Nausea, vomiting, diarrhea (diarrhea), allergic reactions, nephropathy (a common name for some kidney diseases) are possible. Leukopenia (a decrease in the level of leukocytes in the blood) and agranulocytosis (a sharp decrease in the number of granulocytes in the blood) may develop.

Contraindications. Hypersensitivity to sulfonamides, diseases of the hematopoietic system, impaired liver and kidney function, pregnancy. The drug should not be given to premature babies and newborns. Bactrim should be used with caution in young children. When treating with the drug, it is necessary to carefully monitor the blood picture.

Release form. Tablets in a package of 20 pieces. The drug is available in tablets in two dosages: for adults, containing 0.4 g (400 mg) of sulfamethoxazole and 0.08 g (80 mg) of trimethoprim in one tablet; for children containing 100 mg of sulfamethoxazole and 20 mg of trimethoprim in one tablet.

For adults, tablets "bactrim forte" are also produced, containing 800 mg of sulfamethoxazole and 160 mg of trimethoprim, and for children - a syrup, 1 ml of which contains 40 mg of sulfamethoxazole and 8 mg of trimethoprim (suspension of white with a yellowish tinge in 100 ml vials ).

Storage conditions.

BACTRIM SUSPENSION (Bactrim)

Synonyms: Biseptol, Septrin, etc.

Pharmachologic effect. Combined drug. The combination of sulfamethoxazole and trimethoprim provides high efficiency against gram-positive and gram-negative microorganisms, including those resistant to sulfanilamide preparations. Bactrim is rapidly absorbed when taken orally. The maximum concentration in the blood is observed after 1-3 hours and persists for 7 hours.

Indications for use. Septicemia (a form of blood poisoning by microorganisms), infections of the respiratory, urinary tract and gastrointestinal tract caused by microorganisms sensitive to the drug, etc.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Assign inside after meals (morning and evening). Doses are set depending on the age of the child: from 6 weeks. up to 5 months - "/2 teaspoons 2 times a day; from 6 months to 5 years - 1 teaspoon 2 times a day; from 5 to 12 years - 2 teaspoons 2 times a day.

Side effect. Nausea, vomiting, allergic reactions, leukopenia (a decrease in the level of leukocytes in the blood) and agranulocytosis (a sharp decrease in the number of granulocytes in the blood). Treatment is carried out under the control of the blood picture.

Contraindications.

Release form. Suspension (syrup) in vials of 100 ml. The composition of the suspension (based on 5 ml) includes the following substances: sulfamethoxazole-3 (paminobenzenesulfamido) -5-methylisoxazole - 0.2 g; trimethoprim - 2,4-diamino-5-(3,4,5-trimethoxybenzyl) -pyrimidine - 0.04 g.

Storage conditions. List B. In a dry cool dark place.

Lidaprim (Lidaprim)

Pharmachologic effect. Combined preparation containing sulfametrol and trimethoprim. Sulfametrol has a high antibacterial activity, and in combination with trimethoprim (see Biseptol) provides a bactericidal (destroying bacteria) effect against gram-positive and gram-negative microorganisms, including bacteria that are resistant to conventional sulfanilamide drugs.

Indications for use. Indications for the use of lidaprim basically coincide with the indications for the use of biseptol.

Lidaprim is effective in infections of the respiratory tract, ear, throat and nose of the kidneys and urinary tract and gastrointestinal tract, with prostatitis (inflammation of the prostate gland), gonorrhea, gynecological infectious diseases and other infections caused by pathogens sensitive to the drug.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Adults and children over 12 years of age are prescribed the drug orally, usually starting with 2 tablets of lidaprim or 1 tablet of lidaprim forte 2 times a day (morning and evening). Take until the disappearance of acute manifestations of infection (at least 5 days); then 1 tablet or V2 tablets of lidaprim forte 2 times a day.

Patients with chronic pyelonephritis (inflammation of the tissue of the kidney and renal pelvis) and with chronic salmonella carriage are prescribed 2 tablets of lidaprim or 1 tablet of lidaprim forte 2 times a day for a long time (on average 3 months).

In case of gonorrhea, 4 tablets of lidaprim forte are usually prescribed once a day.

In acute infections, you can start with an intravenous infusion of a solution of lidaprim; enter slowly 250 ml (1 vial) 2 times a day.

Children under the age of 2 years are prescribed "/2 teaspoons of suspension 2 times a day, from 2 to 3 years - 1 teaspoon of suspension or 2 tablets for children 2 times a day; 3-6 years old - 1" / 2 teaspoons or 3 tablets for children per day; 6-12 years - 2 teaspoons or 4 tablets for children 2 times a day.

Side effects and contraindications are the same as Biseptol.

Release form. Lidaprim is available in different dosage forms: a) Lidaprim tablets containing 400 mg of sulfametrol and 80 mg of trimethoprim, in a package of 20 or 100 pieces; b) tablets of lidaprim forte, coated, containing 800 mg of sulfametrol and 160 mg of trimethoprim, in a package of 10; 25 or 50 pieces; c) lidaprim tablets for children, containing 100 mg of sulfametrol and 20 mg of trimethoprim, in a package of 20 pieces; d) suspension of lidaprim (for children), containing 5 ml (1 teaspoon) of 200 mg of sulfametrol and 40 mg of trimethoprim, in vials of 50 and 100 ml; e) solution for injection (infusion) in 250 ml glass vials containing 800 mg of sulfametrol and 160 mg of trimethoprim.

Storage conditions.

MAFENID (Maphenidum)

Synonyms: Ambamide, Bensulfamidine, Homosulfamidine, Sulfamilone, Mafenide acetate, etc.

Sulfanilamide antibacterial drug for outdoor use. Available as mafenide acetate.

Pharmachologic effect. Mafenide acetate has a wide spectrum of action, effective against gram-positive and gram-negative bacteria and pathogenic (pathogenic) anaerobes (microorganisms that can exist in the absence of oxygen), pathogens of gas gangrene. It is not inactivated by para-aminobenzoic acid and does not change activity in an acidic environment.

Indications for use. It is used to treat infected burns, purulent wounds, bedsores (tissue necrosis caused by prolonged pressure on them due to lying), trophic ulcers (slowly healing skin defects).

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Ointment (10%) is applied directly to the affected surface, swabs soaked in ointment are introduced into the cavity, napkins smeared with ointment with a layer of 2-3 mm are also applied to the wounds. Usually, 30-70 g of ointment is used per bandage. Before applying a bandage, the wound is cleaned of purulent-necrotic masses (inflamed necrotic / dead / tissues). Dressings are changed daily or 2-3 times a week, depending on the amount of purulent discharge. The duration of treatment is from 1 to 4-5 weeks.

For second-degree burns, a single dressing may be applied.

Side effect. When applying the ointment to a burn or wound surface, burning, pain can be observed, lasting from "/2 to 1-3 hours; with severe pain prescribe analgesics (painkillers).

Contraindications. The use of the ointment is contraindicated if there is a history (medical history) of data on toxic-allergic reactions to sulfanilamide preparations.

Release form. 10% ointment in light-protective glass jars of 50 g and 2 kg.

Storage conditions.

ALGIMAF (Algimafum)

Lyophilized gel (iron dosage form, dehydrated by freezing in a vacuum) sodium-calcium salt of alginic acid containing mafenide and other substances.

Pharmachologic effect. Shows adsorbing (absorbing) and antimicrobial activity, cleans wounds, promotes regeneration (recovery) of tissues.

Indications for use. Applied with superficial burns of 2 and 3 degrees, long-term non-healing ulcers and wounds.

Method of application and dose. Impose on the affected surface (after treatment) a plate of the appropriate size. Fix with a gauze bandage or bandage. It can be left in the wound until the end of epithelialization (recovery of the skin surface or mucous membrane).

Side effect. Passing burning sensation.

Release form. Sterile porous sheets from 50x50 to 135x250 mm and 10 mm thick in bags,

Storage conditions. List B. In a dry, dark place, without bending the packages and protecting them from mechanical damage.

NORSULFAZOL (Norsulfazolum)

Synonyms: Sulfathiazole, Amidothiazole, Aseptosil, Azoseptal, Cibazol, Eleudron, Polyseptil, Pirisulfone, Thiazamide, etc.

Pharmachologic effect. Sulfanilamide drug. It is effective in infections caused by hemolytic streptococcus, pneumococcus, gonococcus, staphylococcus, and also Escherichia coli.

Indications for use. Pneumonia (pneumonia), cerebral meningitis (purulent inflammation of the meninges), gonorrhea, staphylococcal and streptococcal sepsis (blood infection with microbes / streptococci / from the focus of purulent inflammation), dysentery, etc.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Taken inside. For pneumonia and meningitis, the first dose is 2 g, then 1 g every 4-6 g (course dose 20-30 g); with staphylococcal infections at the first dose 3-4 g, then 1 g 4 times a day for 3-6 days. In the treatment of dysentery, 6-4-3 g per day according to a special scheme.

Norsulfazol is prescribed to children every 4-6-8 hours in the following single doses: at the age of 4 months. up to 2 years - 0.1-0.25 g each, from 2 to 5 years - 0.3-0.4 g each, from 6 to 12 years old - 0.4-0.5 g each. double dose.

Side effect. Possible dyspeptic disorders (digestive disorders), allergic reactions, leukopenia (decrease in the level of leukocytes in the blood), neuritis (nerve inflammation), impaired renal function (crystalluria - the presence of salt crystals in the urine).

Contraindications. Hypersensitivity to sulfa drugs.

Release form. Powder; tablets in packs of 10 pieces of 0.25 g and 0.5 g with a score.

Storage conditions. List B. In a dry, dark place.

Norsulfazol is also included in the preparations of inhalipt, sunoref ointment.

NORSULFAZOL-SODIUM (Norsulfazolum-natrium)

Synonyms: Sulfathiazole sodium, Sulfathiazole sodium, Norsulfazol soluble.

Sodium salt of norsulfazole.

Indications for use. The same as for norsulfazole. In addition, with infectious diseases of the eyes.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Intravenously administered in cases where the possibility of introducing nosulfazole into the stomach is excluded (for example, after surgery on gastrointestinal tract, with vomiting and unconsciousness of the patient) and if it is necessary to quickly create a high concentration of the drug in the blood. As soon as the patient's condition allows, they switch to taking the drug inside.

A 5% or 10% solution is injected into a vein; appoint at the rate of 0.5-1.0-2.0 g per infusion (10-20 ml of a 5% or 10% solution; pour slowly). It is advisable to further dilute solutions of norsulfazole soluble in 5% glucose solution or in isotonic sodium chloride solution. When using concentrated solutions, the possibility of phlebitis (inflammation of the vein) at the injection site should be considered. Subcutaneous and intramuscular solutions are not prescribed, as they can cause tissue irritation up to necrosis (tissue necrosis).

Also used in the form of eye drops (10% solution, 2 drops 3-4 times a day) for conjunctivitis (inflammation outer shell eyes), blepharitis (inflammation of the edges of the eyelids) and other infectious eye diseases. Can be taken orally.

Higher doses for adults inside: single - 2 g, daily - 7 g.

Side effects and contraindications. Same as for norsulfazole.

Release form. Powder.

Storage conditions. List B. In a dry, dark place.

Salazodimethoxin (Salazodimethoxintun)

Pharmachologic effect. Sulfanilamide of the prolonged (long) action. - Like salazopyridazine, the drug breaks down in the intestines, with the formation of 5-aminosalicylic acid and sulfadimethoxin, which have anti-inflammatory and antibacterial action. The drug has low toxicity.

Indications for use. Non-specific ulcerative colitis (chronic inflammation of the colon with the formation of ulcers, caused by unclear reasons) in the active stage, mainly in mild and moderate forms of the disease, poor tolerance or ineffectiveness of salazopyridazine.

Method of application and dose. Assign inside (after eating) in approximately the same doses and for the same period as salazopyridazine. Usually give adults 0.5 g 4 times a day (1 g 2 times a day) for 3-4 weeks, and then (if a therapeutic effect has occurred during this period) 0.5 g 2-3 times a day day for the next 2-3 weeks. In severe forms of the disease, the daily dose is increased in the first days to 4 g, and after a decrease in the frequency of stools, the dose is reduced. In mild forms of the disease, you can start with a dose of 1.5 g per day, and if there is no effect, go to 2 g per day.

Children aged 3 to 5 years in the first 7-14 days are prescribed 0.5 g per day, in the next 2 weeks. - 0.25 g per day, on other days (until the 40th - 50th day from the start of treatment) - 0.125 g per day; children from 5 to 7 years old - respectively, 0.8-1.0 g each; 0.4-0.5 g and 0.2-0.25 g; from 7 to 15 years - 1.0-1.5 g; 0.5-0.75 g and 0.25-0.375 g. Daily doses are given in 2-3 doses.

If during the first 14 days from the start of treatment it is not possible to obtain a therapeutic effect, salazodimethoxine is canceled; you can switch to the use of salazopyridazine or salazosulfapyridine.

To prevent recurrence (reappearance of signs of the disease) of ulcerative colitis and Crohn's disease (a disease of unknown cause, characterized by inflammation and narrowing of the lumen of certain sections of the intestine), salazodimethoxine is prescribed for a long time in gradually decreasing doses: for adults, 0.5 g 1-2 times a day, daily for 2-6 months, then 0.25-0.5 g daily or every other day for 6-12 months. For children, the drug is prescribed in smaller

doses, taking into account age and doses used in the acute period of the disease. In case of deterioration of health, the dose of salazodimethoxin is increased,

Side effect. Allergic reactions, leukopenia (decrease in the level of leukocytes in the blood), dyspeptic disorders (digestive disorders).

Contraindications. Hypersensitivity to sulfonamides.

Release form.

Storage conditions. List B. In a dark place.

Salazopyridazine (Salazopyridazinum)

Synonyms: Salazodin.

Pharmachologic effect. Sulfanilamide drug. It has anti-inflammatory and immunosuppressive (suppressing the body's defenses) effect.

Indications for use. Non-specific ulcerative colitis (chronic inflammation of the colon with the formation of ulcers, caused by unclear reasons), as well as in diseases that occur with autoimmune disorders (disorders based on allergic reactions to the body's own tissues or waste products), including as a basic drugs in therapy rheumatoid arthritis(an infectious-allergic disease from the group of collagenoses, characterized by chronic progressive inflammation of the joints).

Method of application and dose. In ulcerative colitis, salazopyridazine is prescribed for adults inside (after meals) in tablets of 0.5 g 4 times a day for 3-4 weeks. If during this period a therapeutic effect is manifested, the daily dose is reduced to 1.0-1.5 g (0.5 g 2-3 times a day) and treatment is continued for another 2-3 weeks. If there is no effect, the drug is stopped. Patients with mild forms of the disease are prescribed the drug first at a daily dose of 1.5 g, and if there is no effect, the dose is increased to 2 g per day.

For children aged 3 to 5 years, salazopyridazine is prescribed, starting with a dose of 0.5 g per day (2-3 doses). If there is no effect within 2 weeks. the drug is canceled, and if there is a therapeutic effect, treatment is continued at this dose for 5-7 days, then the dose is reduced by 2 times and treatment is continued for another 2 weeks. In the case of clinical remission (temporary weakening or disappearance of the manifestations of the disease), the daily dose is again halved and prescribed until the 40-50th day, counting from the start of treatment.

Children aged 5 to 7 years are prescribed the drug, starting with 0.75-1.0 g per day; from 7 to 15 years - with a dose of 1.0-1.2-1.5 g per day. Treatment and dose reduction are carried out according to the same scheme as in children from 3 to 5 years.

The use of salazopyridazine is combined with the general treatments and diet recommended for ulcerative colitis.

Salazopyridazine can also be used rectally (into the rectum) in the form of suspensions (suspensions of solid particles in a liquid) and suppositories.

Suspension of salazopyridazine 5% is used for rectal administration with damage to the rectum and sieve, in the preoperative period and after subtogal colectomy (after removal of part of the colon), with poor tolerance of the drug in the form of tablets. The suspension is slightly warmed up and injected as an enema into the rectum or into the stump of the intestine, 20-40 ml each.

1-2 times a day. Children are administered 10-20 ml (depending on age). Rectal administration can be combined with oral administration.

Candles are used rectally. In the acute stage of the disease, 1 suppository is prescribed 2-4 times a day for 2 weeks. up to 3 months The duration of the course depends on the effectiveness of treatment and tolerability of the drug. The maximum daily dose is 4 suppositories (2 g). At the same time, you can take salazopyridazine tablets (not exceeding a total daily dose of 3 g) and other drugs for the treatment of ulcerative colitis.

In order to prevent relapses (reappearance of signs of the disease), 1-2 suppositories are prescribed per day for 2-3 months.

Doses and regimen of the drug in other forms of colitis with ulcerative lesions are the same as in nonspecific ulcerative colitis.

Side effect. When taking salazopyridazine tablets orally, the same adverse reactions that when using sulfonamides and salicylates: allergic phenomena, leukopenia (decrease in the level of leukocytes in the blood), dyspeptic disorders (digestive disorders), sometimes a slight decrease in the level of hemoglobin (the functional structure of the erythrocyte, which ensures its interaction with oxygen). In such cases, the dose should be reduced or the drug discontinued. After the introduction of the suspension, a burning sensation in the rectum and the urge to defecate (empty bowel) may appear, especially with rapid administration. When using salazopyridazine in suppositories, there may be a burning sensation and soreness in the rectum, sometimes an increase in stool. In case of severe pain during rectal administration of salazopyridazine in suppositories, it is recommended to prescribe the drug rectally in the form of a 5% suspension and orally in tablets.

Contraindications. The drug is contraindicated in the presence of a history (medical history) of data on toxic-allergic reactions in the treatment of sulfonamides and salicylates.

Release forms. Tablets of 0.5 g in a package of 50 pieces; 5% suspension in 250 ml vials containing salazopyridazine, tween-80, benzyl alcohol and polyvinyl alcohol (the drug after shaking is an orange suspension, which then settles); candles (brown) 0.5 g per pack of 10 pieces.

Storage conditions. List B. In a place protected from light at room temperature.

Salazosulfaliridine (Salazosulfapyridinum)

Synonyms: Sulfasalazine, Azopyrine, Azufidin, Salazopyridine, Salazopyrin, Salicylazosulfapyridine, Salisulf.

Pharmachologic effect. The drug has an antibacterial effect against diplococci, streptococci, gonococci, Escherichia coli. A feature of the drug is that it has a pronounced therapeutic effect in patients with nonspecific ulcerative colitis ( chronic inflammation colon with ulceration of unknown cause). The mechanism of this action is not fully understood. A certain role is played by the ability of the drug to accumulate in the connective tissue (including the intestinal tissue) and gradually separate 5-aminosalicylic acid and sulfapyridine, which have anti-inflammatory and antibacterial properties.

Indications for use. Nonspecific ulcerative colitis, rheumatoid arthritis (an infectious-allergic disease from the group of collagenoses, characterized by chronic progressive inflammation of the joints).

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Assign inside. It is recommended on the 1st day for adults 1 tablet (0.5 g) Phrase per day (at regular intervals), on the 2nd day - 2 tablets 4 times and on subsequent days in case of good tolerance of the drug - 3-4 times tablets 4 times a day. After the subsidence clinical symptoms diseases are prescribed maintenance doses (1.5-2.0 g per day) for several months.

For children, salazosulfapyridine is prescribed in smaller doses: at the age of 5-7 years - 1/2-1 tablet (0.25-0.5 g) 3-6 times a day, over 7 years old - 1 tablet (0.5 g ) 3-6 times a day.

Salazosulfapyridine is also effective in mild to moderate forms of Crohn's disease (a disease of unknown cause, characterized by inflammation and narrowing of the lumen of certain sections of the intestine)

Salazosulfapyridine is also used as a basic agent in the treatment of rheumatoid arthritis due to the presence of immunocorrective properties in the drug (restoring immunity / body defenses /). Assign 2-3 g per day (40 mg / kg per day) for 2-6 months.

Treatment should be carried out under close medical supervision; it is necessary to systematically monitor the blood picture.

Side effect. Nausea, vomiting, headache, dizziness may occur. In such cases, cancel the drug, and after 2 days gradually, within 3 days, again increase the dose. Allergic reactions in the form of skin rashes, drug fever (a sharp rise in body temperature in response to taking the drug); leukopenia (decrease in the level of leukocytes in the blood). In these cases, the drug should be discontinued. The drug is excreted in the urine and, with an alkaline reaction, stains it in a yellow-orange color.

Contraindications. Severe toxic-allergic reactions in history (previously) to sulfonamides.

Release form. Tablets of 0.5 g in a package of 50 pieces.

Storage conditions. List B. In a dry, dark place.

Streptocid (Streptocidum)

Synonyms: Sulfanilamide, Streptocid white, Ambezid, Deseptil, Dipron, Prontalbin, Prontalin, Prontoin, Prontosil white, Streptamine, Streptozol, Sulfamidil, etc.

Pharmachologic effect. Sulfanylamide drug. It has an antimicrobial effect against streptococci, meningococci, gonococci, pneumococci, Escherichia coli and some other bacteria.

Indications for use. Erysipelas, tonsillitis, epidemic cerebrospinal meningitis (purulent inflammation of the membranes of the brain), cystitis (inflammation of the bladder), pyelitis (inflammation of the renal pelvis), colitis (inflammation of the colon:), wound infection.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Inside, 0.5-1 g 5-6 times a day. Doses for children

decrease according to age. Higher doses for adults inside: single - 2 g, daily - 7 g.

Locally injected into the wound 5-15 g of sterile powder; externally in the form of 5% liniment or 10% ointment.

Side effect. Headache, dizziness, nausea, vomiting, cyanosis (blue skin and mucous membranes), allergic reactions, leukopenia (decrease in the level of leukocytes in the blood), agranulocytosis (a sharp decrease in the number of granulocytes in the blood), paresthesia (numbness in the limbs), tachycardia (rapid heartbeat ).

Contraindications. Diseases of the hematopoietic system, kidneys, Graves' disease (disease thyroid gland), hypersensitivity to sulfonamides.

Release form. Powder; tablets in a package of 10 pieces of 0.3 g and 0.5 g; 5% liniment in a package of 50 g; ointment 10% in a package of 30 g.

Storage conditions. List B. In a dry, dark place.

STREPTOCIDA LINIMENT 5% (LinimentumStreptocidi5%)

Indications for use. To accelerate the healing of infected wounds, burns of I and II degrees, boils (purulent inflammation of the hair follicle of the skin that has spread to surrounding tissues), carbuncles (acute diffuse purulent-necrotic inflammation of several adjacent sebaceous glands and hair follicles), with superficial pyoderma (purulent inflammation of the skin), acne vulgaris, impetigo (superficial inflammation of the skin, characterized by the appearance of ulcers that dry out with the formation of crusts) and other pyoinflammatory skin diseases.

Method of application and dose. Before prescribing the drug to the patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Liniment is applied to the lesion (under a gauze bandage) 1-2 times a day.

Side effects and contraindications are the same as for streptocide.

Release form. in tubes or glass jars by 30

Storage conditions. In a dry, cool place; banks - in a place protected from light.

"SUNOREF" OINTMENT (Unguentum "Sunoreph")

Indications for use. Acute and chronic rhinitis (inflammation of the nasal mucosa).

Method of application and dose. Locally (lubricate the mucous membranes of the nose).

Side effect. Allergic reactions are possible.

Contraindications. Hypersensitivity to sulfa drugs.

Release form. Ointment composition: streptocide - 5 g, norsulfazol - 5 g, sulfadimezin - 5 g, ephedrine hydrochloride - 1 g, camphor - 3 g, eucalyptus oil- 5 drops, ointment base - up to 100 g, in a package of 15 g.

Storage conditions. In a cool place.

Streptocid is also part of the drug osarcid.

STREPTOCID SOLUBLE (Streptocidumsolubile)

Pharmachologic effect. Sulfanilamide drug. (See Streptocide).

Indications for use. Epidemic, cerebrospinal meningitis (purulent inflammation of the meninges), erysipelas, tonsillitis, cystitis (inflammation of the bladder), pyelitis (inflammation of the renal pelvis), colitis (inflammation of the large intestine), wound infection. The purpose of the drug is especially indicated for vomiting or unconsciousness of the patient.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Subcutaneously, intramuscularly up to 100 ml of 1-1.5% solution 2-3 times a day; intravenously up to 20-30 ml of 2%, 5% or 10% solution.

Side effects and contraindications are the same as for streptocide.

Release form. Powder.

Storage conditions. List B. In a dry, dark place.

Streptocide soluble is also part of the drug inhalipt.

SULGIN (Sulginum)

Synonyms: Sulfaguanidine, Abiguanil, Aseptiguamidine, Ganidan, Guamid, Guanicil, Guasept, Neosulfonamide, Resulfon, Sulfaguanisan, etc.

Pharmachologic effect. Sulfanilamide drug. Sulgin is very slowly absorbed. The main amount of the drug taken orally is retained in the intestine and excreted in the feces. Is an effective tool for the treatment of intestinal infections. Similar in action to phthalazole.

Indications for use. Bacillary dysentery, colitis (inflammation of the large intestine) and enterocolitis (inflammation of the small and large intestine) with diarrhea, carriage of Shigella and typhoid fever bacilli, preparation for intestinal surgery.

Method of application and dose. Inside, 1-2 g 6-5-4-3 times a day (on the first day - 6 times; in 2 and 3 - 5; in 4 - 4, and in 5 - 3 times a day).

Children under 3 years old - 0.2 g / kg per day in 3 divided doses for 7 days; children over 3 years old - 0.4-0.75 g (depending on age) 4 times a day.

For the prevention of postoperative complications in the intestines, 0.05 g / kg every 8 hours for 5 days before surgery and 7 days after surgery.

Higher doses for adults inside: single 2 g, daily 7 g.

Side effect. Possible nausea, vomiting, crystalluria (the presence of salt crystals in the urine).

Contraindications. Hypersensitivity to sulfonamides, impaired renal function.

Release form.

Storage conditions. List B. In a dry, light-protected place.

SULFADIMESIN (Sulfadimezinum)

Synonyms: Sulfadimidine, Diazyl, Diazol, Dimetazil, Dimethyldebenal, Dimethylsulfadiazine, Dimethylsulfapyrimidine, Primazine, Sulfadimerazine, Sulfamethazine, Sulfamesatil, Sulfamesatin, Sulmet, Sulfadimethylpyrimidine, Superseptil.

Pharmachologic effect. Sulfanilamide drug. Active against pneumococci, meningococci, streptococci, gonococci, Escherichia coli and some other microorganisms.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity

to him the microflora that caused the disease in this patient. Inside, 1 g 4-6 times a day. With pneumonia and meningitis, 2 g is prescribed for the first appointment; children at the rate of 0.1 g / kg for the first dose, then 0.25 g / kg every 4, 6, 8 hours. Higher doses for adults inside: single 2 g, daily 7 g.

For the treatment of dysentery in adults on the 1st-2nd day - 1 g 6 times; on the 3rd-4th day - 1 g 4 times; on the 5-6th day - 1 g 3 times a day. The course dose is 25-30 g. After a 5-6 day break, repeat the course of treatment for 5 days, the course dose is 21 g of the drug. With dysentery for children under 3 years old - up to 0.2 g / kg per day in 4 divided doses for 7 days; children over 3 years old - 0.4-0.75 g (depending on age) 4 times a day.

Side effect. Nausea, vomiting, allergic reactions, leukopenia (a decrease in the level of leukocytes in the blood), agranulocytosis (a sharp decrease in the number of granulocytes in the blood), crystalluria (the presence of salt crystals in the urine) are possible.

Contraindications. Hypersensitivity to sulfonamides, diseases of the hematopoietic system, impaired renal function.

Release form. Powder; tablets of 0.5 g in a package of 10 pieces.

Storage conditions. List B. In a place shielded from the light.