Private reactions of authenticity. Pharmaceutical chemistry - Kulbakh V.O Norsulfazol chemical name

Norsulfazole

Sulfacetamidum natrium

Sodium sulfacetamide (sulfacyl sodium)

(Sulfacylum natrium)

2-para-Aminobenzenesulfanyl acetamide-sodium

Description. White crystalline powder, odorless, soluble in water, has low alkalinity of solutions, practically insoluble in alcohol.

Determination of authenticity.

a) the reaction of diazotization and azo coupling with phenols (formation of an azo dye).

b) condensation reaction with aldehydes (formation of colored Schiff bases).

1.2.Specific, saponification of the drug when heated with hydrochloric acid (smell of acetic acid).

+ HCI→ CH 3 COOH+ NaCI+

1.3.Reaction caused by the imide group with solutions of heavy metal salts. Sodium sulfacetamide with a solution of copper sulfate forms a bluish-greenish precipitate that does not change when standing (unlike other sulfonamide drugs)

Quantitation.

1. Using the nitritometry method for the primary aromatic amino group.

2. Using the neutralization method (acidimetry) as a salt of a strong base and a weak acid. Titration is carried out in a mixture of alcohol and acetone to prevent the possibility of hydrolysis. Indicator - methyl orange.

Titrant is a standard solution of hydrochloric acid.

3.Bromatometric method, based on the ability of sulfonamides to halogenate; The standard solution is potassium bromate; titration is carried out in an acidic medium in the presence of potassium bromide. Excess bromine is determined iodometrically;

Application. It is used in the form of 20-30% solutions and ointments (30%). For streptococcal, gonococcal, pneumococcal and coli-bacillary infections.

Storage. The drug should be stored in a container protected from light, in a cool, dark place.

2-(para-aminobenzenesulfamido)-thiazole

Description. White or slightly yellowish crystalline powder, insoluble in water, slightly soluble in a number of organic solvents. Being an amphoteric substance, it dissolves in solutions of acids and alkalis.

Authenticity reactions.

1.1.For the primary aromatic amino group:

a) reaction of diazotization and azo coupling with phenols

b) condensation reaction with aldehydes (formation of a Schiff base).

1.2.Reactions caused by the imide group. With a solution of copper sulfate it forms a dirty purple precipitate. Previously, norsulfazole is converted into a sodium salt by dissolving it in a 0.1 mol/l NaOH solution (distinctive from other sulfonamides).

1.3.The pyrolysis reaction is distinctive from other sulfonamides. This reaction proves the sulfide sulfur in the thiazole ring. When norsulfazole is heated in a dry test tube, a brown melt appears and the smell of hydrogen sulfide appears.

H 2 S can also be determined by the blackening of filter paper moistened with a solution of lead acetate - (PbS).

quantitation

1. Nitritometry method.

2.Bromatometry method of back titration.

3. Argentometry method. This method can be used for the quantitative determination of drugs that form silver salts (potassium chromate as indicator). To reduce the concentration of hydrogen ions (dissolving sediment), the reaction is carried out in the presence of borax:

4. Neutralization method (alkalimetry), based on the ability of sulfonamides to exhibit acidic properties due to the presence of a hydrogen atom in the imide group; acid forms of sulfonamides are titrated in an alcoholic medium with a standard NaOH solution with thymolphthalein indicator.

Application. Used for infections caused by hemolytic streptococcus, pneumococcus, gonococcus, staphylococcus, and E. coli.

Available in powder and tablets of 0.25 and 0.5 g.

The highest single dose is 2 g, the highest daily dose is 7 g.

Storage. In a well-closed container (powder), tablets as indicated on the label..

In 1 tablet sulfathiazole 250 mg or 500 mg.

Release form

Powder, tablets.

pharmachologic effect

Antimicrobial.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

The Pharmacopoeia defines norsulfazole as antibacterial agent . It is a synthetic derivative of sulfanilic acid amide - sulfonamide . The formula of norsulfazole is C9H9N3O2S2.

The mechanism of action is explained by the similarity in structure with para-aminobenzoic acid , which is necessary for the reproduction of microorganisms.

Depressing dihydropteroate synthetase , disrupts synthesis tetrahydrofolic acid . As a result, the synthesis of nucleic acids is inhibited, which inhibits the proliferation of microorganisms.

Currently some strains staphylococci , streptococci , meningococci, pneumococci And gonococci have acquired resistance to the drug. Its activity remains in relation to nocardium , toxoplasma , malarial plasmodia , chlamydia And actinomycetes fungi . The advent of antibiotics has reduced interest in sulfonamides.

Pharmacokinetics

Norsulfazole is a well-absorbed, short-acting sulfonamide. Binds to blood proteins by 55%. Metabolized in the liver. Excreted by the kidneys - 20% are acetyl derivatives that precipitate when the urine is acidic (crystalluria). T1/2 is 3.5 hours, so it is prescribed every 6 hours.

Indications for use

Pneumonia , diseases of the biliary tract, staphylococcal And streptococcal sepsis .

Contraindications

increased sensitivity;
pregnancy;
suppression of bone marrow function.

Side effects

allergic manifestations;
leukopenia ;
digestive disorders;
neuritis ;
crystalluria ;
bone marrow suppression.

Instructions for use of Norsulfazole (Method and dosage)

The use of sulfonamides has recently decreased, since they are inferior in activity to antibiotics. In addition, most microorganisms are resistant to them. Norsulfazole can only be used if antibiotics are intolerant.

At pneumonia taken orally - immediately 2 g, then 1 g after 4-6 hours, when staphylococcal infections- 3-4 g, then 1 g 4 times a day. The highest single dose for adults is 2 g, daily dose is 7 g. For prevention crystalluria Alkaline drinking is recommended.

Norsulfazole sodium or norsulfazole soluble is a powder that can be used orally and also administered intravenously in the form of a 5% or 10% solution (in glucose solution). Concentrated solutions can cause phlebitis. It is not prescribed subcutaneously or intramuscularly, as it can cause. It is used as instillation for infectious eye diseases.

Veterinary medicine has Norsulfazole for animals in its arsenal: 0.5 g tablets, poorly soluble in water, packaged in jars of 1000 pieces or soluble powder.

Prescribed when pleurisy , pneumonia , strepto- And staphylococcal sepsis , enteritis , mastitis , colibacillosis , toxoplasmosis , salmonellosis , pasteurellosis , eimeriosis . In combination with Phthalazole it is used for prevention coccidiosis . Externally for purulent wounds it is used in the form of powders, ointments and emulsions.

The drug is administered to animals orally 2-3 times a day in a mixture with food for 3-6 days. The dose of the drug is 0.025-0.05 g per kg of weight. The initial dose is 2 times higher. Animals are not limited in their intake of water. To increase the effectiveness of treatment, norsulfazole is prescribed in combination with antibiotics.

Overdose

Manifested by nausea, vomiting, increased sweating, bronchospasm, crystalluria with symptoms renal colic .

Treatment is undertaken: gastric lavage, drinking plenty of fluids, symptomatic therapy.

Interaction

Aminoglycosides enhance the antimicrobial effect. Antacids And reduce the absorption of sulfonamides. The hematotoxicity of the drug increases when taken simultaneously with other myelotoxic drugs . The use of large doses is undesirable. Effect indirect anticoagulants significantly enhanced when combined with sulfonamides.

Terms of sale

Dispensed by prescription.

Storage conditions

At a temperature of no more than 250 C.

Best before date

Norsulfazole analogues

Level 4 ATX code matches:

Analogs Sulfathiazole , Sulfathiazole sodium have the same release form and active ingredient.

). 2-(para-Aminobenzenesulfamido)-thiazole. Synonyms: Amidotiazol, Aseptosil, Azoseptale, Cibazol, Eleudron, Poliseptil, Pyrisulfon, Sulfathiazole, Sulphathiazolum, Thiazamide, etc. White or white with a slightly yellowish tint, odorless crystalline powder. Very little soluble in water, little in alcohol, soluble in diluted mineral acids and solutions of caustic and carbonic alkalis. Norsulfazole is effective against infections caused by hemolytic streptococcus, pneumococcus, gonococcus, staphylococcus, and E. coli. The drug is easily absorbed from the gastrointestinal tract and quickly excreted from the body. It is excreted primarily in the urine, mainly in a free, non-acetylated form. Used internally for pneumonia, meningitis, staphylococcal and streptococcal sepsis and other infectious diseases. For pneumonia and meningitis, adults are prescribed 2 g for the first dose, then 1 g every 4 to 6 hours until the body temperature decreases; in the future, take 1 g every 6 - 8 hours. In total, during the course of treatment the patient takes 20 - 30 g of the drug. For staphylococcal infections, 3-4 g are prescribed for the first dose, and then 1 g 4 times a day. The course of treatment lasts 3 - 6 days. For patients with dysentery, the drug is prescribed in the same way as sulfadimezin (see). For children, norsulfazole is prescribed every 4 - 6 - 8 hours in the following single doses: from 4 months to 2 years - 0.1 - 0.25 g, from 2 to 5 years - 0.3 - 0.4 g, from 6 to 12 years - 0.4 - 0.5 g. For the first dose, give a double dose. Higher doses for adults orally: single 2 g, daily 7 g. When using norsulfazole, it is recommended to maintain increased diuresis (introducing 2 - 3 liters of liquid into the body per day: after each dose of the drug, drink 1 glass of water with the addition of 1/2 teaspoon of sodium bicarbonate or a glass of Borjomi). The drug is usually well tolerated, but nausea and, in rare cases, vomiting are possible. Due to the advent of more effective chemotherapeutic agents, the use of norsulfazole is relatively limited. Release forms: powder; tablets of 0.25 and 0.5 g in a package of 10 pieces. Storage: List B. In a well-closed container.

Dictionary of medicines. 2005 .

Synonyms:

See what "NORSULFAZOLE" is in other dictionaries:

Norsulfazole... Spelling dictionary-reference book

Noun, number of synonyms: 1 medicine (1413) ASIS Dictionary of Synonyms. V.N. Trishin. 2013… Synonym dictionary

NORSULFAZOLE- Norsulfazolum. Synonyms: azoseptol, sulfathiazole, thiazamide, cibazole. Properties. White or slightly yellowish crystalline powder, poorly soluble in water and slightly soluble in alcohol. Release form. Available in powder and tablets of 0.25 and 0.5 g. Effective... Domestic veterinary drugs

NORSULFAZOLE- (Norsulfazolum; PC, list B), an antibacterial agent from the sulfonamide group. White or white with a slightly yellowish tint, odorless crystalline powder. Very slightly soluble in water, slightly soluble in alcohol, soluble in diluted... ... Veterinary encyclopedic dictionary

A drug from the group of sulfonamide drugs (See Sulfonamide drugs). Used in tablets and powders in the treatment of infectious diseases (tonsillitis, pneumonia, dysentery, etc.) ... Great Soviet Encyclopedia

Norsulfazole, norsulfazoles, norsulfazole, norsulfazoles, norsulfazole, norsulfazolam, norsulfazole, norsulfazoles, norsulfazole, norsulfazoles, norsulfazole, norsulfazoles (

Gross formula

C 9 H 9 N 3 O 2 S 2

Pharmacological group of the substance Sulfathiazole

Nosological classification (ICD-10)

CAS code

72-14-0

Characteristics of the substance Sulfathiazole

Short-acting sulfanilamide drug.

White or white with a slightly yellowish tint, odorless crystalline powder. Very little soluble in water, little in alcohol, soluble in diluted mineral acids and solutions of caustic and carbonic alkalis.

Pharmacology

pharmachologic effect- antimicrobial.

The mechanism of antimicrobial action is associated with the antagonism of PABA, with which there is a chemical similarity. Sulfathiazole is captured by the microbial cell, prevents the incorporation of PABA into dihydrofolic acid and, in addition, competitively inhibits the bacterial enzyme dihydropteroate synthetase (the enzyme responsible for the incorporation of PABA into dihydrofolic acid), as a result, the synthesis of dihydrofolic acid is disrupted, and the formation of metabolically active tetrahydrofolic acid from it, necessary for for the formation of purines and pyrimidines, the growth and development of microorganisms stops (bacteriostatic effect).

Active against gram-positive and gram-negative cocci (including streptococci, pneumococci, meningococci, gonococci), Escherichia coli, Shigella spp., Klebsiella spp., Vibrio cholerae, Clostridium perfringens, Bacillus anthracis, Corynebacterium diphtheriae, Yersinia pestis, Chlamydia spp., Actinomyces israelii, Toxoplasma gondii.

When taken orally, it is easily absorbed from the gastrointestinal tract. Reversibly binds to blood albumin (55%), solubility in lipids is 15.6%. Metabolized in the liver by conjugation with acetic acid, the content in the blood in acetylated form is 20%. T1/2 - 3.5 hours. Excreted from the body mainly in the urine, mainly in free non-acetylated form, 20% - in the form of acetyl derivatives, which are insoluble at the acidic pH of urine and precipitate (the possibility of developing crystalluria).

NORSULFAZOLE

norsulfazole(Norsulfazolum; PC, list B), an antibacterial agent from the sulfonamide group. White or white with a slightly yellowish tint, odorless crystalline powder. Very slightly soluble in water, slightly soluble in alcohol, soluble in diluted mineral acids, solutions of caustic and carbonic alkalis. For parenteral administration it is used norsulfazole sodium (soluble N. ) (Norsulfasolum-natrium; PC, list B), easily soluble in water. Effective against streptococci, meningococci, pneumococci, staphylococci and E. coli. Easily absorbed from the gastrointestinal tract and wound surface. Toxicity is low. Prescribed for postpartum septic complications, catarrhal bronchopneumonia, diplococcal septicemia of calves, necrobacteriosis, coccidiosis of chickens (with drinking water at 0.25% concentration). Oral doses: cow, horse 5.0 x 20.0 g; sheep, pig 1.0 x 5.0 g; dog 0.3 x 1.0 g; into a vein (norsulfazole sodium): cow 6.0 x 10.0 g; horses 8.0 x 12.0 g; sheep 1.5 2.0 g. Store in a well-closed container.

Veterinary encyclopedic dictionary. - M.: "Soviet Encyclopedia". Editor-in-Chief V.P. Shishkov. 1981 .

Synonyms:

See what "NORSULFAZOLE" is in other dictionaries:

norsulfazole- norsulfazole... Spelling dictionary-reference book

NORSULFAZOLE- (Norsulfazolum). 2 (para Aminobenzenesulfamido) thiazole. Synonyms: Amidotiazol, Aseptosil, Azoseptale, Cibazol, Eleudron, Poliseptil, Pyrisulfon, Sulfathiazole, Sulphathiazolum, Thiazamide, etc. White or white with a slightly yellowish tint... ... Dictionary of medicines

norsulfazole- noun, number of synonyms: 1 medicine (1413) ASIS Dictionary of Synonyms. V.N. Trishin. 2013… Synonym dictionary

Norsulfazole- a drug from the group of sulfonamide drugs (See Sulfonamide drugs). Used in tablets and powders in the treatment of infectious diseases (tonsillitis, pneumonia, dysentery, etc.) ... Great Soviet Encyclopedia

norsulfazole- norsulfazole, norsulfazoles, norsulfazole, norsulfazoles, norsulfazole, norsulfazolam, norsulfazole, norsulfazoles, norsulfazole, norsulfazoles, norsulfazole, norsulfazoles (