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

norsulfazol

Sulfacetamide sodium

Sodium Sulfacetamide (Sulfacyl Sodium)

(Sulfacylum sodium)

2-para- Aminobenzenesulfanyl acetamide-sodium

Description. White crystalline powder, odorless, readily soluble in water, slightly alkaline solutions, practically insoluble in alcohol.

Definition 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 preparation when heated with hydrochloric acid (smell of acetic acid).

+ HCI → CH 3 COOH + NaCI+

1.3 Reaction due to the imide group with solutions of salts of heavy metals. Sodium sulfacetamide with a solution of copper sulfate forms a bluish-greenish precipitate that does not change upon standing (unlike other sulfanilamide preparations)

Quantitation.

1. Nitritometry method for the primary aromatic amino group.

2. 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. The indicator is methyl orange.

Titrant standard solution of hydrochloric acid.

3. Bromatomatometric method based on the ability of sulfonamides to be halogenated; Potassium bromate serves as a standard solution; titration is carried out in an acidic medium in the presence of potassium bromide. The excess of bromine is determined iodometrically;

Application. It is used in the form of 20-30% solutions and ointments (30%).

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. On the primary aromatic amino group:

a) the reaction of diazotization and azo coupling with phenols

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

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

1.3. The pyrolysis reaction is different 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 and a smell of hydrogen sulfide appear.

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

quantitation

1. Nitritometry method.

2. Method of bromatometry back titration.

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

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

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

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

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

Some strains are currently staphylococci , streptococci , meningococci, pneumococci And gonococci acquired resistance to the drug. He remains active in relation to nocardium , toxoplasma , malaria Plasmodium , chlamydia And fungi actinomycetes . The advent of antibiotics has reduced interest in sulfonamides.

Pharmacokinetics

Norsulfazol refers to well-absorbed short-acting sulfonamides. It binds to blood proteins by 55%. It is metabolized in the liver. It is excreted by the kidneys - 20% are acetyl derivatives that precipitate during acidic urine (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

hypersensitivity;
pregnancy;
depression of bone marrow function.

Side effects

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

Instructions for use Norsulfazol (Method and dosage)

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

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

Norsulfazol-sodium or norsulfazol soluble is a powder that can be used orally, as well as administered intravenously in the form of a 5% or 10% solution (on glucose solution). Concentrated solutions can cause phlebitis. Subcutaneously and intramuscularly is not prescribed, because it can cause. It is used in the form of instillations for infectious diseases of the eyes.

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

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

The drug is prescribed to animals inside 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 body weight. The initial dose is 2 times higher. The intake of water by animals is not limited. To increase the effectiveness of treatment, norsulfazol is prescribed in combination with antibiotics.

Overdose

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

Treatment is undertaken: gastric lavage, heavy drinking, symptomatic therapy.

Interaction

Aminoglycosides enhance antimicrobial activity. Antacids And reduce the absorption of sulfonamides. The hematotoxicity of the drug increases with the simultaneous use of other myelotoxic drugs . It is undesirable to use large doses. Effect anticoagulants of indirect action significantly enhanced when combined with sulfonamides.

Terms of sale

Released by prescription.

Storage conditions

At a temperature not exceeding 250 C.

Best before date

Norsulfazol's analogs

Coincidence in the ATX code of the 4th level:

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

). 2-(p-Aminobenzenesulfamido)-thiazole. Synonyms: Amidotiazol, Aseptosil, Azoseptale, Cibazol, Eleudron, Poliseptil, Pyrisulfon, Sulfathiazole, Sulphathiazolum, Thiazamide, etc. White or white with a slightly yellowish tinge, odorless crystalline powder. Very little soluble in water, little in alcohol, soluble in dilute mineral acids and solutions of caustic and carbonic alkalis. Norsulfazol is effective in infections caused by hemolytic streptococcus, pneumococcus, gonococcus, staphylococcus, and also Escherichia coli. The drug is easily absorbed from the gastrointestinal tract and rapidly excreted from the body. It is excreted mainly in the urine, mainly in a free, non-acetylated form. Applied inside with pneumonia, meningitis, staphylococcal and streptococcal sepsis and other infectious diseases. With pneumonia and meningitis, adults are prescribed for the first dose of 2 g, then 1 g every 4 to 6 hours until the body temperature drops; in the future, take 1 g every 6-8 hours. In total, the patient takes 20-30 g of the drug for the course of treatment. With staphylococcal infections, the first dose is 3-4 g, 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). Norsulfazol is prescribed to children every 4 - 6 - 8 hours in the following single doses: at the age of 4 months to 2 years - 0.1 - 0.25 g each, from 2 to 5 years old - 0.3 - 0.4 g each, from 6 to 12 years old - 0.4 - 0.5 g each. At the first dose, a double dose is given. Higher doses for adults inside: single 2 g, daily 7 g. When using norsulfazole, it is recommended to maintain increased diuresis (introduction into the body per day of 2-3 liters of liquid: 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 is possible, in rare cases, vomiting. Due to the advent of more effective chemotherapeutic agents, the use of norsulfazole is relatively limited. Release form: powder; tablets of 0.25 and 0.5 g in a package of 10 pieces. Storage: List B. In a well-closed container.

Medicine Dictionary. 2005 .

Synonyms:

See what "NORSULFAZOL" is in other dictionaries:

Norsulfazol ... Spelling Dictionary

Exist., Number of synonyms: 1 drug (1413) ASIS Synonym Dictionary. V.N. Trishin. 2013 ... Synonym dictionary

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

NORSULFAZOL- (Norsulfazolum; FH, list B), an antibacterial agent from the group of sulfonamides. White or white with a slightly yellowish tinge, odorless crystalline powder. Very slightly soluble in water, slightly soluble in alcohol, soluble in diluted ... ... Veterinary Encyclopedic Dictionary

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

Norsulfazole, norsulfazoles, norsulfazoles, norsulfazoles, norsulfazoles, norsulfazoles, norsulfazoles, norsulfazoles, norsulfazoles, norsulfazoles, norsulfazoles, 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

Sulfanilamide short-acting drugs.

White or white with a slightly yellowish tinge, 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, the formation of metabolically active tetrahydrofolic acid from it, which is necessary for the formation of purines and pyrimidines, stops the growth and development of microorganisms (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%), lipid solubility - 15.6%. It is metabolized in the liver by conjugation with acetic acid, the content in the blood in the acetylated form is 20%. T 1 / 2 - 3.5 hours. It is excreted from the body mainly in the urine, mainly in a free non-acetylated form, 20% - in the form of acetyl derivatives, which are insoluble at an acidic pH value of the urine and precipitate (possibility of developing crystalluria).

NORSULFAZOL

norsulfazole(Norsulfazolum; FH, list B), an antibacterial agent from the group of sulfonamides. White or white with a slightly yellowish tinge, odorless crystalline powder. Very slightly soluble in water, slightly soluble in alcohol, soluble in dilute mineral acids, solutions of caustic and carbonic alkalis. Used for parenteral administration norsulfazol-sodium (soluble N. ) (Norsulfasolum-natrium; FH, list B), easily soluble in water. Effective against streptococci, meningococci, pneumococci, staphylococci and Escherichia coli. Easily absorbed from the gastrointestinal tract and wound surface. Toxicity is low. It is prescribed for postpartum septic complications, catarrhal bronchopneumonia, diplococcal septicemia of calves, necrobacteriosis, chicken coccidiosis (with drinking water at a 0.25% concentration). Doses inside: cow, horse 5.020.0 g; sheep, pig 1.05.0 g; dog 0.31.0 g; in a vein (norsulfazol-sodium): cow 6.010.0 g; horses 8.012.0 g; sheep 1.52.0 g. Store in a well-closed container.

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

Synonyms:

See what "NORSULFAZOL" is in other dictionaries:

norsulfazole- norsulfazol ... Spelling Dictionary

NORSULFAZOL- (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 ... ... Medicine Dictionary

norsulfazole- n., number of synonyms: 1 drug (1413) ASIS Synonym Dictionary. V.N. Trishin. 2013 ... Synonym dictionary

norsulfazol- a drug from the group of sulfa 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, norsulfazoles, norsulfazoles, norsulfazoles, norsulfazoles, norsulfazoles, norsulfazoles, norsulfazoles, norsulfazoles, norsulfazoles, norsulfazoles (