Pharmacological action
Sulfadimethoxine, as a typical representative of sulfonamide drugs, has a bacteriostatic effect on pathological microorganisms. The mechanism of action is revealed by organic chemistry; the main biological component of the drug is a structural analogue of para-aminobenzoic acid , which it competitively inhibits in the formation of folic acid (a key factor in the growth and development of most microorganisms).
Thus, the synthesis of nucleic acids is suppressed (both purine and pyrimidine bases require dihydrofolic acid ), which manifests itself in inhibition of the growth and reproduction of foreign, microscopic organisms. The human cell only consumes and utilizes the metabolic product of vitamin B9 , therefore the drug does not threaten its vital activity.
Sulfadimethoxine is active against a large number of gram-positive and gram-negative microorganisms. Thus, the drug perfectly fights against pneumococci , various types of streptococci and staphylococci , dysenteric shigella , Escherichia coli and Friedlander's bacillus ( Klebsiella ). The effect is somewhat less noticeable in relation to trachoma and proteus .
Pharmacological properties of the drug Sulfadimethoxine
Sulfadimethoxine belongs to the group of long-acting sulfonamides. Has antibacterial activity against gram-negative and gram-positive bacteria: pneumococci, streptococci, staphylococci, Escherichia coli, Friedlander's bacillus, dysentery pathogens; less active against Proteus. Active against trachoma virus. Sulfadimethoxine has no effect on bacterial strains resistant to sulfonamides. When taken orally, it is absorbed relatively slowly. With a single dose of a therapeutic dose (1–2 g), the maximum concentration in the blood plasma is achieved after 8–12 hours. Maintenance doses (0.5–1 g) provide the required therapeutic level in the blood throughout the course of treatment. Compared to other long-acting sulfonamides, sulfadimethoxine penetrates the blood-brain barrier worse (use for purulent meningitis is not advisable). Excreted in the form of metabolites, mainly in the urine.
Pharmacodynamics and pharmacokinetics
The half-life of the drug is 24-48 hours, depending on the individual characteristics of the body. Sulfadimethoxine is well absorbed by the gastrointestinal mucosa. In the systemic circulation it binds to plasma proteins, after which it is evenly distributed throughout all tissues and organs. The drug is able to penetrate the blood-brain barrier and the placenta . The favorite place of accumulation is the serous cavities of the body .
The drug is metabolized in the liver by acetylation. The solubility of products after chemical transformation deteriorates significantly and depends on the acidity of the primary urine. Sulfadimethoxine is excreted primarily by the kidneys and can sometimes lead to the formation of crystals ( crystalluria ).
SULPHADIMETOXINE
SULPHADIMETOXINE. Sulfadimethoxinum. Synonyms: aristin, deposul, madribon, madroxin, depot-sulfamide, sulphastop, supersulfa, ultrasulfan, etc.
Properties.
Crystalline powder of white or creamy white color, tasteless and odorless, slightly soluble in water, soluble in diluted acids and alkalis.
Release form: Available in powder and tablets of 0.2 and 0.5 g.
Store according to list B, in a well-closed container, protected from light. Shelf life: 4 years.
Action and application.
The drug belongs to the prolonging sulfonamides and is slowly absorbed from the gastrointestinal tract of animals. The maximum concentration of the drug in the blood of cattle is observed after 8-12 hours, sheep and goats - 5-8, pigs and dogs - 2-5, chickens - 3-5 hours from the moment of administration. The therapeutic level is maintained for 24-48 hours.
Compared to other long-acting sulfonamides (sulfapyridazine, sulfamonomethoxine), sulfadimethoxine penetrates organs and tissues worse. The exception is bile, where the concentration of the drug can exceed its content in the blood by 1.5-4 times. In the blood, the drug binds to plasma proteins (90 -98%). The acetyl derivative is found in the blood in small quantities. Sulfadimethoxine is excreted from the body slowly, mainly due to large (93-97%) reabsorption in the tubules of the free form of the drug.
Has a wide antimicrobial spectrum of action. It is most active against streptococci, staphylococci, meningococci, pneumococci, E. coli, dysentery pathogens; does not affect bacterial strains resistant to other sulfonamide drugs.
Used for bronchopneumonia of calves, piglets and lambs, infectious inflammatory diseases, nasopharyngeal diseases, acute dysentery, pasteurellosis, coccidiosis, gastroenteritis, colitis in animals.
Prescribed orally 1 time per day for 4-6 days with an interval of 24 hours. Doses (mg/kg animal weight): for cattle 15-30; calves 25-40; sheep and goats 15-30; pigs 25-35; chickens 75-100; rabbits 250-500; dogs 20-25. The initial dose should be 2 times the recommended dose.
To increase the therapeutic effect, it is advisable to use sulfadimethoxin in combination with antibiotics, organic paints, iodine preparations, and vitamins.
Sulfadimethoxine is contraindicated in case of toxic-allergic reactions, diseases of the hematopoietic system, kidneys, and acute hepatitis.
Slaughter of animals for meat is permitted no earlier than 10 days after stopping the use of the drug.
Indications for use of Sulfadimethoxine
Here is a short list of what Sulfadimethoxine effectively helps with in a relatively short period of time:
- pneumonia;
- acute respiratory diseases of the upper respiratory tract;
- bronchitis with confirmed microbial etiology;
- shigella dysentery;
- sinusitis;
- tonsillitis;
- inflammatory lesions of the central nervous system ( meningococcal infection );
- pathologies of the urinary and urinary systems with a positive coccal pathogen.
Sulfadimethoxine can be used in complex therapy, when several drugs of different types are included in a conservative treatment regimen for a more complete spectrum of therapeutic action. In this case, the indications for use are expanded to include the following diseases:
- persistent forms of malaria ;
- wound infection;
- pyoderma – purulent inflammation of the skin due to coccal invasion;
- Erysipelas (or erysipelas ) is an infectious disease with characteristic erythema and bullae on the upper and lower extremities.
Learn about the main antimicrobials in animals
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Contraindications
Sulfadimethoxine should be avoided if there is hypersensitivity or intolerance to individual components of the drug, hereditary or acquired deficiency of glucose-6-dehydrogenase , azotemia of various etiologies.
Under the close supervision of qualified medical personnel, the drug should be used if there is a history of diseases of the hematopoietic system or decompensated forms of heart failure .
Side effects
Conservative treatment is usually well tolerated if treatment is carried out in an inpatient setting. Otherwise, such undesirable reactions as:
- Headache and dizziness .
- Dyspeptic digestive disorders (dry mouth, nausea, vomiting, diarrhea ).
- Drug fever is a sharp rise in temperature immediately after taking the drug.
- Skin, itchy rashes.
- Leukopenia – a decrease in the level of free leukocytes in the systemic circulation, and as a consequence a decrease in the body’s resistance.
- Cholestatic hepatitis is an inflammatory disease of the liver with stagnation of bile in the excretory ducts.
- Allergic reactions - urticaria , dermatitis , angioedema or others.
Separately, it is worth noting that Sulfadimethoxine forms specific crystals in the urine, from which the tablets change its color to rich yellow-brown at a certain acidity, due to the formation of specific crystals.
Instructions for use of Sulfadimethoxine (Method and dosage)
First of all, you should test the sensitivity of the pathogenic microorganisms that caused the disease, because not all strains of coccal infection respond to treatment with sulfonamide drugs.
The tablets should be taken orally at 24-hour intervals. The course of treatment ranges from 7 to 14 days, depending on the pathophysiology of the disease. The doctor will prescribe how to take the tablets in each specific case, but the general regimen for adults is 2 grams on the first day of hospitalization and 1 gram each to maintain a stable level of the biologically active component in the systemic circulation.
The instructions for Sulfadimethoxine are somewhat different in pediatric practice . On the first day, 25 mg/kg is prescribed, and then 12.5 mg/kg in subsequent days for young children. If the child is over 12 years old, then the initial dose is 1 g, and the maintenance dose is 0.5 g.
Pharmacokinetics
After oral administration, it is found in the blood within 30 minutes, the period of maximum concentration is 8 - 12 hours. Unlike other representatives of long-acting sulfonamides, it penetrates poorly through the blood-brain barrier and its concentration in the cerebrospinal fluid is low. However, with inflammation of the meningeal membranes, the permeability of the blood-brain barrier increases sharply. Therapeutic concentration in adults is observed when taking 1 - 2 g on the first day and 0.5 - 1 g on subsequent days. The drug accumulates in the blood, primarily due to a high degree of binding to blood proteins (90 - 99%). Well distributed throughout organs and systems. It penetrates well into the pleural fluid (60 - 90% of the concentration in the blood), into the biliary system, where its concentrations are 1.5 - 4 times higher than in the blood. Unlike other sulfonamides, preferential metabolism occurs along the microsomal glucuronidation pathway, which is NADP-H-dependent and associated with cytochrome P450.
It is excreted slowly, primarily due to retention in the blood by plasma proteins and due to a high degree of reabsorption in the renal tubules (93 - 97.5%). The blood contains 5 - 15% acetylated metabolites, the urine - 10 - 25% acetyl derivatives and 75 - 90% - sulfadimethoxine glucuronide; the latter is highly soluble and does not provoke the development of crystalluria. The acetyl derivative is not reabsorbed and is completely excreted by the kidneys. After 24 hours, 20 - 44% of the dose taken is excreted, after 48 hours - up to 56%, after 96 hours - up to 83.3%.
Overdose
The state of oversaturation of the body with the drug is clinically manifested in intense thirst , severe dry mouth , small amounts of rich yellow-brown urine , pain in the right hypochondrium (liver projection) and lower back (renal localization). Biochemical analysis will reveal a significant increase in enzymes such as AST , ALT and acid phosphatase .
Therapeutic measures for overdose:
- Reflexogenic initiation of vomiting.
- Gastric lavage or high cleansing enema.
- Oral astringents and adsorbents.
- Saline laxatives.
- Forced diuresis , if the drug has managed to be completely absorbed from the gastrointestinal tract.
Domestic veterinary drugs SULFADIMETOXINE. Sulfadimethoxinum.
Synonyms: aristin, deposul, madribon, madroxin, depot-sulfamide, sulphastop, supersulfa, ultrasulfan, etc.
Properties.
Crystalline powder of white or creamy white color, tasteless and odorless, slightly soluble in water, soluble in dilute acids and alkalis.
Release form. Available in powder and tablets of 0.2 and 0.5 g.
Store according to list B, in a well-closed container, protected from light. Shelf life: 4 years.
Action and application.
The drug belongs to the prolonging sulfonamides and is slowly absorbed from the gastrointestinal tract of animals. The maximum concentration of the drug in the blood of cattle is observed after 8-12 hours, sheep and goats - 5-8, pigs and dogs - 2-5, chickens - 3-5 hours from the moment of administration. The therapeutic level is maintained for 24-48 hours.
Compared to other long-acting sulfonamides (sulfapyridazine, sulfamonomethoxine), sulfadimethoxine penetrates organs and tissues less well. The exception is bile, where the concentration of the drug can exceed its content in the blood by 1.5-4 times. In the blood, the drug binds to plasma proteins (90-98%). The acetyl derivative is found in the blood in small quantities. Sulfadimethoxine is excreted from the body slowly, mainly due to large (93-97%) reabsorption in the tubules of the free form of the drug.
Has a wide antimicrobial spectrum of action. It is most active against streptococci, staphylococci, meningococci, pneumococci, E. coli, and dysentery pathogens; does not affect bacterial strains resistant to other sulfonamide drugs.
Used for bronchopneumonia of calves, piglets and lambs, for infectious inflammatory diseases, nasopharyngeal diseases, acute dysentery, pasteurellosis, coccidiosis, gastroenteritis, colitis in animals.
Prescribed orally
1 time per day for 4-6 days with an interval of 24 hours. Doses (mg/kg animal weight): cattle 15-30; calves 25-40; sheep and goats 15-30; pigs 25-35; chickens 75-100; rabbits 250-500; dogs are 20-25. The initial dose should be 2 times the recommended dose.
To increase the therapeutic effect, it is advisable to use sulfadimethoxin in combination with antibiotics, organic paints, iodine preparations, and vitamins.
Sulfadimethoxine is contraindicated in case of toxic-allergic reactions, diseases of the hematopoietic system, kidneys, and acute hepatitis.
Slaughter of animals for meat is permitted no earlier than 10 days after stopping the use of the drug.
Interaction
Sulfadimethoxine should not be combined with:
- Drugs that inhibit hematopoiesis (for example, butadione or analgin ).
- Oral sugar-lowering agents ( sulfonyl urea ).
- Derivatives of para-amine benzoic acid (local anesthetics of the novocaine ).
The effect of pharmacological drugs will be enhanced if, in addition to the main component of the therapeutic course, the following are used:
- non-steroidal anti-inflammatory drugs;
- antithrombotic drugs;
- barbiturates;
- vitamin K antagonists .
The effects of Sulfadimethoxine are reduced by the use of folic acid , oral contraceptives and bactericidal betalactam antibiotics ( penicillins , carbapenems , cephalosporins , etc.).
The toxicity of the drug increases:
- pyrazolone derivatives ;
- salicylates;
- methotrexate and diphenine .
Interaction with other drugs
Reduces the effectiveness of bactericidal antibiotics that act only on dividing microorganisms (including penicillins, cephalosporins).
Procaine, benzocaine and tetracaine reduce antibacterial activity.
Para-aminosalicylic acid and barbiturates enhance the antimicrobial effect.
Salicylates increase activity and toxicity.
Methotrexate and phenytoin increase the toxicity of sulfadimethoxine.
Non-steroidal anti-inflammatory drugs, thioacetazone, chloramphenicol increase the toxic effect on the blood (leukopenia, agranulocytosis).
Strengthens the effect of indirect anticoagulants, phenytoin, sulfonamides with hypoglycemic action; pyrazoline derivatives, indomethacin and salicylates increase the free fraction of the drug in the blood.
Reduces the effectiveness of oral contraceptives.
Enhances the metabolism of cyclosporine.
Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.
Reviews of Sulfadimethoxine
Medical reviews of the drug confirm the effectiveness of the drug in the fight against coccal infection of internal organs and skin, if the conservative course of treatment is fully complied with. Otherwise, pathogenic microorganisms develop resistance to a whole group of drugs, since all sulfonamides have a typical chemical structure.
In surgical hospitals, a complex drug ( dioxomethyltetrahydropyrimidine + sulfadimethoxine + trimecaine + chloramphenicol ) is given a good rating, since in this composition the effect of the main biologically active substance is complemented by analgesic, necrolytic and anti-inflammatory effects. The drug is the drug of choice in the treatment regimen for a large number of purulent nosological units.
Separately, it is worth noting that the following question is often found on forums: “Is sulfadimethoxine an antibiotic or not?” This misconception was dispelled by Dr. Komarovsky on his official website: “The drug has a destructive effect on pathogenic microorganisms, accordingly, based on the pharmacological definition of an antibiotic, Sulfadimethoxine is such.”
