Sulfonamide - instructions for use, dose, side effects, contraindications

Structural analogue of PABA, necessary for microorganisms for the synthesis of dihydrofolic acid. Competitive blockade of dihydropteroate synthetase of bacteria: disruption of the synthesis of dihydropteroic acid (precursor of tetrahydrofolic acid - cofactor of purine synthesis).Only those microorganisms that are forced to synthesize folic acid themselves are sensitive.

Pharmacokinetics:

Not studied.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to sulfanilamide, incl. angina, erysipelas, cystitis, pyelitis, enterocolitis, infectious diseases of the skin and mucous membranes.

ICD-10

I.A00-A09.A09 Diarrhea and gastroenteritis of allegedly infectious origin

I.A30-A49.A46 Erys

X.J00-J06.J00 Acute nasopharyngitis (runny nose)

X.J00-J06.J01 Acute Sinusitis

X.J00-J06.J02 Acute pharyngitis

X.J00-J06.J03 Acute tonsillitis

X.J00-J06.J04 Acute laryngitis and tracheitis

X.J10-J18.J15 Bacterial pneumonia, not elsewhere classified

X.J20-J22.J20 Acute bronchitis

X.J30-J39.J31 Chronic rhinitis, nasopharyngitis and pharyngitis

X.J30-J39.J32 Chronic Sinusitis

X.J30-J39.J37 Chronic laryngitis and laryngotracheitis

X.J40-J47.J42 Chronic bronchitis, unspecified

XI.K80-K87.K81.0 Acute cholecystitis

XI.K80-K87.K81.1 Chronic cholecystitis

XI.K80-K87.K83.0 Cholangitis

XII.L00-L08.L01 Impetigo

XII.L00-L08.L02 Abscess of skin, boil and carbuncle

XII.L00-L08.L03 Phlegmon

XII.L00-L08.L08.0 Pyoderma

XIV.N10-N16.N10 Acute tubulointerstitial nephritis

XIV.N10-N16.N11 Chronic tubulointerstitial nephritis

XIV.N30-N39.N30 Cystitis

XIV.N30-N39.N34 Urethritis and urethral syndrome

XIV.N40-N51.N41 Inflammatory diseases of the prostate

XIV.N70-N77.N70 Salpingitis and oophoritis

XIV.N70-N77.N71 Inflammatory diseases of the uterus, except the cervix

XIV.N70-N77.N72 Inflammatory disease of the cervix

Contraindications:

Severe renal insufficiency, blood diseases, deficiency of glucose-6-phosphate dehydrogenase, nephroses, nephritis, acute porphyria, thyrotoxicosis, I and II trimesters of pregnancy, lactation, hypersensitivity to sulfonamides.

Carefully:

Caution is used in patients with kidney disease (without disturbance of the excretory function), in such cases, treatment should be carried out under the control of blood and urine tests.

Pregnancy and lactation:

Adequate and well-controlled studies in humans and animals have not been conducted. Do not apply! There is no information on the penetration into breast milk. Do not apply!

The category of FDA recommendations is not defined.

Dosing and Administration:

Inside adults - 500 mg-1 g 5-6 times / day; children under 1 year - 50-100 mg, from 2 to 5 years - 200-300 mg, from 6 to 12 years - 300-500 mg per reception.

Maximum doses for adults with oral administration: single 2 g, daily - 7 g.

When applied externally, they are applied to the affected areas of the skin and mucous membranes.

Side effects:

Hypersensitivity (fever, itching, skin rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant liver necrosis, agranulocytosis, aplastic anemia, other blood diseases), photosensitization.

Diseases of the blood (fever, sore throat, pallor, unusual bleeding or bruising, unusual fatigue or weakness).

Hepatitis, Lyell's syndrome.

Disorders from the central nervous system: confusion, disorientation, euphoria, hallucinations, depression.

Colitis caused by Clostridium difficile.

Crystalluria, hematuria; goiter, other thyroid dysfunction, interstitial nephritis, tubular necrosis.

Nausea, vomiting.

Overdose:

Oppression of bone marrow hematopoiesis: leukopenia, agranulocytosis, infection.

Treatment is symptomatic.

Interaction:

Antacids - reduced absorption of sulfonamide in the intestine.

Anticoagulants (coumarin and indanedione derivatives), anticonvulsants, antidiabetics - an increase in toxic effects due to their displacement from the connection with plasma proteins or the slowing of metabolism under the influence of sulfonamides.

Ascorbic acid, methenamine - increased risk of developing crystalluria.

Bactericidal antibacterial agents (including penicillins and cephalosporins) - decreased effectiveness.

Hepatotoxic agents - increased risk of hepatotoxicity.

Local anesthetics (procaine) - decrease in antimicrobial activity (in the hydrolysis release PABC).

Methenamine - with acidification of urine, the risk of formation of an insoluble precipitate is compatible with sulfanilamides.

Methotrexate, phenylbutazone, sulfinperazone - mutual displacement from the connection with plasma proteins.

Nonsteroidal anti-inflammatory drugs - increased severity of side effects.

Oral contraceptives (estrogen-containing) - increased risk of bleeding and pregnancy.

Means that cause hemolysis - an increased risk of toxic effects.

Means that have a sulfonamide group (diuretics, oral hypoglycemic agents - sulfanylurea derivatives, inhibitors of carbonic anhydrase) - the risk of cross-hypersensitivity.

Means that inhibit blood-forming - an increase in leukopenic, thrombocytopenic and myelotoxic effects.

Chloramphenicol, thiamazole - Increased hematotoxicity.

Ciclosporin - increased nephrotoxic effect.

Special instructions:

Most meningococcal serogroups A, B and C; Shigella spp., Escherichia coli resistant to sulfonamides.

Due to the bacteriostatic effect, intense immunity is required to kill the pathogen.

The most active preparations with heterocyclic aromatic substituents (sulfamethoxazole, sulfadiazine, sulfafurazole).

Due to widespread resistance, severe side effects and the development of new more effective antimicrobial agents, sulfonamides in monotherapy are practically not used (except for sulfacetamide for topical use).

Monitoring: general blood test, blood pH, renal ultrasound (systemic application), general urine analysis.

Distinctive characteristics.

Sulfanilamid short-acting for topical application.

Instructions

Sulfanilamide (Sulfanilamidum)

Infectious-inflammatory diseases caused by microorganisms sensitive to sulfanilamide, incl. angina, erysipelas, cystitis, pyelitis, enterocolitis, infectious diseases of the skin and mucous membranes.