Sulfadiazine instructions for use. Sulfadiazine - instructions for use, description, pharmacological action, indications for use, dosage and method of administration, contraindications, side effects

Silver sulfadiazine INN

International name: Sulfadiazine

Dosage form: aerosol for external use, cream for external use, ointment for external use

Chemical name:

4-amino-N-2-pyrimidinylbenzenesulfonamide (as silver salt)

Pharmacological action:

Sulfanilamide drug for local application. Possesses wide range antibacterial action, which includes almost all microorganisms that can infect burn wounds: Escherichia coli, Proteus spp., Staphylococcus spp., Klebsiella spp.; Some types of fungi and yeast are also sensitive. Reduces the activity of SH-containing enzymes of microbial cells. When applied to damaged skin dissociates with the release of silver and sulfanilamide ions, the concentrations of which are sufficient to inhibit growth pathogens and at the same time do not have a damaging effect on tissue cells. Penetrates necrotic tissue. Slightly evaporates from the surface of the wound, has no unpleasant odor and is easily washed off with water.

Pharmacokinetics:

When applied to the wound surface, about 10% of sulfadiazine and 1% of silver are absorbed into the peripheral and systemic bloodstream. Application to a large wound surface is accompanied by an increase in the concentration of sulfadiazine in the blood to 10-20 mcg/ml.

Indications:

Infected superficial wounds and burns with weak exudation, bedsores, trophic and long-term non-healing ulcers (including stump wounds), abrasions, skin grafts.

Contraindications:

Hypersensitivity, inhibition of bone marrow hematopoiesis, glucose-6-phosphate dehydrogenase deficiency, renal/ liver failure, porphyria, pregnancy, neonatal period and infancy(up to 1 month), deep purulent wounds and burns with severe exudation.

Dosage regimen:

Externally. For adults and children over 1 month old, after cleaning the wound, lubricate the damaged surface with a layer of cream or ointment 1.5-2 mm thick 1-2 times a day; Large damaged skin surfaces are covered with a sterile bandage, changed 1-2 times a day. There are no painful effects when changing dressings. Before each repeated application, it is necessary to remove the previous layer of the drug with a stream of water or an antiseptic drug. Maximum dose- 0.3 g ointment.

Side effects:

Burning, itching, brownish-gray discoloration of the skin, skin allergic reactions (skin rash, photosensitivity); at long-term use on large wound surfaces - systemic side effects(leukopenia, headache, dyspepsia).

Special instructions:

When treating patients with liver and/or renal failure, it is necessary to regularly monitor the concentration of sulfonamides in plasma. Silver salts, when reacting with atmospheric oxygen, metals and other chemical components, especially under catalytic heat, darken, so the drug should be stored in a closed container and away from heat sources. It is recommended to protect parts of the body treated with the drug from direct sunlight.

Application. PREPARATIONS FOR TOPICAL APPLICATION IN OPHTHALMOLOGY

SILVER SULFADIAZINE -

(for ophthalmic use)

Indications/Pharmacological action-

Silver sulfadiazine cream is a drug with a wide spectrum of activity, acting against both bacteria (Gram-positive and gram-negative) and fungi. The drug is widely used in humane medicine in the treatment of skin burns. In recent years, this drug, non-toxic to the skin, conjunctiva and cornea, has been used to treat fungal keratitis. Particularly good results were observed in the treatment of superficial keratitis on early stage before disease progression. When using silver sulfadiazine at an early stage of the disease, a better clinical response is observed. The use of the drug in humane medicine is considered unconventional method treatment, while in veterinary ophthalmology this drug is becoming increasingly common for the treatment of fungal keratitis. For medico-legal reasons, in the case of very expensive horses where legal action is possible, a more traditional treatment (natamycin) may be recommended first, or it may be advisable to obtain written consent from the owner to treat his animal with silver sulfadiazine. However, the initial response to treatment may seem promising.

Suggested Dosage/Warnings/Side Effects- the drug is available in the form of a cream, but using a tuberculin syringe without a needle it can also be injected into the conjunctival sac. Typically a dose of 0.2 ml is used, which is drawn into a syringe. The drug does not pass through catheters for subpalpebral lavage standard sizes, but it can be administered using larger drug delivery systems, including red rubber tubes, and administering the drug through such a system may be more or less successful. It is probably best to administer the drug manually. The cream adheres well to the cornea of ​​the eye, which may increase its effectiveness, similar to natamycin when compared with miconazole. Recommended treatment regimens are similar to those for other antifungal drugs: at first the drug is applied very often, then gradually reduce the frequency of application in accordance with

in accordance with the clinical response. Daily removal of dead corneal stroma and epithelial tissue improves drug penetration and a more favorable clinical response.

Silver sulfadiazine is inexpensive drug, it can be purchased at any pharmacy, but the annotation does not indicate the possibility of its ophthalmic use. In contrast, the labeling or summary states that the drug is “not for ophthalmic use,” so the responsibility for ocular use rests entirely with the prescribing veterinarian, and some pharmacists may be reluctant to dispense the drug for ophthalmic use.

Release form / Drugs / FDA certificate -Veterinary drugs: V USA No. Medicines:

Silver sulfadiazine for topical use ( not for ophthalmic use) 10 mg per 1 g of cream base mixed with water. Available in packages of 20, 50, 400 and 1000 g; Silvadene®-(Manon); Flint SSD®(Flint); Rx.

Sulfadiazine is active against gram-negative and gram-positive microorganisms (including Escherichia coli, Pseudomonas aeruginosa, Staphylococcus spp., Proteus spp., Klebsiella spp.), dermatophytes and fungi of the genus Candida (including Candida albicans). Sulfadiazine inhibits dihydropteroate synthetase, competitively blocking the sorption of para-aminobenzoic acid, which leads to a decrease in the formation of dihydrofolic and tetrahydrofolic acid, and then the synthesis of pyrimidine and purine bases, nucleic acids. The antimicrobial properties of the drug are also due to the activity of silver ions, which are gradually released in the wound during the dissociation of the drug. The drug does not have necrolytic properties and is characterized by moderate osmotic activity. Approximately 1% silver and 10% sulfadiazine are absorbed into the peripheral and systemic circulation. The concentration of sulfadiazine in the blood increases to 10 - 20 mcg/ml when applied to large wound surfaces.

Indications

Infected burn wounds, bedsores, abrasions, skin ulcers, transplanted skin areas, as well as prevention of their infection.

Method of administration of silver sulfadiazine and dose

Silver sulfadiazine is applied topically. The dosage is set individually, depending on the indications.
When treating patients with disorders functional state kidneys and/or liver, it is necessary to regularly monitor the concentration of sulfadiazine in the blood serum.
In case of extensive wound surfaces, it is necessary to monitor the function of the kidneys and liver, cellular composition peripheral blood, prescribing abundant alkaline fluids.

Contraindications for use

Hypersensitivity, severe deficiency of glucose-6-phosphate dehydrogenase, burns and deep purulent wounds with severe exudation, breastfeeding, pregnancy, age under 1 year.

Restrictions on use

Hepatic or/and renal failure, glucose-6-phosphate dehydrogenase deficiency.

Use during pregnancy and breastfeeding

The use of sulfadiazine is contraindicated during pregnancy. The use of sulfonamides increases the risk of developing hyperbilirubinemia in the fetus and child, especially when used in III trimester pregnancy and during childbirth. If it is necessary to use sulfadiazine during lactation, it is necessary to decide on stopping breastfeeding, taking into account the degree of significance of therapy for the mother. There is no information about whether sulfadiazine is excreted in human breast milk. Other sulfonamides are found in milk; also, all sulfonamides increase the risk of developing hyperbilirubinemia in a child.

Side effects of silver sulfadiazine

Cardiovascular system and blood (hemostasis, hematopoiesis): leukopenia, neutropenia.
Local reactions: itching and burning at the site of application of the drug.
Others: skin allergic reactions, skin pigmentation disorders, skin necrosis, interstitial nephritis, erythema multiforme.
With prolonged use on large wound surfaces, systemic symptoms may develop. adverse reactions, which are characteristic of sulfonamides, including hematopoietic disorders (thrombocytopenia, hemolytic and aplastic anemia, agranulocytosis, leukopenia), allergic and skin reactions, including exfoliative dermatitis and Stevens-Johnson syndrome; dyspeptic symptoms, hepatocellular necrosis, hepatitis, toxic nephrosis, dysfunction of the central nervous system.

Interaction of silver sulfadiazine with other substances

Cimetidine increases the risk of developing leukopenia.
Sulfadiazine increases the side effects of amiodarone, anesthetics, sulfonylurea derivatives, anticoagulants, antimalarials and anticonvulsants, cyclosporine.
The drug may inactivate enzyme agents, which are used to clean wounds, so the combined use of these drugs is undesirable.
The combined use of sulfadiazine and phosphazide may mutually enhance myelotoxicity, so it is necessary to additionally monitor the hemoglobin content and granulocyte count.

Overdose

In case of an overdose of sulfadiazine, nausea, impaired liver function, crystalluria, impaired renal function, and leukopenia develop. Symptomatic treatment is necessary.

Trade names of drugs with the active ingredient silver sulfadiazine

Combined drugs:
Silver sulfadiazine + Recombinant human epidermal growth factor: Ebermin.

Included in the preparations

ATX:

D.06.B.A Sulfonamides

Pharmacodynamics:

Sulfanilamide drug for external use. Acts bacteriostatically. It has a wide spectrum of antibacterial action, which includes almost all gram-positive and gram-negative microorganisms, including Pseudomonas aeruginosa, Escherichia coli, Proteus spp., Staphylococcus spp., Streptococcus spp., Enteiobacter spp. And Klebsiella spp., some types of fungi and yeast are also sensitive to it.

When applied to damaged skin, it dissociates with the release of silver and sulfanilamide ions and interacts with the sulfhydryl groups of enzymes bacterial cell and reduces their activity, while at the same time does not have a damaging effect on tissue cells. Penetrates necrotic tissue.

Pharmacokinetics:

When applied to the wound surface, about 10% of sulfadiazine and 1% of silver are absorbed into the peripheral and systemic bloodstream. Application to a large wound surface is accompanied by an increase in the concentration of sulfadiazine in the blood to 10-20 mcg/ml. The half-life is 10 hours.

Indications:

Infected, superficial wounds and burns with slight exudation;

Bedsores;

Trophic and long-term non-healing ulcers (including stump wounds);

abrasions;

Skin grafting.

IX.I80-I89.I83.2 Varicose veins veins lower limbs with ulcer and inflammation

XII.L80-L99.L89 Decubital ulcer

XIX.T08-T14.T14.0 Superficial trauma to an unspecified area of ​​the body

XIX.T20-T32.T30 Thermal and chemical burns unspecified localization

XIX.T79.T79.3 Post-traumatic wound infection, not elsewhere classified

XXI.Z80-Z99.Z94 Presence of transplanted organs and tissues

Contraindications:

Allergic reactions to the components of the drug, inhibition of bone marrow hematopoiesis;

Glucose-6-phosphate dehydrogenase deficiency;

Kidney/liver failure;

Porphyria;

Deep purulent wounds and burns with pronounced exudation;

Childhood up to 2 years.

With caution:

Renal failure (dose adjustment may be required), liver failure, old age, bronchial asthma and other allergic reactions in history, AIDS (tendency to adverse reactions).

Pregnancy and lactation:

Use during pregnancy is possible only in cases where the expected benefit of therapy for the mother exceeds potential risk for the fetus. In such cases, the use of the drug should be as short as possible and limited to small areas of the skin.

If necessary, use during lactation breast-feeding should be stopped.

Directions for use and dosage:

Externally. For adults and children over 2 years old, after cleaning the wound, lubricate the damaged surface with a layer of cream 2 mm thick 2 times a day; Large damaged skin surfaces are covered with a sterile bandage, changed 2 times a day, in serious cases up to 4 times. There are no painful effects when changing dressings. Before each repeated application, it is necessary to remove the previous layer of the drug with a stream of water or antiseptic solution. Continue the course of treatment until healing.

Side effects:

Burning, itching, brownish-gray discoloration of the skin, allergic skin reactions (skin rash, photosensitivity); with long-term use on large wound surfaces - systemic side effects (leukopenia, headache, dyspepsia).

Overdose: Not described Interaction:

H 2 -histamine blockers - increases the risk of developing leukopenia.

Special instructions:

Silver salts, reacting with atmospheric oxygen, metals and other chemical components, especially under catalytic heat, darken, so the drug should be stored in a closed container and away from heat sources. It is recommended to protect parts of the body treated with the drug from direct sunlight.

Instructions

Included in the preparations

ATX:

J.01.E Sulfonamides and trimethoprim

Pharmacodynamics:

A structural analogue of PABA, which is necessary for microorganisms to synthesize dihydrofolic acid. Competitive blockade of bacterial dihydropteroate synthetase: disruption of the synthesis of dihydropteroic acid (precursor of tetrahydrofolic acid - a cofactor for purine synthesis). Only those microorganisms that are forced to independently synthesize folic acid are sensitive.

Pharmacokinetics:

F 70-100%. Penetrates through the BBB. Communication with plasma proteins is 38-48%. Biotransformation in the liver (acetylation). The half-life is 10 hours, with chronic renal failure - 34 hours. Elimination by the kidneys (60-85% within 48-72 hours).

Indications:

Prevention and treatment of infectious and inflammatory diseases caused by microorganisms sensitive to sulfadiazine: burns, bedsores, deep wounds.

XII.L80-L99.L89 Decubital ulcer

XIX.T79.T79.3 Post-traumatic wound infection, not elsewhere classified

Contraindications:

Pregnancy, increased sensitivity to sulfadiazine.

Not used in newborns.

With caution:

When treating patients with impaired liver function, it is necessary to regularly monitor the content of sulfadiazine in the blood plasma. When treating patients with impaired renal function, it is necessary to regularly monitor the content of sulfadiazine in the blood plasma.

Pregnancy and lactation:

Adequate and well-controlled studies in humans and animals have not been conducted. Do not use! No information about penetration into breast milk. Do not use!

Directions for use and dosage:

Apply externally usually 2 times a day. Large damaged skin surfaces are covered with sterile gauze; for smaller surfaces this is not required.

Side effects:

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

Blood disorders (fever, sore throat, paleness, unusual bleeding or bruising, unusual tiredness or weakness).

Hepatitis, Lyell's syndrome.

Central nervous system disorders: confusion, disorientation, euphoria, hallucinations, depression.

Colitis caused by Clostridium difficile.

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

Nausea, vomiting.

Overdose:

Suppression of bone marrow hematopoiesis: leukopenia, agranulocytosis, infections.

Treatment is symptomatic.

Interaction:

Cimetidine - increases the risk of developing leukopenia.

Special instructions:

Sulfanilamide of medium duration of action for external use. It is recommended to protect parts of the body treated with the drug from direct sunlight.

Instructions