Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):VED
АТХ:J.04.B.A Anti-leprosy drugs
J.04.B.A.02 Dapson
Pharmacodynamics:Dapson refer to sulfones. The mechanism of antibacterial action of dapsone is that this substance, being a structural analogue para-aminobenzoic acid, interacts with dihydropteridine in place of para-aminobenzoic acid and competitively inhibits dihydropteroate synthetase. This prevents the synthesis of folic acid bacteria. The lack of folic acid, in turn, disrupts the formation of purines, pyrimidines and certain amino acids (methionine) bacteria and, ultimately, leads to the cessation of bacterial growth. Dapson has a bacteriostatic character of the action, since it stops the growth and multiplication of bacteria, but does not cause their death.
Pharmacokinetics:Absorbed within 2-8 hours. It binds to plasma proteins by 70-90%, and the main metabolite of the drug - monoacetylldosone - by 99%. Metabolised in the liver to monoacetylpodson. Eliminated by the kidneys (70-85%) and through the gastrointestinal tract, 20% is excreted unchanged.
Indications:The disease of Hansen (leprosy), tuberculosis, herpetiform dermatitis of Dühring, pneumonia caused by Pneumocystis carinii (pneumocystis pneumonia).
I.A30-A49.A30 Leprosy [Hansen's disease]
I.B50-B64.B50 Malaria caused by Plasmodium falciparum
I.B50-B64.B51 Malaria caused by Plasmodium vivax
I.B50-B64.B52 Malaria caused by Plasmodium malariae
I.B50-B64.B54 Malaria, unspecified
I.B50-B64.B55 Leishmaniasis
I.B50-B64.B58 Toxoplasmosis
I.B50-B64.B59 Pneumocystis
Contraindications:Chronic liver disease, hypersensitivity (including sulfanilamides), severe anemia.
Carefully:Deficiency of glucose-6-phosphate dehydrogenase or methemoglobin reductase.
Pregnancy and lactation:Action category for the fetus by FDA - C. If it is necessary to use dapsone in pregnancy, the expected benefit for the mother and the possible risk to the fetus should be correlated.
Dapsone is excreted in breast milk. Therefore, if it is necessary to use during lactation, the question of stopping breastfeeding should be resolved.
Dosing and Administration:Oral administration. Dosing regimen is selected individually by the attending physician. Can also be used in combination therapy at a dose of 50-100 mg per day or 1-2 mg per kilogram per day. The maximum daily dose is 300 mg.
Side effects:From the digestive system: vomiting, nausea, hepatitis.
From the hematopoiesis side: hemolytic anemia, agranulocytosis, methemoglobinemia.
From the skin: Stevens-Johnson syndrome, toxic epidermal necrolysis, skin rash, exfoliative dermatitis.
From the nervous system: headache.
Overdose:Inhibition of hematopoiesis in the bone marrow: agranulocytosis, leukopenia, infection. Treatment is symptomatic.
Interaction:Simultaneous reception with probenecid leads to a decrease in dapsone excretion and an increase in its concentration in the blood.
Simultaneous reception with rifampicin increases the plasma clearance of the dapsone.
Special instructions:The drug is mainly used to treat leprosy and herpetiform dermatitis. During the treatment, it is necessary to perform a general blood test and monitor the liver transaminases, reticulocyte count, platelet count, methemoglobin concentration, urea nitrogen, creatinine.