Dapsone antibacterial agent, which is active concerning Mycobacterium leprae and tuberculosis. It has bacteriostatic action similar to antagonists of p-aminobenzoic acid.
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Dapsone product description
Dapsone is part of a group of substances called sulfones. The antibacterial result of Dapsone has the following mechanism, this substance, being a structural analog of para-aminobenzoic acid, interacts with dihydropyridine instead of para-aminobenzoic acid and competitively inhibits dihydropteroate synthetase. This prevents the synthesis of folic acid bacteria. Lack of folic acid, in turn, disrupts the formation of purines, pyrimidines and certain amino acids (methionine) of bacteria and, ultimately, leads to the cessation of bacterial growth. Dapsone has a bacteriostatic nature of the action, as it stops the growth and multiplication of bacteria, but does not cause their death.
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 monoacetylldosone. Eliminated by the kidneys (70-85%) and through the gastrointestinal tract, 20% is excreted unchanged.
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. In addition, this medicine is designed for the treatment of tuberculosis, pneumonia caused by Pneumocystis carinii.
Dapsone safety information
The consumption of this medicine is oral. Dosing regimen is individual. As a part of combination therapy, this medical agent is used in a dosage of 50-100 mg/day or 1-2 mg/kg/day. If necessary, the maximum daily dosage is 300mg. The treatment procedure is long.
Among the contraindications, the manufacturer indicates hypersensitivity, incl. to sulfanilamides, a liver dysfunction, severe anemia, a deficiency of glucose-6-phosphate dehydrogenase or methemoglobin reductase (possibly the development of hemolytic anemia). The consumption of this medication during pregnancy and lactation is possible only for prevention therapy in patients with leprosy or herpetiform dermatitis.
Dapsone side effects
On the part of the blood: dose-dependent hemolysis with a growth in the level of hemoglobin and an growth in the amount of reticulocytes (in all patients), hemolytic anemia (pain in the back, legs, stomach area, loss of appetite, pallor of the skin, unusual fatigue or weakness, increase in body temperature), methemoglobinemia (cyanosis of the fingernails, lips or skin, shortness of breath, etc.), pathological changes in the blood (elevated body temperature, sore throat, unusual bleeding and hemorrhages, etc.), incl. agranulocytosis and hypoplastic anemia with fatal outcome, palpitation, cardialgia.
On the part of the skin: itching, dryness, redness or peeling of the skin, hair loss, toxic erythema, erythema multi-form, toxic epidermal necrolysis, nodular erythema, kore and scarlatina-like reactions.
On the part of the CNS and sensory organs: mental disorders, incl. mood changes, peripheral neuritis (sensation of numbness, tingling, burning, pain or weakness in the hands and feet), neurotoxicity (a headache, insomnia, nervousness).
On the part of allergic effects: skin rash, "sulphonic syndrome" (fever, malaise, exfoliative dermatitis, jaundice, lymphadenopathy, methemoglobinemia, anemia), usually develops after 6-8 weeks of therapy.
On the part of the digestive tract: liver damage (icterus sclera or skin), anorexia, nausea, vomiting.