Dapsone
Offer type: salePublished: 25.05.2013
| Seller: |  Andrej |
| Phones: |  +380980343228 Show phone |
| Address: | Ukraine, Zaporiz'ka Oblast', Zaporizhia |
Pharmacology
Pharmacological action - antibacterial, leprosy.
Is an antagonist PABK and violates the synthesis of folate in microbial cells. Antibacterial (bacteriostatic) effect against Mycobacterium leprosy (leprosy action) and tuberculosis. Suppresses the development of dermatitis herpetiformis presumably because of the ability to inhibit the enzymes or to be oxidizing properties, or as a result of immunotropic (immune) effect. Has antibacterial and antifungal activity. Shown effective in rheumatoid arthritis, mitsetome (madorsky foot) caused actinomycete, subcorneal dermatosis, the annular granuloma, some skin lesions in systemic lupus erythematosus, including bullous rashes and vasculitis, lesions of the oral cavity when pemphigoid, degenerative changes of the cartilage, pyoderma gangrenosum; pneumonia caused by Pneumocystis carinii (light and medium gravity forms in combination with trimethoprim); for prevention of malaria caused by Plasmodium vivax (in combination with pyrimethamine and chloroquine) and Plasmodium Falciparum (when resistance to chloroquine).
In animal experiments show carcinogenic effects, the emergence of mesenchymal tumors of the spleen and peritoneum in male rats and female mice, and thyroid carcinomas in female rats. Had no mutagenic effect in studies on test Salmonella typhimurium strains with microsomal activation or without it.
Slowly absorbed from the digestive tract (the period of poluvsasavania - 1.1 h), the optimal suction is acidic. Bioavailability is 70 to 80 % (in patients with a severe form of leprosy may be lower). Cmax in plasma is reached after 2-6 h and varies depending on the dose: single dose of 50 mg amounts to about 0.6-0.7 mcg/ml after a single dose of 100 mg to 1.7 to 1.9 μg/ml, at a dose of 100 mg on reaching the equilibrium concentration of 3.1-3.3 µg/ml (plateau is reached when taken within 8 days). At the dose of 200 mg/day equilibrium concentration ranging from 0.1 to 7 µg/ml and an average of 2.3 µg/ml of protein Binding by 70-90%, the main metabolite of monoacetyldapsone - 99%. It is distributed in all body fluids, it is found in liver, muscle, kidney and skin. Concentration in saliva, the concentration in the blood plasma. Passes through the placenta, enters breast milk. Volume of distribution - 1.5 l/kg (in case of simultaneous use with pyrimethamine - 1.9 l/kg).
Under the action of N-acetyltransferase metabolized in the liver to monoacetyldapsone that it is deacetylated to Dapsone (equilibrium achieved in a few hours). Type acetylation (fast/slow) does not affect the plasma concentration, the pharmacokinetics of a drug, therapeutic and side effects. The other way of a metabolism - N-hydroxylation with the formation of Dapsone hydroxylamine (presumably causes the toxic effect of the drug in the blood) under the influence of the mixed oxidase system in the presence of oxygen and of adenine dinucleotide phosphate. Both metabolite (monoacetyldapsone and Dapsone hydroxylamine) have low activity and do not affect the therapeutic effect of Dapsone, then partially associated with the formation of glucuronidase and sulfates.
Excreted in urine (70-85%) unaltered by active tubular secretion (5-15%) and in the form of water-soluble metabolites and bile (undergoes enterohepatic circulation and may persist in plasma for several weeks after discontinuation). Excreted slowly, so a constant level in the blood is achieved by taking regular doses. T1/2 from plasma on average 28-30 h, can vary from 10 to 50 hours Daily appointment of leprosy patients in a dose of 50-100 mg provides the plasma level exceeding the MIC, even in patients with short T1/2.
Pharmacological action - antibacterial, leprosy.
Is an antagonist PABK and violates the synthesis of folate in microbial cells. Antibacterial (bacteriostatic) effect against Mycobacterium leprosy (leprosy action) and tuberculosis. Suppresses the development of dermatitis herpetiformis presumably because of the ability to inhibit the enzymes or to be oxidizing properties, or as a result of immunotropic (immune) effect. Has antibacterial and antifungal activity. Shown effective in rheumatoid arthritis, mitsetome (madorsky foot) caused actinomycete, subcorneal dermatosis, the annular granuloma, some skin lesions in systemic lupus erythematosus, including bullous rashes and vasculitis, lesions of the oral cavity when pemphigoid, degenerative changes of the cartilage, pyoderma gangrenosum; pneumonia caused by Pneumocystis carinii (light and medium gravity forms in combination with trimethoprim); for prevention of malaria caused by Plasmodium vivax (in combination with pyrimethamine and chloroquine) and Plasmodium Falciparum (when resistance to chloroquine).
In animal experiments show carcinogenic effects, the emergence of mesenchymal tumors of the spleen and peritoneum in male rats and female mice, and thyroid carcinomas in female rats. Had no mutagenic effect in studies on test Salmonella typhimurium strains with microsomal activation or without it.
Slowly absorbed from the digestive tract (the period of poluvsasavania - 1.1 h), the optimal suction is acidic. Bioavailability is 70 to 80 % (in patients with a severe form of leprosy may be lower). Cmax in plasma is reached after 2-6 h and varies depending on the dose: single dose of 50 mg amounts to about 0.6-0.7 mcg/ml after a single dose of 100 mg to 1.7 to 1.9 μg/ml, at a dose of 100 mg on reaching the equilibrium concentration of 3.1-3.3 µg/ml (plateau is reached when taken within 8 days). At the dose of 200 mg/day equilibrium concentration ranging from 0.1 to 7 µg/ml and an average of 2.3 µg/ml of protein Binding by 70-90%, the main metabolite of monoacetyldapsone - 99%. It is distributed in all body fluids, it is found in liver, muscle, kidney and skin. Concentration in saliva, the concentration in the blood plasma. Passes through the placenta, enters breast milk. Volume of distribution - 1.5 l/kg (in case of simultaneous use with pyrimethamine - 1.9 l/kg).
Under the action of N-acetyltransferase metabolized in the liver to monoacetyldapsone that it is deacetylated to Dapsone (equilibrium achieved in a few hours). Type acetylation (fast/slow) does not affect the plasma concentration, the pharmacokinetics of a drug, therapeutic and side effects. The other way of a metabolism - N-hydroxylation with the formation of Dapsone hydroxylamine (presumably causes the toxic effect of the drug in the blood) under the influence of the mixed oxidase system in the presence of oxygen and of adenine dinucleotide phosphate. Both metabolite (monoacetyldapsone and Dapsone hydroxylamine) have low activity and do not affect the therapeutic effect of Dapsone, then partially associated with the formation of glucuronidase and sulfates.
Excreted in urine (70-85%) unaltered by active tubular secretion (5-15%) and in the form of water-soluble metabolites and bile (undergoes enterohepatic circulation and may persist in plasma for several weeks after discontinuation). Excreted slowly, so a constant level in the blood is achieved by taking regular doses. T1/2 from plasma on average 28-30 h, can vary from 10 to 50 hours Daily appointment of leprosy patients in a dose of 50-100 mg provides the plasma level exceeding the MIC, even in patients with short T1/2.
