Dapsone FATOL

Active material: Dapsone
When ATH: J04BA02
CCF: Protivoleproznyj drug group sulfones
When CSF: 07.07
Manufacturer: FATOL ARZNEIMITTEL GmbH (Germany)

Pharmaceutical form, composition and packaging

Pills white, round, lenticular, scored for a fracture on one side of the.

[Ring] calcium hydrogen phosphate dihydrate, microcrystalline cellulose, lactose monohydrate, kopovydon, krospovydon, colloidal silicon dioxide, magnesium stearate (Flora).

25 PC. – blisters (2) – packs cardboard.
25 PC. – blisters (4) – packs cardboard.

DESCRIPTION OF ACTIVE SUBSTANCES

Pharmacological action

Protivoleprosnoe sulfones group tool. It has a bacteriostatic effect. The mechanism of action is due to inhibition of the synthesis of folic acid Activator. Active against a broad spectrum of microorganisms, but mostly against Mycobacterium leprae, as well as Plasmodium, Pneumocystis carinii.

Pharmacokinetics

Slowly absorbed from the digestive tract. Bioavailability – 70-80%. It is well distributed in the body, but especially high concentrations up in the liver, muscle, the kidneys and the skin. Concentration in saliva – 18-27% from the concentration in the blood. It penetrates through the placental barrier. T_max – from 2 to 6 no. When applied in single doses 50 and 100 mg C_max is 0.6-0.7 and 1.7-1.9 ug / ml, respectively.

Metabolised in the liver, with the participation of acetiltransferazy education metabolita – monoazetildapson, which can be deacetilirovaniû and go again in Dapsone. The balance between them is created within a few hours. Acetylation speed depends on, What acetilâtorom is the patient – “fast” or “slow”, with this rate of acetylation clinical efficacy of therapy does not define. Another way its metabolism – This hydroxylation in the liver to dapsongidroksilamina. Dapson binding to plasma proteins – 70-90%, and monoazetildapson – more 90%.

T_1/2 for dapson and monoazetildapson – 10-50 no (an average of about 30 no). 70-85% slowly return to the kidneys in the form of Dapsone and its metabolites (5-15% Dapsone is displayed by active kanalzeva secreta); the rest is excreted in the form of metabolites, partly kon″ûgirovany with glukuronova and sulphuric acids. Enterogepatical circulation is important to maintain certain concentrations of the drug in the blood during long-term therapy.

Testimony

In the combined therapy: treatment and prevention of all forms of leprosy, malaria prevention, treatment and prophylaxis of Pneumocystis pneumonia, Prevention of toxoplasmosis, treatment of cutaneous leishmaniasis.

Dosage regimen

Dosage regimen individual. In a combination therapy is used in dose 50-100 mg/day or 1-2 mg / kg / day. If necessary, the maximum daily dose is 300 mg. Treatment long.

Side effect

From the hematopoietic system: possible haemolytic anaemia, metgemoglobinemiâ (When taking a daily dose of more than 200 mg), agranulocytosis.

From the digestive system: rarely – nausea, vomiting, hepatitis.

Dermatological reactions: skin rash, exfoliative dermatitis, toxic epidermal necrolysis, Stevens-Johnson syndrome.

Other: headache.

Contraindications

Severe anemia, hypersensitivity to Dapsone.

Pregnancy and lactation

If necessary, the use of Dapsone during pregnancy should correlate the alleged benefit to the mother and the potential risk to the fetus.

Dapsone is the breast milk. Therefore, if you must use during lactation should decide on the termination of breastfeeding.

Cautions

Be wary of Dapsone in patients with a deficit glukozo-6-fosfatdegidrogenaza, tk. This category of patients have increased risk of hemolytic anemia.

During treatment needed to be monitored picture peripheral blood.

Drug Interactions

If you are applying with Probenecid appears to be declining excretion of Dapsone and increasing its concentration in the blood plasma.

Rifampicin increases the plasma clearance of Dapsone.