Dapsone-Fatol - instructions for use, dose, side effects, contraindications

Active substanceDapsonDapson

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Dapson

pills inwards

FARMZASCHITA NPC, FSUE Russia

Dapson Fatol

pills inwards

Rimzer Artsynaimitel, AG Germany

Dosage form: & nbsppills

Composition:

1 tablet contains:

active substances: dapsone 50.00 mg;

Excipients: calcium hydrophosphate dihydrate 10.00 mg, microcrystalline cellulose 11,0 mg, lactose monohydrate 21.00 mg, copovidone 3.00 mg, crospovidone 3,0 mg, silicon dioxide colloidal, 1,0 mg, magnesium stearate (vegetable) 1,0 mg.

Description:

White, round, biconvex tablets with a risk for a fault on one side.

Pharmacotherapeutic group:Antimicrobial agent - sulfone

ATX: & nbsp

J.04.B.A Anti-leprosy drugs

J.04.B.A.02 Dapson

Pharmacodynamics:

A protivopleznoe means of the group of sulfones. Has a bacteriostatic effect. Active against a wide range of microorganisms, it is particularly effective against Mycobacterium leprae (the minimum effective concentration is within nanograms, so the therapeutic effect with leper can be achieved with a dose of 25 mg per day), Plasmodium, Pneumocystis carinii.

The mechanism of action, presumably, has at least 2 points of application: on the one hand, an analogue of dihydropteric acid is formeddapsone is absorbed instead of p-aminobenzoic acid), and on the other hand, the enzyme dihydropteroate synthetase is inhibited.As a result of these processes, functions of other systems, for example, dihydrofolate reductase, whose function is to convert unused microorganisms dihydrofolic acid to tetrahydrofolic acid, may occur.

Presumably, in addition to the antibacterial effect, the effect of dapsone is determined by other factors. In particular dapsone is able to inhibit the production of cytotoxic radicals in the chain of myeloperoxidase - hydrogen peroxide - halogenated compounds. Other effects of dapsone were also described: the inhibition of the Artus reaction, the complement system when it was activated by the alternative route, the inhibition of some lysosomal enzyme systems, the reaction of erythrocytes to phytohemagglutinin, and finally, the suppression of binding of leukotriene B₄ with its specific receptors. The effect on the immune system, obviously, is also an important property of dapsone, along with its analgesic and anti-inflammatory effects, revealed in the experiment.

Pharmacokinetics:

Dapsone is almost completely absorbed (70-80%) after oral administration. The maximum concentration of the drug in plasma is achieved through 2-6 hours.At a dose of 100 mg per day, the concentration of dapsone in the blood plasma reaches 1.7 mg / l for a single dose, 3.3 mg / l in a state of equilibrium and drops to 0.7 mg / l after 24 hours. 70-90% dapsone binds to plasma proteins. It penetrates well into various tissues and organs, and the values obtained correspond approximately to the concentrations in the plasma. Dapson can also penetrate into the intracellular space of phagocytes.

The half-life of the dapsone is relatively long, on average about 30 hours. About 90% from the orally administered dose of 100 mg is completely eliminated after about 9 days, but with prolonged treatment with dapsone, the active ingredient is detected in the body for up to 35 days after the last dose. However, the relative cumulation of the drug in the body does not occur.

Dapsone is acetylated in the liver. Another important way of dapsone metabolism is its hydroxylation. It is assumed that the monohydroxylamine of dapsone is responsible for the side effects of the dapsone on the part of the blood. The drug is characterized by hepatoenteric circulation. Dapson is excreted approximately 90% by the kidneys, largely in the form of metabolites and 10% - with feces.

Indications:

- For the treatment of leprosy - in combination with other drugs effective against leprosy;

- herpetiform dermatitis (Dühringa), bullous pemphigoid (in combination with corticosteroids and immunosuppressors or monotherapy with a light course):

- in some cases - treatment of vasculitis (in complex therapy).

Contraindications:

- Hypersensitivity to dapsone or other components of the drug, to sulfonamides and sulfones;

- severe anemia (hemoglobin content less than 10%). In an emergency (for example, with Dühring-Brokk syndrome), it may be necessary to perform dapsone treatment with strict control primarily of the red blood formula;

- severe liver disease;

- children's age till 18 years.

Pregnancy and lactation:

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.

In the first 4 months of pregnancy and during lactation, the drug should be prescribed only in case of emergency, with the utmost care.

Because the dapsone is secreted into breast milk, women taking the drug should refrain from breastfeeding.

Dosing and Administration:

Inside.

It is best to take after eating, washing down with plenty of water. It is used as a rule in complex therapy. One day a week the drug is not taken (for example, on Sundays).

Doses and duration of application

Dosing regimen is individual. The average dose of the drug is 50-100 mg of dapsone, i.e. 1-2 tablets a day, 6 days a week.

If not specified otherwise, the following dosage instructions apply:

Leprosy: the average daily dose is 50-100 mg (1-2 tablets) per day. Taking the drug for a long time for a number of years.

Herpetiform dermatitis (Dühring): treatment should begin with 2 tablets per day (100 mg dapsone) for 1 week. The dose can then be increased to 4 tablets (200 mg dapsone) until the effect is achieved. However, in each specific case it is necessary to strive for the lowest dose - 50 mg. In some cases, 300 mg of dapsone (6 tablets) per day can be taken for a short period of time, although it is necessary to strive for a maintenance dose of 50 mg of dapsone per day, which can be achieved by combining the drug with corticosteroids.

If the clinical picture of the disease is accompanied by symptoms from the gastrointestinal tract,the appointment of gluten-free diet can help reduce the dose of the drug.

The duration of treatment with Dühring's dermatitis is long, for many years. The duration of the break between courses increases with the use of corticosteroids. The possibility and duration of breaks are determined on a case by case basis.

Bullous pemphigoid: 100-150 mg / day.

Vasculitis: 50-150 mg / day.

Side effects:

From the side of the circulatory system: hemolytic anemia, methemoglobinemia, eosinophilia, agranulocytosis.

Hypersensitivity reactions: in the form of the so-called dapsone syndrome: fever, poor health, skin rash, jaundice, swelling of the lymph nodes, mononucleosis, methemoglobinemia and anemia, in severe cases - erythema multiforme or exfoliative dermatitis.

From the nervous system: peripheral neuropathies, dizziness, visual impairment, psychosis, insomnia.

Other: at the beginning of treatment, headaches, abdominal pain and nausea, vomiting, pancreatitis, fever, phototoxicity, tachycardia, albuminuria, hypoalbuminuria without proteinuria, nephrotic syndrome, papillary necrosis, male infiltrity,systemic lupus erythematosus, a syndrome similar to infectious mononucleosis, usually occurring with further administration of the drug.

In very rare cases, agranulocytosis, peripheral motor neuropathy and hypoalbuminemia are possible.

Overdose:

Symptoms of intoxication: dyspnea, nausea and vomiting, headaches, cyanosis, tachycardia, methemoglobinemia, hemolysis, hematuria, renal failure, neurological and psychiatric disorders, vision loss and coma.

There are no exact data on the lethal doses. In one case, taking 1.4 g led to death, and in the other, the patient survived after taking 15 g of dapsone.

Therapy for overdose

It is necessary to do a gastric lavage (always hold). After that it is necessary to accept Activated carbon and possibly a laxative for several days (40 ml of a 20-40% solution of sorbitol).

To increase the excretion of the sulfone and prevent renal failure, infusion therapy is performed (introduction of sufficient quantities of liquid with diuretics and sodium bicarbonate to alkalinize urine).

Treatment of methemoglobinemia is carried out by the introduction of methylene blue 1% 0.2 ml / kg intravenously and / or vitamin C (2 g / d).

In the case of a severe overdose, early hemodialysis, an infusion of erythrocyte mass or blood transfusion is indicated. Oxygen therapy or artificial respiration in the control of pO₂. Symptomatic therapy.

Interaction:

Dapsone increases effectiveness isoniazid, protionamide and rifampicin, which allows to reduce their doses, especially protionamide. Rifampicin increases the plasma clearance of the dapsone and lowers the dapsone level by 7-10 times.

When used together with probenecid a decrease in the excretion of dapsone and an increase in its concentration in the blood are noted.

Pyrimethamine can change some pharmacokinetic parameters of the dapsone (volume of distribution, concentration of the drug in plasma and saliva).

Reception cimetidine and moderate use alcohol do not affect the absorption of dapsone.

Trimetaprim affects the level of dapsone and vice versa.

Special instructions:

If there is a skin rash when taking the drug, take the drug immediately and immediately consult a doctor.

Use with caution dapsone in patients with insufficiency of glucose-6-phosphate dehydrogenase (G6PDG), since in this case the risk of side effects increases substantially.In an emergency, you should try to limit yourself to half the usual recommended dose.

Regular monitoring of the blood condition is necessary (blood tests at the beginning of therapy weekly, and several months later). In the event of a significant decrease in the level of white blood cells, platelets or hemopoiesis, treatment with dapsone should be discontinued. It should be borne in mind that side effects from the blood are usually more pronounced in elderly patients.

Effect on the ability to drive transp. cf. and fur:

The effect of the drug on the ability to drive a car and drive mechanisms is unlikely.

Form release / dosage:

Tablets, 50 mg.

Packaging:

25 tablets per blister (polyvinyl chloride / aluminum). For 2, 4 blisters with instructions for use in a cardboard box.

For 500 or 1000 tablets in a container of white color from polypropylene with a white lid of low density polyethylene with a ring of the first opening, the free space is filled with foam rubber seal, on top of which the instruction is placed. A label is attached to the container. For 100 containers of 500 tablets and 48 containers of 1000 tablets per group package - a box of cardboard (for hospitals).

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

The drug should not be used after the expiry date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-004694/08

Date of registration:20.06.2008 / 27.11.2015

Expiration Date:Unlimited

The owner of the registration certificate:Rimzer Artsynaimitel, AGRimzer Artsynaimitel, AG Germany

Manufacturer: & nbsp

G.L.PHARMA, GmbH Austria

Representation: & nbspSVYCH LLC SVYCH LLC Russia

Information update date: & nbsp18.03.2017

Illustrated instructions

Instructions

Dapson Fatol (Dapson-Fatol)