Active substancePenicillaminePenicillamine
Similar drugsTo uncover
Dosage form: & nbsp

film coated tablets

Composition:

1 tablet contains:

Active substance:

penicillamine 250 mg.

Excipients: potato starch, lactose monohydrate, povidone, talc, magnesium stearate.

Shell: hypromellose, macrogol-4000, titanium dioxide (E 171), dye azorubin (E 122).

Description:Round biconvex tablets covered with a film membrane of violet-pink color with a smooth surface without spots and chips.
Pharmacotherapeutic group:Anti-inflammatory agent
ATX: & nbsp

M.01.C.C.01   Penicillamine

Pharmacodynamics:

Kuprenil® has a high complexing activity with respect to metals, mainly copper, mercury, arsenic, lead, iron and calcium. The drug reduces the resorption of copper from food and eliminates its excess from the tissues. Influences on various links of the immune system (suppression of T-helper function of lymphocytes, inhibition of neutrophil chemotaxis and isolation of enzymes from lysosomes of these cells, enhancement of macrophage function). It has the ability to disrupt collagen synthesis, splitting the cross-links between newly synthesized tropocollagen molecules. Penicillamine is a pyridoxine antagonist; has anti-inflammatory effect.

Pharmacokinetics:

The preparation forms chelates with heavy metal ions - persistent complex compounds, soluble in water and excreted in urine. Easily absorbed from the digestive tract, reaching a maximum concentration in the blood for 1 -3 hours. The drug is metabolized in the liver.

In the gastrointestinal tract, up to 50% of penicillamine is absorbed. The drug is withdrawn in 2 phases: the half-life period (Tg) for the first one is 1 hour, for the second one it reaches 90 hours. About 70-80% of the adsorbed preparation is excreted as metabolites (cysteine- penicillamine, disulphide) with urine.

Indications:

Wilson-Konovalov's disease, copper poisoning, inorganic compounds of mercury, lead (with the exclusion of further lead through the digestive tract), gold, zinc, iron, cystine nephrolithiasis, systemic scleroderma, rheumatoid arthritis.

Contraindications:

- Hypersensitivity to penicillamine and other components of the drug;

- pregnancy and the period of breastfeeding (with the exception of Wilson-Konovalov disease in a dose of up to 1 g / day);

- agranulocytosis;

- kidney failure;

- violations of hemopoiesis;

- children's age up to 3 years (for this dosage form).

Do not use in combination with gold preparations; aminoquinoline and cytostatic agents; phenylbutazone.

Carefully:When conducting surgical interventions, anemia, proteinuria.
Dosing and Administration:

The drug should be administered inside at least 30 minutes before meals, washed down with water, or 2 hours after eating or other medications.

Wilson-Konovalov's disease

Adults: 1.5 - 2 g per day in divided doses. After achieving remission, the dose can be reduced to 0.75 g or 1 g per day. In patients with a negative balance of copper, the minimum effective dose of penicillamine should be used.

A dose of 2 g per day apply for not more than 1 year.

Elderly patients: 20 mg / kg body weight per day in divided doses. The dose should be selected in such a way as to achieve remission of the disease and to maintain a negative balance of copper.

Children: usually 20 mg / kg of body weight per day in divided doses.

The minimum dose is 500 mg per day.

Cystinuria

It is best to establish the minimum effective dose after quantitative determination of the concentration of amino acids in the urine by chromatographic method.

Dissolution of cystine stones.

Adults: 1-3 g per day in divided doses.It is necessary to keep the concentration of cystine in the urine below 200 mg / l.

Prevention of cystine lithiasis.

Adults: 0.5-1 g per day until the cystine concentration in the urine is below 300 mg / l.

Elderly patients: prescribe a minimum dose until the concentration of cystine in the urine is below 200 mg / l.

Children: Assign a minimum dose, which allows you to achieve a cystine concentration in the urine below 200 mg / l.

Attention: during treatment it is recommended to drink a large amount of liquid - at least 3 liters per day. The patient should drink 500 ml of water before bedtime, and then 500 ml at night, when the urine is more concentrated and more acidic than during the day. Usually, the more liquid the patient drinks, the lower his need for penicillamine.

A diet with a low methionine content is also recommended, so that the synthesis of cystine is as low as possible. In view of the low protein content, such a diet is not recommended for children during growth and pregnant women.

Poisoning by lead.

Adults: 1-1.5 g per day in fractional doses until the moment when lead excretion in the urine reaches the limit of 0.5 mg per day.

Elderly patients: 20 mg / kg of body weight per day in fractional doses until the moment when lead excretion in the urine reaches the limit of 0.5 mg per day.

Children: 20 mg / kg body weight per day.

Rheumatoid arthritis.

Adults: 250 mg per day during the first month of application. Then the dose is increased every 4-12 weeks by 250 mg until remission of the disease is achieved. After that, apply the minimum effective dose, which allows you to slow down the symptoms of the disease, relapse within 6 months of the drug, the therapeutic effect is not achieved, treatment should be discontinued.

The maintenance dose is usually 500-750 mg per day. Do not exceed the dose of 1.5 grams of medicinal product per day. After achieving remission of the disease lasting 6 months, the dose of the drug is recommended to be gradually reduced by 250 mg every 12 weeks.

Elderly patients: the initial dose should not exceed 250 mg per day during the first month of application. Then the dose can be increased every 4-12 weeks by 250 mg until remission of the disease is achieved. Do not exceed the dose of 1 g of drug per day.

Children: usually 15-20 mg / kg body weight per day. The initial dose is 2.5 - 5.0 mg per day, it can be increased gradually every 4 weeks for 3-6 months to the minimum effective dose, but not more than 500 mg.

Systemic scleroderma.

250 mg per day during the first month of application. Then the dose is increased every 4-12 weeks by 250 mg to 1 g per day, followed by a decrease to 250-500 mg per day.The effect is estimated after 6-12 months of the drug.

Side effects:

Anorexia, nausea, vomiting, diarrhea, aphthous stomatitis, glossitis; intrahepatic cholestasis, pancreatitis; skin rash; epidermal necrolysis; complete loss or distortion of taste sensations, reversible polyneuritis (due to a deficiency of pyridoxine); nephritis, hematuria; eosinophilia, thrombocytopenia, leukopenia; anemia (aplastic or hemolytic), agranulocytosis; Allergic alveolitis, interstitial pneumonitis, diffuse fibrosing alveolitis, Goodpasture's syndrome; myasthenia gravis, polymyositis, dermatomyositis, polyneuritis; fever; lupus-like reactions (arthralgia, myalgia, erythematous rash, the appearance of antinuclear antibodies and antibodies to DNA); increased mammary glands with the development of galactorrhea (in women); alopecia.

Overdose:There have been no cases of overdose. The antidote is unknown. Treatment is symptomatic.
Interaction:

Kuprenil® is a vitamin antagonist AT6.

The drug can not be used with drugs that can cause a violation of bone marrow function.

The preparation forms persistent complex compounds with heavy metals.

Increase the risk of side effects of antimalarial drugs, levamisole and phenylbutazone.

Antacids reduce the absorption of the drug.

Special instructions:

When using Kuprenil®, you need constant medical supervision: a complete blood test (including platelet count) and urine every three days, then every week; control of kidney function; general and neurological examinations every month. In case of appearance of side effects, which the patient is obliged to inform the doctor, the drug should be immediately canceled, and after their termination it can be reapplied, at the doctor's discretion, starting from the lowest dose.

Precautions should be taken with the simultaneous use of Kuprenil® and anti-inflammatory or other agents that can cause dysfunction of the stagnant brain.

In the case of withdrawal of gold preparations, due to lack of effect, Kuprenil® can be used after 6 months.

Patients with impaired renal function should accordingly reduce the dose of the drug and apply it with caution.

If a patient is recommended iron therapy, a two-hour interval should be observed with Kuprenil®.

Due to the influence of penicillamine on collagen and elastin, any surgical interventions (including dental) during the period of drug use should be performed with caution.

During treatment, urine tests and clinical blood tests should be monitored once every 2 weeks during the first 6 months of treatment, then monthly; 1 time in 6 months control the function of the kidneys and liver. In case of Wilson-Konovalov's disease or cystinuria, concomitantly with penicillamine it is prescribed for permanent admission pyridoxine (due to dietary restrictions used to treat these diseases); with prolonged treatment, these patients should regularly perform X-ray or ultrasound examination of the kidneys and urinary tract. When using Kuprenil®, it is necessary to compensate for the lack of vitamin B6. In case of signs of pyridoxine deficiency in patients with rheumatoid arthritis, in the event that these signs do not pass by themselves, 25 mg of pyridoxine per day is additionally prescribed. In the case of development against the background of treatment of fever, the increase of proteinuria, the appearance of hematuria, the defeat of the lungs,expressed hematologic or neurologic disorders, myasthenia gravis, hemosturia-like reactions or other serious adverse reactions, the drug is canceled and, if necessary, glucocorticosteroids are prescribed. In the case of isolated proteinuria, if it does not increase and does not exceed 1 g / day, penicillamine treatment is continued, in other cases - canceled.

Effect on the ability to drive transp. cf. and fur:The drug does not cause disturbances in psychophysical functions, ability to drive vehicles and service moving mechanical devices.
Form release / dosage:

Film coated tablets 250 mg.

Packaging:

For 15 tablets in a blister of PVC and aluminum foil. Two blisters are placed in a cardboard box together with instructions for use.

100 tablets per bottle of high-density polyethylene with a screw cap made of polypropylene with a sealed gasket. Each bottle is placed in a cardboard box along with the instructions for use.

Storage conditions:

Store at temperatures between 15 ° C and 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package!

Terms of leave from pharmacies:On prescription
Registration number:П N013649 / 01
Date of registration:08.10.2008 / 26.04.2016
Expiration Date:Unlimited
The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel
Manufacturer: & nbsp
Representation: & nbspTeva Teva Israel
Information update date: & nbsp07.02.2018
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