Penicillamine (penicillaminum)
PENITSILLAMIN (Penicillaminum).
D-2- Amino-3- merkapto-3- metilmaslyanaya acid, or 3-D, 3-dimetiltsistein.
Synonyms : Artamin, Kuprenil, Artamin, Beracilline, Cuprenil, Cuprimine, Cupripen, Depamine, Distamine, b-Mercaptovalin, Mercaptyl, Metalcaptase, d-Penicillamin, Sulredox, Troloval and others.
Penicillamine, a synthetic drug, which can be seen on the structure of the molecule as penicillin and is dimetilnym tsisteina amino acid derivatives. The preparation of optically active. Implemented in the form of D-shape, as the L-shape and the racemate more toxic.
The main feature is its high penitsillamina Complexing action against metal ions. It connects primarily ions of copper, mercury, lead and iron, and calcium. Both complexes are removed kidneys.
Penicillamine use in acute and chronic poisoning these metals, as well as disease-Vestfalya Wilson-Konovalov (gepatotserebralnoy dystrophy). The drug enhances remove excess copper from urine tissue of patients suffering from this disease, and there is a more effective than standard connections (see Unitiol).
In addition, Penicillamine suppresses synthesis of collagen in the body and normalize relations between the soluble and insoluble fractions, thus promoting a braking sclerosing development process in the tissues. Under the influence of drugs reduces pathological makroglobulinov, including rheumatoid factor.
When ingestion Penicillamine quickly absorbed and long detected in plasma; The half was 24-75 h.
Assign Penicillamine adults with various forms of rheumatoid arthritis in the absence of effects from the use of conventional anti funds. Penicillamine is regarded as one of the major ( "core") in the treatment of the disease.
Applied also in the system sclerodermia and some other diseases.
Is drug inside through 2 - 2, 5 h after the meal.
In rheumatoid arthritis begin with doses of 150-300 mg per day. After every 2 to 4 weeks increases the dose to 150 mg total daily dose of 600 mg '. The first signs of clinical improvement (decrease artralgy, morning constraints, ekssudativnyh events in joints, etc.) usually occur in 2 to 3 months, less later. Once the therapeutic effect of drugs taken daily maintenance dose of 0,15 - 0,3 g.
When the system sclerodermia Penicillamine nominated in the daily dose of 0,15 - 0,3 g within 7 to 10 days. With good endurance daily dose increased to 0.15 grams each week and bring it to 1 to 2 g. In this dose drug is used for 6 months, then reduce the dose of 0.15 g per week to 0.3 grams per day. Supporting dose of 0.3 grams per day.
Duration of treatment one year or more.
When illness Vestfalya-Wilson-Konovalov using high doses (2 g in the early days), under the control of general and the copper content in the urine. Children over 6 years appoint 0.25 g 1 per day. There are, however, data on penitsillamina (to avoid side effects) with the disease in smaller doses. Started with doses of 0.15 grams per day (for 6 - 8 weeks), then bring to 0.9 grams (but no more than 1, 5 grams) per day. Large doses can cause elevated liver elimination of copper in the blood with the development of haemolytic Stroke. When improve, reduce the daily dose of up to 0.6 - 0.45 g. At the same time, designate pyridoxine (60-100 mg / day). Treatment for long.
In applying penitsillamina various possible adverse reactions. There may develop allergic reactions (skin, etc.), gastrointestinal disorders (loss of appetite, nausea, vomiting, diarrhea), gingivitis, stomatitis, loss of taste. Possible radiation, thrombocytopenia, agranulotsitoz, mialgiya, arthralgia, male phenomenon. With long-term use, there Nephrotoxic Effects (proteinuriya, hematuria), in rare cases volchanochnopodobny, pemfigusopodobny syndromes.
In the treatment process to be systematically studied picture of the blood, a urine, liver function test (at least 1 in every 3 months).
When illness Vestfalya-Wilson-Konovalov periodically exploring the copper content in the urine.
The drug is not suitable for high sensitivity to penicillin, pregnancy, radiation and thrombocytopenia, severe kidney failure, bronchial asthma.
Product : capsules of 0.15 g.
Storage : List B. In dry place at room temperature (not above + 25 'C).
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