Medication Description: Penicillamine (Penicillaminum)
D-2-Amino-3-mercapto-3-methyl butyric acid, or D-3, 3-dimethylcysteine.
Synonyms: Artamin, Kuprenil, Artamin, Beracilline, Cuprenil, Cuprimine, Cupripen, Depamine, Distamine, b-Mercaptovalin, Mercaptyl, Metalcaptase, d-Penicillamin, Sulredox, Troloval, etc.
Penicillamine is a synthetic drug that, by its structure, can be considered as part of the penicillin molecule and is a dimethyl derivative of the amino acid cysteine. The drug is optically active. It is used in the form of the D-form, since the L-form and the racemate are more toxic.
The main property of penicillamine is its high complexing activity against metal ions. It mainly binds ions of copper, mercury, lead and iron, as well as calcium. The resulting complexes are removed by the kidneys.
Penicillamine is used in acute and chronic poisoning with these metals, as well as in Westphal-Wilson-Konovalov disease (hepatocerebral dystrophy). The drug enhances the removal with urine of excess copper from the tissues of patients suffering from this disease, and is reportedly more effective than typical compounds (see Unithiol).
In addition, penicillamine suppresses collagen synthesis in the body and normalizes the relationship between its soluble and insoluble fractions, thereby contributing to the inhibition of the development of the sclerosing process in tissues. Under the influence of the drug, the level of pathological macroglobulins, including rheumatoid factor, is reduced.
When ingestion penicillamine is rapidly absorbed and is detected in the blood plasma for a long time; the elimination half-life makes 24 - 75 h.
Penicillamine is prescribed for adults with various forms of rheumatoid arthritis in the absence of the effect of the use of conventional anti-inflammatory drugs. Penicillamine is considered as one of the main ("basic") agents in the treatment of this disease.
Applied also with systemic scleroderma and in some other diseases.
Take the drug inside through 2 - 2, 5 hours after meals.
In rheumatoid arthritis, a dose of 150-300 mg per day is started. Every 2 to 4 weeks, the dose is increased by 150 mg to a total daily dose of 600 mg. The first signs of clinical improvement (reduction of arthralgia, morning stiffness, exudative phenomena in the joints, etc.) usually appear after 2 - 3 months, less often at a later time. When a therapeutic effect is achieved, the drug is taken in a supporting daily dose of 0.15 - 0.3 g.
In systemic scleroderma, penicillamine is prescribed in a daily dose of 0.15–0.3 g for 7–10 days. With good tolerance, the daily dose is increased by 0.15 g every week and adjusted to 1-2 g. At this dose, the drug is used for 6 months, then the dose is reduced by 0.15 g every week to 0.3 g per day. Maintenance dose is 0.3 g per day.
Duration of treatment is 1 year or more.
In Westphal-Wilson-Konovalov disease, large doses are used (2 g each in the first days), under the control of the general condition and the copper content in the urine. Children over 6 years old appoint 0.25 g 1 time per day.