PENICILLAMINE Film-coated tablet Ref.[7866] Active ingredients: Penicillamine

Source: Medicines & Healthcare Products Regulatory Agency (GB)  Revision Year: 2016  Publisher: Generics [UK] Limited t/a Mylan, Station Close, Potters Bar, Hertfordshire, EN6 1TL, United Kingdom

Pharmacodynamic properties

Pharmacotherapeutic group: Antirheumatic drugs
ATC code: M01CC01

  1. Penicillamine is used to treat severe active rheumatoid arthritis not adequately controlled by NSAID therapy.
  2. Penicillamine is a chelating agent which aids the elimination from the body of certain heavy metal ions, including copper, lead and mercury, by forming stable soluble complexes with them that are readily excreted by the kidney.
  3. It is used in the treatment of Wilson’s disease (hepatolenticular degeneration), in conjunction with a low copper diet, to promote the excretion of copper.
  4. It may be used to treat asymptomatic lead intoxication.
  5. Penicillamine is used as an adjunct to diet and urinary alkalinisation in the management of cystinuria. By reducing urinary concentrations of cystine, penicillamine prevents the formation of calculi and promotes the gradual dissolution of existing calculi.
  6. Desensitisation. Should the physician deem it necessary to attempt to desensitise a patient to penicillamine, it should be noted that this formulation is not suitable for this purpose.

Pharmacokinetic properties

Penicillamine is a thiol-group containing chelating agent, variably absorbed from the gastrointestinal tract. The drug undergoes a rapid distribution phase, followed by a slower elimination phase.

Penicillamine is strongly plasma-protein bound. Most penicillamine is bound to albumin but some is bound to α-globulins or ceruloplasmin.

Penicillamine is not extensively metabolised in man.

About 80% of the absorbed dose is excreted rapidly in the urine, mostly as mixed disulphides. Some of the dose is excreted as a penicillamine copper complex and some as the S-methyl derivative.

Preclinical safety data

Penicillamine has been shown to be teratogenic in rats when given in doses several times higher than those recommended for human use.

There is no known LD50 value for penicillamine. In studies some rats died after oral administration of 10,000 mg/kg, but intra-peritoneal injections of a dose of 660 mg/kg caused no deaths.

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