Penicillamin

Packaging and storage: Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight container. /Penicillamine capsules USP/

Packaging and storage: Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight container. /Penicillamine tablets USP/

DOWNWARD ADJUSTMENT OF DOSAGE OF OTHER ANTI-INFLAMMATORY DRUGS, ESP CORTICOSTEROIDS, IS OFTEN POSSIBLE AFTER ADDN OF PENICILLAMINE TO DRUG REGIMEN.

Pyridoxine, 10-25 mg/day, should be administered concomitantly because penicillamine inhibits pyridoxal-dependent enzymes.

Concurrent use /of 4-aminoquinolines or bone marrow depressants ... or gold compounds or immunosuppressants, excepting glucocorticoids/ with penicillamine may increase the potential for serious hematologic and/or renal adverse reactions.

Concurrent use with 4-aminoquinolines may ... increase the risk of severe dermatologic reactions.

For more Interactions (Complete) data for (D)-PENICILLAMINE (8 total), please visit the HSDB record page.

Penicillamine has been linked to a characteristic pattern of liver injury arising 1 to 6 weeks after starting therapy, with a distinctly cholestatic pattern of serum enzyme elevations (Case 1). The jaundice due to penicillamine can be severe and prolonged and result in protracted, symptomatic cholestasis, but most cases are self-limited. Immunoallergic manifestations of rash, fever and eosinophilia are common, but not invariable. Interesting, most cases of acute liver injury attributed to penicillamine were reported in patients with rheumatic diseases, only rare instances being reported in Wilson disease.

Occupational hepatotoxin - Secondary hepatotoxins: the potential for toxic effect in the occupational setting is based on cases of poisoning by human ingestion or animal experimentation.

Most Common Adverse Effects

ACUTE SENSITIVITY REACTIONS, MANIFESTED BY FEVER, RASHES (PRURITIC, MORBILLIFORM, & URTICARIAL), LEUKOPENIA, EOSINOPHILIA, & THROMBOCYTOPENIA, HAVE BEEN ENCOUNTERED EARLY IN COURSE OF THERAPY. ... INFREQUENTLY, ANOREXIA, NAUSEA, & VOMITING OCCUR. LOSS OF TASTE FOR SALT & SWEET HAS BEEN OBSERVED.

Serious reactions involving the hematologic system (thromobocytopenia, leukopenia, agranulocytosis, aplastic anemia) and renal system (proteinuria, hypoalbuminemia, nephrotic syndrome. ... Other serious reactions reported occasionally are lupus-like disease, pemphigus, goodpasture's syndrome, mysthenia gravis, and dermatomyositis or polymyositis.

SEVERAL CASES OF NEPHROTOXICITY, INCL PATIENTS GIVEN ONLY D-PENICILLAMINE, HAVE BEEN REPORTED. PRESUMABLY ... RESULT FROM HYPERSENSITIVITY REACTIONS. CASE OF OPTIC NEURITIS ... HAS ALSO OCCURRED. ... AFTER THERAPY FOR 1-2 YEAR'S DURATION,SYSTEMIC LUPUS ERYTHEMATOSUS-LIKE SYNDROME ... OBSERVED.

TOXIC EFFECTS ON EYE HAVE BEEN RARE, CONSISTING OF ISOLATED CASES OF OPTIC NEURITIS, RETINAL HEMORRHAGE, MYOPIA, & SUPERFICIAL INFLAMMATION & IRRITATION OF EYES ASSOC WITH DERMATITIS.

For more Human Toxicity Excerpts (Complete) data for (D)-PENICILLAMINE (21 total), please visit the HSDB record page.

Drug Induced Liver Injury Rank (DILIrank 2.0)

Penicillamine

vLess-DILI-concern

2

Warnings & precautions

DOI:10.1016/j.drudis.2016.02.015

ADMIN OF 500 MG/KG/DAY ORALLY TO MALE RATS FOR 60 DAYS BEFORE MATING DECR BODY WT GAIN, FOOD CONSUMPTION, SPONTANEOUS LOCOMOTOR ACTIVITY, & FERTILITY. HOWEVER, PENICILLAMINE ADMIN TO FEMALES FOR 14 DAYS BEFORE & 7 DAYS AFTER MATING DID NOT.

SINGLE ORAL DOSE ADMIN TO HAMSTERS ON DAY 7 OF GESTATION CAUSED INCR FETAL MORTALITY, GROWTH RETARDATION & MALFORMATION. MOST SEVERE MALFORMATIONS WERE EXENCEPHALY & ENCEPHALOCELE.

1000 MG/KG/DAY GIVEN ORALLY TO RATS FROM DAY 7 TO DAY 17 OF GESTATION PRODUCED DISARRANGEMENT OF VERTEBRAE, CERVICAL RIBS, LUMBAR RIBS, & CAUDAL VERTEBRAE IN FETUSES, & ALSO DECR NEONATAL SURVIVAL RATE. IT DID NOT AFFECT BEHAVIOR, LEARNING ABILITY, & FERTILITY OF OFFSPRING.

PENICILLAMINE-INDUCED MYASTHENIC RESPONSES IN GUINEA PIGS WAS STUDIED. ANIMALS SHOWED EDROPHONIUM CHLORIDE-REPAIRABLE DECREMENTAL RESPONSES TO 30-HZ NERVE STIMULATION. 3 REVEALED POST-TETANIC EXHAUSTION. 11 HAD DECR MINIATURE ENDPLATE POTENTIAL AMPLITUDES, COMPARED WITH 6 CONTROLS.

For more Non-Human Toxicity Excerpts (Complete) data for (D)-PENICILLAMINE (13 total), please visit the HSDB record page.

It is recommended that penicillamine not be used to treat pregnant patients with rheumatoid arthritis and that it be avoided if possible in pregnant patients with cystinuria.

Patients 65 years of age or older may be more likely to develop hematologic toxicity with penicillamine. Also, elderly patients are more likely to have age-related renal function impairment, which increases the risk of adverse renal effects in patients receiving penicillamine for the treatment of rheumatoid arthritis.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

The Approved Drug Products with Therapeutic Equivalence Evaluations List identifies currently marketed prescription drug products, incl penicillamine, approved on the basis of safety and effectiveness by FDA under sections 505 and 507 of the Federal Food, Drug, and Cosmetic Act.

Experimental inducer of convulsions in rats. /L-Penicillamine/

MEDICATION

Use (kg; approx.) in Germany (2009): >250

... BY ACID HYDROLYSIS OF PENICILLIN. IT IS PPTD FROM HYDROLYSIS MIXT AS MERCURIC SALT WHICH IS THEN COLLECTED, SUSPENDED IN WATER, & TREATED WITH HYDROGEN SULFIDE TO LIBERATE FREE ACID. PURIFICATION INVOLVES ONLY RECRYSTALLIZATION FROM WATER.

/D-PENICILLAMINE/ IS THE MOST CHARACTERISTIC DEGRADATION PRODUCT OF PENICILLIN TYPE ANTIBIOTICS.

D-ISOMER IS NATURAL FORM.