PENICILLAMINE capsule

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

penicillamine (UNII: GNN1DV99GX) (penicillamine - UNII:GNN1DV99GX)

Available from:

Breckenridge Pharmaceutical, Inc.

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Penicillamine capsules are indicated in the treatment of Wilson's disease, cystinuria, and in patients with severe, active rheumatoid arthritis who have failed to respond to an adequate trial of conventional therapy. Available evidence suggests that penicillamine capsules are not of value in ankylosing spondylitis. Wilson's disease (hepatolenticular degeneration) occurs in individuals who have inherited an autosomal recessive defect that leads to an accumulation of copper far in excess of metabolic requirements. The excess copper is deposited in several organs and tissues, and eventually produces pathological effects primarily in the liver, where damage progresses to postnecrotic cirrhosis, and in the brain, where degeneration is widespread. Copper is also deposited as characteristic, asymptomatic, golden-brown Kayser-Fleischer rings in the corneas of all patients with cerebral symptomatology and some patients who are either asymptomatic or manifest only hepatic symptomatology. Two types of patients require t

Product summary:

Penicillamine Capsules, USP are size '1' ivory-colored capsules imprinted with 'DP' on cap and '250' on body, filled with white to off white granular powder. They are supplied as follows: NDC 51991-974-01 in bottles of 100 Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Dispense in a tightly closed container. Keep container tightly closed.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

PENICILLAMINE- PENICILLAMINE CAPSULE
BRECKENRIDGE PHARMACEUTICAL, INC.
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PENICILLAMINE CAPSULES, USP 250 MG
Physicians planning to use penicillamine should thoroughly familiarize
themselves
with its toxicity, special dosage considerations, and therapeutic
benefits.
Penicillamine should never be used casually. Each patient should
remain constantly
under the close supervision of the physician. Patients should be
warned to report
promptly any symptoms suggesting toxicity.
DESCRIPTION
Penicillamine, USP is a chelating agent used in the treatment of
Wilson's disease. It is
also used to reduce cystine excretion in cystinuria and to treat
patients with severe,
active rheumatoid arthritis unresponsive to conventional therapy (see
INDICATIONS). It
is 3-mercapto-D-valine. It is a white, or practically white,
crystalline powder, freely soluble
in water, slightly soluble in alcohol, and insoluble in ether,
acetone, benzene, and carbon
tetrachloride. Although its configuration is D, it is levorotatory as
usually measured:
[α] 25° = -62.5° ± 2° (c = 1, 1N NaOH),
D
calculated on a dried basis.
The empirical formula is C H
NO S, giving it a molecular weight of 149.21. The
structural formula is:
It reacts readily with formaldehyde or acetone to form a
thiazolidine-carboxylic acid.
Penicillamine Capsules, USP for oral administration contain 250 mg of
penicillamine. Each
capsule contains the following inactive ingredients: D&C Yellow No.
10, gelatin, lactose
monohydrate, magnesium stearate, titanium dioxide, shellac, black iron
oxide, and
potassium hydroxide. "FDA approved dissolution test differs from the
USP".
CLINICAL PHARMACOLOGY
Penicillamine is a chelating agent recommended for the removal of
excess copper in
patients with Wilson's disease. From _in vitro_ studies which indicate
that one atom of
copper combines with two molecules of penicillamine, it would appear
that 1 g of
penicillamine should be followed by the excretion of about 200 mg of
copper; however,
5
11
2
the actual amount excreted is about 1% of this