• Metalcaptase indications
• Uses of Metalcaptase in details
• Metalcaptase description
• Metalcaptase dosage
• Metalcaptase interactions
• Metalcaptase side effects
• Metalcaptase contraindications

What is Metalcaptase?

Metalcaptase is a chelating (KEE-late-ing) agent that binds to excess copper and removes it from the blood stream. In certain conditions, excess copper can build up in the blood stream, leading to tissue damage throughout the body.

Metalcaptase is used to remove excess copper in people with an inherited condition called Wilson's disease.

Metalcaptase is also used to reduce urine levels of an amino acid called cystine, which can cause stones to form in the kidneys and bladder in people with an inherited condition called cystinuria.

Metalcaptase is also used to treat severe rheumatoid arthritis after other medicines have been tried without success. This medicine is not approved to treat juvenile rheumatoid arthritis.

Metalcaptase may also be used for purposes not listed in this medication guide.

Metalcaptase indications

Metalcaptase is 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 Metalcaptase is not of value in ankylosing spondylitis.

Wilson's Disease

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 treatment for Wilson's disease: (1) the symptomatic, and (2) the asymptomatic in whom it can be assumed the disease will develop in the future if the patient is not treated.

The diagnosis, if suspected on the basis of family or individual history or physical examination, can be confirmed if the plasma copper-protein ceruloplasmin** is < 20 mg/dL and either a quantitative determination in a liver biopsy specimen shows an abnormally high concentration of copper ( > 250 mcg/g dry weight) or Kayser-Fleischer rings are present.

Treatment has two objectives:

• to minimize dietary intake of copper;
• to promote excretion and complex formation (i.e., detoxification) of excess tissue copper.

The first objective is attained by a daily diet that contains no more than one or two milligrams of copper. Such a diet should exclude, most importantly, chocolate, nuts, shellfish, mushrooms, liver, molasses, broccoli, and cereals and dietary supplements enriched with copper, and be composed to as great an extent as possible of foods with a low copper content. Distilled or demineralized water should be used if the patient's drinking water contains more than 0.1 mg of copper per liter.

For the second objective, a copper chelating agent is used.

In symptomatic patients this treatment usually produces marked neurologic improvement, fading of Kayser-Fleischer rings, and gradual amelioration of hepatic dysfunction and psychic disturbances.

Clinical experience to date suggests that life is prolonged with the above regimen.

Noticeable improvement may not occur for one to three months. Occasionally, neurologic symptoms become worse during initiation of therapy with Metalcaptase. Despite this, the drug should not be withdrawn. Temporary interruption carries an increased risk of developing a sensitivity reaction upon resumption of therapy, although it may result in clinical improvement of neurological symptoms. If the neurological symptoms and signs continue to worsen for a month after the initiation of Metalcaptase therapy, several short courses of treatment with 2,3 - dimercaprol (BAL) while continuing Metalcaptase may be considered.

Treatment of asymptomatic patients has been carried out for over thirty years. Symptoms and signs of the disease appear to be prevented indefinitely if daily treatment with Metalcaptase is continued.

Cystinuria

Cystinuria is characterized by excessive urinary excretion of the dibasic amino acids, arginine, lysine, ornithine, and cystine, and the mixed disulfide of cysteine and homocysteine. The metabolic defect that leads to cystinuria is inherited as an autosomal, recessive trait. Metabolism of the affected amino acids is influenced by at least two abnormal factors: (1) defective gastrointestinal absorption and (2) renal tubular dysfunction.

Arginine, lysine, ornithine, and cysteine are soluble substances, readily excreted. There is no apparent pathology connected with their excretion in excessive quantities.

Cystine, however, is so slightly soluble at the usual range of urinary pH that it is not excreted readily,and so crystallizes and forms stones in the urinary tract. Stone formation is the only known pathology in cystinuria.

Normal daily output of cystine is 40 to 80 mg. In cystinuria, output is greatly increased and may exceed 1 g/day. At 500 to 600 mg/day, stone formation is almost certain. When it is more than 300 mg/day, treatment is indicated.

Conventional treatment is directed at keeping urinary cystine diluted enough to prevent stone formation, keeping the urine alkaline enough to dissolve as much cystine as possible, and minimizing cystine production by a diet low in methionine (the major dietary precursor of cystine). Patients must drink enough fluid to keep urine specific gravity below 1.010, take enough alkali to keep urinary pH at 7.5 to 8, and maintain a diet low in methionine. This diet is not recommended in growing children and probably is contraindicated in pregnancy because of its low protein content.

When these measures are inadequate to control recurrent stone formation, Metalcaptase may be used as additional therapy, and when patients refuse to adhere to conventional treatment, Metalcaptase may be a useful substitute. It is capable of keeping cystine excretion to near normal values, thereby hindering stone formation and the serious consequences of pyelonephritis and impaired renal function that develop in some patients.

Bartter and colleagues depict the process by which Metalcaptase interacts with cystine to form Metalcaptase-cysteine mixed disulfide as:

CSSC = cystine

CS' = deprotonated cysteine

PSSP = Metalcaptase disulfide

PS' = deprotonated Metalcaptase sulfhydryl

CSSP = Metalcaptase-cysteine mixed disulfide

In this process, it is assumed that the deprotonated form of Metalcaptase, PS', is the active factor in bringing about the disulfide interchange.

Rheumatoid Arthritis

Because Metalcaptase can cause severe adverse reactions, its use in rheumatoid arthritis should be restricted to patients who have severe, active disease and who have failed to respond to an adequate trial of conventional therapy. Even then, benefit-to-risk ratio should be carefully considered. Other measures, such as rest, physiotherapy, salicylates, and corticosteroids should be used, when indicated, in conjunction with Metalcaptase.

How should I use Metalcaptase?

Use Metalcaptase as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Take Metalcaptase on an empty stomach (1 hour before meals or 2 hours after meals).
• Take Metalcaptase at least 2 hours before or after other medicines containing aluminum or magnesium (antacids), iron, or vitamins that contain iron.
• If you are taking Metalcaptase for cystinuria, drink plenty of water while taking Metalcaptase. Drink a pint (16 ounces [480 mL]) at bedtime and another pint during the night, unless directed otherwise by your doctor.
• It may take 1 to 3 months for Metalcaptase to work.
• If you miss a dose of Metalcaptase, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Metalcaptase.

Uses of Metalcaptase in details

Treatment of rheumatoid arthritis, Wilson's disease and prevention of cystine kidney stones.

Metalcaptase description

Metalcaptase is a pharmaceutical of the chelator class. The pharmaceutical form is D-Metalcaptase, as L-Metalcaptase is toxic (it inhibits the action of pyridoxine). It is an α-amino acid metabolite of penicillin, although it has no antibiotic properties.

Metalcaptase dosage

Metalcaptase Dosage

Generic name: Metalcaptase 250mg

Dosage form: tablet

The information at Drugs.com is not a substitute for medical advice. Always consult your doctor or pharmacist.

In all patients receiving Metalcaptase, it is important that Metalcaptase be given on an empty stomach, at least one hour before meals or two hours after meals, and at least one hour apart from any other drug, food, or milk. Because Metalcaptase increases the requirement for pyridoxine, patients may require a daily supplement of pyridoxine.

Wilson’s Disease - Optimal dosage can be determined by measurement of urinary copper excretion and the determination of free copper in the serum. The urine must be collected in copper-free glassware, and should be quantitatively analyzed for copper before and soon after initiation of therapy with Metalcaptase.

Determination of 24-hour urinary copper excretions is of greatest value in the first week of therapy with Metalcaptase. In the absence of any drug reaction, a dose between 0.75 and 1.5 g that results in an initial 24-hour cupriuresis of over 2 mg should be continued for about three months, by which time the most reliable method of monitoring maintenance treatment is the determination of free copper in the serum. This equals the difference between quantitatively determined total copper and ceruloplasmin-copper. Adequately treated patients will usually have less than 10 mcg free copper/dL of serum. It is seldom necessary to exceed a dosage of 2 g/day. If the patient is intolerant to therapy with Metalcaptase, alternative treatment is trientine hydrochloride.

In patients who cannot tolerate as much as 1 g/day initially, initiating dosage with 250 mg/day, and increasing gradually to the requisite amount, gives closer control of the effects of the drug and may help to reduce the incidence of adverse reactions.

Cystinuria - It is recommended that Metalcaptase be used along with conventional therapy. By reducing urinary cystine, it decreases crystalluria and stone formation. In some instances, it has been reported to decrease the size of, and even to dissolve, stones already formed.

The usual dosage of Metalcaptase in the treatment of cystinuria is 2 g/day for adults, with a range of 1 to 4 g/day. For pediatric patients, dosage can be based on 30 mg/kg/day. The total daily amount should be divided into four doses. If four equal doses are not feasible, give the larger portion at bedtime. If adverse reactions necessitate a reduction in dosage, it is important to retain the bedtime dose.

Initiating dosage with 250 mg/day, and increasing gradually to the requisite amount, gives closer control of the effects of the drug and may help to reduce the incidence of adverse reactions.

In addition to taking Metalcaptase, patients should drink copiously. It is especially important to drink about a pint of fluid at bedtime and another pint once during the night when urine is more concentrated and more acid than during the day. The greater the fluid intake, the lower the required dosage of Metalcaptase.

Dosage must be individualized to an amount that limits cystine excretion to 100-200 mg/day in those with no history of stones, and below 100 mg/day in those who have had stone formation and/or pain. Thus, in deter-mining dosage, the inherent tubular defect, the patient’s size, age, and rate of growth, and his diet and water intake all must be taken into consideration.

The standard nitroprusside cyanide test has been reported useful as a qualitative measure of the effective dose*:

* Lotz, M., Potts, J.T. and Bartter, F.C.: BritMed J 2: 521, August 28, 1965 (in Medical Memoranda).

Add 2 mL of freshly prepared 5 percent sodium cyanide to 5 mL of a 24-hour aliquot of protein-free urine and let stand ten minutes. Add 5 drops of freshly prepared 5 percent sodium nitroprusside and mix. Cystine will turn the mixture magenta. If the result is negative, it can be assumed that cystine excretion is less than 100 mg/g creatinine.

Although Metalcaptase is rarely excreted unchanged, it also will turn the mixture magenta. If there is any question as to which substance is causing the reaction, a ferric chloride test can be done to eliminate doubt: Add 3 percent ferric chloride dropwise to the urine. Metalcaptase will turn the urine an immediate and quickly fading blue. Cystine will not produce any change in appearance.

Rheumatoid Arthritis - The principal rule of treatment with Metalcaptase in rheumatoid arthritis is patience. The onset of therapeutic response is typically delayed. Two or three months may be required before the first evidence of a clinical response is noted.

When treatment with Metalcaptase has been interrupted because of adverse reactions or other reasons, the drug should be reintroduced cautiously by starting with a lower dosage and increasing slowly.

Initial Therapy - The currently recommended dosage regimen in rheumatoid arthritis begins with a single daily dose of 125 mg or 250 mg which is thereafter increased at one to three month intervals, by 125 mg or 250 mg/day, as patient response and tolerance indicate. If a satisfactory remission of symptoms is achieved, the dose associated with the remission should be continued. If there is no improvement and there are no signs of potentially serious toxicity after two to three months of treatment with doses of 500-750 mg/day, increases of 250 mg/day at two to three month intervals may be continued until a satisfactory remission occurs or signs of toxicity develop. If there is no discernible improvement after three to four months of treatment with 1000 to 1500 mg of Metalcaptase/day, it may be assumed the patient will not respond and Metalcaptase should be discontinued.

Maintenance Therapy - The maintenance dosage of Metalcaptase must be individualized, and may require adjustment during the course of treatment. Many patients respond satisfactorily to a dosage within the 500-750 mg/day range. Some need less.

Changes in maintenance dosage levels may not be reflected clinically or in the erythrocyte sedimentation rate for two to three months after each dosage adjustment.

Some patients will subsequently require an increase in the maintenance dosage to achieve maximal disease suppression. In those patients who do respond, but who evidence incomplete suppression of their disease after the first six to nine months of treatment, the daily dosage of Metalcaptase may be increased by 125 mg or 250 mg/day at three-month intervals. It is unusual in current practice to employ a dosage in excess of 1 g/day, but up to 1.5 g/day has sometimes been required.

Management of Exacerbations - During the course of treatment some patients may experience an exacerbation of disease activity following an initial good response. These may be self-limited and can subside within twelve weeks. They are usually controlled by the addition of nonsteroidal anti-inflammatory drugs, and only if the patient has demonstrated a true “escape” phenomenon (as evidenced by failure of the flare to subside within this time period) should an increase in the maintenance dose ordinarily be considered.

In the rheumatoid patient, migratory polyarthralgia due to Metalcaptase is extremely difficult to differentiate from an exacerbation of the rheumatoid arthritis. Discontinuance or a substantial reduction in the dosage of Metalcaptase for up to several weeks will usually determine which of these processes is responsible for the arthralgia.

Duration of Therapy - The optimum duration of Metalcaptase therapy in rheumatoid arthritis has not been determined. If the patient has been in remission for six months or more, a gradual, stepwise dosage reduction in decrements of 125 mg or 250 mg/day at approximately three month intervals may be attempted.

Concomitant Drug Therapy - Metalcaptase should not be used in patients who are receiving gold therapy, anti-malarial or cytotoxic drugs, oxyphenbutazone, or phenylbutazone. Other measures, such as salicylates, other nonsteroidal anti-inflammatory drugs or systemic corticosteroids may be continued when Metalcaptase is initiated. After improvement commences, analgesic and anti-inflammatory drugs may be slowly discontinued as symptoms permit. Steroid withdrawal must be done gradually, and many months of Metalcaptase treatment may be required before steroids can be completely eliminated.

Dosage Frequency - Based on clinical experience, dosages up to 500 mg/day can be given as a single daily dose. Dosages in excess of 500 mg/day should be administered in divided doses.

More about Metalcaptase (Metalcaptase)

• Side Effects
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• Dosage Information
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Consumer resources

• Metalcaptase
• Metalcaptase (Advanced Reading)

• Other brands: Metalcaptase

Professional resources

• Metalcaptase (FDA)
• Metalcaptase (AHFS Monograph)

Other formulations

• Metalcaptase

Related treatment guides

• Cystinuria
• Rheumatoid Arthritis
• Wilson's Disease

Metalcaptase interactions

See also:
What other drugs will affect Metalcaptase?

Digoxin: Metalcaptase may decrease the serum concentration of Digoxin. Monitor therapy

Gold Sodium Thiomalate: May enhance the adverse/toxic effect of Metalcaptase. Specifically, this combination may increase the risk for serious hematologic and/or renal adverse reactions. Avoid combination

Polyvalent Cation Containing Products: May decrease the serum concentration of Metalcaptase. Management: Separate the administration of Metalcaptase and oral polyvalent cation containing products by at least 1 hour. Consider therapy modification

Metalcaptase side effects

See also:
What are the possible side effects of Metalcaptase?

Applies to Metalcaptase: oral capsule, oral tablet

Along with its needed effects, Metalcaptase (the active ingredient contained in Metalcaptase) may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor as soon as possible if any of the following side effects occur while taking Metalcaptase:

More Common

• Fever
• joint pain
• lesions on the face, neck, scalp, and/or trunk
• skin rash, hives, or itching
• swollen and/or painful glands
• ulcers, sores, or white spots on lips or in mouth

Less Common

• Bloody or cloudy urine
• shortness of breath, troubled breathing, tightness in chest, or wheezing
• sore throat and fever with or without chills
• swelling of face, feet, or lower legs
• unusual bleeding or bruising
• unusual tiredness or weakness
• weight gain

Rare

• Abdominal or stomach pain (severe)
• blisters on skin
• bloody or black, tarry stools
• chest pain
• coughing or hoarseness
• dark urine
• difficulty in breathing, chewing, talking, or swallowing
• eye pain, blurred or double vision, or any change in vision
• general feeling of discomfort or illness or weakness
• lower back or side pain
• muscle weakness
• painful or difficult urination
• pale stools
• pinpoint red spots on skin
• redness, tenderness, itching, burning, or peeling of skin
• red or irritated eyes
• red, thick, or scaly skin
• ringing or buzzing in the ears
• spitting blood
• yellow eyes or skin

Some side effects of Metalcaptase may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More Common

• Diarrhea
• lessening or loss of sense of taste
• loss of appetite
• nausea or vomiting
• stomach pain (mild)

Metalcaptase contraindications

See also:
What is the most important information I should know about Metalcaptase?

Except for the treatment of Wilson’s disease or certain patients with cystinuria, use of Metalcaptase during pregnancy is contraindicated.

Although breast milk studies have not been reported in animals or humans, mothers on therapy with Metalcaptase should not nurse their infants.

Patients with a history of Metalcaptase-related aplastic anemia or agranulocytosis should not be restarted on Metalcaptase.

Because of its potential for causing renal damage, Metalcaptase should not be administered to rheumatoid arthritis patients with a history or other evidence of renal insufficiency.

Active ingredient matches for Metalcaptase:

Penicillamine in Czech Republic, Germany, Japan, Luxembourg, Taiwan.

Unit description / dosage (Manufacturer)	Price, USD
Tablet, Enteric Coated; Oral; Penicillamine 150 mg
Tablet, Enteric Coated; Oral; Penicillamine 300 mg
Metalcaptase 150 mg
Metalcaptase 300 mg x 20's
List of Metalcaptase substitutes (brand and generic names):
Distamine (Ireland, Malta, United Kingdom)
DISTAMINE 500MG TABLET 1 strip / 10 tablets each (Neon Laboratories Ltd)	$ 7.15
Distamine 500mg Tablet (Neon Laboratories Ltd)	$ 0.72
Distamine 125 / 250mg Film-coated tablets (United Kingdom)
Gerodyl (Netherlands)
Kelatin (Netherlands, Belgium)
Kelatine (Portugal)
Kuprenil
Mercaptovaline
Mercaptyl (Switzerland)
Tablet, Film-Coated; Oral; Penicillamine 150 mg (Abbott)
Tablet, Film-Coated; Oral; Penicillamine 300 mg (Abbott)
Pemine (Italy)
PENAMINE (India)
250 mg x 10's (Medi Globe)	$ 1.81
PENAMINE cap 250 mg x 10's (Medi Globe)	$ 1.81
Pendramine (United Kingdom)
Penicillamine (Austria, Jordan, Kuwait, Lebanon, Oman, Qatar, Saudi Arabia, Sudan, United Arab Emirates, Yemen)
Penicillamine/ d- powder	$ 8.88
Cuprimine 250 mg capsule	$ 5.63
Depen 250 mg titratab	$ 4.73
Penicillamine powder	$ 2.81
Pénicillamine
Penicillamine/ d- powder	$ 8.88
Cuprimine 250 mg capsule	$ 5.63
Depen 250 mg titratab	$ 4.73
Penicillamine powder	$ 2.81
Penicillamine/ d- powder	$ 8.88
Cuprimine 250 mg capsule	$ 5.63
Depen 250 mg titratab	$ 4.73
Penicillamine powder	$ 2.81
Penicillamine - Sine Pharm (China)
Penicillamine Ifet (Greece)
Penicillamine Kent (United Kingdom)
Penicitin (India)
Penicitin 250mg CAP / 10 (Samarth)	$ 1.78
PENICITIN 250 MG CAPSULE 1 strip / 10 capsules each (Samarth)	$ 1.75
PENICITIN cap 250 mg x 10's (Samarth)	$ 1.66
Penicitin 250mg Capsule (Samarth)	$ 0.17
Perdolat
Retadel (Egypt)
Rhumantin (Denmark)
Sufirtan
Sufortan (Mexico)
Sufortanon (Spain)
Trisorcin (Germany)
Trolovol (France)
Tablet, Film-Coated; Oral; Penicillamine 300 mg (Asta medica)
See 98 substitutes for Metalcaptase

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Information checked by Dr. Sachin Kumar, MD Pharmacology