Cuprenil coated pills 250mg N100
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Active ingredients
Penicillamine
Release form
Pills
Composition
In 1 tablet: penicillamine 250 mg.; Excipients: potato starch, lactose monohydrate, povidone, talc, magnesium stearate.
Pharmacological effect
Complexing compound. Forms chelate complexes with ions of copper, mercury, lead, iron, arsenic, calcium, zinc, cobalt, gold. When interacting with the amino acid cysteine forms a disulfide, which has a significantly greater solubility than cysteine. It is supposed that penicillamine affects various parts of the immune system (suppression of T-helper function of lymphocytes, inhibition of neutrophil chemotaxis and secretion of enzymes from the lysosomes of these cells, enhancement of macrophage function). It has the ability to disrupt the synthesis of collagen by cleaving cross-links between newly synthesized tropocollagen molecules. In addition, penicillamine is a pyridoxine antagonist (vitamin B6).
Pharmacokinetics
After ingestion, absorption from the gastrointestinal tract is about 50%. Maximum absorption is observed when taking penicillamine 1.5 h after a meal. Unchanged penicillamine and its metabolites are excreted by the kidneys and through the intestines. About 60% is eliminated within 24 hours. At present, there is no satisfactory method for determining the level of penicillamine in the blood plasma.
Indications
Konovalov-Wilson disease, cystinuria, rheumatoid arthritis.
Contraindications
Lactation (breastfeeding); hypersensitivity to penicillamine.
Use during pregnancy and lactation
During pregnancy in patients with Konovalov-Wilson's disease or cystinuria, penicillamine therapy is continued at a dose of no more than 1 g / day, in patients with rheumatoid arthritis, penicillamine is canceled. If you need penicillamine during lactation, breastfeeding should be stopped.
Dosage and administration
Set individually, taking into account the indications and the patient's response to treatment. Single dose - no more than 500 mg.; In case of Konovalov-Wilson's disease, the daily dose for adults is 0.75-1.5 g. The dose is considered effective if the daily excretion of copper in urine (after the first week of treatment) exceeds 2 mg.In the future, the adequacy of the dose is determined on the basis of measuring the level of free copper in the serum (it should be less than 10 μg / ml). In some cases, the dose may be 2 g / day or more. For children, 20 mg / kg / day in divided doses, the minimum dose is 500 mg / day. For cystinuria, the daily dose for adults is 1-4 g (2 g on average), for children 30 mg / kg. The daily dose is divided into 4 doses, a large single dose is taken at night. The dose is selected individually on the basis of determining urinary cysteine excretion (the optimal level is 100-200 mg / day in patients with no signs of urolithiasis and not exceeding 100 mg / day in patients with urolithiasis). During treatment, drink plenty of water, it is especially important to take an additional amount of liquid (at least 0.5 l) immediately before bedtime and at night. In rheumatoid arthritis, the initial dose is 125-250 mg / day. Then, in case of good tolerance, the dose is increased by 125 mg every 1-2 months. The first signs of a therapeutic effect are usually noted not earlier than the 3rd month of continuous administration. If by this time there is no therapeutic effect, provided that it is well tolerated, the dose will continue to be gradually increased (by 125 mg every 1-2 months). In the absence of a therapeutic effect, penicillamine is canceled by 6 months of therapy. When a satisfactory effect is achieved, a constant dose of penicillamine in the same dose is continued for a long time. It is believed that in rheumatoid arthritis, penicillamine is effective in low (250-500 mg / day) and high (750 mg / day or more) doses, but in some patients only high doses are effective. For children with rheumatoid arthritis, the initial dose is 2.5-5 mg / kg / day, maintenance dose - 15-20 mg / kg / day; They are taken on an empty stomach, at least 1 hour before or 2 hours after meals, and not earlier than 1 hour after taking any other medicines.
Side effects
On the part of the digestive system: anorexia, nausea, vomiting, diarrhea, aphthous stomatitis, glossitis; rarely - hepatitis, intrahepatic cholestasis, pancreatitis. From the side of the central nervous system and peripheral nervous system: complete loss or distortion of taste sensations; rarely - reversible polyneuritis (associated with vitamin B6 deficiency); On the part of the urinary system: rarely - nephritis. On the side of the hematopoietic system: rarely - eosinophilia, thrombocytopenia, leukopenia; anemia (aplastic or hemolytic),agranulocytosis; From the endocrine system: rarely - an increase in the mammary glands sometimes with the development of galactorrhea (in women) .; From the respiratory system: rarely - interstitial pneumonitis, diffuse fibrosing alveolitis, Goodpasture syndrome.; From the musculoskeletal system: rarely - myasthenia, polymyositis, dermatomyositis.; Dermatological reactions: rarely - alopecia.; Allergic reactions: skin rash; rarely - epidermal necrolysis, allergic alveolitis, fever; lupus-like reactions (arthralgia, myalgia, erythematous rash, the appearance of antinuclear antibodies and antibodies to DNA in the blood).
Interaction with other drugs
Iron preparations reduce the absorption of penicillamine and weaken its therapeutic effect. Penicillamine enhances the neurotoxic effect of isoniazid. With simultaneous use with penicillamine, a decrease in the level of digoxin in the blood plasma is possible.
special instructions
Given the possibility of serious, sometimes life-threatening adverse reactions (especially frequent in patients with rheumatoid arthritis), penicillamine is used only under constant medical supervision. During treatment, a urinalysis and a clinical blood test should be monitored 1 time in 2 weeks during the first 6 months of treatment, then monthly; Liver function is monitored 1 time in 6 months. In case of Konovalov-Wilson's disease or cystinuria, penicillamine is prescribed vitamin C 6 for continuous use (due to dietary restrictions used to treat these diseases); With prolonged treatment, these patients should be regularly x-rayed or ultrasound of the kidneys and urinary tract. If signs of vitamin B6 deficiency develop in patients with rheumatoid arthritis, as well as if the symptoms of this deficiency do not resolve on their own, vitamin B6 is also prescribed at a dose of 25 mg / day. A slow, gradual increase in the dose of penicillamine reduces the frequency of some adverse reactions. If a fever, lung, liver, pronounced hematological or neurological disorders, myasthenia, hematuria, lupus-like reactions or other serious adverse reactions develop, penicillamine is canceled and, if necessary, GCS is prescribed.In the case of the development of isolated proteinuria, if it does not increase and does not exceed 1 g / day, penicillamine treatment is continued, in other cases it is canceled.