Colchicum-Dispert^® (Tablets) Instructions for Use

Marketing Authorization Holder

Pharmaselect International Beteiligungs, GmbH (Germany)

Manufactured By

Haupt Pharma Wulfing, GmbH (Germany)

Primary Packaging

HAUPT PHARMA WULFING, GmbH (Germany)

Secondary Packaging

HAUPT PHARMA WULFING, GmbH (Germany)

Or

MAUERMANN – ARZNEIMITTEL, KG (Germany)

Or

KWIZDA PHARMADISTRIBUTION, GmbH (Austria)

Quality Control Release

PHARMASELECT INTERNATIONAL BETEILIGUNGS, GmbH (Germany)

Contact Information

PHARMASELECT INTERNATIONAL BETEILIGUNGS GMBH (Austria)

ATC Code

M04AC01 (Colchicine)

Active Substance

Colchicine (Ph.Eur. European Pharmacopoeia)

Dosage Form

Colchicum-Dispert®

Film-coated tablets 500 mcg: 20, 40, 60 or 100 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets dark red in color, round, shiny.

* [the extract contains 57-64% lactose, 28-32% microcrystalline cellulose].

Excipients : copovidone – 5.33 mg, corn starch – 27.5 mg, lactose monohydrate – 41.6-43.9 mg, magnesium stearate – 0.33 mg, palmitostearic acid – 1.34 mg, talc – 7 mg, microcrystalline cellulose – 3.6-5.2 mg.

Coating composition acacia gum – 0.3 mg, carnauba wax – 0.14 mg, sodium carboxymethylcellulose – 0.273 mg, magnesium oxide – 2.6 mg, macrogol 6000 – 1.093 mg, Opalux AS 250000 [sucrose – 0.7923 mg, dye Ponceau 4R (E124) – 0.26334 mg, dye Quinoline Yellow (E104) – 0.09652 mg, titanium dioxide (E171) – 0.07904 mg, povidone – 0.0133 mg] – 1.2445 mg, povidone K25 – 2.186 mg, sucrose – 86.1515 mg, talc – 11.975 mg, titanium dioxide (E171) – 3.717 mg, shellac – 0.32 mg.

20 pcs. – blisters (1) – cardboard boxes.
20 pcs. – blisters (2) – cardboard boxes.
20 pcs. – blisters (3) – cardboard boxes.
20 pcs. – blisters (5) – cardboard boxes.

Clinical-Pharmacological Group

Drug affecting uric acid metabolism. Antigout drug

Pharmacotherapeutic Group

Antigout agent

Pharmacological Action

The antigout action of colchicine is associated with a decrease in leukocyte migration to the site of inflammation and inhibition of phagocytosis of microcrystals of uric acid salts. It also has an antimitotic effect, suppresses (completely or partially) cell division in the anaphase and metaphase stages, and prevents neutrophil degranulation. By reducing the formation of amyloid fibrils, it prevents the development of amyloidosis.

It is highly effective for relieving acute gout. Within the first 12 hours of therapy, the condition significantly improves in more than 75% of patients. In 80% of cases, it can cause adverse reactions from the gastrointestinal tract before clinical improvement or simultaneously with it.

At a daily dose of 1-2 mg with daily intake, it reduces the likelihood of recurrent acute attacks in 3/4 of patients with gout.

It prevents acute attacks in patients with familial Mediterranean fever (lowers dopamine-beta-hydroxylase activity).

Increases the life expectancy of patients with primary AL-amyloidosis.

Has a positive effect on the skin (softening, reducing dryness) in systemic scleroderma.

Pharmacokinetics

Absorption

Colchicine is rapidly and intensively absorbed from the gastrointestinal tract. The average C_max in blood plasma is 4.2 ng/ml and is reached approximately 70 minutes after a dose of 1 mg.

Distribution

Colchicine rapidly penetrates into tissues and has a high V_d of 473 L. High concentrations of colchicine are found in the liver, kidneys, spleen, leukocytes, and gastrointestinal tract.

Metabolism and Excretion

T_1/2 is 9.3 hours. Colchicine is metabolized in the liver and excreted mainly with bile. Enterohepatic circulation is detected 4-6 hours after oral administration. The largest part of the administered dose is excreted through the intestines and about 23% through the kidneys.

Indications

• Acute attacks of gout;
• Periodic disease (familial Mediterranean fever).

ICD codes

Dosage Regimen

Orally. The tablets should be swallowed whole, without chewing, with a sufficient amount of liquid.

For an acute attack of gout, take 2 tablets (1 mg of colchicine) first, then 0.5-1.5 mg every 1-2 hours until the pain subsides. The total dose of the drug taken per day should not exceed 8 mg. Repeated administration according to the scheme for treating an acute attack of gout can be carried out no earlier than after 3 days.

For the prevention of acute attacks of gout in the first few months of treatment with uricosuric agents, take 0.5-1.5 mg daily or every other day for (usually) 3 months.

Adverse Reactions

Gastrointestinal disorders diarrhea, nausea, vomiting, and stomach pain.

Blood and lymphatic system disorders rarely – cases of leukopenia, agranulocytosis, hypoplastic anemia.

Musculoskeletal and connective tissue disorders in some cases, myopathy was observed after long-term treatment.

Nervous system disorders in some cases, neuropathy was observed after long-term treatment.

Skin and subcutaneous tissue disorders rarely – alopecia.

Contraindications

• Hypersensitivity to the drug;
• Hepatic insufficiency;
• Renal insufficiency;
• Severe inhibition of bone marrow hematopoiesis;
• Lactose intolerance, lactase deficiency, sucrase/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption;
• Pregnancy;
• Breastfeeding period;
• Children under 18 years of age.

Particular caution should be exercised when prescribing to elderly patients, as well as those with cachexia, severe disorders of the gastrointestinal tract, and cardiovascular system.

With caution

Patients with diabetes mellitus (due to the content of sucrose and lactose in the drug).

Use in Pregnancy and Lactation

Contraindicated during pregnancy and breastfeeding.

Use in Hepatic Impairment

Contraindicated: hepatic insufficiency.

Use in Renal Impairment

Contraindicated: renal insufficiency.

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

Particular caution should be exercised when prescribing to elderly patients.

Special Precautions

Treatment should be carried out under careful hematological and clinical supervision.

If severe side effects from the gastrointestinal tract occur, the dose should be reduced or the drug discontinued.

If the number of leukocytes falls below 3000/mcL and platelets below 100000/mcL, administration should be discontinued until the blood picture normalizes.

Effect on ability to drive vehicles and operate machinery

No effect.

Overdose

Acute intoxication has been observed in adults after a dose of about 20 mg and in children after a dose of 5 mg.

Chronic intoxication can be observed in patients suffering from gout after taking a total dose of 10 mg or higher over several days.

Since Colchicine has antimitotic activity, organs with a high proliferation rate are more often affected.

Symptoms approximately 2-6 hours after oral intake of a toxic dose, burning and soreness in the throat and mouth, urge to vomit and difficulty swallowing, nausea, thirst and vomiting are noted, and after that – urge to urinate and defecate, tenesmus and colic (usually in debilitated patients).

Mucous-watery and/or hemorrhagic diarrhea can lead to loss of fluid and electrolytes, which may result in the development of hypokalemia, hyponatremia, and metabolic acidosis. Patients often simultaneously complain of tightness and pain in the heart area. Subsequently, pallor, decreased body temperature, cyanosis, and dyspnea are observed.

Tachycardia and arterial hypotension (up to collapse) may develop.

Neurological disorders manifest in the form of decreased sensitivity, convulsions, and symptoms of paralysis. A fatal outcome is possible within the first three days due to cardiovascular failure and respiratory paralysis.

1-2 weeks after recovery from intoxication, complete, sometimes long-term alopecia may be observed. In some cases, impaired function of the kidneys, lungs, and liver has been noted. There are reports of rare cases of blindness.

Treatment can only be symptomatic, aimed at stabilizing the cardiovascular system. Plasma substitutes or isotonic sodium chloride solution with the addition of glucose and electrolytes (mainly potassium) are administered intravenously by drip, and ECG monitoring is performed.

Digoxin may be prescribed to maintain myocardial contractility. Antibiotic therapy if necessary.

With increased cerebrospinal fluid pressure, dexamethasone is indicated; lumbar puncture may be necessary. For abdominal cramps, atropine, papaverine, or tannalbine are prescribed. Opiates should not be used.

Oxygen therapy or artificial respiration may be necessary.

Drug Interactions

In combination with cyclosporine, especially in patients with impaired renal function, the likelihood of developing myopathy increases.

Enhances the effect of depressant and sympathomimetic agents.

Impairs the absorption of cyanocobalamin.

NSAIDs and other drugs causing myelodepression increase the risk of leukopenia and thrombocytopenia.

Antigout activity is reduced by cytostatics (increase uric acid concentration) and urine-acidifying drugs. Alkalinizing drugs enhance the effect.

Colchicum-Dispert^® can be used in combination with allopurinol and drugs with uricosuric action.

Storage Conditions

The drug should be stored out of the reach of children, in a dry, light-protected place at a temperature not exceeding 25°C (77°F).

Shelf Life

The shelf life is 5 years. The expiration date is indicated on the packaging. The drug must not be used after the expiration date.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.