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Composition:


active ingredient: colchicine;


1 coated tablet contains: 0.52–2.42 mg of Colchicum autumnale seed extract (autumn evergreen) (50-150: 1), methylene chloride extractant, which corresponds to 0.5 mg of the amount of alkaloids in terms of colchicine;


excipients: lactose, monohydrate; microcrystalline cellulose; magnesium stearate; talc; copovidone; stearic acid 50; corn starch;


shell: talc, povidone K 29, titanium dioxide (e 171), polyethylene Glycols 6000, light magnesium oxide, Acacia, sucrose, shellac, sodium croscarmellose, Opalux AS 250000 (sucrose, ponceau 4R (E 124), Quinoline yellow (E 104), titanium dioxide (E 171), povidone), carnauba wax.


Dosage form.


Coated tablets.


Basic physical and chemical properties: dark red, round, coated tablet.


Pharmacotherapeutic group.


Medications used to treat gout that do not affect uric acid metabolism.


ATX code M04A C01.


Pharmacological properties.


Pharmacodynamics.


Colchicine binds to microtubules at the stage of interphase cell division, which inhibits microtubule polymerization and thereby prevents the formation of cytoskeletal structure, reduces motility and degranulates intracellular lysosomes. Consequently, colchicine simultaneously acts as a toxin and reduces the release of lysosomes, chemoattractants, and lactic acid.


By acting on white blood cells, colchicine inhibits phagocytosis of uric acid crystals. It disrupts the cell membrane of white blood cells and reduces their mobilization, migration and adhesive ability. Colchicine reduces the invasion of new granulocytes and prevents cell division and migration.


Colchicine does not affect the concentration of uric acid in the blood and tissues.


Pharmacokinetics.


Suction


Colchicine is rapidly and effectively absorbed in the gastrointestinal tract. Approximately 60 minutes after taking 2 coated tablets (containing a total of 2×0.5 mg of alkaloids, 2×0.38 mg of colchicine), a peak level of colchicine of 4.2 ng/mL in blood plasma was recorded.


Distribution


The oral bioavailability of colchicine is 25-50 %. In blood plasma, colchicine binds weakly or moderately to proteins (30-50 %) and after reabsorption is rapidly removed from the blood plasma and distributed in various tissues.


Colchicine is rapidly distributed in peripheral blood leukocytes, and its concentration in these cells can exceed the concentration in blood plasma after 72 hours (after 15 minutes, the concentration is five times higher than the concentration in blood plasma). Colchicine has been found to have a beneficial effect in the treatment of acute gout by affecting polymorphonuclear leukocytes. Colchicine mainly accumulates in white blood cells, which justifies the beneficial effect of colchicine in gouty arthritis due to inhibition of granulocyte migration to the site of inflammation.


Metabolism and elimination


Colchicine is partially acetylated in the liver and slowly metabolized in other tissues.


Excretion of the drug and its metabolites mainly occurs in the feces, only 10-20% is excreted in the urine. The percentage of urinary excretion may be higher in patients with impaired liver function. Due to the high concentration of colchicine in the tissues, only 10% of a single dose is eliminated within 24 hours. Withdrawal of colchicine may continue for >10 days after treatment.


After oral administration of colchicine at a dose of 1 mg, the average elimination half-life was 4.4 hours in patients with normal renal function and 18.8 hours in patients with renal dysfunction.


Clinical characteristics.


Indications.


Adults


* treatment of acute gout attacks;


* prevention of gout attacks;


* treatment of pericarditis and Prevention of recurrent pericarditis;


* Behcet's disease.


Adults, children and teenagers


* for familial Mediterranean Fever to prevent seizures and prevent amyloidosis.


Contraindications.


Hypersensitivity to colchicine or to the components of the drug.


Patients with impaired renal or hepatic function should avoid using colchicine together with P-glycoprotein inhibitors or strong CYP3A4 inhibitors due to the increased risk of side effects of colchicine. Life-threatening and fatal toxicity of colchicine has been reported in these patients when used at therapeutic doses.


The drug is contraindicated in patients on dialysis.


Interactions with other drugs and other types of interactions.


Colchicine may impair the absorption of vitamin B12.


Colchicine is a substrate of CYP3A4 and the transport protein P-glycoprotein.


In the presence of CYP3A4 or P-glycoprotein inhibitors, the concentration of colchicine in the blood may increase.


Concomitant use of colchicine with cyclosporine, HMG-CoA reductase inhibitors (statins), fibrates, ketoconazole, some anti-HIV drugs, macrolide antibiotics, cimetidine, verapamil, diltiazem, ranolazine, digoxin, a significant amount of grapefruit juice (1000 ml/day) and other CYP3A4 or P-glycoprotein inhibitors, especially in patients with renal insufficiency, may cause disorders with bone marrow side effects, agranulocytosis, neuromyopathy, myopathy or rhabdomyolysis and other side effects, as well as high, potentially life-threatening serum colchicine levels.


Life-threatening and fatal drug interactions have been reported in patients treated with colchicine in combination with strong P-glycoprotein and CYP3A4 inhibitors.


If treatment with a P-glycoprotein inhibitor or a strong CYP3A4 inhibitor is necessary, patients with normal renal or hepatic function may need to adjust the dose of colchicine. Concomitant use of such inhibitors and colchicine should be avoided in patients with renal or hepatic insufficiency (see Section "contraindications").


Concomitant use of Atorvastatin, simvastatin, pravastatin, fluvastatin, gemfibrozil or fibrates (associated with myotoxicity) and cyclosporine with colchicine may lead to myopathy. Symptoms usually disappear after discontinuation of use for a period of 1 week to several months.


Concomitant use of colchicine and erythromycin/clarithromycin is contraindicated.


Elevated plasma colchicine levels have been reported with a single dose of ketoconazole, ritonavir, verapamil, and diltiazem.


Application features.


Colchicine is potentially toxic, so it is important not to exceed the dose prescribed by a specialist with the necessary knowledge and experience.


Patients with impaired renal function and cardiovascular diseases.


Patients with impaired renal function may experience bone marrow disease, agranulocytosis, neuromyopathy, myopathy, and rhabdomyolysis.


Significant caution is required in patients with more severe circulatory and renal disorders (dehydration, changes in blood pressure, impaired renal function).


Patients with gastrointestinal disorders.


In patients with gastrointestinal disorders, symptoms may increase, which is associated with the antimitotic effect of colchicine, which leads to diarrhea, nausea, vomiting and abdominal pain.


Treatment of acute attacks of gout in patients with impaired renal function.


For the treatment of gout attacks, patients with mild renal impairment (creatinine clearance 50-80 mL/min) or moderate (creatinine clearance 30-50 mL/min) should use the drug with caution. Patients with moderate renal impairment should reduce the dose or increase the interval between doses. Treatment of such patients should be carried out under close supervision to avoid side effects.


Patients with severe renal impairment (creatinine clearance less than 30 mL/min) should first take 1 tablet (0.5 mg) per day. The dosage should be increased under close control to avoid side effects. Although the dose does not need to be adjusted for the treatment of gout attacks, patients with severe renal impairment should be repeated no more than once every 2 weeks. Patients with gout attacks who require repeated courses of treatment should consider using alternative therapy.


Colchicine treatment is contraindicated in patients on dialysis (see the section "contraindications").


Treatment of acute attacks of gout in patients with impaired liver function.


For the treatment of gout attacks in patients with mild to moderate hepatic impairment, no adjustment of the recommended dose is required, but careful monitoring of the occurrence of side effects is necessary. Patients with severe hepatic impairment should consider reducing the dose.


Treatment of elderly patients.


Colchicum-Dyspert should be used with caution in elderly patients.


For elderly patients, the dosage should be selected with caution, taking into account the increased frequency of decreased renal or hepatic function or other concomitant drug therapy.


The drug contains excipients in the composition of Opalux as 250000, which can cause the development of allergic reactions, including asthma, in patients sensitive to these substances.


Patients with rare hereditary diseases such as galactose intolerance, Lappa lactase deficiency, or impaired glucose-galactose malabsorption should not take this medication.


Allergic reactions are more common in patients with hypersensitivity to acetylsalicylic acid.


The drug should be kept out of the reach of others before and after use.


Use during pregnancy or lactation.

Pregnancy


The effect of the drug has not been studied in the treatment of gout attacks in pregnant women, but published data from a number of studies have not shown evidence of an increased risk of miscarriage, stillbirth, or teratogenic effects in pregnant women who used colchicine to treat familial Mediterranean fever. Published data from animal studies on the effect on reproductive function and development indicate that colchicine exhibits embryophetal toxicity, teratogenicity and changes postnatal development at exposures achieved after the use of the drug in the specified therapeutic or higher doses.


Colchicine can be used during pregnancy only if there is an urgent need and it is impossible to replace it with other, safer drugs.


Breast-feeding


Colchicine is excreted in breast milk.


Physico-chemical and available pharmacodynamic/toxicological data on colchicine indicate the release of colchicine from breast milk and a threat to the child, so the risk to the infant is not excluded.


Colchicum-Dyspert should not be used during breast-feeding.


Fertility


Published data from non-clinical studies have shown that colchicine-induced disruption of microtubule formation affects meiosis and mitosis.


The use of colchicine causes morphological abnormalities of spermatozoa and a decrease in the number of spermatozoa in men, as well as a violation of the process of sperm penetration, second meiotic division and egg cell division in women taking colchicine.


Although infertility in men due to colchicine administration is rare, cases of azoospermia have been reported after discontinuation of the drug.


Clinical Case Reports and epidemiological studies in women on colchicine treatment have not established a clear link between colchicine use and female infertility.


Ability to influence the reaction rate when driving vehicles or other mechanisms.


Studies of the effect on the ability to drive vehicles and work with other mechanisms have not been conducted.


Dosage and administration.


Tablets should be swallowed whole, washed down with a sufficient amount of liquid, regardless of food intake.


Treatment of acute gout attacks should be started as soon as possible (within the first 12 hours after the onset of a gout attack). The expected effect will occur within 12 hours.


First, you should take 2 tablets (1 mg of the drug), then after 1 hour 1 tablet (0.5 mg of the drug). After that, the tablets should not be taken for 12 hours.


If necessary, you can repeat the procedure after 12 hours. The maximum daily dose is 1 tablet (0.5 mg of the drug) every 8 hours until symptoms subside.


The course of treatment should be completed after relieving symptoms or taking 12 tablets (6 mg). During the course of treatment, you should take no more than 12 tablets (6 mg).


A second course of treatment is carried out no earlier than 3 days (72 hours) after the end of the previous course.


Prevention of gout attacks: adults should take 1-2 tablets (0.5–1 mg of the drug) per day for no more than 6 months. Individual duration of treatment should be determined after evaluating factors such as the frequency of exacerbations, the duration of the disease, and the presence and size of tophi.


Treatment of familial Mediterranean fever.


It can be taken as a single dose or divided into several doses exceeding 1 mg per day and taken twice a day.


The dosage of colchicine should be gradually increased to a maximum of 3 mg per day to monitor the course of the disease in the absence of a response to treatment at the standard dosage. Increase the daily dose should be carefully monitored to avoid side effects. Careful monitoring is necessary in the presence of impaired renal or hepatic function. For such patients, the initial dose should be reduced by 50 %.


Adults should take 2-6 tablets (1-3 mg of the drug) per day. Most patients require 1-1.5 mg per day, but some patients may need a dosage of 2.0 mg or more.


For children, colchicine can only be taken as prescribed by a doctor under the supervision of a healthcare professional.


The recommended dose of colchicine for children is:


- 1 tablet (0.5 mg of the drug) per day for children under 5 years of age;


- 1-2 tablets (0.5–1 mg of the drug) per day for children aged 5 to 10 years;


- 2-3 tablets (1-1.5 mg of the drug) per day for children over 10 years of age.


Children with amyloid nephropathy may need large daily doses: from 3 to 4 tablets (1.5–2 mg of the drug) per day.


Treatment of acute pericarditis and recurrent pericarditis.


The recommended daily dose of colchicine for acute and recurrent pericarditis is 1-2 tablets (0.5 mg -1 mg) per day


In most clinical trials, the dose of colchicine used is 2 tablets (1 mg).


Behcet's Disease.


The recommended dose of colchicine is 2-4 tablets (1-2 mg of the drug) per day.


Impaired renal function


Use with caution in patients with mild renal impairment. For patients with moderate renal impairment, it is necessary to reduce the dose or increase the interval between doses. Such patients should be carefully monitored for the occurrence of side effects of colchicine. For information on the treatment of patients with severe renal impairment, see the section "contraindications".


Impaired liver function


Use with caution in patients with mild/moderate hepatic impairment. Such patients should be carefully monitored for the occurrence of side effects of colchicine. For patients with severe liver disorders, see the section "contraindications".


Special patient groups


Concomitant use of colchicine with certain drugs, mainly cytochrome P450 3A4 (CYP3A4)/P-glycoprotein inhibitors, increases the risk of colchicine toxicity. If the patient has received concomitant therapy with a moderate or potent CYP3A4 inhibitor or a P-glycoprotein inhibitor, the maximum recommended dose of colchicine for oral administration should be reduced and side effects should be carefully monitored.


Children.


The drug is not recommended for use in children under 4 years of age due to insufficient data on use.


Overdose.


Overdose and neglect of drug interaction recommendations can lead to poisoning, which is accompanied by severe pain, and can also lead to death.


Colchicine has a narrow therapeutic range and is extremely toxic in overdose. Patients with impaired renal or hepatic function, gastrointestinal or heart disease, and elderly patients are particularly at risk of toxicity. Patients with colchicine overdose, even in the absence of early symptoms, should immediately undergo medical supervision.


Acute intoxication can occur after oral administration of approximately 20 mg (40 tablets) of colchicine in adults and 5 mg (10 tablets) in children. Chronic intoxication may occur after repeated doses of the drug in patients with gout after ingestion of a dose of 10 mg or more for several days.


Because colchicine inhibits mitosis, more organs are affected with a higher rate of proliferation.


Symptoms


The exact dose of colchicine, which has significant toxicity, is unknown. Deaths were reported after taking colchicine at a dose of 7 mg for 4 days, while other patients survived after taking more than 60 mg. A review of 150 patients after colchicine overdose found that those who took less than 0.5 mg/kg survived and tended to have milder toxicity, manifested by gastrointestinal disorders, while those who took 0.5 mg to 0.8 mg/kg had more severe reactions, such as myelosuppression. There was a 100% mortality rate in those who took more than 0.8 mg/kg.


The first stage of acute colchicine poisoning begins within 24 hours of ingestion and includes gastrointestinal disorders such as dehydration, abdominal pain, hemorrhagic gastroenteritis, hypovolemia, diarrhea, nausea and vomiting, accompanied by electrolyte imbalance, leukocytosis and low blood pressure in severe cases.


The second stage with life-threatening complications in the period from 24 to 72 hours after administration may be accompanied by symptoms such as multi-organ failure, acute renal failure, confusion, coma, peripheral motor and sensory neuropathy, myocardial depression, pancytopenia, arrhythmia, respiratory failure, coagulopathy.


Death can occur as a result of respiratory and cardiovascular failure.


If the patient survives, recovery of damaged organs may be accompanied by a return of leukocytosis and alopecia, which begins approximately 1 week after the initial overdose.


Tags: Colchicine