Colchicina – Wikipedia

The colchicine It is an alkaloid originally extracted from such plants Colchicum (in particular the Colchicum autumnale ) and also present in such plants Glorious , Androcymbium It is Merthenera ^[2] . Its chemical structure, empictized empirically in 1945 by Dewar ^[3] , consisting of 2 epthacy groups, one of which is defined by Dewar Tropolone, combined with a Trimetossibenzene, was definitively identified only in 1955 by H. Corrodi, E. Hardegger. ^{[4] [5] [6]} It is presented in the form of yellowish and odorless, crystalline or amorphous dust and is very soluble in chloroform, ethanol and water.

It is currently used as a drug for the treatment of gout, but it seems to be useful in various syndromes with phlogistic phenomena.
It is also the first choice drug to alleviate the symptoms of “family Mediterranean fever” (FMF), an auto -inflammatory disease belonging to the “periodic fever” category (FP).

Relatively recent (2007) is its use by cardiologists in the treatment of pericardies and in the prevention of recurrence of this inflammatory process of the pericardium (e.g. Dressler syndrome).

Colchicin is linked to the fundamental subunit of micro -tubes, tubulin, causing depolimerization. This determines an antimitotic effect on the cell that is blocked at the metaphase stage for the lack of genesis of the mythotic spindle.

Although the high toxicity of colchicin prevents use as an anticancer compound, this action allows you to inhibit cellular motility by preventing leukocytes from reaching the area of ​​interest and blocking their engulfing activity. In addition to this action, Colchicin is also able to inhibit the production of the Leukatriene B4.

Colchicin is administered by mouth and is quickly absorbed by the gastrointestinal system reaching the maximum plasma concentration in a time range between 30 minutes and 2 hours.

Colchicin is mainly released into the bile and is eliminated in an unchanged form through the stool. A small part, however, is transformed into oxolchycin which accumulates at a renal level and is eliminated very slowly.

Colchicina’s half -life time is around 65 minutes.

Colchicin is substantially used for the treatment of gout. It is able, in fact, to eliminate the pain and inflammation that you have during an attack of Gottosa arthritis in a time between 12 and 24 hours. Although colchicin is more specific for the gottoso attack of non -steroidal anti -inflammatory drugs (NSAIDs), the latter are more used as they are free from some annoying side effects (in particular diarrhea).

In rare cases it is also used in other forms of arthritis.

In some cases, it also represents support therapy for other periodic fevers such as periodic syndromes associated with the cryopirine and periodic syndrome associated with the tumor necrosis factor receptor. ^{[7] [8]} The response to colchicin is used to perfect the diagnosis of different periodic fevers. ^[9]

Colchicin is commonly used, as off-label drug, to relieve mucocutaneous symptoms in the Behçet syndrome . ^[ten]

The use of uricosuric drugs can, at the beginning, trigger an acute gottoso attack for which, during the first month of therapy, a prophylaxis with colchicin or fans is performed.

Colchicin is also suitable for the prophylaxis of family Mediterranean fever.

Recently, following a systematic revision of the scientific literature, the use of colchicine for pericarditis therapy, in association with fans or steroids or monotherapy, and for the prevention of recurrence, is reported. This strategy seems very promising, allowing success of up to 90% of cases, even if the data derive from very heterogeneous studies and observations.

The National Association of Hospital Cardiologists (Anmco) has launched a phase IV study, multicenter, randomized, in double blind against placebo that will evaluate the effectiveness of the drug in the treatment of pericarditis in the first episode; the effectiveness in the prevention of recurrence; the effectiveness in the treatment of recurrence; The effectiveness in the prevention and treatment of post-pericardiotomic syndrome. A series of secondary end-cans will also be evaluated with these primary end-cans including the effectiveness in association with ASA, the reduction of the frequency of complications and a cost-effective analysis for the purposes of correct health policy.

In March 2020, a clinical experimentation on 6000 people affected by infection of the Sars-Cov-2 virus began, financed by the Quebec government, to test the potential effectiveness of use for 30 days of Colchicin in reducing the symptoms of the crownavirus. ^[11]

The most common adverse effects that occur with colchicin are the appearance of nausea, diarrhea, vomiting and abdominal pain.

In the event of prolonged administration, bonos, neuriti, alopecia and myopathy can be determined.

The use of colchicin can interfere with the function of the ileal mucosa determining reversible malabsorption of vitamin B12.

The use of high doses of colchicin can produce an overdose syndrome that may have a mortality of 30%. The syndrome is mainly presented with problems borne by the gastrointestinal system (nausea, vomiting, diarrhea and abdominal pain) with consequent water-shaft problems, alterations of the spine and polypnea functionality. Generally death comes in second or third day for cardiovascular collapse or septic shock. In the absence of an antidote, an urgent hospitalization is used in intensive care for carrying out a gastric lavender and duodenal aspiration, correction of the water and electrolytic status, antibiotic therapy and any symptomatic treatment.

In humans the toxic dose of colchicin is around 10 mg. In case of renal failure, it is recommended to reduce the dosage of the drug.

It is also recommended not to use colchicin under pregnancy or during breastfeeding.

There is contraindication to use even in the case of serious heart, kidney or gastrointestinal or hypersensitivity problems.

In the event of a cyclosporine therapy, colchicin can increase its plasma concentration and determine an increased risk of muscle and renal toxicity.

The interaction between colchicin and verapamil (football-antagonist) is particularly severe.

B.G. Cot : General and clinical pharmacology. Fourth Italian edition; Piccin, Padua.
Mycek MJ, Harvey Ra E Champe PC : Pharmacology. Second Italian edition; Zanichelli Editore, Bologna
Bruni A., Nicholetti M. : Reasoned dictionary of herbal medicine and phytotherapy; Piccin, Padua 2003