Thiocolchicoside

Thiocolchicoside
ATC Code M03BX05
Formula C27H33NO10S
Molar Mass (g·mol−1) 563.6
Physical State solid
Melting Point (°C) 190-198
Boiling Point (°C) 929.624
PKS Value 12.74
CAS Number 602-41-5
PUB Number 9915886
Drugbank ID DB11582
Solubility 10 mg/ml in water

Grundlagen

Thiocolchicoside is a muscle relaxant with anti-inflammatory and analgesic effects. Thiocolchicoside is a semisynthetic derivative of colchicine, a natural anti-inflammatory substance extracted from the flower seeds of the autumn crocus (Colchicum autumnale). The substance is used to treat orthopedic, traumatic, and rheumatologic conditions. It is also used as an adjuvant in the treatment of painful muscle contractions and acute spinal disorders in adults and adolescents 16 years of age and older.

Due to its pronounced and sometimes serious side effects, the EMA (European medicines agency) recommends thiocolchicoside only as an adjuvant in acute muscle spasms and advises against longer-term treatment.

Pharmakologie

Pharmacodynamics

Thiocolchicoside is a synthetic sulfur derivative of colchicine. It selectively binds to so-called GABAA receptors and therefore mimics the action of the naturally occurring neurotransmitter gamma-aminobutyric acid (GABA) in the body. GABA-ergic neurons are involved in processes such as muscle relaxation, anxiety relief, sedation and anesthesia. GABA may also regulate heart rate and blood pressure.

Pharmacokinetics

Thiocolchicoside is rapidly absorbed after oral administration. Oral bioavailability is approximately 25%. It is metabolized in the liver and excreted in the form of its three major metabolites either in feces (~79%) or urine (20%). The plasma half-life is approximately 7 hours.

Toxizität

Side effects

Side effects of thiocolchicoside may include nausea, allergic reactions, and vasovagal syncope. Liver damage, pancreatitis, seizures, hematopoietic disorders, severe skin disorders, rhabdomyolysis, and reproductive disorders have been reported in rare cases.

Contraindications

It has a strong convulsion-inducing effect and should not be administered to individuals prone to seizures. This includes, for example, people suffering from epilepsy.

Thiocolchicoside is teratogenic in experimental animals and also damages chromosomes. There are insufficient data in humans to clearly indicate a teratogenic effect. However, use in pregnancy is not recommended due to lack of safety.

Editorial principles

All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

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