Peringatan Keamanan

Has been shown to cause chromosomal aneuploidy and male infertility. Should be avoided during all stages of pregnancy, lactation and puberty. Is a potential risk factor for cancer.

In 2013, The European Medical Association (EMA) mandated that the use of thiocolchicoside-containing medicines by mouth or injection should be restricted across the European Union (EU). These drugs are now recommended only as an add-on treatment for painful muscle contractures resulting from spinal conditions in adults and adolescents 16 years old and older. Additionally, the dose of thiocolchicoside by mouth or injection should be limited. This is due to experimental evidence suggesting that thiocolchicoside was metabolized into M2 or SL59.0955, that has the propensity to damage dividing cells, resulting in aneuploidy (an abnormal number or arrangement of chromosomes). As a result, the CHMP (committee for medicinal products for human use) examined the safety profile of this medicine and consider what regulatory action might be appropriate L1656.

The CHMP reviewed the evidence, with consideration of opinions from experts in medicines safety, and concluded that aneuploidy may occur with M2 at levels not significantly greater than those measured after recommended doses of thiocolchicoside ingested orally. Aneuploidy is a strong risk factor for fetal harm, decreased fertility in men, and could theoretically increase the risk of developing cancer L1656.

The maximum recommended oral dose is 8 mg every 12 hours; treatment length should not exceed 7 consecutive days. When given intramuscularly (IM), the maximum dose is 4 mg every 12 hours, for a maximum of 5 days L1656.

In addition to the above toxicity, a study was done on the hepatotoxic potential of thiocolchicoside. It was observed that serum AST and ALT levels increased following of the administration oral thiocolchicoside at 8 mg/day. Two weeks after discontinuing thiocolchicoside therapy, liver enzymes had decreased to levels within the normal range. Although infrequent, thiocolchicoside should be considered a rare hepatotoxic agent in clinical practice A32121.

Thiocolchicoside

DB11582

small molecule experimental

Deskripsi

Thiocolchicoside is a semi-synthetic derivative of the colchicine, a natural anti-inflammatory glycoside which originates from the flower seeds of Superba gloriosa. It is a muscle relaxant with anti-inflammatory and analgesic effects. It has potent convulsant activity and should not be administered to individuals prone to seizures.L1663

Struktur Molekul 2D

Berat 563.62
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Approximately 7.7h [L1670].
Volume Distribusi The apparent volume of distribution of thiocolchicoside is estimated to be approximately 42.7 L after an intramuscular injection of 8 mg [L1658].
Klirens (Clearance) Primarily extrarenal elimination (75% of the total body clearance) [A32123].

Absorpsi

Oral bioavailability is ~25% After intramuscular administration, thiocolchicoside Cmax occur in 30 min and .reach values of 113 ng/mL after a 4 mg dose and 175 ng/mL after a 8 mg dose. The corresponding values of AUC are respectively 283 and 417 ng.h/mL. The pharmacologically active metabolite SL18.0740 is found at lower concentrations with a Cmax of 11.7 ng/mL occurring 5 h post administration and an AUC of 83 ng.h/mL L1658. After oral administration, no thiocolchicoside is detected in plasma. Only two metabolites are observed: The pharmacologically active metabolite SL18.0740 and an inactive metabolite SL59.0955. For both metabolites, maximum plasma concentrations occur 1hour after thiocolchicoside administration. After a single oral dose of 8 mg of thiocolchicoside the Cmax and AUC of SL18.0740 are about 60 ng/mL and 130 ng.h/mL respectively. For SL59.0955 these values are much lower: Cmax around 13 ng/mL and AUC ranging from 15.5 ng.h/mL (until 3h) to 39.7 ng.h/mL (until 24h) L1658.

Metabolisme

Thiocolchicoside is rapidly absorbed after oral administration and metabolized into 3 main metabolites L1661. Firstly, in the intestines to 3-demethylcolchicine (inactive metabolite). This product is further metabolized in circulation by either conjugation to 3-O-glucurono-demethylcolchicine (active metabolite) or demethylated to didemethylcolchicine (inactive metabolite)

Rute Eliminasi

Thiocolchicoside is not eliminated unchanged, rather as one of three metabolites found in either feces (~79 %) or in urine 20%. 3- demethylcolchicine (M2) and 3-O-glucurono-demethylcolchicine (M1) are found in both urine and feces, where as di-demethylcolchicine is found only in feces L1670.

Interaksi Obat

667 Data
Buprenorphine Thiocolchicoside may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Thiocolchicoside.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Thiocolchicoside.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Thiocolchicoside.
Hydrocodone Thiocolchicoside may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Thiocolchicoside.
Magnesium sulfate The therapeutic efficacy of Thiocolchicoside can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Thiocolchicoside may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Thiocolchicoside may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Thiocolchicoside.
Mirtazapine Thiocolchicoside may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Thiocolchicoside.
Orphenadrine Thiocolchicoside may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Thiocolchicoside may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Thiocolchicoside.
Pramipexole Thiocolchicoside may increase the sedative activities of Pramipexole.
Ropinirole Thiocolchicoside may increase the sedative activities of Ropinirole.
Rotigotine Thiocolchicoside may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Thiocolchicoside.
Sodium oxybate Thiocolchicoside may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Thiocolchicoside may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Thiocolchicoside.
Thalidomide Thiocolchicoside may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Thiocolchicoside may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Thiocolchicoside.
Ethanol Thiocolchicoside may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Thiocolchicoside may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Thiocolchicoside.
Fluvoxamine The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Alaproclate.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Thiocolchicoside.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Thiocolchicoside.
Imipramine The risk or severity of CNS depression can be increased when Imipramine is combined with Thiocolchicoside.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Thiocolchicoside.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Thiocolchicoside.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Thiocolchicoside.
Maprotiline The risk or severity of CNS depression can be increased when Maprotiline is combined with Thiocolchicoside.
Doxepin The risk or severity of CNS depression can be increased when Doxepin is combined with Thiocolchicoside.
Desipramine The risk or severity of CNS depression can be increased when Desipramine is combined with Thiocolchicoside.
Pizotifen The risk or severity of CNS depression can be increased when Pizotifen is combined with Thiocolchicoside.
Dosulepin The risk or severity of CNS depression can be increased when Dosulepin is combined with Thiocolchicoside.
Zopiclone The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with Zopiclone.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Thiocolchicoside.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Thiocolchicoside.
Tryptophan The risk or severity of CNS depression can be increased when Tryptophan is combined with Thiocolchicoside.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Thiocolchicoside.
Lorazepam The risk or severity of CNS depression can be increased when Lorazepam is combined with Thiocolchicoside.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Thiocolchicoside.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Thiocolchicoside.
Reserpine The risk or severity of CNS depression can be increased when Reserpine is combined with Thiocolchicoside.
Eletriptan The risk or severity of CNS depression can be increased when Eletriptan is combined with Thiocolchicoside.
Enflurane The risk or severity of CNS depression can be increased when Enflurane is combined with Thiocolchicoside.
Temazepam The risk or severity of CNS depression can be increased when Temazepam is combined with Thiocolchicoside.
Reboxetine The risk or severity of CNS depression can be increased when Reboxetine is combined with Thiocolchicoside.
Butabarbital The risk or severity of CNS depression can be increased when Butabarbital is combined with Thiocolchicoside.
Butalbital The risk or severity of CNS depression can be increased when Butalbital is combined with Thiocolchicoside.
Methysergide The risk or severity of CNS depression can be increased when Methysergide is combined with Thiocolchicoside.
Cabergoline The risk or severity of CNS depression can be increased when Cabergoline is combined with Thiocolchicoside.
Phenytoin The risk or severity of CNS depression can be increased when Phenytoin is combined with Thiocolchicoside.
Topiramate The risk or severity of CNS depression can be increased when Topiramate is combined with Thiocolchicoside.
Clemastine The risk or severity of CNS depression can be increased when Clemastine is combined with Thiocolchicoside.
Venlafaxine The risk or severity of CNS depression can be increased when Venlafaxine is combined with Thiocolchicoside.
Etomidate The risk or severity of CNS depression can be increased when Etomidate is combined with Thiocolchicoside.
Morphine The risk or severity of CNS depression can be increased when Morphine is combined with Thiocolchicoside.
Talbutal The risk or severity of CNS depression can be increased when Talbutal is combined with Thiocolchicoside.
Pentobarbital The risk or severity of CNS depression can be increased when Pentobarbital is combined with Thiocolchicoside.
Valproic acid The risk or severity of CNS depression can be increased when Valproic acid is combined with Thiocolchicoside.
Zolmitriptan The risk or severity of CNS depression can be increased when Zolmitriptan is combined with Thiocolchicoside.
Dihydroergotamine The risk or severity of CNS depression can be increased when Dihydroergotamine is combined with Thiocolchicoside.
Tolcapone The risk or severity of CNS depression can be increased when Tolcapone is combined with Thiocolchicoside.
Hydromorphone The risk or severity of CNS depression can be increased when Hydromorphone is combined with Thiocolchicoside.
Olanzapine The risk or severity of CNS depression can be increased when Olanzapine is combined with Thiocolchicoside.
Cetirizine The risk or severity of CNS depression can be increased when Cetirizine is combined with Thiocolchicoside.
Protriptyline The risk or severity of CNS depression can be increased when Protriptyline is combined with Thiocolchicoside.
Trimethadione The risk or severity of CNS depression can be increased when Trimethadione is combined with Thiocolchicoside.
Clobazam The risk or severity of sedation, somnolence, and CNS depression can be increased when Clobazam is combined with Thiocolchicoside.
Chlorzoxazone The risk or severity of CNS depression can be increased when Chlorzoxazone is combined with Thiocolchicoside.
Clozapine The risk or severity of CNS depression can be increased when Clozapine is combined with Thiocolchicoside.
Meprobamate The risk or severity of CNS depression can be increased when Meprobamate is combined with Thiocolchicoside.
Thiethylperazine The risk or severity of CNS depression can be increased when Thiethylperazine is combined with Thiocolchicoside.
Palonosetron The risk or severity of CNS depression can be increased when Palonosetron is combined with Thiocolchicoside.
Sulpiride The risk or severity of CNS depression can be increased when Sulpiride is combined with Thiocolchicoside.
Alprazolam The risk or severity of CNS depression can be increased when Alprazolam is combined with Thiocolchicoside.
Dexbrompheniramine The risk or severity of CNS depression can be increased when Dexbrompheniramine is combined with Thiocolchicoside.
Loxapine The risk or severity of CNS depression can be increased when Loxapine is combined with Thiocolchicoside.

Target Protein

Gamma-aminobutyric acid receptor subunit alpha-1 GABRA1
Gamma-aminobutyric acid receptor subunit beta-2 GABRB2
Glycine receptor subunit alpha-2 GLRA2
Glycine receptor subunit alpha-3 GLRA3
Glycine receptor subunit beta GLRB
Gamma-aminobutyric acid receptor subunit gamma-2 GABRG2
GABA(A) Receptor GABRA1
Glycine receptor subunit alpha-1 GLRA1
Tumor necrosis factor ligand superfamily member 11 TNFSF11

Referensi & Sumber

Artikel (PubMed)
  • PMID: 8983937
    Perucca E, Poitou P, Pifferi G: Comparative pharmacokinetics and bioavailability of two oral formulations of thiocolchicoside, a GABA-mimetic muscle relaxant drug, in normal volunteers. Eur J Drug Metab Pharmacokinet. 1995 Oct-Dec;20(4):301-5.
  • PMID: 8161719
    Sandouk P, Bouvier d'Yvoire M, Chretien P, Tillement JP, Scherrmann JM: Single-dose bioavailability of oral and intramuscular thiocolchicoside in healthy volunteers. Biopharm Drug Dispos. 1994 Jan;15(1):87-92.
  • PMID: 14563464
    Tuzun F, Unalan H, Oner N, Ozguzel H, Kirazli Y, Icagasioglu A, Kuran B, Tuzun S, Basar G: Multicenter, randomized, double-blinded, placebo-controlled trial of thiocolchicoside in acute low back pain. Joint Bone Spine. 2003 Sep;70(5):356-61.
  • PMID: 19780000
    Ketenci A, Basat H, Esmaeilzadeh S: The efficacy of topical thiocolchicoside (Muscoril) in the treatment of acute cervical myofascial pain syndrome: a single-blind, randomized, prospective, phase IV clinical study. Agri. 2009 Jul;21(3):95-103.
  • PMID: 11554898
    De Riu PL, Rosati G, Sotgiu S, Sechi G: Epileptic seizures after treatment with thiocolchicoside. Epilepsia. 2001 Aug;42(8):1084-6.
  • PMID: 21955206
    Reuter S, Gupta SC, Phromnoi K, Aggarwal BB: Thiocolchicoside suppresses osteoclastogenesis induced by RANKL and cancer cells through inhibition of inflammatory pathways: a new use for an old drug. Br J Pharmacol. 2012 Apr;165(7):2127-39. doi: 10.1111/j.1476-5381.2011.01702.x.
  • PMID: 7981928
    Sabouraud A, Chappey O, Dupin T, Scherrmann JM: Binding of colchicine and thiocolchicoside to human serum proteins and blood cells. Int J Clin Pharmacol Ther. 1994 Aug;32(8):429-32.
  • PMID: 27042729
    Authors unspecified: Thiocolchicoside: review of adverse effects. Prescrire Int. 2016 Feb;25(168):41-3.
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Contoh Produk & Brand

Produk: 0 • International brands: 12
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  • Myoril
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