Тиозид 4 , Таблетки

Форма выпуска и состав

Лекарственный препарат Muscoflex поступает в продажу в форме капсул и раствора для инъекций в ампулах.

Капсулы покрыты пищевым желатином и расфасованы в блистеры по 10 шт. в каждом. В фирменной картонной коробке упакованы 2 блистера, 20 капсул. Каждая единица содержит 4 мг активного вещества (тиоколхикозида).

В состав медикамента входят вспомогательные вещества:

  • лактозы моногидрат;
  • кукурузный крахмал;
  • магния стеарат.

Срок годности капсул составляет 3 года с даты изготовления, которая выдавлена на блистерах. Цена упаковки лекарства варьируется в пределах 76–110 рублей в зависимости от статуса аптеки и региона. Российские аналоги (Артоксан, Артикард, Окситен) имеют практически одинаковую стоимость с турецким препаратом, но таблетки могут быть выписаны бесплатно в рамках одной из действующих программ.

Раствор для инъекций заключен в прозрачные стеклянные ампулы емкостью 2 мл.

В каждой ампуле содержатся такие компоненты:

  • тиоколхикозид;
  • хлорид натрия;
  • вода для инъекций.

Ампулы расфасованы в картонные контейнеры по 6 шт. Раствор представляет собой прозрачную маслянистую жидкость с желтоватым оттенком. Контейнеры и инструкция по применению упакованы в фирменную картонную коробку, на которую нанесено название, штрихкод, реквизиты производителя и основные предостережения. Срок годности раствора – 2 года. Цена упаковки варьируется в пределах 72–96 рублей.

Хранить медикамент нужно в темном, защищенном от света и недоступном для детей месте при температуре +12–25°C.

Side effects

Side effects of thiocolchicoside can include nausea, allergy and vasovagal reactions.
Liver injury, pancreatitis, seizures, blood cell disorders, severe cutaneous disorders, rhabdomyolysis, and reproductive disorders have all been recorded in the French and European pharmacovigilance databases and in the periodic updates that the companies concerned submit to regulatory agencies. These data do not specify the frequency of the disorders nor do they identify the most susceptible patient populations. Thiocolchicoside is teratogenic in experimental animals and also damages chromosomes. Human data are limited to a follow-up of about 30 pregnant women (no major malformations) and reports of altered spermatogenesis, including cases of azoospermia. In practice, there is no justification for exposing patients to the adverse effects of thiocolchicoside. It is better to use an effective, well-known analgesic for patients complaining of muscle pain, starting with paracetamol.

Although muscle relaxants may have the major side effect of sedation, thiocolchicoside is free from sedation effects possible due to non-interference with nicotinic receptors.

Properties

State
Solid
Experimental Properties
Property Value Source
melting point (°C) 190-198 http://henankerui.lookchem.com/products/CasNo-602-41-5-Thiocolchicoside-12752892.html
boiling point (°C) 929.624 http://henankerui.lookchem.com/products/CasNo-602-41-5-Thiocolchicoside-12752892.html
water solubility 10 mg/mL https://www.sigmaaldrich.com/catalog/product/sigma/sml1476?lang=en&region=CA
logP 0.34 http://www2.unipr.it/~santipat/Posters/2003/tio2003.pdf
pKa 12.74 https://www.ebi.ac.uk/chembldb/compound/inspect/CHEMBL1705373
Predicted Properties
Property Value Source
Water Solubility 0.348 mg/mL ALOGPS
logP 0.78 ALOGPS
logP -0.16
logS -3.2 ALOGPS
pKa (Strongest Acidic) 12.2
pKa (Strongest Basic) -1.2
Physiological Charge
Hydrogen Acceptor Count 10
Hydrogen Donor Count 5
Polar Surface Area 164.01 Å2
Rotatable Bond Count 7
Refractivity 145.06 m3·mol-1
Polarizability 57.72 Å3
Number of Rings 4
Bioavailability 1
Rule of Five No
Ghose Filter No
Veber’s Rule No
MDDR-like Rule Yes
Predicted ADMET features
Not Available

Identification

Name
Thiocolchicoside
Accession Number
DB11582
Type
Small Molecule
Groups
Experimental
Description

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 .

Structure
Synonyms
  • TCC
  • Thiocolchicine 2-glucoside analog
External IDs
210-017-7
International/Other Brands
Biocolchid (Biogalenic)ColtramylColtraxEusilen (Velka)MiorelMusco-RilMuscorilMyolax (Adwya)MyorilNeoflaxNeuroflaxTDP (Aamorb)
Categories
  • Alkaloids
  • Central Nervous System Depressants
  • Muscle Relaxants
  • Muscle Relaxants, Centrally Acting Agents
  • Musculo-Skeletal System
UNII
T1X8S697GT
CAS number
602-41-5
Weight
Average: 563.62 Monoisotopic: 563.182517441
Chemical Formula
C27H33NO10S
InChI Key
LEQAKWQJCITZNK-AXHKHJLKSA-N
InChI
InChI=1S/C27H33NO10S/c1-12(30)28-16-7-5-13-9-18(37-27-24(34)23(33)22(32)19(11-29)38-27)25(35-2)26(36-3)21(13)14-6-8-20(39-4)17(31)10-15(14)16/h6,8-10,16,19,22-24,27,29,32-34H,5,7,11H2,1-4H3,(H,28,30)/t16-,19+,22+,23-,24+,27+/m0/s1
IUPAC Name
N-oxy}tricyclohexadeca-1(16),2,4,6,11,14-hexaen-10-yl]acetamide
SMILES
COC1=C(O2O(CO)(O)(O)2O)C=C2CC(NC(C)=O)C3=CC(=O)C(SC)=CC=C3C2=C1OC

Spectra

Mass Spec (NIST)
Not Available
Spectra
Spectrum Spectrum Type Splash Key
Predicted MS/MS Spectrum — 10V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum — 20V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum — 40V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum — 10V, Negative (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum — 20V, Negative (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum — 40V, Negative (Annotated) Predicted LC-MS/MS Not Available

References

General References
  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. De Riu PL, Rosati G, Sotgiu S, Sechi G: Epileptic seizures after treatment with thiocolchicoside. Epilepsia. 2001 Aug;42(8):1084-6.
  6. 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.
  7. 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.
  8. Authors unspecified: Thiocolchicoside: review of adverse effects. Prescrire Int. 2016 Feb;25(168):41-3.
  9. Carta M, Murru L, Botta P, Talani G, Sechi G, De Riu P, Sanna E, Biggio G: The muscle relaxant thiocolchicoside is an antagonist of GABAA receptor function in the central nervous system. Neuropharmacology. 2006 Sep;51(4):805-15. Epub 2006 Jun 30.
  10. Efe C, Purnak T, Ozaslan E, Milanlioglu A: Thiocolchicoside-induced liver injury. Clinics (Sao Paulo). 2011;66(3):521-2.
  11. Mascia MP, Bachis E, Obili N, Maciocco E, Cocco GA, Sechi GP, Biggio G: Thiocolchicoside inhibits the activity of various subtypes of recombinant GABA(A) receptors expressed in Xenopus laevis oocytes. Eur J Pharmacol. 2007 Mar 8;558(1-3):37-42. Epub 2006 Dec 12.
  12. Lopez-Corcuera B, Geerlings A, Aragon C: Glycine neurotransmitter transporters: an update. Mol Membr Biol. 2001 Jan-Mar;18(1):13-20.
  13. Sandouk P, Chappey O, d’Yvoire MB, Scherrmann JM: Pharmacokinetics of thiocolchicoside in humans using a specific radioimmunoassay. Ther Drug Monit. 1995 Oct;17(5):544-8.
  14. European Medicines Agency recommends restricting use of thiocolchicoside by mouth or injection
  15. Thiocolchicine EMA label
  16. Thiocolchicine Pubchem
  17. Thiocolchicine
  18. THIOCOLCHICOSIDE AS MUSCLE RELAXANT: A REVIEW
  19. To compare the efficacy and safety of fixed dose combination of thiocolchicoside and aceclofenac versus chlorzoxazone, aceclofenac and paracetamol in patients with acute lower backache associated with muscle spasm
  20. The effect of topical thiocolchicoside in preventing and reducing the increase of muscle tone, stiffness, and soreness: A real-life study on top-level road cyclists during stage competition
  21. Neurotransmitters as food supplements: the effects of GABA on brain and behavior
  22. GABA AND GLYCINE receptor modulators
  23. hiocolchicoside, 99% (HPLC)
  24. Review of the toxicology, pharmacodynamics and pharmacokinetics of thiocolchicoside, a GABA-agonist muscle relaxant with anti-inflammatory and analgesic actions
External Links
KEGG Drug
D07276
PubChem Compound
PubChem Substance
ChemSpider
BindingDB
ChEBI
ChEMBL
CHEMBL213907
Drugs.com
Drugs.com Drug Page
Wikipedia
Thiocolchicoside
ATC Codes
M03BX05 — Thiocolchicoside

  • M03BX — Other centrally acting agents
  • M03B — MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS
  • M03 — MUSCLE RELAXANTS
  • M — MUSCULO-SKELETAL SYSTEM

M03BX55 — Thiocolchicoside, combinations

  • M03BX — Other centrally acting agents
  • M03B — MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS
  • M03 — MUSCLE RELAXANTS
  • M — MUSCULO-SKELETAL SYSTEM
MSDS
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Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Drug Interaction
Unlock Additional Data
2,5-Dimethoxy-4-ethylthioamphetamine The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Thiocolchicoside.
4-Methoxyamphetamine The risk or severity of adverse effects can be increased when 4-Methoxyamphetamine is combined with Thiocolchicoside.
5-methoxy-N,N-dimethyltryptamine The risk or severity of adverse effects can be increased when Thiocolchicoside is combined with 5-methoxy-N,N-dimethyltryptamine.
7-Nitroindazole The risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Thiocolchicoside.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline The risk or severity of adverse effects can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Thiocolchicoside.
Acepromazine The risk or severity of adverse effects can be increased when Acepromazine is combined with Thiocolchicoside.
Aceprometazine The risk or severity of adverse effects can be increased when Aceprometazine is combined with Thiocolchicoside.
Acetazolamide The risk or severity of adverse effects can be increased when Acetazolamide is combined with Thiocolchicoside.
Acetophenazine The risk or severity of adverse effects can be increased when Acetophenazine is combined with Thiocolchicoside.

Additional Data Available

  • Extended Description

    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more

  • Severity

    Severity

    A severity rating for each drug interaction, from minor to major.

    Learn more

  • Evidence Level

    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more

  • Action

    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more

Food Interactions
Not Available

References

  1. ^
  2. Soonawalla DF, Joshi N (May 2008). «Efficacy of thiocolchicoside in Indian patients suffering from low back pain associated with muscle spasm». Journal of the Indian Medical Association. 106 (5): 331–5.  .
  3. «Thiocolchicoside: review of adverse effects». Prescrire International. 25 (168): 41–3. February 2016.  .
Skeletal ()
(primarily ,)
  • short duration:
  • intermediate duration:
  • long duration:
  • unsorted: Hexafluronium (Hexafluorenium)

esters
()
Other
  • Thiocolchicoside
(, )
  • # (, )
  • # ()
Semisynthetic
  • ()
  • ()
  • (, , )
  • (, , , , +naltrexone)
Synthetic
  • # ()
  • #
-type
  • Butacetin‡
  • #
  • Parapropamol‡
Propionates
  • #
Oxicams
Acetates
  • # ()
  • ()
  • ()
Others
  • (e.g., , )
  • (e.g., #)
  • Nav1.7/1.8-selective: §
  • §
  • §
Others
  • (e.g., #)
  • #
  • ‡ from market
  • :

    • §Never to phase III
(NSAIDs) (primarily and , also )
  • #
derivativesand related substances
  • Isoxepac
  • Prodolic acid
  • Tiopinac
derivatives(profens)
  • #
N-Arylanthranilic acids()
  • Flutiazin
Other
Items listed in bold indicate initially developed compounds of specific groups. #†. ‡ medications.

Template:GABA receptor antagonists
Template:Glycine receptor antagonists

(and )
  • A-582,941
  • A-867,744
  • ABT-560
  • ABT-894
  • Ethoxysebacylcholine
  • EVP-4473
  • MEM-63,908 (RG-3487)
  • ()
  • NS-1738
  • PHA-709,829
  • Sebacylcholine
  • SIB-1508Y
  • Suberyldicholine
  • TC-1734
  • TC-6683
  • XY-4083
(and )
  • (e.g., , , , many others)
  • ABT-126
  • Anatruxonium
  • AQW051
  • (e.g., , )
  • (e.g., , )
  • Diadonium
  • DHβE
  • Thiocolchicoside
  • Tropeinium
(and )
  • ()
See also: Receptor/signaling modulators • Muscarinic acetylcholine receptor modulators • Acetylcholine metabolism/transport modulators
Стаж работы Ярослава составляет 25 лет, из них 15 лет в клинической травматологии. Закончив лечебный факультет, одного из крупнейших медицинских вузов СССР в 1982 г., Ярослав Филатов проходил многочисленные усовершенствования и повышения квалификации, последняя из них пройдена в 2017 г.
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