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Few Muscle Relaxants

Afloqualone

Drug Nomenclature

Synonyms: Aflocualona; HQ-495
INN: Afloqualone [rINN (en)]
INN: Aflocualona [rINN (es)]
INN: Afloqualone [rINN (fr)]
INN: Afloqualonum [rINN (la)]
INN: Афлоквалон [rINN (ru)]
Chemical name: 6-Amino-2-fluoromethyl-3-o-tolylquinazolin-4(3H)-one
Molecular formula: C16H14FN3O =283.3
CAS: 56287-74-2

Pharmacopoeias. In Japan.

Profile

Afloqualone is a centrally acting skeletal muscle relaxant that has been given orally for the treatment of muscle spasm associated with musculoskeletal conditions. Photosensitivity reactions have been reported.

Eperisone Hydrochloride

Eperisone HydrochlorideDrug Nomenclature

INN: Eperisone Hydrochloride [rINNM (en)]
INN: Hidrocloruro de eperisona [rINNM (es)]
INN: Épérisone, Chlorhydrate d’ [rINNM (fr)]
INN: Eperisoni Hydrochloridum [rINNM (la)]
INN: Еперизона Гидрохлорид [rINNM (ru)]
Chemical name: 4´-Ethyl-2-methyl-3-piperidinopropiophenone hydrochloride
Molecular formula: C17H25NO,HCl =295.8
CAS: 64840-90-0 (eperisone)

Pharmacopoeias. In Japan.

Profile

Eperisone is a centrally acting skeletal muscle relaxant that has been used in the symptomatic treatment of muscle spasm and spasticity. It may also have a vasodilator action. Eperisone hydrochloride has been given by mouth in usual doses of 50 mg three times daily after food.

Effects on the skin. A non-pigmenting fixed drug eruption developed in a 42-year-old woman after taking oral diclofenac sodium and eperisone hydrochloride. There was no residual hyperpigmentation and the rash and accompanying itching and burning sensation resolved within 7 days after stopping both drugs. On rechallenge with eperisone, an erythematous plaque developed at the same site within a couple of hours. The lesion disappeared within 5 days with no sequelae.

Proprietary Preparations

Indonesia: Eprinoc; Epsonal; Forelax; Forres; Myonal; Myonep; Myori; Permyo; Rizonax; Zonal;

Japan: Myonal;

Malaysia: Myonal;

Philippines: Myonal;

Singapore; Myonal;

Thailand: Myonal.

Idrocilamide

Drug Nomenclature

Synonyms: Idrocilamida; LCB-29
INN: Idrocilamide [rINN (en)]
INN: Idrocilamida [rINN (es)]
INN: Idrocilamide [rINN (fr)]
INN: Idrocilamidum [rINN (la)]
INN: Идроциламид [rINN (ru)]
Chemical name: N-(2-Hydroxyethyl)cinnamamide
Molecular formula: C11H13NO2 =191.2
CAS: 6961-46-2

Adverse Effects

When given by mouth idrocilamide was reported to produce abdominal pain, nausea, and drowsiness. Excitement, euphoria and hallucinations, and depression may occur.

Uses and Administration

Idrocilamide is a centrally acting muscle relaxant. It is reported to have local muscle relaxant and anti-inflammatory effects and is now mainly used topically.

Proprietary Preparations

Belgium: Srilane;

France: Srilane;

Hong Kong; Srilane ;

Switzerland: Talval.

Mephenesin

MephenesinDrug Nomenclature

Synonyms: Cresoxydiol; Glykresin; Mefenesiini; Mefenesin; Mefenesina; Mephenesinum
BAN: Mephenesin
INN: Mephenesin [rINN (en)]
INN: Mefenesina [rINN (es)]
INN: Méphénésine [rINN (fr)]
INN: Mephenesinum [rINN (la)]
INN: Мефенезин [rINN (ru)]
Chemical name: 3-(o-Tolyloxy)propane-1,2-diol
Molecular formula: C10H14O3 =182.2
CAS: 59-47-2
ATC code: M03BX06

Note. The name tolynol has been applied to both mephenesin and p,α-dimethylbenzyl alcohol.

Pharmacopoeias. In Italy.

Profile

Mephenesin is a centrally acting skeletal muscle relaxant used for the symptomatic treatment of painful muscle spasm associated with musculoskeletal conditions. Its clinical usefulness is considered to be limited by its brief duration of action. It is given orally in doses of 1.5 to 3 g daily in divided doses. It is also applied topically, usually with rubefacients.

Porphyria. Mephenesin is considered to be unsafe in patients with porphyria because it has been shown to be porphyrinogenic in in-vitro systems.

Preparations

Proprietary Preparations

France: Decontractyl;

Germany: DoloVisano M.

Multi-ingredient

Belgium: Algipan;

France: Algipan; Decontractyl; Traumalgyl;

India: Acks; Flamar; Inflazone; Medicreme; Relaxyl;

Italy: Relaxar;

South Africa: Spas mend.

Mephenoxalone

Drug Nomenclature

Synonyms: AHR-233; Mefenoxalona; Methoxadone; OM-518
INN: Mephenoxalone [rINN (en)]
INN: Mefenoxalona [rINN (es)]
INN: Méphénoxalone [rINN (fr)]
INN: Mephenoxalonum [rINN (la)]
INN: Мефеноксалон [rINN (ru)]
Chemical name: 5-(2-Methoxyphenoxymethyl)oxazolidin-2-one
Molecular formula: C11H13NO4 =223.2
CAS: 70-07-5
ATC code: N05BX01

Profile

Mephenoxalone has actions similar to those of meprobamate. It has been given orally in a dose of 200 to 400 mg three times daily as a muscle relaxant in the treatment of muscle spasm. It has also been given for the treatment of anxiety.

Preparations

Proprietary Preparations

Czech Republic: Dimexol; Dorsiflex;

The Netherlands: Dorsiflex;

Turkey: Dorsiflex.

Multi-ingredient

Turkey: Dorsilon

Metaxalone

MetaxaloneDrug Nomenclature

Synonyms: AHR-233; Mefenoxalona; Methoxadone; OM-518
INN: Mephenoxalone [rINN (en)]
INN: Mefenoxalona [rINN (es)]
INN: Méphénoxalone [rINN (fr)]
INN: Mephenoxalonum [rINN (la)]
INN: Мефеноксалон [rINN (ru)]
Chemical name: 5-(2-Methoxyphenoxymethyl)oxazolidin-2-one
Molecular formula: C11H13NO4 =223.2
CAS: 70-07-5
ATC code: N05BX01

Adverse Effects, Treatment, and Precautions

As for Chlorzoxazone.

Metaxalone may cause drowsiness; patients affected should not drive or operate machinery.

Patients taking metaxalone excrete in the urine a metabolite which gives a false positive reaction to copper sulfate-based tests for glycosuria.

Interactions

The CNS effects of metaxalone may be enhanced by alcohol and other CNS depressants.

Pharmacokinetics

Metaxalone is absorbed from the gastrointestinal tract, metabolised in the liver, and excreted in urine as metabolites. The plasma elimination half-life is about 2 to 3 hours.

Uses and Administration

Metaxalone is a centrally acting skeletal muscle relaxant. Its mode of action may be related to its sedative properties. It is used as an adjunct in the symptomatic treatment of painful muscle spasm associated with musculoskeletal conditions. The usual oral dose is 800 mg three or four times daily.

Proprietary Preparations

USA: Skelaxin

Pridinol Mesilate

Drug Nomenclature

 
Synonyms: C-238 (pridinol); Pridinol Mesylate; Pridinol, mesilato de
INN: Pridinol Mesilate [rINNM (en)]
INN: Mesilato de pridinol [rINNM (es)]
INN: Pridinol, Mésilate de [rINNM (fr)]
INN: Pridinoli Mesilas [rINNM (la)]
INN: Придинола Мезилат [rINNM (ru)]
Chemical name: 1,1-Diphenyl-3-piperidinopropan-1-ol methanesulphonate
Molecular formula: C20H25NO,CH3SO3H =391.5
CAS: 511-45-5 (pridinol); 968-58-1 (pridinol hydrochloride); 6856-31-1 (pridinol mesilate)
ATC code: M03BX03

Profile

Pridinol mesilate is a centrally acting muscle relaxant used in the symptomatic treatment of muscle spasm. The usual initial oral dose is 2 to 8 mg three times daily, reduced to 4 to 8 mg daily for maintenance treatment. It is also given by intramuscular injection or rectally, and has been applied in compound topical preparations.

Pridinol has been used as the hydrochloride for its antimuscarinic properties in the management of parkinsonism.

Preparations

Proprietary Preparations

Germany: Myoson; Parks ;

Hong Kong; Konlax ;

Italy: Lyseen;

Poland: Polmesilat.

Multi-ingredient

Argentina: Blokum Flex; Curinflam Plus; Diclogesic Relax; Diclomar Flex; Diclonex Relax; Dioxaflex Plus; Dolvan Flex; Doxtran Flex; Flexidol Relax; Iglodine Flex; Metaflex Plus NF; Mextran Flex; Mio Aldoron NF; Mio-Virobron NF; Nalgiflex Relax; Oxa Sport; Oxadisten; Pancloflex; Rodinac Flex; Silfox Flex; Tomanil Flex; Vesalion Flex; Viartril Flex; Voltaren Flex; Xedenol Flex;

Italy: Algolisina.

Thiocolchicoside

Drug Nomenclature

 
INN: Thiocolchicoside [rINN (en)]
INN: Tiocolchicósido [rINN (es)]
INN: Thiocolchicoside [rINN (fr)]
INN: Thiocolchicosidum [rINN (la)]
INN: Тиокольхикозид [rINN (ru)]
Chemical name: 3,10-Di(demethoxy)-3-glucopyranosyloxy-10-methylthiocolchicine
Molecular formula: C27H33NO10S =563.6
CAS: 602-41-5
ATC code: M03BX05

Pharmacopoeias. In France.

Profile

Thiocolchicoside is a muscle relaxant that has been claimed to possess GABA-mimetic and glycinergic actions. It is used in the symptomatic treatment of painful muscle spasm. The usual initial oral dose is 16 mg daily given in 2 divided doses. It has also been given intramuscularly, in doses up to 8 mg daily, or applied as cream or ointment. Photosensitivity reactions may occur.

Preparations

Proprietary Preparations

Brazil: Coltrax; Muscoril;

Czech Republic: Muscoril;

France: Coltramyl; Miorel; Myoplege;

Greece: Disintryl; Haliver; Klesidren; Muscoril; Thiacomin ;

India: Myoril;

Italy: Decontril; Miotens; Muscoflex; Muscoril; Sciomir; Strialisin; Teraside; Ticathion; Tiorilene; Tioside;

Poland: Muscoril;

Portugal: Coltramyl; Relmus;

Turkey: Muscoflex; Muscoril;

Venezuela: Biocolchid; Coltrax; Colval; Cosiden ; Eusilen; Lampral; Tiochax; Tractil.

Multi-ingredient

Italy: Muscoril Trauma;

Mexico: Neuroflax;

Portugal: Adalgur N; Relmus Compositum ;

Spain: Adalgur;

Venezuela: Colfene.

Tolperisone Hydrochloride

Drug Nomenclature

 
Synonyms: N-553; Tolperisona, hidrocloruro de
BAN: Tolperisone Hydrochloride [BANM]
INN: Tolperisone Hydrochloride [rINNM (en)]
INN: Hidrocloruro de tolperisona [rINNM (es)]
INN: Tolpérisone, Chlorhydrate de [rINNM (fr)]
INN: Tolperisoni Hydrochloridum [rINNM (la)]
INN: Тольперизона Гидрохлорид [rINNM (ru)]
Chemical name: 2,4´-Dimethyl-3-piperidinopropiophenone hydrochloride
Molecular formula: C16H23NO,HCl =281.8
CAS: 728-88-1 (tolperisone); 3644-61-9 (tolperisone hydrochloride)
ATC code: M03BX04

Pharmacopoeias. In Japan.

Profile

Tolperisone hydrochloride is a centrally acting muscle relaxant that has been used for the symptomatic treatment of spasticity and muscle spasm, in usual doses of 50 to 150 mg three times daily by mouth. It has also been given by injection.

Preparations

Proprietary Preparations

Argentina: Miodom;

Austria: Mydocalm;

Czech Republic: Mydocalm;

Germany; Mydocalm;

Hong Kong; Mydocalm;

Hungary: Myderison; Mydetonjfw; Muscalm;

Poland: Mydocalm; Tolperis;

Russia: Mydocalm;

Switzerland: Mydocalm;

Thailand: Biocalm; Musocalm; Mydocalm; Mydono; Mydosone; Myoxan; Risocalm; Shiwalax ; Soneriper; Spamus ; Tanderon.

Multi-ingredient

Mexico: Mydocalm-A

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