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(1-Methylethyl)carbamic acid 2-(((aminocarbonyl)oxy)methyl)-2-methylpentyl ester
Also known as: 78-44-4, Isomeprobamate, Carisoprodate, Soma, Carisoprodatum, Carisoma
Molecular Formula
C12H24N2O4
Molecular Weight
260.33  g/mol
InChI Key
OFZCIYFFPZCNJE-UHFFFAOYSA-N
FDA UNII
21925K482H

A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202)
Carisoprodol is a Muscle Relaxant. The physiologic effect of carisoprodol is by means of Centrally-mediated Muscle Relaxation.
1 2D Structure

(1-Methylethyl)carbamic acid 2-(((aminocarbonyl)oxy)methyl)-2-methylpentyl ester

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
[2-(carbamoyloxymethyl)-2-methylpentyl] N-propan-2-ylcarbamate
2.1.2 InChI
InChI=1S/C12H24N2O4/c1-5-6-12(4,7-17-10(13)15)8-18-11(16)14-9(2)3/h9H,5-8H2,1-4H3,(H2,13,15)(H,14,16)
2.1.3 InChI Key
OFZCIYFFPZCNJE-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CCCC(C)(COC(=O)N)COC(=O)NC(C)C
2.2 Other Identifiers
2.2.1 UNII
21925K482H
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Carisoma

2. Carisoprodate

3. Isobamate

4. Isomeprobamate

5. Isopropylmeprobamate

6. Mio Relax

7. Soma

8. Somalgit

9. Soprodol

10. Vanadom

2.3.2 Depositor-Supplied Synonyms

1. 78-44-4

2. Isomeprobamate

3. Carisoprodate

4. Soma

5. Carisoprodatum

6. Carisoma

7. Isobamate

8. Isoprotane

9. Isoprothane

10. Sanoma

11. Isopropyl Meprobamate

12. Atonalyt

13. Flexartal

14. Miolisodal

15. Mioratrina

16. Skutamil

17. Somalgit

18. Apesan

19. Arusal

20. Flexal

21. Mioril

22. Nospasm

23. Relasom

24. Somanil

25. Rela

26. Carlsoprol

27. Brianil

28. Calenfa

29. Caprodat

30. Carisol

31. Carlsodol

32. Carlsoma

33. Carsodal

34. Diolene

35. Domarax

36. Isoprotan

37. Izoprotan

38. Mediquil

39. Mioriodol

40. Somadril

41. Stialgin

42. Carisoprodolum

43. Carsodol

44. Carisoprodolum [inn-latin]

45. Tonolyt Isopropyl Meprobamate

46. Nci-c56235

47. Sch 7307

48. Miolisodol

49. Flexartel

50. Cb 8019

51. Carisoprodol Civ

52. 2-methyl-2-propyl-1,3-propanediol Carbamate Isopropylcarbamate

53. [2-(carbamoyloxymethyl)-2-methylpentyl] N-propan-2-ylcarbamate

54. (1-methylethyl)carbamic Acid 2-(((aminocarbonyl)oxy)methyl)-2-methylpentyl Ester

55. Nsc-172124

56. Isopropylcarbamic Acid, Ester With 2-(hydroxymethyl)-2-methylpentyl Carbamate

57. Mls000028401

58. Chebi:3419

59. Artifar

60. Caridolin

61. Chinchen

62. Fibrosona

63. Flexagilt

64. Flexagit

65. Flexidon

66. Listaflex

67. Meprodat

68. Neotica

69. Muslax

70. Scutamil-c

71. Carbamic Acid, Ester With 2-methyl-2-propyl-1,3-propanediol Isopropylcarbamate

72. Carbamic Acid, (1-methylethyl)-, 2-(((aminocarbonyl)oxy)methyl)-2-methylpentyl Ester

73. Carbamic Acid, Isopropyl-, 2-(hydroxymethyl)-2-methylpentyl Ester Carbamate (ester)

74. Ncgc00015278-09

75. Smr000058433

76. 21925k482h

77. (+-)-2-methyl-2-propyl-1,3-propanediol Carbamate Isopropylcarbamate

78. Dsstox_cid_4733

79. Carbamic Acid, (1-methylethyl)-, 2-[[(aminocarbonyl)oxy]methyl]-2-methylpentyl Ester

80. Dsstox_rid_77514

81. Dsstox_gsid_24733

82. Isopropylmeprobamate

83. 2-((carbamoyloxy)methyl)-2-methylpentyl Isopropylcarbamate

84. 2-methyl-2-propyltrimethylene Carbamate Isopropylcarbamate

85. Carisoprodolo [dcit]

86. N-isopropy-2-methyl-2-propyl-1,3-propanediol Dicarbamate

87. Carisoprodolo

88. Prazolamine

89. Carbamic Acid 2-isopropylcarbamoyloxymethyl-2-methyl-pentyl Ester

90. (+/-)-2-methyl-2-propyl-1,3-propanediol Carbamate Isopropylcarbamate

91. Carbamic Acid, Ester With 2-(hydroxymethyl)-2-methylpentylisopropyl Carbamate

92. Ccris 4764

93. Hsdb 3021

94. Sr-01000000076

95. Einecs 201-118-7

96. Nsc 172124

97. Brn 1791537

98. Carisoprodol [usp:inn:ban]

99. 2-{[(aminocarbonyl)oxy]methyl}-2-methylpentyl Isopropylcarbamate

100. Cas-78-44-4

101. Prestwick_50

102. Unii-21925k482h

103. Mfcd00057661

104. Soma (tn)

105. N-isopropyl-2-methyl-2-propyl-1,3-propanediol Dicarbamate

106. Spectrum_000102

107. Opera_id_1100

108. Prestwick0_000423

109. Prestwick1_000423

110. Prestwick2_000423

111. Prestwick3_000423

112. Spectrum2_001153

113. Spectrum3_000328

114. Spectrum4_000265

115. Spectrum5_000661

116. Carisoprodol [mi]

117. Carisoprodol [inn]

118. Carisoprodol [jan]

119. 1,3-propanediol, 2-methyl-2-propyl-, Carbamate Isopropylcarbamate (ester)

120. Carbamic Acid, Ester With 2-(hydroxymethyl)-2-methylpentyl Isopropylcarbamate

121. Carisoprodol [hsdb]

122. Carisoprodol [vandf]

123. Chembl1233

124. Lopac0_000319

125. Schembl33286

126. Bspbio_000406

127. Bspbio_001935

128. Carisoprodol [mart.]

129. Kbiogr_000730

130. Kbioss_000542

131. Mls001148409

132. Mls002454391

133. Carisoprodol [who-dd]

134. Divk1c_000816

135. Spectrum1500162

136. Carisoprodol (jan/usp/inn)

137. Spbio_001105

138. Spbio_002345

139. Bpbio1_000448

140. Gtpl7610

141. Dea No. 8192

142. Dtxsid8024733

143. Hms502i18

144. Kbio1_000816

145. Kbio2_000542

146. Kbio2_003110

147. Kbio2_005678

148. Kbio3_001155

149. Carisoprodol Civ [usp-rs]

150. Ninds_000816

151. Carisoprodol [ep Impurity]

152. Carisoprodol [orange Book]

153. Hms1569e08

154. Hms1920k03

155. Hms2091a06

156. Hms2096e08

157. Hms2234f13

158. Hms3259o15

159. Hms3372h19

160. Hms3713e08

161. Pharmakon1600-01500162

162. Hy-b1380

163. Carisoprodol [usp Monograph]

164. Carisoprodol 1.0 Mg/ml In Methanol

165. Tox21_110122

166. Tox21_200623

167. Ac-212

168. Ccg-40092

169. Nsc172124

170. Nsc756671

171. Akos015842914

172. Tox21_110122_1

173. Wln: Zvo1x3&1&1ovmy1&1

174. Cs-4819

175. Db00395

176. Lp00319

177. Nc00502

178. Nsc-756671

179. Sdccgsbi-0050307.p005

180. Idi1_000816

181. Ncgc00015278-03

182. Ncgc00015278-04

183. Ncgc00015278-05

184. Ncgc00015278-06

185. Ncgc00015278-07

186. Ncgc00015278-08

187. Ncgc00015278-11

188. Ncgc00015278-12

189. Ncgc00015278-14

190. Ncgc00015278-15

191. Ncgc00089734-02

192. Ncgc00089734-03

193. Ncgc00089734-04

194. Ncgc00089734-05

195. Ncgc00089734-06

196. Ncgc00089734-07

197. Ncgc00258177-01

198. Sbi-0050307.p004

199. Soma Compound Component Carisoprodol

200. Carisoprodol 100 Microg/ml In Acetonitrile

201. Ab00051932

202. C3573

203. Eu-0100319

204. Ft-0601536

205. Ft-0656125

206. Carbamic Acid,3-propanediol Isopropylcarbamate

207. Carisoprodol Component Of Soma Compound

208. C 8759

209. D00768

210. N-isopropyl-2-methyl-2-propyl-1, Dicarbamate

211. Ab00051932_15

212. 057c661

213. Carisoprodol Compound Component Carisoprodol

214. Q416905

215. Sr-01000000076-2

216. Sr-01000000076-4

217. Sr-01000000076-6

218. W-104280

219. 1, 2-methyl-2-propyl-, Carbamate Isopropylcarbamate

220. Carisoprodol Component Of Carisoprodol Compound

221. Z1565440360

222. N-isopropyl-2-methyl-2-propyl-1,3-propanediol, Dicarbamate

223. 2-[(carbamoyloxy)methyl]-2-methylpentyl Propan-2-ylcarbamate

224. Carisoprodol, European Pharmacopoeia (ep) Reference Standard

225. 1,3-propanediol, 2-methyl-2-propyl-, Carbamate Isopropylcarbamate

226. 2-[(carbamoyloxy)methyl]-2-methylpentyl N-(propan-2-yl)carbamate

227. Carisoprodol, United States Pharmacopeia (usp) Reference Standard

228. (rs)-2-{[(aminocarbonyl)oxy]methyl}-2-methylpentyl Isopropylcarbamate

229. Carbamic Acid, Isopropyl-, 2-(hydroxymethyl)-2-methylpentyl Ester Carbamate

230. Carbamic Acid, Isopropyl-, 2-(hydroxymethyl)-2-methylpentyl Ester, Carbamate

231. Carisoprodol Solution, 1.0 Mg/ml In Methanol, Ampule Of 1 Ml, Certified Reference Material

2.4 Create Date
2005-03-25
3 Chemical and Physical Properties
Molecular Weight 260.33 g/mol
Molecular Formula C12H24N2O4
XLogP31.9
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count4
Rotatable Bond Count9
Exact Mass260.17360725 g/mol
Monoisotopic Mass260.17360725 g/mol
Topological Polar Surface Area90.6 Ų
Heavy Atom Count18
Formal Charge0
Complexity281
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count1
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Information
1 of 4  
Drug NameCarisoprodol
PubMed HealthCarisoprodol (By mouth)
Drug ClassesSkeletal Muscle Relaxant, Centrally Acting
Drug LabelCarisoprodol tablets USP are available as 350 mg round, white tablets. Carisoprodol is a white, crystalline powder, having a mild, characteristic odor and a bitter taste. It is slightly soluble in water; freely soluble in alcohol, in chloroform, and...
Active IngredientCarisoprodol
Dosage FormTablet
RouteOral
Strength350mg
Market StatusPrescription
CompanyWatson Labs; Vintage Pharms; Mutual Pharm; Mirror Pharms; Sciegen Pharms; Aurobindo Pharma; Sun Pharm Inds; Accelrx Labs

2 of 4  
Drug NameSoma
PubMed HealthCarisoprodol (By mouth)
Drug ClassesSkeletal Muscle Relaxant, Centrally Acting
Drug LabelSOMA (carisoprodol) Tablets are available as 250 mg and 350 mg round, white tablets. Carisoprodol is a white, crystalline powder, having a mild, characteristic odor and a bitter taste. It is slightly soluble in water; freely soluble in alcohol, in ch...
Active IngredientCarisoprodol
Dosage FormTablet
RouteOral
Strength250mg; 350mg
Market StatusPrescription
CompanyMeda Pharms

3 of 4  
Drug NameCarisoprodol
PubMed HealthCarisoprodol (By mouth)
Drug ClassesSkeletal Muscle Relaxant, Centrally Acting
Drug LabelCarisoprodol tablets USP are available as 350 mg round, white tablets. Carisoprodol is a white, crystalline powder, having a mild, characteristic odor and a bitter taste. It is slightly soluble in water; freely soluble in alcohol, in chloroform, and...
Active IngredientCarisoprodol
Dosage FormTablet
RouteOral
Strength350mg
Market StatusPrescription
CompanyWatson Labs; Vintage Pharms; Mutual Pharm; Mirror Pharms; Sciegen Pharms; Aurobindo Pharma; Sun Pharm Inds; Accelrx Labs

4 of 4  
Drug NameSoma
PubMed HealthCarisoprodol (By mouth)
Drug ClassesSkeletal Muscle Relaxant, Centrally Acting
Drug LabelSOMA (carisoprodol) Tablets are available as 250 mg and 350 mg round, white tablets. Carisoprodol is a white, crystalline powder, having a mild, characteristic odor and a bitter taste. It is slightly soluble in water; freely soluble in alcohol, in ch...
Active IngredientCarisoprodol
Dosage FormTablet
RouteOral
Strength250mg; 350mg
Market StatusPrescription
CompanyMeda Pharms

4.2 Therapeutic Uses

Muscle Relaxants, Central

National Library of Medicine's Medical Subject Headings online file (MeSH, 1999)


Carisoprodol is used as an adjunct to rest, physical therapy, analgesics, and other measures for the relief of discomfort associated with acute, painful musculoskeletal conditions. /Included in US product label/

American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 1391


4.3 Drug Warning

Occasionally, patients may have allergic or idiosyncratic reactions to carisoprodol. In patients who have not received carisoprodol previously, these reactions are usually evident by the time of the fourth dose of the drug. Idiosyncratic reactions may be characterized by extreme weakness, transient quadriplegia, dizziness, ataxia, temporary loss of vision, diplopia, mydriasis, dysarthria, agitation, euphoria, confusion, and disorientation. These symptoms usually subside within several hours; however, symptomatic and supportive therapy, including hospitalization, may be necessary in some patients. Rash, erythema multiforme, pruritus, urticaria, eosinophilia, and fixed drug eruption have occurred in patients receiving carisoprodol who previously had similar reactions to meprobamate. Severe allergic reactions have been characterized by asthmatic episodes, fever, weakness, dizziness, angioedema, smarting eyes, hypotension, and anaphylactic shock.

American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 1391


The most frequent adverse effects of carisoprodol are drowsiness and dizziness. Other adverse CNS effects include vertigo, ataxia, tremor, agitation, irritability, headache, depressive reactions, syncope, and insomnia.

American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 1391


Because carisoprodol is metabolized by the liver and excreted by the kidneys, the drug should be used with caution in patients with impaired hepatic or renal function. Patients should be warned that carisoprodol may impair ability to perform hazardous activities requiring mental alertness or physical coordination such as operating machinery or driving a motor vehicle.

American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 1391


Adverse GI effects of carisoprodol include nausea, vomiting, hiccups, increased bowel activity, and epigastric distress. Adverse cardiovascular effects include tachycardia, postural hypotension, and facial flushing. Although a causal relationship to carisoprodol has not been established, leukopenia and pancytopenia have occurred rarely in patients receiving carisoprodol along with other drugs.

American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 1391


For more Drug Warnings (Complete) data for CARISOPRODOL (13 total), please visit the HSDB record page.


4.4 Drug Indication

Carisoprodol is indicated for the relief of discomfort related to acute, painful musculoskeletal conditions. **Important limitations of use**: Should only be used for acute treatment periods up to two or three weeks Adequate evidence of effectiveness for more prolonged use has not been established Not recommended in pediatric patients less than 16 years of age


FDA Label


5 Pharmacology and Biochemistry
5.1 Pharmacology

Carisoprodol is a centrally acting skeletal muscle relaxant that does not act directly on skeletal muscle but acts directly on the central nervous system (CNS). This drug relieves the painful effects of muscle spasm. A metabolite of carisoprodol, _meprobamate_, possesses both anxiolytic and sedative properties. Clinical studies have shown that this drug causes impairment of psychomotor performance in neuropsychological tests.


5.2 MeSH Pharmacological Classification

Muscle Relaxants, Central

A heterogeneous group of drugs used to produce muscle relaxation, excepting the neuromuscular blocking agents. They have their primary clinical and therapeutic uses in the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. They have been used also for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in MULTIPLE SCLEROSIS. (From Smith and Reynard, Textbook of Pharmacology, 1991, p358) (See all compounds classified as Muscle Relaxants, Central.)


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety
CARISOPRODOL
5.3.2 FDA UNII
21925K482H
5.3.3 Pharmacological Classes
Muscle Relaxant [EPC]; Centrally-mediated Muscle Relaxation [PE]
5.4 ATC Code

M - Musculo-skeletal system

M03 - Muscle relaxants

M03B - Muscle relaxants, centrally acting agents

M03BA - Carbamic acid esters

M03BA02 - Carisoprodol


5.5 Absorption, Distribution and Excretion

Absorption

The absolute bioavailability of carisoprodol has not yet been established. The mean time to peak plasma concentrations (Tmax) of this drug was about 1.5-2 hours in clinical studies. Co-administration of a fatty meal with carisoprodol (350 mg tablet) had no impact on carisoprodol pharmacokinetics.


Route of Elimination

Carisoprodol is eliminated by the kidneys as well as other routes. The half-life of meprobamate is approximately 10 hours.


Volume of Distribution

0.93 to 1.3 L/kg, according to 4 different clinical studies.


Clearance

Following an oral dose of carisoprodol, the oral clearance (Cl/F) was 39.52 16.83 L/hour.


Carisoprodol crosses the placenta. The drug distributes into milk in concentrations 2-4 times higher than concurrent maternal plasma concentrations.

American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 1391


Plasma concentrations of carisoprodol required for sedative, skeletal muscle relaxant, or toxic effects are not known. One manufacturer reports that plasma concentrations of 4-7 ug/mL were attained in 4 hours following oral administration of 350 mg of carisoprodol to healthy adults. Following usual therapeutic dosages, the onset of action is usually within 30 minutes and the duration of action is 4-6 hours.

American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 1391


The objective of this study was to quantify the excretion of carisoprodol and meprobamate in human milk and estimate the dose received by breast-fed infants. The concentrations of carisoprodol and meprobamate were measured in breast milk on 4 consecutive days at steady-state conditions in one woman using carisoprodol 2100 mg/d. The average milk concentrations were 0.9 microg/mL for carisoprodol and 11.6 ug/mL for meprobamate. Based on the milk concentrations measured, the absolute dose ingested by an exclusively breast-fed infant could be estimated at 1.9 mg/kg per day, and the relative dose would be 4.1% of the weight-adjusted maternal dose. ...

PMID:11360042 Nordeng H et al; Ther Drug Monit 23 (3): 298-300 (2001)


5.6 Metabolism/Metabolites

The main pathway of carisoprodol is liver metabolism is by the cytochrome enzyme CYP2C19 to form meprobamate. This enzyme exhibits genetic polymorphism, which may affect the metabolism of this drug.


The major pathway of carisoprodol metabolism is via the liver by cytochrome enzyme CYP2C19 to form meprobamate. This enzyme exhibits genetic polymorphism.

US Natl Inst Health; DailyMed. Current Medication Information for CARISOPRODOL (carisoprodol ) tablet (May 2010). Available from, as of November 17, 2010: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=19431


Carisoprodol is metabolized in the liver; animal studies indicate the drug may induce liver microsomal enzymes. Animal studies also indicate that the drug is excreted in urine, principally as hydroxycarisoprodol and hydroxymeprobamate, and to a lesser extent as meprobamate; trace amounts of carisoprodol are excreted unchanged in urine. The drug may be removed by hemodialysis or peritoneal dialysis.

American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 1391


Carisoprodol is a muscle relaxant analgesic, which has an active metabolite i.e. meprobamate. We conducted an open three-panel single-dose administration study with 15 healthy volunteers: five poor metabolizers of mephenytoin, five poor metabolizers of debrisoquine and five extensive metabolizers of both substrates. The aim was to investigate if the elimination of carisoprodol and meprobamate is dependent on the two metabolic polymorphisms of mephenytoin and debrisoquine. The subjects were given single oral doses of 700 mg carisoprodol and 400 mg meprobamate on separate occasions. The disposition of carisoprodol was clearly correlated to the mephenytoin hydroxylation phenotype. The mean serum clearance of carisoprodol was four times lower in poor metabolizers of mephenytoin than in extensive metabolizers, which confirms the hypothesis from our previous study that N-dealkylation of carisoprodol cosegregates with the mephenytoin hydroxylation polymorphism. However, mean serum clearance of meprobamate did not differ between the two groups. Also, polymorphic debrisoquine hydroxylation did not influence the elimination of carisoprodol or meprobamate. Poor metabolizers of mephenytoin thus have a lower capacity to metabolize carisoprodol and may therefore have an increased risk of developing concentration dependent side-effects such as drowsiness and hypotension, if treated with ordinary doses of carisoprodol.

PMID:8946470 Dalen P et al; Pharmacogenetics 6 (5): 387-94 (1996)


5.7 Biological Half-Life

The terminal half-life is approximately 2 hours.


Carisoprodol is eliminated by both renal and non-renal routes with a terminal elimination half-life of approximately 2 hours. The half-life of meprobamate is approximately 10 hours.

US Natl Inst Health; DailyMed. Current Medication Information for CARISOPRODOL (carisoprodol ) tablet (May 2010). Available from, as of November 17, 2010: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=19431


The plasma half-life of carisoprodol is approximately 8 hours.

American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 1391


5.8 Mechanism of Action

The mechanism of action of carisoprodol in relieving discomfort associated with acute painful musculoskeletal conditions has not been confirmed. In studies using animal models, the muscle relaxation that is induced by carisoprodol is associated with a change in the interneuronal activity of the spinal cord and of the descending reticular formation, located in the brain. The abuse potential of this drug is attributed to its ability to alter GABAA function. This drug has been shown to modulate a variety of GABAA receptor subunits. GABAA receptor modulation can lead to anxiolysis due to inhibitory effects on neurotransmission.


Carisoprodol is a CNS depressant which has sedative and skeletal muscle relaxant effects. The precise mechanism of action of the drug is not known. The skeletal muscle relaxant effects of orally administered carisoprodol are minimal and are probably related to its sedative effect. The drug does not directly relax skeletal muscle and, unlike neuromuscular blocking agents, does not depress neuronal conduction, neuromuscular transmission, or muscle excitability. In animals, carisoprodol appears to modify central perception of pain without abolishing peripheral pain reflexes and to have slight antipyretic activity, but these effects have not been demonstrated in clinical studies.

American Society of Health System Pharmacists; AHFS Drug Information 2010. Bethesda, MD. (2010), p. 1391


Carisoprodol is an increasingly abused, centrally-acting muscle relaxant. Despite the prevalence of carisoprodol abuse, its mechanism of action remains unclear. Its sedative effects, which contribute to its therapeutic and recreational use, are generally attributed to the actions of its primary metabolite, meprobamate, at GABA(A) receptors (GABA(A)R). Meprobamate is a controlled substance at the federal level; ironically, carisoprodol is not currently classified as such. Using behavioral and molecular pharmacological approaches, we recently demonstrated carisoprodol, itself, is capable of modulating GABA(A)R function in a manner similar to central nervous system depressants. Its functional similarities with this highly addictive class of drugs may contribute to the abuse potential of carisoprodol. The site of action of carisoprodol has not been identified; based on our studies, interaction with benzodiazepine or barbiturate sites is unlikely. ...

PMID:20419052 Full text: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2858432 Gonzalez LA et al; Mol Cell Pharmacol 1 (4): 180-186 (2009)


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