Details of the Drug

General Information of Drug (ID: DMWR1JC)

Drug Name

Carisoprodol

Synonyms

carisoprodol; 78-44-4; Isomeprobamate; Carisoprodate; Carisoprodatum; Isoprotane; Isobamate; Isoprothane; Carisoma; Sanoma; Isopropyl meprobamate; SOMA; Somalgit; Atonalyt; Mioratrina; Mioartrina; Flexartal; Skutamil; Miolisodal; Mioril; Apesan; Relasom; Nospasm; Flexal; Arusal; Somanil; Carlsoprol; Carisoprodolum; Domarax; Stialgin; Somadril; Carsodal; Mioriodol; Mediquil; Izoprotan; Isoprotan; Carisol; Caprodat; Calenfa; Diolene; Carlsoma; Carlsodol; Brianil; Flexidon; Flexagilt; Caridolin; Meprodat; Listaflex; Flexagit; Fibrosona; Chinchen; Carsodol

Indication

Disease Entry	ICD 11	Status	REF
Back pain	ME84.Z	Approved	[1]
Musculoskeletal disorder	FA00-FC0Z	Approved	[2]
------------------------------------------------------------------------------------

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

260.329

Logarithm of the Partition Coefficient (xlogp)

1.9

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Absorption Tmax: The time to maximum plasma concentration (Tmax) is 1.5-2 h []
BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [3]
Clearance: The apparent oral clearance of drug is 39.52 +/- 16.83 L/h []
Half-life: The concentration or amount of drug in body reduced by one-half in 2 hours []
Metabolism: The drug is metabolized via the liver []
MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 76.8255 micromolar/kg/day [4]
Vd: The volume of distribution (Vd) of drug is 0.93-1.3 L/kg [5]

Chemical Identifiers

Formula: C12H24N2O4
IUPAC Name: [2-(carbamoyloxymethyl)-2-methylpentyl] N-propan-2-ylcarbamate
Canonical SMILES: CCCC(C)(COC(=O)N)COC(=O)NC(C)C
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)
InChIKey: OFZCIYFFPZCNJE-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 2576
ChEBI ID: CHEBI:3419
CAS Number: 78-44-4
DrugBank ID: DB00395
TTD ID: D05PLH
VARIDT ID: DR00993
INTEDE ID: DR0277
ACDINA ID: D00101

Combinatorial Drugs (CBD)

Click to Jump to the Detailed CBD Information of This Drug

Repurposed Drugs (RPD)

Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Mephenytoin 4-hydroxylase (CYP2C19)_{Main DME}	DEGTFWK	CP2CJ_HUMAN	Substrate	[6]

------------------------------------------------------------------------------------

Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Carisoprodol (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Arn-509	DMT81LZ	Moderate	Increased metabolism of Carisoprodol caused by Arn-509 mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[7]
Oliceridine	DM6MDCF	Major	Additive CNS depression effects by the combination of Carisoprodol and Oliceridine.	Acute pain [MG31]	[8]
Voriconazole	DMAOL2S	Moderate	Decreased metabolism of Carisoprodol caused by Voriconazole mediated inhibition of CYP450 enzyme.	Aspergillosis [1F20]	[9]
Dihydrocodeine	DMB0FWL	Major	Additive CNS depression effects by the combination of Carisoprodol and Dihydrocodeine.	Chronic pain [MG30]	[10]
Olopatadine	DMKMWQG	Moderate	Additive CNS depression effects by the combination of Carisoprodol and Olopatadine.	Conjunctiva disorder [9A60]	[11]
Alfentanil	DMVO0UB	Major	Additive CNS depression effects by the combination of Carisoprodol and Alfentanil.	Corneal disease [9A76-9A78]	[8]
Remifentanil	DMZTXCH	Major	Additive CNS depression effects by the combination of Carisoprodol and Remifentanil.	Corneal disease [9A76-9A78]	[8]
Osilodrostat	DMIJC9X	Moderate	Decreased metabolism of Carisoprodol caused by Osilodrostat mediated inhibition of CYP450 enzyme.	Cushing syndrome [5A70]	[12]
Lumacaftor	DMCLWDJ	Moderate	Increased metabolism of Carisoprodol caused by Lumacaftor mediated induction of CYP450 enzyme.	Cystic fibrosis [CA25]	[13]
Ethanol	DMDRQZU	Moderate	Additive CNS depression effects by the combination of Carisoprodol and Ethanol.	Cystitis [GC00]	[11]
Esketamine	DMVU687	Moderate	Additive CNS depression effects by the combination of Carisoprodol and Esketamine.	Depression [6A70-6A7Z]	[9]
Cenobamate	DM8KLU9	Moderate	Decreased metabolism of Carisoprodol caused by Cenobamate mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[14]
Brimonidine	DMQLT4N	Moderate	Additive CNS depression effects by the combination of Carisoprodol and Brimonidine.	Glaucoma [9C61]	[15]
Fenofibrate	DMFKXDY	Moderate	Decreased metabolism of Carisoprodol caused by Fenofibrate mediated inhibition of CYP450 enzyme.	Hyper-lipoproteinaemia [5C80]	[9]
Allopregnanolone	DMNLHAC	Moderate	Additive CNS depression effects by the combination of Carisoprodol and Allopregnanolone.	Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z]	[16]
Lasmiditan	DMXLVDT	Moderate	Additive CNS depression effects by the combination of Carisoprodol and Lasmiditan.	Migraine [8A80]	[17]
Flibanserin	DM70DTN	Moderate	Additive CNS depression effects by the combination of Carisoprodol and Flibanserin.	Mood disorder [6A60-6E23]	[18]
Thalidomide	DM70BU5	Moderate	Additive CNS depression effects by the combination of Carisoprodol and Thalidomide.	Multiple myeloma [2A83]	[19]
Fedratinib	DM4ZBK6	Moderate	Decreased metabolism of Carisoprodol caused by Fedratinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[7]
Modafinil	DMYILBE	Moderate	Decreased metabolism of Carisoprodol caused by Modafinil mediated inhibition of CYP450 enzyme.	Narcolepsy [7A20]	[9]
Levomethadyl Acetate	DM06HG5	Major	Additive CNS depression effects by the combination of Carisoprodol and Levomethadyl Acetate.	Opioid use disorder [6C43]	[10]
Apraclonidine	DMO4PVE	Moderate	Additive CNS depression effects by the combination of Carisoprodol and Apraclonidine.	Optic nerve disorder [9C40]	[15]
Pentazocine	DM1XBHS	Major	Additive CNS depression effects by the combination of Carisoprodol and Pentazocine.	Pain [MG30-MG3Z]	[8]
Dextropropoxyphene	DM23HCX	Major	Additive CNS depression effects by the combination of Carisoprodol and Dextropropoxyphene.	Pain [MG30-MG3Z]	[20]
Butorphanol	DM5KYPJ	Major	Additive CNS depression effects by the combination of Carisoprodol and Butorphanol.	Pain [MG30-MG3Z]	[8]
Oxymorphone	DM65AGJ	Major	Additive CNS depression effects by the combination of Carisoprodol and Oxymorphone.	Pain [MG30-MG3Z]	[8]
Dezocine	DMJDB0Y	Major	Additive CNS depression effects by the combination of Carisoprodol and Dezocine.	Pain [MG30-MG3Z]	[8]
Nalbuphine	DMOSQGU	Major	Additive CNS depression effects by the combination of Carisoprodol and Nalbuphine.	Pain [MG30-MG3Z]	[8]
Buprenorphine	DMPRI8G	Major	Additive CNS depression effects by the combination of Carisoprodol and Buprenorphine.	Pain [MG30-MG3Z]	[21]
Hydrocodone	DMQ2JO5	Major	Additive CNS depression effects by the combination of Carisoprodol and Hydrocodone.	Pain [MG30-MG3Z]	[8]
Meperidine	DMX4GND	Major	Additive CNS depression effects by the combination of Carisoprodol and Meperidine.	Pain [MG30-MG3Z]	[8]
Oxycodone	DMXLKHV	Major	Additive CNS depression effects by the combination of Carisoprodol and Oxycodone.	Pain [MG30-MG3Z]	[8]
Lonafarnib	DMGM2Z6	Moderate	Decreased metabolism of Carisoprodol caused by Lonafarnib mediated inhibition of CYP450 enzyme.	Premature ageing appearance [LD2B]	[22]
Enzalutamide	DMGL19D	Moderate	Increased metabolism of Carisoprodol caused by Enzalutamide mediated induction of CYP450 enzyme.	Prostate cancer [2C82]	[23]
Fentanyl	DM8WAHT	Major	Additive CNS depression effects by the combination of Carisoprodol and Fentanyl.	Sensation disturbance [MB40]	[8]
Sufentanil	DMU7YEL	Major	Additive CNS depression effects by the combination of Carisoprodol and Sufentanil.	Sensation disturbance [MB40]	[8]
Armodafinil	DMGB035	Moderate	Decreased metabolism of Carisoprodol caused by Armodafinil mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[9]
Tizanidine	DMR2IQ4	Moderate	Additive CNS depression effects by the combination of Carisoprodol and Tizanidine.	Tonus and reflex abnormality [MB47]	[24]
-----------


⏷ Show the Full List of 38 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Docusate sodium	E00563	23673837	Surfactant
Sodium benzoate	E00432	517055	Antimicrobial preservative; lubricant
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Stearic acid	E00079	5281	Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Carmellose sodium	E00625	Not Available	Disintegrant
Crospovidone	E00626	Not Available	Disintegrant
Hypromellose	E00634	Not Available	Coating agent
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Potassium sorbate	E00566	23676745	Antimicrobial preservative
Povidone	E00667	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Vinylpyrrolidone	E00668	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
--------------------


⏷ Show the Full List of 15 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Carisoprodol 350 mg tablet	350 mg	Oral Tablet	Oral
Carisoprodol 250 mg tablet	250 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1	Carisoprodol FDA Label
2	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7610).
3	BDDCS predictions, self-correcting aspects of BDDCS assignments, BDDCS assignment corrections, and classification for more than 175 additional drugs
4	Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
5	Lewandowski TA: Pharmacokinetic modeling of carisoprodol and meprobamate disposition in adults. Hum Exp Toxicol. 2017 Aug;36(8):846-853. doi: 10.1177/0960327116672912. Epub 2016 Oct 10.
6	Association between blood carisoprodol:meprobamate concentration ratios and CYP2C19 genotype in carisoprodol-drugged drivers: decreased metabolic capacity in heterozygous CYP2C191/CYP2C192 subjects? Pharmacogenetics. 2003 Jul;13(7):383-8.
7	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
8	US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.".
9	Cerner Multum, Inc. "Australian Product Information.".
10	US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.".
11	Warrington SJ, Ankier SI, Turner P "Evaluation of possible interactions between ethanol and trazodone or amitriptyline." Neuropsychobiology 15 (1986): 31-7. [PMID: 3725002]
12	Product Information. Isturisa (osilodrostat). Recordati Rare Diseases Inc, Lebanon, NJ.
13	Cerner Multum, Inc. "Canadian Product Information.".
14	Product Information. Xcopri (cenobamate). SK Life Science, Inc., Paramus, NJ.
15	Product Information. Alphagan (brimonidine ophthalmic). Allergan Inc, Irvine, CA.
16	Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA.
17	Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
18	Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
19	Product Information. Thalomid (thalidomide). Celgene Corporation, Warren, NJ.
20	Hansen BS, Dam M, Brandt J, et al "Influence of dextropropoxyphene on steady state serum levels and protein binding of three anti-epileptic drugs in man." Acta Neurol Scand 61 (1980): 357-67. [PMID: 6998251]
21	Sekar M, Mimpriss TJ "Buprenorphine, benzodiazepines and prolonged respiratory depression." Anaesthesia 42 (1987): 567-8. [PMID: 3592200]
22	Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
23	Benoist G, van Oort I, et al "Drug-drug interaction potential in men treated with enzalutamide: Mind the gap." Br J Clin Pharmacol 0 (2017): epub. [PMID: 28881501]
24	Product Information. Zanaflex (tizanidine). Acorda Therapeutics, Hawthorne, NY.