General Information of Drug (ID: DMUDJZM)

Drug Name
Dextromethorphan Drug Info
Synonyms
Albutussin; Canfodion; Cosylan; Demorphine; Destrometerfano; Dextromethorfan; Dextromethorphane; Dextromethorphanum; Dextrometorfano; Dextrometorphan; Dextromorphan; Dexyromethorphan; Dormetan; Levomethorphan; Levomethorphane; Levomethorphanum; Levometorfano; Methorphan; RACEMETHORPHAN; Trocal; Balminil DM; Balminil DM Children; Benylin Adult Formula Cough Suppressant; Benylin DM for Children; Benylin Pediatric Cough Suppressant; Delsym Cough Formula; Demorphan hydrobromide; Destrometerfano [DCIT]; Dextromethorfan [Czech]; Dextromethorphan Bromhydrate; Hold DM; Koffex DM; Novahistex DM; Novahistine DM; Pertussin DM Extra Strength; Robitussin Maximum Strength Cough Suppressant; Robitussin Pediatric; Robitussin Pediatric Cough Suppressant; Triaminic DM Long Lasting for Children; BA 2666; Benylin DM 12 Hour; Benylin DM for Children 12 Hour; Sucrets 4 Hour Cough Suppressant; Vicks 44 Cough Relief; Calmylin #1; Cough-X; Creo-Terpin; D-Methorphan; Delta-Methorphan; Dextromethorphan (USP); Dextromethorphane [INN-French]; Dextromethorphanum [INN-Latin]; Dextrometorfano [INN-Spanish]; Diabe-Tuss DM Syrup; Hihustan M.; L-Methorphan; Levomethorphane [INN-French]; Levomethorphanum [INN-Latin]; Levometorfano [INN-Spanish]; Neurodex (TN); Pertussin CS Children's Strength; Romilar (TN); Dextromethorphan [USP:INN:BAN]; Levomethorphan [BAN:DCF:INN]; Levomethorphan [INN:BAN:DCF]; Morphinan, 3-methoxy-17-methyl-, (9-alpha,13-alpha,14-alpha)-(9CI); Cis-1,3,4,9,10,10a-Hexahydro-6-methoxy-11-methyl-2H-10,4alpha-iminoethanophenanthren; (+)-3-Methoxy-17-methylmorphinan; (-)-3-Methoxy-N-methylmorphinan; (9alpha,13alpha,14alpha)-17-methyl-3-(methyloxy)morphinan; 3-Methoxy-17-methyl-9alpha,13alpha,14alpha-morphinan; 3-Methoxy-17-methylmorphinan; 3-Methoxy-N-methylmorphinon; 9alpha,13alpha,14alpha-Morphinan, 3-methoxy-17-methyl-(8CI)
Indication
Disease Entry ICD 11 Status REF
Allergic rhinitis CA08.0 Approved [1]
Common cold CA00 Approved [1]
Cough MD12 Approved [2]
Fever MG26 Approved [1]
Headache 8A80-8A84 Approved [1]
Rhinitis FA20 Approved [1]
Vasomotor/allergic rhinitis CA08 Approved [1]
Therapeutic Class
Analgesics
Cross-matching ID
PubChem CID
5360696
ChEBI ID
CHEBI:4470
CAS Number
CAS 125-71-3
TTD Drug ID
DMUDJZM
VARIDT Drug ID
DR00891
INTEDE Drug ID
DR0476
ACDINA Drug ID
D00177

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Opioid receptor sigma 1 (OPRS1) TT5TPI6 SGMR1_HUMAN Agonist [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [4]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Approved [5]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Approved [6]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Approved [6]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Approved [7]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Approved [8]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Approved [9]
Cholesterol 24-hydroxylase (CYP46A1) DEKP5HX CP46A_HUMAN Approved [10]
Cytochrome P450 102A1 (cyp102) DE4OGUF CPXB_BACMB Approved [11]
Cytochrome P450 130A1 (cyp130) DE6CQ0I CP130_MYCTU Approved [12]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Opioid receptor sigma 1 (OPRS1) DTT SIGMAR1 7.092 5.716 5.411 6.434
Cholesterol 24-hydroxylase (CYP46A1) DME CYP46A1 5.361 4.062 4.087 5.966
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 7.867 5.142 5.52 7.08
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 3.307 5.005 3.921 5.327
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 11.76 5.931 6.164 9.423
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Allergic rhinitis
ICD Disease Classification CA08.0
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Opioid receptor sigma 1 (OPRS1) DTT SIGMAR1 2.77E-06 -0.12 -0.62
Cytochrome P450 2B6 (CYP2B6) DME CYP2B6 4.88E-01 -1.69E-05 -1.28E-04
Cholesterol 24-hydroxylase (CYP46A1) DME CYP46A1 1.79E-06 -3.32E-01 -6.53E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 9.96E-01 -3.17E-03 -1.84E-02
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 2.40E-01 -3.31E-02 -1.97E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 7.30E-01 -1.91E-02 -1.41E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 1.90E-01 -9.81E-03 -5.96E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.04E-02 6.29E-02 3.54E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Dextromethorphan 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: 6953).
3 Dextromethorphan/quinidine: AVP 923, dextromethorphan/cytochrome P450-2D6 inhibitor, quinidine/dextromethorphan. Drugs R D. 2005;6(3):174-7.
4 Comparative contribution to dextromethorphan metabolism by cytochrome P450 isoforms in vitro: can dextromethorphan be used as a dual probe for both CTP2D6 and CYP3A activities? Drug Metab Dispos. 2001 Nov;29(11):1514-20.
5 Polymorphism of human cytochrome P450 2D6 and its clinical significance: Part I. Clin Pharmacokinet. 2009;48(11):689-723.
6 Multiple human cytochromes contribute to biotransformation of dextromethorphan in-vitro: role of CYP2C9, CYP2C19, CYP2D6, and CYP3A. J Pharm Pharmacol. 1998 Sep;50(9):997-1004.
7 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
8 Enzymes in addition to CYP3A4 and 3A5 mediate N-demethylation of dextromethorphan in human liver microsomes. Biopharm Drug Dispos. 1999 Oct;20(7):341-6.
9 Characterization of dextromethorphan N-demethylation by human liver microsomes. Contribution of the cytochrome P450 3A (CYP3A) subfamily. Biochem Pharmacol. 1994 Jul 5;48(1):173-82.
10 Broad substrate specificity of human cytochrome P450 46A1 which initiates cholesterol degradation in the brain. Biochemistry. 2003 Dec 9;42(48):14284-92.
11 The bacterial P450 BM3: a prototype for a biocatalyst with human P450 activities. Trends Biotechnol. 2007 Jul;25(7):289-98.
12 Function, essentiality, and expression of cytochrome P450 enzymes and their cognate redox partners in Mycobacterium tuberculosis: are they drug targets? Appl Microbiol Biotechnol. 2019 May;103(9):3597-3614.