General Information of Drug (ID: DMRQD04)

Drug Name
Tramadol Drug Info
Synonyms Conzip; Ryzolt; Tramadol Hydrochloride; Ultram Er; Rybix Odt; Ultram
Indication
Disease Entry ICD 11 Status REF
Osteoarthritis FA00-FA05 Approved [1]
Pain MG30-MG3Z Approved [2]
Chronic pain MG30 Investigative [1]
Premature ejaculation HA03.0Z Investigative [1]
Therapeutic Class
Analgesics
Cross-matching ID
PubChem CID
33741
ChEBI ID
CHEBI:75725
CAS Number
CAS 123154-38-1
TTD Drug ID
DMRQD04
VARIDT Drug ID
DR00088
INTEDE Drug ID
DR1627
ACDINA Drug ID
D00693

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 2C receptor (HTR2C) TTWJBZ5 5HT2C_HUMAN Modulator [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [5]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Approved [5]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Approved [6]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Approved [5]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
5-HT 2C receptor (HTR2C) DTT HTR2C 4.233 3.329 3.843 3.888
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 3.307 5.005 3.921 5.327
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 Osteoarthritis
ICD Disease Classification FA00-FA05
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
5-HT 2C receptor (HTR2C) DTT HTR2C 1.02E-02 -0.45 -0.37
5-HT 2C receptor (HTR2C) DTT HTR2C 2.27E-01 0.27 0.6
P-glycoprotein 1 (ABCB1) DTP P-GP 1.19E-01 -1.32E-01 -2.77E-01
P-glycoprotein 1 (ABCB1) DTP P-GP 1.65E-01 -1.47E-01 -4.48E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 8.03E-01 9.92E-03 4.89E-02
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 1.42E-01 -4.97E-02 -3.73E-01
Cytochrome P450 2B6 (CYP2B6) DME CYP2B6 9.90E-01 3.10E-03 1.75E-02
Cytochrome P450 2B6 (CYP2B6) DME CYP2B6 5.35E-01 1.10E-02 1.19E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 2.59E-01 6.29E-02 3.14E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 4.84E-01 -8.38E-02 -8.46E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 4.66E-01 4.25E-02 1.20E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 4.75E-01 5.15E-02 3.64E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Tramadol 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: 8286).
3 The inhibitory effects of tramadol on 5-hydroxytryptamine type 2C receptors expressed in Xenopus oocytes. Anesth Analg. 2004 May;98(5):1401-6, table of contents.
4 Tramadol hydrochloride: pharmacokinetics, pharmacodynamics, adverse side effects, co-administration of drugs and new drug delivery systems. Biomed Pharmacother. 2015 Mar;70:234-8.
5 Clinical pharmacology of tramadol. Clin Pharmacokinet. 2004;43(13):879-923.
6 Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8.