General Information of Drug (ID: DMOSQGU)

Drug Name
Nalbuphine Drug Info
Synonyms
Intapan; Nalbufina; Nalbuphinum; Intapan (TN); Nalbuphine (INN); Nubain (TN); (5alpha,6alpha)-17-(cyclobutylmethyl)-4,5-epoxymorphinan-3,6,14-triol; 17-cyclobutylmethyl-4,5alpha-epoxymorphinan-3,6alpha,14-triol
Indication
Disease Entry ICD 11 Status REF
Pain MG30-MG3Z Approved [1]
Prurigo nodularis EC91.0 Phase 2/3 [2]
Uremic pruritus EC90.10 Phase 2/3 [2]
Therapeutic Class
Analgesics
Cross-matching ID
PubChem CID
5311304
ChEBI ID
CHEBI:7454
CAS Number
CAS 20594-83-6
TTD Drug ID
DMOSQGU
VARIDT Drug ID
DR01344

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Nalfurafine hcl DMA9DHW Uremic pruritus EC90.10 Approved [6]
CHLOROXINE DMFZBMQ Erythema ME64.0 Approved [7]
Difelikefalin DMHZBEO Pruritus EC90 Approved [2]
Dezocine DMJDB0Y Pain MG30-MG3Z Approved [8]
Asimadoline DMND3AB Diarrhea-predominant irritable bowel syndrome DD91.01 Phase 3 [9]
JNJ 67953964 DMJ8Y5N Major depressive disorder 6A70.3 Phase 3 [10]
PHN-131 DM1SV8I Pain MG30-MG3Z Phase 2/3 [11]
CR-845 DMJYTUQ Pain MG30-MG3Z Phase 2/3 [12]
Carfentanil DM7ADGX N. A. N. A. Phase 2 [13]
Apadoline DM1B8IT Pain MG30-MG3Z Phase 2 [14]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [15]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [16]
Methotrexate DM2TEOL Anterior urethra cancer Approved [17]
Folic Acid DMEMBJC Colorectal carcinoma Approved [18]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [17]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [17]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [19]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [17]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [20]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [21]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Prolactin (PRL)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Verapamil DMA7PEW Angina pectoris BA40 Approved [22]
Ranitidine DM0GUSX Gastric ulcer DA60 Approved [23]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [24]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [25]
Methotrexate DM2TEOL Anterior urethra cancer Approved [26]
Thioridazine DM35M8J Schizophrenia 6A20 Approved [27]
Naloxone DM3FXMA Narcotic depression 6A7Z Approved [28]
Aripiprazole DM3NUMH Bipolar I disorder Approved [29]
Fluoxetine DM3PD2C Bipolar depression Approved [30]
Penicillamine DM40EF6 Cystinuria 5C60.2 Approved [31]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Opioid receptor kappa (OPRK1) TTQW87Y OPRK_HUMAN Modulator [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [4]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Prolactin (PRL) OTWFQGX7 PRL_HUMAN Gene/Protein Processing [5]

References

1 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: 1663).
2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
4 Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37.
5 Effects of nalbuphine on anterior pituitary and adrenal hormones and subjective responses in male cocaine abusers. Pharmacol Biochem Behav. 2007 Apr;86(4):667-77. doi: 10.1016/j.pbb.2007.02.012. Epub 2007 Feb 20.
6 Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology. Bioorg Med Chem Lett. 2010 Jan 1;20(1):121-4.
7 In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
8 Pharmacological profiles of opioid ligands at kappa opioid receptors. BMC Pharmacol. 2006 Jan 25;6:3.
9 Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
10 Kappa Opioid Receptor Antagonists as Potential Therapeutics for Mood and Substance Use Disorders. Handb Exp Pharmacol. 2022;271:473-491.
11 Nalbuphine: an autoradiographic opioid receptor binding profile in the central nervous system of an agonist/antagonist analgesic. J Pharmacol Exp Ther. 1988 Jan;244(1):391-402.
12 Peptide Kappa Opioid Receptor Ligands: Potential for Drug Development. AAPS J. 2009 June; 11(2): 312-322.
13 Wax PM, Becker CE, Curry SC: Unexpected gas casualties in Moscow: a medical toxicology perspective. Ann Emerg Med. 2003 May;41(5):700-5.
14 Novel developments with selective, non-peptidic kappa-opioid receptor agonists. Expert Opin Investig Drugs. 1997 Oct;6(10):1351-68.
15 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
16 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
17 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
18 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
19 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
20 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
21 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
22 Verapamil-induced hyperprolactinemia complicated by a pituitary incidentaloma. Ann Pharmacother. 1995 Oct;29(10):999-1001. doi: 10.1177/106002809502901009.
23 [Impotence and gynecomastia secondary to hyperprolactinemia induced by ranitidine]. Therapie. 1994 Jul-Aug;49(4):361-2.
24 Differential effects of estrogen receptor antagonists on pituitary lactotroph proliferation and prolactin release. Mol Cell Endocrinol. 2005 Jul 15;239(1-2):27-36. doi: 10.1016/j.mce.2005.04.008.
25 Cholinergic modulation of the cerebral metabolic response to citalopram in Alzheimer's disease. Brain. 2009 Feb;132(Pt 2):392-401. doi: 10.1093/brain/awn326. Epub 2009 Jan 19.
26 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
27 The effect of thioridazine on prolactinoma growth in a schizophrenic man: case report. Gen Hosp Psychiatry. 1985 Oct;7(4):364-6. doi: 10.1016/0163-8343(85)90053-2.
28 Influence of naloxone on muscle sympathetic nerve activity, systemic and calf haemodynamics and ambulatory blood pressure after exercise in mild essential hypertension. J Hypertens. 1995 Apr;13(4):447-61.
29 The efficacy, safety, and tolerability of aripiprazole for the treatment of schizoaffective disorder: results from a pooled analysis of a sub-population of subjects from two randomized, double-blind, placebo-controlled, pivotal trials. J Affect Disord. 2009 May;115(1-2):18-26. doi: 10.1016/j.jad.2008.12.017. Epub 2009 Feb 23.
30 Serum prolactin levels among outpatients with major depressive disorder during the acute phase of treatment with fluoxetine. J Clin Psychiatry. 2006 Jun;67(6):952-7. doi: 10.4088/jcp.v67n0612.
31 Massive breast enlargement in a patient receiving D-penicillamine for systemic sclerosis. J Rheumatol. 1985 Oct;12(5):990-1.