Details of the Drug

General Information of Drug (ID: DM65AGJ)

Drug Name

Oxymorphone

Synonyms

Oxymorphone (abuse-resistant, pain); Oxymorphone (abuse-resistant, pain), Pain Therapeutics/ King Pharmaceuticals; Oxymorphone (abuse-resistant, pain), Pain Therapeutics/Pfizer

Indication

Disease Entry	ICD 11	Status	REF
Pain	MG30-MG3Z	Approved	[1]
Chronic pain	MG30	Investigative	[2]
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Therapeutic Class

Neurology Agents

Affected Organisms

Humans and other mammals

ATC Code

N02AA11: Oxymorphone

N02AA: Natural opium alkaloids

N02A: OPIOIDS

N02: ANALGESICS

N: NERVOUS SYSTEM

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

301.34

Logarithm of the Partition Coefficient (xlogp)

0.8

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [3]
Elimination: 1.9% of drug is excreted from urine in the unchanged form [3]
Half-life: The concentration or amount of drug in body reduced by one-half in 1.3 +/- 0.7 hours [4]
Metabolism: The drug is metabolized via the hepatic []
MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.42665 micromolar/kg/day [5]
Water Solubility: The ability of drug to dissolve in water is measured as 24 mg/mL [3]

Chemical Identifiers

Formula: C17H19NO4
IUPAC Name: (4R,4aS,7aR,12bS)-4a,9-dihydroxy-3-methyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one
Canonical SMILES: CN1CC[C@]23[C@@H]4C(=O)CC[C@]2([C@H]1CC5=C3C(=C(C=C5)O)O4)O
InChI: InChI=1S/C17H19NO4/c1-18-7-6-16-13-9-2-3-10(19)14(13)22-15(16)11(20)4-5-17(16,21)12(18)8-9/h2-3,12,15,19,21H,4-8H2,1H3/t12-,15+,16+,17-/m1/s1
InChIKey: UQCNKQCJZOAFTQ-ISWURRPUSA-N

Cross-matching ID

PubChem CID: 5284604
ChEBI ID: CHEBI:7865
CAS Number: 76-41-5
UNII: 9VXA968E0C
DrugBank ID: DB01192
TTD ID: D02NSF
INTEDE ID: DR1226
ACDINA ID: D00503

Repurposed Drugs (RPD)

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Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Opioid receptor (OPR)	TTN4QDT	NOUNIPROTAC	Modulator	[6]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Substrate	[7]
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Substrate	[7]

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Molecular Interaction Atlas (MIA)

MIA Detail

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Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Oxymorphone

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Dezocine	DMJDB0Y	Major	Additive hypotensive effects by the combination of Oxymorphone and Dezocine.	Pain [MG30-MG3Z]	[8]
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Coadministration of a Drug Treating the Disease Different from Oxymorphone (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Oliceridine	DM6MDCF	Major	Additive CNS depression effects by the combination of Oxymorphone and Oliceridine.	Acute pain [MG31]	[9]
Cariprazine	DMJYDVK	Major	Additive CNS depression effects by the combination of Oxymorphone and Cariprazine.	Bipolar disorder [6A60]	[9]
Dihydrocodeine	DMB0FWL	Major	Additive CNS depression effects by the combination of Oxymorphone and Dihydrocodeine.	Chronic pain [MG30]	[10]
Levomilnacipran	DMV26S8	Moderate	Additive CNS depression effects by the combination of Oxymorphone and Levomilnacipran.	Chronic pain [MG30]	[11]
Vilazodone	DM4LECQ	Moderate	Additive serotonergic effects by the combination of Oxymorphone and Vilazodone.	Depression [6A70-6A7Z]	[11]
Vortioxetine	DM6F1PU	Moderate	Additive serotonergic effects by the combination of Oxymorphone and Vortioxetine.	Depression [6A70-6A7Z]	[11]
Milnacipran	DMBFE74	Moderate	Additive CNS depression effects by the combination of Oxymorphone and Milnacipran.	Depression [6A70-6A7Z]	[11]
Desvenlafaxine	DMHD4PE	Moderate	Additive serotonergic effects by the combination of Oxymorphone and Desvenlafaxine.	Depression [6A70-6A7Z]	[11]
OPC-34712	DMHG57U	Major	Additive CNS depression effects by the combination of Oxymorphone and OPC-34712.	Depression [6A70-6A7Z]	[9]
Clomipramine	DMINRKW	Moderate	Additive serotonergic effects by the combination of Oxymorphone and Clomipramine.	Depression [6A70-6A7Z]	[11]
Esketamine	DMVU687	Moderate	Additive CNS depression effects by the combination of Oxymorphone and Esketamine.	Depression [6A70-6A7Z]	[12]
Mepenzolate	DM8YU2F	Moderate	Additive CNS depression effects by the combination of Oxymorphone and Mepenzolate.	Digestive system disease [DE2Z]	[13]
5-hydroxy-L-tryptophan	DMDWZGJ	Moderate	Additive serotonergic effects by the combination of Oxymorphone and 5-hydroxy-L-tryptophan.	Discovery agent [N.A.]	[11]
Heroin diacetylmorphine	DMDBWHY	Major	Additive CNS depression effects by the combination of Oxymorphone and Heroin diacetylmorphine.	Dissociative neurological symptom disorder [6B60]	[10]
Dantrolene	DM1D8XY	Major	Additive CNS depression effects by the combination of Oxymorphone and Dantrolene.	Fever [MG26]	[9]
Solifenacin	DMG592Q	Moderate	Additive CNS depression effects by the combination of Oxymorphone and Solifenacin.	Functional bladder disorder [GC50]	[13]
Belladonna	DM2RBWK	Moderate	Additive antimotility effects by the combination of Oxymorphone and Belladonna.	Infectious gastroenteritis/colitis [1A40]	[13]
Suvorexant	DM0E6S3	Major	Additive CNS depression effects by the combination of Oxymorphone and Suvorexant.	Insomnia [7A00-7A0Z]	[9]
Amobarbital	DM0GQ8N	Major	Additive CNS depression effects by the combination of Oxymorphone and Amobarbital.	Insomnia [7A00-7A0Z]	[9]
Tasimelteon	DMLOQ1V	Major	Additive CNS depression effects by the combination of Oxymorphone and Tasimelteon.	Insomnia [7A00-7A0Z]	[9]
Paraldehyde	DMOC1BX	Major	Additive CNS depression effects by the combination of Oxymorphone and Paraldehyde.	Insomnia [7A00-7A0Z]	[9]
ITI-007	DMUQ1DO	Major	Additive CNS depression effects by the combination of Oxymorphone and ITI-007.	Insomnia [7A00-7A0Z]	[9]
Quazepam	DMY4D87	Major	Additive CNS depression effects by the combination of Oxymorphone and Quazepam.	Insomnia [7A00-7A0Z]	[9]
Estazolam	DMZGXUM	Major	Additive CNS depression effects by the combination of Oxymorphone and Estazolam.	Insomnia [7A00-7A0Z]	[9]
Polyethylene glycol	DM4I1JP	Moderate	Increased risk of lowers seizure threshold by the combination of Oxymorphone and Polyethylene glycol.	Irritable bowel syndrome [DD91]	[14]
Remimazolam	DMLVSYX	Major	Additive CNS depression effects by the combination of Oxymorphone and Remimazolam.	Labour/delivery anaesthesia complication [JB0C]	[9]
Allopregnanolone	DMNLHAC	Moderate	Additive CNS depression effects by the combination of Oxymorphone and Allopregnanolone.	Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z]	[15]
Lasmiditan	DMXLVDT	Moderate	Additive CNS depression effects by the combination of Oxymorphone and Lasmiditan.	Migraine [8A80]	[16]
Flibanserin	DM70DTN	Moderate	Additive CNS depression effects by the combination of Oxymorphone and Flibanserin.	Mood disorder [6A60-6E23]	[17]
Prasugrel	DM7MT6E	Moderate	Altered absorption of Oxymorphone due to GI dynamics variation caused by Prasugrel.	Myocardial infarction [BA41-BA43]	[18]
Levomethadyl Acetate	DM06HG5	Major	Additive CNS depression effects by the combination of Oxymorphone and Levomethadyl Acetate.	Opioid use disorder [6C43]	[10]
Pimavanserin	DMR7IVC	Major	Additive CNS depression effects by the combination of Oxymorphone and Pimavanserin.	Parkinsonism [8A00]	[9]
Methylscopolamine	DM5VWOB	Moderate	Additive antimotility effects by the combination of Oxymorphone and Methylscopolamine.	Peptic ulcer [DA61]	[13]
Quetiapine	DM1N62C	Major	Additive CNS depression effects by the combination of Oxymorphone and Quetiapine.	Schizophrenia [6A20]	[19]
Aripiprazole	DM3NUMH	Major	Additive CNS depression effects by the combination of Oxymorphone and Aripiprazole.	Schizophrenia [6A20]	[9]
Iloperidone	DM6AUFY	Major	Additive CNS depression effects by the combination of Oxymorphone and Iloperidone.	Schizophrenia [6A20]	[9]
Paliperidone	DM7NPJS	Major	Additive CNS depression effects by the combination of Oxymorphone and Paliperidone.	Schizophrenia [6A20]	[9]
Molindone	DMAH70G	Major	Additive CNS depression effects by the combination of Oxymorphone and Molindone.	Schizophrenia [6A20]	[9]
Thiothixene	DMDINC4	Major	Additive CNS depression effects by the combination of Oxymorphone and Thiothixene.	Schizophrenia [6A20]	[19]
Asenapine	DMSQZE2	Major	Additive CNS depression effects by the combination of Oxymorphone and Asenapine.	Schizophrenia [6A20]	[9]
Brilinta	DMBR01X	Moderate	Altered absorption of Oxymorphone due to GI dynamics variation caused by Brilinta.	Thrombosis [DB61-GB90]	[18]
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Allura red AC dye	E00338	33258	Colorant
Alpha-tocopherol	E00243	14985	Antimicrobial preservative; Antioxidant
D&C red no. 27	E00381	83511	Colorant
D&C red no. 30	E00456	3000709	Colorant
FD&C blue no. 1	E00263	19700	Colorant
FD&C blue no. 2	E00446	2723854	Colorant
methylparaben	E00149	7456	Antimicrobial preservative
Quinoline yellow WS	E00309	24671	Colorant
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sodium stearyl fumarate	E00545	23665634	lubricant
Sunset yellow FCF	E00255	17730	Colorant
Citric acid monohydrate	E00271	22230	Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
Eisenoxyd	E00585	56841934	Colorant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Ferrosoferric oxide	E00231	14789	Colorant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Polysorbate 80	E00665	Not Available	Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Polyvinyl alcohol	E00666	Not Available	Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Propylene glycol	E00040	1030	Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Triacetin	E00080	5541	Humectant; Plasticizing agent; Solvent
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⏷ Show the Full List of 24 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Oxymorphone 20 mg tablet	20 mg	12 HR Extended Release Oral Tablet	Oral
Oxymorphone 40 mg tablet	40 mg	12 HR Extended Release Oral Tablet	Oral
Oxymorphone 10 mg tablet	10 mg	12 HR Extended Release Oral Tablet	Oral
Oxymorphone 5 mg tablet	5 mg	12 HR Extended Release Oral Tablet	Oral
Oxymorphone 7.5 mg tablet	7.5 mg	12 HR Extended Release Oral Tablet	Oral
Oxymorphone 30 mg tablet	30 mg	12 HR Extended Release Oral Tablet	Oral
Oxymorphone 15 mg tablet	15 mg	12 HR Extended Release Oral Tablet	Oral
Oxymorphone 10 mg tablet	10 mg	Oral Tablet	Oral
Oxymorphone 5 mg tablet	5 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2	Oxymorphone FDA Label
3	BDDCS applied to over 900 drugs
4	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
5	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
6	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: 7094).
7	Exposure to oral oxycodone is increased by concomitant inhibition of CYP2D6 and 3A4 pathways, but not by inhibition of CYP2D6 alone. Br J Clin Pharmacol. 2010 Jul;70(1):78-87.
8	Product Information. Buprenex (buprenorphine). Reckitt and Colman Pharmaceutical, Richmond, VA.
9	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.".
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	Vizcaychipi MP, Walker S, Palazzo M "Serotonin syndrome triggered by tramadol." Br J Anaesth 99 (2007): 919. [PMID: 18006535]
12	Cerner Multum, Inc. "Australian Product Information.".
13	Product Information. Apadaz (acetaminophen-benzhydrocodone). KemPharm, Inc, Coralville, IA.
14	Product Information. Suprep Bowel Prep Kit (magnesium/potassium/sodium sulfates). Braintree Laboratories, Braintree, MA.
15	Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA.
16	Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
17	Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
18	Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".
19	Cerner Multum, Inc. "Canadian Product Information.".