Naltrexone

Opioid Antagonist — ALIMENTARY TRACT AND METABOLISM

Key facts

Naltrexone is an ofp drug in the Opioid Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 1984. Its mechanism of action is classified as Opioid Antagonists. DrugCentral lists 16 molecular targets, including OPRM1, Oprm1 and OPRK1. Recorded indications include Alcoholism, Chronic pain, Chronic Pain with Opioid Tolerance and Obesity.

• Approval status: ofp (first approved 1984 by the FDA).
• Drug class: Opioid Antagonist.
• Mechanism of action: Opioid Antagonists.
• Molecular targets: OPRM1, Oprm1, OPRK1 and OPRM1 (16 listed in DrugCentral).
• Indications: Alcoholism, Chronic pain, Chronic Pain with Opioid Tolerance, Obesity and Prevention of opioid abuse and others.
• ATC code: A08AA62 (Centrally acting antiobesity products).
• Molecular formula: C20H23NO4; molecular weight 341.41 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (8)

• Alcoholism
• Chronic pain
• Chronic Pain with Opioid Tolerance
• Obesity
• Prevention of opioid abuse
• Severe pain
• Severe Pain with Opioid Tolerance
• Therapeutic opioid induced constipation

Off-label uses (1)

• Neuropathic pain

Contraindications (45)

• Acute exacerbation of asthma
• Acute hepatic failure
• Acute hepatitis
• Acute nephropathy
• Acute pancreatitis
• Alcohol intoxication
• Alcohol withdrawal delirium
• Benign intracranial hypertension
• Benign prostatic hyperplasia
• Central nervous system depression
• Chronic diarrhea
• Chronic disease of respiratory system
• Chronic obstructive lung disease
• Cor pulmonale
• Decreased respiratory function
• Depressive disorder
• Disease of liver
• Disorder of biliary tract
• Disorder of gallbladder
• Drug-induced psychosis
• Eosinophilic asthma
• Gastrointestinal obstruction
• Gastrointestinal perforation
• Gastrointestinal ulcer
• Hepatic failure
• Hypercapnia
• Hypothyroidism
• Impaired renal function disorder
• Increased Creatine Phosphokinase
• Injury of head
• + 15 more

Mechanism & targets

• Mechanism of action (MoA): Opioid Antagonists
• Established pharmacologic class: Opioid Antagonist

Molecular targets (16)

Target	Gene	Action	Activity
Mu-type opioid receptor	OPRM1	unknown	Ki 9.77
Mu-type opioid receptor	Oprm1	unknown	Ki 9.58
Kappa-type opioid receptor	OPRK1	unknown	Ki 9.51
Mu-type opioid receptor	OPRM1	antagonist	Ki 9.38
Mu-type opioid receptor	Oprm1	unknown	Ki 9.34
Opioid receptor	Oprd1|Oprm1|Oprk1|Sigmar1	unknown	Ki 9.26
Opioid receptors; mu and delta	Oprd1|Oprm1	unknown	Ki 9.06
Kappa-type opioid receptor	Oprk1	unknown	Ki 8.97
Kappa-type opioid receptor	OPRK1	antagonist	Ki 8.93
Kappa-type opioid receptor	Oprk1	unknown	Ki 8.84
Delta-type opioid receptor	Oprd1	unknown	Ki 8.32
Delta-type opioid receptor	OPRD1	antagonist	Ki 7.99
Delta-type opioid receptor	Oprd1	unknown	Ki 7.91
Cytochrome P450 2D6	CYP2D6	unknown	IC50 6.00
Neuronal acetylcholine receptor subunit alpha-7	CHRNA7	unknown	IC50 4.60
Neuronal acetylcholine receptor subunit alpha-4	Chrna4	unknown	IC50 4.51

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1984-11-20	FDA	—	TEVA WOMENS	Yes

ATC classification

ATC code	Therapeutic hierarchy
A08AA62	ALIMENTARY TRACT AND METABOLISM › ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS › ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS › Centrally acting antiobesity products
N02AA56	NERVOUS SYSTEM › ANALGESICS › OPIOIDS › Natural opium alkaloids
N07BB04	NERVOUS SYSTEM › OTHER NERVOUS SYSTEM DRUGS › DRUGS USED IN ADDICTIVE DISORDERS › Drugs used in alcohol dependence

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Injection site reaction	8630.2
Injection site mass	4700.8
Injection site pain	4488.0
Injection site induration	1902.2
Needle issue	1407.2
Product administered at inappropriate site	1165.7
Feeling abnormal	1027.6
Therapeutic response shortened	936.7
Injection site swelling	735.4
Alcohol use	720.7
Withdrawal syndrome	670.5
Injection site abscess	506.9

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Naltrexone is on its molecule page.

• Molecular formula: C₂₀H₂₃NO₄
• Molecular weight: 341.41 g/mol
• CAS number: 16590-41-3
• InChIKey: DQCKKXVULJGBQN-XFWGSAIBSA-N
• PubChem CID: 5360515

OC1=C2O[C@H]3C(=O)CC[C@@]4(O)[C@H]5CC(C=C1)=C2[C@@]34CCN5CC1CC1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Naltrexone used for?

DrugCentral lists the following indications for Naltrexone: Alcoholism, Chronic pain, Chronic Pain with Opioid Tolerance, Obesity, Prevention of opioid abuse, Severe pain, Severe Pain with Opioid Tolerance and Therapeutic opioid induced constipation.

How does Naltrexone work?

Naltrexone is classified as Opioid Antagonists; its molecular targets in DrugCentral include OPRM1, Oprm1, OPRK1 and OPRM1 (antagonist).

When was Naltrexone first approved?

Naltrexone was first approved by the FDA in 1984.

What drug class does Naltrexone belong to?

Naltrexone is in the Opioid Antagonist class.

What is the chemical formula of Naltrexone?

Naltrexone has the molecular formula C20H23NO4 and a molecular weight of 341.41 g/mol.

Sources

• DrugCentral drug card 1765 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1201149 — compound record and bioactivity
• PubChem CID 5360515 — chemical identifiers
• DrugBank DB00704 — drug record
• FDA UNII 5S6W795CQM — substance identity
• DailyMed: FDA labels for Naltrexone — current prescribing information (label search)
• UniProt P35372 (OPRM1) — target protein
• UniProt P41145 (OPRK1) — target protein
• UniProt P41143 (OPRD1) — target protein
• UniProt P10635 (CYP2D6) — target protein
• UniProt P36544 (CHRNA7) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.