Tapentadol

Opioid Agonist — NERVOUS SYSTEM

Key facts

Tapentadol is an ofp drug in the Opioid Agonist class catalogued in DrugCentral. It was first approved by the FDA in 2008. Its mechanism of action is classified as Opioid Agonists. DrugCentral lists 3 molecular targets, including OPRM1, SLC6A2 and SLC22A1. Recorded indications include Pain.

• Approval status: ofp (first approved 2008 by the FDA).
• Drug class: Opioid Agonist.
• Mechanism of action: Opioid Agonists.
• Molecular targets: OPRM1, SLC6A2 and SLC22A1 (3 listed in DrugCentral).
• Indications: Pain.
• ATC code: N02AX06 (Other opioids).
• Molecular formula: C14H23NO; molecular weight 221.34 g/mol.

Indications & contraindications

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

Indications (1)

• Pain

Contraindications (24)

• Acute exacerbation of asthma
• Alcohol intoxication
• Asthenia
• Benign intracranial hypertension
• Central nervous system depression
• Chronic obstructive lung disease
• Coma
• Cor pulmonale
• Decreased respiratory function
• Disease of liver
• Disorder of biliary tract
• Exacerbation of asthma
• Hypercapnia
• Hypoxia
• Injury of head
• Kyphoscoliosis with Respiratory Compromise
• Lesion of brain
• Morbid obesity
• Myxedema
• Pancreatitis
• Paralytic ileus
• Seizure disorder
• Sleep apnea
• Substance abuse

Mechanism & targets

• Mechanism of action (MoA): Opioid Agonists
• Established pharmacologic class: Opioid Agonist

Molecular targets (3)

Target	Gene	Action	Activity
Mu-type opioid receptor	OPRM1	agonist	Ki 7.02
Sodium-dependent noradrenaline transporter	SLC6A2	inhibitor	Ki 6.32
Solute carrier family 22 member 1	SLC22A1	unknown	IC50 4.66

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2008-11-20	FDA	—	JANSSEN PHARMS

ATC classification

ATC code	Therapeutic hierarchy
N02AX06	NERVOUS SYSTEM › ANALGESICS › OPIOIDS › Other opioids

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
Serotonin syndrome	404.0
Toxicity to various agents	313.3
Drug abuse	278.0
Delirium	249.8
Product packaging quantity issue	200.5
Drug interaction	192.1
Sopor	190.4
Somnolence	152.3
Drug dose titration not performed	150.4
Respiratory depression	143.3
Constipation	134.2
Overdose	119.7

Chemical structure

• Molecular formula: C₁₄H₂₃NO
• Molecular weight: 221.34 g/mol
• CAS number: 175591-09-0
• InChIKey: KWTWDQCKEHXFFR-SMDDNHRTSA-N
• PubChem CID: 9838022

CC[C@H]([C@@H](C)CN(C)C)C1=CC(O)=CC=C1

Frequently asked questions

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

What is Tapentadol used for?

DrugCentral lists the following indications for Tapentadol: Pain.

How does Tapentadol work?

Tapentadol is classified as Opioid Agonists; its molecular targets in DrugCentral include OPRM1 (agonist), SLC6A2 (inhibitor) and SLC22A1.

When was Tapentadol first approved?

Tapentadol was first approved by the FDA in 2008.

What drug class does Tapentadol belong to?

Tapentadol is in the Opioid Agonist class.

What is the chemical formula of Tapentadol?

Tapentadol has the molecular formula C14H23NO and a molecular weight of 221.34 g/mol.

Sources

• DrugCentral drug card 4283 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1201776 — compound record and bioactivity
• PubChem CID 9838022 — chemical identifiers
• DrugBank DB06204 — drug record
• FDA UNII H8A007M585 — substance identity
• DailyMed: FDA labels for Tapentadol — current prescribing information (label search)
• UniProt P35372 (OPRM1) — target protein
• UniProt P23975 (SLC6A2) — target protein
• UniProt O15245 (SLC22A1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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