Pentazocine

Partial Opioid Agonist/Antagonist — NERVOUS SYSTEM

Key facts

Pentazocine is an ofp drug in the Partial Opioid Agonist/Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 1967. Its mechanism of action is classified as Competitive Opioid Antagonists and Partial Opioid Agonists. DrugCentral lists 11 molecular targets, including SIGMAR1, OPRK1 and OPRM1. Recorded indications include General anesthesia, Labor pain, Local anesthesia and Pain.

• Approval status: ofp (first approved 1967 by the FDA).
• Drug class: Partial Opioid Agonist/Antagonist.
• Mechanism of action: Competitive Opioid Antagonists; Partial Opioid Agonists.
• Molecular targets: SIGMAR1, OPRK1, OPRM1 and SIGMAR1 (11 listed in DrugCentral).
• Indications: General anesthesia, Labor pain, Local anesthesia and Pain.
• ATC code: N02AD01 (Benzomorphan derivatives).
• Molecular formula: C19H27NO; molecular weight 285.43 g/mol.

Indications & contraindications

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

Indications (4)

• General anesthesia
• Labor pain
• Local anesthesia
• Pain

Contraindications (64)

• Acute abdominal pain
• Acute erosive gastritis
• Acute nephropathy
• Alcohol intoxication
• Alcohol withdrawal delirium
• Alcoholism
• Anemia
• Anemia due to enzyme deficiency
• Asthenia
• Benign intracranial hypertension
• Benign prostatic hyperplasia
• Bradycardia
• Breastfeeding (mother)
• Central nervous system depression
• Coma
• Conduction disorder of the heart
• Constipation
• Cor pulmonale
• Decreased respiratory function
• Dehydration
• Dependent drug abuse
• Disease of liver
• Disorder of gallbladder
• Drug-induced psychosis
• Dysfunction of sphincter of Oddi
• Exacerbation of asthma
• Factor II deficiency
• Gastrointestinal hemorrhage
• Gastrointestinal ulcer
• Gout
• + 34 more

Mechanism & targets

• Mechanism of action (MoA): Competitive Opioid Antagonists; Partial Opioid Agonists
• Established pharmacologic class: Partial Opioid Agonist/Antagonist

Molecular targets (11)

Target	Gene	Action	Activity
Sigma non-opioid intracellular receptor 1	SIGMAR1	modulator	EC50 8.76
Kappa-type opioid receptor	OPRK1	unknown	Ki 8.66
Mu-type opioid receptor	OPRM1	unknown	Ki 8.41
Sigma non-opioid intracellular receptor 1	SIGMAR1	unknown	Ki 8.27
Mu-type opioid receptor	Oprm1	unknown	Ki 8.16
Sigma non-opioid intracellular receptor 1	Sigmar1	unknown	Ki 7.92
Opioid receptor	Oprd1|Oprm1|Oprk1|Sigmar1	unknown	IC50 7.90
Delta-type opioid receptor	OPRD1	unknown	EC50 7.31
Kappa-type opioid receptor	OPRK1	unknown	Ki 7.12
Transmembrane protein 97	TMEM97	unknown	Ki 5.83
Sigma intracellular receptor 2	Tmem97	unknown	Ki 5.83

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1967-07-24	FDA	—	HOSPIRA

ATC classification

ATC code	Therapeutic hierarchy
N02AD01	NERVOUS SYSTEM › ANALGESICS › OPIOIDS › Benzomorphan derivatives
N02AD51	NERVOUS SYSTEM › ANALGESICS › OPIOIDS › Benzomorphan derivatives

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
Amaurosis fugax	703.6
Haemorrhagic stroke	627.1
Ocular discomfort	624.0
Head discomfort	545.9
Urinary tract disorder	538.7
Blindness	458.3
Altered state of consciousness	448.3
Generalised oedema	448.1
Eye pain	429.7
Haematemesis	426.7
Diplopia	376.8
Ascites	363.6

Chemical structure

• Molecular formula: C₁₉H₂₇NO
• Molecular weight: 285.43 g/mol
• CAS number: 359-83-1
• InChIKey: VOKSWYLNZZRQPF-UHFFFAOYSA-N
• PubChem CID: 441278

CC1C2CC3=CC=C(O)C=C3C1(C)CCN2CC=C(C)C

Frequently asked questions

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

What is Pentazocine used for?

DrugCentral lists the following indications for Pentazocine: General anesthesia, Labor pain, Local anesthesia and Pain.

How does Pentazocine work?

Pentazocine is classified as Competitive Opioid Antagonists and Partial Opioid Agonists; its molecular targets in DrugCentral include SIGMAR1 (modulator), OPRK1, OPRM1 and SIGMAR1.

When was Pentazocine first approved?

Pentazocine was first approved by the FDA in 1967.

What drug class does Pentazocine belong to?

Pentazocine is in the Partial Opioid Agonist/Antagonist class.

What is the chemical formula of Pentazocine?

Pentazocine has the molecular formula C19H27NO and a molecular weight of 285.43 g/mol.

Sources

• DrugCentral drug card 3424 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL100116 — compound record and bioactivity
• PubChem CID 441278 — chemical identifiers
• DrugBank DB00652 — drug record
• FDA UNII RP4A60D26L — substance identity
• DailyMed: FDA labels for Pentazocine — current prescribing information (label search)
• UniProt Q99720 (SIGMAR1) — target protein
• UniProt P41145 (OPRK1) — target protein
• UniProt P35372 (OPRM1) — target protein
• UniProt P41143 (OPRD1) — target protein
• UniProt Q5BJF2 (TMEM97) — 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.