Meperidine

Summary

Meperidine (CHEMBL607) is an approved small-molecule opioid analgesic (ATC N02AB52) targeting OPRD1, OPRK1, and OPRM1; indicated across 4 conditions including sciatica and scoliosis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N02AB52 (+2 more)
• Targets: 3 (OPRD1, OPRK1, OPRM1)
• Indications: 4 conditions
• Clinical trials: 55
• Chemistry: 247.33 Da · C15H21NO2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL607
Name	Meperidine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	4058
ChEBI	CHEBI:6754
ATC	N02AB52, N02AB02, N02AB72
Molecular formula	C15H21NO2
Molecular weight	247.33
InChIKey	XADCESSVHJOZHK-UHFFFAOYSA-N

SMILES: CCOC(=O)C1(CCN(CC1)C)C2=CC=CC=C2

IUPAC name: ethyl 1-methyl-4-phenylpiperidine-4-carboxylate

ChEBI definition: A piperidinecarboxylate ester that is piperidine which is substituted by a methyl group at position 1 and by phenyl and ethoxycarbonyl groups at position 4. It is an analgesic which is used for the treatment of moderate to severe pain, including postoperative pain and labour pain.

Pharmacological roles (ChEBI): opioid analgesic, κ-opioid receptor agonist, μ-opioid receptor agonist, antispasmodic drug.

Also known as: IDS-NP-001, Isonipecaine, Meperidine, Meperidol, Pethanol, Pethidine, Pethidine dbl, Pethidineter, Petidina, Renaudin, meperidine, MEPERIDINE

Parent form; salt/anhydrous children: CHEMBL429713, CHEMBL1701

Patent coverage: 12,515 distinct patent families (43,837 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
OPRD1	δ receptor	Agonist	5	0.2%	P41143
OPRK1	κ receptor	Agonist	5.63	0%	P41145
OPRM1	μ receptor	Agonist	6.5	0%	P35372

Broader ChEMBL bioactivity targets: 12 (assay-derived). Sample: Opioid receptor, Opioid receptors; mu/kappa/delta, Opioid receptor, Sodium-dependent serotonin transporter, Alpha-1A adrenergic receptor, Mu-type opioid receptor, Kappa-type opioid receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, Sodium-dependent serotonin transporter, Sodium-dependent dopamine transporter.

Bioactivity

ChEMBL activities: 16 potent at pChembl ≥ 5 of 22 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
OPRM1	6.5	IC50	315	nM	CHEMBL_ACT_125905
KCNH2	6.49	IC50	323.6	nM	CHEMBL_ACT_1523678
P31652	6.38	Ki	412	nM	CHEMBL_ACT_92210
P97266	6.35	Ki	451	nM	CHEMBL_ACT_1033451
P32300	6.3	IC50	500	nM	CHEMBL_ACT_1004730
OPRM1	6.3	IC50	500	nM	CHEMBL_ACT_256996
P33533	6.16	EC50	700	nM	CHEMBL_ACT_14555958
P33533	6.16	ED50	700	nM	CHEMBL_ACT_14701502
OPRM1	5.82	AC50	1500	nM	CHEMBL_ACT_25146765
SLC6A4	5.72	AC50	1900	nM	CHEMBL_ACT_25150063
OPRK1	5.62	IC50	2370	nM	CHEMBL_ACT_125906
ADRA1A	5.59	AC50	2560	nM	CHEMBL_ACT_25137767
OPRK1	5.41	AC50	3902	nM	CHEMBL_ACT_25129175
OPRM1	5.24	AC50	5800	nM	CHEMBL_ACT_25157258
ADRA1A	5.11	AC50	7800	nM	CHEMBL_ACT_25217870
OPRM1	5.03	EC50	9400	nM	CHEMBL_ACT_2607519

Target pathways

Aggregated over 3 target gene(s): OPRD1, OPRK1, OPRM1.

Top Reactome pathways

6 total, by targets touching each:

Pathway	Targets	Genes
Peptide ligand-binding receptors	3	OPRD1, OPRK1, OPRM1
G alpha (i) signalling events	3	OPRD1, OPRK1, OPRM1
Interleukin-4 and Interleukin-13 signaling	2	OPRD1, OPRM1
MECP2 regulates neuronal receptors and channels	2	OPRK1, OPRM1
Opioid Signalling	1	OPRM1
G-protein activation	1	OPRM1

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	3
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	3
phospholipase C-activating G protein-coupled receptor signaling pathway	3
neuropeptide signaling pathway	3
G protein-coupled opioid receptor signaling pathway	3
signal transduction	3
immune response	2
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	2
response to nicotine	2
eating behavior	2
response to ethanol	2
sensory perception	2
sensory perception of pain	2
adult locomotory behavior	1
negative regulation of gene expression	1

Indications & clinical

Indications

4 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
sciatica	3	MONDO:0024333	HP:0011868
scoliosis	2	MONDO:0005392	EFO:0004273

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 55.

Phase distribution

Phase	Trials
PHASE4	21
Not specified	14
PHASE2	9
PHASE3	5
PHASE2/PHASE3	3
PHASE1	2
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06736938	PHASE4	NOT_YET_RECRUITING	Balanced Analgosedation in Bronchoscopy: Propofol/Pethidine Versus Midazolam/Pethidine
NCT00596414	PHASE4	COMPLETED	Sedation and Analgesia for Transjugular Liver Biopsy: A Randomized Double Blind Placebo Controlled Trial
NCT00937924	PHASE4	COMPLETED	Adjunct Sedatives in Endoscopic Ultrasound (EUS) and Endoscopic Retrograde Cholangiopancreatography (ERCP) Procedures
NCT01229527	PHASE4	COMPLETED	Comparison Between Two Different Dosages of Remifentanil During Colonoscopy
NCT01394731	PHASE4	COMPLETED	Analgesic Effects of Intravenous Paracetamol on Labor Pain
NCT01555671	PHASE4	COMPLETED	Study of the Effectiveness of Administration of Meperidine on the Length of Active Phase of Labor in Women
NCT01693185	PHASE4	COMPLETED	Remifentanil Only vs. Midazolam and Meperidine During Elective Colonoscopy
NCT01709422	PHASE4	COMPLETED	Efficacy and Safety Profiles of Combination Sedation Propofol With Midazolam and Meperidine.
NCT02027311	PHASE4	COMPLETED	Etomidate vs. Midazolam for Sedation During ERCP
NCT02179294	PHASE4	COMPLETED	A Randomised Controlled Trial of Remifentanil Intravenous Patient Controlled Analgesia (PCA) Versus Intramuscular Pethidine for Pain Relief in Labour
NCT02475824	PHASE4	COMPLETED	Midazolam With Meperidine and Dexmedetomidine vs. Midazolam With Meperidine and Propofol for Sedation During ERCP
NCT02486328	PHASE4	COMPLETED	The Effect of Different Sedation Regimes on Cognitive Function in Lower Gastrointestinal System Endoscopy
NCT02493192	PHASE4	UNKNOWN	Birth Ball Versus Meperidine and Haloperidol Injection for Pain Relief During First Stage of Labour
NCT02494180	PHASE4	COMPLETED	A Non-inferiority Trial on Pain Relief During Oocyte Retrieval
NCT02684942	PHASE4	COMPLETED	Comparison of Meperidine and Fentanyl on Pain Scale and QOL in Brachytherapy
NCT03032458	PHASE4	COMPLETED	Efficacy of Pethidine, Ketorolac And Xylocaine Gel As Analgesics For Pain Control In Shockwave Lithotripsy
NCT04068948	PHASE4	COMPLETED	Comparing Pediatric Dental Oral Sedation Outcomes With and Without Meperidine in Children Aged 3-7 Years
NCT04735965	PHASE4	UNKNOWN	Comparison of Dexmedetomidine and Meperidine for the Prevention of Shivering Following Coronary Artery Bypass Graft
NCT05110469	PHASE4	COMPLETED	Comparison of MgSO4 Versus Meperidine for Prevention of Shivering During Spinal Anesthesia
NCT05284409	PHASE4	COMPLETED	Comparative Study Between the Prophylactic Intravenous Administrations of Acetaminophen vs Dexamethasone vs Pethidine Regarding the Incidence of Shivering Induced by Single Shot Spinal Anesthesia in the Orthopedic Surgeries of the Lower Limbs
NCT05386121	PHASE4	UNKNOWN	Erector Spinae Plane Block Versus Quadratus Lumborum Block for Open Renal Surgeries in Children
NCT03167905	PHASE2/PHASE3	ACTIVE_NOT_RECRUITING	CODEPAD (Collaborative Outcomes of DEpression and Pain Associated With Delivery)
NCT06775431	PHASE3	RECRUITING	Comparing Prophylactic Intravenous Pethidine and Intrathecal Pethidine in Preventing Post Spinal Shivering in Caesarean Section
NCT00163553	PHASE3	UNKNOWN	Neuraxial Pethidine After Lumbar Surgery Trial
NCT01833312	PHASE3	TERMINATED	Cooling Plus Best Medical Treatment Versus Best Medical Treatment Alone for Acute Ischaemic Stroke
NCT02707250	PHASE2/PHASE3	UNKNOWN	Oblique Subcostal Tap Block Efficacy in Laparoscopic Cholecystectomy
NCT03115047	PHASE3	COMPLETED	Shivering Treatment After Cesarean Delivery: Meperidine vs. Dexmedetomidine
NCT04686058	PHASE3	COMPLETED	Sedation Techniques for Outpatient Colonoscopy
NCT06082076	PHASE2/PHASE3	UNKNOWN	Prevention of Shivering Associated With Spinal Anesthesia
NCT01236651	PHASE2	UNKNOWN	Meperidine Versus Drotaverine Regarding the Effect on the Duration of the First Stage of Labor in Full Term Primigravidae
NCT02382432	PHASE2	COMPLETED	Dexmedetomidine in Post Spinal Anesthesia Shivering
NCT02441673	PHASE2	UNKNOWN	Nefopam vs Tramadol in the Prevention of Post Anaesthetic Shivering
NCT02549118	PHASE2	UNKNOWN	Tenoxicam for Intrapartum Analgesia
NCT02557087	PHASE2	UNKNOWN	Hyoscine ButylBromide for Intrapartum Analgesia
NCT02578251	PHASE2	UNKNOWN	Paracetamol for Intrapartum Analgesia
NCT02619019	PHASE2	COMPLETED	Effect of Spinal Dexamethasone During Transuretheral Prostatectomy
NCT02858310	PHASE1/PHASE2	COMPLETED	E7 TCR T Cells for Human Papillomavirus-Associated Cancers
NCT03968146	PHASE2	COMPLETED	Erector Spinae Plane Block in Scoliotic Adolescents
NCT06326944	PHASE2	UNKNOWN	Fascia Transversalis Versus Transversus Abdominis Plane Block for Children Undergoing Inguinal Hernia Surgery
NCT02867800	PHASE1	COMPLETED	Abatacept for GVHD Prophylaxis After Hematopoietic Stem Cell Transplantation for Pediatric Sickle Cell Disease

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 3 clinical and 6 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

612 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
Dihydroergotamine	ChEMBL + PubChem	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
PROPOXYPHENE	ChEMBL + PubChem	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
TAFAMIDIS	ChEMBL + PubChem	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
ALVIMOPAN	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
AMIODARONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
AMLODIPINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
AMOXAPINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
BENZTROPINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
BUPRENORPHINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
BUTORPHANOL	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
CANNABIDIOL	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
CINNARIZINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
CODEINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
ECONAZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
FENTANYL	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
FLUSPIRILENE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
HYDROCODONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
HYDROMORPHONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
LANSOPRAZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
LEVORPHANOL	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
LOPERAMIDE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
LOXAPINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
METHADONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
METHYLNALTREXONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
MICONAZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
MORPHINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
NAFTOPIDIL	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
NALBUPHINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
NALFURAFINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
NALMEFENE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
NALOXONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
NALTREXONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
NELFINAVIR	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
OLICERIDINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
OXYCODONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
OXYMORPHONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
PAROXETINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
PASIREOTIDE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
PENTAZOCINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
PIMOZIDE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
RALOXIFENE	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
RITONAVIR	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
SAMIDORPHAN	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
SAQUINAVIR	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
SUNITINIB	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
TAMOXIFEN	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
TRAMADOL	ChEMBL	Phase 4 (approved)	OPRD1, OPRK1, OPRM1
ASIMADOLINE	ChEMBL	Phase 3	OPRD1, OPRK1, OPRM1
ATICAPRANT	ChEMBL	Phase 3	OPRD1, OPRK1, OPRM1
CEBRANOPADOL	ChEMBL	Phase 3	OPRD1, OPRK1, OPRM1
NAVACAPRANT	ChEMBL	Phase 3	OPRD1, OPRK1, OPRM1
TRIMEBUTINE	ChEMBL	Phase 3	OPRD1, OPRK1, OPRM1
BREMAZOCINE	ChEMBL	Phase 2	OPRD1, OPRK1, OPRM1
CARFENTANIL	ChEMBL	Phase 2	OPRD1, OPRK1, OPRM1