New Release: Alpha testing version has been released.

Aceclofenac

M01A - NSAIDs and antirheumatic products, non-steroids ATC M01AB16 Small molecule Natural product

🧬 Cross-allergy: NSAIDs

JFDA label: AIRTAL TABLET

Mechanism of Action

Inhibitor of Prostaglandin G/H synthase 2 — Cyclooxygenase-2 inhibitor

TargetActionGene / class
Prostaglandin G/H synthase 2 efficacy INHIBITOR PTGS2

Indications

Approved

  • Arthralgia — Arthralgia
  • Arthritis, Rheumatoid — rheumatoid arthritis
  • Myalgia — Myalgia
  • Osteoarthritis — osteoarthritis
  • Rheumatic Diseases — rheumatic disease
  • Spondylitis — spondylitis

Off-label

  • Pulpitis

Class profile

cox1_IC50_uM2.0
cox2_IC50_uM0.3
cox2_selectivity6.666666666666667
inhibitionTypereversible
preferentialCOX21
selectiveCOX20
plateletEffect0
sourceWarner1999/Vane1996/ChEMBL

Pregnancy & Lactation

Pregnancy

Lactation

Compatible Hale L1

If a mother requires aceclofenac, it is not a reason to discontinue breastfeeding; however, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.

Monitoring

EfficacyPain and inflammation control (VAS/NRS scores, joint mobility, functional status); minimum effective dose
ToxicityBlood pressure (raises BP, antagonises antihypertensives); renal function (SCr, eGFR — especially in elderly, heart failure, CKD, dehydrated); Hb/faecal occult blood (GI bleeding); LFTs; oedema
Clinical pearlUse the lowest effective dose for the shortest duration. Consider co-prescribing a proton pump inhibitor if GI risk factors present. COX-2 selective agents reduce GI but not CV risk.
CounselingTake with food or milk to reduce GI upset. Report black stools, blood in urine, or significant ankle swelling. Monitor blood pressure regularly if hypertensive.

Chemistry & Properties

2D structure
FormulaC16H13Cl2NO4
Molecular weight354.19 g/mol
IUPAC name2-[2-[2-(2,6-dichloroanilino)phenyl]acetyl]oxyacetic acid
CAS89796-99-6
PubChem CID71771
InChIKeyMNIPYSSQXLZQLJ-UHFFFAOYSA-N
logP3.91 (XLogP 4.3)
Polar surface area75.63 Ų
H-bond acceptors / donors4 / 2
Drug-likeness (QED)0.77
Lipinski violations0
SMILESO=C(O)COC(=O)Cc1ccccc1Nc1c(Cl)cccc1Cl

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrantNo

Enzyme interactions

EnzymeRoleDetail
CYP1A2Substrate
CYP2B6Inhibitor
CYP2B6Substrate
CYP2C19Substrate
CYP2C9Inhibitor
CYP2C9Substrate
CYP3A4Substrate

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (2)

BrandForm / strengthPackAgentCitizen (JOD)
AIRTAL TABLET Tablet 100 mg 10 tab pack varies THE ARAB DRUG STORE P.S.C 1.270
AIRTAL TABLET Tablet 100 mg 40 tab pack varies THE ARAB DRUG STORE P.S.C 4.740