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
| Target | Action | Gene / 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_uM | 2.0 |
|---|---|
| cox2_IC50_uM | 0.3 |
| cox2_selectivity | 6.666666666666667 |
| inhibitionType | reversible |
| preferentialCOX2 | 1 |
| selectiveCOX2 | 0 |
| plateletEffect | 0 |
| source | Warner1999/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
| Efficacy | Pain and inflammation control (VAS/NRS scores, joint mobility, functional status); minimum effective dose |
|---|---|
| Toxicity | Blood 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 pearl | Use 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. |
| Counseling | Take 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
| Formula | C16H13Cl2NO4 |
|---|---|
| Molecular weight | 354.19 g/mol |
| IUPAC name | 2-[2-[2-(2,6-dichloroanilino)phenyl]acetyl]oxyacetic acid |
| CAS | 89796-99-6 |
| PubChem CID | 71771 |
| InChIKey | MNIPYSSQXLZQLJ-UHFFFAOYSA-N |
| logP | 3.91 (XLogP 4.3) |
| Polar surface area | 75.63 Ų |
| H-bond acceptors / donors | 4 / 2 |
| Drug-likeness (QED) | 0.77 |
| Lipinski violations | 0 |
SMILES
O=C(O)COC(=O)Cc1ccccc1Nc1c(Cl)cccc1ClBiology & Pharmacokinetics
Pharmacokinetics
| BBB penetrant | No |
|---|
Enzyme interactions
| Enzyme | Role | Detail |
|---|---|---|
| CYP1A2 | Substrate | — |
| CYP2B6 | Inhibitor | — |
| CYP2B6 | Substrate | — |
| CYP2C19 | Substrate | — |
| CYP2C9 | Inhibitor | — |
| CYP2C9 | Substrate | — |
| CYP3A4 | Substrate | — |
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)
| Brand | Form / strength | Pack | Agent | Citizen (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 |