THE INDIAN PHARMACIST Official Circular Pharmacy Logo THE INDIAN PHARMACISTLearn. Explore. Practise. Excel.
MEDICINE MONOGRAPH CODE: [7.17] ID: TIP-MED-000119

Celecoxib

Active Ingredient / Scientific Identity: Celecoxib • Class: Selective Cyclooxygenase-2 (COX-2) Inhibitor — Diaryl-Substituted Pyrazole Sulfonamide (Schedule H)

⚖️ Compare Profile
Generic / Entity NameCelecoxib ([7.17])
Verified Indian Brands / RefGeneric Compendial Entry (No Commercial Brand Claimed)
Pharmacological ClassSelective Cyclooxygenase-2 (COX-2) Inhibitor — Diaryl-Substituted Pyrazole Sulfonamide (Sc
Available Dosage FormsCapsules: 100 mg, 200 mg
Regulatory ClassificationSchedule H Prescription Drug (To be sold by retail on the prescription of a Registere
Key Warning & Review DateRenal: Avoid if eGFR <30 mL/min. Hepatic: Reduce dose by 50% in moderate hepatic impairment (Child–Pugh B); contraindicated i
Reviewed: 2026-11-10
Safety Matrix:⚖️ Legal Status: Schedule H Prescription Drug (To be sold by retail o✔️ Standard Clinical Dispensing Precautions

1. Clinical & Scientific Overview

Celecoxib (TIP-MED-000119, Reference Code [7.17]) is classified under Pain, Inflammation, Rheumatology & Gout Medicines (Ch 07) as a Selective Cyclooxygenase-2 (COX-2) Inhibitor — Diaryl-Substituted Pyrazole Sulfonamide (Schedule H). Within the Indian regulatory and compendial framework, it is governed under Schedule H Prescription Drug (To be sold by retail on the prescription of a Registered Medical Practitioner only — Drugs Rules 1945).

Verified Indian Market Examples / Compendial Status:
Representative Indian Market Examples (Edition 2.7 Ch 07 [7.17], p. 87): Celact (Sun), Zycel (Zydus), Cobix (Cipla), Celebrex (Pfizer) — Strengths & Dosage Forms: Capsules: 100 mg, 200 mg
Representative Indian Market Examples (Edition 2.7 Ch 07 [7.17], p. 87): Celact (Sun), Zycel (Zydus), Cobix (Cipla), Celebrex (Pfizer) — Strengths & Dosage Forms: Capsules: 100 mg, 200 mg
Dosage Forms & Available Strengths:
Capsules: 100 mg, 200 mg
Routes: Oral / Parenteral / Topical as specified by formulation

3. Mechanism of Action & Pharmacodynamics

Selective Cyclooxygenase-2 (COX-2) Inhibitor — Diaryl-Substituted Pyrazole Sulfonamide (Schedule H) acting on target receptor/enzyme pathways in Pain, Inflammation, Rheumatology & Gout Medicines (Ch 07): clinical efficacy is mediated via Selective Cyclooxygenase-2 (COX-2) Inhibitor — Diaryl-Substituted Pyrazole Sulfonamide (Schedule H) for Osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute musculoskeletal pain (lower incidence of gastroduodenal ulcers than non-selective NSAIDs at 200 mg/day, PRECISION trial).

4. Therapeutic Indications & Evidence-Supported Uses

  • Osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute musculoskeletal pain (lower incidence of gastroduodenal ulcers than non-selective NSAIDs at 200 mg/day, PRECISION trial)

🇮🇳 Jurisdiction & Indication Note: Indications and schedules reflect Indian compendial and regulatory records (CDSCO / Indian Pharmacopoeia & NFI / NLEM 2022). Where international reference labels (US FDA DailyMed / NCBI StatPearls) are cited for pharmacokinetic or mechanistic parameters, international approvals do not automatically imply CDSCO approval in India.

5. Educational Dosage Context, Formulations & Administration

Educational Dosing & Regimen Summary: Osteoarthritis: 200 mg PO OD (or 100 mg BD). Rheumatoid Arthritis / AS: 100–200 mg PO BD (Max 400 mg/day; use lowest effective dose)

Administration & Meal Timing: May be taken with or without food (take with food for 200 mg BD doses to improve absorption and comfort) | Morning (OD) or Morning & Evening (BD)

6. Pharmacokinetics, Metabolism & Renal/Hepatic Adjustment

Absorption & Disposition:
Absorption, distribution, metabolism, and excretion follow class pharmacokinetic profile; verify patient renal/hepatic function.
Metabolism & Biotransformation:
Renal: Avoid if eGFR <30 mL/min. Hepatic: Reduce dose by 50% in moderate hepatic impairment (Child–Pugh B); contraindicated in Child–Pugh C
Elimination & Renal Adjustment:
Renal: Avoid if eGFR <30 mL/min. Hepatic: Reduce dose by 50% in moderate hepatic impairment (Child–Pugh B); contraindicated in Child–Pugh C
Hepatic Impairment Considerations:
Renal: Avoid if eGFR <30 mL/min. Hepatic: Reduce dose by 50% in moderate hepatic impairment (Child–Pugh B); contraindicated in Child–Pugh C

7. Contraindications, Precautions & High-Risk Warnings

Contraindications & Red-Flag Precautions:
  • CONTRAINDICATED in Sulfonamide ('Sulfa') Allergy (Celecoxib contains a benzenesulfonamide moiety — unlike Etoricoxib!), established ischaemic heart disease (MI/angina), cerebrovascular disease (stroke/TIA), peripheral arterial disease, NYHA II–IV Heart Failure, active GI bleed, CKD (eGFR <30 mL/min), and Child–Pugh C cirrhosis

Key Clinical Precautions: Renal: Avoid if eGFR <30 mL/min. Hepatic: Reduce dose by 50% in moderate hepatic impairment (Child–Pugh B); contraindicated in Child–Pugh C

8. Adverse Effects Profile

Common & Mechanism-Related Adverse Effects:
  • Dyspepsia, abdominal pain, mild peripheral oedema, blood pressure elevation, dizziness
  • Atherothrombotic cardiovascular events (MI, stroke), heart failure decompensation, GI ulceration/bleeding (especially if combined with low-dose Aspirin!), acute kidney injury, SJS/TEN
Serious / Dose-Limiting Adverse Effects:
  • Monitor for severe hypersensitivity, organ toxicity, or dose-limiting adverse events.

9. Major Drug–Drug, Drug–Food & Drug–Herb Interactions

  • CYP2C9 INHIBITED BY FLUCONAZOLE: Fluconazole doubles Celecoxib plasma levels -> halve Celecoxib dose! Celecoxib inhibits CYP2D6 -> increases Metoprolol, Nebivolol, Amitriptyline, and Dextromethorphan levels; increases Lithium and Warfarin INR; co-administration with low-dose Aspirin negates much of Celecoxib's GI-sparing advantage (add a PPI!)

10. Clinical Monitoring, Patient Counselling & Storage

Clinical & Laboratory Monitoring: Monitor clinical response, baseline renal/hepatic parameters, and relevant serum biomarkers.

Pharmacist Patient Counselling Points:

  • Patient Counselling Checklist: COUNTER ALLERGY CHECK: Ask every patient about 'Sulfa' (Sulfonamide) allergy before dispensing Celecoxib (Celact/Zycel)! If the patient also takes Aspirin 75 mg for heart protection, a stomach protector (Pantoprazole) is still required
  • Meal & Clock Timing Instruction: May be taken with or without food (take with food for 200 mg BD doses to improve absorption and comfort) (Morning (OD) or Morning & Evening (BD))
  • Missed Dose Protocol: Take PRN or skip missed dose; never double dose
  • Geriatric Dispensing Pearl: If an oral NSAID cannot be avoided in an older adult without CV/renal disease, Celecoxib 100–200 mg/d + PPI has the lowest GI bleed rate, but monitor BP, eGFR, and HF signs closely

Storage, Stability & Dispensing Safeguards: Store below 25°C–30°C in original moisture- and light-resistant packaging out of reach of children. Available forms: Capsules: 100 mg, 200 mg

11. Visual Pharmacology & Mechanism Diagram (svg-v339-01-adme-12-step-journey)

THE 12-STEP ORAL DRUG JOURNEY THROUGH THE HUMAN BODY (LADME) Note: IV bolus enters Step 6 directly (F = 100%); Sublingual & Transdermal routes bypass Step 4–5 Portal First-Pass Metabolism 1. Oral Administration • Tablet / Capsule swallowed • Gastric emptying to duodenum pH 1.5–3.5 (Stomach) 2. Disintegration & Dissolution • Tablet breaks into granules • API dissolves in GI fluid Noyes-Whitney Dissolution Rate 3. GI Epithelial Absorption • Crosses intestinal villi • Passive / Active / P-gp efflux Small Intestine (Large Surface Area) 4. Portal Circulation • Mesenteric veins → Portal vein • Delivers blood to liver sinusoids Pre-systemic Venous Conduit 5. First-Pass Metabolism • Gut & hepatic CYP450 extraction • High: GTN, Propranolol, Morphine Determines Bioavailability (F = f_a × (1-E_H)) 6. Systemic Circulation • Hepatic vein → IVC → Heart • Unbound vs Albumin-bound drug Only FREE drug is active 7–8. Tissue Distribution (Vd) • Capillary permeation to organs • Blood-Brain & Placental barriers Vd = Dose / C_0 (L or L/kg) 9. Target Site of Action • Receptors (GPCR, Ion channel) • Enzymes & Carrier Transporters Pharmacodynamic Effect (E_max, EC50) 10. Hepatic Biotransformation • Phase I (CYP450 Oxidation/Hydrolysis) • Phase II (Glucuronidation/Sulfation) Converts lipophilic drug → hydrophilic metabolite 11. Renal & Biliary Elimination • Nephron: Filtration + Secretion − Reabsorption • Biliary excretion & Enterohepatic recycling Total Clearance CL_tot = CL_renal + CL_hepatic 12. Excretion from the Body • Urine (Primary polar metabolite route) • Bile/Faeces, Expired Air, Sweat, Milk Elimination Half-Life t1/2 = (0.693 × Vd) / CL
svg-v339-01-adme-12-step-journey — 8.1 Complete 12-Step Journey of an Orally Administered Drug (ADME): Figure 8.1: The 12-step physiological journey of a typical orally administered solid dosage form through Liberation, Absorption, Distribution, Metabolism, and Excretion (LADME). Note: Parenteral (IV), sublingual, and inhalational routes bypass gastrointestinal absorption and/or hepatic first-pass metabolism.

12. Authoritative References, Regulatory Sources & Editorial Disclaimer

Primary Compendial & Guideline Reference: Indian Pharmacist Desk Reference — Professional Edition 2.7 (2026–27) • Ch 07 [7.17] (p. 87)

Official Verification Portals: Indian Pharmacopoeia Commission (IPC) & National Formulary of India (NFI) • Central Drugs Standard Control Organization (CDSCO) • Ministry of Health & Family Welfare — NLEM 2022 • NCBI Bookshelf / StatPearls Pharmacology Reference • DailyMed (US FDA Official Prescribing Reference)

Last Medically & Pharmaceutically Reviewed: 2026-11-10 • Verification Status: HANDBOOK_SOURCE_CONTENT

Educational & Clinical Disclaimer: This reference profile is published solely for pharmacy education, academic study, and professional clinical reference. It does not substitute for patient-specific clinical judgement, qualified specialist oncology/medical supervision, or official CDSCO/IP prescribing information. Never self-medicate with prescription, Schedule H/H1/X, NDPS, or oncology medicines.