DICLOFENAC SODIUM

Clinical safety rating: avoid

ACE inhibitors and ARBs may have diminished antihypertensive effect Increases risk of serious cardiovascular thrombotic events and GI bleeding.

How it works

Non-selective COX-1 and COX-2 inhibitor, reducing prostaglandin synthesis via inhibition of cyclooxygenase, leading to anti-inflammatory, analgesic, and antipyretic effects.

What the body does with it

Metabolism	Primarily hepatic via CYP2C9 and other CYP enzymes; undergoes glucuronidation. Minor renal clearance.
Excretion	Approximately 65% renal as glucuronide conjugates and inactive metabolites, ~20% biliary/fecal. Less than 1% unchanged in urine.
Half-life	Terminal elimination half-life approximately 2 hours (range 1.3–3.1 h). Short half-life requires frequent dosing; no accumulation with normal dosing intervals.
Protein binding	Greater than 99.5% bound to albumin.
Volume of Distribution	Approximately 0.12–0.17 L/kg (total Vd at steady state 0.12–0.17 L/kg). Low Vd indicates minimal tissue distribution; primarily confined to plasma and extracellular fluid.
Bioavailability	Oral: 50–60% (first-pass metabolism); rectally: approximately 50–70% (similar to oral); intramuscular: 90–100%; topical: 6–10% (systemic absorption, but local concentrations higher); ophthalmic: minimal systemic absorption (<0.5%).
Onset of Action	Oral: 30 minutes (analgesic); topical: 2–4 hours; ophthalmic: 30 minutes; rectal: 30–60 minutes; intramuscular: 15–30 minutes.
Duration of Action	Oral: 4–6 hours (immediate-release); topical: 6–8 hours; ophthalmic: 4–6 hours; rectal: 4–8 hours; gastrointestinal and renal adverse effects may persist longer.

Classification & Brands

Action Class	NSAID's- Non-Selective COX 1&2 Inhibitors (acetic acid)
Brand Substitutes	Diclonir Injection, 3D Injection, Powerflam Injection, Recoflam Injection, Iconac Injection, Walkfree Injection, NAC -AQ Injection, Vivian Plus 75mg Injection, Dilona Aqua 75mg Injection, Vivogesic AQ 75mg Injection

Dosing & administration

Oral: 50 mg two to three times daily; maximum 150 mg/day. Topical: 1% gel applied four times daily. Rectal: 100 mg suppository once daily.

Dosage form	SOLUTION/DROPS
Renal impairment	eGFR 30-59 mL/min: No adjustment needed; monitor renal function. eGFR <30 mL/min: Contraindicated. Hemodialysis: Not recommended.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Use caution; reduce dose by 50%. Child-Pugh C: Contraindicated.
Pediatric use	For children ≥1 year: Oral suspension 0.5-1 mg/kg/dose two to three times daily; maximum 3 mg/kg/day. For juvenile idiopathic arthritis: 1-2 mg/kg/day divided two to three times daily. Not recommended in children <1 year.
Geriatric use	Start at lowest effective dose (e.g., 50 mg once daily); use for shortest duration. Avoid in patients with high GI or cardiovascular risk. Monitor renal function and electrolytes.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

ACE inhibitors and ARBs may have diminished antihypertensive effect Increases risk of serious cardiovascular thrombotic events and GI bleeding.

FDA category	Positive
Breastfeeding	Excreted in breast milk in low amounts (M/P ratio 0.02-0.79). Considered compatible with breastfeeding; monitor infant for gastrointestinal effects.
Teratogenic Risk	Category C in first and second trimesters; Category D in third trimester. Risk of premature ductus arteriosus closure and oligohydramnios in third trimester. Avoid after 30 weeks gestation.

Warnings & precautions

■ FDA Black Box Warning

Increased risk of serious cardiovascular thrombotic events (including MI and stroke) and serious GI adverse events (including bleeding, ulceration, and perforation of stomach/intestines). Contraindicated in CABG surgery.

Side Effect Profile

Serious Effects

Absolute Contraindications

Absolute: Hypersensitivity to diclofenac or NSAIDs, history of asthma/urticaria with NSAIDs, CABG surgery, active peptic ulcer/GI bleeding. Relative: Severe renal or hepatic disease, advanced age, concurrent anticoagulants, pregnancy (3rd trimester).

Clinical Precautions

Precautions

Cardiovascular risk (HTN, CHF, edema), GI risk (bleeding, ulcers), renal toxicity, hepatic toxicity, anaphylactoid reactions, skin reactions (including SJS/TEN), and hematologic effects (anemia). Use lowest effective dose for shortest duration.

Clinical Tips & Counseling

Drug interactions

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DICLOFENAC SODIUM

Clinical safety rating: avoid

ACE inhibitors and ARBs may have diminished antihypertensive effect Increases risk of serious cardiovascular thrombotic events and GI bleeding.

How it works

Non-selective COX-1 and COX-2 inhibitor, reducing prostaglandin synthesis via inhibition of cyclooxygenase, leading to anti-inflammatory, analgesic, and antipyretic effects.

What the body does with it

Metabolism	Primarily hepatic via CYP2C9 and other CYP enzymes; undergoes glucuronidation. Minor renal clearance.
Excretion	Approximately 65% renal as glucuronide conjugates and inactive metabolites, ~20% biliary/fecal. Less than 1% unchanged in urine.
Half-life	Terminal elimination half-life approximately 2 hours (range 1.3–3.1 h). Short half-life requires frequent dosing; no accumulation with normal dosing intervals.
Protein binding	Greater than 99.5% bound to albumin.
Volume of Distribution	Approximately 0.12–0.17 L/kg (total Vd at steady state 0.12–0.17 L/kg). Low Vd indicates minimal tissue distribution; primarily confined to plasma and extracellular fluid.
Bioavailability	Oral: 50–60% (first-pass metabolism); rectally: approximately 50–70% (similar to oral); intramuscular: 90–100%; topical: 6–10% (systemic absorption, but local concentrations higher); ophthalmic: minimal systemic absorption (<0.5%).
Onset of Action	Oral: 30 minutes (analgesic); topical: 2–4 hours; ophthalmic: 30 minutes; rectal: 30–60 minutes; intramuscular: 15–30 minutes.
Duration of Action	Oral: 4–6 hours (immediate-release); topical: 6–8 hours; ophthalmic: 4–6 hours; rectal: 4–8 hours; gastrointestinal and renal adverse effects may persist longer.

Classification & Brands

Action Class	NSAID's- Non-Selective COX 1&2 Inhibitors (acetic acid)
Brand Substitutes	Diclonir Injection, 3D Injection, Powerflam Injection, Recoflam Injection, Iconac Injection, Walkfree Injection, NAC -AQ Injection, Vivian Plus 75mg Injection, Dilona Aqua 75mg Injection, Vivogesic AQ 75mg Injection

Dosing & administration

Oral: 50 mg two to three times daily; maximum 150 mg/day. Topical: 1% gel applied four times daily. Rectal: 100 mg suppository once daily.

Dosage form	SOLUTION/DROPS
Renal impairment	eGFR 30-59 mL/min: No adjustment needed; monitor renal function. eGFR <30 mL/min: Contraindicated. Hemodialysis: Not recommended.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Use caution; reduce dose by 50%. Child-Pugh C: Contraindicated.
Pediatric use	For children ≥1 year: Oral suspension 0.5-1 mg/kg/dose two to three times daily; maximum 3 mg/kg/day. For juvenile idiopathic arthritis: 1-2 mg/kg/day divided two to three times daily. Not recommended in children <1 year.
Geriatric use	Start at lowest effective dose (e.g., 50 mg once daily); use for shortest duration. Avoid in patients with high GI or cardiovascular risk. Monitor renal function and electrolytes.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

ACE inhibitors and ARBs may have diminished antihypertensive effect Increases risk of serious cardiovascular thrombotic events and GI bleeding.

FDA category	Positive
Breastfeeding	Excreted in breast milk in low amounts (M/P ratio 0.02-0.79). Considered compatible with breastfeeding; monitor infant for gastrointestinal effects.
Teratogenic Risk	Category C in first and second trimesters; Category D in third trimester. Risk of premature ductus arteriosus closure and oligohydramnios in third trimester. Avoid after 30 weeks gestation.