Trade Names:Cataflam- Tablets 50 mg (as potassium)
Trade Names:Diclofenac- Tablets, delayed-release 25 mg (as sodium)- Tablets, delayed-release 50 mg (as sodium)
Trade Names:Flector- Patch, transdermal 180 mg (as epolamine)
Trade Names:Solaraze- Gel 3%
Trade Names:Voltaren- Gel 1%- Tablets, delayed-release 75 mg (as sodium)- Solution, ophthalmic 0.1% (as sodium)
Trade Names:Voltaren-XR- Tablets, ER 100 mg (as sodium)Apo-Diclo (Canada)Apo-Diclo Rapide (Canada)Apo-Diclo SR (Canada)Novo-Difenac (Canada)Novo-Difenac K (Canada)Novo-Difenac SR (Canada)Nu-Diclo (Canada)Nu-Diclo-SR (Canada)PMS-Diclofenac (Canada)PMS-Diclofenac SR (Canada)Sandoz Diclofenac (Canada)Sandoz Diclofenac Rapide (Canada)Sandoz Diclofenac SR (Canada)Voltaren Ophtha (Canada)Voltaren Rapide (Canada)
Decreases inflammation, pain, and fever, probably through inhibition of cyclooxygenase activity and prostaglandin synthesis.
Bioavailability is approximately 50% because of first-pass metabolism (oral doseforms). Food decreases T max and C max .Immediate-release tablets
T max is approximately 1 h.ER tablets
T max is approximately 5.3 h.Delayed-release tablets (50 mg dose)
T max is approximately 2.3 h.Solaraze topical gel
Following application of 2 g 3 times daily for 6 days, mean AUC is 9 ng•h/mL, mean C max is 4 ng/mL, and mean T max is 4.5 h.Topical patch
Following a single application of the patch on the upper inner arm, C max of 0.7 to 6 ng/mL was noted between 10 and 20 h of application. With twice-daily application of patch, plasma concentrations ranged from 1.3 to 8.8 ng/mL after 5 days.Voltaren gel
C max with application of 160 mg/day is 15 and 54 ng/mL with application of 480 mg/day. T max is 14 h with the application of 160 mg/day and 10 h with the application of 480 mg/day. The amount reaching the systemic circulation is 158 times lower with 160 mg/day compared with oral treatment.
More than 99% protein bound (albumin). Vd is approximately 1.4 L/kg (oral).
Undergoes hepatic metabolism. Five metabolites have been identified.
Approximately 65% is excreted in the urine and 35% in the bile as conjugates of unchanged diclofenac plus metabolites. The half-life is 1 to 2 h. Plasma elimination half-life after application of topical patch is approximately 12 h.
No differences in pharmacokinetics have been detected in studies with patients with renal function impairment.Hepatic Function Impairment
Because hepatic metabolism accounts for 100% of diclofenac elimination, patients with hepatic disease may require reduced doses.
Treatment of primary dysmenorrhea; relief of mild to moderate pain.Immediate-release, ER, and delayed-release tablets
Relief of signs and symptoms of osteoarthritis and rheumatoid arthritis.Delayed-release tablets
Acute and long-term use in the relief of signs and symptoms of ankylosing spondylitis.Ophthalmic
Treatment of postoperative inflammation after cataract removal; temporary relief of pain and photophobia following corneal refractive surgery.Solaraze topical gel
Treatment of actinic keratosis.Patch
Treatment of acute pain because of minor strains, sprains, and contusions.Voltaren topical gel
Treatment of pain of osteoarthritis or joint pain amenable to topical treatment (eg, knees, hands).
Treatment of perioperative pain in the setting of coronary artery bypass graft surgery; patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs; hypersensitivity to any component of the product; sensitivity to benzyl alcohol, diclofenac, polyethylene glycol monomethyl ether 350, or hyaluronate sodium (topical). Do not apply topical patch to nonintact or damaged skin regardless of the cause (eg, burns or wounds, eczema, exudative dermatitis, infected lesion).
Different tablet formulations of diclofenac are not necessarily bioequivalent.Actinic KeratosisAdult
Topical gel Apply gel to lesions twice daily. The recommended duration of treatment is 60 to 90 days.Analgesia and Primary Dysmenorrhea
PO 50 mg 3 times daily; may give initial dose of 100 mg if needed.Ankylosing Spondylitis
PO Delayed-release tablets 100 to 125 mg/day in divided doses; may give additional 25 mg at bedtime.Minor Strains, Sprains, and ContusionsAdults
Topical patch Apply 1 patch to most painful area twice daily.OsteoarthritisAdults
100 mg daily.Immediate-release, delayed-release tablets
100 to 150 mg/day in divided doses.Topical gel
Using the dosing card supplied in the product carton, apply up to the 2 or 4 g line (2 g for elbows, wrist, or hand; 4 g for each knee, ankle, or foot). Apply 4 times daily by gently massaging gel into the skin, ensuring application to the entire affected area. Do not apply more than 8 g/day to any single joint of the upper extremities or more than 16 g/day to any single joint of the lower extremities.Rheumatoid ArthritisAdults
100 mg daily. If response is unsatisfactory, the dosage may be increased to 100 mg twice daily.Delayed-release tablets
150 to 200 mg/day in divided doses.Immediate-release tablets
150 to 200 mg/day in divided doses.OphthalmicCataract Surgery
1 drop in affected eye 4 times daily beginning 24 h after cataract surgery and continuing during the first 2 wk of postoperative period.Corneal Refractive Surgery
1 or 2 drops within 1 h prior to corneal refractive surgery; then, within 15 min after surgery, apply 1 or 2 drops to the operative eye and continue 4 times daily for up to 3 days.
Do not store immediate-release and ER tablets at temperatures higher than 86°F. Protect from moisture.Delayed-release tablets
Store at 68° to 77°F. Protect from moisture.Ophthalmic solution
Store at 59° to 77°F. Protect from light.Topical patch
Store at 59° to 86°F.Topical gel
Store at 59° to 86°F. Do not freeze. Protect from heat.
Antihypertensive effect of ACE inhibitors may be diminished.Aminoglycosides (eg, gentamicin)
Aminoglycoside concentrations may be elevated, increasing the risk of adverse reactions.Aspirin
Protein binding of diclofenac may be reduced; in addition, the risk of gastric erosion and bleeding may be increased.Azole antifungal agents (eg, fluconazole)
Diclofenac plasma concentrations may be elevated, increasing the risk of adverse reactions.Bisphosphonates (eg, alendronate)
Coadministration may increase the risk of gastric ulceration.Cyclosporine
May increase nephrotoxicity.Digoxin
May increase digoxin serum concentrations.Furosemide and thiazide diuretics
May inhibit diuretic and antihypertensive effects.Heparin
Risk of hemorrhagic adverse reactions may be increased.Lithium
May decrease lithium Cl.Methotrexate
May increase methotrexate levels.SSRIs (eg, fluoxetine)
Risk of upper GI bleeding may be increased.Warfarin
May increase risk of gastric erosion and bleeding.
May prolong bleeding time.
Arrhythmia, CHF, hypertension, MI, syncope, tachycardia.Topical gel ( Solaraze )
Dizziness, headache, insomnia (3% or less).Oral
Dizziness, headache (1% to 10%); coma, hallucinations, meningitis.Topical gel ( Solaraze )
Headache (7%); asthenia, hypokinesia (2%); migraine (1%).Topical patch
Dizziness, headache, hyperkinesia, hypoesthesia, paresthesia, somnolence (1%).
Pruritus, rash (1% to 10%); angioedema, erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis.Topical gel ( Solaraze )
Pruritus (52%); rash (46%); dry skin (27%); contact dermatitis (33%); exfoliation (24%); vesiculobullous rash (4%); hyperesthesia, photosensitivity (3%); alopecia, skin carcinoma, skin ulcer (2%); acne (1%).Topical gel ( Voltaren )
Application-site dermatitis (4%).Topical patch
Pruritus (5%); application-site dryness, atrophy, discoloration, erythema, hyperhidrosis, irritation, vesicles (4%); dermatitis (2%).
Lacrimation complaints (30%); keratitis (28%); elevated IOP, transient ocular burning and stinging (15%); abnormal vision, acute elevated IOP, blurred vision, conjunctivitis, corneal deposits, corneal edema, corneal lesions, corneal opacity, discharge, eyelid swelling, injection, irritation, iritis, itching, lacrimation disorder, ocular allergy, redness (5% or less); rhinitis (3% or less); corneal erosion, corneal infiltrates, corneal perforation, corneal thinning, corneal ulceration, epithelial breakdown, superficial punctuate keratitis (postmarketing).Oral
Tinnitus (1% to 10%).Topical gel ( Solaraze )
Conjunctivitis (4%); eye pain (2%).
Abdominal pain, nausea, vomiting (3% or less).Oral
Abdominal pain, constipation, diarrhea, dyspepsia, flatulence, GI ulcers (gastric/duodenal), gross bleeding/perforation, heartburn, nausea, vomiting (1% to 10%); hematemesis, hepatitis, jaundice.Topical gel ( Solaraze )
Dyspepsia (3%); abdominal pain, diarrhea (2%).Topical patch
Nausea, constipation, diarrhea, dry mouth, gastritis, upper abdominal pain, and vomiting (3%); dysgeusia (2%); dyspepsia (1%).
Interstitial nephritis, renal failure.Topical gel ( Solaraze )
Anemia, increased bleeding time (1% to 10%); agranulocytosis, aplastic anemia, hemolytic anemia, lymphadenopathy, pancytopenia, thrombocytopenia.
Elevated liver enzymes (1% to 10%); liver failure.
Application-site reaction (84%); pain (26%); paresthesia (20%); edema (4%).
Edema (1% to 10%).Topical gel ( Solaraze )
Edema, increased CPK (4%); increased AST (3%); increased ALT, increased creatinine (2%); hypercholesterolemia, hyperglycemia (1%).
Back pain (4%); myalgia (3%); arthralgia, arthrosis, neck pain (2%).
Abnormal renal function (1% to 10%).
Asthma, dyspnea, pharyngitis, pneumonia, rhinitis, sinusitis (2%).Ophthalmic
Exacerbation of asthma, dyspnea.
Asthenia, chills, facial edema, fever, pain, viral infection (3% or less).Topical gel ( Solaraze )
Flu syndrome (10%); accidental injury, infection (4%); chest pain, pain (2%); allergic reaction (1%).
NSAIDs may cause an increased risk of serious CV thrombotic events, MI, and stroke, which can be fatal. This risk may increase with length of therapy. Patients with CV disease or risk factors for CV disease may be at greater risk. NSAIDs cause an increased risk of serious GI adverse reactions, including bleeding, inflammation, perforation of the stomach or intestines, and ulceration, which can be fatal. These events can occur any time during use and without warning symptoms. Elderly patients are at greater risk of serious GI events.
Monitor for signs and symptoms of GI bleeding. Closely monitor BP during the initiation of treatment and throughout the course of therapy. Carefully monitor patients who may be adversely affected by alterations in platelet function (eg, patients with coagulation disorders, patients receiving anticoagulant therapy). Obtain baseline assessments of pain and ability to perform activities of daily living. Ensure CBC, serum electrolytes, and serum transaminases are evaluated periodically during prolonged therapy. Note dark, tarry stools; epigastric pain; indigestion; or unusual bleeding or bruising. If used in patients with advanced renal disease, monitor renal function. Monitor refractive stability for a year following corneal refractive procedures in patients treated with the ophthalmic solution.
Check hemoglobin or hematocrit in patients on long-term treatment if they exhibit signs or symptoms of anemia.
Category C (immediate-release tablets, ER tablets, ophthalmic solution, topical patch, delayed-release tablets, Voltaren topical gel). Category B ( Solaraze topical gel). Can cause premature closure of the ductus arteriosus; avoid in late pregnancy.
Safety and efficacy not established.
Use with caution.
Acute renal function impairment, hyperkalemia, hyponatremia, interstitial nephritis, and renal papillary necrosis may occur. Not recommended in patients with advanced renal disease.
Monitor patient for signs and symptoms of hepatic function impairment. If noted, discontinue therapy immediately.
Use with caution in patients with fluid retention, heart failure, or hypertension.
Do not give diclofenac to patients with the aspirin triad, which typically occurs in patients with asthma who experience rhinitis with or without nasal polyps, or those who exhibit severe, potentially fatal bronchospasm after taking aspirin or other NSAIDs.
Anemia has been reported and may be the result of fluid retention, occult or gross GI bleeding, or an incompletely described effect on erythropoiesis.
Patients with asthma may have aspirin-sensitive asthma, which may be associated with severe and sometimes fatal bronchospasm. Do not administer diclofenac to patients with this type of aspirin-sensitivity because of possible cross-reactivity.
There have been reports that ocularly applied NSAIDs may cause increased bleeding of ocular tissue in conjunction with surgery.
Use with caution when initiating treatment with delayed-release tablets in patients with considerable dehydration.
Borderline elevations of 1 or more LFTs may occur in patients taking diclofenac.
New hypertension or worsening of preexisting hypertension, either of which may contribute to increased risk of CV events, may occur.
Renal papillary necrosis and other renal injury may occur.
NSAIDs inhibit platelet aggregation and have been reported to prolong bleeding time.
Serious and sometimes fatal skin adverse reactions, including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis, may occur.
Acute renal failure, coma, drowsiness, epigastric pain, GI bleeding, hypertension, lethargy, nausea, respiratory depression, vomiting.
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