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diclofenac (Voltaren, Cataflam, Flector patch, Cambia, Pennsaid, Zipsor, Zorvolex)

Tradenames: Voltaren, Cataflam, Flector patch Indications: 1) temporary relief of minor aches, pains, fever 2) migraine 3) musculoskeletal inflammation - osteoarthritis, bursitis Contraindications: Caution: 1) patients on anticoagulation therapy 2) surgical patients with known bleeding tendencies Dosage: 1) 50 mg PO BID/TID (diclofenac potassium) 2) 100 mg PO QD (extended release Voltaren XR) 3) 18-35 mg TID (Zorvolex) Tabs: - 25, 50, 75 mg (diclofenac potassium) - 100 mg (Voltaren XR) - 18, 35 mg (Zorvolex) [14] Capusle: liquid-filled Zipsor Oral solution: Cambia for migraine - see diclofenac topical for dosage of topical gel Pharmacokinetics: 1) food decreases rate, but not extent of absorption 2) mean plasma levels after oral doses of 50 & 75 mg are 1.5 & 1.9 mg/L, respectively 3) metabolized in the liver by cyt P450 2C9 Monitor: - serum ALT & serum AST 4-8 weeks after starting ANY diclofenac product & then periodically [10] - monitor blood pressure as hypertension can occur with NSAIDs Adverse effects:, 1) peptic ulceration, GI bleed [4] - standard dose proton pump inhibitors are 1st line for prevention NSAID-related peptic ulcers [15] 2) dizziness, drowsiness, edema, rash 3) cardiovascular risk a) greater than that of rofecoxib (Vioxx) RR=1.91 vs 1.66 b) dose-depenedent cardiovascular risk [11] c) risk of major cardiovascular events within 30 days of starting diclofenac is 0.1% [16] Drug interactions: 1) aluminum & magnesium hydroxide may decrease diclofenac absorption 2) diclofenac may decrease renal elimination of: a) Li+ b) digoxin c) methotrexate 3) diclofenac may decrease antihypertensive & diuretic effects of furosemide & HCTZ 4) diclofenac may increase renal toxicity of cyclosporine 5) any drug which inhibits cyt P450 2C9 can increase diclofenac levels 6) any drug which induces cyt P450 2C9 can diminish diclofenac levels Laboratory: 1) specimen: serum, plasma (EDTA), urine 2) methods: a) serum/plasma: HPLC, GC b) urine: GC Mechanism of action: 1) non-specific inhibition of cyclo-oxygenase (COX-1 & COX-2) 2) weak anti-platelet activity (weaker than naproxen)

Interactions

drug interactions drug adverse effects of NSAIDs monitor with non steroidal anti-inflammatory agents (NSIADs)

Related

cytochrome P450 2C9; cytochrome P450 BP-1; cytochrome P450 MP-4; S-mephenytoin-4-hydroxylase; limonene 6-monooxygenase; limonene 7-monooxygenase (CYP2C9, CYP2C10)

Specific

Diclofenac Ophthalmic diclofenac topical (Solaraze, Voltaren gel)

General

non-steroidal anti-inflammatory agent (NSAID)

Properties

INHIBITS: cyclooxygenase MISC-INFO: elimination route LIVER 1/2life 1-2 HOURS protein-binding >99% elimination by hemodialysis - peritoneal dialysis - pregnancy-category B safety in lactation - ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed, WB Saunders, Philadelpha 1995
  5. Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: 220233 (subscription needed) http://www.prescribersletter.com
  6. Journal Watch 21(18):143-44, 2001
  7. Journal Watch 24(23):177, 2004 - Roth SH, Shainhouse JZ. Efficacy and safety of a topical diclofenac solution (pennsaid) in the treatment of primary osteoarthritis of the knee: a randomized, double-blind, vehicle-controlled clinical trial. Arch Intern Med. 2004 Oct 11;164(18):2017-23. PMID: 15477437 - Tugwell PS, Wells GA, Shainhouse JZ. Equivalence study of a topical diclofenac solution (pennsaid) compared with oral diclofenac in symptomatic treatment of osteoarthritis of the knee: a randomized controlled trial. J Rheumatol. 2004 Oct;31(10):2002-12. PMID: 15468367
  8. Prescriber's Letter 15(1): 2008 New Topical NSAIDs: Voltaren Gel and Flector Patch Detail-Document#: 240104 (subscription needed) http://www.prescribersletter.com
  9. FDA MedWatch Voltaren Gel (diclofenac sodium topical gel) 1% - Hepatic Effects Labeling Changes http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm193047.htm
  10. Prescriber's Letter 17(4): 2010 New Drug: Pennsaid (Diclofenac Sodium Topical Solution 1.5%) COMMENTARY: New Drug: Pennsaid (Diclofenac Sodium Topical Solution 1.5%) GUIDELINES: Choosing Non-Opioid Analgesics for Osteoarthritis (AHRQ, 2009) Detail-Document#: 260405 (subscription needed) http://www.prescribersletter.com
  11. Fosbol EL et al Cause-Specific Cardiovascular Risk Associated With Nonsteroidal Antiinflammatory Drugs Among Healthy Individuals. Circ Cardiovasc Qual Outcomes published online Jun 8, 2010; DOI: 10.1161/CIRCOUTCOMES.109.861104 http://circoutcomes.ahajournals.org/cgi/rapidpdf/CIRCOUTCOMES.109.861104v1.pdf
  12. Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Detail-Document#: 260704 (subscription needed) http://www.prescribersletter.com
  13. Deprecated Reference
  14. Prescriber's Letter 21(2): 2014 Comparison of Diclofenac Products Detail-Document#: 300205 (subscription needed) http://www.prescribersletter.com
  15. Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
  16. Schmidt M, Sorensen HT, Pedersen L Diclofenac use and cardiovascular risks: series of nationwide cohort studies. BMJ 2018;362:k3426 PMID: 30181258 https://www.bmj.com/content/362/bmj.k3426

Component-of

5 fluorouracil/diclofenac adapalene/diclofenac/tamoxifen amantadine/baclofen/diclofenac/gabapentin/lidocaine amitriptyline/diclofenac/lidocaine/prilocaine diclofenac topical (Solaraze, Voltaren gel) diclofenac/lidocaine diclofenac/lidocaine/menthol diclofenac/misoprostol (Arthrotec)