diclofenac (Voltaren, Cataflam, Flector patch, Cambia, Pennsaid, Zipsor, Zorvolex)
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Introduction
Tradenames: Voltaren, Cataflam, Flector patch
Indications
- temporary relief of minor aches, pains, fever
- migraine
- musculoskeletal inflammation
Contraindications
Caution:
- patients on anticoagulation therapy
- surgical patients with known bleeding tendencies
Dosage
- 50 mg PO BID/TID (diclofenac potassium)
- 100 mg PO QD (extended release Voltaren XR)
- 18-35 mg TID (Zorvolex)
Tabs:
Capusle: liquid-filled Zipsor
Oral solution: Cambia for migraine
- see diclofenac topical for dosage of topical gel
Pharmacokinetics
- food decreases rate, but not extent of absorption
- mean plasma levels after oral doses of 50 & 75 mg are 1.5 & 1.9 mg/L, respectively
- metabolized in the liver by cyt P450 2C9
elimination via liver
1/2life = 1-2 hours
protein binding = >99 %
elimination by hemodialysis = -
elimination by peritoneal dialysis = -
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
,
- peptic ulceration, GI bleed[4]
- standard dose proton pump inhibitors are 1st line for prevention NSAID-related peptic ulcers[15]
- dizziness, drowsiness, edema, rash
- cardiovascular risk
- greater than that of rofecoxib (Vioxx) RR=1.91 vs 1.66
- dose-depenedent cardiovascular risk[11]
- risk of major cardiovascular events within 30 days of starting diclofenac is 0.1%[16]
Drug interactions
- aluminum & magnesium hydroxide may decrease diclofenac absorption
- diclofenac may decrease renal elimination of:
- diclofenac may decrease antihypertensive & diuretic effects of furosemide & HCTZ
- diclofenac may increase renal toxicity of cyclosporine
- any drug which inhibits cyt P450 2C9 can increase diclofenac levels
- any drug which induces cyt P450 2C9 can diminish diclofenac levels
- drug interaction(s) of cholinesterase inhibitors with NSAIDs
- drug interaction(s) of lithium carbonate with NSAIDs
- drug interaction(s) of NSAIDs with oral contraceptive
- drug interaction(s) of NSAIDs with SSRIs
- drug interaction(s) of NSAIDs with antidepressants
- drug interaction(s) of aspirin with NSAIDs
- drug interaction(s) of apixaban with NSAIDs
- drug interaction(s) of warfarin with NSAIDs
- drug interaction(s) of NSAIDs with beta blockers
- drug interaction(s) of NSAIDs with ARBs
- drug interaction(s) of NSAIDs with aldosterone antagonis
- drug interaction(s) of NSAIDs with glucocorticoid
- drug interaction(s) of NSAIDs, diuretics & angiotensin II receptor antagonists
- drug interaction(s) of NSAIDs, diuretics & ACE inhibitors
- drug interaction(s) of NSAIDs with ACE inhibitors
- drug interaction(s) of NSAIDs & antihypertensives
- drug interaction(s) of NSAIDs & loop diuretics
- drug interaction(s) of NSAIDs & aspirin
Laboratory
Mechanism of action
- non-specific inhibition of cyclo-oxygenase (COX-1 & COX-2)
- weak anti-platelet activity (weaker than naproxen)
More general terms
More specific terms
Additional terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 4.0 4.1 Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed, WB Saunders, Philadelpha 1995
- ↑ Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Journal Watch 21(18):143-44, 2001
- ↑ 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: https://www.ncbi.nlm.nih.gov/pubmed/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: https://www.ncbi.nlm.nih.gov/pubmed/15468367 - ↑ Prescriber's Letter 15(1): 2008 New Topical NSAIDs: Voltaren Gel and Flector Patch Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=240104&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ FDA MedWatch Voltaren Gel (diclofenac sodium topical gel) 1% - Hepatic Effects Labeling Changes http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm193047.htm
- ↑ 10.0 10.1 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#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260405&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 11.0 11.1 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:http://dx.doi.org/ 10.1161/CIRCOUTCOMES.109.861104 http://circoutcomes.ahajournals.org/cgi/rapidpdf/CIRCOUTCOMES.109.861104v1.pdf
- ↑ Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Deprecated Reference
- ↑ 14.0 14.1 Prescriber's Letter 21(2): 2014 Comparison of Diclofenac Products Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=300205&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 15.0 15.1 Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
- ↑ 16.0 16.1 Schmidt M, Sorensen HT, Pedersen L Diclofenac use and cardiovascular risks: series of nationwide cohort studies. BMJ 2018;362:k3426 PMID: https://www.ncbi.nlm.nih.gov/pubmed/30181258 https://www.bmj.com/content/362/bmj.k3426