Functional class
Func. class.: Nonsteroidal antiinflam- matory products (NSAIDs), nonopioid analgesic
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Drug reference
Func. class.: Nonsteroidal antiinflam- matory products (NSAIDs), nonopioid analgesic
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Chem. class.: Phenylacetic acid
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Do not confuse: Cataflam/Catapres
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ACTION: Inhibits COX-1, COX-2 by blocking arachidonate, resulting in analgesic, antiinflammatory, antipyretic effects
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USES: Acute, chronic RA; osteoarthri- tis; ankylosing spondylitis; analgesia; D primary dysmenorrhea; patch: mild to moderate pain
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CONTRAINDICATIONS: Hyper- sensitivity to aspirin, iodides, other NSAIDs, bovine protein, asthma, serious CV disease; eczema, exfoliative dermatitis, skin abra- sions (gel, patch); treatment of periopera- tive pain in CABG surgery Precautions: Pregnancy, breastfeeding, children, bleeding disorders, GI disorders, cardiac disorders, hypersensitivity to other antiinflammatory agents, CCr <30 mL/min, accidental exposure, acute bronchospasm, hypersensitivity to benzyl alcohol
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Black Box Warning: GI bleeding/perfora- tion, MI, stroke Black Box Warning: Stroke/MI: may in- crease HF and hypertension; increased CV thrombotic events, which may be fatal; those with CV disease may be at greater risk • Pain: location, character, aggravating/ alleviating factors, ROM prior to and 1 hr after dose • Actinic keratosis: check lesions prior to use and periodically • LFTs (may be elevated), uric acid (may be decreased—serum; increased—urine) periodically; also BUN, creatinine, electro- lytes (may be elevated) • Serious skin disorders/anaphy- laxis: if rash develops, discontinue im- mediately, may be fatal; patients with asthma, aspirin hypersensitivity, nasal polyps may develop hypersensitivity • GI bleed: Increased risk for peptic/du- odenal ulceration, perforation, obstruc- tion, GI bleeding • Blood dyscrasias (thrombocytopenia): Bruising, fatigue, bleeding, poor healing; blood counts during therapy; watch for decreasing platelets; if low, therapy may need to be discontinued and restarted after hematologic recovery; check stool guaiac • Beers: avoid chronic use in older adults unless other alternatives are inef- fective; increased risk of GI bleeding • Pregnancy/breastfeeding: use only if benefit outweighs fetal risks <30 wk, do not use after 30 wk; discontinue breast- feeding, excretion is unknown
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SIDE EFFECTS CNS: Dizziness, headache CV: HF, MI, stroke, edema EENT: Tinnitus GI: Nausea, anorexia, vomiting, diarrhea, constipation, flatulence, GI bleeding, hepatotoxicity GU: Nephrotoxicity: hematuria HEMA: Anemia, blood dyscrasias INTEG: Rash, pruritus, photosensitivity SYST: Anaphylaxis, Stevens-Johnson syndrome, exfoliative dermatitis, toxic epidermal necrolysis
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INTERACTIONS • Need for dosage adjustment: antidiabetics Increase: hyperkalemia—potassium- sparing diuretics Increase: anticoagulant effect—antico- agulants, NSAIDs, platelet inhibitors, salicylates, thrombolytics, SSRIs Increase: toxicity—phenytoin, lithium, cycloSPORINE, methotrexate, digoxin, lithium, cidofovir Increase: GI side effects—aspirin, other NSAIDs, bisphosphonates, corticosteroids Decrease: antihypertensive effect—beta- blockers, diuretics, ACE inhibitors Decrease: effect of diuretics Drug/Herb Increase: bleeding risk—garlic, ginger, ginkgo; monitor for bleeding
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DOSAGE AND ROUTES Osteoarthritis • Adult: PO (diclofenac potassium/ delayed-release diclofenac sodium) 50 mg bid-tid, max 150 mg/day; DELAYED RE- LEASE 50 mg bid-tid or 75 mg bid, max 150 mg/day; EXTENDED RELEASE (ex- tended-release diclofenac sodium) 100 mg daily, max 150 mg/day; TOPICAL GEL 1% 4 g for each of lower extremities qid, max 16 g/day; 2 g for each of upper extremities qid, max 8 g/day; TOPICAL SOL apply 40 drops to each affected knee qid; apply 10 drops at a time, spread over entire knee Rheumatoid arthritis • Adult: PO (diclofenac potassium/de- layed-release diclofenac sodium) 50 mg tid- qid, max 200 mg/day; DELAYED RELEASE 50 mg tid-qid or 75 mg bid, max 200 mg/ day; EXTENDED RELEASE (extended-re- lease diclofenac sodium) 100 mg daily, may increase to 200 mg/day, max 200 mg/day Ankylosing spondylitis • Adult: PO DELAYED RELEASE (de- layed-release diclofenac sodium) 25 mg qid and 25 mg at bedtime, max 125 mg/day Acute migraine with/without aura • Adult: PO (powder for oral solution) 50 mg as a single dose, mix contents of packet in 1-2 oz water Mild to moderate pain • Adult: PO (diclofenac potassium) 25 mg qid Dysmenorrhea or nonrheumatic inflammatory conditions • Adult: PO (diclofenac potassium) 50 mg tid or 100 mg initially, then 50 mg tid, max 200 mg first day, then 150 mg/day, immediate release only Pain of strains/sprains • Adult: TOPICAL PATCH apply patch to area bid Actinic keratosis • Adult: TOPICAL GEL apply to area bid Hepatic dose • Adult: PO Moderate to severe hepatic impairment: use not recommended Renal dose • Avoid: Use of topical gel, patch, solution, potassium oral tablet for advanced renal disease
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Available forms: Epolamine: topical patch 1.3%; potassium: tablets 50 mg; tablets, liquid filled 25 mg; oral powder for solution 50 mg; sodium: delayed-release tablets (enteric-coated) 25, 50, 75 mg; Pennsaid: extended-release tablets, 100 mg
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Administer: PO route • Do not break, crush, or chew enteric products • Take with a full glass of water to en- hance absorption, remain upright for ½ hr; if dose is missed, take as soon as re- membered within 2 hr if taking 1-2×/ day; do not double doses • Allow 6 hr between use with another NSAID • Store at room temperature Powder: • Mix powder in 30-60 mL water only • Mix solution; have patient drink im- mediately • Powder (Cambia) and Zorvolex may be less effective if taken with food; Zor- volex capsules are not interchangeable with other formulations of oral product Topical patch route • Wash hands before handling patch • Remove and release liner prior to ad- ministration • Use only on normal, intact skin • Remove before bath, shower, swimming; do not use heat or occlusive dressings • Discard removed patch in trash away from children, pets • Store at room temperature Topical gel route • Apply to intact skin; do not use heat or occlusive dressings • Use only for osteoarthritis, mild to moderate pain • Store at room temperature, avoid heat, do not freeze Topical solution route • Apply to clean, dry skin • Wait until dry before applying clothing, other creams/lotions • Wait ≥30 min after use before bathing, swimming • Store at room temperature
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Assess: • CABG: do not use oral, topical, gel, patch in perioperative pain in coronary ar- tery bypass graft surgery for 10-14 days
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Evaluate: • Therapeutic response: decreased in- flammation in joints, after cataract surgery D
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That product must be continued for prescribed time to be effective; to contact prescriber prior to surgery regarding when to discontinue this product • To report bleeding, bruising, fatigue, malaise; blood dyscrasias do occur • To notify prescriber immediately, stop product if rash occurs • To avoid aspirin, alcoholic beverages, NSAIDs, or other OTC medications unless approved by prescriber • To take with food, milk, or antacids to avoid GI upset; to swallow whole • To use caution when driving; drowsi- ness, dizziness may occur • To hepatotoxicity: report flulike symptoms, nausea, vomiting, jaundice, pruritus, lethargy • To use sunscreen to prevent photosen- sitivity • To notify all providers of product use • To notify prescriber if pregnancy is planned or suspected • Stroke/MI: to notify prescriber imme- diately, seek medical attention if chest pain, slurred speech, weakness, short- ness of breath occur • Gel: to use dosing card to measure; not to apply where cosmetics, sunscreen have been applied • Transdermal: not to use in water (swimming/bathing); to use only on intact skin; not to cover with occlusive dressing; to apply adhesive tape or mesh sleeve if patch begins to peel off See Appendix B
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PHARMACOKINETICS PO: Peak 2-3 hr; TOPICAL Patch: Peak 12 hr; elimination half-life 1-2 hr, patch 12 hr, 99% bound to plasma proteins, metabolized in liver to metabolite, excreted in urine
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• Adult: PO (diclofenac potassium/ delayed-release diclofenac sodium) 50 mg bid-tid, max 150 mg/day; DELAYED RE- LEASE 50 mg bid-tid or 75 mg bid, max 150 mg/day; EXTENDED RELEASE (ex- tended-release diclofenac sodium) 100 mg daily, max 150 mg/day; TOPICAL GEL 1% 4 g for each of lower extremities qid, max 16 g/day; 2 g for each of upper extremities qid, max 8 g/day; TOPICAL SOL apply 40 drops to each affected knee qid; apply 10 drops at a time, spread over entire knee Rheumatoid arthritis
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• Adult: PO (diclofenac potassium/de- layed-release diclofenac sodium) 50 mg tid- qid, max 200 mg/day; DELAYED RELEASE 50 mg tid-qid or 75 mg bid, max 200 mg/ day; EXTENDED RELEASE (extended-re- lease diclofenac sodium) 100 mg daily, may increase to 200 mg/day, max 200 mg/day Ankylosing spondylitis
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• Adult: PO DELAYED RELEASE (de- layed-release diclofenac sodium) 25 mg qid and 25 mg at bedtime, max 125 mg/day Acute migraine with/without aura
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• Adult: PO (powder for oral solution) 50 mg as a single dose, mix contents of packet in 1-2 oz water Mild to moderate pain
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• Adult: PO (diclofenac potassium) 25 mg qid Dysmenorrhea or nonrheumatic inflammatory conditions
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• Adult: PO (diclofenac potassium) 50 mg tid or 100 mg initially, then 50 mg tid, max 200 mg first day, then 150 mg/day, immediate release only Pain of strains/sprains
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• Adult: TOPICAL PATCH apply patch to area bid Actinic keratosis
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• Adult: TOPICAL GEL apply to area bid Hepatic dose
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• Adult: PO Moderate to severe hepatic impairment: use not recommended Renal dose
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