Dosing & Uses
Dosage Forms & Strengths
tablet as potassium
- 50mg (Cataflam)
tablet delayed release as sodium
- 25mg
- 50mg
- 75mg
tablet, extended-release
- 100mg (Voltaren XR)
capsule
- 18mg (Zorvolex)
- 25mg (Zipsor)
- 35mg (Zorvolex)
powder packet for oral solution
- 50mg packet (Cambia)
solution for IV injection
- 37.5mg/mL (Dyloject)
Rheumatoid Arthritis
Diclofenac potassium: 50 mg PO q8-12hr
Diclofenac sodium: 50 mg PO q8hr or 75 mg PO q12hr
Extended release: 100 mg PO once daily; may be increased to 100 mg PO q12hr
Osteoarthritis
Diclofenac potassium: 50 mg PO q8-12hr
Diclofenac sodium: 50 mg PO q8hr or 75 mg PO q12hr
Extended release: 100 mg PO once daily; may be increased to 100 mg PO q12hr
Zorvolex: 35 mg PO TID
Ankylosing Spondylitis
Diclofenac sodium: 25 mg PO 4 or 5 times daily
Diclofenac potassium: 50 mg PO q12hr
Dysmenorrhea
Immediate-release (Cataflam): 100 mg PO once, then 50 mg PO q8hr PRN
Mild-to-Moderate Acute Pain
Immediate-release tab (Cataflam): 100 mg PO once, then 50 mg PO q8hr PRN
Zipsor: 25 mg PO QID PRN
Zorvolex: 18 mg or 35 mg PO TID
Pain (IV Administration)
Indicated for management of mild-to-moderate pain and moderate-to-severe pain alone or in combination with opioid analgesics
Use for the shortest duration consistent with individual patient treatment goals
37.5 mg IV bolus injection infused over 15 seconds q6hr as needed, not to exceed 150 mg/day
To reduce the risk of renal adverse reactions, patients must be well hydrated prior to IV administration
Acute Migraine
Oral solution: 50 mg (1 packet) in 30-60 mL of water, mixed well and drunk immediately
Not for prophylaxis
Dosing Considerations
Diclofenac potassium: Cambia, Cataflam, Zipsor
Diclofenac sodium: Voltaren XR
Administration
Take with food or 8-12 oz of water to avoid GI adverse effects
Zorvolex: Take on empty stomach; food decreases AUC by 11% and peak concentration by 60%
Oral solution: Do not use liquids other than water to reconstitute; foods decrease effectiveness
May be combined with misoprostol
Dosage Forms & Strengths
tablet as potassium
- 50mg
tablet delayed release as sodium
- 25mg
- 50mg (Cataflam)
- 75mg
tablet, extended-release
- 100mg (Voltaren XR)
powder packet for oral solution
- 50mg packet (Cambia)
Juvenile Idiopathic arthritis (Off-label)
Safety and efficacy not established; drug has been used safely in limited number of children aged 3-16 years with juvenile rheumatoid arthritis
<3 years: Safety and efficacy not established
≥3 years: 2-3 mg/kg/day for up to 4 weeks
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
Frequency Not Defined
Abdominal distention and flatulence
Abdominal pain or cramps
Constipation
Diarrhea
Dizziness
Dyspepsia
Edema
Fluid retention
Headache
Nausea
Peptic ulcer or GI bleeding
Pruritus
Rash
Tinnitus
Acute hepatitis
Agranulocytosis
Asthma
Aplastic anemia
Asymptomatic hepatitis
Blood urea nitrogen (BUN) >40 mg/dL (>14.3 mmol/L)
Cholestasis
Chronic active hepatitis
Congestive heart failure (CHF)
Decreased hemoglobin
Epistaxis
Fatal fulminant hepatitis
Hemolytic anemia (may be autoimmune)
Hepatocellular necrosis
Hypertension
Jaundice
Leukopenia
Nephrotoxicity
Purpura
Serum creatinine >2 mg/dL (>177 μmol/L)
Thrombocytopenia
Warnings
Black Box Warnings
Cardiovascular risk
- Nonsteroidal anti-inflammatory drugs (NSAIDs) may increase risk of serious cardiovascular thrombotic events, myocardial infarction (MI), and stroke, which can be fatal
- Risk may increase with duration of use
- Patients with existing cardiovascular disease or risk factors for such disease may be at greater risk
- NSAIDs are contraindicated for perioperative pain in setting of coronary artery bypass graft (CABG) surgery
Gastrointestinal risk
- NSAIDs increase risk of serious GI adverse events, including bleeding, ulceration, and gastric or intestinal perforation, which can be fatal
- GI adverse events may occur at any time during use and without warning symptoms
- Elderly patients are at greater risk for serious GI events
Contraindications
Absolute: Hypersensitivity to diclofenac, history of aspirin triad, treatment of perioperative pain associated with CABG; active gastrointestinal bleeding
IV: Moderate-to severe renal insufficiency in the perioperative period and patients who are at risk for volume depletion
Zipsor capsules are contraindicated in patients with history of hypersensitivity to bovine protein
Cautions
Use caution in patients with bronchospasm, cardiac disease, CHF, hepatic porphyria, hypertension, fluid retention, severe renal impairment, smoking, systemic lupus erythematosus
Platelet aggregation and adhesion may be decreased; may prolong bleeding time
Use caution in blood dyscrasias or bone marrow depression; also with thrombocytopenia, agranulocytosis, and aplastic anemia
Long-term administration of NSAIDs may result in renal papillary necrosis and other renal injury; patients at greatest risk include elderly individuals, those with impaired renal function, hypovolemia, heart failure, liver dysfunction, or salt depletion, and those taking diuretics, angiotensin-converting enzyme inhibitors, or angiotensin-receptor blockers
Therapy may increase risk of hyperkalemia, especially in renal disease, diabetics, the elderly, and concomitant use of agents that may induce hyperkalemia; monitor potassium closely
May cause dizziness blurred vision and neurologic effects that may impair physical and mental abilities
Risk of serious skin reactions, including Stevens Johnson syndrome and necrotizing enterocolitis
Persistent urinary symptoms, including bladder pain and dysuria, hematuria or cystitis may occur after initiating therapy; discontinue therapy with symptom onset and evaluate cause
Increase in transaminase levels reported within 2 months of therapy; may occur at any time; monitor transaminase levels periodically beginning 4-8 weeks after initiation of therapy
May increase risk of aseptic meningitis (rare), especially in patients with systemic lupus erythrmatosus, and mixed connective tissue disorders
Use caution if patient dehydrated before initiating therapy; rehydrate patient before initiating therapy and monitor renal function closely
Injectable dosage form not recommended for long-term use
Overuse of acute migraine drugs (eg, ergotamine, triptans, opioids, nonsteroidal anti-inflammatory drugs or combination of these drugs for 10 or more days per month) may lead to exacerbation of headache (medication overuse headache); may present as migraine-like daily headaches or as a marked increase in frequency of migraine attacks; detoxification of patients, including withdrawal of overused drugs and treatment of withdrawal symptoms (which often includes a transient worsening of headache) may be necessary
Different formulations not bioequivalent even if milligram strength the same; do not interchange products
Withhold for at least 4-6 half-lives prior to surgical or dental procedures
Heart failure risk
- NSAIDS have the potential to trigger HF by prostaglandin inhibition that leads to sodium and water retention, increased systemic vascular resistance, and blunted response to diuretics
- NSAIDS should be avoided or withdrawn whenever possible
- AHA/ACC Heart Failure Guidelines; Circulation. 2016;134
Pregnancy & Lactation
Pregnancy category: C; avoid use in late pregnancy (may cause premature closure of ductus arteriosus); category D if >30 weeks after gestation
Quebec Pregnancy Registry identified 4705 women who had spontaneous abortions by 20 weeks' gestation; each case was matched to 10 control subjects (n=47,050) who had not had spontaneous abortions; exposure to nonaspirin NSAIDs during pregnancy was documented in approximately 7.5% of cases of spontaneous abortions and approximately 2.6% of controls
Lactation: Excreted in breast milk; not recommended
Pregnancy Categories
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Pharmacology
Mechanism of Action
Inhibits cyclooxygenase (COX)-1 and COX-2, thereby inhibiting prostaglandin synthesis
May also inhibit neutrophil aggregation/activation, inhibit chemotaxis, decrease proinflammatory cytokine level, and alter lymphocyte activity
Absorption
~100% absorbed
Bioavailability: 50-60%
Peak plasma time: Oral solution, 10-30 min; prompt-release tablet/capsule, 1 hr; extended-release tablet, 2-3 hr
Peak plasma concentration (50 mg dose): 1-1.5 mcg/mL
Onset of action: potassium salt faster acting than sodium salt (dissolves in stomach instead of duodenum)
Distribution
Protein bound: 99-99.8%
Vd: 1.3-1.4 L/kg
Metabolism
Metabolized in liver by hydroxylation and conjugation with glucuronic acid, taurine amide, sulfuric acid, and other biogenic ligands, as well as conjugation of unchanged drug
Metabolites: 3'-hydroxydiclofenac, 4'-hydroxydiclofenac (3'-hydroxy-4'-methoxydiclofenac), 5-hydroxydiclofenac, 4',5-dihydroxydiclofenac
Enzymes inhibited: COX-1, COX-2
Elimination
Half-life: 1.2-2 hr
Clearance: 263-350 mL/min
Excretion: Urine (50-70%), feces (30-35%)
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Formulary
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