Dosing and uses of Lodine (etodolac)
Adult dosage forms and strengths
tablet
- 400mg
- 500mg
capsule
- 200mg
- 300mg
tablet, extended-release
- 400mg
- 500mg
- 600mg
Pain
Immediate release: 200-400 mg PO q6-8hr; not to exceed 1000 mg/day (not evaluated)
Osteoarthritis
Immediate release: 600-1000 mg/day PO divided q8-12hr or 900 mg/day PO divided q8hr; doses >1000 mg/day not evaluated
Extended release: 400-1000 mg PO once daily; not to exceed 1200 mg/day (not evaluated)
Rheumatoid Arthritis
Immediate release: 600-1000 mg/day PO divided q8-12hr or 900 mg/day PO divided q8hr; doses >1000 mg/day not evaluated
Extended release: 400-1000 mg PO once daily; not to exceed 1200 mg/day (not evaluated)
Dosing Considerations
Take with food or 8-12 oz of water to avoid gastrointestinal (GI) effects
<60 kg: Not to exceed 20 mg/kg PO
Mild-to-moderate renal impairment: Dose adjustment not necessary
Severe renal impairment; Not recommended
Hepatic impairment: Dose adjustment not necessary
Malignant Glioma (Orphan)
Orphan designation for treatment of malignant glioma (plus propranolol)
Sponsor
- Vicus Therapeutics, LLC; 55 Madison Avenue, Suite 400; Morristown, NJ 07960
Pediatric dosage forms and strengths
tablet, extended-release
- 400mg
- 500mg
- 600mg
Juvenile Rheumatoid Arthritis
<6 years
- Safety and efficacy not established
6-16 years
- 20-30 kg (extended release): 400 mg PO once daily
- 31-45 kg (extended release): 600 mg PO once daily
- 46-60 kg (extended release): 800 mg PO once daily
- >60 kg (extended release): 1000 mg PO once daily
Dosing considerations
- Safety and effectiveness of conventional tablets for juvenile rheumatoid arthritis not established
Lodine (etodolac) adverse (side) effects
1-10%
Dyspepsia (10%)
Dizziness (3-9%)
Nervousness (1-3%)
Pruritus (1-3%)
Blurred vision (1-3%)
Depression (1-3%)
Chills/fever (1-3%)
>1%
Asthenia, malaise
Blurred vision
Bronchospasm
Dysuria, urinary frequency
Edema
Melena
Rash
Tinnitus
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 risk factors for or existing cardiovascular 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
- Aspirin allergy
- Perioperative pain associated with coronary artery bypass graft
- Previous allergic reactions or asthma after taking aspirin or other NSAIDs
Cautions
Use caution in patients with history of asthma (bronchial)
Caution in bleeding disorder, duodenal/gastric/peptic ulcer, stomatitis, systemic lupus erythematosus, ulcerative colitis, upper GI disease, late pregnancy (may cause premature closure of ductus arteriosus)
Use with caution in cardiac disease, hepatic and renal impairment
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
Advanced renal disease: Monitor closely
Risk of severe GI toxicities, including inflammation, ulcers, bleeding, and perforation
Increased risk of serious cardiovascular thrombotic events, MI, and stroke
Heart Failure risk
- NSAIDS have the potential to trigger HF by prostaglandin inhibition that leads tosodium 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 and lactation
Pregnancy category: C; avoid in late pregnancy (may cause premature closure of ductus arteriosus)
Quebec Pregnancy Registry identified 4705 women who had a spontaneous abortion by 20 weeks' gestation; each case was matched to 10 control subjects (n=47,050) who had not had a spontaneous abortion; exposure to nonaspirin NSAIDs during pregnancy was documented in approximately 7.5% of cases of spontaneous abortion and approximately 2.6% of controls
Lactation: Unknown whether drug is 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 of Lodine (etodolac)
Mechanism of action
Inhibits synthesis of prostaglandins in body tissues by inhibiting at least 2 cyclo-oxygenase (COX) isoenzymes, COX-1 and COX-2
May inhibit chemotaxis, alter lymphocyte activity, decrease proinflammatory cytokine activity, and inhibit neutrophil aggregation; these effects may contribute to anti-inflammatory activity
Absorption
Bioavailability: 80-100%
Onset: 2-4 hr
Duration: 4-6 hr
Peak plasma time: Immediate release, 1-2 hr (adults); extended release, 5-7 hr (children)
Distribution
Protein bound: ≥99%
Vd: 0.4 L/kg (Immediate release); 0.57 L/kg (adults; extended release) or 0.08 L/kg (children; extended release)
Metabolism
Hepatic
Metabolites: Hydroxylated metabolites (6-, 7-, 8-OH), hydroxylated metabolite glucuronides, unidentified metabolites (33%)
Elimination
Half-life: Immediate release, 5-8 hr (adults); extended release, 12 hr (children)
Dialyzable: No
Excretion: Urine (73%), feces (16%)
