LODINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LODINE (LODINE).
Inhibition of prostaglandin synthesis via cyclooxygenase (COX) inhibition, with selectivity for COX-2 over COX-1.
| Metabolism | Primarily hepatic via CYP2C9; undergoes conjugation; multiple metabolites including 6-hydroxyetodolac. |
| Excretion | Primarily renal (60% as metabolites, <1% unchanged); biliary/fecal (30-35%) |
| Half-life | Terminal elimination half-life approximately 7.5 hours; in elderly or renal impairment, half-life may be prolonged up to 10 hours, requiring dose adjustment |
| Protein binding | >99% bound, primarily to albumin |
| Volume of Distribution | Approximately 0.4 L/kg (range 0.3-0.5 L/kg), indicating distribution into total body water |
| Bioavailability | Oral: ~80% with extensive first-pass metabolism; absolute bioavailability not defined due to lack of IV formulation |
| Onset of Action | Oral: analgesic effect within 30-60 minutes; anti-inflammatory effect within 1-2 weeks of continuous dosing |
| Duration of Action | Analgesic duration 4-6 hours; anti-inflammatory effect sustained with regular dosing |
200 to 400 mg orally every 6 to 8 hours as needed; maximum daily dose 1200 mg.
| Dosage form | TABLET |
| Renal impairment | GFR 30-89 mL/min: no adjustment needed; GFR <30 mL/min: not recommended. |
| Liver impairment | Child-Pugh Class A or B: use with caution, consider reducing dose by 50%; Child-Pugh Class C: contraindicated. |
| Pediatric use | Not established for children under 18 years; safety and efficacy not determined. |
| Geriatric use | Initiate at lowest effective dose (e.g., 200 mg every 8-12 hours); maximum daily dose 400 mg; monitor renal function and GI bleeding risk. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LODINE (LODINE).
| Breastfeeding | Excreted in breast milk in low concentrations; M/P ratio not established. Avoid use or discontinue nursing due to potential adverse effects in infant. |
| Teratogenic Risk | Pregnancy Category C: Avoid during first and second trimester unless clearly needed; may cause premature closure of ductus arteriosus and oligohydramnios in third trimester. |
| Fetal Monitoring | Monitor maternal renal function, blood pressure, and signs of bleeding; fetal ultrasound for oligohydramnios and ductus arteriosus patency if used in third trimester. |
■ FDA Black Box Warning
Nonsteroidal anti-inflammatory drugs (NSAIDs) cause an increased risk of serious gastrointestinal adverse events including inflammation, bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. Elderly patients and patients with a prior history of peptic ulcer disease and/or GI bleeding are at greater risk.
| Serious Effects |
Hypersensitivity to etodolac or any component; history of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs; perioperative pain in the setting of coronary artery bypass graft (CABG) surgery; advanced renal disease; patients with known aspirin-sensitive asthma.
| Precautions | Cardiovascular thrombotic events (MI, stroke), especially with prolonged use or pre-existing cardiovascular disease; GI toxicity; hypertension; fluid retention; renal toxicity; hepatic dysfunction; anaphylactoid reactions; serious skin reactions; asthma exacerbation; hematologic effects; use in late pregnancy should be avoided. |
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| Fertility Effects | May impair female fertility via inhibition of prostaglandin synthesis affecting ovulation; reversible upon discontinuation. |