LODINE XL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LODINE XL (LODINE XL).
Nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2), reducing prostaglandin synthesis leading to anti-inflammatory, analgesic, and antipyretic effects.
| Metabolism | Hepatic metabolism primarily via CYP2C9 and CYP2C8 isoenzymes; also undergoes conjugation (glucuronidation). |
| Excretion | Renal excretion of metabolites accounts for approximately 70% of a dose; fecal excretion accounts for about 20%. |
| Half-life | Terminal elimination half-life is approximately 6-7 hours. Steady-state is achieved within 2 days. |
| Protein binding | More than 99% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 0.4 L/kg, indicating distribution primarily in extracellular fluid. |
| Bioavailability | Oral bioavailability is approximately 100% (complete absorption). |
| Onset of Action | Oral administration: onset of analgesic effect within 30 minutes to 1 hour. |
| Duration of Action | Duration of action is approximately 12-24 hours for pain relief, allowing once-daily dosing. |
400 mg or 600 mg orally once daily.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | GFR 30-60 mL/min: reduce dose to 200 mg once daily; GFR <30 mL/min: contraindicated. |
| Liver impairment | Child-Pugh class B or C: contraindicated. |
| Pediatric use | Not approved for use in pediatric patients. |
| Geriatric use | Initiate at 200 mg once daily; maximum 400 mg once daily. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LODINE XL (LODINE XL).
| Breastfeeding | Trace amounts of etodolac are excreted into breast milk; M/P ratio unknown. Due to low levels and short half-life, it is considered compatible with breastfeeding when used at low doses for short term. Caution in preterm infants or those with renal impairment. Monitor infant for rash, gastrointestinal effects. |
| Teratogenic Risk | NSAIDs including LODINE XL (etodolac) are associated with increased risk of oligohydramnios and premature closure of the ductus arteriosus in the third trimester. Avoid use after 30 weeks gestation. First and second trimester use should be limited to lowest effective dose and shortest duration due to potential risks of miscarriage and congenital anomalies (cardiac, gastroschisis). |
■ FDA Black Box Warning
NSAIDs cause an increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors may be at greater risk. LODINE XL is contraindicated for treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery. NSAIDs cause an increased risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These events can occur at any time during use and without warning symptoms. Elderly patients and patients with prior history of peptic ulcer disease and/or GI bleeding are at greater risk.
| Serious Effects |
History of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs; perioperative pain in the setting of coronary artery bypass graft (CABG) surgery; known hypersensitivity to etodolac or any component of the formulation; advanced renal disease (unless benefit outweighs risk); history of GI bleeding or perforation related to previous NSAID therapy; active peptic ulcer disease or GI bleeding.
| Precautions | Cardiovascular thrombotic events, gastrointestinal bleeding/ulceration/perforation, hepatotoxicity, hypertension, fluid retention and edema, renal toxicity (including renal papillary necrosis and other renal injury), anaphylactoid reactions, serious skin adverse reactions (e.g., exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis), hematologic toxicity (inhibition of platelet aggregation, prolonged bleeding time), exacerbation of asthma, photosensitivity, and use in pregnancy (avoid in third trimester due to premature closure of ductus arteriosus). |
Loading safety data…
| Fetal Monitoring | Monitor maternal renal function, blood pressure, and signs of bleeding. Fetal ultrasound to assess amniotic fluid index if used beyond 20 weeks gestation; decelerations or oligohydramnios may require discontinuation. Monitor ductus arteriosus if used near term. |
| Fertility Effects | Etodolac may delay or inhibit ovulation due to prostaglandin synthesis inhibition; consider in patients attempting conception. Reversible effect upon discontinuation. |