Etodolac

Trade Names:Etodolac- Capsules 200 mg- Capsules 300 mg- Tablets 400 mg- Tablets 500 mg- Tablets, extended-release 400 mg- Tablets, extended-release 500 mg- Tablets, extended-release 600 mg

Pharmacology

Decreases inflammation, pain, and fever, probably through inhibition of cyclooxygenase activity and prostaglandin synthesis.

Pharmacokinetics

Absorption

Well-absorbed. Bioavailability is 80% or more. C _max is approximately 14 to 37 mcg/mL. T _max is approximately 1.4 h. Food decreases C _max approximately 50% and increases T _max by 1.4 to 3.8 h.

Distribution

Vd is approximately 390 mL/kg. More than 99% protein bound.

Metabolism

Extensively metabolized in the liver.

Elimination

Terminal t _½ is 6.4 h. Cl is 49 mL/h/kg. Approximately 72% is recovered in the urine, with 1% as unchanged drug; 16% is excreted in feces.

Special Populations

Cl may be reduced.

50% greater apparent Cl of total etodolac.

Indications and Usage

Relief of mild to moderate pain; relief of signs and symptoms of rheumatoid arthritis and osteoarthritis.

Contraindications

Treatment of perioperative pain in the setting of coronary artery bypass graft surgery; patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs; hypersensitivity to any component of the product.

Dosage and Administration

PO 200 to 400 mg q 6 to 8 h as needed. Dosages more than 1,000 mg/day have not been adequately evaluated.

PO 300 mg twice daily or 3 times daily, or 400 or 500 mg twice daily. Dosages more than 1,000 mg/day have not been adequately evaluated.

General Advice

• Food delays peak action of medication by 1 to 4 h. Give with food, milk, or antacids if stomach upset occurs.

Storage/Stability

Store at 68° to 77°F. Dispense in tight, light-resistant container. Protect from moisture.

Drug Interactions

Antihypertensive effect of ACE inhibitors may be diminished.

May increase PT. Watch for signs and symptoms of bleeding.

Protein binding of etodolac may be reduced; in addition, the risk of gastric erosion and bleeding may be increased.

May decrease diuretic effect.

May increase lithium levels and effects.

May increase methotrexate levels.

Laboratory Test Interactions

Drug may cause small decrease.

Drug may cause false-positive results.

Drug may cause results that are false positive for ketones.

Adverse Reactions

Cardiovascular

Vasculitis (postmarketing).

CNS

Dizziness, headache (1% to 10%); asthenia, depression, malaise, nervousness (at least 1%).

Dermatologic

Pruritus, rash (1% to 10%); cutaneous vasculitis with purpura, erythema multiforme, hyperpigmentation, Stevens-Johnson syndrome, toxic epidermal necrolysis (postmarketing).

EENT

Tinnitus (1% to 10%); blurred vision (at least 1%).

GI

Abdominal pain, constipation, diarrhea, dyspepsia, flatulence, GI ulcers, gross bleeding/perforation, heartburn, nausea, vomiting (1% to 10%); gastritis, melena (at least 1%).

Genitourinary

Abnormal renal function (1% to 10%); dysuria, urinary frequency (at least 1%); elevated BUN, renal failure, renal insufficiency, renal papillary necrosis (postmarketing).

Hematologic

Anemia (1% to 10%).

Hematologic-Lymphatic

Increased bleeding time (1% to 10%); agranulocytosis, hemolytic anemia, leukopenia, neutropenia, pancytopenia (postmarketing).

Hepatic

Elevated liver enzymes (1% to 10%); cholestatic hepatitis, cholestatic jaundice, duodenitis, hepatic failure, intestinal ulceration, jaundice, liver necrosis, pancreatitis (postmarketing).

Metabolic-Nutritional

Hyperglycemia in previously controlled diabetic patients (postmarketing).

Respiratory

Pulmonary infiltration with eosinophilia (postmarketing).

Miscellaneous

Edema (1% to 10%); chills and fever (at least 1%); allergic reactions, anaphylactic/anaphylactoid reactions (postmarketing).

Precautions

Pregnancy

Category C . Avoid in late pregnancy.

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Use with caution.

Hypersensitivity

May occur; use with caution in aspirin-sensitive individuals because of possible cross-sensitivity.

Renal Function

Not recommended in patients with advanced renal disease. Acute renal insufficiency, interstitial nephritis, hyperkalemia, hyponatremia, and renal papillary necrosis may occur.

Hepatic Function

Cl may be reduced in patients with severe hepatic failure.

Special Risk Patients

Use with caution in patients with fluid retention or heart failure.

Anaphylactoid reactions

Do not administer to patients with aspirin triad, which occurs typically in asthmatic patients who experience rhinitis with or without nasal polyps, or in patients who exhibit severe, potentially fatal bronchospasm after taking aspirin or other NSAIDs.

Asthma

Patients with asthma may have aspirin-sensitive asthma, which may be associated with severe and sometimes fatal bronchospasm. Do not administer etodolac to patients with this type of aspirin sensitivity and use with caution in patients with preexisting asthma.

Hypertension

New hypertension or worsening of preexisting hypertension, either of which may contribute to increased risk of CV events, may occur.

Platelet function

NSAIDs inhibit platelet aggregation and have been reported to prolong bleeding time.

Skin reactions

Serious and sometimes fatal skin adverse reactions, including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis, may occur.

Overdosage

Symptoms

Acute renal failure, anaphylactoid reactions, drowsiness, epigastric pain, GI bleeding, hypertension, lethargy, nausea, respiratory depression, vomiting.

Patient Information

• Advise patient to discontinue drug and immediately notify health care provider if any of the following occur: persistent or recurrent GI upset or stomach pain, skin rash or itching, vomiting blood, bloody or black stools, rapid weight gain or swelling, changes in urine patterns, joint pain, fever, bleeding or unusual bruising, unexplained tiredness or fatigue, intestinal flu-like symptoms, yellowing of the skin or eyes, visual changes.
• Advise patient to seek emergency medical assistance if any of the following occur: shortness of breath or trouble breathing, chest pain, weakness in one part or on one side of body, slurred speech, swelling of the face or throat.
• Advise patient to inform health care provider or dentist of medication regimen before treatment or surgery.
• Caution patient not to use aspirin or drink alcoholic beverages while taking this medication.
• Advise patient that drug may cause drowsiness and to use caution while driving or performing tasks requiring mental alertness.

Copyright © 2009 Wolters Kluwer Health.