Etogesic SR Tablet (Sustained Release)

Etogesic SR Tablet (Sustained Release) 600 mg is a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic and antipyretic properties. Its therapeutic effects are due to its ability to inhibit prostaglandin synthesis. It is indicated for relief of signs and symptoms of rheumatoid arthritis and osteoarthritis.

Etogesic SR Tablet (Sustained Release) 600 mg is an NSAID used to treat osteoarthritis and rheumatoid arthritis, as well as acute pain.

For acute and long-term management of signs and symptoms of osteoarthritis and rheumatoid arthritis, as well as for the management of pain.

• Chronic Back Pain
• Extra-Articular Rheumatism
• Juvenile Idiopathic Arthritis (JIA)
• Muscle Spasms
• Nonspecific Pain Post Traumatic Injury
• Osteoarthritis (OA)
• Pain
• Acute
• Postoperative pain
• Rheumatoid Arthritis
• Spinal Disorders

Etogesic SR Tablet (Sustained Release) 600 mg is an anti-inflammatory agent with analgesic and antipyretic properties. It is used to treat osteoarthritis, rheumatoid arthritis and control acute pain. The therapeutic effects of etodolac are achieved via inhibition of the synthesis of prostaglandins involved in fever, pain, swelling and inflammation. Etogesic SR Tablet (Sustained Release) 600 mg is administered as a racemate. As with other NSAIDs, the S-form has been shown to be active while the R-form is inactive. Both enantiomers are stable and there is no evidence of R- to S- conversion in vivo.

Similar to other NSAIDs, the anti-inflammatory effects of etodolac result from inhibition of the enzyme cycooxygenase (COX). This decreases the synthesis of peripheral prostaglandins involved in mediating inflammation. Etogesic SR Tablet (Sustained Release) 600 mg binds to the upper portion of the COX enzyme active site and prevents its substrate, arachidonic acid, from entering the active site. Etogesic SR Tablet (Sustained Release) 600 mg was previously thought to be a non-selective COX inhibitor, but it is now known to be 5 – 50 times more selective for COX-2 than COX-1. Antipyresis may occur by central action on the hypothalamus, resulting in peripheral dilation, increased cutaneous blood flow, and subsequent heat loss.

Based on mass balance studies, the systemic bioavailability of etodolac from either the tablet or capsule formulation is at least 80%.

• 390 mL/kg

> 99% bound, primarily to albumin

It is not known whether etodolac is excreted in human milk; however, based on its physical-chemical properties, excretion into breast milk is expected. Etogesic SR Tablet (Sustained Release) 600 mg is extensively metabolized in the liver. The hydroxylated-etodolac metabolites undergo further glucuronidation followed by renal excretion and partial elimination in the feces (16% of dose). Approximately 1% of a etodolac dose is excreted unchanged in the urine with 72% of the dose excreted into urine as parent drug plus metabolite.

Terminal t_1/2, 7.3 ± 4.0 hours. Distribution t_1/2, 0.71 ± 0.50 hours

• Oral cl=49.1 mL/h/kg [Normal healthy adults]
• Oral cl=49.4 mL/h/kg [Healthy males (18-65 years)]
• Oral cl=35.7 mL/h/kg [Healthy females (27-65 years)]
• Oral cl=45.7 mL/h/kg [Eldery (>65 years)]
• Oral cl=58.3 mL/h/kg [Renal impairement (46-73 years)]
• Oral cl=42.0 mL/h/kg [Hepatic impairement (34-60 years)]

Selective COX-2 inhibitors have been associated with increased risk of serious cardiovascular events (e.g. myocardial infarction, stroke) in some patients. Current data is insufficient to assess the cardiovascular risk of etodolac. Etogesic SR Tablet (Sustained Release) 600 mg may increase blood pressure and/or cause fluid retention and edema. Risk of GI toxicity including bleeding, ulceration and perforation. Risk of direct renal injury, including renal papillary necrosis. Anaphylactoid and serious skin reactions (e.g. exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis) have been reported. Common adverse events include abdominal pain, constipation, diarrhea, dyspepsia, flatulence, GI bleeding, GI perforation, nausea, peptic ulcer, vomiting, renal function abnormalities, anemia, dizziness, edema, liver function test abnormalities, headache, prolonged bleeding time, pruritus, rash, tinnitus. Symptoms of overdose include lethargy, drowsiness, nausea, vomiting, and epigastric pain.

• Avoid alcohol.
• Take with food. Food reduces irritation.

• Etogesic SR Tablet (Sustained Release) 600 mg 300 mg capsule: 600 mg daily in 1-2 divided doses
• Etogesic SR Tablet (Sustained Release) 600 mg 600 mg ER tablet: Once daily