Indications:
● Etodolac is licensed for the treatment of inflammation and pain caused by osteoarthritis and rheumatoid arthritis.
● Etodolac is used for the treatment of inflammation and pain caused by osteoarthritis, rheumatoid arthritis, and juvenile rheumatoid arthritis.
● It is also used for treating soft tissue injuries, such as tendinitis and bursitis, and the treatment of menstrual cramps.
Drug Interaction:
They work by reducing the levels of prostaglandins, which are chemicals that are responsible for pain and the fever and tenderness that occur with inflammation. Etodolac blocks the enzyme that makes prostaglandins (cyclooxygenase), resulting in lower concentrations of prostaglandins. As a consequence, inflammation, pain and fever are reduced.
Etodolac is associated with several suspected or probable interactions that affect the action of other drugs. The following examples are the most common suspected interactions.
Etodolac may increase the blood levels of lithium (Eskalith) by reducing the elimination of lithium from the body by the kidneys. Increased levels of lithium may lead to lithium toxicity.
Etodolac may reduce the blood pressure lowering effects of blood pressure medications. This may occur because prostaglandins play a role in the regulation (lowering) of blood pressure.
When etodolac is used in combination with aminoglycosides (for example, gentamicin) the blood levels of the aminoglycoside may increase, presumably because the elimination of aminoglycosides from the body is reduced. This may lead to more aminoglycoside-related side effects. Individuals taking oral blood thinners or anticoagulants [for example, warfarin (Coumadin)] should avoid etodolac because etodolac also thins the blood, and excessive blood thinning may lead to bleeding.
Pharmacodynamics:
Etodolac is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic and antipyretic activities in animal models. The mechanism of action of Etodolac, like that of other NSAIDs, is not completely understood, but may be related to prostaglandin synthetase inhibition.
Etodolac is a racemic mixture of [-]R- and [+]S-Etodolac. As with other NSAIDs, it has been demonstrated in animals that the [+]S-form is biologically active. Both enantiomers are stable and there is no [-]R to [+]S conversion in vivo.
Pharmacokinetics:
Absorption: The systemic bioavailability of Etodolac from Etodolac tablets is 100% as compared to solution and at least 80% as determined from mass balance studies. Etodolac is well absorbed and had a relative bioavailability of 100% when 200 mg capsules were compared with a solution of Etodolac. Based on mass balance studies, the systemic availability of Etodolac is at least 80%. Etodolac does not undergo significant first-pass metabolism following oral administration. Mean (± 1 SD) peak plasma concentrations (Cmax) range from approximately 14 ± 4 mcg/mL to 37 ± 9 mcg/mL after 200 mg to 600 mg single doses and are reached in 80 ± 30 minutes. The dose-proportionality based on the area under the plasma concentration-time curve (AUC) is linear following doses up to 600 mg every 12 hours. Peak concentrations are dose proportional for both total and free Etodolac following doses up to 400 mg every 12 hours, but following a 600 mg dose, the peak is about 20% higher than predicted on the basis of lower doses. The extent of absorption of Etodolac is not affected when Etodolac is administered after a meal. Food intake, however, reduces the peak concentration reached by approximately one-half and increases the time to peak concentration by 1.4 to 3.8 hours.
Antacid Effects: The extent of absorption of etodolac is not affected when etodolac is administered with an antacid. Coadministration with an antacid decreases the peak concentration reached by about 15 to 20%, with no measurable effect on time-to-peak.
Food Effects: The extent of absorption on etodolac is not affected when etodolac is administered after a meal. Food intake, however, reduces the peak concentration reached by approximately one half and increases the time-to-peak concentration by 1.4 to 3.8 hours.
Distribution: Etodolac has an apparent steady-state volume of distribution about 0.362 L/kg. Within the therapeutic dose range, etodolac is more than 99% bound to plasma proteins. The free fraction is less than 1% and is independent of etodolac total concentration over the dose range studied.
Metabolism: Etodolac is extensively metabolized in the liver, with renal elimination of etodolac and its metabolites being the primary route of excretion. The intersubject variability of etodolac plasma levels, achieved after recommended doses, is substantial.
Protein Binding: Data from in vitro studies, using peak serum concentrations at reported therapeutic doses in humans, show that the etodolac free fraction is not significantly altered by acetaminophen, ibuprofen, indomethacin, naproxen, piroxicam, chlorpropamide, glipizide, glyburide, phenytoin, and probenecid.
Side Effects:
Upset stomach, diarrhea, gas, nausea, vomiting, constipation, fatigue, or dizziness may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.
Contraindication:
● Hypersensitivity to Thiocolchicoside or Aceclofenac or any component of the tablet.
●In patients in whom substances with a similar action (e.g. aspirin, or other NSAIDs), precipitate attacks of asthma, bronchospasm, acute rhinitis or urticaria or patients are hypersensitive to these drugs.
● Severe heart failure or severely impaired hepatic or renal organ function and during the last three months of pregnancy.
Storage :
Store at room temperature away from light and moisture.