Etodolac

BRAND NAME:

Lodine: Lodine consists of Etodolac as the main active Ingredient, which is available in the market in tablets.

MECHANISM OF ACTION:

By reducing cyclooxygenase (COX), etodolac reduces inflammation. It lowers prostaglandins in the periphery, which fuel inflammation. Additionally, it binds to the top part of the active site of the COX enzyme, preventing the entry of arachidonic acid. It was previously believed that etodolac was a nonselective COX inhibitor; however, studies have shown that it is 5–50 times more selective for COX-2 than COX-1. Activation of the central hypothalamus can produce antipyresis by encouraging peripheral dilatation and increased cutaneous blood flow, which causes heat loss.

PHARMACOKINETICS:

Absorption: Etodolac has a systemic bioavailability greater than 80%. The peak concentration happens about 6 hours after dosing.

Distribution: 390 ml/kg is the volume of distribution. Over 99% of etodolac is bound to plasma proteins, mostly albumin, and this binding occurs regardless of the dose range and etodolac concentration.

Metabolism: It undergoes substantial metabolism in the liver. Metabolites include 6-,7-, and 8-hydroxylated etodolac and etodolac glucuronide. In a single dose of 14C-etodolac, hydroxylated metabolites were less than 10% of the total drug in serum. Under normal renal function, hydroxylated etodolac metabolites do not accumulate in the plasma. 

Excretion: Approximately 1% of an etodolac tablet dose is eliminated unaltered in the urine, whereas 72% is excreted as the parent drug.

PHARMACODYNAMICS: 

It is a Non-steroidal anti-inflammatory drug that exhibits anti-inflammatory, analgesic, and antipyretic properties. The therapeutic effect of etodolac is achieved by inhibition of the synthesis of prostaglandins. It is administered as a racemate.

DOSAGE AND ADMINISTRATION:

 Etodolac is available in the form of extended-release oral tablets of strength 400 mg, 500 mg, and 600mg, capsules, and immediate-release oral tablets of strength 400mg and 500mg. These are prescribed based on age, patient condition, and medical conditions.

Dosage for osteoarthritis:

• In adults above 18 years, the dose of immediate-release tablets starts from 300mg 2 or 3 times per day, 400mg two times per day, and 500 mg two times per day. For long-term use, 600mg per day is recommended.

• For extended-release tablets, the dosage is limited between 400 – 1000mg taken per day.

Dosage for acute pain:

• Adults with intense pain should take immediate-release oral tablets (200-400mg) every 6-8 hours.

Dosage for rheumatoid arthritis:

• For adults over 18, the suggested starting dose for rheumatoid arthritis is 300mg taken 2-3 times per day, 400mg taken twice a day, and 50mg twice daily. Long-term use may result in a daily dosage of 600mg

• For adults over 18, the recommended beginning dose for extended-release tablets is 400-1000mg once a day.

Dosage for juvenile rheumatoid arthritis:

 The starting dose of extended-release tablets for children aged between 6 to 16 is recommended based on their weight.

• Weight between 20 – 30 Kg, the recommended dose is 400mg taken once per day.

• Weight between 30-45 Kg, the recommended dose is 600mg taken once per day.

• Weight between 45 -60 Kg, the recommended dose is two 400 mg tablets taken once per day

• Above 60 kg, the are two 500 mg tablets taken once per day.

CONTRAINDICATIONS:

Etodolac extended-release pills are not recommended for people with asthma, urticarial, or hypersensitivity, as well as for the management of peri-operative discomfort.

DRUG INTERACTIONS:

Etodolac may interact with some drugs and lead to cause serious side effects. So before taking etodolac, it is needed to discuss with the health care provider the drugs which have already been used for other treatments. Below are the drugs that can cause interaction with etodolac.

• Arrhythmia drug – Digoxin may increase the risk of kidney damage.

• Blood pressure drugs – Angiotensin-converting enzyme (ACE) inhibitors will decrease the blood pressure.

• Diuretics – Furosemide and hydrochlorothiazide interacting with these drugs can reduce the diuretic effects.

• Nonsteroidal anti-inflammatory drugs – Aspirin and ketorolac used with etodolac may cause stomach bleeding and ulcers.

• Anticoagulant, blood thinner – Warfarin taken with etodolac may increase stomach bleeding.

• Disease-modifying antirheumatic drug – Methotrexate.

• Bipolar disorder drug – Etodolac may cause the quantity of lithium in your blood to grow to hazardous levels.

• Transplant drug – Cyclosporine, used together with etodolac may increase the risk of kidney damage.

FOOD INTERACTIONS:

Avoid consuming alcohol. Taking this medicine along with food can reduce the irritation.

ADVERSE EFFECTS:

•  Dizziness

•  Jaundice

•  Kidney problems

•  Stomach bleeding

•  Swelling or rapid weight gain

•  Skin ashes

•  Change in vision

•  Loss of appetite

•  Dark urine

•  Bloody tarry stools

•  Anemia

•  Headache

•  Nausea

•  Constipation

•   Upper stomach pain

•   Tiredness

•   Light headed

•   Little or no urination

•  Swelling in feet or ankles

TOXICITY:

If the medicine was taken heavily other than the prescribed dose it may lead to some toxic effects like

•  Drowsiness

•  Vomiting

•  Stomach pain

•  Stomach bleeding

•  Coma

•  Blood vomitings

•  Bloody and tarry stools

STORAGE: 

Store at ambient temperature (68℉ to 77℉/20℃ to 25℃). It can withstand temperatures ranging from 59℉ to 86℉ (15℃ to 30℃) for a limited time. Store in a cool, dry place.