Etoricoxib

BRAND NAMES:

ARCOXIA: ARCOXIA medication, containing etoricoxib, is used to treat osteoarthritis and rheumatoid arthritis symptoms both acutely and chronically. Available strengths include 30 mg, 60 mg, 90 mg, and 120 mg.

NUCOXIA MR: It is a combination of Etoricoxib 60 mg, and thiocolchicoside 4 mg used to reduce pain and relax muscles.

Etoford P: Etoford P is the combination of Etoricoxib 60 mg and Paracetamol 325 mg, used to relieve pain and inflammation with ankylosing spondylitis, rheumatoid arthritis, and osteoarthritis.

MECHANISM OF ACTION:

Etoricoxib, like any other selective COX-2 inhibitor ("coxib"), inhibits only isoform 2 of the cyclooxygenase (COX-2). It inhibits COX-2 more selectively than COX-1 by approximately 106 times. It lowers the production of prostaglandins (PGs) from arachidonic acid. Compared to standard non-steroidal anti-inflammatory medicines (NSAID), selective COX-2 inhibitors have reduced activity on COX-1. Reduced exercise is the reason for decreased gastrointestinal side effects.

PHARMACOKINETICS:

Etoricoxib is easily absorbed from the gastrointestinal tract after oral administration. Peak plasma concentrations are attained in about an hour in fasted people; meal slows absorption by about 2 hours but has no effect on the extent of absorption. Plasma protein binding is approximately 92%. Etoricoxib has a half-life of roughly 22 hours in steady-state conditions. Etoricoxib is highly metabolized, with less than 2% of a given dose recovered in urine as the parent substance. The primary mode of metabolism is via cytochrome P450 isoenzymes, particularly CYP3A4, to create the 6'-hydroxymethyl derivative of etoricoxib, which is then oxidized to the 6'-carboxylic acid derivative, the main metabolite. Both are inactive or weak COX-2 inhibitors. Excretion occurs primarily through urine (70%), with just 20% of a dosage in the feces. 

CONTRAINDICATIONS:

Etoricoxib is also not recommended for patients with inflammatory bowel disorders, moderate to severe heart failure, or renal impairment with a creatinine clearance of less than 30 mL/min. When delivering etoricoxib to dehydrated individuals, exercise caution; it may be necessary to rehydrate patients before administering etoricoxib.

DRUG INTERACTIONS:

Etoricoxib may interact with:

• Antiasthmatics: Salbutamol
• Diuretics
• Antihypertensive: losartan, minoxil, valsartan, ramipril, and enalapril
• Anticoagulants: Aspirin, Warfarin
• Oral contraceptives
• Antibiotics: Rifampicin
• Antiarrhythmics: Digoxin
• Immuno-suppressants: Methotrexate

SIDE EFFECTS:

Etoricoxib's common side effects:

• Swelling in legs
• Stomach pain
• Irregular heartbeat and rhythm
• Constipation
• Mouth ulcers
• Increased blood pressure
• Indigestion
• Peripheral edema
• Difficulty breathing

Severe side effects include:

• Breathing issues such as wheezing or shortness of breath.
• If you have severe stomachache, black stools, blood in your vomit, or bleeding while urinating.
• Any signs of an allergic reaction, such as swelling around the lips or face or a severe itchy skin rash.

TOXICITY:

This lowered activity is the reason for lower gastrointestinal toxicity, as established in multiple large clinical trials. Some clinical trials and meta-analyses demonstrated that therapy with COXIB caused an increased incidence of cardiovascular adverse events compared to placebo.

STORAGE CONDITIONS:

Store at temperatures 68 ̊ F and 77 ̊ F (20 ̊ C and 25 ̊ C) and keep away from sunlight, heat, and moisture.