Arcoxia

General information

Arcoxia is a non-steroidal anti-inflammatory drug (NSAID) with the active substance etoricoxib. It is available in the form of film-coated tablets (30, 60, 90, 120 mg). The drug selectively inhibits COX-2, providing anti-inflammatory, analgesic and antipyretic action. It is used for symptomatic treatment of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute gout and pain of various origins. It is taken orally once a day, regardless of food. Contraindicated in peptic ulcer disease, severe hepatic or renal insufficiency, cardiovascular disease, pregnancy and under 16 years of age.

Trade name: Arcoxia

International Nonproprietary Name (INN): Etoricoxib

Pattern: Film-coated tablets

Composition:

The active substance: etoricoxib in dosages of 30 mg, 60 mg, 90 mg or 120 mg in one tablet.

Auxiliary components: calcium hydrophosphate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate. The tablet shell contains substances such as hypromellose, titanium dioxide, triacetin, as well as colorants (depending on the dosage: for example, indigo carmine for 60 mg dosage or iron oxide yellow for 120 mg dosage).

The tablets have a biconvex, apple-like shape with engraving indicating the dosage (e.g., “ARCOXIA 90” and “202” for 90 mg). The color varies: 30 mg is light green, 60 mg is dark green, 90 mg is white, and 120 mg is light green.

Pharmacologic properties

Pharmacodynamics:

Arkoxia belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs), subgroup of coxibs. Etoricoxib is a highly selective inhibitor of cyclooxygenase-2 (COX-2), an enzyme involved in the synthesis of prostaglandins - mediators of inflammation, pain and fever. The drug blocks COX-2 in therapeutic doses without affecting cyclooxygenase-1 (COX-1), which minimizes the effect on the synthesis of protective prostaglandins in the gastric mucosa and platelet function. This provides a pronounced anti-inflammatory, analgesic and antipyretic effect with a lower risk of gastrointestinal complications compared to non-selective NSAIDs.

Clinical studies show that etoricoxib dose-dependently inhibits COX-2, maintaining efficacy in the daily dose range up to 150 mg with no significant effect on COX-1. The analgesic effect occurs within 24 minutes of administration and persists for up to 24 hours.

Pharmacokinetics:

Absorption: After oral administration, etoricoxib is rapidly absorbed from the gastrointestinal tract. Bioavailability is approximately 100%. Maximum plasma concentration (Cmax) is reached in 1 hour when taken on an empty stomach. Simultaneous ingestion of food may delay the achievement of Cmax by 2 hours, but does not affect the overall degree of absorption.

Distribution: Etoricoxib is well distributed in body tissues, the volume of distribution is about 120 liters. Binding to blood plasma proteins exceeds 92%, which ensures stable presence of the drug in the systemic bloodstream.

Metabolism: The drug is metabolized in the liver with the participation of cytochrome P450 isoenzymes (CYP3A4 and CYP2C9). The main pathway of metabolism is oxidation to form 6'-hydroxymethyl etoricoxib, which is then partially conjugated to glucuronic acid.

Extraction: Etoricoxib is excreted predominantly through the kidneys (70%) as metabolites and partially through the intestine (20%). The elimination half-life is about 22 hours, which allows taking the drug once a day. Less than 1% of the dose is excreted unchanged with urine. Etoricoxib is not eliminated by hemodialysis, there are no data on excretion by peritoneal dialysis.

Indications for use

The drug Arcoxia is used for symptomatic treatment of the following diseases and conditions:

• Osteoarthritis (arthrosis): control of pain and inflammation in degenerative changes of the joints.
• Rheumatoid arthritis: reduction of pain and stiffness of the joints.
• Ankylosing spondylitis (Bechterew's disease): reduction of inflammation and pain in the spine.
• Acute gouty arthropathy: rapid relief of pain in gouty attacks.
• Acute pain (including postoperative pain, such as after dental interventions): short-term use for pain relief.
• Chronic low back pain: symptomatic therapy for inflammatory processes.

The drug is prescribed to reduce the severity of symptoms, but does not affect the progression of the underlying disease.

Contraindications

The use of Arcoxia is prohibited in the following conditions:

• Hypersensitivity to etoricoxib or any auxiliary component of the drug.
• Allergic reactions (bronchospasm, rhinitis, urticaria) to acetylsalicylic acid or other NSAIDs in the anamnesis.
• Gastric or duodenal ulcer in the active phase, erosive-ulcerous lesions of the GI tract.
• Gastrointestinal bleeding or perforation in the anamnesis associated with the intake of NSAIDs.
• Severe hepatic insufficiency (Child-Pugh class C, greater than 10 points).
• Severe renal insufficiency (creatinine clearance less than 30 mL/min).
• Ischemic heart disease, congestive heart failure (NYHA II-IV), cerebrovascular disease.
• Uncontrolled arterial hypertension (blood pressure above 140/90 mm Hg).
• Pregnancy and breastfeeding period.
• Age under 16 years of age.

How to use and dosage

How to take: Tablets are taken orally, drinking enough water (about 100 ml). The drug can be taken regardless of food, but taking on an empty stomach accelerates the onset of the effect. The duration of treatment is determined by a doctor depending on the patient's condition.

Dosages:

• Adults:
  • Osteoarthritis: 30 mg or 60 mg once daily.
  • Rheumatoid arthritis and ankylosing spondylitis: 60 mg or 90 mg once daily.
  • Acute gouty arthropathy: 120 mg once daily (maximum duration - 8 days).
  • Acute pain (postoperative): 90 mg or 120 mg once daily (maximum 3 days).
  • Chronic low back pain: 60 mg once daily.
• Children: The drug is contraindicated in patients under 16 years of age.

Dose adjustment:

• In mild hepatic insufficiency (5-6 Child-Pugh score): maximum dose - 60 mg per day.
• In moderate hepatic insufficiency (7-9 Child-Pugh score): maximum dose - 30 mg per day.
• In severe hepatic insufficiency (more than 10 points): use is prohibited.
• In renal insufficiency (creatinine clearance more than 30 ml/min): dose adjustment is not required.
• With creatinine clearance less than 30 ml/min: the drug is contraindicated.
• Elderly patients: dose adjustment is not required, but it is necessary to monitor the condition due to increased risk of side effects.

Side effects

The following adverse reactions may occur during the use of Arcoxia:

• Gastrointestinal tract: nausea, dyspepsia, abdominal pain, diarrhea, flatulence, heartburn; rarely - ulcers, bleeding.
• Cardiovascular system: increase in blood pressure, edema, palpitations; rarely - heart failure.
• Nervous system: headache, dizziness, drowsiness, weakness.
• Kidney: fluid retention, deterioration of renal function (especially in patients with dehydration).
• Liver: increase in transaminase levels (ALT, AST).
• Skin: rash, itching; rarely - angioedema.
• General reactions: flu-like syndrome, asthenia.

The frequency of side effects increases with prolonged use or exceeding the recommended doses.

Overdose

Symptoms: When taking a single dose of up to 500 mg or a daily dose of 150 mg for 21 days, no significant symptoms of overdose have been reported. Increased side effects are possible: nausea, vomiting, abdominal pain, dizziness, increased blood pressure, renal dysfunction.

First aid measures:

• Gastric lavage (within 1-2 hours after ingestion).
• Take activated charcoal to reduce absorption.
• Symptomatic therapy (control of BP, renal function).
• Hemodialysis is ineffective for excretion of etoricoxib.

If an overdose is suspected, consult a physician immediately.

Interaction with other drugs

Influence on the effect of other drugs:

• Peroral anticoagulants (warfarin): increase in INR by 13% at a dose of 120 mg daily, blood coagulation control is required.
• Lithium: increase in plasma lithium concentration due to decreased renal excretion.
• Methotrexate: in doses of 60-90 mg does not affect pharmacokinetics, but at 120 mg may increase toxicity.
• ACE inhibitors and angiotensin II antagonists: decreased hypotensive effect, risk of worsening renal function.
• Cyclosporine, tacrolimus: increased nephrotoxicity.
• Rifampicin: decrease of etoricoxib plasma concentration by 65%.

Compatibility with alcohol and food: Consumption of alcohol during treatment increases the risk of side effects from the GI tract and liver, so it is not recommended. Food intake does not affect efficacy, but may slow absorption.

Special Instructions

Pregnancy and breastfeeding: The drug is contraindicated in pregnancy due to the risk of premature closure of the arterial duct in the fetus and disorders of labor activity. There are no data on etoricoxib penetration into breast milk in humans, but animal studies confirm its excretion with milk, therefore breastfeeding during treatment is prohibited.

Effects on driving and driving mechanisms: In some patients the drug may cause dizziness, drowsiness or weakness. In such cases one should refrain from driving and working with mechanisms until the symptoms disappear.

Elderly people: Dose adjustment is not required, but monitoring is necessary due to increased risk of side effects (hypertension, edema, renal impairment).

Children: Use in patients younger than 16 years of age is prohibited due to lack of data on safety and efficacy.

Storage conditions

Arkoxia tablets should be stored in the original package at a temperature not exceeding 30 °C. The storage place should be protected from direct sunlight and moisture. The drug should be kept out of reach of children. Shelf life - 3 years from the date of manufacture indicated on the package. After expiration date the use of the drug is prohibited.