Etoricoxib

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Available since: 2019-09-19

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Clinical Pharmacology

NSAIDs. A selective inhibitor of COX-2, in therapeutic concentrations, blocks the formation of prostaglandins and has anti-inflammatory, analgesic and antipyretic effects. Selective inhibition of COX-2 is accompanied by a decrease in the severity of clinical symptoms associated with the inflammatory process, while there is no effect on the function of platelets and the mucous membrane of the gastrointestinal tract.

Etoricoxib has a dose-dependent effect of inhibiting COX-2, without affecting COX-1 when used in a daily dose of up to 150 mg. It has no effect on the production of prostaglandins in the gastric mucosa and at the time of bleeding. In our studies, no decrease in arachidonic acid and platelet aggregation caused by collagen was observed.

Pharmacokinetics

After ingestion is rapidly absorbed from the gastrointestinal tract. Bioavailability when administered is about 100%. After ingestion by adults on an empty stomach at a dose of 120 mg Cmax is 3.6 mcg / ml, Tmax -1 h after administration. Eating does not have a significant effect on the severity and rate of absorption of Etoricoxib when taken in a dose of 120 mg. At the same time, Cmax values are reduced by 36% and Tmax is increased by 2 hours. The average geometric value of AUC0-24 was 37.8 mcg x h / ml. The pharmacokinetics of etoricoxib within the range of therapeutic doses is linear.

Plasma protein binding exceeds 92%. Vd in equilibrium is about 120 liters. Etorikoksib penetrates through the placental and BBB.

Intensively metabolized in the liver, with the participation of cytochrome P450 isoenzymes and the formation of 6-hydroxymethyl-etoricoxib. 5 Etoricoxib metabolites were detected, the main ones - 6-hydroxymethyl-etoricoxib and its derivative - 6-carboxy-acetyl-Etoricoxib. The major metabolites do not affect COX-1 and are completely inactive or inactive with respect to COX-2.

Excreted by the kidneys as metabolites. Less than 1% is excreted in the urine unchanged.

With a single intravenous injection, 70% is excreted by the kidneys, 20% through the intestine, mainly in the form of metabolites. Less than 2% was found unchanged.

The equilibrium state is reached after 7 days with a daily dose of 120 mg, with a cumulation factor of about 2, which corresponds to T1 / 2 - about 22 hours. The plasma clearance is approximately 50 ml / min.

In patients with minor impaired liver function (5-6 points on the Child-Pugh scale), a single dose of etoricoxib at a dose of 60 mg / day was accompanied by an increase in AUC by 16% compared with healthy individuals.

In patients with moderate hepatic impairment (7–9 on the Child-Pugh scale) who took the drug at a dose of 60 mg every other day, the AUC value was the same as in healthy individuals who took the drug daily at the same dose.

Hemodialysis had little effect on elimination (clearance of dialysis - about 50 ml / min).

Indications

Symptomatic therapy of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis; pain and symptoms of inflammation associated with acute gouty arthritis; short-term treatment of pain associated with dental surgery.

Composition

1 tab .:

Etoricoxib 90 mg.

Excipients: anhydrous calcium hydrophosphate - 39 mg, microcrystalline cellulose - 38.25 mg, povidone K30 - 9 mg, magnesium stearate - 1.5 mg, croscarmellose sodium - 2.25 mg.

The composition of the tablet shell: Opadry II white 32К580000С - 6 mg: hypromellose 15 cPs 2.4 mg, lactose monohydrate 1.68 mg, titanium dioxide 1.44 mg, triacetin 0.48 mg.

Etoricoxib is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Costarox	Sandoz)		pills
Costarox			pills
Arcoxia	Merck Sharp & Dohme	Netherlands	pills

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Dosage and Administration

The drug is taken orally at a dose of 60-120 mg 1 time / day.

In patients with hepatic insufficiency (5-9 points on the Child-Pugh scale) it is recommended not to exceed the daily dose of 60 mg.

Adverse reactions

On the part of the digestive system: often - epigastric pain, nausea, diarrhea, dyspepsia, flatulence; sometimes - abdominal distension, belching, increased peristalsis, constipation, dryness of the oral mucosa, gastritis, gastric or duodenal ulcers, irritable bowel syndrome, esophagitis, ulcers of the oral mucosa, vomiting; very rarely - gastrointestinal ulcers (with bleeding or perforation), hepatitis.

The nervous system: often - headache, dizziness, weakness; sometimes - a violation of taste, drowsiness, sleep disorders, sensitivity disorders, incl. paresthesia / hyperesthesia, anxiety, depression, impaired concentration; very rarely - hallucinations, confusion.

From the senses: sometimes - blurred vision, conjunctivitis, tinnitus, vertigo.

On the part of the urinary system: sometimes - proteinuria; very rarely - renal failure, usually reversible with drug withdrawal.

Allergic reactions: very rarely - anaphylactic / anaphylactoid reactions, including marked reduction in blood pressure and shock.

Since the cardiovascular system: often - heartbeat, increased blood pressure; sometimes - hot flashes, cerebrovascular accident, atrial fibrillation, congestive heart failure, non-specific ECG changes, myocardial infarction; very rarely - hypertensive crisis.

On the part of the respiratory system: sometimes - cough, shortness of breath, nosebleeds; very rarely - bronchospasm.

Dermatological reactions: often - ecchymosis; sometimes - swelling of the face, itchy skin, rash; very rarely - urticaria, Stevens-Johnson syndrome, Lyell's syndrome.

Infectious complications: sometimes - gastroenteritis, infections of the upper respiratory tract, urinary tract.

On the part of the musculoskeletal system: sometimes - muscle cramps, arthralgia, myalgia.

On the part of the metabolism: often - edema, fluid retention; sometimes - changes in appetite, weight gain.

From the laboratory studies: often - increased activity of hepatic transaminases; sometimes - increased nitrogen in the blood and urine, increased activity of CK, decreased hematocrit, decreased hemoglobin, hyperkalemia, leukopenia, thrombocytopenia, increased serum creatinine, increased uric acid; rarely, an increase in serum sodium.

Other: often - flu-like syndrome; sometimes - pain in the chest.

Contraindications

A complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including a history of).

Erosive and ulcerative changes of the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding, cerebrovascular or other bleeding.

Inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute phase.

Hemophilia and other bleeding disorders.

Severe heart failure (NYHA class II-IV functional classes).

Severe liver failure (more than 9 points on the Child-Pugh scale) or active liver disease.

Renal failure severe (CC less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia.

The period after coronary artery bypass surgery; peripheral artery disease, cerebrovascular disease, clinically severe coronary artery disease.

Persistent arterial hypertension with BP values greater than 140/90 mm Hg. Art.

Pregnancy, lactation (breastfeeding).

Children and adolescents up to 16 years.

Hypersensitivity to Etoricoxib.

Pregnancy and Lactation

The drug is contraindicated in pregnancy and lactation.Etoricoxib may adversely affect female fertility and is not recommended for women planning a pregnancy.

Special instructions

It is used with caution in indications of a history of ulcerative lesions of the gastrointestinal tract, Helicobacter pylori infection, in elderly patients, patients who have been receiving NSAIDs for a long time, with severe somatic diseases, dyslipidemia / hyperlipidemia, diabetes, hypertension, edema and fluid retention, smoking , in patients with QA less than 60 ml / min, with concomitant therapy with the following drugs: anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), GCS (for example, dnizolonom), selective serotonin reuptake inhibitors (e.g., citalopram, fluoxetine, paroxetine, sertraline), chronic alcoholism.

During the period of treatment requires careful monitoring of blood pressure during the first 2 weeks and periodically thereafter.

During the period of treatment should regularly monitor the performance of the liver and kidneys. In case of increased activity of hepatic transaminases 3 times or more relative to VGN, treatment should be discontinued.

Given the increased risk of adverse effects with increasing duration of treatment, it is necessary to periodically assess the need for continued treatment and the possibility of reducing the dose.

It should not be used simultaneously with other NSAIDs.

Influence on ability to drive motor transport and control mechanisms

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed. Patients who have experienced episodes of dizziness, drowsiness or weakness should refrain from activities that require concentration.