Buy Costarox pills 90 mg 7 pcs
  • Buy Costarox pills 90 mg 7 pcs


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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.


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).


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.


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 nameManufacturerCountryDosage 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.


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.

  • Brand name: Costarox
  • Active ingredient: Etoricoxib
  • Dosage form: Film Coated pills
  • Manufacturer: Merck Sharp & Dohme

Studies and clinical trials of Etoricoxib (Click to expand)

  1. Chronic oral etoposide and tamoxifen in the treatment of far-advanced hepatocellular carcinoma
  2. Evaluation of the efficacy of etoricoxib in ankylosing spondylitis: Results of a fifty-two–week, randomized, controlled study
  3. A liquid chromatography–mass spectrometry method for the quantification of both etoricoxib and valdecoxib in human plasma
  4. Simultaneous quantitation of etoricoxib, salicylic acid, valdecoxib, ketoprofen, nimesulide and celecoxib in plasma by high-performance liquid chromatography with UV detection
  5. Isolation and Structural Characterization of the Photolysis Products of Etoricoxib.
  6. Simultaneous determination of unlabeled and carbon-13-labeled etoricoxib, a new cyclooxygenase-2 inhibitor, in human plasma using HPLC–MS/MS
  7. Investigating the hydrate conversion propensity of different etoricoxib lots
  8. Detection of a minor amorphous phase in crystalline etoricoxib by dynamic mechanical analysis: Comparison with raman spectroscopy and modulated differential scanning calorimetry
  9. Validation of a capillary zone electrophoresis method for the comparative determination of etoricoxib in pharmaceutical formulations
  10. Effect of rofecoxib, etoricoxib, celecoxib, and naproxen on urinary excretion of prostanoids in elderly volunteers
  11. PII-42The effect of etoricoxib on the pharmacodynamics and pharmacokinetics of warfarin
  12. Validated liquid chromatographic ultraviolet method for the quantitation of Etoricoxib in human plasma using liquid–liquid extraction
  13. Résultats du programme de l'étude multinationale de l'étoricoxib et du diclofénac dans le traitement d'affections rhumatologiques (MEDAL) : comparaison de critères cardiovasculaires à la suite de traitements à long terme par l'étoricoxib ou le diclofénac chez des patients atteints d'une arthrose ou d'une polyarthrite rhumatoïde
  14. In vitro metabolism considerations, including activity testing of metabolites, in the discovery and selection of the COX-2 inhibitor etoricoxib (MK-0663)
  15. Complementary studies of the gastrointestinal safety of the cyclo-oxygenase-2-selective inhibitor etoricoxib
  16. A multinational randomized, controlled, clinical trial of etoricoxib in the treatment of rheumatoid arthritis [ISRCTN25142273]
  17. Etoricoxib - preemptive and postoperative analgesia (EPPA) in patients with laparotomy or thoracotomy - design and protocols
  18. Vergelijking van etoricoxib en diclofenac bij mensen met artrose en reumatoïde artritis
  19. Antiinflammatory effects of etoricoxib alone and combined with NSAIDs in LPS-induced reactive arthritis
  20. The selective COX-2 inhibitor Etoricoxib reduces acute inflammatory markers in a model of neurogenic laryngitis but loses its efficacy with prolonged treatment
  21. Absorption and distribution of etoricoxib in plasma, CSF, and wound tissue in patients following hip surgery—a pilot study
  22. Oral voriconazole and miconazole oral gel produce comparable effects on the pharmacokinetics and pharmacodynamics of etoricoxib
  23. Anti-inflammatory and analgesic actions of etoricoxib (an NSAID) combined with misoprostol

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