Etoricoxib - Instructions For Use, 90 Mg, Price, Analogues, Reviews

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Etoricoxib

Etoricoxib: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Etoricoxib

ATX code: M01AH05

Active ingredient: Etoricoxib (Etoricoxib)

Producer: JSC "Biochemist" (Russia)

Description and photo update: 2020-29-04

Prices in pharmacies: from 245 rubles.

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Etoricoxib is a non-steroidal anti-inflammatory drug (NSAID).

Release form and composition

Etoricoxib is available in the form of film-coated tablets: dosage 60 mg - round, biconvex, green; dosage 90 mg - round, biconvex, white; dosage 120 mg - oval, biconvex, light green, with a line on one side. The cross-section shows the film coat corresponding to the dosage of the tablet color, and the core is almost white or white.

Tablets are packed in 2, 4, 7, 10 or 14 pieces. in blister strip packaging, 20 or 30 pcs. in light-protective glass jars. The cardboard box contains instructions for the use of Etoricoxib and 1 can or 1-2 blisters.

Composition of 1 tablet:

• active substance: etoricoxib - 60, 90 or 120 mg;
• tablet core: povidone K30, microcrystalline cellulose, magnesium stearate, croscarmellose sodium, calcium hydrogen phosphate anhydrous (anhydrous disubstituted calcium phosphate);
• film shell: dosage 60 mg - Opadray II green 32K210011 (triacetin, lactose monohydrate, hypromellose 2910, titanium dioxide, iron oxide yellow dye, aluminum varnish based on indigo carmine dye), dosage 90 mg - Opadray II white 32K280000 (triacetin, lactose monohydrate, hypromellose 2910, titanium dioxide), dosage 120 mg - Opadray II green 32K210012 (triacetin, lactose monohydrate, hypromellose 2910, titanium dioxide, iron oxide yellow oxide, aluminum varnish based on indigo carmine dye).

Pharmacological properties

Pharmacodynamics

Etoricoxib is an NSAID drug, a selective inhibitor of cyclooxygenase-2 (COX-2). When used in therapeutic doses, it has antipyretic, anti-inflammatory and analgesic effects, blocks the formation of inflammatory mediators - prostaglandins.

Selective inhibition of COX-2 leads to a decrease in the severity of symptoms caused by the inflammatory process. Etoricoxib does not adversely affect the gastrointestinal tract mucosa and platelet function.

The COX-2 inhibition process has a dose-dependent effect. When taking a daily dose of up to 150 mg, there is no effect on COX-1.

Etoricoxib does not affect bleeding time or prostaglandin production in the gastric mucosa. Collagen-induced platelet aggregation and arachidonic acid reduction were not observed in ongoing studies.

Pharmacokinetics

The main pharmacokinetic characteristics of Etoricoxib are:

• absorption: after taking the drug inside, etoricoxib is rapidly absorbed. Its bioavailability is almost 100%. After an adult patient has taken a dose of 120 mg on an empty stomach, the maximum plasma concentration (C _max) is reached within 1 hour and is 3.6 μg / ml. The average area under the concentration-time curve (AUC _{0-24 h}) is 37.8 μg × h / ml. When the drug is used in the range of therapeutic doses, the pharmacokinetics is linear. Simultaneous food intake does not significantly affect the rate and degree of absorption, however, it reduces C _max by 36% and increases the time to reach it by 2 hours. Antacids do not affect pharmacokinetics;
• distribution: at equilibrium, the volume of distribution (V _dss) of etoricoxib is approximately 120 liters; the drug binds to plasma proteins at a level of more than 92%, penetrates the blood-brain and placental barriers;
• metabolism: Etoricoxib undergoes active biotransformation in the liver under the action of the cytochrome P450 isoenzyme (CYP). As a result, five metabolites are formed; the main ones are 6-hydroxymethylethoricoxib and 6-carboxyacetylethoricoxib - they have little effect on COX-2 and have no effect on COX-1 at all;
• Elimination: In studies, healthy volunteers were injected intravenously with 25 mg of labeled radioactive etoricoxib. It was found that 70% is excreted by the kidneys, 20% through the intestines. The drug is excreted mainly in the form of metabolites. Less than 2% was found unchanged. With a daily intake of the drug at a dose of 120 mg, the equilibrium concentration is reached after 7 days, the cumulation coefficient is approximately 2, which indicates a half-life of 22 hours. Plasma clearance of etoricoxib is about 50 ml / min.

Pharmacokinetics of Etoricoxib in special patient groups:

• race: no differences in pharmacokinetics were found in patients of different races;
• gender: there are no differences in pharmacokinetic parameters in women and men;
• old age: in patients over 65 years of age, the pharmacokinetic parameters are comparable to those in younger people, so there is no need to adjust the dose for the elderly;
• childhood: in children under 12 years of age, the effect of etoricoxib has not been studied. The studies found that the pharmacokinetic data of the drug are comparable in adolescents 12-17 years old with a body weight of 40-60 kg, who received a daily dose of 60 mg, with adolescents 12-17 years old with a body weight of more than 60 kg, who received a daily dose of 90 mg, and adults taking 90 mg per day;
• patients with impaired renal function: after a single dose of 120 mg in adult patients with moderate to severe renal impairment and end-stage chronic renal failure undergoing hemodialysis, the pharmacokinetic characteristics did not differ significantly from those in healthy volunteers. Hemodialysis had little effect on drug excretion (dialysis clearance - approximately 50 ml / min);
• patients with impaired hepatic function: with minor functional impairments of the liver (5-6 points on the Child-Pugh scale), a single dose of 60 mg caused an increase in AUC by 16%. In moderate disorders (7–9 points), a dose of 60 mg every other day did not cause changes in the pharmacokinetics of the drug in comparison with healthy individuals who took the drug at a dose of 60 mg daily. In patients with severe functional impairment (> 9 points), studies on the effect of etoricoxib have not been conducted.

Indications for use

• relief of moderate and severe pain after dental surgery;
• symptomatic treatment of ankylosing spondylitis, rheumatoid arthritis, osteoarthritis, as well as pain and inflammation symptoms caused by acute gouty arthritis.

Contraindications

Absolute:

• blood clotting disorders, including hemophilia;
• any bleeding, including cerebrovascular;
• confirmed hyperkalemia, progressive kidney disease, severe renal failure [creatinine clearance (CC) <30 ml / min];
• active liver disease, severe liver failure (> 9 points on the Child - Pugh scale);
• exacerbation of inflammatory bowel disease (eg, ulcerative colitis or Crohn's disease);
• active gastrointestinal bleeding, erosive and ulcerative changes in the mucous membrane of the stomach or duodenum;
• arterial hypertension, not amenable to adequate control [persistent blood pressure (BP)> 140/90 mm Hg. Art.];
• the period after surgery for coronary artery bypass grafting; cerebrovascular disease, peripheral arterial disease, clinically expressed ischemic heart disease;
• II – IV functional class (NYHA classification) heart failure;
• combination (including incomplete) bronchial asthma or recurrent nasal / paranasal sinus polyposis with intolerance to acetylsalicylic acid or other NSAIDs;
• age under 16;
• period of pregnancy and lactation;
• hypersensitivity to any component of the drug.

Relative (Etoricoxib is used with extreme caution):

• mild and moderate hepatic impairment (5-9 points on the Child-Pugh scale);
• frequent alcohol consumption;
• renal failure (CC <60 ml / min);
• edema and fluid retention of any genesis;
• severe somatic diseases;
• arterial hypertension;
• presence of Helicobacter pylori infection;
• a history of ulcerative lesions of the gastrointestinal tract;
• diabetes;
• dyslipidemia or hyperlipidemia;
• smoking;
• elderly age;
• long-term use of NSAIDs;
• simultaneous use of anticoagulants, antiplatelet agents, oral glucocorticosteroids, selective serotonin reuptake inhibitors.

Etoricoxib, instructions for use: method and dosage

Etoricoxib tablets are taken orally with a little water. The timing of meals is of no fundamental importance.

Recommended dosage regimens:

• gouty arthritis in the acute period: 120 mg 1 time per day for no more than 8 days. The average therapeutic dose is 60 mg once a day;
• ankylosing spondylitis, rheumatoid arthritis: Etoricoxib 90 mg once a day;
• osteoarthritis: 60 mg once a day;
• acute pain after dental procedures: Etoricoxib 90 mg once a day for no more than 8 days.

Etoricoxib should be used in the lowest effective dose for the shortest possible course.

Side effects

• from the skin and subcutaneous tissues: often (1-10%) - ecchymosis; infrequently (0.1-1%;) - rash, itching, swelling of the face; rarely (0.01-0.1%) - erythema; very rarely (<1%) - urticaria, Lyell's syndrome, Stevens-Johnson syndrome; unknown frequency (based on the available data, it is not possible to establish the frequency): fixed drug erythema;
• from the kidneys and urinary tract: infrequently - proteinuria; very rarely - renal failure;
• from the liver and biliary tract: often - increased activity of hepatic transaminases; very rarely - jaundice, hepatitis; unknown frequency - liver failure;
• from the gastrointestinal tract: often - nausea, flatulence, diarrhea, heartburn, dyspepsia, epigastric pain; infrequently - dryness of the oral mucosa, increased peristalsis, belching, gastritis, bloating, oral mucosa ulcers, esophagitis, vomiting, constipation, irritable bowel syndrome, gastric or duodenal ulcers; very rarely - ulcers of the gastrointestinal tract (with perforation or bleeding);
• on the part of metabolism and nutrition: often - fluid retention, edema; infrequently - increased appetite, increased body weight;
• from the immune system: very rarely - anaphylactoid and anaphylactic reactions (including shock), hypersensitivity reactions;
• from the respiratory system: infrequently - nosebleeds, shortness of breath, cough; very rarely - bronchospasm;
• from the side of the heart and blood vessels: often - increased blood pressure, palpitations; infrequently - hot flashes, angina pectoris, cerebrovascular accident, atrial fibrillation, nonspecific changes in the electrocardiogram, congestive heart failure, myocardial infarction; very rarely - arrhythmia, tachycardia, hypertensive crisis;
• from the nervous system and psyche: often - weakness, dizziness, headache; infrequently - impaired sensitivity (including paresthesia and hyperesthesia), insomnia or drowsiness, impaired concentration, anxiety, taste disturbance, depression; very rarely - a feeling of anxiety, confusion, hallucinations;
• from the musculoskeletal and connective tissue: infrequently - arthralgia, muscle cramps, myalgia;
• from the organs of hearing and vision: infrequently - vertigo, tinnitus, blurred vision, conjunctivitis;
• from the blood system: infrequently - thrombocytopenia, leukopenia;
• infectious and parasitic diseases: infrequently - infections of the upper respiratory tract or urinary tract, gastroenteritis;
• others: often - flu-like syndrome; infrequently - chest pain;
• laboratory data: infrequently - hyperkalemia, a decrease in hematocrit and hemoglobin, an increase in nitrogen in the blood and urine, uric acid, serum creatinine, creatine phosphokinase activity.

Overdose

In clinical trials, healthy volunteers received a dose of up to 500 mg of etoricoxib once or daily for 21 days, a dose of up to 150 mg. No significant toxic effects of the drug were identified. It has been suggested that an overdose of an anti-inflammatory drug can cause adverse reactions from the digestive system.

Etoricoxib is not excreted during hemodialysis. Excretion during peritoneal dialysis has not been studied. In case of taking an excessive dose of the drug, symptomatic treatment should be carried out.

special instructions

During the period of taking Etoricoxib, it is necessary to carefully monitor blood pressure indicators. Before starting the drug, regularly in the first two weeks of therapy and periodically during further treatment, blood pressure monitoring is required.

Regular monitoring of the functional state of the kidneys and liver is also important. If there is an increase in the activity of liver enzymes 3 times or more compared to the upper limit of the norm, Etoricoxib is canceled. With long-term treatment, the risk of side effects increases, so the doctor should periodically evaluate the possibility of reducing the dose of the drug and the need to continue therapy.

Etoricoxib should not be taken in conjunction with other NSAIDs.

The film shell of tablets contains a small amount of lactose, which must be taken into account when prescribing an anti-inflammatory drug for patients with lactase deficiency.

Etoricoxib can have a negative effect on female fertility, so it is not recommended for women who are planning a pregnancy.

Influence on the ability to drive vehicles and complex mechanisms

During treatment with the drug, care must be taken to vehicle drivers and persons engaged in potentially hazardous activities. If episodes of weakness, dizziness or drowsiness occur while taking Etoricoxib, until the end of the course of therapy, you should refrain from work requiring concentration of attention and speed of reactions.

Application during pregnancy and lactation

Etoricoxib is contraindicated during pregnancy and lactation. If the course of therapy is mandatory in lactating women, they should stop breastfeeding.

Pediatric use

Etoricoxib is not used to treat children under 16 years of age.

With impaired renal function

With confirmed hyperkalemia, progressive kidney disease and severe renal failure (CC <30 ml / min), Etoricoxib is contraindicated.

The drug is used with caution in renal failure with CC <60 ml / min, edema and fluid retention in the body.

For violations of liver function

In active liver disease and severe liver failure (> 9 points on the Child-Pugh scale), Etoricoxib is contraindicated.

With mild to moderate liver failure (5-9 points on the Child-Pugh scale), the drug should be used with caution, not exceeding the dose of 60 mg per day. Observance of precautions during treatment is required for people who abuse alcohol.

Use in the elderly

Etoricoxib is recommended to be used with caution in the treatment of elderly patients.

Drug interactions

Pharmacodynamic interaction:

• acetylsalicylic acid (ASA): Patients taking low-dose ASA for the prevention of cardiovascular disease are allowed to use Etoricoxib. However, it should be borne in mind that when using the combination, the number of cases of ulcerative lesions of the gastrointestinal tract and the development of other side effects increases in comparison with monotherapy. Etoricoxib does not reduce the prophylactic effect of ASA in cardiovascular diseases. In a daily dose of 120 mg, the drug does not affect the antiplatelet properties of ASA in low doses (81 mg per day);
• oral anticoagulants (for example, warfarin): with the simultaneous use of etoricoxib in a daily dose of 120 mg, an increase in INR (International Normalized Ratio) and prothrombin time was noted. If combined use with warfarin or similar drugs is required, these indicators should be monitored, especially in the first few days of taking etoricoxib;
• diuretics, ACE inhibitors (angiotensin converting enzyme): Etoricoxib may reduce their hypotensive effect. In case of impaired renal function (including in the case of dehydration or age-related changes) there is a risk of worsening functional kidney failure;
• tacrolimus, cyclosporine: when combined with etoricoxib, the risk of nephrotoxicity increases.

Pharmacokinetic interaction:

• glucocorticosteroids: no significant drug interactions with etoricoxib have been identified;
• ketoconazole (a potent inhibitor of CYP3A4), antacids: no significant change in the pharmacokinetics of etoricoxib was found;
• digoxin: no changes in its AUC and elimination were noted, however, C _max increases by about 33%, which may be important in case of overdose of digoxin;
• rifampicin (a powerful inducer of hepatic metabolism): there is a significant (65%) decrease in the AUC of etoricoxib;
• Methotrexate: The effects of etoricoxib at daily doses of 60, 90 and 120 mg were studied in two studies in patients with rheumatoid arthritis who received the drug for 7 days simultaneously with methotrexate in the range of daily doses of 7.5–20 mg. Etoricoxib doses of 60 and 90 mg had no effect on the plasma concentration and renal clearance of methotrexate. In one of the studies, a dose of 120 mg also had no effect on the indicated parameters of methotrexate, however, in another study, an increase in the concentration of methotrexate by 28% and a decrease in its renal clearance by 13% was noted. Given these data, it is recommended to carefully monitor patients receiving etoricoxib at a dose of ≥ 90 mg concomitantly with methotrexate, due to the existing risk of developing the toxic effects of methotrexate;
• lithium: Etoricoxib may increase its plasma concentration;
• combined oral contraceptives (COCs): in studies, the patient took 120 mg of etoricoxib for 21 days simultaneously with COCs containing 0.035 mg of ethinylestradiol and 0.5-1 mg of norethindrone. There was an increase in the AUC of ethinylestradiol by 50-60%, but no significant increase in the concentration of norethisterone was found. These data should be considered when prescribing COCs to women receiving etoricoxib, since this combination increases the incidence of thromboembolism.

Analogs

The analogues of Etoricoxib are Arkoksia, Atorica tabs, Bixitor, Costarox, Rixia, Strega tabs, Etoria, Etoriax, Etorelex, Etoricoxib-Teva, Etoricoxib Sanofi, etc.

Terms and conditions of storage

Store at temperatures up to 30 ° C out of reach of children.

The shelf life is 1.5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Etorikoxib

There are no reviews about Etorikoxib, but there are many reports of other drugs containing a similar active ingredient. According to most patients, these drugs effectively and quickly relieve pain and are well tolerated.

Nevertheless, individual patients indicate the development of a large number of side effects, due to which they had to interrupt treatment. Numbness of the extremities, pain under the rib, heartburn, stomach pain, temporary loss of sensitivity, increased blood pressure are mentioned. They also note the relatively high cost of anti-inflammatory drugs, the active substance of which is etoricoxib.

Price for Etoricoxib in pharmacies

The price of Etoricoxib is currently unknown due to the lack of the drug in pharmacies. The approximate cost of some analogues:

• Arkoksia (7 tablets per pack): 90 mg - from 365 rubles, 120 mg - from 540 rubles;
• Etoria (14 tablets per pack): 60 mg - from 258 rubles;
• Costarox (7 tablets per pack): 90 mg - from 220 rubles, 120 mg - from 302 rubles.

Etoricoxib: prices in online pharmacies

Drug name Price Pharmacy

Etoricoxib tablets p.p. 90mg 7pcs 245 RUB Buy

Etoricoxib 90 mg film-coated tablets 7 pcs. 245 RUB Buy

Etoricoxib tablets p.p. 120mg 7pcs RUB 315 Buy

Etoricoxib 120 mg film-coated tablets 7 pcs. RUB 315 Buy

Etoricoxib 60 mg film-coated tablets 28 pcs. RUB 488 Buy

Etoricoxib tablets p.p. 60mg 28pcs 491 r Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!