Kostarox tabs 90mg #28

Kostarox user manual

You can buy Kostarox here

The composition and release form of Kostarox

Tablets, film coated light green color, round, biconvex.
1 tab.
Etoricoxib 120 mg
Excipients: calcium hydrophosphate anhydrous - 52 mg, microcrystalline cellulose - 51 mg, povidone K30 - 12 mg, magnesium stearate - 2 mg, croscarmellose sodium - 3 mg.
The composition of the tablet shell: Opadry II green 32K510003 - 3 mg: hypromellose 15 cPs 3.2 mg, lactose monohydrate 2.24 mg, titanium dioxide 1.776 mg, triacetin 0.64 mg, indigo carmine aluminum varnish (3-5%) 0.04 mg, ferric oxide yellow 0.104 mg.

pharmachologic effect

NSAIDs. 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, and 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 the conducted 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 µg / 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, the values ​​of Cmax are reduced by 36% and Tmax is increased by 2 hours. The average geometric value of AUC0-24 was 37.8 µg 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 l. Etorikoksib penetrates through the placental and BBB.
Intensively metabolized in the liver, with the participation of isoenzymes of cytochrome P450 and the formation of 6-hydroxymethyl-etoricoxib. 5 metabolites of etoricoxib were detected, the main ones - 6-hydroxymethyl-ethoroxib and its derivative - 6-carboxy-acetyl-etoricoxib. The major metabolites do not affect COX-1 and are completely inactive or inactive towards 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 erotricoxib 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 Kostarox at a dose of 60 mg every other day, the AUC value was the same as in healthy individuals who took Kostarox daily at the same dose.
Hemodialysis had little effect on elimination (clearance of dialysis - about 50 ml / min).

Indications for Kostarox

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.

Contraindications for Kostarox

A complete or incomplete combination of asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including a history of).
Erosive and ulcerative changes in 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 classification 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 arterial disease, cerebrovascular disease, clinically severe coronary artery disease.
Persistent arterial hypertension with BP values ​​greater than 140/90 mm Hg. st.
Pregnancy, lactation period (breastfeeding).
Children and adolescents up to 16 years.
Hypersensitivity to Etoricoxib.

Dosage

Kostarox 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.

Side effects of Kostarox

On the part of the digestive system: often - epigastric pain, nausea, diarrhea, dyspepsia, flatulence; sometimes - bloating, 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, concentration disorders; 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 a pronounced decrease 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, itching, 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 - swelling, 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 CPK, 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.

Drug interaction

In patients receiving warfarin, administration of etoricoxib at a dose of 120 mg / day was accompanied by an increase of about 13% MHO and prothrombin time. In patients receiving warfarin or similar drugs, MHO should be monitored when starting therapy or changing the dosing regimen of Etoricoxib, especially in the first few days.
There are reports that non-selective NSAIDs and selective COX-2 inhibitors are able to weaken the hypotensive effect of ACE inhibitors. This interaction should be taken into account when treating patients taking Etoricoxib concurrently with ACE inhibitors. In patients with impaired renal function (for example, during dehydration or in old age), such a combination may exacerbate renal functional impairment.
Etoricoxib can be used simultaneously with acetylsalicylic acid in low doses, intended for the prevention of cardiovascular diseases. However, the simultaneous appointment of acetylsalicylic acid in low doses and etoricoxib may lead to an increase in the frequency of ulcerative lesions of the gastrointestinal tract and other complications compared with taking etoricoxib alone. After reaching equilibrium, the administration of etoricoxib at a dose of 120 mg 1 time / day does not affect the antiplatelet activity of acetylsalicylic acid at low doses (81 mg / day). Kostarox does not replace the preventive action of acetylsalicylic acid in cardiovascular diseases. Cyclosporine and tacrolimus increase the risk of nephrotoxicity during the administration of Etoricoxib.
There is evidence that non-selective NSAIDs and selective COX-2 inhibitors may increase the concentration of lithium in the plasma. This interaction should be taken into account in the treatment of patients taking Etoricoxib concurrently with lithium.
There is evidence of an increase in plasma methotrexate concentration by 28% (according to AUC) and a 13% decrease in its renal clearance under the influence of etoricoxib.
The administration of etoricoxib at a dose of 120 mg with oral contraceptives containing 35 mcg of ethinyl estradiol and from 0.5 to 1 mg of norethindrone for 21 days, simultaneously or with a difference of 12 hours, increases the steady-state AUC0-24 of ethinyl estradiol by 50-60%. However, the concentration of norethisterone usually does not increase to a clinically significant extent. This increase in ethinyl estradiol concentration should be taken into account when selecting the appropriate oral contraceptive for simultaneous use with Etoricoxib. This fact can lead to an increase in the frequency of thromboembolism, due to the increased exposure to ethinyl estradiol.
Etoricoxib does not affect AUC0-24 in the equilibrium state or the elimination of digoxin. At the same time, etoricoxib increases Cmax (on average by 33%), which may be of importance when digoxin overdose develops.
The simultaneous administration of etoricoxib and rifampicin (a powerful inducer of hepatic metabolism) leads to a 65% reduction in plasma AUC of etoricoxib. This interaction should be considered while administering etoricoxib with rifampicin.

special instructions for Kostarox

Kostarox used with caution in indications of a history of ulcerative lesions of the gastrointestinal tract, Helicobacter pylori infection, in elderly patients, patients receiving long-term NSAIDs, 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 increasing 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 reactions. Patients who have experienced episodes of dizziness, drowsiness, or weakness should refrain from activities that require concentration.

Pregnancy and lactation

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

Use in childhood

Kostarox contraindicated in children and adolescents up to 16 years.

In case of impaired renal function

Contraindicated in severe renal failure (CC less than 30 ml / min), progressive kidney disease.

With abnormal liver function

Kostarox contraindicated in severe liver failure (more than 9 points on the Child-Pugh scale) or active liver disease. In patients with moderate hepatic impairment (5-9 points on the Child-Pugh scale), it is recommended not to exceed the daily dose of 60 mg.

Use in old age

With caution used in the elderly.

Terms of sell

You can buy Kostarox without a prescription.