Hard capsules Locobile-200 Windlas Biotech treat osteoarthritis, rheumatoid arthritis (3 blisters x 10 tablets)

The mechanism of action of Celecoxib is to inhibit the synthesis of prostaglandin, mainly through inhibition of isenzyme cyclooxygenase - 2 (COX - 2), reducing the formation of prostatglandin.

Celecoxib inhibits selectively on COX - 2, so the adverse effect on the digestive tract is less than non -selective steroid anti -inflammatory anti -inflammatory drugs.

pharmacokinetics

absorption:

Good absorption through the gastrointestinal tract. When taking a single dose of 200 mg, the peak concentration in plasma occurs 3 hours after taken.

The peak concentration in plasma is 705 ng/ml. When using many doses, stable state is achieved or before the 5th.

When used with foods high in fat, the peak plasma concentration level is delayed in about 1-2 hours with an increase in AUC about 10 % to 20 %.

Distribution:

The volume of distribution in a stable state when using a dose of 200 mg, healthy people is 429 liters.

Links to plasma proteins: 97% associated with albumin and bind to glycoprotein with less degrees.

Metabolism:

Metabolic through the liver: Celecoxib metabolizes mainly through cytochrom P450 2C9.

Three metabolites, alcohol compounds, carboxylic acids and glucuronide compounds have been determined in human plasma. CYP3A4 is involved in Celecoxib hydroxylation but lower level. The metabolites do not work like COX - 1 or COX - 2.

Era:

Celecoxib excreted by metabolism in the liver in a constant form (

Caution when using

Effects on the digestive system:

Complications for stomach (ulcers, perforation, hemorrhage), some deaths, occurred in patients treated with Celecoxib.

Needs on treatment for patients at risk of gastric complications with NSAIDs; Elderly, patients use any other NSAID drugs or acetylsalicylic acid, glucocorticoid, patients using alcohol or patients with a history of gastrointestinal diseases such as ulcers and diarrhea.

Increased risk of adverse gastrointestinal tract when using Celecoxib (ulcerative or other digestive tract complications) simultaneously with acetylsalicylic acid (even in low doses). There is no statistical significant difference when comparing the safety of the digestive tract between COX inhibitors - 2 selective + acetylsalicylic acid compared to NSAIDs + Acetylsalicylic acid in long -term clinical trials.

Simultaneous use NSAID:

It is necessary to avoid using Celecoxib with NSAID not aspirin.

Risk of cardiovascular thrombosis:

Non -steroid anti -inflammatory drugs (NSAIDs), non -aspirin, body sugar, may increase the risk of cardiovascular thrombosis, including myocardial and stroke, which can lead to death.

This risk can appear early in the first few weeks of taking the drug and can increase over time.

The risk of cardiovascular thrombosis is recorded mainly in high doses. Doctors need to periodically evaluate the appearance of cardiovascular events, even if the patient does not have previous cardiovascular symptoms.

Patients need to be warned about the symptoms of serious cardiovascular events and need to see a doctor as soon as these symptoms appear. To minimize the risk of adverse incidents, the lowest daily daily dosage is required in the shortest possible time.

Selective inhibitors of COX - 2 are not substitutes for acetylsalicylic acid to prevent coronary artery diseases to inhibit platelet gathering. Therefore, anti -platelet drugs should not be stopped.

Increase the volume of circulation and edema:

Like other drugs known to inhibit the synthesis of prostaglandin. Increase the volume of circulation and edema has been recorded in patients using Celecoxib.

Therefore, Celecoxib should be carefully used in patients with a history of heart failure, left ventricular dysfunction or hypertension and in patients with a history of edema for any reason, because Prostaglandin inhibitors can impair kidney function and increase fluid volume, need caution in patients treated with diuretics or risk of blood volume.

Hypertension:

Similar to all NSAIDs, Celecoxib may lead to the onset of hypertension or seriously causing hypertension, or increasing the rate of cardiovascular events. Therefore, blood pressure should be closely monitored while starting treatment with Celecoxib and during treatment.

Effects on the liver and kidneys:

Damage to kidney or liver function. And especially heart function impairment usually occurs in the elderly and therefore need to maintain patients monitoring. NSAIDs, including Celecoxib, can cause kidney toxicity.

Patients with the highest risk of kidney toxicity are patients with impaired renal function, heart failure, liver dysfunction, users of diuretics, enzyme inhibitors, angiotensin II receptor and elderly. These patients should be carefully monitored during treatment with Celecoxib.

Some cases of severe liver failure, including acute hepatitis (some deaths), liver necrosis and liver failure (some deaths or liver transplantation) have been reported when using Celecoxib. Among the cases of reporting on the onset time, most serious liver events have occurred within a month after the start of Celecoxib treatment.

If during the treatment process, patients with impaired functional organs of the body are described above, it is necessary to take appropriate treatments and should stop celecoxib treatment.

Inhibition of CYP2D6 enzyme:

Celecoxib inhibits CYP2D6 enzyme. Although this is not a strong enzyme inhibitor, it is necessary to reduce the dose for drugs metabolized by CYP2D6.

Poor metabolism through CYP2C9 enzyme:

Patients known as poor metabolic people through CYP2C9 enzymes should be carefully treated.

Hypersensitivity reaction and hypersensitivity reaction to the skin:

Serious skin reactions, some of which are fatal, including flaking dermatitis, Stevens - Johnson syndrome, and poisoned epidermal necrosis, have been reported with rare frequency. Patients with a history of sulphonamid allergies or any drug allergies may have a risk of serious skin reactions or hypersensitivity reactions. Celecoxib should be stopped as soon as the skin rash appears, mucosal damage, or any signs of hypersensitivity.

General:

Celecoxib can cover signs of fever and signs of other inflammatory symptoms.

Use with oral anticoagulant:

In patients treated simultaneously with Warfarin, serious bleeding events, some of which are fatal, have been reported. Increase prothrombin time (Inr international normalization index) when used at the same time has been reported. Therefore, closely monitor patients using Warfarin/Coumarin oral drugs.

especially when using Celecoxib or changing the dosage of Celecoxib. Concomitant use of anticoagulants with NSAIDs may increase the risk of bleeding.

Be careful when combining Celecoxib with warfarin or other oral anticoagulants, including new anticoagulants (such as Apixaban, Dabigatran and Rivaroxaban).

excipients:

The drug contains lactose. Patients with genetic problems rarely intolerant to galactose, lactase deficiency or malposure - Galactose should not be used.

Pregnant women

Data from epidemiological studies show that the risk of natural miscarriage increases after using Prostaglandin synthesis inhibitors in the early stages of pregnancy.

Potential risks of fetal harm is not known, but cannot be excluded. Celecoxib, like other drugs inhibiting Prostaglandin synthesis, can cause uterine contractions and early closed ductus artery during the last 3 months of pregnancy.

Celecoxib is contraindicated during pregnancy and in women who are wishing to become pregnant. If women are pregnant during treatment, celecoxib should be terminated.

Based on the pharmaceutical mechanism, the use of NSAIDs, including Celecoxib, can be delayed or prevented ovulation, related to the ability to recover infertility in some women.

breastfeeding women

Celecoxib is excreted in breast milk for breastfeeding with similar concentrations in plasma. The use of Celecoxib is studied on the number of breastfeeding women is limited and has recorded very low secretion of celecoxib. Women who use Celecoxib should not breastfeed.

The ability to drive, operate machinery

Patients with dizziness or drowsiness while using Celecoxib should not drive or operate machinery.

Interactive drug

anticoagulant drugs:

Recognized cases of increasing bleeding time and prothrombin time, mainly in the elderly, in patients using Celecoxib simultaneously with Warfarin, there were cases of death.

Hypertension:

NSAIDS drugs can reduce the effects of hypertension drugs including enzyme inhibitors, Angiotensin II receptor resistant drugs, diuretics and beta channel blockers.

For NSAIDs including Celecoxib, the risk of acute renal impairment, recovery, increased in some patients with impaired renal function (for example, patients reduce the volume of circulatory, patients use diuretics, or elderly patients) when concurrent with enzyme inhibitors, Angiotensin II and/or diuretic drugs.

Therefore, be careful when used in combination with drugs, especially in the elderly. Patients need to drink enough water and monitor kidney function at the beginning of treatment, and then periodically monitor.

ciclosporin and tacrolimus:

Sharing NSAID and Ciclosporin or Tacrolimus may increase the toxicity of Ciclosporin or Tacrolimus. Kidney function should be monitored when using Celecoxib.

Acetylsalicylic acid:

Celecoxib can be used with low -dose acetylsalicylic acids but not an alternative to acetylsalicylic acid to prevent cardiovascular events.

In the conducted studies, similar to other NSAIDs, the risk of gastric ulcer or stomach complications compared to the use of single cerecoxib is recorded when used with low doses of acetylsalicylic.

Inhibition of CYP2D6 enzyme:

Celecoxib is CYP2D6 inhibitor. The concentration of drugs in plasma metabolized through this enzyme can increase when used simultaneously with Celecoxib.

Examples of drugs metabolized by CYP2D6 are 3 -round antidepressants and selective inhibitors to reabsorb Serotonin painkillers, anti -arrhythmic drugs. It is recommended to reduce the dose of metabolic drugs through CYP2D6 when starting with celecoxib or increasing the dose of metabolized drugs through CYP2D6 enzyme if stopped with Celecoxib.

Use Celecoxib 200 mg twice daily, increasing the concentration of dextromethorphan and metoprolol (metabolites through CYP2D6) 2.6 times and 1.5 times.

CYP2C19 enzyme inhibitor:

In vitro studies have shown that Celecoxib may inhibit CYP2C19. However, clinical data is still unclear. The drugs metabolized by CYP2C19 are diazepam, citalopram and imipramin.

methotrexate:

In patients with rheumatoid arthritis, interactions between Celecoxib and Methotrexate (low doses) have no statistical significance. However, it is necessary to fully consider the toxicity related to methotrexate when combining these two drugs.

Lithi:

For healthy people, use Celecoxib 200 mg twice a day with 450 mg x 2 times/day lithium increases the average CMAX 16% and 18% AUC for lithium concentration. Therefore, patients treated with lithium should be closely monitored when used simultaneously with Celecoxib or stop using lithium.

Oral contraceptive pills:

In interactive study, Celecoxib has no clinical effects on pharmacokinetics of oral contraceptives (1 mg/35micrograms ethinylestradiol).

glibenclamid/tolbutamid:

Celecoxib does not affect the pharmacokinetics of tolbutamid (trips via CYP2C9) or Glibenclamid.

Poor metabolism through CYP2C9 enzyme:

For those who metabolize through poor CYP2C9 enzymes will increase the systemic effect of Celecoxib, when treated simultaneously with CYP2C9 enzyme inhibitors like fluconazole will increase Celecoxib level. It is necessary to avoid combining these drugs in people with poor metabolism through CYP2C9 enzymes.

CYP2C9 Inhibition and Touch:

Because Celecoxib is metabolized mainly through CYP2C9 enzymes, it is recommended to use half of the dose in patients with Fluconazol simultaneously. Simultaneous use of Celecoxib 200 mg once and 200 mg of fluconazole once a day, a powerful CYP2C9 inhibitor increases the average CMAX 60% and AUC is 130% for Celecoxib. Simultaneous use of CYP2C9 enzyme induction drugs such as Rifampicin, Carbamazepin and Barbiturat may reduce the concentration of Celecoxib in plasma.

ketoconazole and stomach antacids:

Ketoconazole or stomach antacids are not affected by the pharmacokinetics of Celecoxib.

Children:

Interactive research is only done in adults, not done in children.

Cavalry:

Due to the absence of studies on the correlation of the drug, not mixing this drug with other drugs.