Celebrex capsules 400mg 1pc + 200mg 5pcs

Composition

1 capsule contains:

Active ingredient:  Celecoxib

Pharmacological action

Celecoxib has anti-inflammatory, analgesic and antipyretic effects, blocking the formation of inflammatory prostaglandins (Pg) mainly due to the inhibition of cyclooxygenase-2 (COX-2). COX-2 induction occurs in response to inflammation and leads to the synthesis and accumulation of prostaglandins, especially prostaglandin E2, while increasing the manifestations of inflammation (swelling and pain). In therapeutic doses in humans, celecoxib significantly does not inhibit cyclooxygenase-1 (COX-1) and does not affect prostaglandins synthesized as a result of COX-1 activation, and also does not affect normal physiological processes associated with COX-1 and occurring in tissues, and primarily in the tissues of the stomach, intestines and platelets.

Effect on renal function

Celecoxib reduces urinary excretion_of PGE2 and 6-keto-PGF1(a prostacyclin metabolite), but does not affect serum thromboxane_B2 and urinary excretion of 11-dehydro-thromboxane_B2, a metabolite of thromboxane (both COX – 1 products). Celecoxib does not cause a decrease in glomerular filtration rate (GFR) in elderly patients and people with chronic renal failure, and transitorily reduces sodium excretion. In patients with arthritis, the observed incidence of peripheral edema, hypertension, and heart failure is comparable to that of nonselective COX inhibitors, which have inhibitory activity against COX-1 and COX-2. This effect was most pronounced in patients receiving diuretic therapy. However, there was no increase in the incidence of increased blood pressure and heart failure, and peripheral edema was mild and resolved independently.

Indications

-osteoarthritis; – rheumatoid arthritis – – pain syndrome of various etiologies (including postoperative, toothache, menstrual, bone and muscle pain).

Contraindications

-a history of allergic reactions (urticaria, bronchospasm) associated with taking acetylsalicylic acid or other NSAIDs; – severe renal impairment; – severe liver function disorders – – third trimester of pregnancy – – lactation (breastfeeding); – known hypersensitivity to sulfonamides – – hypersensitivity to the components of the drug.

Side effects

From the digestive system:  often-abdominal pain, diarrhea, dyspepsia; rarely-nausea, vomiting, heartburn, anorexia; with prolonged use in high doses – ulceration of the gastrointestinal mucosa, bleeding, NSAIDs-gastropathy, constipation, flatulence, increased AST and ALT activity. From the central nervous system and peripheral nervous system:  rarely – headache, dizziness, drowsiness or insomnia, blurred vision, depression, agitation, confusion, anxiety, hallucinations, hearing loss, tinnitus. Respiratory system disorders:  rarely – sore throat, cough, shortness of breath, bronchospasm. From the urinary system: rarely-renal failure, edematous syndrome. From the hematopoietic system:  rarely – agranulocytosis, anemia, leukopenia, thrombocytopenia. From the cardiovascular system:  rarely – arterial hypertension, arrhythmia, hot flashes, palpitations, congestive heart failure, tachycardia. Allergic reactions:  bullous skin rash, angioedema, bronchospasm, anaphylaxis, vasculitis, erythema multiforme, Stevens-Johnson syndrome. Other services:  alopecia, increased sweating, nosebleeds. There are isolated reports of acute pancreatitis.

Interaction

When Celebrex is co-administered with the CYP2C9 inhibitor fluconazole, it is possible to increase the concentration of celecoxib in plasma (celecoxib should be used at the lowest recommended dose). It has been established in vitro that celecoxib is an inhibitor of CYP2D6, so there is a possibility of drug interaction with other drugs that are biotransformed with the participation of this isoenzyme. Antacids (aluminum and magnesium) reduce the absorption of celecoxib by 10%, which does not cause clinically significant effects. When studying the effect of Celebrex on the pharmacokinetics and / or Pharmacodynamics of CYP2C9 substrates glyburide, glibenclamide, tolbutamide in vivo, no clinically significant interaction was found. In vitro studies have shown that the CYP2C19 isoenzyme can participate in celecoxib metabolism only to a small extent. In an in vivo study, multiple doses of celecoxib (200 mg twice daily for 7 days) did not affect the clearance of a single dose of the CYP2C19 phenytoin substrate. The risk of clinically significant inhibition of CYP2C19 substrate metabolism by celecoxib is considered to be negligible. When Celebrex is co-administered with warfarin and similar medications, it is possible to increase prothrombin time and develop serious bleeding (it is necessary to monitor clotting parameters and apply precautionary measures). There was no clinically significant interaction of celecoxib with ketoconazole, lithium preparations, and methotrexate.

How to take, course of use and dosage

Adults with osteoarthritis are prescribed Celebrex in a daily dose of 200 mg in 1 or 2 doses. In clinical trials, doses up to 400 mg / day were used. In rheumatoid arthritis, the drug is prescribed in a daily dose of 200-400 mg, divided into 2 doses. In clinical trials, doses up to 800 mg/day were used. For pain syndrome, the recommended single dose is 100-200 mg. If necessary, it is possible to use the drug in the same dose with an interval between doses of at least 4-6 hours until the maximum daily dose of 400 mg is reached. In acute pain and algodismenorrhea, the recommended initial dose is 400 mg, then, if necessary, another dose of 200 mg is possible; the maximum dose on the first day of treatment is 600 mg/day; in subsequent days, the daily dose of the drug can vary from 200 mg to 400 mg. The use of Celebrex in patients under 18 years of age has not been studied.

Overdose

There is no clinical experience of overdose. Healthy volunteers received a single dose of up to 1200 mg and multiple doses of up to 1200 mg 2 times / day without clinically significant adverse effects. Treatment:  conduct symptomatic therapy. Hemodialysis is ineffective.

Special instructions

Celebrex should be used with caution in patients with peptic ulcer of the stomach or duodenum, ulcerative colitis, heart failure, edematous syndrome, arterial hypertension. Celebrex can be used with low doses of acetylsalicylic acid. Due to the lack of action on platelets, Celebrex does not replace acetylsalicylic acid in the preventive treatment of cardiovascular disorders. If the activity of CYP2C9 decreases, Celebrex should be prescribed with caution, since in this case the plasma level of celecoxib may increase excessively. Monitoring of laboratory parameters During the use of the drug, it is necessary to monitor the picture of peripheral blood and laboratory parameters of liver and kidney function. If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study. Clinical data on the efficacy and safety of Celebrex in children and adolescents under 18 years of age are not available. Influence on the ability to drive motor vehicles and manage mechanismthe question of the possibility of engaging in potentially dangerous activities that require increased attention and speed of psychomotor reactions should be resolved only after evaluating the individual patient’s response to the drug.

Storage conditions

The drug should be stored in a dry, inaccessible place for children, while the drug should be stored in a dry, inaccessible place for children at a temperature of 15° to 30°C. The temperature is from 15° to 30°C.

Shelf life

3 years

Active ingredient

Celecoxib

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Description

For adults as directed by your doctor

Indications

Osteoarthritis, Sciatica, Sciatica, Osteoarthritis, Osteochondrosis, Lumbago, Rheumatoid Arthritis, Arthritis