Description
Latin name
CELEBREX
Release form
Capsules.
Packing
10 pcs
Pharmacological action
Celebrex – NSAIDs. Specific cyclooxygenase-2 inhibitor (COX-2).
COX-2 is induced in response to an inflammatory process. This leads to the synthesis and accumulation of inflammatory prostanoids, in particular prostaglandin E2, which causes inflammation, swelling and pain. The anti-inflammatory effect of the drug is carried out by blocking the production of inflammatory prostanoids by inhibiting COX-2.
In vivo and ex vivo studies indicate that celecoxib has a very low affinity for the cyclooxygenase-1 (COX-1) enzyme. Therefore, when used in therapeutic doses, celecoxib does not affect prostaglandins synthesized as a result of the activation of COX-1, and due to this it does not affect the normal physiological processes associated with COX-1 in tissues, especially in the tissues of the stomach, intestines and platelets.
Indications
– osteoarthritis
– rheumatoid arthritis
– pain of various etiologies (including postoperative, toothache, menstrual, bone and muscle pain).
Contraindications
– a history of allergic reactions (urticaria, bronchospasm), associated with the use of acetylsalicylic acid or other NSAIDs
– severe renal dysfunction
– severe liver dysfunction
– III trimester of pregnancy
– lactation (breastfeeding)
– known hypersensitivity to
sulfonamides – increased sensitivity to the component.
Use during pregnancy and lactation
The use of Celebrex during pregnancy (especially in the third trimester) is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. If you need to use Celebrex during lactation, you should decide on the termination of breastfeeding.
Composition
1 caps. contains celecoxib 100 mg.
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, NSAID gastropathy, constipation, flatulence, increased activity of AST and ALT.
From the side of the central nervous system and peripheral nervous system: rarely – headache, dizziness, drowsiness or insomnia, blurred vision, depression, agitation, confusion, anxiety, hallucinations, hearing loss, tinnitus.
From the respiratory system: rarely – sore throat, cough, shortness of breath, bronchospasm.
From the urinary system: rarely – renal failure, edematous syndrome.
From the hemopoietic 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: alopecia, sweating, nosebleeds. There are separate reports of acute pancreatitis.
Drug Interaction
When co-administered with Celebrex with a CYP2C9 inhibitor, fluconazole may increase plasma concentrations of celecoxib (celecoxib should be used at the lowest recommended dose).
It has been established in vitro that celecoxib is a CYP2D6 inhibitor, so there is a potential for drug interaction with other drugs, which are biotransformed with the participation of this isoenzyme.
Antacids (aluminum and magnesium) reduce the rate of absorption of celecoxib by 10%, which does not cause clinically relevant effects.
No clinically relevant interaction was found in the study of the effect of Celebrex on the pharmacokinetics and / or pharmacodynamics of CYP2C9 substrates of glyburide, glibenclamide, tolbutamide in vivo.
In vitro studies have shown that CYP2C19 isoenzyme can only participate to a small extent in the metabolism of celecoxib. In the in vivo study, multiple doses of celecoxib (200 mg 2 times / day for 7 days) did not affect the clearance of a single dose of CYP2C19 substrate phenytoin. The risk of clinically relevant inhibition of CYP2C19 substrate metabolism by celecoxib is considered to be negligible.
When combined with Celebrex with warfarin and similar drugs, an increase in prothrombin time and the development of serious bleeding may occur (coagulation indices and precautions should be monitored).
No clinically relevant interaction of celecoxib with ketoconazole, lithium preparations, methotrexate was detected.
Overdose
There is no clinical experience of overdose. Healthy volunteers were given up to 1200 mg once and up to 1200 mg twice daily without clinically significant adverse effects.
Treatment: carry out symptomatic therapy. Hemodialysis is ineffective.
Storage conditions
The drug should be stored in a dry place inaccessible to children at a temperature of 15 ° to 30 ° C.
The Expiration of
is 3 years.
pharmacy terms and conditions for prescription
dosage form
dosage form
capsules
