Celebrex - instructions for use, analogs, reviews and release forms (capsules or tablets of 100 mg and 200 mg) of the drug for the treatment of pain in arthrosis and arthritis in adults, children and pregnancy. Composition and interaction with alcohol

In this article, you can read the instructions for using the drug Celebrex. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Celebrex in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Celebrex in the presence of existing structural analogues.Use to treat pain in arthrosis and arthritis in adults, children, as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.

Celebrex non-steroidal anti-inflammatory drug (NSAID). Celecoxib (Celebrex drug active substance) possesses anti-inflammatory, analgesic and antipyretic activity by blocking formation of inflammatory prostaglandins mainly due to inhibition of COX-2. Induction of COX-2 occurs in response to the inflammatory process and leads to the synthesis and accumulation of prostaglandins, especially prostaglandin E2, thus there is increasing incidence of inflammation (swelling and pain). At therapeutic doses in humans celecoxib did not significantly inhibit COX-1 and does not affect the prostaglandins, synthesized by the activation of COX-1 and has no effect on normal physiological processes associated with COX-1 and occurring in tissues, especially in the tissues of the stomach, intestines and platelets.

Influence on kidney function. Celecoxib reduced urinary excretion of prostaglandin E2 and 6-keto-prostaglandin F1 (prostacyclin metabolite), but has no effect on serum thromboxane B2 and urinary excretion of 11-dehydro thromboxane B2, metabolite thromboxane (both - Products of COX-1).Celecoxib does not cause a decrease in the glomerular filtration rate in elderly patients and patients with chronic renal failure, transiently reduces excretion of sodium. In patients with arthritis, the observed incidence of peripheral edema, arterial hypertension, and heart failure is comparable to that of non-selective COX inhibitors that have inhibitory activity against COX-1 and COX-2.

Composition

Celecoxib + excipients.

Pharmacokinetics

When taken on an empty stomach, Celebrex is well absorbed. Absolute bioavailability of the drug has not been studied. Influence of food intake: taking celecoxib along with fatty foods increases the time to reach Cmax by about 1-2 hours and increases total absorption by about 20%. Binding to plasma proteins does not depend on the concentration and is about 97%, celecoxib does not bind to red blood cells. Penetrates through the blood-brain barrier (BBB). Celecoxib is metabolized in the liver, excreted in feces and urine in the form of metabolites (57% and 27%, respectively), less than 3% of the accepted dose - in unchanged form.

Indications

• symptomatic treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis;
• pain syndrome: back pain, musculoskeletal, postoperative and other types of pain;
• treatment of primary dysmenorrhea.

Forms of release

Capsules 100 mg and 200 mg (sometimes mistakenly called pills).

Other dosage forms, whether injections in ampoules for injections or candles, do not exist.

Instructions for use and dosage

The drug is taken orally, regardless of the meal, the capsules are not chewed with water.

Since the risk of possible cardiovascular complications may increase with increasing dose and duration of Celebrex, it should be prescribed as shortly as possible and at the lowest recommended doses. The maximum recommended daily dose for long-term admission is 400 mg.

With symptomatic treatment of osteoarthritis, the recommended dose is 200 mg per day for 1 or 2 doses. The safety of taking the drug in doses up to 400 mg twice a day was noted.

With the symptomatic treatment of rheumatoid arthritis, the recommended dose is 100 mg or 200 mg 2 times a day. The safety of taking the drug in doses up to 400 mg twice a day was noted.

With the symptomatic treatment of ankylosing spondylitis, the recommended dose is 200 mg per day in 1 or 2 doses. If necessary, the dose may be increased to 400 mg per day.

In the treatment of pain syndrome and primary dysmenorrhea, the recommended initial dose is 400 mg, followed, if necessary, by taking an additional dose of 200 mg on the first day. In the following days, the recommended dose is 200 mg twice a day (if necessary).

Older patients usually do not need dose adjustment. However, in patients with a body weight below 50 kg, treatment should be started with the lowest recommended dose.

In patients with mild liver failure (class A on the Child-Pugh scale), dose adjustment is not required, in the case of moderate-degree liver failure (class B on the Child-Pugh scale), treatment should begin at the minimum recommended dose.

In patients with mild to moderate renal insufficiency, dose adjustment is not required. The experience of using the drug in patients with renal insufficiency is not severe.

Patients taking Fluconazole (inhibitor of CYP2C9),Celebrex should be given at the lowest recommended dose.

Side effect

• exacerbation of allergic diseases;
• influenza-like syndrome;
• accidental injury;
• peripheral edema;
• diarrhea;
• dyspepsia;
• vomiting;
• flatulence;
• stomach ulcer and duodenal ulcer;
• intestinal perforation;
• gastrointestinal bleeding;
• Diseases of the teeth (postextraction lunechke alveolitis);
• dizziness;
• insomnia;
• drowsiness;
• confusion of consciousness;
• hallucinations;
• urinary tract infection;
• acute renal insufficiency;
• interstitial nephritis;
• bronchitis;
• cough;
• pharyngitis;
• rhinitis;
• sinusitis;
• upper respiratory tract infection;
• itching;
• skin rash;
• hives;
• anaphylaxis;
• angioedema;
• anemia, ecchymosis, thrombocytopenia;
• weighting of the course of arterial hypertension;
• increased blood pressure;
• arrhythmia;
• tides;
• palpitation;
• tachycardia;
• noise in ears;
• blurring of vision;
• loss of taste;
• loss of smell;
• vasculitis;
• hemorrhages in the brain;
• photosensitization;
• skin peeling (including with erythema multiforme and Stevens-Johnson syndrome);
• toxic epidermal necrolysis;
• violation of the menstrual cycle;
• embolism of the pulmonary arteries;
• pain in the chest.

Contraindications

• bronchial asthma, urticaria, or allergic reactions after taking acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (NSAIDs), including other COX-2 inhibitors;
• condition after aortocoronary bypass surgery;
• peptic ulcer in the phase of exacerbation;
• gastrointestinal bleeding;
• inflammatory bowel disease;
• Heart failure (2-4 functional classes according to the NYHA classification);
• clinically confirmed CHD;
• diseases of peripheral arteries and cerebrovascular diseases of severe degree;
• severe hepatic insufficiency (no experience of use);
• severe renal failure (no experience of use);
• pregnancy;
• lactation period (breastfeeding);
• age to 18 years (no experience of application);
• hypersensitivity to the components of the drug;
• hypersensitivity to sulfonamides.

Application in pregnancy and lactation

Clinical experience with celecoxib during pregnancy is limited. The potential risk of using Celebrex during pregnancy is not established, but can not be ruled out.Celecoxib, which is an inhibitor of prostaglandin synthesis, in case of admission during pregnancy, especially in the 3rd trimester, can cause weakness of uterine contractions and premature closure of the ductus arteriosus.

There is limited evidence that celecoxib is excreted in breast milk. Given the potential for the development of side effects when taking celecoxib in a breastfeeding baby, the advisability of continuing breastfeeding should be assessed, given the importance of taking Celebrex for the mother.

Use in children

Contraindicated in children under the age of 18 years (no experience of use).

special instructions

Celecoxib (like all coxibs) can increase the risk of serious complications from the cardiovascular system, such as thrombosis, myocardial infarction and stroke, which can lead to death. The risk of these reactions may increase with the duration of the drug, as well as in patients with diseases of the cardiovascular system. To reduce the risk of these reactions in patients taking Celebrex, it should be prescribed at the lowest recommended doses and as short as possible.The attending physician and patient should keep in mind the possibility of such complications even in the absence of previously known cardiovascular symptoms. Patients should be informed of the signs and symptoms of adverse effects on the cardiovascular system and the measures to be taken if they occur.

Caution should be used celecoxib (like other NSAIDs) in patients with arterial hypertension. At the beginning of therapy with Celebrex, and during the course of treatment should regularly monitor blood pressure.

Effect on the gastrointestinal tract. In patients taking celecoxib, very rare cases of perforation, ulceration and bleeding from the gastrointestinal tract were observed. The risk of these complications in the treatment of NSAIDs is highest in elderly patients with cardiovascular diseases, in patients receiving Acetylsalicylic acid concomitantly, and patients with ulcerative gastrointestinal lesions, bleeding in the acute stage and in anamnesis. Most spontaneous reports of serious side effects from the gastrointestinal tract related to elderly and weakened patients.

Joint use with Warfarin and other anticoagulants.Serious reports have been reported, and some of them have been fatal, bleeding in patients who received concomitant treatment with warfarin or similar agents. Since there was reported an increase in prothrombin time, then after starting treatment with Celebrex or changing its dose, it is necessary to monitor anticoagulant activity.

Fluid retention and swelling. As with the use of other drugs that inhibit the synthesis of prostaglandins, fluid retention and swelling may occur in a number of patients taking Celebrex, so caution should be exercised when prescribing this medication to patients with conditions predisposing or worsening due to fluid retention. Patients with a history of heart failure or hypertension should be closely monitored.

Influence on kidney function. Celebrex should be used with caution in patients with impaired renal function. The function of the kidney in these patients should be carefully monitored.

Cailebrex should be used with caution in patients with dehydration. In such cases, it is advisable to first rehydrate, and then begin therapy with Celebrex.

Effect on liver function. Celebrex should be used with caution in the treatment of patients with moderate hepatic impairment and prescribe at the lowest recommended dose. In some cases, severe liver reactions have been reported, including fulminant hepatitis (sometimes fatal), liver necrosis (sometimes fatal or the need for liver transplantation). Most of these reactions developed 1 month after the initiation of celecoxib. Patients with symptoms of impaired liver function, or in case of abnormal liver function by laboratory methods, require careful monitoring to promptly diagnose more severe liver reactions during treatment with Celebrex.

Anaphylactic reactions. When taking Celebrex, cases of anaphylactic reactions were reported.

Celebrex, given the antipyretic effect, can reduce the diagnostic significance of such a symptom as fever, and affect the diagnosis of infection.

Very rarely, when taking celecoxib, there were serious reactions from the skin, such as exfoliative dermatitis,Stevens-Johnson syndrome and toxic epidermal necrolysis, some of them fatal. The risk of occurrence of such reactions in patients at the beginning of therapy is higher, in most noted cases such reactions began in the first month of therapy. You should stop taking Celebrex with skin rash, changes in the mucous membranes, or other signs of hypersensitivity.

Impact on the ability to drive vehicles and manage mechanisms

The effect of celecoxib on the ability to drive vehicles and control mechanisms has not been investigated. Based on the pharmacodynamic properties and general safety profile, it seems unlikely that Celebrex has such an effect.

Drug Interactions

Studies have shown that celecoxib, although not a substrate of CYP2D6, inhibits its activity. Therefore, there is a possibility of drug interaction with drugs whose metabolism is associated with cytochrome CYP2D6.

With simultaneous administration with warfarin and other anticoagulants, an increase in prothrombin time is possible.

The intake of alcohol enhances and increases the likelihood of side effects of Celebrex on the body (especially gastrointestinal bleeding).

For patients taking fluconazole (inhibitor CYP2C9), celecoxib should be given at the lowest recommended dose, Ketoconazole (CYP3A4 inhibitor) does not have a clinically significant effect on celecoxib metabolism.

Inhibition of prostaglandin synthesis can reduce the effect of ACE inhibitors and angiotensin 2 antagonists. This interaction should be taken into account when assigning celecoxib in conjunction with ACE inhibitors / angiotensin 2 antagonists. However, no significant pharmacodynamic interaction with lisinopril was observed with respect to influence on BP.

Known previously non-steroidal anti-inflammatory drugs (NSAIDs) in some patients may reduce the natriuretic effect of Furosemide and thiazides by inhibiting renal synthesis of prostaglandins, this should be borne in mind when assigning celecoxib.

There was no clinically significant effect of celecoxib on the pharmacokinetics of combination contraceptives containing 1 mg of norethisterone / 35 μg of ethinylestradiol).

There was an increase in the concentration of lithium in the plasma by about 17% with the combined use of lithium and celecoxib. Patients receiving lithium therapy should be closely monitored for the appointment or withdrawal of celecoxib.

There was no clinically significant interaction between celecoxib and antacids (aluminum and magnesium preparations), omeprazole, methotrexate, glibenclamide, phenytoin, or tolbutamide.

Celebrex does not affect the antiplatelet effect of acetylsalicylic acid, therefore it can not be regarded as a substitute for acetylsalicylic acid, which is prescribed for the prevention of cardiovascular diseases.

Other NSAIDs. It should avoid the simultaneous use of celecoxib with other NSAIDs (not containing acetylsalicylic acid).

Analogues of Celebrex

Structural analogs for the active substance:

• Coxib.

Analogues on the therapeutic effect (means for the treatment of pain in the joints):

• Actasulide;
• Ambien;
• Amelotex;
• Anopyrine;
• Apizarthron;
• Arkoxy;
• Arthro Active;
• Askalcin;
• Asqaff;
• Aspizol;
• Aspirin;
• Aflubin;
• Acylpyrine;
• Acifein;
• Badyaga;
• Betalgon;
• Bethanicomylon;
• Biopin;
• I took it;
• Brustan;
• Burana;
• Beliefed;
• Viprosal B;
• Voltaren Akti;
• Guevadal;
• Gialgan Phidias;
• Humisol;
• Diklobene;
• Diqlovit;
• Diclofenac;
• Diclofenacol;
• Dimexide;
• Deep Relief;
• Deep Heath;
• Dolgit;
• Ibufen;
• Iprene;
• Capsicam;
• Ketanov;
• Ketonal DUO;
• Ketorol;
• Ketorolac Rhompharm;
• Meloksikam;
• Mentoclar;
• MIG 200;
• MIG 400;
• Movix;
• Nyz;
• Nemux;
• Niflugel;
• Nifluryl;
• Novigan;
• Oxadol;
• Ostenil;
• Pamol;
• Payne;
• Pentalgin;
• Pirabutol;
• Pliwalgin;
• Protradon;
• Prohodol;
• Rapent Rapid;
• Revalgine;
• Remetan;
• Remidon;
• Solpaflex;
• Teraflex Advance;
• Thermo rheumont;
• Tetralgin;
• Tiapride;
• Tobitil;
• Fendivia;
• Finalgon;
• Flamax forte;
• Flamax;
• Fleksen;
• Floiled;
• Flugalin;
• Fortalgin C;
• Hyrumat;
• Hotemin;
• Yunispaz.

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