Celebrex capsules 200 mg 30 pcs
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Active ingredients
Celecoxib
Release form
Capsules
Composition
Capsules, composition (1 capsule.): Active substance: celecoxib - 200 mg; excipients: lactose monohydrate - 49.8 mg; sodium lauryl sulfate - 8.1 mg; Povidone K30 - 6.7 mg; croscarmellose sodium - 2.7 mg; magnesium stearate - 2.7 mg; shell: titanium dioxide - about 1.7 mg; gelatin - about 58.3 mg; ink for capsules, 200 mg: yellow ink SB-3002 (contain shellac - 22–27%, ethanol - 33–38%, isopropanol - 3–7%, butanol - 4–9%, propylene glycol - 3–6%, ammonia water - 1–2%, iron dye yellow oxide (E172) - 18–22%
Pharmacological effect
anti-inflammatory, antipyretic, analgesic
Pharmacokinetics
Suction. When taken on an empty stomach, celecoxib is well absorbed, Tmax in plasma is about 2-3 hours. Cmax in plasma after administration of 200 mg is 705 ng / ml. The absolute bioavailability of the drug has not been studied. Cmax and AUC are approximately proportional to the dose taken in the dose range up to 200 mg 2 times a day; when using celecoxib at higher doses, the degree of increase in Cmax and AUC occurs less proportionally .; The influence of food intake. Taking celecoxib with fatty foods increases Tmax by about 4 hours and increases absorption by about 20% .; Distribution. Plasma protein binding does not depend on concentration and is about 97%; celecoxib does not bind to red blood cells. Celecoxib penetrates through the BBB .; Metabolism. Celecoxib is metabolized in the liver by hydroxylation, oxidation, and partially glucuronidation. Metabolism mainly proceeds with the participation of cytochrome P450 CYP2C9 (see "Interaction"). Metabolites found in blood are pharmacologically inactive with respect to COX-1 and COX-2 .; Cytochrome P450 CYP2С9 activity is reduced in individuals with a genetic polymorphism, such as a polymorphism that is homozygous for CYP2С9 * 3, which leads to a decrease in the efficiency of enzymes .; Inference. Celecoxib is metabolized in the liver, excreted through the intestine and kidneys as metabolites (57 and 27%, respectively), less than 1% of the dose taken - unchanged. With repeated use, T1 / 2 is 8–12 hours, and clearance is about 500 ml / min. With repeated use of Css in plasma is achieved by the 5th day. The variability of the main pharmacokinetic parameters (AUC, Cmax, T1 / 2) is about 30%. The average Vss is about 500 L / 70 kg in young healthy adult patients, indicating a wide distribution of celecoxib in the tissue .; Special patient groups; Elderly patients.In patients older than 65 years, there is an increase of 1.5–2 times the average Cmax, AUC values of celecoxib, which is largely due to a change in body weight rather than age (in elderly patients, as a rule, there is a lower average body weight than in younger people, which is why, ceteris paribus, higher celecoxib concentrations are achieved. For the same reason, older women usually have a higher plasma concentration than older men. These pharmacokinetic features, as a rule, do not require dose adjustment. However, in elderly patients with a body weight below 50 kg, treatment should be started with the lowest recommended dose .; Race. The representatives of the Negroid race AUC celecoxib is about 40% higher than the Europeans. The causes and clinical significance of this fact are unknown, therefore the treatment of such patients is recommended to begin with the minimum recommended dose .; Liver dysfunction. Celecoxib plasma concentrations in patients with a mild degree of liver failure (class A according to the Child-Pugh classification) change slightly. In patients with moderately severe hepatic insufficiency (Child-Pugh class B), plasma celecoxib concentration can be almost doubled; Impaired renal function. In elderly patients with reduced GFR> 65 ml / min / 1.73 m2 associated with age-related changes, and in patients with GFR of 35–60 ml / min / 1.73 m2, the pharmacokinetics of celecoxib does not change. There is no significant association between serum creatinine content (or creatinine clearance) and celecoxib clearance. It is assumed that the presence of severe renal failure does not affect the clearance of celecoxib, since the main route of its elimination is the transformation in the liver into inactive metabolites.
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.
Contraindications
hypersensitivity to celecoxib or any other component of the drug; ; known hypersensitivity to sulfonamides; ;bronchial asthma,urticaria or allergic reactions after taking acetylsalicylic acid or other NSAIDs, including other COX-2 inhibitors; condition after coronary artery bypass surgery; ; peptic ulcer in the acute stage or gastrointestinal bleeding; inflammatory bowel disease; heart failure (NYHA II – IV); clinically confirmed coronary heart disease, peripheral arterial disease and cerebrovascular diseases in the severe stage; ; severe hepatic and renal failure (no experience of use); ; pregnancy and lactation (see. "Use during pregnancy and lactation"); ; age up to 18 years (no experience of use) .; With care: diseases of the gastrointestinal tract (peptic ulcer, bleeding in history), the presence of Helicobacter pylori infection; combined use with anticoagulants (warfarin), antiplatelet agents (acetylsalicylic acid, clopidogrel), oral GCS (prednisolone), diuretics, SSRIs (citalopram, fluoxetine, paroxetine, sertraline); fluid retention and edema; abnormal liver function of moderate severity (see. "Special instructions"); diseases of the cardiovascular system (see "Special instructions"); cerebrovascular diseases; dyslipidemia / hyperlipidemia; diabetes; peripheral arterial disease; simultaneous use with inhibitors of an isoenzyme CYP2С9; patients who are slow metabolizers or are suspected of having such a condition; long-term use of NSAIDs; severe somatic diseases.
Use during pregnancy and lactation
There are insufficient data on the use of celecoxib in pregnant women. The potential risk of using the drug Celebrex during pregnancy has not been established, but it cannot be excluded .; In accordance with the mechanism of action, with the use of NSAIDs, including celecoxib, some women may develop changes in the ovaries, which can cause complications during pregnancy. For women who are planning a pregnancy or are being screened for infertility, consideration should be given to discontinuing NSAIDs, including celecoxib .; Celecoxib, belonging to the group of inhibitors of GHG synthesis, when taken during pregnancy, especially in the third trimester, can cause weakness of uterine contractions and premature closure of the arterial duct in the fetus.The use of inhibitors of GHG synthesis at an early stage of pregnancy may adversely affect the course of pregnancy .; There is limited evidence that celecoxib is excreted in breast milk. Studies have shown that celecoxib is secreted into breast milk at very low concentrations. However, taking into account the potential for side effects of celecoxib in an infant to be fed, the feasibility of canceling either breastfeeding or taking celecoxib should be evaluated, given the importance of taking Celebrex for the mother.
Dosage and administration
Inside, without chewing, drinking water, regardless of the meal .; Since the risk of possible complications on the part of the cardiovascular system may increase with increasing doses and the duration of taking Celebrex, it should be prescribed in the shortest possible courses and in the smallest effective doses. The maximum recommended daily dose for long-term use - 400 mg. Symptomatic treatment of osteoarthritis: the recommended dose is 200 mg per day for 1 or 2 doses .; Symptomatic treatment of rheumatoid arthritis: the recommended dose is 100 or 200 mg 2 times a day .; Symptomatic treatment of ankylosing spondylitis: the recommended dose is 200 mg per day for 1 or 2 doses. In some patients, the effectiveness of the use of 400 mg 2 times a day has been noted .; Treatment of pain 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 2 times a day, as needed .; Special patient groups; Elderly patients. Usually, dose adjustment is not required. However, in patients with a body weight below 50 kg, it is better to begin treatment with the lowest recommended dose .; Liver dysfunction. Patients with a mild degree of liver failure (class A according to Child-Pugh classification) do not require dose adjustment; in case of moderate hepatic insufficiency (Class B according to Child-Pugh classification), treatment should be started with the minimum recommended dose. Experience with the use of the drug in patients with severe liver failure (class C according to the classification of Child-Pugh) is not (see"Contraindications") .; Impaired renal function. In patients with mild and moderate renal insufficiency, dose adjustment is not required. Experience with the use of the drug in patients with severe renal insufficiency is not (see. "Contraindications", "Special instructions") .; Simultaneous use with fluconazole. Patients taking fluconazole (CYP2C9 isoenzyme inhibitor), Celebrex should be prescribed in the minimum recommended dose. Caution should be exercised when used simultaneously with other inhibitors of the isoenzyme CYP2C9 .; Celebrex should be used with caution in patients who are slow metabolizers or suspected of such a condition, since this can lead to the accumulation of high concentrations of celecoxib in the blood plasma. In such patients, the initial recommended dose of the drug should be halved.
Side effects
While taking the drug Celebrex, the following reactions are possible on the part of organs and systems with the following gradation in frequency: often - ≥1 and <10%; infrequently - ≥0.1 and <1%; rarely ≥0.01 and <0.1%; General: often - exacerbation of allergic diseases, flu-like syndrome, accidental injuries; infrequently - swelling of the face .; On the part of the cardiovascular system: often - peripheral edema; infrequently - weighting of the course of arterial hypertension, increase in blood pressure, arrhythmia, hot flashes, palpitations, tachycardia; rarely, congestive heart failure, ischemic stroke and myocardial infarction .; On the part of the gastrointestinal tract: often - abdominal pain, diarrhea, dyspepsia, flatulence, diseases of the teeth (postextraction alveolar alveolitis); infrequently - vomiting; rarely - gastric and duodenal ulcer, esophageal ulceration, intestinal perforation, pancreatitis .; On the part of the nervous system: often - dizziness, increased muscle tone, insomnia; infrequently - anxiety, drowsiness; rarely confusion; On the part of the kidneys and urinary system: often - urinary tract infection .; On the part of the respiratory system: often - bronchitis, cough, pharyngitis, rhinitis, sinusitis, infections of the upper respiratory tract .; On the part of the skin: often - itching, skin rash; infrequently - alopecia, urticaria .; From the side of blood: infrequently - anemia, ecchymosis, thrombocytopenia .; From the senses: infrequently - tinnitus,blurred vision .; On the part of the immune system: rarely - angioedema, bullous eruptions .; On the part of the hepatobiliary system: rarely - increased activity of liver enzymes .; Side effects identified in post-marketing observations; Immune system: anaphylaxis .; The nervous system: loss of taste, loss of smell, aseptic meningitis, hallucinations .; On the part of the organ of vision: conjunctivitis .; On the part of the vessels: vasculitis, hemorrhage in the brain .; On the part of the digestive tract: gastrointestinal bleeding .; On the part of the hepatobiliary system: hepatitis, liver failure, fulminant hepatitis, hepatic necrosis (see "Special Instructions", effect on liver function), cholestasis, cholestatic hepatitis, jaundice .; On the part of the kidneys and urinary system: acute renal failure (see "Special instructions", the impact on the kidney function), interstitial nephritis, nephrotic syndrome, minimal renal impairment, hyponatremia .; On the part of the skin: photosensitivity reactions, peeling of the skin (including erythema multiforme and Stevens-Johnson syndrome), toxic epidermal necrolysis, drug rash combined with eosinophilia and systemic symptoms (DRESS - Drug Reaction (or Rash) with Eosinophilia and Systemic Symptoms - or hypersensitivity syndrome), acute generalized exantmatous pustus; On the part of the reproductive system: menstrual disorders, decreased fertility in women (see. "Use during pregnancy and lactation") .; Respiratory, thoracic and mediastinal disorders: pulmonary embolism .; Systemic disorders: pain in the chest.
Overdose
The clinical experience of overdose is limited. Without clinically significant side effects, single doses up to 1200 mg and multiple doses up to 1200 mg were applied in 2 doses per day .; Treatment: it is necessary to ensure the conduct of appropriate maintenance therapy. Presumably dialysis is not an effective method of removing the drug from the blood due to the high degree of binding of the drug to plasma proteins.
Interaction with other drugs
In vitro studies have shown that celecoxib, although not a substrate of the CYP2D6 isoenzyme, inhibits its activity.Therefore, there is the likelihood of drug interactions in vivo with drugs whose metabolism is associated with the CYP2D6 isoenzyme .; Warfarin and other anticoagulants: while taking it may increase the PV .; Fluconazole, ketoconazole: with the simultaneous use of 200 mg of fluconazole 1 time per day, an increase in plasma concentration of celecoxib is noted in 2 times. This effect is associated with inhibition of celecoxib metabolism by fluconazole via the CYP2C9 isoenzyme. Patients taking fluconazole (an inhibitor of the isoenzyme CYP2C9), celecoxib should be used in the lowest recommended dose (see. "
Dosage and administration
"). Ketoconazole (a CYP3A4 isoenzyme inhibitor) does not have a clinically significant effect on celecoxib metabolism .; ACE inhibitors / angiotensin II antagonists: Inhibition of the synthesis of PG can reduce the antihypertensive effect of ACE inhibitors and / or angiotensin II antagonists. This interaction should be taken into account when using celecoxib in conjunction with ACE inhibitors and / or angiotensin II antagonists. However, there was no significant pharmacodynamic interaction with lisinopril regarding the effect on blood pressure; In elderly patients who are dehydrated (including patients receiving diuretic therapy) or in patients with impaired renal function, the simultaneous use of NSAIDs, including selective COX-2 inhibitors, with ACE inhibitors may lead to a deterioration in renal function, including possible acute renal failure these effects are usually reversible .; Diuretics: previously known NSAIDs in some patients may reduce the natriuretic effect of furosemide and thiazides by reducing renal GHG synthesis, this should be borne in mind when using celecoxib .; Oral contraceptives: there was no clinically significant effect on the pharmacokinetics of the contraceptive combination (1 mg norethisterone + 35 μg ethinyl estradiol) .; Lithium: There has been an increase in plasma lithium levels by about 17% when co-taking lithium and celecoxib. Patients receiving lithium therapy should be closely monitored when taking or canceling celecoxib .; Other NSAIDs: the simultaneous use of celecoxib and other NSAIDs (not containing acetylsalicylic acid) should be avoided .; Other drugs: there were no clinically significant interactions between celecoxib and antacids (aluminum- and magnesium-containing drugs), omeprazole, methotrexate, glibenclamide,phenytoin or tolbutamide .; Celecoxib does not affect the antiplatelet effect of acetylsalicylic acid, taken in low doses. Celecoxib has a weak effect on platelet function, so it cannot be considered as a substitute for acetylsalicylic acid used in the prevention of cardiovascular diseases.special instructions
Celebrex, given the antipyretic effect, can reduce the diagnostic significance of a symptom such as fever and affect the diagnosis of infection .; Impact on the CAS. Celecoxib, like all coxibs, can increase the risk of serious complications from CVS, such as thrombosis, myocardial infarction and stroke, which can be fatal. The risk of these reactions may increase with the dose, the duration of the drug, as well as in patients with CVD diseases and risk factors for such diseases. To reduce the risk of these reactions in patients taking Celebrex, it should be prescribed in the lowest effective doses and as short as possible (at the discretion of the attending physician). The attending physician and patient should keep in mind the possibility of such complications even in the absence of previously known symptoms of impaired CVS function. Patients should be informed about the signs and symptoms of adverse effects on the cardiovascular system and measures to be taken in case of their occurrence .; When using NSAIDs (selective COX-2 inhibitors) in patients after coronary artery bypass surgery for the treatment of pain in the first 10–14 days, it is possible to increase the incidence of myocardial infarction and cerebral circulation disorders .; Due to the weak effect of celecoxib on platelet function, it cannot be a substitute for acetylsalicylic acid for the prevention of thromboembolism. Also in this regard, antiplatelet therapy (for example, acetylsalicylic acid) should not be canceled in patients at risk of developing thromboembolic complications .; Like all NSAIDs, celecoxib can lead to an increase in blood pressure, which can also be a cause of complications from the CVS. All NSAIDs, incl. and celecoxib, in patients with arterial hypertension should be used with caution.Monitoring of blood pressure should be carried out at the beginning of celecoxib therapy, as well as during the course of treatment. Effect on the digestive tract. Celecoxib patients had extremely rare cases of perforation, ulceration and bleeding from the gastrointestinal tract. The risk of developing these complications in the treatment of NSAIDs is highest in the elderly, patients with cardiovascular diseases, patients simultaneously receiving acetylsalicylic acid, and patients with gastrointestinal diseases such as ulcers, bleeding, inflammation in the acute stage and in history. Other risk factors for the development of bleeding from the gastrointestinal tract are simultaneous use with oral GCS and anticoagulants, a long period of NSAID therapy, smoking, alcohol consumption .; Most of the spontaneous reports of serious side effects on the gastrointestinal tract were elderly and debilitated patients .; Combined use with warfarin and other anticoagulants. It was reported about serious (some of them fatal) bleeding in patients who received concomitant treatment with warfarin or similar means. Since an increase in PV has been reported, anticoagulant activity should be monitored after initiation of treatment with Celebrex or a change in its dose .; Fluid retention and edema. As with the use of other drugs that inhibit GHG synthesis, a number of patients taking Celebrex may experience fluid retention and edema, so care should be taken when prescribing this drug to patients with conditions predisposing or worsening due to fluid retention. Patients with a history of heart failure or arterial hypertension should be closely monitored .; Impact on renal function. NSAIDs, incl. and celecoxib may have a toxic effect on kidney function. It was found that celecoxib is not more toxic than other NSAIDs. Celebrex should be used with caution in patients with impaired renal function, heart failure, impaired liver function, and in elderly patients. Renal function in such patients should be carefully monitored .; Caution must be exercised when using the drug Celebrex 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 not be used in patients with severe liver function impairment (Child-Pugh class C); Celebrex should be used with caution in the treatment of patients with moderately severe liver failure and should be administered at the lowest recommended dose .; In some cases, severe reactions of the liver were observed, including fulminant hepatitis (sometimes fatal), liver necrosis (sometimes fatal or the need for liver transplantation). Most of these reactions developed 1 month after the start of celecoxib. Patients with symptoms and / or signs of abnormal liver function, or those patients who have abnormal liver function detected by laboratory methods, should be closely monitored for more severe liver reactions during treatment with Celebrex .; Anaphylactic reactions. Cases of anaphylactic reactions have been reported while taking Celebrex .; Serious reactions from the skin. It has been extremely rare for celecoxib to have severe skin reactions, such as exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis, some of which were fatal. The risk of such reactions in patients at the beginning of therapy is higher; in the majority of cases noted, such reactions began in the first month of therapy. You should stop taking Celebrex with a skin rash, changes in the mucous membranes or other signs of hypersensitivity .; GKS therapy. Celebrex cannot replace GCS or be used as a therapy for GCS deficiency .; Influence on ability to drive vehicles and work with mechanisms. The effect of celecoxib on the ability to drive a car and control mechanisms has not been investigated. However, based on the pharmacodynamic properties and overall safety profile, it seems unlikely that Celebrex has such an effect.