Celebrex

Celebrex is a modern non-steroidal anti-inflammatory drug with a complex of actions - eliminates painful sensations, reduces body temperature with fevers, blocks inflammation.

Functionality is due to the presence of the active component of celecoxib. Does not affect the processes of the gastrointestinal tract. The maximum concentration of Celebrex after oral administration comes after 3 hours. Further, the preparation completely binds to plasma proteins and is evenly distributed throughout the body. The ability of Celebrex to penetrate through the natural protective barriers of the body is noted.

Celebrex causes significantly fewer side effects than other NSAID drugs. It is assigned only to adults.

Clinical and pharmacological group

NSAIDs. Highly selective COX-2 inhibitor.

Terms of sale from pharmacies

Can buywithout a doctor's prescription.

Price

How much does Celebrex cost in pharmacies? The average price is at the level of178 rubles.

Composition and form of release

The drug is available in the form of gelatin capsules, the contents of the capsules is white.

The main active ingredient of the drug is celecoxib, its content in one capsule can be 200 and 400 mg. It also includes auxiliary components, which include:

• Croscarmellose sodium.
• Water ammonia.
• Ethanol.
• Gelatin.
• Propylene glycol.
• Lactose monohydrate.
• Isopropanol.
• Magnesium stearate.
• Sodium lauryl sulfate.

Pharmacological effect

The mechanism of action of the active substance celecoxib is to suppress COX-2, which are activated in response to the release of biological substances after the onset of inflammation. The medicine has an analgesic, antipyretic effect and has an anti-inflammatory effect. According to research, Celebrex is effective in reducing the incidence of colon cancer. The drug does not affect the course of natural functions of platelets, stomach and intestines, reduces the risk of ulcers and complications, compared with other NSAIDs.

Anti-inflammatory medication does not affect the mortality from cardiovascular diseases, increases the likelihood of a non-fatal heart attack, but reduces the likelihood of a non-fatal stroke. The drug is perfectly absorbed from the digestive tract, reaches its maximum concentration 2-3 hours after application. Fatty foods increase this figure to 6-7 hours. As a result of biotransformation, three metabolites are produced, secreted through the liver.

Indications for use

The reception of Celebrex capsules is indicated for the treatment of various inflammatory pathologies, as well as reducing the severity of the pain syndrome:

• Back pain.
• Pain after surgery.
• Symptomatic treatment aimed at reducing the severity of inflammation in the pathology of the structures of the musculoskeletal system - rheumatoid arthritis (autoimmune lesion of joints), osteoarthrosis (degenerative-dystrophic joint damage accompanied by the development of an inflammatory reaction).

Also, the drug is used to treat primary algodismorrhoea in women (menstruation, accompanied by severe pain)

Contraindications

Absolute contraindications:

• progressive kidney disease, severe renal failure with creatinine clearance less than 30 ml / min, hyperkalemia (confirmed);
• exacerbation of inflammatory bowel diseases (ulcerative colitis, Crohn's disease);
• deficiency of lactase, glucose-galactose malabsorption, lactose intolerance;
• increased sensitivity to any component of the drug;
• increased sensitivity to sulfonamides;
• a combination of recurrent nasal polyposis and paranasal sinuses, bronchial asthma and intolerance to acetylsalicylic acid or other NSAIDs, including other COX-2 inhibitors (including in the anamnesis);
• chronic heart failure (II-IV functional class according to NYHA);
• ischemic heart disease (clinically confirmed), expressed cerebrovascular diseases, peripheral arterial disease;
• hemorrhagic stroke;
• condition after coronary artery bypass grafting;
• subarachnoid hemorrhage;
• bleeding from the gastrointestinal tract, exacerbation of peptic ulcer of the stomach or duodenum, active erosive and ulcerative lesions of the mucous membrane of the stomach or duodenum;
• severe hepatic impairment;
• pregnancy and lactation;
• age to 18 years.

Relative contraindications:

• Helicobacter pylori infection;
• impaired liver function of medium severity;
• chronic renal failure with clearance of creatinine 30-60 ml / min;
• cerebrovascular diseases;
• dyslipidemia, hyperlipidemia;
• long-term use of NPFP;
• Diseases of the digestive tract (Crohn's disease, ulcerative colitis, peptic ulcer and duodenal ulcer, bleeding in the anamnesis);
• clinically significant decrease in the volume of circulating blood;
• diseases of peripheral arteries;
• diseases of the cardiovascular system, arterial hypertension;
• edema and fluid retention;
• diabetes;
• liver disease (including history);
• hepatic porphyria;
• severe stomatological diseases;
• elderly age;
• tuberculosis;
• smoking, alcoholism.

Caution should be given to Celebrex patients who are slow metabolizers, as well as suspected of this condition.

Intended use for pregnancy and lactation

Indications for Celebrex in pregnant women should be carefully evaluated by doctors. This drug can be prescribed only if the expected benefit from the therapy is significantly greater than the potential risk of fetal pathology.

In the last trimester of pregnancy Celebrex is contraindicated, because it can disrupt the contractile activity of the uterus during labor and lead to the premature closure of the oval window.

Dosage and route of administration

As indicated in the instructions for use Celebrex taken inside, regardless of food intake, without chewing, washing with water.

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

1. With symptomatic treatment of osteoarthritis, the recommended dose is 200 mg / day for 1 or 2 doses.
2. With the symptomatic treatment of rheumatoid arthritis, the recommended dose is 100 mg or 200 mg 2 times / day.
3. With symptomatic treatment of ankylosing spondylitis, the recommended dose is 200 mg / day in 1 or 2 doses. Some patients noted the effectiveness of the drug at a dose of 400 mg 2 times / day.
4. 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 2 times / 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 hepatic insufficiency (class A on the Child-Pugh scale), dose adjustment is not required. In the case of a moderate degree of hepatic insufficiency (class B on the Child-Pugh scale), treatment should begin with the minimum recommended dose. Experiments with the use of the drug in patients with severe hepatic insufficiency (class C on the Child-Pugh scale) do not.

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.

For patients taking fluconazole (CYP2C9 inhibitor), Celebrex should be given at the lowest recommended dose. With caution, the drug should be used concurrently with other inhibitors of the isoenzyme CYP2C9.

Celebrex should be used with caution in patients who are slow metabolizers or with suspicion on this state, because 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 reduced by a factor of 2.

Adverse Reactions

Celebrex has the following side effects:

1. From the hemopoietic system: thrombocytopenia, ecchymosis, anemia.
2. From the urinary system: infectious diseases of the urinary tract.
3. From the side of the peripheral and central nervous systems: insomnia, dizziness, increased muscle tone, drowsiness, anxiety, confusion.
4. From the cardiovascular system: increased blood pressure, peripheral edema, palpitation, arrhythmia, tachycardia, hot flashes, myocardial infarction, ischemic stroke, symptoms of congestive heart failure.
5. On the part of the respiratory system: cough, bronchitis, pharyngitis, sinusitis, rhinitis, infectious diseases of the upper respiratory tract.
6. On the part of the gastrointestinal tract: dyspepsia, diarrhea, abdominal pain, bloating, dental disease, vomiting, increased activity hepatic transaminases, pancreatitis, esophagus manifestation, duodenal ulcer and stomach, intestinal perforation.
7. Allergic reactions: itching, skin rash, hives, painful rashes, angioedema.

Overdose Symptoms

Often, with overdose of Celebrex, there is a significant increase in side effects. In case of intoxication of the body with this medication, immediate symptomatic treatment should be performed.

special instructions

Celebrex can influence the diagnosis of infection, which is associated with its antipyretic effect.

The cardiovascular system

Like all coxibes, celecoxib increases the risk of serious complications from the cardiovascular system (myocardial infarction, thrombosis, stroke), which can lead to death. The risk of these side effects increases with increasing dose and duration of the course of the drug, as well as in patients with increased risk or the existing diseases of the cardiovascular system. To reduce the risk of the reactions described above, the drug should be taken in a minimally effective dose; the course of taking the drug should be as short as possible (at the doctor's discretion).

When taking COX-2 inhibitors by patients, in the first 10-14 days after aortocoronary bypass surgery, the risk of myocardial infarction as well as cerebral circulation disorders increases.

Celebrex can not serve as a substitute for acetylsalicylic acid in the prevention of thromboembolism, which is due to its weak effect on the function of thrombocytes.

Celebrex, like other NSAIDs, is able to increase blood pressure, which is why when taking the drug requires regular monitoring of blood pressure.

GIT

When taking celecoxib, extremely rare cases of ulceration, perforation and bleeding of the gastrointestinal tract are described; the highest risk is in patients with cardiovascular diseases, in patients, taking patients with acetylsalicylic acid in patients with ulcers, bleeding and inflammatory diseases in the history of an exacerbation and in the elderly. Also, the risk of bleeding from the gastrointestinal tract is increased in patients taking oral glucocorticosteroids, anticoagulants, NSAIDs (long-term), alcohol users, smokers. The highest risk of undesirable effects from the gastrointestinal tract is in the elderly and weakened patients.

Kidneys

Celebrex is not more than other NSAIDs, it is able to exert a toxic effect on kidney function. With caution should apply the drug to patients with impaired renal function, liver, heart failure, as well as people of advanced age. Kidney function should be closely monitored in these patient groups. With dehydration, you first need to rehydrate, and then begin treatment with Celebrex.

Liver

If the liver function is of moderate severity, the initial dose of Celebrex should be reduced by half. In severe violations of the liver drug is contraindicated.

There are reports of severe reactions from the liver (sometimes with a fatal outcome or the need for liver transplantation), mostly started 1 month after initiation of celecoxib (in particular, fulminant hepatitis, liver necrosis, liver failure).

Patients with impaired liver function, as well as with its symptoms, need careful observation during Celebrex therapy to avoid severe liver reactions.

Skin covers

There are reports of extremely rare serious (sometimes fatal) reactions from the skin (in particular, exfoliative dermatitis, toxic epidermal necrolysis, Stevens-Johnson syndrome). Especially the risk of these complications was increased in the first month of taking the drug. When there are changes in mucous membranes, skin rashes or other symptoms of hypersensitivity, Celebrex therapy is recommended to be discontinued.

Glucocorticosteroid therapy

Do not use celecoxib for the therapy of glucocorticosteroid insufficiency.

Inhibition of the isoenzyme function of CYP2D6

At the time of taking celecoxib, it is necessary to reduce the dose of drugs metabolized by the isoenzyme CYP2D6, due to the fact that celecoxib is a moderate inhibitor of this isoenzyme.

Fluid retention and swelling

When taking Celebrex, the risk of fluid retention and edema increases, so caution should be exercised a drug for patients prone to fluid retention, or those whose condition is deteriorating because of it. Patients with an arterial hypertension or a heart failure in the anamnesis should be under observation.

Impact on the ability to drive vehicles

The effect of celecoxib on the ability to manage motor transport and other complex mechanisms is not described, however, because the drug may cause dizziness and other side effects, care should be taken when performing potentially hazardous activities.

Compatibility with other drugs

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

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

With the simultaneous use of fluconazole at a dose of 200 mg 1 time / day, there was an increase in the concentration of celecoxib in the blood plasma by a factor of 2. This effect is associated with inhibition of celecoxib metabolism by fluconazole via the CYP2C9 isoenzyme. For patients taking fluconazole (CYP2C9 inhibitor), celecoxib should be given at the lowest recommended dose. Ketoconazole (inhibitor of the isoenzyme CYP3A4) does not have a clinically significant effect on the metabolism of celecoxib.

Inhibition of prostaglandin synthesis can reduce the effect of ACE inhibitors and angiotensin II antagonists. This interaction should be taken into account in the appointment of celecoxib in conjunction with ACE inhibitors / angiotensin II antagonists. However, there was no significant pharmacodynamic interaction with lisinopril in terms of the effect on BP.

In elderly patients, in patients with dehydration (including those receiving diuretic therapy) or in patients with impaired renal function, concurrent use NSAIDs, including selective COX-2 inhibitors, with ACE inhibitors can lead to impaired renal function, including possible acute renal failure. Usually, these effects are reversible.

The previously known NSAIDs in some patients may reduce the natriuretic effect of furosemide and thiazides for account for the inhibition of 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 combined contraceptive preparations 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.

Celecoxib does not affect the antiplatelet effect of acetylsalicylic acid, taken in low doses. Celecoxib has a weak effect on the function of platelets, so it can not be considered as a substitute for acetylsalicylic acid, which is prescribed for the prevention of cardiovascular diseases.

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

Patient Reviews

We offer you to familiarize yourself with the opinions of people using Celebrex:

1. Eugene. The drug is very effective. I prefer to use short courses in 5-7 days, when the arthritic pain is very strong. For it is fraught - there is a constant therapy with warfarin. It is necessary to cover with a nolpaz and follow the MNO, the benefit of "Coagulation" at hand. While in terms of bad consequences carried (fie-fie).
2. Vera. A year ago I was diagnosed with acute arthritis. My fingers and joints ached terribly, I could not do anything with my hands. The doctor prescribed Celebrex and advised to take a course of physiotherapy. The combination of these two types of therapy gave an excellent result - my fingers became more flexible, the pain is almost not bother. However, when taking capsules sometimes I feel sick.
3. Tatyana. The only drug that really helps quickly, does not have a big effect on the stomach, and most importantly on the liver... Arkoxia does not help me at all, it raises blood pressure and liver tests. The main thing to find your drug. I found it. At the time of treatment, liquefied blood should be omega-3 in large doses. Not less than 2 grams per day.

Analogues

According to the active ingredient and pharmacological action, the following analogues of the medicamentous preparation are released, in the format of capsules and tablets coated with a film membrane:

• Arthoxy;
• Dylax;
• Zicel;
• Renseleks;
• Revmoxib;
• Flogoxib;
• Celecoxib;
• Celcox;
• Arkoxia;
• Orothix;
• Exciseus;
• Bekstra;
• Dinastat;
• Prex.

Before buying an analogue, consult your doctor.

Shelf life and storage conditions

Store in a dry place inaccessible to children at a temperature of + 15... + 30 ° C. Shelf life - 3 years.

How to choose probiotics for the intestine: a list of drugs.

Effective and inexpensive cough syrups for children and adults.

Modern non-steroidal anti-inflammatory drugs.

Review of tablets from the increased pressure of the new generation.

Antiviral drugs are inexpensive and effective.