Celebrex

Celebrex is an analgesic and anti-inflammatory drug. Consider the main indications for its use, dosage, side effects and other pharmacological properties.

The drug is classified as a non-steroidal anti-inflammatory drug. Used to eliminate pain, stiffness in rheumatism and osteoarthritis, as well as in inflammatory processes. Effectively relieves pain in menstruation in women. It is used in symptomatic therapy of many diseases, unlike other nonsteroidal anti-inflammatory drugs.

The active component is celecoxib, its effectiveness is based on inhibition of the enzyme cyclooxygenase, which is activated due to inflammatory processes in the body. The medicine has antipyretic, anti-inflammatory and analgesic effect. The therapeutic dose does not affect the function of platelets and the level of coagulation of the blood.

Indications Celebrex

Supportive treatment for many diseases involves the use of various drugs. In the indications for the use of Celebrex it is indicated that I prescribe it for symptomatic therapy. The medicine eliminates attacks of acute pain, arthritis (osteoarthritis, rheumatoid), spondylitis, algodismenorea. It can be used in the complex therapy of adenomatous polyposis to reduce the size and quantity of adenomatous colorectal polyps.

The use of this medication increases the risk of developing thrombosis in vital organs. Therefore, treatment is recommended to be carried out in minimum effective doses and for a short period of time. This drug does not replace acetylsalicylic acid, because it does not have antiplatelet properties. During the therapy, you need to control blood pressure, as there is a risk of developing hypertension.

Use with extreme caution in patients with chronic heart failure due to the risk of fluid retention in the body and the development of peripheral edema. In the process of therapy, it is recommended to monitor kidney function, since tablets can have a nephrotoxic effect.

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Release form

Celebrex is available in the form of capsules, this form of release is due to ease of use and convenience in the selection of the therapeutic dosage. Capsules with an enteric coating contain 100 and 200 mg of active ingredient. In one package can be 10 or 20 pieces of tablets.

The active component of the drug is celecoxib, as additional: Na lauryl sulfate, croscarmellose Na, povidone, lactose monohydrate and Mg stearate.

[2], [3]

Pharmacodynamics

The mechanism of action of the active substance is based on suppression of cyclooxygenase 2 activity and minimal suppression of cyclooxygenase 1. Pharmacodynamics indicate that COX2 amplification is based on a response to the release of biologically active substances due to inflammation. The drug has anti-inflammatory, analgesic and antipyretic properties, and with prolonged use reduces the risk of cancer of the colon.

The active ingredient does not interfere with the functioning of the stomach and intestines. According to medical studies, a dosage of 120 mg per day does not affect blood clotting and platelet function. Celecoxib reduces the risk of nonfatal stroke, increases the risk of non-fatal heart attack, and does not affect cardiovascular mortality. 

[4], [5], [6], [7], [8]

Pharmacokinetics

The effectiveness of the drug is largely determined by the processes of absorption, distribution and metabolism. The pharmacokinetics of Celebrex indicate its absorption from the digestive tract. The maximum concentration in the blood plasma occurs 3 hours after admission. Oily foods slow the absorption process. In this case, the maximum concentration is noted after 6-7 hours, so it is recommended to take the tablets on an empty stomach. Metabolites, formed as a result of biotransformation of the active component, are excreted through the liver. The substance penetrates the blood-brain barrier.

With special care, Celebrex is prescribed to patients with a small body weight, since they have an elevated concentration of the substance in the blood. In case of violations of the liver or kidneys, a dose adjustment is required. The drug has a temporary decrease in sodium excretion, which can cause fluid retention and swelling. This condition does not require treatment, as the swelling itself passes. 

[9], [10], [11], [12], [13], [14],

Dosing and administration

To achieve a stable therapeutic effect, an individual course of therapy is chosen for each patient. The method of application and dose of Celebrex depends on the disease that is treated, the age of the patient and other characteristics of his body. The recommended dose is 200 mg twice a day. But since the medicine causes complications from the cardiovascular system, the treatment is broken into courses of short duration with interruptions.

• Osteoarthritis - 200 mg once a day or 100 mg twice a day. The maximum dosage is 800 mg, without the risk of side effects.
• Rheumatoid arthritis is 200-400 mg twice a day.
• Ankylosing spondylitis is a daily dose of 200 mg once a day or twice in 100 mg. The maximum dosage is 400 mg.
• With familial adenomatous polyposis, 400 mg twice a day.
• To eliminate acute pain - 400-600 mg per day with a gradual decrease in dosage to 200 mg.

When treating patients with severe disturbances in the baking function, a dosage adjustment is required, which, as a rule, is reduced by a factor of 2.

[16], [17], [18], [19], [20]

Use Celebrex during pregnancy

Symptomatic treatment of various diseases and attacks of acute pain in expectant mothers is carried out only by safe drugs that do not affect the development of the fetus. The use of Celebrex during pregnancy is possible on strict indications. This takes into account the possible risk of side effects in the child and the negative impact on the mother's body.

The drug is contraindicated to use in the third trimester. The active substance suppresses the production of prostaglandins, which causes disturbances in the contractile activity of the uterus. It is not used during lactation, since the active components are excreted in breast milk.

Contraindications

Any pharmacological agent has a number of restrictions on use. Consider contraindications to the use of Celebrex:

• Hypersensitivity to the active ingredient and other components of the drug.
• Intolerance to sulfonamides.
• Increased risk of allergic reactions with NSAIDs or acetylsalicylic acid.
• Application as an analgesic in the postoperative period with aortocoronary bypass.

If the above recommendations are not followed, there is a risk of developing negative symptoms from all organs and systems.

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Side effects Celebrex

Violation of the rules for the use of medication causes side effects. If the drug is used for longer than 12 weeks at a dosage of 100-800 mg, then there may be such adverse reactions as:

• Frequent - skin allergic reactions, abnormalities in the work of the gastrointestinal tract, peripheral puffiness, infections of the upper respiratory tract and urinary tract, insomnia, cough, rhinitis.
• Infrequent - anemia, arterial hypertension, tinnitus and visual impairment, hives, arrhythmias.
• Rare - chronic heart failure, increased activity of transaminases, confusion, angioedema.

If the tablets are used for a long period of time (more than 3 years) at a dosage of 400-800 mg, then the following symptoms are possible:

• Frequent - arterial hypertension, ear and fungal infections, stool disorders, prostatitis, angina.
• Infrequent - sleep disorders, increased hemoglobin, conjunctival hemorrhage, decreased hematocrit, arrhythmia, hemorrhoidal and vaginal bleeding, coronary atherosclerosis.

Overdose

If non-compliance with medical recommendations for the use of Celebrex, exceeding the recommended dosage or course of therapy, there are adverse symptoms. Overdosing manifests itself as an increase in side effects.

Symptomatic therapy and measures to remove celecoxib from the body are performed to eliminate signs of overdose.

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Interactions with other drugs

Effective treatment involves the use of several drugs at the same time. Interactions with other drugs are possible only with appropriate medical indications. Since Celebrex is biotransformed with the active participation of P450 2C9, it is allowed to use it with certain medications.

• When used with warfarin, there is a risk of fatal bleeding.
• When used with ketonazole or fluconazole, the concentration of celecoxib in the blood increases twofold.
• In the case of combined treatment with lithium preparations, its increase in blood by 15-17% is observed. This interaction requires careful medical monitoring and regular testing of analyzes of basic life indicators.
• With the use of angiotensin 2 blockers or angiotensin-converting enzyme (ACE inhibitors), their antihypertensive properties decrease.
• Do not use with other non-steroidal anti-inflammatory drugs.

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Storage conditions

The medicinal properties of Celebrex, like other tableted preparations, depend on the conditions of its storage. Capsules should be kept in their original packaging, in a dry place, protected from sunlight and out of the reach of children. The permissible storage temperature is 16-25 ° C.

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Shelf life

Celebrex is allowed to be used for 3 years from the date of its manufacture, which is indicated on the package of the product. At the expiration date, the drug is contraindicated to take and must be disposed of. The use of delayed tablets leads to uncontrolled side effects on the part of all organs and systems of the body.