"Celecoxib": instruction manual, reviews. Drug analogues

Treatment of diseases associated with musculoskeletal injuries requires the pharmaceutical market to create new drugs with fewer side effects and greater efficacy. Scientists have discovered and synthesized a new generation of non - steroidal anti - inflammatory drugs based on celecoxib. These medicines have less toxicity and are more easily tolerated by the body.

Description of the drug "Celecoxib"

The substance celecoxib has a pale yellow color and belongs to the group of coxibes that exhibit selective inhibition of the second type of cyclooxygenase. Medicines based on this compound have pronounced anti-inflammatory and analgesic properties. The original drug based on celecoxib is the "Celebrex" medication developed by the American company "Faizer". Its pharmacodynamic characteristics were studied and toxicity on the human body was investigated.

The remaining drugs containing the active substance celecoxib are generics, including the drug "Celecoxib".

Dosage forms

The drug is produced in hard gelatin capsules with a dosage of active substance of 100 mg and 200 mg. Unlike other non-steroidal anti-inflammatory drugs, it does not have a dosage form in the form of ointments, gels, injectable solutions or suspensions. At use by some patients the form of release of a preparation "Tselecoxib" - a tablet though the question is about capsules is wrongly called.

Composition

The active substance is the substance celecoxib in the amount of 100 mg and 200 mg. The contents of the capsules contain auxiliary components that ensure the filling of the space, the flowability and stability of the granulated mixture. These include milk sugar, sodium lauryl sulfate, polyvinylpyrrolidone (K30), croscarmellose sodium, magnesium stearate.

The instructions for use with the preparation "Celecoxib" contain a characteristic of the composition and appearance of the gelatin capsule shell. According to the description, outwardly they are matte, almost white in color and are marked with the signs "100" or "200", located on the blue or yellow strip, respectively. This allows you to recognize capsules with different dosages. The composition of yellow and blue ink is also detailed with the indication of harmless to the body dyes.

Similar drugs

The drug "Celecoxib", analogues of which also contain the active substance celecoxib, are able to exhibit the same therapeutic effect on the osteoarthritis of the human skeleton.

The original preparation "Celebrex" and its generics "Celecoxib", "Arthoxy", "Zicel", "Revmoxib", "Ranseleks" are considered interchangeable medicines. However, according to the price category, the original will cost an order of magnitude more expensive than its counterparts.

In the preparation "Celebrex" celecoxib is contained in a dosage of 100 and 200 mg, as in the drug "Celecoxib". The auxiliary components of the contents of capsules and its shell may differ in both qualitative and quantitative composition, which does not affect their properties. With regard to the form of the generic release of the drug "Celecoxib", analogues are produced only in hard gelatin capsules for internal use.

There are non-steroidal anti-inflammatory substances that act equally on the second type of cyclooxygenase, but with differences in the composition of the active component, pharmacokinetic and pharmacodynamic characteristics. These include the sulfonamide compound nimesulide, which in a daily dosage of 200 mg effectively fights the symptoms of osteoarthritis and rheumatoid arthritis. Preparations based on it have an anti-inflammatory and analgesic effect by inhibiting cyclooxygenase of the second and to a lesser extent - the first type, affecting a variety of mediators of pain and inflammation.

Like nimesulide, celecoxib is a representative of the sulfonamide class of substances and also in the daily dosage of 200 mg it eliminates the manifestations of osteoarthritis. It does not inhibit the first type of cyclooxygenase and affects a small number of mediators of the pain and inflammatory process.

An alternative to treatment with oral coxibs is injectable NSAIDs. One of the main advantages of the drug "Celecoxib" is the price. Injections (ampoules for injections) of other non-steroidal anti-inflammatory drugs will cost much more, but the effectiveness of such injections far exceeds the result of the use of drugs in solid forms.

Mechanism of action

The drug "Celecoxib" is a medicine representing a new generation of non-steroidal anti-inflammatory drugs with anti-inflammatory, analgesic, antipyretic activity. The mechanism of its action is associated with blocking the formation of prostaglandins of inflammation due to a decrease in COX activity 2.

Inflammatory reactions trigger the induction of cyclooxygenase of the second type, which in turn accelerates the synthesis and accumulation of prostaglandin substances, which increase inflammation. The state of edema and pain are developing.

The first dose of cyclooxygenase is not affected by the therapeutic dose of the drug Celecoxib. The instructions for use describe the inertness of the drug with respect to this enzyme and the physiological processes associated with its activity that occur in the cells of the gastrointestinal tract and platelet structures.

Also in the manual are data on the effect of the drug on the work of the kidneys. Under the action of celecoxib, E2 prostaglandin and F1 6-keto-prostaglandin are less removed in the urine, however, the excretion of B211-dehydro-thromboxane does not change, which indicates the selective action of the drug.

The use of the drug "Celecoxib" does not lead to a decrease in the rate of filtration in the renal glomeruli of the elderly and in patients with renal insufficiency.

Indications for use

According to the pharmacodynamic characteristics of the drug "Celecoxib" its use will be effective for the treatment of rheumatoid and psoriatic arthritis, chronic inflammation with pain in the spine and sacroiliac joints, osteoarthrosis.

Due to its analgesic properties, it is used to eliminate the painful condition with musculoskeletal pain, after surgery, with dysmenorrhea, which is accompanied by painful menstruation. The anti-inflammatory effect of the drug is aimed at reducing the outgrowths and polyps in the colon and rectum with the diagnosis of "adenomatous polyposis."

How to use

Take the medicine "Celecoxib" instruction for use recommends inside, without tying with food. Capsules do not open and do not chew, but swallow whole, drinking a lot of water.

The maximum amount of celecoxib, which is allowed to take a day, is 0.4 g. This drug is used in excess only in rare cases.

Cardiovascular complications can result in high doses and long-term therapy with the drug Celecoxib. The instruction contains information on small dosages for symptomatic treatment of each indication. Recommendations for short use are given.

To eliminate the symptoms accompanying osteoarthritis and ankylosing spondylitis, one day or two times 200 mg of the drug is taken per day.

To eliminate the symptoms of rheumatoid arthritis use a daily dose of 200 or 400 mg, which is taken twice.

Pain syndrome and primary dysmenorrhea on the first day are treated with a high dose of 400 mg, with the possible intake of another 200 mg, the next day, 200 mg twice a day are used.

Elderly people, as well as patients who have a mild degree of inadequate liver function or a mild or moderate degree of inadequate renal function, do not recalculate the dose.

Low weight (less than 50 kg), average severity of liver failure - patients of these categories prescribe treatment with low doses of the drug.

Usually for treatment of inflammatory processes in joints complex treatment based on the use of several medicines in different dosage forms is used. Combine capsules "Celecoxib", ointment or gel warming type "Apizatron" or "Finalgona. Preparations for topical use cause a temporary effect, so they are used together with medications for internal administration.

Who is prohibited from using

Not all patients with joint diseases can take the drug "Celecoxib". Instruction for use contains a list of diseases and conditions in which this drug will do more harm than good. This includes:

• Urticaria, bronchial asthma, an allergic condition from the effects of aspirin and other non-steroidal anti-inflammatory drugs;
• Recovery after surgery associated with aortocoronary bypass surgery ;
• Exacerbation of peptic ulcer;
• Gastric and intestinal bleeding;
• Inflammation of the mucosa in the intestine;
• Heart failure;
• Ischemic heart disease;
• Damage to the arteries along the periphery and cerebral vessels with impaired cerebral blood flow;
• Hepatic failure of a severe form;
• Renal failure of severe form;
• Carrying a child;
• Breastfeeding;
• Age to eighteen years;
• Hypersensitivity to excipients;
• Hypersensitivity to sulfonamide components.

With caution use the drug "Celecoxib" should people with diseases of the gastrointestinal tract, associated with peptic ulcer disease, bleeding in the past, infection with mucous bacteria of the genus Helicobacter pylori.

Water retention in the body and swelling of soft tissues, violations in the work of the liver of the middle stage, heart and vascular disease, lipid metabolism in the body, which increases the level of cholesterol in the blood plasma, diabetes sugar, somatic diseases in severe form also cause for extreme Neat use of the drug "Celecoxib" under the supervision of a doctor.

Side effects

Despite the innovative achievements in creating a new generation of coxibes, these substances and drugs based on them are not devoid of side effects.

Accompanying "Celecoxib" preparation instructions for use, reviews of patients and specialists - these sources contain information about possible undesirable consequences that can occur in the work of vital organs.

Possible negative effect on the digestive system is characterized by NSAID-gastropathy, abdominal pain, nausea, vomiting, heartburn, decreased need for food and diarrhea. Prolonged intake of large doses can provoke ulceration and bleeding in the mucous membrane of the stomach and intestines, bleeding gums, excessive activation of liver transferases.

Nervous disorders are manifested by agitation, headache, dizziness, drowsiness, insomnia, depressive states.

Influence on the cardiovascular system is due to increased pressure in the arteries, tachycardia.

The drug "Celecoxib" reduces resistance to infectious diseases of the respiratory system, which can be expressed in the development of sinusitis, rhinitis, pharyngitis, pain in the nasopharynx, cough, dyspnea, bronchospasm.

The effect of medication on the sensory organs causes a decrease in auditory perception and the appearance of noise in the ears.

The drug "Celecoxib" influences the urinary system in such a way that renal insufficiency may develop with the development of edematous syndrome.

As for the hemopoietic organs, the drug can cause the manifestation of agranulocytosis, anemia, leukopenia, thrombocytopenia.

There may be skin rashes of an allergic nature with the appearance of itching, urticaria, photosensitivity, angioedema in the facial area, extremities, genitals.

Reception Features

The drug "Celecoxib" has a drawback associated with an increased risk of adverse effects on the cardiovascular system, leading to thrombosis, myocardial infarction, and stroke. Especially the risk increases with prolonged use of medication by patients who have heart and vascular disease.

To reduce the risk of such complications, patients taking the drug "Celecoxib" are prescribed a minimum dose for the shortest period of treatment. The patient should discuss with the attending physician possible signs of the disease and get recommendations on how to respond when they occur.

To reduce cardiovascular symptoms, a combination of acetylsalicylic acid in minimal doses with the drug "Celecoxib" is used. The doctors' testimonies testify to the antiaggregant effect of aspirin for the dilution of blood when taking coxibs, which do not have such antithrombotic properties. Usually, this combination is indicated for elderly patients with impaired musculoskeletal system and cardiovascular system, when the gastrointestinal toxicity of indiscriminate non-steroidal anti-inflammatory drugs increases. But the use of celecoxib with other NSAIDs is not recommended.

As for patients suffering from high blood pressure, constant monitoring of this parameter is required when taking "Celecoxib".

Particular attention should be paid to monitoring the state of the body when combined with anticoagulant (warfarin) and antiaggregant substances (acetylsalicylic acid, clopidogrel), using selective inhibitors (citalopram, sertraline) inhibiting the reuptake of serotonin, inhibitors of CYP2C9 isoenzyme, tableted forms of glucocorticosteroids.

The reception of the drug "Celecoxib" promotes the production of prostaglandin substances, which retard fluid in the body and promote the development of edema. Especially careful when treating this medication you need to be people suffering from heart muscle insufficiency and high blood pressure. If there are signs of swelling of the tissues, you should cancel the drug "Celecoxib".

In patients with impaired renal function, coxib therapy should be accompanied by constant monitoring of their basic indicators.

When dehydrating the body, taking the drug is possible only after the course of rehydration to restore the water balance.

Reception of the drug "Celecoxib" due to antipyretic effect leads to complication of the diagnosis of such an indicator as an elevated temperature in the development of infectious conditions.

The action of the drug can cause disturbances in the liver, especially in people with existing liver disorders. Severe manifestations are associated with fulminant hepatitis, necrosis of the liver. Such conditions appear not immediately, but only 30 days after the application of the drug "Celecoxib". Then it is required to monitor liver parameters when treating this drug, and in case of severe lesions, it is necessary to cancel the reception in a timely manner.

Feedback on the treatment of "Tselecoxib"

Admission of non-steroidal anti-inflammatory drugs is carried out only according to the doctor's prescription. The results of using the drug "Tselecoxib", reviews about its effects are ambiguous. One medicine helps to cope with the inflammatory processes in the joints, for others it is ineffective and causes a number of undesirable phenomena.

How else do patients evaluate the drug Celecoxib? The reviews indicate a number of problems: pain in the stomach, kidneys, menstrual irregularities. In such patients, the physician conducts the abolition of the medication and prescribes an alternative treatment.

Based on the opinions of patients on the effect of the drug on the inflamed joints, we can conclude that it is effective in fighting arthritis. To eliminate pain symptoms, swelling of tissues in the area of chronic damage, patients undergo a course of therapy with the drug "Celecoxib" in the autumn and spring periods. It is used by athletes with joint injuries.

Especially effective is a medicament in combination with warming ointments and gels for external use. However, according to the recommendations contained in the instructions for use, this non-steroidal anti-inflammatory drug is used in short courses to avoid stress on the kidneys, liver, heart and stomach. Otherwise, it is possible to avoid failures in the work of these bodies.