The treatment of diseases associated with damage to the musculoskeletal system 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 are less toxic and easier to tolerate.
Description of the drug “Celecoxib”
The celecoxib substance has a pale yellow color and belongs to the group of coxibs that exhibit selective inhibition of the second type cyclooxygenase. Medicines based on this compound have pronounced anti-inflammatory and analgesic properties. The original drug based on celecoxib is considered to be the drug Celebrex developed by the American company Fayser. Its pharmacodynamic characteristics were studied and toxicity to the human body was investigated.
The rest of the medicines 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 the 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 an ointment, gel, injection solutions or suspensions. When used by some patients, the form of release of the drug “Celecoxib” is mistakenly called tablets, although this is precisely about capsules.
Structure
The active substance is celecoxib in the amount of 100 mg and 200 mg. The composition of the contents of the capsules includes auxiliary components that ensure the filling of the space, flowability and stability of the granular mixture. These include milk sugar, sodium lauryl sulfate, polyvinylpyrrolidone (K30), croscarmellose sodium, magnesium stearate.
The instructions for use attached to the preparation “Celecoxib” contain a characteristic of the composition and appearance of the gelatin shell of the capsules. According to the description, they are externally matte, have almost white color and are marked with the signs “100” or “200”, located on a blue or yellow strip, respectively. This allows you to recognize capsules with different dosages. The composition of yellow and blue ink is also painted in detail, indicating dyes that are harmless to the body.
Similar drugs
The drug "Celecoxib", analogues of which also contain the active substance celecoxib, are able to exhibit the same therapeutic effect on osteoarthritis of the human skeleton.
The original drug Celebrex and its generics Celecoxib, Artoxib, Zitsel, Revmoxib, Rancelex are considered interchangeable medicines. However, in 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 medicine “Celecoxib”. Auxiliary components of the contents of the capsules and its shell can vary both in qualitative and in quantitative composition, which does not affect their properties. As for the release form of the generic 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 cyclooxygenase, but having 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 osteoarthrosis and rheumatoid arthritis. Preparations based on it have an anti-inflammatory and analgesic effect due to the inhibition of cyclooxygenase of the second and, to a lesser extent, of the first type, affect a variety of mediators of pain and inflammation.
Like nimesulide, celecoxib is a representative of the sulfonamide class of substances and also in a daily dosage of 200 mg eliminates the manifestations of osteoarthrosis. It does not inhibit cyclooxygenase of the first type and acts on a small number of mediators of pain and inflammation.
An alternative to coxib treatment for oral use are injectable NSAIDs. One of the main advantages of 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 from 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 the activity of COX 2.
Inflammatory reactions trigger the induction of cyclooxygenase of the second type, in turn, accelerates the synthesis and accumulation of prostaglandin substances, which increase inflammation. A state of edema and pain develops.
The cyclooxygenase of the first type is not affected by the therapeutic dose of Celecoxib. Instructions for use describe the inertness of the drug in relation to this enzyme and the physiological processes associated with its activity that occur in the cells of the gastrointestinal tract and platelet structures.
The instructions also provide information regarding the effect of the drug on kidney function. Under the influence of celecoxib, prostaglandin and F1 6-keto-prostaglandin are less excreted in the urine E2, but the release of B2 11-dehydro-thromboxane is not changed, which indicates the selective action of the drug.
The use of the drug “Celecoxib” does not lead to a decrease in the filtration rate in the renal glomeruli of the elderly and in patients with renal failure.
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, osteoarthritis.
Due to its analgesic properties, it is used to eliminate the pain state in musculoskeletal pain, after surgical interventions, with dysmenorrhea, which is accompanied by painful menstruation. The anti-inflammatory effect of the drug is aimed at reducing outgrowths and polyps in the colon and rectum with a diagnosis of adenomatous polyposis.
How to use
To take the medicine "Celecoxib", the instructions for use recommends by mouth, without binding to eating. Capsules do not open and do not chew, but swallow whole, drinking plenty of water.
The maximum amount of celecoxib that can be taken per day is 0.4 g. This drug is used in excess only in rare cases.
High doses and prolonged therapy with Celecoxib can lead to cardiovascular complications. The instructions contain information on small dosages for the symptomatic treatment of each indication. Recommendations regarding short-term use are provided.
To eliminate the symptoms that accompany osteoarthritis and ankylosing spondylitis, 200 mg of the drug is taken once or twice per day.
To eliminate the symptoms of rheumatoid arthritis, a daily dose of 200 or 400 mg is used, which is taken twice.
Pain and primary dysmenorrhea on the first day are treated with a high dose of 400 mg, with a possible intake of another 200 mg, the next day they use 200 mg 2 times a day.
Elderly people, as well as patients with a mild degree of insufficient liver function or a mild to moderate degree of insufficient renal function, do not recalculate the dose.
Low weight (less than 50 kg), moderate severity of liver failure - patients of these categories are prescribed treatment with low doses of the drug.
Usually, complex treatment is used to treat inflammatory processes in the joints, based on the use of several drugs in different dosage forms. Combine capsules "Celecoxib", ointment or gel warming type "Apisatron" or "Finalgon. Preparations for local use cause a temporary effect, so they are used together with medications for internal use.
Who is forbidden to use
Not all patients with joint diseases may take Celecoxib. Instructions for use contain a list of diseases and conditions in which this tool will do more harm than good. This includes:
- urticaria, bronchial asthma, allergic condition from the action of aspirin and other non-steroidal anti-inflammatory drugs;
- recovery after surgery associated with coronary artery bypass grafting ;
- exacerbation of peptic ulcer;
- gastric and intestinal bleeding;
- inflammation of the mucous membrane in the intestine;
- heart failure;
- coronary heart disease;
- damage to arteries along the periphery and cerebral vessels with impaired cerebral blood flow;
- severe liver failure;
- severe renal failure;
- bearing a child;
- breastfeeding;
- age up to eighteen years;
- hypersensitivity to excipients;
- hypersensitivity to sulfonamide components.
Caution is required to use the drug “Celecoxib” for people with diseases of the gastrointestinal tract associated with peptic ulcer, bleeding in the past, infection of the mucosa with bacteria of the Helicobacter pylori genus.
Water retention in the body and soft tissue edema, malfunction of the liver of the middle stage, heart and vascular disease, lipid metabolism in the body, in which there is an increase in plasma cholesterol, diabetes mellitus, severe somatic diseases are also the reason for extremely careful use of the drug "Celecoxib" under the supervision of a doctor.
Side effects
Despite innovative achievements in creating a new generation of coxibs, these substances and medicines based on them are not without side effects.
The accompanying preparation "Celecoxib" instructions for use, reviews of patients and specialists - these sources contain information about possible undesirable consequences that may occur in the work of vital organs.
A possible negative effect on the digestive system is characterized by NSAID gastropathy, pain in the abdomen, nausea, vomiting, heartburn, decreased need for food, and diarrhea. Long-term use 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 excitement, headache, dizziness, drowsiness, insomnia, and depressive states.
The effect 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, shortness of breath, bronchospasm.
The effect of the drug on the senses causes a decrease in auditory perception and the appearance of tinnitus.
The drug “Celecoxib” affects the urinary system in such a way that renal failure may occur with the development of edematous syndrome.
As for the blood-forming organs, the medicine can cause the manifestation of agranulocytosis, anemia, leukopenia, thrombocytopenia.
Skin rashes of an allergic nature may occur with the appearance of itching, urticaria, photosensitivity, angioedema in the facial region, extremities, genitals.
Features of the reception
“Celecoxib” has a disadvantage associated with an increased risk of negative effects on the cardiovascular system, leading to thrombosis, myocardial infarction, and stroke. Especially the risk increases with prolonged use of the drug by patients who have heart and vascular diseases.
To reduce the risk of developing such complications, patients taking Celecoxib are prescribed the minimum dose for the shortest treatment period. The patient should discuss with the attending physician the possible signs of the disease and receive recommendations on how to respond when they occur.
To reduce cardiovascular symptoms, a combination of acetylsalicylic acid in minimum doses with the drug “Celecoxib” is used. Reviews of doctors indicate the antiplatelet effect of aspirin to thin the blood when taking coxib, which do not have such antithrombotic properties. Typically, this combination is indicated for elderly patients with disorders of the musculoskeletal system and cardiovascular system, when 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 indicator is required when taking Celecoxib.
Particular attention should be paid to monitoring the state of the body when combined with anticoagulant (warfarin) and antiplatelet agents (acetylsalicylic acid, clopidogrel), using selective inhibitors (citalopram, sertraline) that inhibit the reuptake of serotonin, inhibitors of the CYP2C9 isoenzyme and glucose isoenzyme tablets.
Taking Celecoxib promotes the production of prostaglandin substances that trap fluid in the body and contribute to the development of edema. Especially careful when treating with this medication you need to be people suffering from heart failure and high blood pressure. If signs of tissue swelling occur, celecoxib should be discontinued.
In patients with impaired renal function, coxib treatment should be accompanied by constant monitoring of their key indicators.
With dehydration, taking the drug is possible only after a rehydration course to restore water balance.
Taking Celecoxib due to the antipyretic effect complicates the diagnosis of such an indicator as fever with the development of infectious conditions.
The action of the drug can cause disturbances in the liver, especially in people with pre-existing liver disorders. Severe manifestations are associated with fulminant hepatitis, necrosis of the liver. Such conditions do not occur immediately, but only 30 days after the use of Celecoxib. Then monitoring of liver parameters during treatment with this agent is required, and in case of detection of severe lesions, it is necessary to cancel the reception in a timely manner.
Reviews on the treatment of "Celecoxib"
Non-steroidal anti-inflammatory drugs are only prescribed by a doctor. The results of the use of the drug “Celecoxib”, reviews about its action are mixed. One medicine helps to cope with inflammatory processes in the joints, for others it is ineffective and causes a number of undesirable effects.
How else do patients evaluate Celecoxib? Reviews indicate a number of problems: pain in the stomach, kidneys, menstrual irregularities. For such patients, the doctor will cancel the medication and prescribe an alternative treatment.
Based on the opinions of patients about the effect of the drug on inflamed joints, it can be concluded that it is effective in combating arthritis. To eliminate pain symptoms, swelling of tissues in the area of ​​chronic lesions, patients undergo a course of therapy with Celecoxib in the autumn and spring. It is used by athletes with joint injuries.
The medication is especially effective 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, failures in the work of these bodies cannot be avoided.