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Celecoxib Use, Side Effect, Mechanism of action and other Information


Uses Celecoxib

Symptomatic treatment of inflammation and pain associated with osteoarthritis and rheumatoid arthritis. Celebrex is a sulfa non-steroidal anti-inflammatory drug, also known as an NDSAI. It is a prescription medication that is used to treat a number of different ailments such as rheumatoid arthritis, acute pain, menstrual symptoms, osteoarthritis, as well as issues with the color and rectum. Celebrex is a drug that is marketed by Pfizer and is sold under numerous brand names
Celecoxib 100 mg tablets
Celecoxib 100 mg tablets

Side effects Celecoxib

Like all medications of this variety, Celebrex may cause some unwanted side effects, especially with repeated use. These common side effects may include raised liver enzymes, headaches, and dizziness. Others may experience swelling of the face and/or the body. Doctors and patients will need to work together to discuss side effects and whether or not the benefits of the medication outweigh the risk of side effects.
Most patients do not experience side effects serious or bothersome enough to discontinue therapy. Celebrex needs to be used carefully by patients who are taking any over the counter or prescription medications as it is known to interact with several medications. Doctors should be given a list of all medications currently be taken by a patient before Celebrex therapy begins.
Common side effect(> 1%)

Gastrointestinal: 
·         Abdominal pain
·         diarrhea
·         dyspepsia
·         flatulence
·         nausea
Nervous System: 

·         Headache
·         dizziness
Psychiatric: 
·         insomnia
Respiratory:
·          Pharyngitis
·         Rhinitis
·         Sinusitis
·         upper respiratory tract infection
Skin:
·          Itching
·         rash
Other: 
·         Peripheral edema

Rare side effect (1% -0.1%)

Blood: 
Anemia
Cardiovascular: 
Hypertension
 heart
Gastrointestinal: 
Constipation, burping, gastritis, stomatitis, vomiting
Liver: 
abnormal liver function, increased ACT and ALT
Metabolism:
 Abnormal renal function test results
Nervous System: 
blurred vision, hypertonia, paraesthesia
Psychiatric:
 Anxiety, depression
Respiratory:
 Cough, shortness of breath

How Celecoxib Works ?

Celebrex – a specific inhibitor of cyclooxygenase type-2 (COX-2, COX-2).
Celeccoxib is a new class of agent, mechanism of action consists in inhibiting prostaglandin synthesis, primarily through inhibition of cyclooxygenase type-2 (COX-2, COX-2). Celecoxib does not effect the COX-1. COX-2 is induced in response to inflammatory stimuli. This leads to the synthesis and accumulation of inflammatory prostanoids, particularly prostaglandin E2, which causes inflammation, swelling and pain. Celecoxib acts as an anti-inflammatory drug by blocking the production of inflammatory prostanoids by inhibition of cyclooxygenase type-2 (COX-2).
 
Celecoxib Structure
Celecoxib Structure

Studies in vivo and ex vivo show that celecoxib has a very low affinity for the expressed constitutively the enzyme cyclooxygenase type 1. Therefore, celecoxib at therapeutic doses has no effect on prostanoids synthesized by activation of COX-1 (COX-1), and thus does not prevent the normal physiological processes associated with COX-1 (COX-1) in the tissues, especially in the stomach , intestines, blood platelets.

Pharmacokinetics Celecoxib

In the fasting celecoxib is well absorbed, and after about 2-3 hours it reached a peak concentration in plasma. Bioavailability of 99%.

Plasma protein binding, which does not depend on the dose, at therapeutic concentrations of drug in plasma is about 97%.
In elderly patients with a body weight below average (50 kg) treatment should begin with a minimum recommended dose.

Celecoxib is metabolized in the liver by hydroxylation, oxidation and some glyukuronidirovaniya. Studies in vitro and in vivo studies indicate that the metabolism is mainly by cytochrome P450 CYP2C9. The main metabolites found in blood, do not have a noticeable inhibitory effect on COX-1 or COX-2.
Excretion of celecoxib is mainly the liver, less than 1% of the dose excreted in the urine in unchanged form. After receiving multiple half-life is 8-12 hours, a clearance – about 500 ml / min. Repeated reception of the equilibrium concentration of drug in plasma is achieved by the 5th day.
The drug can easily cross the blood-brain barrier.
In patients with moderate hepatic insufficiency celecoxib concentrations in plasma approximately two times higher than in the corresponding control group. For patients with mild hepatic impairment dose adjustment is required. Celebrex treatment of patients with moderate hepatic impairment should begin with a minimum recommended dose.
Pharmacokinetics of celecoxib in the elderly volunteers with age-related decrease in the rate klubochkovoi filtration rate (GFR) (mean GFR> 65 mL/min/1.73 m2) and in patients with chronic stable renal insufficiency (GFR 35-60 mL/min/1.73 m2) compared with the pharmacokinetics of drug in patients with normal renal function. Severe renal insufficiency should not affect the clearance of celecoxib.

Dosage and administration Celecoxib

Adults:
Osteoarthritis:
 Recommended dose is 200 mg taken once daily or divided into two doses. If necessary, apply a dose of 200 mg twice a day.

Rheumatoid arthritis: the recommended daily dose is 200-400 mg and is divided into two doses.
Older: choosing the dosage is usually not required. However, in elderly patients with a body weight below average (50 kg) is recommended to start treatment with the lowest recommended dose.

Abnormal liver function: For patients with mild hepatic impairment the dosage selection is not required. Celebrex therapy in patients with moderate hepatic impairment start with the lowest recommended dose. Clinical experience in treating patients with severely impaired liver function is not available.

Renal impairment: in patients with mild to moderate renal impairment the dosage selection is not required. Clinical experience in treating patients with severely impaired renal function is not available.

Children:
The use of Celebrex in patients younger than 18 years has not been studied.

Overdose Celecoxib 200 mg:

Clinical experience of overdose are not available. Healthy volunteers received a single dose of 1200 mg and repeated up to 1200 mg twice a day with no clinically significant adverse effects. In cases of suspected overdose should provide appropriate supportive care. Dialysis is probably not an effective method for removing drugs.
Incompatibility is unknown

Contraindications Celecoxib

Hypersensitivity to any ingredient of the product, known hypersensitivity to sulfonamides.
Patients who after taking aspirin or NSAIDs occurred asthma, urticaria and allergic reaction type.

Pregnancy and lactation Celecoxib

Clinical data on the use of Celebrex during pregnancy are not available. Animal studies have found toxic effects on the fetus during development. Possible risk to humans is unknown. Celebrex should not be used during pregnancy without any obvious need. Because the man has not been studies to assess the impact of the closure of Celebrex botallova duct, it is necessary to avoid its use in the third trimester of pregnancy.
Studies in rats indicate that celecoxib is released in milk in concentrations similar to those in plasma. Since human research has been conducted, Celebrex should not be used during breast-feeding.


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