Celebrex Anti Inflammatory Analgesic And Antipyretic Activities Biology Essay

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It is a NSAID that exhibits anti inflammatory analgesic and antipyretic activities. Celebrex is used to treat acute pain, rheumatoid arthritis, Familial adenomatous polypsis, Primary dysmenorrhoea, osteoarthritis, painful menstruation, and ankylosing spondylitis

HISTORY:

Needleman the chief scientist at Monsanto Company was working since 1991 on cox-2 and prepared a large amount of this enzyme. This chemical backbone was refined and named as"CELECOXIB".Intially it was known as celebra and later changed to Celebrex. Celebrex was approved on December -31- 1998 by united states of food and drug administration. It was a hopeful new treatment to the millions of people suffering from rheumatoid arthritis and acute pain.

Celebrex is used to reduce the inflammation, acute pain and if possible it may even reduce the undergoing disease. The market of COX-2 inhibitor was enormous up to 5 billion dollars a year in U.S.

Celebrex was tested against other NSAID'S and it was found as effective as other NSAID'S at relieving pain and inflammation compared to placebo treated patients .Pfizer had spent more on marketing to the arthritis sufferers, including an emphasis on consumer print and advertisements.

In 1999 FDA has approved Celebrex for the treatment of familial adenomatous polyp sis. But this should not be substituted traditional treatment such as surgical reduction of tumour but frequent endoscopic surveillance. Celebrex was believed to reduce the growth of polyps and thus considered as an aid to prevent the cancer development from patients.

FDA has announced that it was a great apprehension over Celebrex and its class drugs but at that time FDA decided to keep the option open to approve the Celebrex.

In 2005 FDA has approved Celebrex for treating Ankylosing Spondylitis.Ankylosing Spondylitis is the chronic inflammatory disease which causes loss of movement of neck and spinal cord. After several clinical trials FDA has given approval for treating Ankylosing Spondylitis

Later on in the year 2006 juvenile rheumatoid arthritis was added in the list of approved uses of Celebrex. After a six months of clinical study showing only few mild side effects, gave a way to approval.

Clinical trials on more than 13,000 patients from different countries were done.

Pharmacology:

Celebrex inhibits the prostaglandin synthesis, primarily via inhibition of cyclo oxygenase -2 (cox-2).There are two types of cyclo oxygenase ,COX-1 and COX-2.COX-2 produces prostaglandins which causes pain and inflammation during injury.Whereas,COX-1 produces others which as useful effects. When NSAID such as Celebrex is administered, it blocks the prostaglandin production and gives relief from pain and inflammation. But when NSAID'S such as diclofenac is used it blocks the action of both COX-1 and COX-2 but effects the intestinal lining.

Pharmcodynamics:

Platelets: Several Clinical studies have been done by administrating Celebrex of single dose 800mg and multiple doses of 600mg twice a day up to a week. This did not show any effect on reduction of platelets aggregation or increasing of bleeding time. As it shows lack of platelets effect, Celebrex cannot be used as a substitution of Aspirin for cardiovascular prophylaxis.

Fluid Retention:

Celebrex inhibits the prostaglandin which leads to sodium and water retention through increased absorption in renal thick medullary ascending loop of henle and in distal nephron.In collecting duct, prostaglandins inhibits the water reabsorption by counteracting the action of anti diuretic hormone.

Pharmacokinetics:

Absorption:

Celebrex gets absorbed and the peak plasma concentration is achieved at 3 hours after the oral dose. When administered empty stomach, it causes peak plasma level and area under curve up to 200mg BID. Higher doses lead to proportional increase in Cmax and AUC.

Excretion:

Drug is eliminated by hepatic metabolism. Less than 3%of the drug is eliminated through urine and feces.Radiolabelled single dose drug when administered, 57% of the drug is eliminated through faeces and the rest through urine. Carboxylic acid metabolite is eliminated through both urine and faeces whereas small amount of glucuronide is found only in urine. As the drug is insoluble, absorption gets delayed making the half life determinations variable.

Renal Insuffiecncy:

Adverse effects:

Cardiovascular-Aggravated hypertension, angina pectoris, myocardial infarction, coronary artery disorder.

Gastrointestinal-constipation, vomiting, dry mouth, diverticulitis, dysphasia.

Hearing and vestibular: deafness, tinnitus.

Heart rate and rhythm: palpitation and tachycardia.

General: Allergy aggravated allergy reaction, chest pain, face oedema, fatigue fever.

Skin and appendages: Alopecia, dermitis, skin dry, skin disorders, utricaria.

DRUG INTERACTION:

Metabolism of Celebrex is via cytochrome P450 2C9 in the liver. Co administration of celecoxib with drugs that are known to inhibit CYP2C9 should be done with caution. Interaction occurs when Celecoxib is administered along with other drugs that inhibit CYP2C9.

Warfarin:

Serious bleeding may occurs which even may be fatal in association increase in prothrombin time in patients receiving Celebrex concurrently with warfarin.

Aspirin:

Concomitant administration of aspirin with Celebrex increases GI ulceration.

Concomitant use of NSAID:

Concomitant use of Celebrex with any non-aspirin NSAID should be avoided due to increased adverse reactions.

Mechanism of Action:

Celebrex is a NSAID that exhibits anti inflammatory analgesic and antipyretic activities. Celebrex inhibits the prostaglandin synthesis primarily via inhibition of cyclooxygenase-2(COX-2). Celebrex doesn't inhibit cyclooxygenase-1(COX-1) isoenzyme.COX-2 is present in endothelial cells, blood vessels, synovial fibroblast and immune cells. Both the COX-1 and COX-2 are involved in the production of prostaglandins from arachidonic acid.COX-2 gets converted into active metabolites such as prostaglandins D2.prostagladins E2, thromboxane, prostacyclin.These causes the physiological responses such as inflammation, fever. When the drug is administered the polar sulphonamide side chain binds to the hydrophilic region which is in close proximity to active binding site of COX-2. Celebrex gets absorbed and the peak plasma concentration is achieved at 3 hours after the oral dose. Later on the drug proceeds to the liver where the cytochrome enzyme CYP2C9 breaks down the drug into carboxylic acid and glucuronide.

Medication:

It was available in capsules including 50mg.100mg, 200mg, and 400mg.

Uses:

Celebrex gives relief from pain and swelling.

It is used to treat arthritis, painful menstruation, acute pain and other discomfort.

Celebrex is used to decrease growth in the intestine of patient with family history condition. Celebrex blocks the enzyme in the body that makes prostaglandins. Decrease in prostaglandins helps to reduce pain and swelling.

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