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Michelle A.

Borres BSMT 1-C


ELECOXIB
BRAND NAME: Celebrex

IDENTIFICATION OF SUBSTANCE:

Trade name: Celecoxib
Product Number: C-1502
Manufacturer/Supplier:
LC Laboratories
165 New Boston Street
Woburn, MA 01801 USA
COMPOSITION/DATA ON COMPONENTS:

Chemical Name: 4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl] benzenesulfonamide
Synonyms: Celebrex, Celebra, Celecox, Onsenal, Solexa, SC-58635, YM-177
CAS Registry Number: 169590-42-5
Molecular Weight: 381.37
Molecular Formula: C
17
H
14
F
3
N
3
O
2
S

STRUCTURAL FORMULA:





PHYSICAL AND CHEMICAL PROPERTIES:
Form: solid powder
Color: white
Odor: none



Melting point/Melting range: 160-162 C
Danger of explosion: none

Solubility in / Miscibility with water: very poorly soluble in water; maximum solubility in plain
water is estimated to be about 10-50 M; buffers, serum, or other additives may increase or
decrease the aqueous solubility
Solvent content: none
Organic solvents: Soluble in ethanol at 100 mg/Ml
CELECOXIB is approved by the FDA in the following formulation(s):
Manufacturer: GD SEARLE
Approval date: December 31, 1998
Strength(s): 100MG, 200MG

Manufacturer: GD SEARLE
Approval date: August 29, 2002
Strength(s): 400MG

Manufacturer: GD SEARLE
Approval date: December 15, 2006
Strength(s): 50MG
USES
ADVANTAGES
Relieves pain and swelling (inflammation)
Used to treat or reduces the symptoms and signs of Osteoarthritis, Rheumatic
arthritis, Menstrual Cramps, and Colonic Polyps.
Blocks the enzyme that makes prostaglandins (cyclooxygenase 2), resulting in
lower concentrations of Prostaglandins.
* PROSTAGLANDINS are chemicals that are important contributors to the
inflammation of arthritis that causes pain, fever, swelling and tenderness.
Differs from other NSAIDs in that it causes less inflammation and ulceration of
the stomach and intestine (at least with short-term use) and does not interfere
with the clotting of blood.
Celecoxib is approved as an adjunctive (secondary) treatment among patients
with FAP.
* In FAP (Familial Adenomatous Polyposis), patients develop large numbers
of polyps in their colons, and the polyps invariably become malignant. The
only cure of FAP is removal of the entire colon.


DISADVANTAGES
If too much, can cause common adverse effects like, headache, abdominal
pain, dyspepsia, diarrhea, nausea, flatulence, and insomnia.

Other side effects include fainting, kidney failure, heart failure, aggravation of
hypertension, chest pain, ringing in the ears, deafness, stomach and intestinal
ulcers, bleeding, blurred vision, anxiety, photosensitivity, weight gain, water
retention, flu-like symptoms, drowsiness and weakness.

Should not be used if youre pregnant or having breastfeeding.
HOW CELEBREX WORKS
The human body contains many enzymes that facilitate chemical reactions in the body.
One of these enzymes is Cyclooxygenase-2 (COX-2), which is involved in causing
inflammation and pain in parts of the body where there is arthritis or injury.

CELEBREX at recommended doses selectively inhibits COX-2, which helps relieve
arthritis pain and inflammation as well as acute pain in adults.





HISTORY
Honorees Peter Isakson, Ph.D., Jamie Masferrer, Ph.D., Karen Seibert, Ph.D., and John Talley,
Ph.D. of Pharmacia created the molecule Celecoxib, the basis for the medicine Celebrex,
which blocks the inflammation-triggering action of the COX-2 enzyme, bringing relief to millions
of people around the world who suffer from osteoarthritis, rheumatoid arthritis, and pain.
Dr. John Talley and his team of medicinal chemists manipulated molecules and made thousands
of different analogs. They finally found a compound that was a strong selective inhibitor of
COX-2, but it had a long half-life - it lingered in the body too long. The molecule was sent back
to the laboratory and modified, and the scientists synthesized the compound that eventually
became Celebrex.
Clinical trials of Celebrex began in 1995. In all, some 13,000 volunteers in countries all over the world
took part in the trials. In June 1998, the company submitted an application to the Food and Drug
Administration (FDA) to market the drug. The FDA gave the application an accelerated review, and on
December 30, 1998, Celebrex (100mg and 200mg) was approved for the treatment of osteoarthritis and
rheumatoid arthritis. August 29, 2002 for 400mg Celebrex and December 15, 2006 for 50mg. It has also
been approved for familial adenomatous polyposis, a rare and devastating disease that often leads to
colon cancer.








INDICATIONS AND USAGE

CELEBREX is indicated:

1) For relief of the signs and symptoms of osteoarthritis.
2) For relief of the signs and symptoms of rheumatoid arthritis in adults.
3) For the management of acute pain in adults .
4) For the treatment of primary dysmenorrhea.
5) To reduce the number of adenomatous colorectal polyps in familial adenomatous polyposis
(FAP), as an adjunct to usual care (e.g., endoscopic surveillance, surgery). The efficacy and safety
of CELEBREX treatment in patients with FAP beyond six months have not been studied.

CONTRAINDICATIONS

1) CELEBREX is contraindicated in patients with known hypersensitivity to celecoxib.
2) CELEBREX should not be given to patients who have demonstrated allergic-type reactions to
sulfonamides.
3) CELEBREX should not be given to patients who have experienced asthma, urticaria, or allergic-
type reactions after taking aspirin or other NSAIDs.

SOURCES:
http://www.medicinenet.com/celecoxib/article.htm
http://www.drugs.com/celebrex.html
http://www.celebrex.com/about-celebrex.aspx

MY VIDEO: http://www.youtube.com/watch?v=53FKGMPEAdU




Cebu Doctors University
North Reclamation Area, Mandaue City








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