Anti COX|| Drugs An enzyme called cyclooxygenase that use in synthesized of different - PowerPoint Presentation

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Anti COX|| Drugs

An enzyme called cyclooxygenase that use in synthesized of different type of

prostanoids in the body.These prostanoids including prostaglandins, prostacyclin and thromboxane , they are important biological mediators that play important role in the development of pain and inflammation in the body. So it is possible to get relief from pain and inflammation by inhibiting the COX enzyme.

What is the COX?

There are three different types of COX enzymes such

as:COX1 COX2 COX3. They are similar in different aspects and have some differences too.:Types of COX

COX2

COX1inducible enzyme constitutive enzyme Name macrophages, leukocytes and fibroblasts.kidney, stomach and platelets Location the synthesis of prostaglandins that causes pain and inflammation in the body.

as it protects gastric mucosa, regulate gastric acid and maintain normal functions of kidney by stimulating

prostaglainds

.

functiondependent on cytokinescontinuousproductionplay an important role in inflammation and pyrexia. need inhibition protective in naturno need to inhibition Usefulness

Difference between COX1 and COX2

N.B:

There

are different types of drugs that are used to inhibit COX-2 enzyme including

Celecoxib

.

Nonsteriodial

antiinflammatoru

drugs inhibit both COX-1 and COX-2 enzymes.

Side effect of non selective COX inhibitor

Acid or sour stomachanxietybelchingdizzinessdry mouthhyperventilationIrritabilityshakingstomach discomfort, upset, or pain

trouble sleeping

unusual drowsiness, dullness, tiredness, weakness, or feeling of sluggishness

irregular h

eartbeatdark urinedecreased frequency or amount of urinediarrheadifficult breathing

drowsinessfaintingfast breathingfeeling that something terrible will happenfevergeneral tiredness and weakness

headache

heartburn

increased thirst

indigestion

Incidence

of side effect:allergystudies found that 1-2 % of NSAIDs patients shows allergic reaction including rash, urticaria, angioedema.

GIT Effects

- 10–20% of NSAID patients experience dyspepsia. In the 1990s high doses of prescription NSAIDs were associated with serious upper gastrointestinal adverse events, including

bleeding.Over

the past decade, deaths associated with gastric bleeding have declined.-According to the American Gastroenterological Association (AGA), each year the side effects of NSAIDs hospitalize over 100,000 people and kill 16,500 in the U.S., mostly due to bleeding stomach ulcers. -over 50% of patients who take NSAIDs have sustained some mucosal damage to their small intestine.

bronchospasm and asthma

-The reported incidence varies widely affecting between 8% and 20% of adult asthmatics. Reye's Syndrome -About 90% of cases are associated with aspirin (salicylate) use in children.others-more than 30 million Americans use NSAIDs for pain from headaches, arthritis.-researchers estimate that NSAIDs would be responsible for up to 20 % of hospital admissions for congestive heart failure.

Discovery of selective cox 2

The COX-2 enzyme was discovered in 1988 by Daniel Simmons, a Brigham Young University researcher.The mouse COX-2 gene was cloned by UCLA scientist Dr. Harvey Herschman, a finding published in 1991]Celebrex (and other brand names for celecoxib) was introduced in 1999 and rapidly became the most frequently prescribed new drug in the United States

Celecoxib

was the first specific inhibitor of COX-2 approved to treat patients with rheumatism and osteoarthritis

celecoxib

Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID). It works by reducing hormones that cause inflammation and pain in the body.

Uses:

Celecoxib is used to treat pain or inflammation caused by many conditions such as:ankylosing spondylitis menstrual pain.Osteoarthritis

Rheumatoid arthritis

to treat juvenile rheumatoid arthritis in children who are at least 2 years old. It is also used in the treatment of hereditary polyps in the colon.

Side effect:

Celecoxib can increase your risk of fatal heart attack or stroke, especially if you use it long term or take high doses, or if you have heart disease. Do not use this medicine just before or after heart bypass surgery (coronary artery bypass graft, or CABGCelecoxib may also cause stomach or intestinal bleeding, which can be fatal. These conditions can occur without warning while you are using this medicine, especially in older adults. You should not take this medicine if you already have bleeding in your stomach or intestines.

Rofecoxib

For relief of the signs and symptoms of osteoarthritis.For relief of the signs and symptoms of rheumatoid arthritis in adults.For the management of acute pain in adults.For the treatment of primary dysmenorrhea.For the acute treatment of migraine attacks with or without aura in adults.

uses

:

Gastrointestinal

Serious gastrointestinal toxicity such as bleeding, ulceration, and perforation of the stomach, small or large intestineGeneral:fatigue, dizziness, influenza-like diseaseRenal,ocular,hepatic,cardiovascular side effects

Side effect

Meloxicam

is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and fever reducer effects

1-Rheumatoidartheritis

It is an autoimmune disease disorder that affect joints.It results in warm swollen stiff and painful joint.2-osteoartheritis It is a type of joint disease that result from breakdowen of joint cartilage and bone.3-Juvenile rheumatoid artheritisThe most common type of artheritis in children under the age of 17 years.It cause persistant joint pain and stiffess.4-Acute inflammatory pain.5-Ankylosing spondylitisIt is a type of artheritis

in which there is inflammation of the joints of the spine.

Uses

& Benefits of

Meloxicam

GIT:

Stomach upset, nausea, dizziness, or diarrhea:CVSPersons with hypertension, high cholesterol, or diabetes are at risk for cardiovascular side effectsOther:Headache,bleedingSide effects

NSAIDs vs. COX-2 inhibitors, which is better?

COX-2 inhibitors impede prostaglandin production. COX-1 is an enzyme which is normally present in a variety of tissues in the body, including sites of inflammation and the stomach. Some of the prostaglandins made by COX-1 protect the inner lining of the stomach. Common NSAIDs such as aspirin block both COX-1 and COX-2.

When the COX-1 enzyme is blocked,

inflammation is reduced, but the protection of the lining of the

stomach also is lost. This can cause stomach upset as well as

ulceration and bleeding from the stomach and even the intestines.

The other cyclooxygenase, COX-2, also produces prostaglandins, but the COX-2 enzyme is located specifically in areas of the body that commonly are involved in inflammation but not in the stomach. When the COX-2 enzyme is blocked, inflammation is reduced; however, since the COX-2 enzyme does not play a role in protecting the stomach or intestine, COX-2 specific NSAIDs do not have the same risk of injuring the stomach or intestines.

Old NSAIDs (for example, aspirin, ibuprofen, naproxen, etc.) all act by blocking the action of both the COX-1 and COX-2 enzymes. COX-2 inhibitors selectively block the COX-2 enzyme and therefore have a lower risk of causing ulcers of the stomach or intestine.

Group 6

651660

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