3 - NSAIDs

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What are NSAIDs and how do they work?

What NSAIDs are approved in the United States?


What are the side effects of NSAIDs?
For what conditions are NSAIDs used?
Are there any differences between NSAIDs?
With which drugs do NSAIDs interact?
What are
NSAIDs and
how do they
work?
PROSTAGLANDINS
are a group of chemicals made by the body's cells that
serve a variety of purposes. They promote
inflammation, which is important for healing but also
causes pain and fever; they help platelet function in
blood clotting; and they protect the stomach lining
from acid damage.
The enzyme cyclooxygenase produces prostaglandins inside the
body's cells (COX). COX-1 and COX-2 are two COX enzymes. Both
enzymes produce prostaglandins, which are inflammatory
mediators that cause pain and fever. Only COX-1, on the other
hand, produces prostaglandins, which help platelets and protect
the stomach. NSAIDs (nonsteroidal anti-inflammatory drugs) block
COX enzymes, lowering prostaglandin levels throughout the body.
As a result, the severity of ongoing inflammation, discomfort, and
fever is decreased. NSAIDs can cause stomach ulcers and
promote bleeding because the prostaglandins that protect the
stomach and help platelets and blood clotting are decreased.
What NSAIDs
are approved
in the United
States?
The following list is an example of NSAIDs available:
What are the side effects
of NSAIDs?
NSAIDs are associated with
several side effects.
The frequency of side effects
varies among NSAIDs.
Common side effects are:
Other important side effects are:
kidney failure (primarily with chronic use)
liver failure
Ulcers
prolonged bleeding after injury or surgery.

NSAIDs can cause fluid retention which can lead to


edema, which is most commonly manifested by
swelling of the ankles.
WARNING!!
Some people are allergic to NSAIDs, and when they
take one, they may experience shortness of breath.
People with asthma are more likely to have a severe
allergic reaction to NSAIDs. Individuals who have a
severe NSAID allergy are likely to have a similar
reaction to another NSAID.
The use of non-steroidal anti-inflammatory
drugs (NSAIDs) raises the risk of potentially
lethal stomach and intestinal side effects (for
example, bleeding, ulcers, and perforation of the
stomach or intestines). These incidents can
happen at any time during treatment with no
warning signs or symptoms.
For what conditions are
NSAIDs used?
Specific uses include the treatment of:
headaches,
arthritis,
ankylosing spondylitis,
sports injuries, and
menstrual cramps.
Ketorolac (Toradol) is only used to relieve
moderately serious acute pain that would normally
be treated with opioids for a brief period of time.
In people who are at high risk for strokes and
heart attacks, aspirin (also known as an NSAID) is
used to reduce blood clotting and prevent
strokes and heart attacks. NSAIDs are also used
in many cold and allergy remedies.
Are there any differences
between NSAIDs?
NSAIDs differ in potency, length of action, elimination
from the body, the intensity with which they inhibit
COX-1 versus COX-2, and their proclivity for ulcers and
bleeding. The greater an NSAID's ability to block COX-
1, the more likely it is to cause ulcers and facilitate
bleeding. Celecoxib (Celebrex), an NSAID that blocks
COX-2 but has no effect on COX-1, is known as a
selective COX-2 inhibitor. Other NSAIDs cause less
bleeding and ulcers than selective COX-2 inhibitors.
Most NSAIDs only prevent blood from clotting for a
few hours. Ketorolac (Toradol) is a very powerful
nonsteroidal anti-inflammatory drug (NSAID) that is
used to treat moderately intense acute pain that
typically involves opioids. Ketorolac is more likely
than other NSAIDs to cause ulcers. As a result, it is
only used for a maximum of five days. Individuals who
do not respond to one NSAID can respond to another,
despite the fact that they have a similar mechanism
of action.
With which drugs do
NSAIDs interact?
NSAIDs also make it harder for blood to clot, which
leads to further bleeding. When combined with other
medications that increase bleeding (for example,
warfarin [Coumadin]), the risk of severe bleeding or
bleeding complications increases. As a result, people
who are taking blood thinners should stop taking
NSAIDs for an extended period of time.
NSAIDs can also raise blood pressure in patients with
hypertension (high blood pressure) and thus
counteract the effects of antihypertensive drugs.
The harmful effects of cyclosporine on kidney function
are exacerbated by NSAIDs.
When taking NSAIDs, people who consume more than
three alcoholic drinks a day may be at an elevated risk
of developing stomach ulcers.
SUMMARY
Nonsteroidal anti-inflammatory drugs (NSAIDs) are a class of
drugs are used to treat inflammation, mild to moderate pain, and
fever. Examples of the most common NSAIDs include: aspirin
salsalate (Amigesic), diflunisal (Dolobid), ibuprofen (Motrin),
ketoprofen (Orudis), nabumetone (Relafen), piroxicam (Feldene),
naproxen (Aleve, Naprosyn,) diclofenac (Voltaren), indomethacin
(Indocin), sulindac (Clinoril), tolmetin (Tolectin), etodolac
(Lodine), ketorolac (Toradol), oxaprozin (Daypro), celecoxib
(Celebrex).
ANTINFLAMATORY
MNEMONICS
Antirheumatic agents (disease modifying): members
CHAMP
C Cyclophosphamide

H Hydroxycloroquine and choloroquinine

A Auranofin and other gold compounds

M Methotrexate

P Penicillamine
ASPIRIN: side effects
A Aplastic anemia

S Salt and water retention


P Peptic ulcer
I
Rash (skin rash)
R
I Induce bronchial asthma

N Nephrotoxicity
ASPIRIN: side effects
ABCD Luv TV
• Allergy
• Bleeding (Intracranial/Gastrointestinal)
• Children under 12yrs (risk of Reye’s Syndrome)
• Disorder of Bleeding (Including Hemophilia)
• Liver Disease
• Ulcerations e.g Peptic Ulcer
• Thrombocytopenia
• Von willebrand Disease
NSAIDS: Classification
SOFIA PPP

• SALICYLATES
• OXICAME DERIVATIVES
• FENAMIC ACID DERIVATIVES
• INDOLE DERIVATIVES
• ARYL ACETIC ACID DERIVATIVES
• PROPIONIC ACID DERIVATIVES
• PYRROLO DERIVATIVES
• PYRAZOLON DERIVATIVES
NSAIDS: Contraindication
BARS

• Bleeding (Coagulopathy)
• Asthma (10% of asthmatic patients are
NSAID Sensitive)
• Renal Disease (Hypovolemia)
• Stomach (Peptic Ulcer or Gastritis)
Steroids: side effects
BECLOMETHASONE

• Buffalo hump • Thin arms and legs


• Easy bruising • Hypertension/ Hyperglycaemia
• Cataracts • Avascular necrosis of femoral head
• Larger appetite • Skin thinning
• Obesity • Osteoporosis
• Moonface • Negative nitrogen balance
• Euphoria • Emotional liability

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