Aspirin (ASA) is a potent inhibitor of prostaglandin and produces adverse effects like gastric intolerance and bleeding.
Aspirin is also a good anti platelet aggregation making it useful in preventing heart attacks.
What are the 1st generation NSAIDS?
Salicylates
Para-chlorobenzoic acid derivatives, or indoles
Phenylacetic acids
Propionic acid derivatives
Fenamates
Oxicams
What is the 2nd generation NSAIDS?
Selective COX-2 inhibitors
What are the 5 Cardinal Signs of Inflammation?
Calor (Heat)
Dolor (Pain)
Rubor (Redness)
Tumor (Swellling)
Functio Laesa (Loss of Function)
INFLAMMATION
A reaction to tissue injury caused by the release of chemical mediators that trigger both a vascular response and the migration of fluid and cells (leukocytes, or white blood cells) to the injured site.
What are the chemical mediators under the inflammation?
The chemical mediators are (1) histamines, (2) kinins, and (3) prostaglandins.
Infection is caused by microorganisms and results in inflammation, but not all inflammations are caused by infections.
Prostaglandins - cause pain, fever, and swelling.
Kinins - cause pain and increase blood flow to the area.
Acetaminophen does not affect platelets so it doesn't cause bleeding problems like aspirin can do.
Used to decrease inflammation and pain for patients who have some type of musculoskeletal condition
NSAIDS- Mimic the effects of corticosteroids (cortisone), but they are not chemically related to corticosteroids
Maybe classified as Salicylates and Nonsalicylates.
ASPIRIN- Most frequently used anti-inflammatory agent before the introduction of ibuprofen
Aspirin decreases platelet aggregation, and thus blood clotting is decreased.
Hypersensitivity: tinnitus, vertigo, bronchospasm
Salicylates are present in numerous foods such as prunes, raisins, and licorice and in spices such as curry and paprika.
ASPIRIN: It can cause GI distress, which includes anorexia, nausea, vomiting, diarrhea, and abdominal pain, so it should be taken with water, milk, or food.
It should not be taken during the last trimester of pregnancy because it could cause premature closure of the ductus arteriosus in the fetus.
Aspirin should not be taken by children with flu symptoms because it may cause the potentially fatal Reye syndrome.
ASPIRIN: The onset of action for aspirin is within 30 minutes. It peaks in 1 to 2 hours, and the duration of action is an average of 4 to 6 hours.
PARA-CHLOROBENZOIC ACID: INDOMETHIACIN
INDOMETHACIN
Used for rheumatoid arthritis (RA), gouty arthritis, and osteoarthritis and is a potent prostaglandin inhibitor.
INDOMETHIACIN is Very irritating to the stomach and should be taken with food
PARA-CHLOROBENZOIC ACID DERIVATIVE
Sulindac & Tolmetin
PARA-CHLOROBENZOIC ACID DERIVATIVE
Produce less severe adverse reactions than indomethacin.
May cause sodium and water retention, and increased blood pressure.
PHENYLACETIC ACID DERIVATIVES
Diclofenac sodium and Ketorolac
DICLOFENAC SODIUM
Antiinflammatory effects are similar to those of aspirin, but it has minimal to no antipyretic effects.
It is indicated for RA, osteoarthritis, and ankylosing spondylitis.
KETOROLAC
First injectable NSAID
Has greater analgesic properties.
Recommended for short-term management of pain.
For postsurgical pain, it has shown analgesic efficacy equal or superior to that of opioid analgesics.
PROPIONIC ACID DERIVATIVES
These drugs are aspirin-like but have stronger effects and create less GI irritation
Gastric upset occurs, but it is not as severe as with aspirin and indomethacin. Ibuprofen is the most widely used propionic acid
Five other propionic acid agents are:
Fenoprofen calcium
Naproxen
Ketoprofen
Flurbiprofen
Oxaprozin
IBUFROPEN
Because ibuprofen can increase the effects of warfarin, sulfonamides, many of the cephalosporins, and phenytoin, it should be avoided with these drugs.
Hypoglycemia may result when ibuprofen is taken with insulin or an oral hypoglycemic drug.
Risk of toxicity is high when ibuprofen is taken concurrently with calcium channel blockers.
FENAMATES
Includes potent NSAIDs used for acute and chronic arthritic conditions.
Gastric irritation is a common side effect; patients with a history of peptic ulcer should avoid taking fenamates.
Side effects include edema, dizziness, tinnitus, and pruritus.
Two fenamates: (1) meclofenamate sodium monohydrate and (2) mefenamic acid.
OXICAMS
Piroxicam, Meloxicam, Oxicams, are indicated for long-term arthritic conditions such as RA and osteoarthritis.
OXICAMS: They too can cause gastric problems such as ulceration and epigastric distress, but the incidence is lower than for some other NSAIDs.