NSAIDS Flashcards
what are the large and chemically diverse group of drugs with the following properties?
analgesic
anti-inflammatory
anti-pyretic
what does the activation of the arachidonic acid (AA) pathway cause?
pain
headache
fever
inflammation
why is analgesia used as a treatment of headache and pain?
because it blocks the undesirable effects of prostaglandins which cause headaches
what do we use Antipyretics for?
to reduce fever
how do anti-pyretics reduce fever?
they Inhibit prostaglandin E2 within the area of the brain that controls temperature
how do NSAIDS relief inflammation ?
- they inhibit leukotriene pathway
- they inhibit prostaglandin pathway
- they inhibit both
what is the function of the AA pathway ?
to extract small parts of the cell membrane and produce products like leukotrienes, prostaglandins, prostacyclin, and thromboxane
give examples of the products of the AA pathway
leukotrienes, prostaglandins, and thromboxane
what THE STEROIDS inhibit
arachidonic acid -AA-
the asprin and NSAIDS inhibit :
cyclooxygenase (prostaglandins , thromboxane)
cox1,cox2
what is the enzyme that product AA
PHOSPHOLIPASE
THE AA mechanism work in two way:
lipoxygenase that return aa to leukotrenes
-cyclooxygenase that return AA to prostaglandins and thromboxane
-
what does thromboxane do in the body?
- vasoconstriction
- platelet aggregation
what does the prostaglandins do in the body ??
vasodilation, fever and pain
what do leukotrienes do in the body ?
vascular permeability
Cox1 inhibitor action :
Supports renal and platelet function
Protect gastroduodenal mucus
What is Cox 1 used for ?
Gastrointestinal toxicity,
renal toxicity,
Platelet impairment
Cox 2 inhibitor action:
Immediate inflammation, pain and fever
What is Cox 2 used as?
Anti-inflammatory
Anti-pyretic
Analgesic
What do we use NSAID’s for ?
Arthritis Muscular pain Headache Toothache Use with obioids to decrease the pain after giving dosage Pain Edema Vasoconstriction
What are the adverse effects of NSAID’s
Diarrhea Nausea Vomiting Gastric damage Skin reactions (rash) Rental reaction Chronic nephritis Renal papillary necrosis (renal hypertension)
What are the 6 structurally related groups ? (Cox 1)
Acetic acids Carboxylic acids Propionic acids Enolic acids Fenamic acids Nonacidic compounds
what are examples of acetic acid?
diclofenac potassium (Cataflam) indomethacin (Indocin) diclofenac sodium (Voltaren)
examples of carboxylic acid:
Acetylated
- Aspirin (ASA) acetyl salicylic acid
- diflunisal (Dolobid)
Non-acetylated
-salicylamide (similar to aspirin but less harsh on the stomach)
examples of propanoic acid:
Ibuprofen (Motrin, others)
ketorolac (Toradol)
naproxen (Naprosyn)
examples of enolic acid
phenylbutazone (Butazolidin)
for treating arthritis
examples of fanatic acid:
rarely used because it causes heart disease
examples of cox 2 inhibitors
celecoxib (Celebrex)
Etorocoxib (Arcoxia).
examples of non acidic compounds:
nabumetone (Relafen)
can aspirin be given to children ?
No
what is Non-aspirin salicylates?
ASA with magnesium or sodium
what are the characteristics of Non-aspirin salicylates?
Cause less bleeding.
May not be as effective as aspirin.
Dimer of salicylic acid.
Absorbed primarily from lower intestine - less G.I. Irritation.
how do salicylates work ?
block cyclooxygenase
what are the Therapeutic effects of salicylates?
Analgesia.
Good for low intensity, somatic pain.
PGE1 sensitises pain receptors, salicylates decrease PG synthesis.
