NSAIDs Flashcards
Signs of inflammation
SLHRP
Swelling, Loss of function, heat, redness and pain
Fill in the Eicosanoids Effects
When Eicosanoids bind to GPCRs in the target cells, the generation of what causes dilation? Constriction?
Generation of cAMP (Gs) = dilation
Release of calcium (Gq) = constriction
20-carbon polyunsaturated fatty acid that is the most abundant and important precursor of eicosanoids
Arachidonic acid
On Arachidonic acid, which carbon has an inflammatory effect?
6 carbon
PGH synthase has both ____ & _____ activities
COX and hydroperoxidase
“Housekeeping” function; COX 1
Constitutively expressed in various tissues
PGH synthase-I
Expressed upon stimulus in inflammatory and immune cells
COX 2
Stimulated by growth factors, tumor promoters, and cytokines
PGH synthase-2
What are PGH synthase 1 and 2 inhibited by?
NSAIDS
Synthesis of prostaglandins
What classification of drug is this?
PGE1
Relaxes smooth muscles and expand blood vessels
Used for erectile dysfunction by injection or as a suppository
Alprostadil
Eicosanoid drugs
What classification of drug is this?
PGE1 derivative; Cytoprotective
Prevents peptic ulcer
Terminates early pregnancy in combo with mifepristone
Misoprostol
Eicosanoid drugs
What classification of drug is this?
Topically active PGF2a derivative (prodrug)
Constrict blood vessels
Used in ophthalmology to treat high pressure inside the eye
Latanoprost
Eicosanoid drugs
What classification of drug is this?
PGI2; powerful vasodilator
Inhibitor of platelet aggregation
Used to treat pulmonary arterial hypertension by IV injection or inhalation
Should not be used with anticoagulants
Prostacyclin (epoprostenol)
Eicosanoid drugs
NSAIDs mechanism of action: inhibition of ____ & _______
prostaglandin and COX 1 and 2
Side effects of NSAIDs
Blood coagulation, hypersensitivity, Reye’s
Synthetic PGE1 analog
Used prophylactically to prevent NSAID-induced gastric ulcers in patients at high risk
Misoprostol
Many NSAIDs are highly bound to _____ ______
serum albumin
Absorbed as an ionic form from the small intestine and, to lesser extend, from the stomach as an acid form
Inhibits COX 1 and 2 reversibly
May suppress COX-2 induction
salicylates
The only NSAID that irreversibly inhibits COX by acetylating a serine residue in the active site
Aspirin (acetylsalicylic acid)
What classification of drug is this?
Dimer of this group
Hydrolyzed to two salicylates in the small intestine and absorbed
Does not cause GI bleeding
Salsalate (Disalcid)
Salicylates
What classification of drug is this?
More potent analgeic than aspirin but produces fewer side effects
Less antipyretic activity than aspirin
3-4 fold longer half life than aspirin
Diflunisal (Dolobid)
Salicylates
What classification of drug is this?
One of the most potent NSAIDs in use
High incidence of side effects; not suitable for a long-term use
Not stable in solution due to the hydrolysis of the amide bond
Indomethacin
Arylacetic acid
What classification of drug is this?
Prodrug; the sulfoxide group id reduced to the active sulfide intermediate in the circulatory system
Less GI side effects
Suitable for a long-term use to treat chronic inflammation
Sulindac
Arylacetic acids
What classification of drug is this?
Pyranocarboxylic acid
As potent as indomethacin
Somewhat selective for COX-2
Less GI bleeding; suitable for long-term use to manage osteoarthritis
Etodolac
Arylacetic acids
What classification of drug is this?
The most widely used NSAID in the world
As potent as indomethacin
Somewhat selective for COX-2
Inhibits both COX and lipoxygenase pathways
Diclofenac
Arylpropionic acid
Popular OTC analgesic
More potent than aspirin, but less than indomethacin
Moderate degrees of gastric irritation
Bioequivalent racemic mixture
Ibuprofen
Arylpropionic acid
S-(+)-enantiomer; more potent than ibuprofen
Moderate degrees of gastric irritation
Used to treat rheumatoid arthritis and osteoarthritis
Naproxen (Aleve)
Cyclized heteroarylpropionic acid derivative
Short-term management of moderate to severe pain
Analgesic activity similar to centrally acting analgesics
Widely accepted alternative to narcotic analgesics
Ketorolac
What classification of drug is this?
Nonacidic prodrug
Metabolized rapidly which is an effective inhibitor of COX
Minimum gastric side effects
Potent anti-inflammatory, but weak analgesic activity
Nabumetone
Non-carboxylate
What classification of drug is this?
Belongs to the oxicam class, which resembles the peroxy radical intermediate in COX
Enolic acid
Long acting; single daily dose; somewhat COX-2 selective
As potent as indomethacin
Meloxicam
Preferential inhibition of _____ gives anti-inflammatory effects with lower incidence of gastric ulceration
COX-2
What is the suffix for COX-2 inhibitors?
(-coxib)
First NSAID to be marketed as selective COX-2 inhibitor
Used for osteoarthritis and rheumatoid arthritis
Good efficacy against pain, inflammation, and fever
As potent as naproxen; less risk of GI side effects; no antiplatelet activity
Celecoxib (Celebrex)
Analgesic and antipyretic effects similar to aspirin but with fewer adverse effects
not NSAID
Much weaker as an anti-inflammatory agent
Acetaminophen
