NSAIDs and Antihistamines Flashcards
Inflammation
normal, protective response to tissue injury caused by physical trauma, noxious chemicals, microbiological agents
Nonselective COX Inhibitors: Salicylates examples
aspirin
Nonselective COX Inhibitors: Non-Salicylates examples
ibuprofen, ketoprofen, diclofenac, ketorolac
COX2 Inhibitor example
Celecoxib
Aspirin MOA
irreversibly inactivates COX
inhibits prostaglandin synthesis at PGE2
Low dose of Aspirin (<300mg)
inhibit platelet aggregation
SE of Aspirin
GI irritation
prolongs bleeding- cant have before surgery
blocks PGE2 and PGF2a that stops protective mucous secretions of stomach
Reye Syndrome
Countering SE of Aspirin
take with food and water
antacids
Reye Syndrome
fatal hepatitis with cerebral edema
aspirin during viral infections
Ibuprofen/ Ketoprofen MOA
inhibits COX
Diclofenac
formed in combination with misoprostol
0.1% used in post op eye inflammation
Ketorolac
used to treat seasonal allergic conjunctivitis
Celecoxib
inhibits COX2
used for osteoarthritis, rheumatoid arthritis, acute pain
reduced risk for GI issues
Celecoxib should not be used on…
patients allergic to sulfonamides
Acetaminophen
analgesic and antipyretic
no anti-inflammatory effect
Pharmacokinetics of Acetaminophen
made by glucuronidation and sulfation; part is hydroxylated to NAPQI- dangerous unless reacting with glutathione
Comparing Acetaminophen with Aspirin
no effect on platelets
does not cause Reye Syndrome
SE of Acetaminophen
large doses cause hepatic necrosis- liver failure
Countering SE of Acetaminophen
acetylcysteine
Histamines
lead to inflammatory responses- runny nose, anaphylactic shock
H1 Receptors (Gq)
smooth muscle, endothelium, brain
H2 Receptors (Gs)
Gastric Mucosa
Triple Response of Lewis- intradermal injection of histamine
red spot- few mm
flare- 1 cm beyond site
wheal- 1-2 min
First vs Second Gen H1 Receptor Antagonists
sedative vs nonsedative
First Gen H1 Receptor Antagonists
mine and zine
sedation
lipid soluble- CNS penetration, cross BBB
Second Gen H1 Receptor Agonists
Dine
non sedating or weak sedation
no drug interactions
does not cross BBB
Promethazine
H1
motion sickness, morning sickness
Cetirizine
H1
mast cell stabilizer and anti-inflammatory
Cyproheptadine
H1
appetite stimulant
Increase effects of antihistamines
MAOI
Antihistamines with no CNS entry
loratadine
fexofenadine