Anti-Inflammatory Drugs

Question 1

histamine

Answer 1

vasodilation/redness
swelling (vascular permeability)
bronchoconstriction (type 1)
hypotension

histidine — [L-histadine decarboxylase —- > histamine

Question 2

LTB4

Answer 2

pain

chemotactic for neutrophils*

Question 3

LTC4, LTD4, LTE4

Answer 3

peptido leukotrienes
swelling (vascular permeability)
eosinophil chemotactic
bronchoconstriction (type 1)*

Question 4

PGD2

Answer 4

bronchoconstriction (type 1)

Question 5

PGE2

Answer 5

vasodilation/redness
pain
fever* (IL-1 –> PGE2 –> hypothalamus –> fever)

Question 6

PGI2 (prostacyclin)

Answer 6

vasodilation/redness

pain

Question 7

TXA2 (thromboxane)

Answer 7

causes platelet aggregation

vasoconstriction

Question 8

bradykinin

Answer 8

strong vasodilator – hypotension

+lots more

Question 9

kallidin

Answer 9

strong vasodilator – hypotension

+lots more

Question 10

Diphenhydramine

Answer 10

Sedating Antihistamine

H1 inverse agonist, but also blocks muscarinic, alpha adrenergic, and serotonin receptors

sedation, drying of secretions (anticholinergic), GI disturbances

Question 11

Chlorpheniramine

Answer 11

Sedating Antihistamine

H1 inverse agonist, but also blocks muscarinic, alpha adrenergic, and serotonin receptors

sedation, drying of secretions (anticholinergic), GI disturbances

Question 12

Cetirizine (OTC)

Answer 12

non-sedating antihistamine (H1 inverse agonist)
doesn’t penetrate CNS
P-glycoprotein substrate

Question 13

Fexofenadine

Answer 13

non-sedating antihistamine (H1 inverse agonist)
doesn’t penetrate CNS
P-glycoprotein substrate

Question 14

Loratadine (OTC)

Answer 14

non-sedating antihistamine (H1 inverse agonist)
doesn’t penetrate CNS
P-glycoprotein substrate

Question 15

zileuton

Answer 15

lipoxygenase inhibitor

inhibits 5-lipoxygenase –> prevents synthesis of LTB4 (reduced pain and neutrophil chemotaxis)

hepatic tox d/t P450 inhibition (interactions?)

Question 16

zafirlukast

Answer 16

leukotriene receptor antagonist (LTD4 agonist = decreased bronchioconstiction)

inhibits CYP450 (drug interactions?)

Question 17

montelukast

Answer 17

leukotriene receptor antagonist (LTD4 agonist = decreased bronchioconstiction)

prescribed more b/c of once PO admin and no restrictions to meals

Question 18

acetylsalicylate

Answer 18

aspirin (OTC) – NSAID

irreversibly acetylates COX 1 and COX2 serine residues

Question 19

ibuprofen

Answer 19

NSAID w/ fewer side effects than aspirin

Question 20

naproxen

Answer 20

NSAID

Question 21

ketorolac

Answer 21

NSAID

Question 22

indomethacin

Answer 22

NSAID – most potent*

Question 23

sulindac

Answer 23

NSAID

Question 24

ketoprofen

Answer 24

NSAID

Question 25

piroxicam

Answer 25

NSAID – serious GI bleeding*

Question 26

celecoxib

Answer 26

COX 2 inhibitor – 10 to 20x more selective for COX2

Question 27

acetaminophen

Answer 27

analgesic, antipyretic, but NOT anti-inflammatory

inhibits COX in the CNS

serious hepatic injury

Question 28

H2 receptor stimulation will cause…

Answer 28

gastric acid secretion

Question 29

actions of kallidin and bradykinin via B2 receptor…

Answer 29

Kallidin and bradykinin are more active than des-arg forms

hypotension, edema, pain, Na+ excretion

Question 30

actions of kallidin and bradykinin via B1 receptor…

Answer 30

des arg forms most active (thanks to kininase I)

chronic inflammation

vasodilation, pain