Autacoids: Histamine, Bradykinin, NO

Question 1

Histidine to Histamine uses what rxn and cofactor

Answer 1

decarboxylation and vitamin B6

Question 2

histamines are found in what major sites: (3)

Answer 2

mast cell granules
brain
ECL cells of stomach

Question 3

stimulation of H1 receptors (Gq) causes what 2 things:

Answer 3

1. bronchial and GI smooth m. contraction
2. edema

Question 4

stimulation of H2 receptors (Gs) causes what to happen

Answer 4

increased acid secretion in GI tract

Question 5

what 2 downstream signaling molecules promote exocytosis

Answer 5

cAMP
Ca2+

Question 6

2 main inhibitors of mast cell degranulation

Answer 6

Cromolyn sodium
Nedocromil

Question 7

the 2 antihistamines that penetrate BBB and reach TMN (where histamine is produced)—-causing drowsiness

Answer 7

Diphenhydramine
Dimenhydrinate

Question 8

1st generation antihistamines (diphenhydramine and dimenhydrinate) vs. 2nd generation anti-histamines (cetirizine)

Answer 8

2nd generation do not cross BBB and does not cause drowsiness

Question 9

type of histamine that blocks its own release; self-inhibitory autoreceptor

Answer 9

H3 (Gi)

Question 10

histamine antagonists that can be used to tx Alzheimer’s (increases cognitive enhancement)

Answer 10

H3 antagonist

Question 11

sx’s include urticaria pigmentosa; in children

Answer 11

cutaneous mastocytosis

Question 12

sx’s include flushing, N/V/D, tachycardia, hypotension, syncope; in adults

Answer 12

systemic mastocytosis

Question 13

treatment of mastocytosis

Answer 13

Antihistamines of H1 and H2

Question 14

mepyramine
cetirizine

Answer 14

antihistamines (H1 antagonists)

Question 15

cimetidine, ranitidine

Answer 15

antihistamines (H2 antagonists)

Question 16

what degrades bradykinin

Answer 16

ACE kinase

Question 17

what leads to increase in bradykinin and a dry cough commonly seen when treating HTN with this medicine

Answer 17

ACE inhibitor

Question 18

actions of bradykinin and kallidin resemble what

Answer 18

histamine

Question 19

bradykinin and kallidin lead to what

Answer 19

vasodilation

Question 20

what is the problem of bradykinin and kallidin

Answer 20

causes angioedema

Question 21

Ach binds to M3 and what is released in endothelial vascular smooth m cell that causes relaxation

Answer 21

NO (nitric oxide)

Question 22

increase in intracellular Ca2+ leads to what activation

Answer 22

MLCK

Question 23

activation of MLCK leads to what

Answer 23

MLC phosphorylation then contraction

Question 24

when cAMP is increased and so is PKA, what happens

Answer 24

MLCK is phosphorylated and contraction doesn’t happen

Question 25

NO increases cGMP which leads to phosphorylated MLC inhibiting what

Answer 25

contraction