Histamine/PG

Question 1

• endogenous substances in the body (histamine, serotonin, peptides, prostaglandins, leukotrienes)
• short duration of action and act near site of synthesis/release
• high levels cause undesirable effects

Answer 1

autacoids

Question 2

• in basophils/mast cells: high levels in potential sites of injury, nose/mouth/feet, blood vessels
• in brain : neurotransmitter function
• ECL cells in stomach: activate acid production

Answer 2

histamine

Question 3

immunologic histamine release - allergens cross link ______ on the cell surface eliciting granulation
-releases histamine causes type ____ allergic reaction (hay fever, acute urticaria)

Answer 3

IgE

type 1

Question 4

in CV system, H1 receptor mediated response is vasodilation mediated by increase in _______ release, reflex tachycardia, and increased _______ of post capillary vessels

Answer 4

NO

permeability

Question 5

effect of H1 on bronchiolar smooth muscle?

Answer 5

bronchoconstriction

Question 6

effect of H1 on GI smooth muscle?

Answer 6

contraction, high doses produce diarrhea

Question 7

• rapidly absorbed when taken orally
• distribute to most tissues
• 1st gen last 4-6 hrs, 2nd gen last 12-24 hours
• used for allergic reactions (not bronchial asthma)
• motion sickness, sedative effects

Answer 7

antihistamines

Question 8

• have local anesthetic action (Na channel blockers)
• diphenhydramine and promethazine more potent than procaine
• also antiparkinsonian, anticholinergic, adrenregic blocking, serotonin blocking

Answer 8

H1 antagonists

Question 9

• sedation
• antimuscarinic - urinary retention, blurred vision
• CYP450 inhibition (ketoconazole)

Answer 9

H1 antagonist toxicity

Question 10

• at higher doses get cAMP dependent vasodilation and direct cardiac stimulation
• increased contractility and pacemaker
• antagonists have little effect on cardiac function

Answer 10

H2 mediated response

Question 11

-stimulate parietal cells to secrete gastric acid

Answer 11

H2 receptor mediated response

Question 12

• ranitidine, cimetidine, nizatidine, famotidine
• reduce gastric acid secretion - peptic ulcer, GERD
• effective doses don’t impact intestinal secretion, other H2 peripheral effects (HR)

Answer 12

H2 antagonists

Question 13

-nervous system: presynaptic receptor activation modulates nuerotransmitter release

Answer 13

H3 mediated response

Question 14

• family of oxygenation products of polyunsaturated LCFAs

- highly potent molecules, very short half life

Answer 14

eicosanoids

Question 15

• converts arachidonic acid to prostaglandins

- constitutively expressed, widely distributed, has housekeeping functions

Answer 15

COX-1

Question 16

• converts AA to prostaglandins
• inducible, production of inflammatory molecules, expressed in vascular endothelium (PGI2)
• renal isozyme essential for normal function

Answer 16

COX-2

Question 17

all eicosanoid receptors are _______

Answer 17

G-protein coupled

Question 18

TXA2 and PGF in vascular smooth muscle?

Answer 18

vasoconstrictor

Question 19

PGE2 and PGI2 in vascular smooth muscle?

Answer 19

vasodilation

Question 20

prostaglandin effects on GI smooth muscle?

Answer 20

longitudinal muscle contraction, relaxation of circular muscle, colicky cramps

Question 21

PGE2 and PGI2 on airway?

Answer 21

relaxation

Question 22

TXA2 and PGF on airway?

Answer 22

contraction

Question 23

TXA2 effect on platelets?

Answer 23

aggregation

Question 24

PGE1 and PGI2 effects on platelets?

Answer 24

inhibit aggregation

Question 25

major prostaglandin products of renal cortex?

Answer 25

PGE2 and PGI2

Question 26

prostaglandin effects on kidney?

Answer 26

vasodilation

Question 27

COX-1 in kidney promote salt _______ in the collecting ducts -COX-2: increase medullary blood flow and _______ tubular sodium reabsorption

Answer 27

excretion inhibit

Question 28

______ enhances penile erection by relaxing smooth muscles in corpus cavernosum

Answer 28

PGE1

Question 29

PGF and low concentration PGE2 in uterus?

Answer 29

contraction

Question 30

high PGE2 in uterus?

Answer 30

relaxation

Question 31

-oral PGE1 that induces first and second trimester abortion

Answer 31

misoprostol

Question 32

PGE2 given vaginally for abortion, stimulates contraction of uterus, controlled release for induction of labor

Answer 32

dinoprostone

Question 33

PGF2-alpha control of post partum hemorrhage

Answer 33

carboprost

Question 34

- increase edema and vascular permeability - modulation of lymphocyte function - PGD2 released from mast cells, recruit eosinophils

Answer 34

PGE2 and PGI2

Question 35

PGE1, relaxes smooth muscle | -used for ductus arteriosus, neonates awaiting cardiac surgery, erectile dysfunction

Answer 35

alprostadil

Question 36

- treatment of NSAID induced ulcer | - combined with mifepristone to terminate early pregnancy

Answer 36

misoprostol

Question 37

used to induce labor

Answer 37

PGE2, PGF2a

Question 38

treatment of open angle glaucoma, PGF2a

Answer 38

latanoprost

Question 39

inhibitor of platelets and vasodilator, treat pulmonary hypotension

Answer 39

prostacyclin (PGI2)

Question 40

- treat pulm HTN | - requires constant IV infusion, 3-5 min half life

Answer 40

epoprostenol

Question 41

inhaled treatment for pulm HTN

Answer 41

iloprost

Question 42

SQ injection or IV for pulm HTN

Answer 42

treprostinil

Question 43

- potent chemoattractants - proinflammatory mediators of asthma and IBD - cardiac depression

Answer 43

leukotrienes

Question 44

5-LOX enzyme inhibitor

Answer 44

zileuton

Question 45

leukotriene receptor antagonist

Answer 45

montelukast