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IC > Histamine/PG > Flashcards

Histamine/PG Flashcards

1
Q
  • 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
A

autacoids

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2
Q
  • 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
A

histamine

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3
Q

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

A

IgE

type 1

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4
Q

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

A

NO

permeability

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5
Q

effect of H1 on bronchiolar smooth muscle?

A

bronchoconstriction

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6
Q

effect of H1 on GI smooth muscle?

A

contraction, high doses produce diarrhea

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7
Q
  • 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
A

antihistamines

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8
Q
  • have local anesthetic action (Na channel blockers)
  • diphenhydramine and promethazine more potent than procaine
  • also antiparkinsonian, anticholinergic, adrenregic blocking, serotonin blocking
A

H1 antagonists

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9
Q
  • sedation
  • antimuscarinic - urinary retention, blurred vision
  • CYP450 inhibition (ketoconazole)
A

H1 antagonist toxicity

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10
Q
  • at higher doses get cAMP dependent vasodilation and direct cardiac stimulation
  • increased contractility and pacemaker
  • antagonists have little effect on cardiac function
A

H2 mediated response

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11
Q

-stimulate parietal cells to secrete gastric acid

A

H2 receptor mediated response

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12
Q
  • ranitidine, cimetidine, nizatidine, famotidine
  • reduce gastric acid secretion - peptic ulcer, GERD
  • effective doses don’t impact intestinal secretion, other H2 peripheral effects (HR)
A

H2 antagonists

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13
Q

-nervous system: presynaptic receptor activation modulates nuerotransmitter release

A

H3 mediated response

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14
Q
  • family of oxygenation products of polyunsaturated LCFAs

- highly potent molecules, very short half life

A

eicosanoids

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15
Q
  • converts arachidonic acid to prostaglandins

- constitutively expressed, widely distributed, has housekeeping functions

A

COX-1

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16
Q
  • converts AA to prostaglandins
  • inducible, production of inflammatory molecules, expressed in vascular endothelium (PGI2)
  • renal isozyme essential for normal function
A

COX-2

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17
Q

all eicosanoid receptors are _______

A

G-protein coupled

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18
Q

TXA2 and PGF in vascular smooth muscle?

A

vasoconstrictor

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19
Q

PGE2 and PGI2 in vascular smooth muscle?

A

vasodilation

20
Q

prostaglandin effects on GI smooth muscle?

A

longitudinal muscle contraction, relaxation of circular muscle, colicky cramps

21
Q

PGE2 and PGI2 on airway?

A

relaxation

22
Q

TXA2 and PGF on airway?

A

contraction

23
Q

TXA2 effect on platelets?

A

aggregation

24
Q

PGE1 and PGI2 effects on platelets?

A

inhibit aggregation

25
Q

major prostaglandin products of renal cortex?

A

PGE2 and PGI2

26
Q

prostaglandin effects on kidney?

A

vasodilation

27
Q

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

A

excretion

inhibit

28
Q

______ enhances penile erection by relaxing smooth muscles in corpus cavernosum

A

PGE1

29
Q

PGF and low concentration PGE2 in uterus?

A

contraction

30
Q

high PGE2 in uterus?

A

relaxation

31
Q

-oral PGE1 that induces first and second trimester abortion

A

misoprostol

32
Q

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

A

dinoprostone

33
Q

PGF2-alpha control of post partum hemorrhage

A

carboprost

34
Q
  • increase edema and vascular permeability
  • modulation of lymphocyte function
  • PGD2 released from mast cells, recruit eosinophils
A

PGE2 and PGI2

35
Q

PGE1, relaxes smooth muscle

-used for ductus arteriosus, neonates awaiting cardiac surgery, erectile dysfunction

A

alprostadil

36
Q
  • treatment of NSAID induced ulcer

- combined with mifepristone to terminate early pregnancy

A

misoprostol

37
Q

used to induce labor

A

PGE2, PGF2a

38
Q

treatment of open angle glaucoma, PGF2a

A

latanoprost

39
Q

inhibitor of platelets and vasodilator, treat pulmonary hypotension

A

prostacyclin (PGI2)

40
Q
  • treat pulm HTN

- requires constant IV infusion, 3-5 min half life

A

epoprostenol

41
Q

inhaled treatment for pulm HTN

A

iloprost

42
Q

SQ injection or IV for pulm HTN

A

treprostinil

43
Q
  • potent chemoattractants
  • proinflammatory mediators of asthma and IBD
  • cardiac depression
A

leukotrienes

44
Q

5-LOX enzyme inhibitor

A

zileuton

45
Q

leukotriene receptor antagonist

A

montelukast

IC (29 decks)

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