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MDTI > Prostaglandins > Flashcards

Prostaglandins Flashcards

1
Q

Eicosanoids

A

enzyme derived products of arachadonic acid

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2
Q

eicosanoids catalyzed by cyclooxygenase

A

Prostanoids

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3
Q

five types of prostanoids

A

PGD2, PGE1/2, PGF2a, PGI2, TXA2

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4
Q

isoeicosanoids

A

free radical catalyzed products of AA

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5
Q

arachadonic acid (AA)

A

one of the fatty acids that makes up the phospholipid bilayer

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6
Q

phospholipase A2 (PLA2)

A

required for the release of AA from cell membranes

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7
Q

role of COX in AA pathway

A

converts free AA to an intermediary compound that is rapidly converted by isomerases and syntheses into prostanoids

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8
Q

what enzyme converts intermediate into TxA2?

A

thromboxane synthase (in platelets)

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9
Q

what enzyme converts intermediate into PGE2?

A

PGE2 isomerase (in GI endothelial cells)

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10
Q

what enzyme converts intermediate to PGI2?

A

PGI2 isomerase (in vascular endothelial cells)

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11
Q

activation of PLA2

A

by diverse stimuli such as inflammation, chemical, and physical stimuli

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12
Q

two forms of PLA2

A

cytosolic and inducible

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13
Q

cytosolic PLA2

A

constitutive, present in concentrations high enough for regulatory functions of the cell.

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14
Q

inducible PLA2

A

activated in setting of inflammation or cancer. responsible for greater proportion of free AA in these conditions

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15
Q

isoforms of COX

A

COX1 (constitutively) and COX2 (inducible)

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16
Q

expression of COX1

A

constitutive. but does contribute some degree of prostanoid formation during inflammation

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17
Q

expression of COX2

A

expressed in times of inflammation and cancer

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18
Q

function of COX1

A

housekeeping functions: cytoprotective in GI, platelet function

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19
Q

what cells only express COX1?

A

platelets

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20
Q

tissue distribution of COX1

A

broad distribution

21
Q

what induces COX2 up regulation?

A

inflammatory stimuli, cytokines, growth factor, tumor promoters

22
Q

COX2 is the predominant isoform in what cells?

A

endothelial cells

23
Q

distribution of COX2

A

kidney, brain, synovial cells, macrophages, monocytes

24
Q

what down regulates COX2

A

glucocorticoid

25
Q

cellular mechanism of action of prostanoids

A

GPCR binding specific to prostaglandin activates second messenger system

26
Q

catabolism of prostanoids

A

made quickly and degraded quickly. use as drugs is therefore limited unless made into stable analogs

27
Q

what cells produce TxA2

A

platelets, macrophages, kidney parenchymal cells

28
Q

COX isoform responsible for TxA2

A

COX1

29
Q

TxA2 activity

A

induces platelet aggregation, vasoconstriction and smooth muscle cell proliferation

30
Q

where is prostacyclin I2 (PGI2) produced?

A

endothelial cells

31
Q

COX isoform for PGI2

A

COX2

32
Q

activity of PGI2

A

inhibits platelet aggregation and smooth muscle cell proliferation, vasodilates, proinflammatory

33
Q

role of prostaglandin E (PGE1/2)

A

cytoprotection in the GI by inhibition of gastric acid secretion (COX1), regulates renal blood flow via vasodilation (COX2), regulates salt via renin (COX2), induces uterine/GI smooth muscle contraction (COX1/2), cryogenic role for body temp (COX1/2), pro inflammatory effects (COX2)

34
Q

role of prostaglandin F2a (PGF2a)

A

induces vascular smooth muscle and uterine contraction (luteal regression), vasoconstriction (COX1/2)

35
Q

role of PGD2

A

cutaneous dilation, inhibits platelet aggregation, promotes sleep, mast cell product, chemotaxis of Th2, hair follicles

36
Q

role of inflammation in prostanoid release

A

increases sPLA2, which increases AA release, which increases prostanoid production via increased COX2 expression

37
Q

prostanoids involved in dolor

A

nocioception: PGE1/2, PGI2

38
Q

prostanoids involved in rubor

A

vasodilation: PGE1/2, PGI2

39
Q

prostanoids involved in calor

A

fever: PGE1/2

40
Q

prostanoids involved in tumor

A

vasodilation, edema, leukocyte infiltration, chemotaxis: PGI2, PGE2, PGD

41
Q

steroids

A

reduce the release ofAA from cell membrane by targeting PLA2

42
Q

NSAIDs

A

reduce the production of intermediary compounds by targeting COX

43
Q

Ridogrel

A

reduces production of TxA2 by targeting thromboxane synthase

44
Q

antagonist to prostanoid

A

none known

45
Q

carbaprost

A

PGF2 analog used as abortifacient, post-partum bleeding to expel placenta

46
Q

misoprostol

A

PGE analogue used as abortifacient and for gastric cytoprotection

47
Q

dinoprostone

A

PGE analogue used to induce labor

48
Q

treatment for PDA

A

PGE analog

MDTI (42 decks)

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