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2=Endocrinology > L6. Autacoids > Flashcards

L6. Autacoids Flashcards

1
Q

2 main categories of autacoids

A

histamine

eicosanoids

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2
Q

4 categories of eicosanoids

A
  1. prostanoids
  2. leukotrienes
  3. 12-HETE
  4. lipoxins
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3
Q

3 types of prostanoids

A
  1. Prostacyclins PGI2
  2. prostaglandins
  3. Thromboxane TXA2
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4
Q

3 types of prostaglandins

A

PGD2
PGF2a
PGE2

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5
Q

describe syntheiss of histamine

A

precursor L-histidine via L-histidine decarboxylase

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6
Q

which 2 cells store histamine

A

mast cells

basophils

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7
Q

2 times when histamine is release

A
  1. inflammation/allergic reaction

2. drugs

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8
Q

name 4 drugs which cause histamine release

A
  1. morphine
  2. radiocontrast media
  3. tubocurarine
  4. vancomycin
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9
Q

how does histamine release affect Ca2+?

A

increases cytosolic Ca2+

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10
Q

4 main histamine receptor

A

H1-H4

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11
Q

location of H1 receptor

A

smooth muscle

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12
Q

4 effect of histamine on H1 receptor

A
  1. vasodilation
  2. increased vascular perm
  3. contraction of smooth muscle
  4. itch and pain due to stimulation in nerve endings
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13
Q

2 location of H2 receptor

A

gastric parietal cells, heart

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14
Q

location of H3 receptor

A

presynaptic terminals

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15
Q

what is the triple response to histamine

A
  1. red spot
  2. brighter red flush/ flare
  3. wheal
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16
Q

what is the red spot caused by?

A

direct vasodilator effect

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17
Q

what is the flare caused by?

A

indirect vasodilation

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18
Q

what is the wheal caused by?

A

increased capillary permeability

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19
Q

2 pathophysiological roles of histamine

A
  1. type 1 hypersensitivity reactions

2. gastric acid secretion from gastric paritel cells

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20
Q

which receptor does histamine act on to produce hypersensitivity reaction

A

H1

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21
Q

which receptor does histamine act on to produce gastric acid secretion

A

H2

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22
Q

what 2 conditions are antihistamines only useful in treating

A

hayfever, urticaria

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23
Q

2 pathological conditions caused by excessive gastric acid secretion

A
  1. GORD - gastro-oesophageal reflux disease

2. peptic ulcers

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24
Q

2 examples of H1 receptor antagonists - which have a sedative effect

A

promethazine, chlorpheniramine

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25
3 examples of H1 receptor antagonists - which dont have a sedative effect
cetrizine fexofenadine terfenadine
26
3 examples of H2 receptor antagonists
1. cimetidine 2. ranitidine 3. famotidine
27
what are eicosanoids
lipid autacoids derived from PM phospholipids
28
are eicosanoids stored? why?
no - they are formed from membrane phospholipids as needed
29
which enzyme converts arachnidonate into its prostanoids?
cyclo-oxygenases
30
what is released from the phospholipisd to form the eicosanoids
arachidonic acid
31
which enzyme converts arachnidonate into leukotrienes?
5-lipoxygenases
32
which enzyme forms PGE2?
reductase
33
2 forms of cyclo-oxyegnases
COX 1 COX2
34
where are COX1 enzyes?
most cells
35
where are COX2 enzymes?
inflammatoyr clels
36
how do NSAIDS work?
inhibit COX 1 and 2
37
what are coxibs? how do thye work?
inhibit COX2
38
advantages of COX2 over 1?
less GI SE
39
where is TXA2 produced
platelets
40
where is PGI2 produceed
vascular endothelium
41
effects of PGD2 and PGI2 and PGE2
vasodilation
42
effects of TXA2
vasoconstriction
43
prostanoid responsible for myometrial contraction
PGF21
44
where is PGE2 produced? in response to what?
hypothalamus; pyrogens
45
5 clinical uses of prostanoid agonists
1. medical abortion 2. gastric cytoprotection 3. impotence 4. inhibit platelet aggregation 5. glaucoma
46
clincial use of prostanoid antagonists
anti-inflammatory
47
3 examples of NSAIDS
aspirin, ibuprofen , naproxen
48
2 examples of Coxibs
celecoxib, etoricoxib
49
can pcm be used as an anti-inflammatory? explain?
no - only affects COX in brain not periphery - only has anti-pyretic and analgesic effects
50
4 clinical uses of NSAIDS
1. anti-inflammatory 2. analgesic 3. antipyretic 4. prophylaxis on MI
51
why should only a low aspirin dose be used as prophlyaxis against MI?
low doses selectively inhibit TXA2 - without inhibiting PGI2
52
what leukotrine is produced by neutrophils
LTB4
53
which leukotriene modulates renal function
12-HETE
54
function of lipoxins A and B
oppose actions of LTB4
55
function of LTB4
chemoattractant for inflammatory cells
56
2 function of cysteinul-leukotrienes
bronchoconstrictors | increase vascular permeability
57
clinical use of Cys-L antagonists - give 1 example of a drug
asthma - montelukast
58
does histamine cause vaso constriction or vasodilation
vasodilation
59
T/F : Arachidonic acid is produced by the action of cyclooxygenase enzyme on the membrane phospholipids.
false
60
which prostanoid protects gastric mucosa?
PGE2
61
Cysteinylleukotrienes are potent ____________
bronchoconstricor
62
Allergic reactions which is called Type I hypersensitivity reactions result from the production of
IgE
63
Prostanoids and leukotrienes are both formed from
arachidonic acid
64
example of irreverisble COX inhibitor drug
aspirin
65
does pcm have an anti-inflammatoyr effct?
no
66
what category of drugs does loratadine belong to
antihistamine
67
why do NSAIDS have an anti-inflammtory effect
they inhibit prostaglandins

2=Endocrinology (8 decks)

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