L6. Autacoids

Question 1

2 main categories of autacoids

Answer 1

histamine

eicosanoids

Question 2

4 categories of eicosanoids

Answer 2

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

Question 3

3 types of prostanoids

Answer 3

1. Prostacyclins PGI2
2. prostaglandins
3. Thromboxane TXA2

Question 4

3 types of prostaglandins

Answer 4

PGD2
PGF2a
PGE2

Question 5

describe syntheiss of histamine

Answer 5

precursor L-histidine via L-histidine decarboxylase

Question 6

which 2 cells store histamine

Answer 6

mast cells

basophils

Question 7

2 times when histamine is release

Answer 7

1. inflammation/allergic reaction

2. drugs

Question 8

name 4 drugs which cause histamine release

Answer 8

1. morphine
2. radiocontrast media
3. tubocurarine
4. vancomycin

Question 9

how does histamine release affect Ca2+?

Answer 9

increases cytosolic Ca2+

Question 10

4 main histamine receptor

Answer 10

H1-H4

Question 11

location of H1 receptor

Answer 11

smooth muscle

Question 12

4 effect of histamine on H1 receptor

Answer 12

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

Question 13

2 location of H2 receptor

Answer 13

gastric parietal cells, heart

Question 14

location of H3 receptor

Answer 14

presynaptic terminals

Question 15

what is the triple response to histamine

Answer 15

1. red spot
2. brighter red flush/ flare
3. wheal

Question 16

what is the red spot caused by?

Answer 16

direct vasodilator effect

Question 17

what is the flare caused by?

Answer 17

indirect vasodilation

Question 18

what is the wheal caused by?

Answer 18

increased capillary permeability

Question 19

2 pathophysiological roles of histamine

Answer 19

1. type 1 hypersensitivity reactions

2. gastric acid secretion from gastric paritel cells

Question 20

which receptor does histamine act on to produce hypersensitivity reaction

Answer 20

H1

Question 21

which receptor does histamine act on to produce gastric acid secretion

Answer 21

H2

Question 22

what 2 conditions are antihistamines only useful in treating

Answer 22

hayfever, urticaria

Question 23

2 pathological conditions caused by excessive gastric acid secretion

Answer 23

1. GORD - gastro-oesophageal reflux disease

2. peptic ulcers

Question 24

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

Answer 24

promethazine, chlorpheniramine

Question 25

3 examples of H1 receptor antagonists - which dont have a sedative effect

Answer 25

cetrizine fexofenadine terfenadine

Question 26

3 examples of H2 receptor antagonists

Answer 26

1. cimetidine 2. ranitidine 3. famotidine

Question 27

what are eicosanoids

Answer 27

lipid autacoids derived from PM phospholipids

Question 28

are eicosanoids stored? why?

Answer 28

no - they are formed from membrane phospholipids as needed

Question 29

which enzyme converts arachnidonate into its prostanoids?

Answer 29

cyclo-oxygenases

Question 30

what is released from the phospholipisd to form the eicosanoids

Answer 30

arachidonic acid

Question 31

which enzyme converts arachnidonate into leukotrienes?

Answer 31

5-lipoxygenases

Question 32

which enzyme forms PGE2?

Answer 32

reductase

Question 33

2 forms of cyclo-oxyegnases

Answer 33

COX 1 COX2

Question 34

where are COX1 enzyes?

Answer 34

most cells

Question 35

where are COX2 enzymes?

Answer 35

inflammatoyr clels

Question 36

how do NSAIDS work?

Answer 36

inhibit COX 1 and 2

Question 37

what are coxibs? how do thye work?

Answer 37

inhibit COX2

Question 38

advantages of COX2 over 1?

Answer 38

less GI SE

Question 39

where is TXA2 produced

Answer 39

platelets

Question 40

where is PGI2 produceed

Answer 40

vascular endothelium

Question 41

effects of PGD2 and PGI2 and PGE2

Answer 41

vasodilation

Question 42

effects of TXA2

Answer 42

vasoconstriction

Question 43

prostanoid responsible for myometrial contraction

Answer 43

PGF21

Question 44

where is PGE2 produced? in response to what?

Answer 44

hypothalamus; pyrogens

Question 45

5 clinical uses of prostanoid agonists

Answer 45

1. medical abortion 2. gastric cytoprotection 3. impotence 4. inhibit platelet aggregation 5. glaucoma

Question 46

clincial use of prostanoid antagonists

Answer 46

anti-inflammatory

Question 47

3 examples of NSAIDS

Answer 47

aspirin, ibuprofen , naproxen

Question 48

2 examples of Coxibs

Answer 48

celecoxib, etoricoxib

Question 49

can pcm be used as an anti-inflammatory? explain?

Answer 49

no - only affects COX in brain not periphery - only has anti-pyretic and analgesic effects

Question 50

4 clinical uses of NSAIDS

Answer 50

1. anti-inflammatory 2. analgesic 3. antipyretic 4. prophylaxis on MI

Question 51

why should only a low aspirin dose be used as prophlyaxis against MI?

Answer 51

low doses selectively inhibit TXA2 - without inhibiting PGI2

Question 52

what leukotrine is produced by neutrophils

Answer 52

LTB4

Question 53

which leukotriene modulates renal function

Answer 53

12-HETE

Question 54

function of lipoxins A and B

Answer 54

oppose actions of LTB4

Question 55

function of LTB4

Answer 55

chemoattractant for inflammatory cells

Question 56

2 function of cysteinul-leukotrienes

Answer 56

bronchoconstrictors | increase vascular permeability

Question 57

clinical use of Cys-L antagonists - give 1 example of a drug

Answer 57

asthma - montelukast

Question 58

does histamine cause vaso constriction or vasodilation

Answer 58

vasodilation

Question 59

T/F : Arachidonic acid is produced by the action of cyclooxygenase enzyme on the membrane phospholipids.

Answer 59

false

Question 60

which prostanoid protects gastric mucosa?

Answer 60

PGE2

Question 61

Cysteinylleukotrienes are potent ____________

Answer 61

bronchoconstricor

Question 62

Allergic reactions which is called Type I hypersensitivity reactions result from the production of

Answer 62

IgE

Question 63

Prostanoids and leukotrienes are both formed from

Answer 63

arachidonic acid

Question 64

example of irreverisble COX inhibitor drug

Answer 64

aspirin

Question 65

does pcm have an anti-inflammatoyr effct?

Answer 65

no

Question 66

what category of drugs does loratadine belong to

Answer 66

antihistamine

Question 67

why do NSAIDS have an anti-inflammtory effect

Answer 67

they inhibit prostaglandins