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Pharmacy Year 2 Semester 2 > Week 5 TBL > Flashcards

Week 5 TBL Flashcards

1
Q

Prostaglandins are involved in what?

A 
Carcinogenesis
Bone remodelling
Sleep 
Inflammation and pain
Allergy and immunity
Vascular homeostasis and haemostasis
Fever generation
Ovulation, fertilisation and parturition
Gastrointestinal function
Renal function
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2
Q

How do prostaglandins act?

A

5 basic types of receptor
Called P receptors and preceding letter indicated the natural prostanoid to which each receptor is most sensitive
e.g. EP, DP, DF
Subscript numerals indicate that receptor has subtypes e.g. EP1, EP4

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3
Q

IP receptor binds what?

What does it mediate?

A

PGI2

  • vasodilation
  • inhibits platelet aggregation
  • Fibrinolysis
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4
Q

What are prostaglandins?

A

Polyunsaturated, oxygenated derivatives of three C20 fatty acids (AA, DGLA, EPA)

Classified into10 types (PGA-PGJ) according to:

  • the code of ring variants (A-J) and
  • number of double bonds in their side chain (1-3)
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5
Q

If R1 is a carbonyl and R2 is a hydroxyl group.
and the whole structure has 2 double bonds
What name of prostaglandin is it?

A

E2

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6
Q

IF R1 us a hydroxyl group and R2 us a carbonyl group
and the whole structure has 2 double bonds
What name of prostaglandin is it?

A

D2

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7
Q

If both R1 and R2 are hydroxyl groups
and the whole structure has 2 double bonds
What name of prostaglandin is it?

A

F2(alpha)

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8
Q

What is PGE2 involved in?

A

inflammatory

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9
Q

What is PGD2 involved in?

A

immunity

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10
Q

What is PGF2(alpha) involved in?

A

vasoconstriction

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11
Q

What is PGI2 involved in?

A

Potent vasodilator that inhibits platelet aggregation

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12
Q

What is a prostanoid?

A

Prostanoids are a subclass of eicosanoids consisting of the prostaglandins (mediators of inflammatory and anaphylactic reactions), the thromboxanes (mediators of vasoconstriction), and the prostacyclins (active in the resolution phase of inflammation.)

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13
Q

What is TXA2?

A

Thromboxane A2

a potent inducer of platelet aggregation

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14
Q

Draw Prostaglandin E?

A

ok

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15
Q

Draw Prostaglandin F?

A

ok

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16
Q

Draw Prostaglandin D?

A

ok

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17
Q

What are prostaglandins made of?

A 
20C fatty acids 
Major substrate = ARACHIDONIC ACID (AA) (gives rise to ‘2’ series PG)
But can also be derived from: 
   Dihomogamma-linolenic acid (DGLA) 
   (‘1’ series PG) or
   Eicosapentaenoic acid (EPA) 
   (‘3’ series PG)
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18
Q

When DGLA is the precusor molecule, how many double bonds are in the resulting prostaglandin?

A

One

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19
Q

When arachodonic acid is the precusor molecule, how many double bonds are in the resulting prostaglandin?

A

Two

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20
Q

When EPA is the precusor molecule how many double bonds are in the resulting prostaglandin?

A

Three

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21
Q

How many double bonds in DGLA?

A

Three

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22
Q

How many double bonds in AA?

A

Four

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23
Q

How many double bonds in EPA?

A

Five

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24
Q

What kind of enzyme adds carbons?

A

elongase

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25
Q

What kind of enzyme adds double bonds?

A

Desaturase

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26
Q

Which pathways involve our cells all the time with regards to eiconasoids?

A

Fatty acid pathways omega-3, omega-6 and omega-9

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27
Q

EPA is what omega?

A

Omega-3 fatty acid

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28
Q

AA is what omega?

A

Omega-6 fatty acid

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29
Q

DGLA is what omega?

A

Omega-6 fatty acid

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30
Q

Omega means?

A

The end

Omega 3= double bond 3 carbons from the end

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31
Q

What are the essential fatty acids?

A 
alpha-linolenic acid (ALA)
linoleic acid (LA)
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32
Q

What will happen to your body if you have no fat?

A
  • Skin red, unstable

- disorders that come from essential fatty acids

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33
Q

Why are they called essential fatty acids?

A

Mammals cannot make them, we must take them from our diet

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34
Q

Nutrients needed for ALA

A

flaxseed, rapeseed, soy oils

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35
Q

ALA is the start of which pathway?

A

omega-3

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36
Q

LA is the start of which pathway?

A

omega-6

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37
Q

Nutrients needed for LA

A

safflower, cottonseed, soy, cornoils

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38
Q

Why do people eat fish for brain power?

A

DHA is at the end of the omega-3 pathway and is used for brain-power
Babies are born with the correct amount of DHA (from their mothers) in their nervous system
in the omega-3 only a small amount (less than 5%)of ALA is converted to DHA and EPA
hence fish can increase the amount of EPA and then hence the amount of DHA –> brain power!
Having a lot of plant oils will not give you the amount of DHA you need

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39
Q

What things can you eat to increase the amount of EPA in the omega-3 fatty acid pathway?

A

oily fish
fish oils
krill oil
algae

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40
Q

What things can you eat to increase the amount of gamma linoleic acid at the start of the omega-6 pathway?

A

borage and evening primrose oils

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41
Q

What things can you eat to increase the amount of DGLA in the omega-6 pathway?

A

liver, organ meats

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42
Q

What things can you eat to increase the amount of AA in the omega-6 pathway?

A

animal fats, butter, egg yolks

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43
Q

Full name of DGLA

(‘1’ series PG)

A

Dihomogamma-linolenic acid

44
Q

Full name of EPA?

3 series PG

A

Eicosapentaenoic acid

45
Q

Full name of AA?

2 series PG

A

Arachodonic acid

46
Q

What does a phospholipase enzyme do?

A

Convert membrane-bound phospholipid into Arachodonic acid

47
Q

What inhibits a phosopholipase enzyme?

A

Corticosteroids

48
Q

What does a COX enzyme do?

A

Convert AA to the Cyclic endoperoxides
i.e.
PGG2 and PGH2

49
Q

What inhibits a COX enzyme?

A

Coxibs and NSAIDs

50
Q

What does COX stand for?

A

Cyclooxygenase

51
Q

What does NSAID stand for?

A

Non-steroidal anti-inflammatory drug

52
Q

The cyclic endoperoxides PGG2 and PGH2 go on to make what important molecules?

A 
PGD2
PGE2
PGF2
PGI2
TXA2 (Thromboxane)
53
Q

What do prostaglandins generally mediate?

A

mediators of inflammatory and anaphylactic reactions

54
Q

What do prostacyclins generally do?

A

They’re active in the resolution phase of inflammation

55
Q

What do thromboxanes do?

A

Mediators of vasoconstriction

56
Q

True or false, AA is toxic in high concentrations

Why/why not?

A

True
it also explains why AA is metabolised by COX1 immediately after being cleaved why PLA2.
It is not free in the cell.

57
Q

What does PLA2 do?

A

Phospholipase A2 frees (cleaves) arachodonic acid from the cell

58
Q

NSAIDs inhibit what enzyme?

A

COX (cyclo-oxygenase)

59
Q

How do cyclooxygenases make Prostanoids?

A

Cox1 and cox2 work one after the other once AA is released from the membrane
Cox transforms AA to unstable intermediate(s)
And then depending where the reaction takes place and what the system wants, other prostaglandins are made

60
Q

Too much prostaglandin being made uncontrollably can stimulate activity, causing health issues such as…?
PGE2 and COX2 over expression

A

Cancer

61
Q

Cancer has overexpression of what?

A

COX2 enzyme

PGE2

62
Q

Why are coxibs bad? What do they do?

A

Specialist inhibitors of COX2
Side effect was cardiovascular disease
people in clinical trials had heart attacks
COX2 also needed in CVS

63
Q

Difference between the isoforms COX1 and COX2

A

COX-1 - constitutive - in all cells, does basic housekeeping
COX-2 - induced (by cytokines, inflammatory stimuli, induced when cells need a lot of PGs) If you don’t switch it off then there will be inflammation etc

64
Q

low levels of COX-1 needed for

A

homeostasis, vital for cell function

65
Q

Some cell types need COX2 such as

A

CVS cells

66
Q

When a physiological stimulus is there, what happens to AA?

A 
COX-1 pathway activated 
-TXA2 and PGI2 made 
Control of platelet aggregation and vascular tone 
-PGE2 also made
Cytoprotection
67
Q

What happens when PGs are no longer needed?

A

They are metabolised by other enzymes in the body
into inactive metabolites
Uncontrolled overexpression of PGs you get inflammation that cannot resolve

68
Q

Uncontrolled overexpression of PGs you get what?

A

Inflammation that cannot resolve

69
Q

What is a knock-out mice model?

A

mice bred so certain information is removed from the genome

e.g. COX2 knockout mice have no COX2 enzyme

70
Q

Phenotypic changes in COX1 knockout mice?

A
  • reduced platelet aggregation
  • Decreased amino acid-induced inflammation
  • sensitive to radiation injury
  • resistant to indomethacin-induced gastric ulceration
71
Q

Phenotypic changes in COX2 knockout mice?

A
  • Defective ovulation, fertilisation, implantation, decidualisation
  • Decreased brain injury induced by ischaemia
  • supression of tumourgenesis
  • renal nephropathy
  • cardiac fibrosis
  • peritonisis
  • failure of patent ductus arteriosus closure
72
Q

How many domains does a GPCR have?

A

Seven

73
Q

How many types of prostaglandin are there?

A

5

74
Q

PG receptors are…

A

G-protein coupled transmembrane receptors

Linked to cAMP and/or Ca2+ signalling

75
Q

AA is converted to PGG2 via COX

What does PGG2 make?

A

PGH2

76
Q

PGH2 activates what GPCR transmembrane domains?

A 
PGI2
PGD2 
PGE2
PGF2alpha
PGF2
TXA2
PGD2
77
Q

How many receptors are used by PGE?

Why?

A

Four
(EP1, EP2, EP3, EP4)
For ten properties

78
Q

Complete this

DP receptor binds ___ and mediates what?

A

PGD2

  • vasodilation
  • inhibits platelet aggregation
  • GI relaxation
79
Q

FP receptor binds ___ and mediates….

A

PGF2(alpha)

  • luteolysis (degradation of corpus luteum in menstral cycle)
  • bronchoconstriction
80
Q

IP receptor binds ___ and mediates…

A

PGI2

  • vasodilation
  • inhibits platelet aggregation
  • fibrinolysis
81
Q

TP receptor binds ___ and mediates..

A

TXA2 (Thromboxane)

  • vasoconstriction
  • platelet aggregation
  • bronchoconstriction
82
Q

What does the EP1 receptor mediate?

A

GI contraction

Pyrexia (fever)

83
Q

What does EP2 receptor mediate?

A

bronchodilation
vasodilation
stimulates GI fluid secretion

84
Q

What does EP3 receptor mediate?

A

GI relaxation
inhibition of gastric acid secretion
inhibition of ANS transmitters
pyrexia

85
Q

What does EP4 receptor mediate?

A

vasodilatation
bone homeostasis
pyrexia

86
Q

Methods of relatting PGs to therapeutics?

A

substrate substitution
enzyme inhibitors
prostaglandin replacement therapy/use of synthetic, selective analogues

87
Q

If you change your diet to eat less meat and more fish, what will happen?

A

Less omega-6 fatty acids produced (therefore less and DGLA AA)
More omega-3 fatty acids produced (therefore more EPA)
This will produce an anti-inflammatory environment
Not to trigger baseline inflammatory conditions

88
Q

GLA comes from primose oil

what effect?

A

Calming effect as it promotes more PG1 instead of PG2

89
Q

fish oil in diet is good because…

A

Fish oil is rich in DHA and EHA

it promotes PG3 instead of PG2

90
Q

Omega-3 fatty acids were significant in clinical trails because fish oil supplementation resulted in

A

reduction of fasting blood triglycerides

(but not total HDL or LDL cholesterol) in hyperlipidaemic subjects

91
Q

in only one condition Coxibs are still used

Which? Why?

A

Arthritis

Because risk of CVD is considered worth it to reduce pain

92
Q

renal syndrome side effects of NSAIDs due to decrease in PGE2

A
  • increase Na+ retention
  • peripheral oedema
  • increase in blood pressure
  • increase in weight
  • congestive heart failure (rarely)
93
Q

renal syndrome side effects of NSAIDs due to decrease in PGI2

A
  • hyperkalaemia

- acute renal failure

94
Q

‘Prostaglandin replacement therapy’/use of synthetic, selective analogues

A

Arthrotec = diclofenac + misoprostol
(NSAID + reduced stomach acid)

Diclofenac: NSAID
Misoprostol: EP1/3 agonist, which restores cytoprotection; prevents stomach ulcers

95
Q

Arthrotec is?

A

Diclofenac + misoprostol

NSAID + reduced stomach acid

96
Q

What is Diclofenac?

A

NSAID

97
Q

What is Misoprostol?

A

EP1/EP3 agonist, which restures cytoprotection and prevents stomach ulcers

98
Q

PGE2 can lead to carcinogenesis,

how?

A

cAMP and calcium concentration induce:

1) direct targeting of gene transcription, inducing cell proliferation (growth) and migration (potential metastasis)
2) –> HIF-1alpha causes VEF transcription and angiogenesis
3) Production of Survivin which inhibits apoptosis
4) —> MMPs –> increase invasiveness
5) –> PKA and PKC–>MAPK—1)

99
Q

How do prostacyclins reduce intra-ocular pressure in glaucoma?

A

Reduce intra-ocular pressure relieving the optic nerve; allow fluid to drain freely

Latanoprost – PGF2a analogue
Bimatoprost – PGF2a analogue

100
Q

Additional therapeutic uses for PGE analogues

A 
Adjuncts to mifepristone and other agents used to terminate pregnancy
Cervical ripening
Potential uses to manage:
Preterm labour
Dysmenorrhoea
Airway disease
101
Q

What are the stimuli which induce AA production from phospholipid A?

A

cPLA2

sPLA2

102
Q

PGH2 and PGH3 make…

A 
L-PGDS
H-PGDS
mPEGS-1
PGFS
PGIS
TXAS
103
Q

L-PGDS and H-PGDS make what PG?

A

PGD2

104
Q

mPEGS-1 makes what PG?

A

PGE2

105
Q

PGFS makes what PG?

A

PGF2alpha

106
Q

PGIS makes what PG?

A

PGI2

107
Q

TXAS makes what?

A

TXA2

Pharmacy Year 2 Semester 2 (33 decks)

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