Santanam Flashcards

(47 cards)

1
Q

Arachidonic acid is cleaved from membrane phospholipid by what

A

PLA2

PLC - specifically cleaves phosphatidylinositides, also requires Diglyceride lipase to get to AA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what are eicosanoids

A

oxygenated products of polyUNsaturated FAs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What affects the function of eicosanoids

A

nature of the precursor fatty acids

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

TXA2 vs TXA3

A

TXA2 - vasoconstrictor

TXA3 - inactive

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What is prostaglandin synthetase

A

Enzyme complex of:

  • COX
  • Peroxidase
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Which COX is constitutive? Inducible?

A

COX-1 : Constitutive

COX-2 : Inducible

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Where do you find COX-1

A

BV, stomach, kidney

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What is COX-2 involved with?

A

Inflammation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What causes elevation of COX-2

A

Inflammation and cytokines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What is the effect of glucocorticoids on COX-2?

A

Decreased COX-2 activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Mechanism of Action: Prostaglandins

A
  1. Acts locally: paracrine, autocrine - short half life

2. Interacting with a receptor (GPCRs) ***

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What happens after Prostaglandins bind receptor?

A

Inc or dec of adenylate cyclase

stimulation of phosphatidylinositol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Where is the major effect of prostaglandins seen? name the four types/areas

A

Smooth muscle: vascular, GI, airway, and reproductive

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Which enzyme is involved with the linear pathway

A

Lipoxygenase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Which enzyme is involved with the cyclic pathway

A

PGH synthetase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

In the COX pathway, what is the resulting product of action of COX on AA?

A

Unstable endoperoxide (PGG2)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What is the action of peroxidase in COX pathway?

A

C15 hydroperoxide (PGG2) –> C15 hydroxyl group (PGH2)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What are the four products of COX pathway? what is the intermediate for all four?

A
  • TXA2
  • PGI2
  • PGE2
  • PGF2a

Intermediate: PGH2 with hydroxyl group

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Where is COX-2 constitutively expressed?

A

Brain and kidney

20
Q

What does COX-1 protect against? how?

A

HCl via increase in stomach mucus

21
Q

What is a common side effect of COX-1 inhibition?

A

GI ulcers

dec stomach mucus, more susceptible to damage due to HCl in stomach

22
Q

Effect of prostacyclin on:

Vascular:
Airway:
GI:
Reproductive:
Pain:
A
  • Vasodilator and Inhibit platelet aggregation
  • Bronchodilator
  • Inhibit gastric acid secretion, increased mucus secretion
  • Relaxes uterine muscle
  • Induces pain
23
Q

Effect of Prostaglandin on:

Vascular:
Airway:
GI:
Reproductive:
Pain:
A

Vascular, Airway, GI, pain: same as prostacyclin

CONTRACTS uterine smooth muscle - low conc
relaxes in high conc

24
Q

What is the effect of prostaglandins on fever?

A

Direct pyrogen in hypothalamus

25
What cytokine stimulates PGE2?
IL-1
26
Effect of Thromboxane on: Vascular: Airway: Reproductive:
- Vasoconstrictor and stimulates Platelet aggregation - Bronchoconstrictor - Uterine contraction
27
What is major product of platelet COX-1? COX-2?
Thromboxane Prostacyclin
28
Effect of Prostaglandin F2a on: Vascular: Airway: Reproductive:
- Vasoconstrictor - Bronchoconstrictor - Contracts uterine muscle
29
What effect does PGF2a have on the eye?
Decreases intraocular pressure
30
What is PGF2a used to treat? What is defective in this disease?
Glaucoma | loss of COX-2
31
What keeps DA open in fetus?
PGE2/1 and PGI2
32
What happens to DA after birth?
Closes because of decreased PGE2/1, PGI2
33
What is used to keep DA open in cyanotic heart disease?
Alprostadil via IV infusion
34
What is used to close DA?
Indomethacin
35
What specific enzyme is used in the lipoxygenase pathway?
5-lipoxygenase
36
What is the intermediate in LOX pathway?
5-HETE
37
Name two chemotactic agents for PMN, Eosinophils, monocytes formed in the linear pathway
- 5-HETE | - LTB4
38
What does LTE4 (LTC4, LTD4) do?
Potent bronchoconstrictor Inc vascular permeability Components of slow reacting substance of anaphylaxis
39
What are LTE4, LTC4, LTD4 known as
Cysteinyl leukotrienes
40
What is the side group on 5-HETE and what is it converted to by ______ to LTA4?
5-hydroperoxide to 5,6-epoxide by Dehydrase
41
What enzyme converts LTA4 to Cysteinyl leukotrienes
Glutathione-S-transferase
42
What enzyme converts LTA4 to LTB4?
Hydrolase
43
What is the LOX pathway associated with?
Asthma, anaphylactic shock, CVD
44
Which leukotriene produces hyperalgesia
LTB4
45
Which leukotrienes are chemoattractants for eosinophils?
Cysteinyl leukotrienes
46
What is FLAP?
5-LOX activated protein
47
Which receptor does Zafirlukast, Montelukast antagonize?
Cys-LT1 (LTD4)