Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharmacology & Medical Chemistry II > Exam 2: Lecture 1, Eicosanoids > Flashcards

Exam 2: Lecture 1, Eicosanoids Flashcards

You may prefer our related Brainscape-certified flashcards:
USMLE® Step 1 flashcards AP® Chemistry flashcards Periodic Table flashcards Chemistry 101 flashcards Organic Chemistry 101 flashcards
1
Q

What are Autacoids?

A

Physiologically active endogenous molecules producing powerful widespread physiological and pharmacological effect

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

What makes up the eicosanoids?

A

Prostaglandins, thromboxane and leukotrienes

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

Hormone info

A

Produced: Gland/Tissue
Stored: Gland/Tissue
Binding: Receptor
Transport: Blood

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

Neurotransmitter info

A

Produced: Neuron
Stored: Vesicle
Binding: Receptor
Transport: Synapse

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

Autacoid info

A

Produced: Cell
Stored: Membrane/Vesicle
Binding: Receptor
Transport: Tissue

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

How are Eicosanoids made?

A

Made from the oxygenation of polyunsaturated long-chain FA fatty acids

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

When are Eicosanoids released?

A

In response to a wide variety of physical, chemical and hormonal factors

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

Eicosanoids General Info 1:

A

Fatty Acids of membranes = source

Produced de novo from biological membrane

Not stored, short life (secs to min)

Biological membranes composed of 500-1000 lipid species, 7nm thick

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

Eicosanoids General Info 2:

A

Oxygenation of FA = makes them

Formed from 20-carbon FA, contain 3-5 Double bonds

Affect all cells and tissues, perform function of local hormones

Arachidonic Acid metabolites

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

Arachidonic Acid is…

A

Most abundant of eicosanoid precursors

Has 4 double bonds

Chemical/physical/inflammatory stimulation = intense and sustained AA production

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

3 Classes of Phospholipase A2

A

cytosolic cPLA2

Secretory sPLA2

Calcium independent iPLA2

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

cPLA2

A

Acute release of AA

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

sPLA2

A

Sustained production of AA

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

iPLA2

A

Negligible AA production

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

Under Normal Conditions, AA is….

A

incorporated into the cell membrane and there is negligible AA biosynthesis

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

Zileuton (Zuflo)

A

Selectively inhibits 5-Lipoxygenase enzyme

Effective against exercise/antigen/aspirin- induced asthma attacks

Side effect: Headache/Respiratory infections/Nausea/Diarrhea/Abdominal pain

Notable: Live functions Test, possible interaction with (Theophylline/warfarin)

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

Zafirlucast (Accolate)

A

Leukotriene (LTD4) receptor antagonist

Effective against exercise/antigen/aspirin- induced asthma attacks

Side effects: Headache/Respiratory infections/Nausea/Diarrhea/Abdominal pain

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

Iloprost (Ventavis)

A

…

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

Epoprostenol (Flolan)

A

PGI2

Occasionally used in dialysis machines to prevent platelet aggregation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Alprostadil (Caverject, Edex, Muse, Prostin)

A

PGE1

used in impotence treatment.

available for injection into the penis or for insertion into the urethra

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Misoprostol (Cytotec)

A

PGE1 Analog

Approved in the USA for peptic ulcer prevention in patients taking high doses of NSAID’s for arthritis

Used in Pediatrics as an infusion to maintain potency of ductus arteriosus in infants during surgical correction

Used in combo with Mifepristone for abortion Europe

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Dinoprostone (Prostin E2, Prepidil, Cervidil) + Latanorpost

A

produce strong uterine contraction

used as efficient abortifacients in 2nd trimester of pregnancy for priming the cervix before abortion

side effect: nausea/vomiting/diarrhea

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Dinoprostone (Prostin E2, Prepidil, Cervidil) + Latanorpost

A

produce strong uterine contraction

used as efficient abortifacients in 2nd trimester of pregnancy for priming the cervix before abortion

side effect: nausea/vomiting/diarrhea

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

2 Major Pathways of Arachidonic Acid Oxygenation

A

Cyclooxygenase (COX) and Lipoxygenase (LOX)

25
Q

Two Isoforms COX

A

COX I - found in many tissues, important under normal conditions

COX II - found in inflammatory tissue, expressed during inflammation

26
Q

COX pathway

A

Prostaglandins PGG2, PGH2, PGE2, PGF2a, PGI2 and TXA2

27
Q

LOX pathway

A

LTA4, LTB4, LTC4, LTD4, Lipoxins, 5-HPETE, and 5-HETE

28
Q

Receptor: DP1

A

Ligand: PGD2

G-protein/2nd Messanger: Gc, increase cAMP

29
Q

Receptor: EP1

A

Ligand: PGE2

G-protein/2nd Messanger: Gq, increase Ca

30
Q

Receptor: EP4

A

Ligand: PGE2

G-protein/2nd Messanger: Gs, increase cAMP

31
Q

Receptor: BLT1

A

Ligand: LTB4

G-protein/2nd Messanger: Gi, Increase Ca, Decrease AMP

32
Q

Receptor: CysLT1

A

Ligand: LTB4

G-protein/2nd Messanger: Gq, Increase Ca, Increase PLC

33
Q

Physiological Effects Eicosanoid Agonists

A

Produce multiple diverse effects upon smooth muscles, platelets and the CNS

Regulate vascular tone, bronchial tone, uterine tone, chemotaxis, and platelet aggregation

Important in some pathologies and participate in “Slow-reacting substance of anaphylaxis”. some are released in large amounts from endometrium during menstruation

34
Q

PGE2 agonist effect

A

Vascular tone, gastric protection, uterine tone, fever, platelet aggregation

35
Q

PGF2a agonist effect

A

Vascular tone, bronchoconstriction, intense pain, uterine contraction

36
Q

PGE1 agonist effect

A

Vasodilation, heat, and redness during inflammation

37
Q

PGI2 agonist effect

A

inhibition of platelet aggregation, vasodilation, gastric protection, inflammation

38
Q

TXA2 agonist effect

A

powerful vasoconstrictor, powerful platelet activator

39
Q

PGD2 (produced in mast cells)

A

vasodilation, platelet inhibitor

40
Q

Eicosanoid Agonists Surface Receptors Info

A

Eicosanoid effect is close to site of synthesis

major effects seems to be produced by the activation of cell surface receptors specific to different eicosanoids

41
Q

Gs-protein coupled receptors

A

DP1, EP2, EP4, and FP

42
Q

IP3 and DAG receptors

A

EP1, FP and TP

43
Q

Target: Phospholipase A2

A

Corticosteroids (antagonist)

44
Q

Target: COX I and II

A

NSAIDs (antagonist)

45
Q

Target: 5-Lipoxygenase Enzyme

A

Zileuton

46
Q

Target: LTD4 Receptor

A

Zafirlukast

47
Q

LTs first found in…

A

Leukocytes

48
Q

PGs first found in…

A

seminal fluid

49
Q

TXs first found in…

A

thrombocytes

50
Q

LOX pathway forms….

A

LTB4, LTC4, LTD4, and LTE4

51
Q

Leukotriene LTB4 is a…

A

chemotactic factor important in all types of inflammation

52
Q

LTD4 acts on receptors causing…

A

WBC adherence, chemotaxis and activation of monocytes

53
Q

LTC4 and LTD4 are active participants in….

A

Slow-reacting substance of anaphylaxis (SRS-A)

important mediator of bronchoconstriction

54
Q

Relative potency of vasoconstrictor effects….

A

LTD4>LTC4>LTE4> Histamine

55
Q

PGE2 and PGI2 limit…

A

in vitro T-lymphocytes proliferation

56
Q

PGE2 inhibits…

A

B-Lymphocytes differentiation

57
Q

Eicosanoids and Immune System

A

Immune system affects eicosanoid synthesis

T and B-cells probably supply AA to monocytes and macrophages

May mediate cell-cell interaction

58
Q

Leukotrienes, TXA2, and PAF stimulate….

A

T-cell clonal expansion

59
Q

Leukotrienes stimlate…..

A

interleukin formation, receptor expression and interferon release

Pharmacology & Medical Chemistry II (43 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions