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Pharmacology > Eicosanoids > Flashcards

Eicosanoids Flashcards

1
Q

Who discovered prostaglandins and in what year?

A

Ulf von Euler in 1938

The structure was described by Bergstrom in 1950, who won the Nobel Prize in 1982.

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2
Q

What are the three main classes of eicosanoids?

A

Prostaglandins, leukotrienes, thromboxanes

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3
Q

From what substance are eicosanoids produced?

A

Membrane arachidonic acid

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4
Q

What is the molecular structure characteristic of eicosanoids?

A

A five-membered ring and two side chains

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5
Q

What type of hormones are eicosanoids considered?

A

Local hormones or paracrine substances

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6
Q

What is the full name of the fatty acid from which prostanoids are synthesized?

A

5,8,11,14-eicosatetraenoic acid

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7
Q

What enzymes liberate arachidonic acid from plasma membranes?

A

Phospholipases (PLA)

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8
Q

Which two forms of cyclooxygenase are involved in prostaglandin production?

A

COX-1 and COX-2

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9
Q

Name the four principal in-vivo prostaglandins.

A

PGE2, PGI2, PGD2, PGF2α

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10
Q

What is the role of COX-1 in the body?

A

Responsible for gastric epithelial cytoprotection and homeostasis

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11
Q

What does COX-2 respond to?

A

Induced by inflammation, hormones, and growth factors

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12
Q

What is the common substrate produced by both COX isoforms?

A

PGH2

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13
Q

What are the effects of TXA2?

A

Potent vasoconstrictor and smooth muscle mitogen

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14
Q

What are the two key isoenzymes for prostaglandin synthesis?

A

PGH-1 synthase (COX-1) and PGH-2 synthase (COX-2)

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15
Q

What type of receptors do eicosanoids activate?

A

G-protein coupled receptors

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16
Q

How do eicosanoids primarily act on their target cells?

A

By activating adenylyl cyclase to increase intracellular cAMP

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17
Q

Fill in the blank: The cysteinyl leukotrienes are known as _______.

A

Bronchoconstrictors

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18
Q

What is the role of corticosteroids in eicosanoid synthesis?

A

Block all known pathways of eicosanoid synthesis

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19
Q

What is the therapeutic use of Alprostadil?

A

Used in erectile dysfunction

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20
Q

What is the effect of PGE2 on uterine contractions at low concentrations?

A

Promotes uterine contractions

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21
Q

True or False: PGI2 is a potent inhibitor of platelet aggregation.

A

True

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22
Q

What is the primary action of PGE2 in the CNS?

A

Increases body temperature

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23
Q

What is the effect of PGE2 and PGI2 in inflammation?

A

Chemoattractants and enhance edema formation

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24
Q

What are the effects of LTC4 and LTD4?

A

Potent bronchoconstrictors

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25
Q

What is the role of lipoxygenases in metabolism?

A

Play important roles in inflammation

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26
Q

What is the significance of LTB4?

A

Potent chemoattractant for T lymphocytes, neutrophils, eosinophils, monocytes, and mast cells

27
Q

Fill in the blank: The leukotriene products are proposed to have a role in _______.

A

Renal regulation

28
Q

What are the effects of PGF2α in the reproductive system?

A

Contracts uterine muscle

29
Q

What are the effects of PGE2 in the kidneys?

A

Increases medullary blood flow and inhibits tubular sodium reabsorption

30
Q

What is the therapeutic use of Dinoprostone?

A

Induction of labour

31
Q

What does TXA2 do in the cardiovascular system?

A

Potent platelet aggregator

32
Q

What is the relationship between eicosanoids and asthma?

A

Cysteinyl leukotrienes are implicated in asthma

33
Q

Fill in the blank: NSAIDs inhibit _______ activity.

A

PGH-1 synthase

34
Q

What is the effect of PGE2 on smooth muscle?

A

Ca++ dependent relaxation

35
Q

What is the role of COX-2 derived prostanoids in the kidneys?

A

Increase medullary blood flow

36
Q

What does PGD2 promote in the CNS?

A

Induces sleep

37
Q

What is the effect of PGE2 on platelet aggregation?

A

Inhibits platelet aggregation

38
Q

What is the significance of the isoeicosanoid pathway?

A

One of the routes of arachidonic acid metabolism

39
Q

What are the effects of PGE2 and PGI2 in the respiratory system?

A

Relax respiratory muscles

40
Q

What do the cysteinyl leukotrienes promote at the site of inflammation?

A

Endothelial permeability and migration of inflammatory cells

41
Q

Fill in the blank: PGE2 and PGI2 are the major _______ associated with inflammation.

A

Prostanoids

42
Q

What is the therapeutic use of Latanoprost?

A

Reduction of intraocular pressure

43
Q

What is the effect of PGE2 on bone turnover?

A

Increases bone turnover

44
Q

What is the effect of PGE2 on the respiratory system?

A

PGE2 is a potent bronchodilator

PGE2 plays a significant role in widening the air passages in the lungs.

45
Q

Which substances are powerful bronchoconstrictors?

A

PGF2α and TXA2

These substances can induce narrowing of the airways, making breathing more difficult.

46
Q

What role do LTC4 and LTD4 play in asthma?

A

They are important cytokines in asthma

These leukotrienes contribute to inflammation and bronchoconstriction in asthmatic patients.

47
Q

Name two LT-receptor inhibitors effective in asthma.

A

Zafirlukast and Montelukast

These medications help to block the action of leukotrienes in asthma management.

48
Q

How do corticosteroids work in asthma?

A

By inhibiting eicosanoid synthesis

Corticosteroids reduce inflammation in the airways by blocking the production of eicosanoids.

49
Q

What is the mechanism of action of Cromolyn in asthma treatment?

A

Inhibits the liberation of eicosanoids, histamine, and platelet activating factor from mast cells

Cromolyn stabilizes mast cells to prevent the release of inflammatory mediators.

50
Q

What is Misoprostol used for in gastrointestinal treatment?

A

It provides cytoprotection in peptic ulcer

Misoprostol is a PGE1 analogue that protects the stomach lining.

51
Q

What are the effects of PGE2 on T-lymphocyte proliferation?

A

Limits T-lymphocyte proliferation

PGE2 plays a role in modulating immune responses.

52
Q

What does TXA2 stimulate in T-cells?

A

T-cell clonal expansion

TXA2 promotes the proliferation of T-cells, which can enhance immune responses.

53
Q

True or False: Aspirin inhibits COX activity during inflammation.

A

True

Aspirin is known for its anti-inflammatory properties by inhibiting cyclooxygenase enzymes.

54
Q

What is Latanoprost used for?

A

It is used in glaucoma

Latanoprost is a PGF2α derivative that helps lower intraocular pressure.

55
Q

How do corticosteroids inhibit eicosanoid synthesis?

A

By stimulating the synthesis of inhibitory proteins called annexins or lipocortins

These proteins help to block the activity of phospholipase A2.

56
Q

What are 5-LOX inhibitors used for?

A

Indicated in mild to moderate asthma

These inhibitors target leukotriene synthesis to reduce asthma symptoms.

57
Q

What is Ergotism?

A

Dementia, hallucinations, vasospasm, stimulation of uterine muscle

Ergotism is a condition resulting from excessive consumption of ergot alkaloids.

58
Q

What are semi-synthetic ergot alkaloids?

A

Bromocriptine and Cabergoline

These are modified forms of natural ergot alkaloids with specific therapeutic uses.

59
Q

What receptors do ergot alkaloids affect?

A

Adrenoceptors and serotonin receptors: 5-HT1A and 5-HT1D

They can act as agonists or partial agonists at these receptors.

60
Q

What is the clinical use of ergotamine?

A

Used clinically in migraine

Ergotamine’s action on 5-HT receptors helps relieve migraine headaches.

61
Q

What is the primary function of Oxytocin during labor?

A

Mediates myometrial contractility

Oxytocin is essential for stimulating uterine contractions.

62
Q

What is the half-life of Oxytocin?

A

5 minutes

This short half-life necessitates careful dosing during labor.

63
Q

What does Atosiban do?

A

It is an oxytocin receptor antagonist used to treat pre-term labor

Atosiban helps to inhibit contractions and prevent premature delivery.

64
Q

What does Oxytocin stimulate in mammary glands?

A

Contraction of myoepithelial cells around the mammary alveoli

This action promotes milk ejection during breastfeeding.

Pharmacology (18 decks)

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