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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
What is the role of lipoxygenases in metabolism?
Play important roles in inflammation
26
What is the significance of LTB4?
Potent chemoattractant for T lymphocytes, neutrophils, eosinophils, monocytes, and mast cells
27
Fill in the blank: The leukotriene products are proposed to have a role in _______.
Renal regulation
28
What are the effects of PGF2α in the reproductive system?
Contracts uterine muscle
29
What are the effects of PGE2 in the kidneys?
Increases medullary blood flow and inhibits tubular sodium reabsorption
30
What is the therapeutic use of Dinoprostone?
Induction of labour
31
What does TXA2 do in the cardiovascular system?
Potent platelet aggregator
32
What is the relationship between eicosanoids and asthma?
Cysteinyl leukotrienes are implicated in asthma
33
Fill in the blank: NSAIDs inhibit _______ activity.
PGH-1 synthase
34
What is the effect of PGE2 on smooth muscle?
Ca++ dependent relaxation
35
What is the role of COX-2 derived prostanoids in the kidneys?
Increase medullary blood flow
36
What does PGD2 promote in the CNS?
Induces sleep
37
What is the effect of PGE2 on platelet aggregation?
Inhibits platelet aggregation
38
What is the significance of the isoeicosanoid pathway?
One of the routes of arachidonic acid metabolism
39
What are the effects of PGE2 and PGI2 in the respiratory system?
Relax respiratory muscles
40
What do the cysteinyl leukotrienes promote at the site of inflammation?
Endothelial permeability and migration of inflammatory cells
41
Fill in the blank: PGE2 and PGI2 are the major _______ associated with inflammation.
Prostanoids
42
What is the therapeutic use of Latanoprost?
Reduction of intraocular pressure
43
What is the effect of PGE2 on bone turnover?
Increases bone turnover
44
What is the effect of PGE2 on the respiratory system?
PGE2 is a potent bronchodilator ## Footnote PGE2 plays a significant role in widening the air passages in the lungs.
45
Which substances are powerful bronchoconstrictors?
PGF2α and TXA2 ## Footnote These substances can induce narrowing of the airways, making breathing more difficult.
46
What role do LTC4 and LTD4 play in asthma?
They are important cytokines in asthma ## Footnote These leukotrienes contribute to inflammation and bronchoconstriction in asthmatic patients.
47
Name two LT-receptor inhibitors effective in asthma.
Zafirlukast and Montelukast ## Footnote These medications help to block the action of leukotrienes in asthma management.
48
How do corticosteroids work in asthma?
By inhibiting eicosanoid synthesis ## Footnote Corticosteroids reduce inflammation in the airways by blocking the production of eicosanoids.
49
What is the mechanism of action of Cromolyn in asthma treatment?
Inhibits the liberation of eicosanoids, histamine, and platelet activating factor from mast cells ## Footnote Cromolyn stabilizes mast cells to prevent the release of inflammatory mediators.
50
What is Misoprostol used for in gastrointestinal treatment?
It provides cytoprotection in peptic ulcer ## Footnote Misoprostol is a PGE1 analogue that protects the stomach lining.
51
What are the effects of PGE2 on T-lymphocyte proliferation?
Limits T-lymphocyte proliferation ## Footnote PGE2 plays a role in modulating immune responses.
52
What does TXA2 stimulate in T-cells?
T-cell clonal expansion ## Footnote TXA2 promotes the proliferation of T-cells, which can enhance immune responses.
53
True or False: Aspirin inhibits COX activity during inflammation.
True ## Footnote Aspirin is known for its anti-inflammatory properties by inhibiting cyclooxygenase enzymes.
54
What is Latanoprost used for?
It is used in glaucoma ## Footnote Latanoprost is a PGF2α derivative that helps lower intraocular pressure.
55
How do corticosteroids inhibit eicosanoid synthesis?
By stimulating the synthesis of inhibitory proteins called annexins or lipocortins ## Footnote These proteins help to block the activity of phospholipase A2.
56
What are 5-LOX inhibitors used for?
Indicated in mild to moderate asthma ## Footnote These inhibitors target leukotriene synthesis to reduce asthma symptoms.
57
What is Ergotism?
Dementia, hallucinations, vasospasm, stimulation of uterine muscle ## Footnote Ergotism is a condition resulting from excessive consumption of ergot alkaloids.
58
What are semi-synthetic ergot alkaloids?
Bromocriptine and Cabergoline ## Footnote These are modified forms of natural ergot alkaloids with specific therapeutic uses.
59
What receptors do ergot alkaloids affect?
Adrenoceptors and serotonin receptors: 5-HT1A and 5-HT1D ## Footnote They can act as agonists or partial agonists at these receptors.
60
What is the clinical use of ergotamine?
Used clinically in migraine ## Footnote Ergotamine's action on 5-HT receptors helps relieve migraine headaches.
61
What is the primary function of Oxytocin during labor?
Mediates myometrial contractility ## Footnote Oxytocin is essential for stimulating uterine contractions.
62
What is the half-life of Oxytocin?
5 minutes ## Footnote This short half-life necessitates careful dosing during labor.
63
What does Atosiban do?
It is an oxytocin receptor antagonist used to treat pre-term labor ## Footnote Atosiban helps to inhibit contractions and prevent premature delivery.
64
What does Oxytocin stimulate in mammary glands?
Contraction of myoepithelial cells around the mammary alveoli ## Footnote This action promotes milk ejection during breastfeeding.

Pharmacology (18 decks)

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