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Autocoids Flashcards

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1
Q

What are the Autocoids

A

Naturally available substances

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2
Q

Examples of autocoids

A

Eicosanoids
Angiotensin
Nrurotensin
NO
Kinins
Histamine
Serotonin
Endothelins

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3
Q

Features of the Eicosanoids

A

Oxygenation products of AA
Wide range of therapeutic usefulness
Prostaglandins
Thromboxanes
Leukotrienes

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4
Q

AA libearted from where

A

Cell membrane phospholipids

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5
Q

Which enzyme is responsible for the generation of AA from the cell membrane

A

Phospholipase A

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6
Q

What are the forms of PLA

A

Cardiac
Cytosolic— Ca dependent
Secretory— Ca dependent

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7
Q

Pathways of AA

A

1-COX Pathway
2- 5-Lipoxygenase pathways

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8
Q

How is the COX pathway occur

A

COX coverts AA to PGG2 and then Eicosanoids

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9
Q

Isoforms of COX

A

COX-1= always secreted, important for physiological situations.
COX-2=specific for pathological situations, secreted when needed
COX-3

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10
Q

COX-2 inhibitors

A

NSAIDs
Rofecoxib
Celecoxib
Nimesulide

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11
Q

Side effects of COX-1 inhibitors

A

COX is responsible for inhibition of gastric acid secretion and helps to secrete gastric mucus
Inhibiting COX-1 can result with decrease in mucus secretion and cause ulcers

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12
Q

COX enzymes converts AA to what?

A

Prostaglandin G2
Which is an unstable cyclic endoperoxide and coverts to PGH2
PGH2 also unstable and yields to PGI2,PGE2,PGF2a,PGD2, Thromboxane A2 and Thrombaxe B2.

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13
Q

Why corticoids are used as an anti-inflammatory drug?

A

They induce the formation of lipocortin that inhibts PLA
They can also inhibit COX-2 gene expression

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14
Q

What are the general effects of Eicosanoids

A

Effect on
Vascular
Airway
Reproductive
GI smooth muscles

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15
Q

Vasoconstrictor Eicasonids

A

TXA2
PGF2a

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16
Q

Vasodilator prostaglandins

A

PGI2
PGE2

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17
Q

GI smooth muscle contractor Eicosanoids

A

PGs
TXA2

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18
Q

Constrictor of bronchial smooth muscles

A

TXA2
PGE2
PGF2a

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19
Q

Bronchodilator Eicosanoids

A

PGI2
PGE2
PGE1

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20
Q

Inhibitors of platelet aggregation

A

PGE1
PGI2

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21
Q

Enhances the Platelet aggregation

A

TXA2

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22
Q

Role of aspirin

A

Aspirin inhibts TXA2 formation only in platelets
Inhibits vasodilator PGI2 formation
Antiaggregant

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23
Q

Kidney synthesizes which Eicasonoids

A

PGs— PGE1,PGE2,PGD2— for glomerular filtration due to their vasodilator effect

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24
Q

Effects of PGs in the reproductive system

A

PGE2 and PGF2a are oxytocic molecules— normal delivery
Used for the abortion and initiation of labor
PGE1 helps erection
Seminal vesicles, prostate and testes produce PGs

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25
Eicasonoids involved in fever
PGE1 PGE2
26
Eicasonoid that regulates natural sleep
PGD2
27
Eicosanoids that decrease the intraocular pressure
PGE PGF
28
Dinoprostone
Synthetic analogue of PGE2 Produces contraction of uterine muscles
29
Alprostadil
PGE1 analogue Used for the treatment of erectile dysfunction in men
30
Epoprostenol
PGI2 analogue Uses for pulmonary hypertension
31
Eicosanoids that involved in Patent Ductus Arteriousus
PGE2 and PGI2 NSAIDs are used for the duct closure If duct should remain open Alprostadil is administered
32
Misoprostol
PGE1 analogue Used for ulcer treatment COX-1 effects are minimized where administered with NSAIDs
33
How is the Lipoxygenase Pathway
AA— Leukotriene A4—Leukotriene B4—Leukotriene C4—Leukotriene D4—Leukotriene E4
34
Which Leukotriene types are Bronchoconstrictors
LTC4 LTD4
35
Zileuton and Zafirkulast used in which disease
Asthma
36
Features of Lipoxins
Derived from AA Gamma-6 fatty acid 2 types= LXA and LXB Formed by platelets but platelets cannot synthesize them alone. Inhibit chemotaxis,transmigration,superoxide generation and NF-kB activation. Antagonize the receptors of cysteine leukotrienes so that inflammation stop. Signal macrophages to phagocyte the remains of these cells.
37
LTA4 will form bc of platelets?
LTA4 converted to LXA4 and LXB4 by 12-Lipoxygenase. LTA4 will form LTC4,LTD4,LTE4 which are synthesized in platelets.
38
LXA4 will form?
Cysteinyl-Lipoxins— LXC4,LXD4,LXE4
39
Lipoxins act on which receptors?
LXA4R and inhibit chemotaxis,transmigrationisuperoxide generation and NF-kB activation
40
Lipoxins antagonize which receptors?
Cysteinyl Leukotrienes receptors so that inflammation can stop
41
During the acute inflammatory process, the pro inflammatory cytokines such as IFN-y and IL-1beta can induce the expression of?
Anti-inflammatory mediators such as Lipoxins and IL-4, which promote the resolution phase of ingfalmmation.
42
How is the production of Histamine
B-imidazoleethylamine = Histamine Histidine———— Histamine by Histidine Decarbozylase
43
What inhibits the conversion of Histidine to Histamine
Alpha-fluoromethyl histidine Tritocaline
44
Histamine is present in
Mast cells— as a complex with heparin Neuronal histamine Enterokromaffine cells (APUD cells)
45
How is the liberation of Histamine from Mast cells
Mast cells contain IgE as receptors on their surface. As the ag interacts with IgE, histamine liberated.
46
Can Histamine be absorbed?
Yes but the microorganisms in the GIT metabolism histamine. Histamine is metabolized by histamine N-methyl transferase or diamond oxidase. End product is methyl imidazole acetic acid
47
Histamine receptors
H1—G protein coupled receptor — produces phosphoinositidyl hydrolysis H2— G protein coupled receptor — inhibition of Adenylate cyclase activity. H3— inhibits Acetyl Choline release
48
Agonists do H1,H2,H3
H1: 2-methyl histamine H2: 4-methyl histamine H3: alpha-methyl histamine
49
Betazole used in?
H1 analogue Meniere’s Disease
50
Pharmacological effects of histamine
Decrease in blood pressure Vasodilation (sometimes vasoconstriction) Increase PGI2 secretion Increase in capillary permeability Lewis’ triple response: edema, flare and urticaria Increases leukocyte infiltration to the tissues during inflammation. Contracts uterus smooth muscle Increases gastric acid secretion via H2 receptor stimulation.
51
Role of histamine in endogenous pathological situations
Systemic or local reaction Allergic reactions due to physical factors Drug mediated allergic reactions Histamine mediated headache Mast cell or basophil tumors Peptic ulcer Prutitus,flare,pain sensation Tissue proliferation and repair H1 involved in awakefulness
52
Serotonin formed from
Tryptophan— tryptophan hydroxylase— 5-hydroxytryptophan— l-aromatic acid decarboxylase— serotonin
53
Serotonin present in
Enteric NS Thrombocytes Enterokromaffin cells (APUD cells)
54
Serotonin receptor subtypes
5-HT1a— regulation of sleep 5-HT1b 5-HTm 5-HT2a 5-HT2b 5-HT2c 5-HT3—should not used in pregnant women 5-HT4 5-HT6 5-HT7
55
Pharmacological effects of serotonine
Produces severe vasoconstriction Migraine Renal vessels are sensitive to serotonin Decrease cardiac rate suddenly Stimulates respiration but the bronchi are not sensitive to serotonine Increases peristaltic movements in small intestine Mediates pain sensation Initiates emesis Dumping syndrome
56
Kinins produced from
Prekallikrein— activated haegeman— kaliikrein Kallikrein converts Kininogens to Kinins
57
Pharmacological effects of Kinins
Dilation of arterioles Constriction of venules Contracts intestinal muscles Stimulate pain receptor in the tissues B1 and B2 receptors. Tachykinins and bradykinins
58
Which drug inhibits kallikrein
Aprotinin
59
Endothelia secreted from where and how?
Vascular endothelium Synthesized as pre-pro-endothelin Endothelia-1— Endothelin-2— Endothelin-3
60
Receptors of Endothelin
ETa ETb
61
Antagonist of endothelin receptor
Bosentan— pulmonary hypertension
62
Pharmacological effects of endothelins
Vasoconstriction Renal vascular bed is very sensitive endothelins Bronchoconstriction occurs Mito genie activity occurs In hypertension,myocardial infraction, pulmonary hypertension, chronic renal failure— ET-1 increases ET-1 RECEPTOR ANTAGONISTS DO NOT DECREASE THE VASCULAR TONUS
63
Features of Urotensin-2
Strongest vasoconstrictor Effect on BV May help to depression
64
NO synthesized from?
L-arginine by nitric oxide synthase
65
Forms of Nitric Oxide Synthase
NNOS ENOS Both constitutive INOS is Inducible NOS
66
NOS inhibitor
L-NAME
67
How does NO causes vasodilation in vascular smooth muscles?
NO binds to Guanylate Cyclase and cGMP is formed CGMP deactivates MLCK MLCK cannot phosphorylated MLC Myosin and actin cannot combine to form the contracted muscle filaments
68
Clinical implications of NO system
Hypertension Atherosclerosis Immune system Excitotoxicity, ischemia Neurotransmitter release Impotence
69
Features of Neurotensin
Acts as a neuromodilator of neurotransmitter Vasodilation Increased vascular permeability Anterior pituitary hormones Hyperglycemia Inhibition of gastric acid 3 types of receptors Therapeutic potential in Parkinson’s and schizophrenia

Pharmacology (6 decks)

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