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Autacoids Flashcards

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1
Q

Definition of Autacoids

A

They are heterogeneous group of locally acting hormones or inflammatory mediators that apear during inflammation or tissue injury

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2
Q

T or F

Autacoids act systemically

A

F

They do not act systemically

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3
Q

classification of Autacoids

A

Amine autacoid
Lipid-derived autacoid
Peptide autacoid
Other autacoid

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4
Q

Histamine is derived from?

A

Histidine—》Decaboxylase—–》histamine

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5
Q

Where histamine is storage?

A

In mast crll and basophil in a complex with heparin.

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6
Q

Is there histamine in the brain

A

Non mast cell histamine presents in the brain as a neurotransmitter

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7
Q

Histamine is abundant in :

A

GIT mucosa, skin epidermis, lung, brain

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8
Q

When is histamine released?

A 
Type 1 hypersensitivity
Trauma
Snake venom
Basic Drugs: Succinyl choline, atropine, morphine
D-tubocurarin
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9
Q

Fate of histamine

A

Distructed by histaminase.

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10
Q

T or F

Histamine acts on G protein coupled receptor

A

T

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11
Q

What the 4 subtype of histamine receptors?

A

H1—CNS, Smooth muscle, skine
H2—heart, stomach, mast cell
H3—CNS
H4—Immune cells

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12
Q

Action of H1 receptor:

A

+ Ach, glutamate release
Spasmogenic
Triple Response

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13
Q

Action of H2 receptor:

A

+ inotropic
+ Hcl secretion, pepsin, Intrinsic factor
-ve feedback of histamine release

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14
Q

Histamine antagonists

A

1.Physio..: adrenaline
2.Mast cell stabilizer: cromolyn, nedocromil
3.Immunotherapy
H Receptors blockers

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15
Q

How mast cell stabilizers works?

A

They prevent Ca+ entry to mast cell during immune reaction

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16
Q

Why adrenaline is given in anaphylactic shock?

A

It causes bronchodilatation and vasoconstriction.

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17
Q

Which H1-R blockers can cross BBB?

A

First generation: Diphenhydrate, Chlorpheniramine, Promethazine, Cyproheptadine

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18
Q

H1-R blockers classification:

A

1st gen: highly lipid soluble, cross BBB, less potent, short duration and cheap
2nd gen: no CNS effect, more potent, long duration, Expensive

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19
Q

1st gen H1-R blockers can cross BBB

A

Can cause sedation, but in children less than 6 years cause paradoxical excitation and convulsion

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20
Q

1st gen H1-Blockers examples:

A

Diphenhydrate
Chlorpheniramine
Promethazine
Cyproheptadine

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21
Q

2nd gen H1-Blocker examples:

A

Terfenadine
Certizine
Astimazole
Fexofenadine

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22
Q

Why 1st gen H1-blockers have an atropine like action?

A

Due to blocking of muscarinic receptors.

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23
Q

1st gen H1-blockers cause orthostatic hypotension

A

Due to blocking of alpha1 receptors

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24
Q

1st gen H1 blockers increas appetite:

A

Due to Blocking of 5HT

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25
1st gen H1 Blockers cause local anesthetic effect
Due to blocking of Na+ channel of excitable membrane.
26
H2-R Antagonist examples:
Cimitidine Rantidine Famotidine
27
What are the Ergot Alkaloids?
They are produced from fungus that infects grain
28
Mechanism of action of E.Alkaloids
Their effects include agonist, partial agonist, and antagonist action at alpha adrenoceptors and serotonin receptors. And agonist or partial agonist actions at CNS dopamine receptors.
29
E.Alkaloid effect on serotonin receptors especially:
5-HT1A and 5-HT1D | less for 5-HT2 and 5-HT3
30
Effects of E.Alkaloid on CNS:
Powerful hallucingen | Suppress prolactine secretion from pituitary
31
Why E.alkaloid supress prolactine?
Because of stimulatory effect on D-R
32
Examples of E.Alkaloid that effect on CNS:
bromocriptine pergolide cabergoline
33
Effects of E.alkaloid on the Vascular S.M:
VC of BV :partial agonist at alpha-R | VC of cerebral BV: by acting on 5HT-2-R (BV)
34
What are the E.alkaloids that effect on Vascular S.M
ergotamine ergonovine methysergide
35
Which E.alkaloid is more selective than other ergot alkaloids in affecting the uterus?
Ergonovine
36
Effects of E.alkaloids on Uterine S.M:
causing uterine contraction, vasospasm of uterine blood vessels. as on vascular S.M, apears to combine alpha agonist, serotonin agonist
37
T or F | No significant effect on bronchial or urinary muscles.
T
38
E.Alkaloid induce vomiting due to:
Its effect on smooth muscle | Its effect on 5HT-R
39
E.alkaloids effects on S.M
GIT---》 nausea, vomiting, diarrhoea.
40
Which E.alkaloid that use in Mograine
Ergotamine
41
Ergotamine routes of administration:
Oral, inhaler, sublingual, rectal, suppository
42
Ergotamine is often combined with caffeine (100 mg caffeine for each 1 mg ergotamine tartrate)
To facilitate absorption of the ergot alkaloid
43
T or F | The vasoconstriction induced by ergotamine is long-lasting and cumulative when the drug is taken repeatedly.
T
44
Which E.alkaloids use in Hyperprolactinemia?
Bromocriptine | Cabergoline
45
v.v.v.i | Which E.alkaloid use in Postpartum Hemorrhage?
Ergonovine Used only for control of postpartum uterine bleeding and should never be given before delivery It is given at the time of delivery of the placenta or immediately afterward if bleeding is significant.
46
Which E.alkaloid that use in Diagnosis of variant angina?
Methylergometrine It used to produce prompt vasoconstriction during coronary angiography to diagnose variant angina Not use now.
47
Which E.alkaloid that use in senile cerebral insufficiency (alzehimer's dementia) ?
Dihydroergotoxine
48
Toxicity of E.alkaloids:
1_GIT: N,V,D. 2_Prolong vasospasm----》gangrene, bowel infarction. 3_Drowsiness 4_C.T proliferation in retroperitoneal space
49
Treatment of prolonged vasospasm caused by E.alkaloid toxicity:
Large doses of nitroprusside or nitroglycerine
50
Contraindication of E.alkaloids:
Obstructive vascular disease | Collagen disease
51
What are the Eicosanoids?
They are Fatty acid derivative that release in inflammation and tissue injury 20 carbon double bound molecules.
52
Name some eicosanoids
Prostaglandine Thromboxane Leukotrienes
53
How eicosanoids synthesis?
Arachidonic acid is derived from phospholipid of the cell membrane under effect of phospholipase A2, which then further metabolised by cyclo-oxygenase (COX) to prostaglandine and thromboxane.
54
Phospholipase inhibitors?
Corticosteroids
55
Cyclo-oxygenase inhibitors
``` NSAID acetylesalicylic acid (aspirin) ```
56
Lipoxygenase metabolises arachidonic acid to:
Leukotrienes
57
Which cox type is ubiquitous?
Cox-1
58
Cox-2 is inducible by :
Pro-inflammatory stimuli (LPS, TNFalphan IL2, IFNgamma etc)
59
Where cox-2 localizes?
Inflammatory and neoplastic sites (small amounts in kidney, uterus, ovary, CNS [neocortex, hippocampus])
60
Why aspirin is contraindicated in peptic ulcer?
Aspirin inhibits prostaglandine synthasis which protects mucosal wall thus aggrevating and causing ulceration
61
Role of Cox-2
Pro-inflammatory and mitogenic functions (neuronal plasticity)
62
How corticosteroids effect on eicosanoid synthesis?
They block all the known pathways of eicosanoid synthesis and inhibit phospholipase A2 activity, thus preventing the release of arachidonic acid.
63
How NSAIDs effect on eicosanoid synthesis?
Block both of PG and TX formation by reversibly inhibiting cox activity Aspirin is an ireversible.
64
5-LOX inhibitor that use for bronchial asthma
Zileuton
65
Selective antagonists of receptor for leukotrienes that used clinically in mild to moderate asthma:
Zafirlukast Montelukast Pranlukast
66
Synthetic preparation of PGE2, is administered vaginally for oxytocic use:
Dinoprostone
67
Dinoprostone functions
Stimulate of the contraction of the uterus throughout pregnancy. Directly effects the collagenase of the cervix, resulting in softening. it is approved for inducing abortion in the second trimester of pregnancy, for missed abortion and for repening of the cervix for induction of labor in patients at or near term
68
Adverse effect of Dinoprostone:
Diarrhea
69
Oral oxytocic synthetic analog of PGE1 | It prevents of NSAID-induced peptic ulcers
Misoprostol
70
Adverse effect of misoprostol
Diarrhea
71
An analog of PGF2alpha used in second trimester abortion Control postpartum hemorrhage Second-line treatment for erectile dysfunction
Carboprost tromethamine
72
Adverse effect of Carboprost tromethamine:
Bronchospasm
73
PGI2 analog | Treatment of Pulmonary hypertension
Epoprostenol
74
PGE1 treatment of certain types of congenital heart disease (transposition of the great arteries, pulmonary atresia, pulmonary artery stenosis
Alprostadil
75
It is important to maintain the patency of the neonate's ductus arteriosus until corrective surgery can be carried out. Which drug?
Alprostadil
76
Adverse effects of alprostadil:
Penile pain, urethral burning, vaginal itching in partner (locally), dizziness and tachycardia (if absorbed systemically)
77
A stable long-acting PGF2alpha derivative:
Latanoprost
78
First prostanoid used for glucoma
Latanoprost
79
Other prostanoids used now for glucoma:
Bimatoprost | Travoprost
80
Adverse effects of Latanoprost:
Gradual change in iris color, keratopathy, comeal erosion (rare)
81
Effects of PGs inhibition
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