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فارما > Autacoids > Flashcards

Autacoids Flashcards

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
Q

1st gen H1 Blockers cause local anesthetic effect

A

Due to blocking of Na+ channel of excitable membrane.

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26
Q

H2-R Antagonist examples:

A

Cimitidine
Rantidine
Famotidine

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27
Q

What are the Ergot Alkaloids?

A

They are produced from fungus that infects grain

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28
Q

Mechanism of action of E.Alkaloids

A

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.

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29
Q

E.Alkaloid effect on serotonin receptors especially:

A

5-HT1A and 5-HT1D

less for 5-HT2 and 5-HT3

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30
Q

Effects of E.Alkaloid on CNS:

A

Powerful hallucingen

Suppress prolactine secretion from pituitary

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31
Q

Why E.alkaloid supress prolactine?

A

Because of stimulatory effect on D-R

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32
Q

Examples of E.Alkaloid that effect on CNS:

A

bromocriptine
pergolide
cabergoline

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33
Q

Effects of E.alkaloid on the Vascular S.M:

A

VC of BV :partial agonist at alpha-R

VC of cerebral BV: by acting on 5HT-2-R (BV)

34
Q

What are the E.alkaloids that effect on Vascular S.M

A

ergotamine
ergonovine
methysergide

35
Q

Which E.alkaloid is more selective than other ergot alkaloids in affecting the uterus?

A

Ergonovine

36
Q

Effects of E.alkaloids on Uterine S.M:

A

causing uterine contraction, vasospasm of uterine blood vessels.
as on vascular S.M, apears to combine alpha agonist, serotonin agonist

37
Q

T or F

No significant effect on bronchial or urinary muscles.

A

T

38
Q

E.Alkaloid induce vomiting due to:

A

Its effect on smooth muscle

Its effect on 5HT-R

39
Q

E.alkaloids effects on S.M

A

GIT—》 nausea, vomiting, diarrhoea.

40
Q

Which E.alkaloid that use in Mograine

A

Ergotamine

41
Q

Ergotamine routes of administration:

A

Oral, inhaler, sublingual, rectal, suppository

42
Q

Ergotamine is often combined with caffeine (100 mg caffeine for each 1 mg ergotamine tartrate)

A

To facilitate absorption of the ergot alkaloid

43
Q

T or F

The vasoconstriction induced by ergotamine is long-lasting and cumulative when the drug is taken repeatedly.

A

T

44
Q

Which E.alkaloids use in Hyperprolactinemia?

A

Bromocriptine

Cabergoline

45
Q

v.v.v.i

Which E.alkaloid use in Postpartum Hemorrhage?

A

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
Q

Which E.alkaloid that use in Diagnosis of variant angina?

A

Methylergometrine
It used to produce prompt vasoconstriction during coronary angiography to diagnose variant angina
Not use now.

47
Q

Which E.alkaloid that use in senile cerebral insufficiency (alzehimer’s dementia) ?

A

Dihydroergotoxine

48
Q

Toxicity of E.alkaloids:

A

1_GIT: N,V,D.
2_Prolong vasospasm—-》gangrene, bowel infarction.
3_Drowsiness
4_C.T proliferation in retroperitoneal space

49
Q

Treatment of prolonged vasospasm caused by E.alkaloid toxicity:

A

Large doses of nitroprusside or nitroglycerine

50
Q

Contraindication of E.alkaloids:

A

Obstructive vascular disease

Collagen disease

51
Q

What are the Eicosanoids?

A

They are Fatty acid derivative that release in inflammation and tissue injury
20 carbon double bound molecules.

52
Q

Name some eicosanoids

A

Prostaglandine
Thromboxane
Leukotrienes

53
Q

How eicosanoids synthesis?

A

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
Q

Phospholipase inhibitors?

A

Corticosteroids

55
Q

Cyclo-oxygenase inhibitors

A 
NSAID
acetylesalicylic acid (aspirin)
56
Q

Lipoxygenase metabolises arachidonic acid to:

A

Leukotrienes

57
Q

Which cox type is ubiquitous?

A

Cox-1

58
Q

Cox-2 is inducible by :

A

Pro-inflammatory stimuli (LPS, TNFalphan IL2, IFNgamma etc)

59
Q

Where cox-2 localizes?

A

Inflammatory and neoplastic sites (small amounts in kidney, uterus, ovary, CNS [neocortex, hippocampus])

60
Q

Why aspirin is contraindicated in peptic ulcer?

A

Aspirin inhibits prostaglandine synthasis which protects mucosal wall thus aggrevating and causing ulceration

61
Q

Role of Cox-2

A

Pro-inflammatory and mitogenic functions (neuronal plasticity)

62
Q

How corticosteroids effect on eicosanoid synthesis?

A

They block all the known pathways of eicosanoid synthesis and inhibit phospholipase A2 activity, thus preventing the release of arachidonic acid.

63
Q

How NSAIDs effect on eicosanoid synthesis?

A

Block both of PG and TX formation by reversibly inhibiting cox activity
Aspirin is an ireversible.

64
Q

5-LOX inhibitor that use for bronchial asthma

A

Zileuton

65
Q

Selective antagonists of receptor for leukotrienes that used clinically in mild to moderate asthma:

A

Zafirlukast
Montelukast
Pranlukast

66
Q

Synthetic preparation of PGE2, is administered vaginally for oxytocic use:

A

Dinoprostone

67
Q

Dinoprostone functions

A

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
Q

Adverse effect of Dinoprostone:

A

Diarrhea

69
Q

Oral oxytocic synthetic analog of PGE1

It prevents of NSAID-induced peptic ulcers

A

Misoprostol

70
Q

Adverse effect of misoprostol

A

Diarrhea

71
Q

An analog of PGF2alpha
used in second trimester abortion
Control postpartum hemorrhage
Second-line treatment for erectile dysfunction

A

Carboprost tromethamine

72
Q

Adverse effect of Carboprost tromethamine:

A

Bronchospasm

73
Q

PGI2 analog

Treatment of Pulmonary hypertension

A

Epoprostenol

74
Q

PGE1
treatment of certain types of congenital heart disease (transposition of the great arteries, pulmonary atresia, pulmonary artery stenosis

A

Alprostadil

75
Q

It is important to maintain the patency of the neonate’s ductus arteriosus until corrective surgery can be carried out.
Which drug?

A

Alprostadil

76
Q

Adverse effects of alprostadil:

A

Penile pain, urethral burning, vaginal itching in partner (locally), dizziness and tachycardia (if absorbed systemically)

77
Q

A stable long-acting PGF2alpha derivative:

A

Latanoprost

78
Q

First prostanoid used for glucoma

A

Latanoprost

79
Q

Other prostanoids used now for glucoma:

A

Bimatoprost

Travoprost

80
Q

Adverse effects of Latanoprost:

A

Gradual change in iris color, keratopathy, comeal erosion (rare)

81
Q

Effects of PGs inhibition

A

Page 16

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