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Pharmacology > 4.1 - Autocoids - Histamine > Flashcards

4.1 - Autocoids - Histamine Flashcards

1
Q

– Local Hormones
– Site of action is within the site of secretion
– Produces virtually by ALL cells

A

Autocoids

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2
Q

Autocoids

A
  • Histamine
  • Serotonin
  • Eicosanoids
  • Bradykinin
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3
Q

Histamine

A
  • Biosynthesis
  • Receptors
  • Location
  • Responses
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4
Q

Biosynthesis

A
  • Precursor
  • Locations
  • Step
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5
Q

Precursor

A

L-histidine

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6
Q

Locations

A
  • Mast cells
  • Basophils
  • Enterochromaffin-like cells
  • CNS
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7
Q

Step

A

L-histidine ➡️1️⃣ Histamine

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8
Q

1️⃣

A

L-histidine decarboxylase

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9
Q

Receptors

A
  • H1
  • H2
  • H3
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10
Q

H1

— Gq linked

A

• Location & Responses

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11
Q

Extravascular SM

bronchial

A

BrochoCONSTRICTION

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12
Q

Vascular SM

BV

A

Vasodilation

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13
Q

Sensory Nerve Endings

A

Pain & Itch

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14
Q 
Endothelial cells
(Lining of blood vesssels)
A

Contraction

— ⬆️ capillary permeability

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15
Q

CNS

A

Stimulation

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16
Q

Triple Response of Lewis

— effects of dermal injection of Histamine

A
  • Red Dot (flush)
  • Localized Swelling (wheal)
  • Spreading erythema (flare)
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17
Q

H2

— Gs linked

A

• Location & Responses

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18
Q

Parietal cells (stomach)
– HCl
– Intrinsic Factor

H I P
– Hydralazine
– Isoniazid
– Procainamide

A

Basal gastric acid secretion

— peak: at night

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19
Q

Mast cells and Basophils

A

Degranulation

– Histamine release

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20
Q

H3

A

Presynaptic (CNS)

— inhibition of Histamine Release

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21
Q

Drugs

A
  • Agonists

* Antagonists

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22
Q

Agonists

A
  • Histamine

* Betahistine

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23
Q

– Pulmonary Function Test

– Determine the adequacy of acid secretion (gastric)

A

Histamine

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24
Q

– H1 agonist
– H3 antagonist
– Mgt of Vertigo

A

Betahistine (Serc®)

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25
Q

Antagonists

A
  • Physiologic

* Pharmacologic

26
Q

Physiologic

A

Epinephrine

– B2 agonist — Dilation

27
Q

Pharmacologic

— Antihistamines

A
  • H1 Antagonists

* H2 Antagonists

28
Q

H1 Antagonists

A
  • 1st Gen

* 2nd Gen

29
Q

1st Gen
— Classical/ Sedating
— Anticholinergic effects

A
  • Ethanolamines
  • Ethylenediamines
  • Piperazines
  • Alkylamines
  • Phenothiazine
  • Piperidine
30
Q

Ethanolamines
— Most sedating ‼️
— Significant anticholinergic effects

A
  • Diphenhydramine
  • Dimenhydrinate
  • Doxylamine
  • Carbinoxamine
31
Q

DOC: Acute Dystonic Crisis (Torticollis)

A

Diphenhydramine

32
Q

Salt of Diphen

A

Dimenhydrinate

33
Q

– Unisom®

– Sleeping Aid

A

Doxylamine

37
Q

Less sedating

A

Cetirizine

38
Q

Anti-motion sickness

A
  • Meclizine

* Cyclizine

39
Q

Components of Alkylamines

A

Components of cold medication

40
Q

Alkylamines

A
  • BromPHENIRAMINE

* ChlorPHENIRAMINE

41
Q

Phenothiazine

A

Promethazine
— Phenergan®
— Anesthetic agent

42
Q

PiperiDINE

A

CyproheptaDINE
— Anti-serotonergic
— Mgt of 5-HY syndrome

43
Q

2nd Gen

— Less sedating/ Non-sedating

A
  • Less Sedating (Piperazines)

* Non-Sedating (Piperidines)

44
Q

Less Sedating (Piperazines)

A
  • Cetirizine

* Levocetorizine

45
Q

Non-sedating (Piperidines)

— For pilots, drivers or workers that requires to be fully awake

A
  • Loratadine
  • Desloratadine
  • Fedofenadines
46
Q

Mgt of allergic reactions

– Prevention and Treatment

A

1st Gen: More effective

47
Q

Mgt of Parkinsonism & EPS

A

– Acute dystonia

Diphenhydramine

48
Q

Sleep Aids

A

– Unisom®
— Diphenhydramine
— Doxylamine

49
Q

Mgt of motion sickness

A
  • Meclizine

* Cyclizine

50
Q

Component of Cold Preparations

A

Alkylamines

51
Q

Anesthetic adjuncts

A

Promethazine

52
Q

Mgt of 5-HT Syndrome

A

Cyproheptadine

53
Q

Mgt of Malignant Hyperthermia

A

Dantrolene

54
Q

Mgt of Neuroleptic Malignant Syndrome

A
  • Bromocriptine

* Dantrolene

55
Q

S/E: H1 Antagonists

A
  • Sedation
  • Anticholinergic effects
  • Cardiotoxicity
56
Q

C/I: H1 Antagonists

A
  • BPH

* Glaucoma

57
Q

H2 Antagonists

A
  • CimeTIDINE — Least potent
  • RaniTIDINE
  • NizaTIDINE
  • FamoTIDINE — Most potent
58
Q

Uses: H2 ANTAGONISTS

A
  • Mgt of GERD
  • Mgt of Acid Peptic Diseases
  • DOC in mgt of acute GI ulcer bleeding
  • Adjuct in the mgt of allergic reactions
59
Q

Mgt of GERD

A

• 1st line: PPIs

— H2 blockers: 60-70%

60
Q

Mgt of acid peptic diseases

A

1st line: PPIs

61
Q

S/E: Cimetidine

A 
– Enzhme inhibition
– Anti-andronergic effects
  - gynecomastia
  - impotence
– ⬆️ prolactin levels (galactorrhea)
62
Q

Uses: H1 Agonists

A
  • Mgt of Allergic Rxns
  • Mgt of Parkinsonism & EPS
  • Sleep Aids
  • Mgt of Motion Sickness
  • Anesthetic Adjunct
  • Mgt of 5-HT
63
Q

Ethylenediamines

A
  • Pyrilamine

* Tripelennamine

64
Q

PiperaZINES

— Less sedating

A
  • Hydroxyzine — Cetirizine
  • Meclizine
  • Cyclizine

Pharmacology (21 decks)

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