Test 2: lecture 22 autocoids 1 Flashcards

1
Q

what are two amine derived autacoids

A

histamine
5-Hydroxytryptamine, aka Serotonin

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2
Q

what are two peptide derived autacoids

A

angiotensin
bradykinin

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3
Q

histamine is a major mediator for —

A

inflammation
anaphylaxis
gastric acid
arousal (awake)

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4
Q

where can you find histamine in the body

A

Major storage in specialized vesicles (granules):
* Mast cells (skin, bronchial and intestinal mucosa)
* Basophil granulocytes (blood)
* Enterochromaffin-like cells (stomach mucosa)

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5
Q

how to make histamine

A

histidine (L-histidine decarboxylase)→ histamine

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6
Q

— are antagonists of H1 receptor

A

pyrilamine
Benadryl (diphenhydramine)
Chlorphen… (Diathal)
Claratin, Zyrtec

histamine receptor found in smooth muscle, endothelial cells and CNS

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7
Q

— is a antagonist of H2 receptors

A

ranitidine (zantac)
cimetidine (tagamet)

will cause decreased gastric acid production

Histamine receptor found in gastric parietal cells, cardiac muscle, mast cells and CNS

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8
Q

— is an agonist of H1 receptor

A

2-methyl-histamine

histamine receptor found in smooth muscle, endothelial cells and CNS

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9
Q

— cells in the stomach mucosa can release histamine

A

Enterochromaffin-like cells

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10
Q

histamine can be released in response to —

A
  • Tissue injury/trauma
  • Physical agents: heat, cold, (heart burn from cold water), x-rays, etc.
  • Chemical compounds: (e.g. morphine, tubocurarine
  • Immunological: IgE → allergy and resistance to parasites).
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11
Q

histamine released from mast cells will cause what clinical signs

A

small red spots- local dilation of blood vessels
large red flare
wheal

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12
Q

histamine will — post capillary venules. Will — permeability of endothelium. mediates attraction of — cells and irriates nerve endings

A

dilate

increase- allows for edema/swelling

inflammatory cells ( neutrophils, eosinophils, basophiles, monocytes,
lymphocytes)

cause pain/itching

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13
Q

what antibody does histamine cause allergic reaction

A

IgE

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14
Q

what kind of allergic diseases does mast cells play a role in

A

asthma, eczema, allergic rhinitis, flea allergy dermatitis

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15
Q

anaphylaxis is a large release of histamine which causes

A

systemic vasodilation → shock

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16
Q

which histamine receptor deals with pain and itching

17
Q

which histamine receptor for sleep-wake cycle

A

H1 and/or H3

promotes wakefulness

18
Q

presynaptic H3 receptors will reduce release of — in the brain and peripheral nerves

A

aCh, amines, peptides

19
Q

histamine effects on cardiovascular system

A

will cause vasodilation of aterioles and NO release (which also causes vasodilation) → ↓BP

heart will compinsate by ↑HR

Flushing, sense of warmth, headache (vasodilation)

Urticaria (hives)

20
Q

what will histamine do in the lungs
what is the exception?

A

humans and GP: cause bronchostriction (H1)

histamine is toxic to GP

rabbits and other species: bronchodilation (H2>H1)

21
Q

histamine will do what to the smooth muscle of the GI tract

A

Guinea pigs/Human: contraction of intestinal smooth muscle- H1

Contraction of guinea pig ileum standard bioassay for histamine.

22
Q

histamine will do what to smooth muscle of uterus

A

some species are sensitive and histamine can induce contractions→ abortion

23
Q

which histamine receptor causes activation of gastric parietal(oxyntic) cells to realease gastric acid

A

H2

will cause increases production of pepsin, and intrinsic factor

can block with H2 but not H1 antihistamine drugs

24
Q

H3 agonist will — acid secretion stimulated by food

25
fish poinsoning/ bacterial histamine production will causes
- Flushing - Hypotension - Tachycardia - Headache - Wheals / hives / urticaria - Bronchoconstriction - Gastrointestinal upset Histamine should not be given to asthmatics, patients with active ulcer disease or gastrointestinal bleeding
26
--- is a physiologic antagnoist to histamine and will cause rapid bronchodilation
epinephrine (EpiPen) acts on different receptors then H1 which cause constriction
27
--- and --- will inhibit release of histamine
**Cromoglicate, nedocromil**: asthma treatment (Human). **Beta 2 adrenoreceptor agonists** also reduce histamine release
28
side effects of 1st gen H1 receptor antagonists
drowsiness dry mucous membranes decreased GI motility inhibits muscarinic cholinoreceptor, serotonin, local anaesthetic receptors 1st gen: * Ethanolamines: e.g. diphenhydramine (**Benadryl®**) * Alkylamines: Chlorpheniramine Maleate (diathal) * Ethylaminediamines: e.g. **pyrilamine** (Histall®; H)
29
--- is often used in small animal practice as H1 receptor antagonist; also acts as serotonin/epinephrine reuptake inhibitor (SNRI), so has mild antidepressant properties
Chlorpheniramine (diathal) has less sedating effect then other 1st gen H1 anatgonists (benadryl)
30
what are some second gen H1 receptor antagonists?
Cetirizine (Zyrtec®) Loratadine (Claritin®)
31
why are 2nd gen H1 receptor antagonists less sedative
less lipid soluble, can't get into CNS as easily Loratadine (Claritin®), Cetirizine (Zyrtec®)
32
H1 receptor antagonists DO NOT block gastric secretion, these are contolled by ---
H2 receptors
33
H1 receptor antagonists will prevent --- in the lungs
bronchochonstriction should use EPI in emergency, then H1 anathonist
34
some --- gen H1 antagonist drugs can help with motion sickness / vestibular disturbances / anti-nausea /
1st
35
what are some H2 antagonists
cimetidine (Tagamet®, prototype) ranitidine Famotidine Pepcid complete nizatidine
36
H2 blockers can be used to treat
decrease release of gastric acid - duodenal ulcers - uremic gastritis, stress-related erosive gastritis, esophagitis - duodenal gastric reflux →prokinetic effects promoting gastric emptying, GI motility