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23 spring: pharm > Test 2: lecture 22 autocoids 1 > Flashcards

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

A

H1

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

A

inhibit

25
Q

fish poinsoning/ bacterial histamine production will causes

A
  • 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
Q

— is a physiologic antagnoist to histamine and will cause rapid bronchodilation

A

epinephrine (EpiPen)

acts on different receptors then H1 which cause constriction

27
Q

— and — will inhibit release of histamine

A

Cromoglicate, nedocromil: asthma treatment (Human).

Beta 2 adrenoreceptor agonists also reduce histamine release

28
Q

side effects of 1st gen H1 receptor antagonists

A

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
Q

— is often used in small animal practice as H1 receptor antagonist; also acts as serotonin/epinephrine reuptake inhibitor (SNRI), so has mild antidepressant properties

A

Chlorpheniramine (diathal)

has less sedating effect then other 1st gen H1 anatgonists (benadryl)

30
Q

what are some second gen H1 receptor antagonists?

A

Cetirizine (Zyrtec®)
Loratadine (Claritin®)

31
Q

why are 2nd gen H1 receptor antagonists less sedative

A

less lipid soluble, can’t get into CNS as easily

Loratadine (Claritin®), Cetirizine (Zyrtec®)

32
Q

H1 receptor antagonists DO NOT block gastric secretion, these are contolled by —

A

H2 receptors

33
Q

H1 receptor antagonists will prevent — in the lungs

A

bronchochonstriction

should use EPI in emergency, then H1 anathonist

34
Q

some — gen H1 antagonist drugs can help with motion sickness / vestibular disturbances / anti-nausea /

A

1st

35
Q

what are some H2 antagonists

A

cimetidine (Tagamet®, prototype)
ranitidine
Famotidine
Pepcid complete
nizatidine

36
Q

H2 blockers can be used to treat

A

decrease release of gastric acid

  • duodenal ulcers
  • uremic gastritis, stress-related erosive gastritis, esophagitis
  • duodenal gastric reflux →prokinetic effects promoting gastric emptying, GI motility

23 spring: pharm (46 decks)

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