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Justin Lyle Cards > Smooth Muscle Histamine > Flashcards

Smooth Muscle Histamine Flashcards

1
Q

what are autacoids

A

biological factors which act like local hormones, have a brief duration and act near the site of synthesis

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2
Q

histamine is a(n) _____________________

A

autacoid

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3
Q

paracrine autacoid

A

effects are mostly localized but large amounts can be produced and moved into circulation

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4
Q

endocrine autacoid effect

A

may have systemic effect by being transported via circulation

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5
Q

endogenous peptides that cause vasoconstriction

A
  1. angiotensin 2. vasopressin 3. endothelins 4. neuropeptide Y 5. urotensin
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6
Q

endogenous peptides that cause vasodilation

A
  1. bradykinins/kinins 2. natriuretic peptides 3. vasoactive intestinal peptides 4. substance P 5. neurotensin 6. calcitonin gene related peptide 7. adrenomedullin
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7
Q

Fx/Activity of histamine

A
  1. allergic and inflammatory rxns 2. anaphylaxis 3. gastric acid secretion (H2) 4. neurotransmitter 5. neuromodulator 6. immune fx via chemotaxis of WBC
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8
Q

histamine is sequestered/bound in granules on _______________ & _____________ cells

A

basophils; mast

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9
Q

mast cell histamine is located in what tissues

A
  1. nose, mouth, feet 2. internal body surfaces 3. blood vessels at pressure points and bifurcations
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10
Q

non-mast cell histamine is found in which tissues

A
  1. brain 2. enterochromaffin-like (ECL) cells
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11
Q

fx of non-mast cell histamine in the brain

A
  1. neuroendocrine control 2. CV regulation 3. thermal and body weight regulation 4. sleep and arousal
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12
Q

fx of non-mast cell histamine in the ECL cells of the fundus of the stomach

A

activates the acid producing parietal cells of the mucosa

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13
Q

release of histamine is mediated by _______________ via negative feedback in skin mast cells and basophils

A

H3

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14
Q

what types of histamine releasing cell is not mediated by H3 negative feedback

A

lung mast cells

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15
Q

_______________ release causes local vasodilation and release of inflammatory mediators (ex. CRP) and Antibodies

A

histamine

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16
Q

_______________ has a chemotactic attraction for inflammatory cells - neutrophils, eosinophils, basophils, monocytes, and lymphocytes

A

histamine

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17
Q

__________________ inhibits the release of lysosome contents and several T&B lymphocytes

A

histamine

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18
Q

rexposure of antigen causes degranulation –> release of histamine and other mediators, this is a ____________________ allergic reaction common with hay fever and urticaria

A

type I

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19
Q

what defines chemical release of histamine

A
  1. non-injury related release of histamine 2. release is triggered by an amine or a drug (morphine)
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20
Q

all histamine receptors are what type of receptor?

A

G-protein coupled (metabotropic)

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21
Q

H1 is similar to what other receptor

A

muscarinic R

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22
Q

H2 is similar to what other receptor

A

5-HT R

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23
Q

H3 & H4 receptors are _______% similar to eachother

A

40

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24
Q

T/F: all histamine receptors have constitutive activity

A

TRUE

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25
Q

T/F: drugs that act on histamine R’s could be an agonist at 1 receptor and an antagonist or reverse antagonist at another

A

TRUE

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26
Q

H1 & H2 receptors are _________-synaptic

A

post

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27
Q

H3 receptors are ____________-synaptic

A

pre

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28
Q

H1 receptors are found in what tissues

A
  1. smooth muscle 2. endothelium 3. brain
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29
Q

H2 receptors are found in what tissues

A
  1. gastric mucosa 2. cardiac muscle 3. mast cells 4. brain
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30
Q

H3 receptors are found where

A
  1. brain 2. myenteric plexus 3. neurons 4. heteroreceptors 5. presynaptic autoreceptors
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31
Q

H4 receptors are found where

A
  1. eosinophils 2. neutrophils 3. CD4 cells
32
Q

Actions of H1 receptors (@ molecular level)

A

increase phophoinositol hydrolysis –> increased IP3 and ICF Ca2+

33
Q

Actions of H2 R (@ molecular level)

A
  1. increase ICF cAMP 2. activates the IP3-DAG cascade (inc ICF Ca and protein kinase C)
34
Q

actions of H3 receptors

A

decrease histamine release

35
Q

actions of H4

A

chemotaxic effects on eosinophils and mast cells

36
Q

histamine receptors are stimulants of sensory nerve endings, especially those that cause ____________ &______________

A

pain; itching

37
Q

which histamine receptor is responsible for the urticarial response, reactions to insects and stings, and signal inspiration and expiration is respiratory neurons

A

H1

38
Q

which histamine receptor(s) are responsible for appetite and satiety

A

H1 and H3

39
Q

which histamine receptor regulates the Neurotransmitter release inthe brain and peripheral tissues (Ach, amine/peptide release)?

A

H3

40
Q

low dose histamine will cause _______ - mediated __________________ effects in the CV system

A

H1; vasodilatory

41
Q

higher dose histamine will cause _____________ - mediated, ____________________

A

H2; cAMP vasodialtion

42
Q

edema is the result of ______________ effects on microcirculation

A

H1

43
Q

CV effects of histamine release

A
  1. decrease in SBP and DBP 2. reflex tachycardia 3. arterial vasodilation –> warmth, flushing, and HA
44
Q

histamine release causes an increase in HR via the _____________ receptor, in response to the decrease in BP

A

H2

45
Q

which histamine is responsible for bronchoconstriction

A

H1

46
Q

T/F: H1 mediated bronchoconstriction is not normally an issue in small doses

A

TRUE

47
Q

H1 stimulation –> bronchoconstriction should be avoided in patients with what dz’s?

A

asthma & cystic fibrosis

48
Q

effects of H1 stimulation on the GI

A
  1. contraction of intestinal smM 2. large doses of Histamine –> diarrhea
49
Q

histamine release –> H2 agonism on _______________ cells –> increase in gastric acid secretion –> increase in ____________,________, & ___________

A

parietal; AC (autacoid); cAMP, ICF Ca

50
Q

what is the “triple response” of histamine

A
  1. red spot (redness 2/2 VD of microcirc) 2. wheal/edema (inflammation 2/2 capillary/venular endothelium separation) 3. flare (itching 2/2 depolarization of sensory nerve ending)
51
Q

dose related effects of histamine release

A
  1. flushing 2. hotn 3. tachycardia 4. wheals 5. bronchoconstriction 6. GI upset
52
Q

what is an example of a physiologic anti-histamine

A

epinephrine

53
Q

how doe physiologic anti-histamines, like epinephrine work?

A

have the opposite effect of histamine on smM but act on different receptors

54
Q

what are some examples of histamine release inhibitors

A
  1. cromolyn 2. nedocromil 3. B2 agonists
55
Q

what is an example of a H1 histamine receptor antagonists

A

diphenhydramine

56
Q

what are examples of H2 receptor antagonist drugs

A
  1. famotidine 2. ranitidine 3. cimetidine
57
Q

T/F: H3 and H4 receptor antagonist drugs are not available for clinical use

A

TRUE

58
Q

MOA of histamine release inhibitors

A
  1. reduce mast cell degranulation resulting from IgE -Ag complex
59
Q

biggest difference between 1st generation and 2nd generation H1 antagonist drugs?

A

2nd generation are non sedating, 1st generation = strong sedating effects

60
Q

meds that are 1st generation H1 antagonists

A
  1. diphenhydramine 2. hydroxyzine (atarax) 3. meclizine 4. chlorpheniramine 5. promethazine
61
Q

meds that are 2nd generation H1 antagonists

A
  1. foxofendadine (allegra) 2. loratidine (claritan) 3. cetirizine (Zyrtec)
62
Q

H1 antagonist meds are absorbed rapidly with peak in __________ hrs and DOA of _____________h

A

1-2; 4-6

63
Q

2nd generation H1 antagonists meds have a duration of action of _____________ hours

A

12-24

64
Q

why do 2nd generation H1 antagonist meds have longer DOA compared to 1st generation

A

decreased lipid solubility with 2nd gen

65
Q

H1 (2nd generation) antagonists are metabolized by the ___________________ liver enzyme

A

CYP3A4

66
Q

MOA of H1 antagonists

A

reversible competitive binding to H1 , negligable effects on H2, little to no effect on H3

67
Q

what are effects of H1 antagonists that are specfic to 1st generation meds

A
  1. sedation 2. anticholinergic effects 3. local anesthetics
68
Q

effects of H1 antagonists (1st and 2nd gen)

A
  1. anti nausea/emesis 2. anti-parkinsonism 3. andreonrectpro blocking
69
Q

toxicity of H1 antagonists

A
  1. excitation and convulsions in children 2. postural hotn 3. allergic response
70
Q

clincial use of H1 antagonists

A
  1. prevention of allergic rxns 2. prevention of motion sickness (1st gen)
71
Q

T/F: H1 antagonist medications are an effective way to treat pregnancy induced morning sickness

A

false; H1 antagonists are teratogenic!

72
Q

what drug category is the first line in the prevention and treatment of allergic rxn’s, especially if given prior to exposure

A

H1 antagonists

73
Q

in the tx of allergic rhinitis (hay fever), H1 antagonists are a 2nd line tx after ______________________

A

corticosteroids

74
Q

purpose of using of H1 antagonists for atopic dermatitis

A

used more for sedation than anti-itch effect, it decreases awarness of itching (due to being so tired)

75
Q

H1 antagonists have no effect on the tx of ________________ & ______________

A

asthma; angioedeam

76
Q

if clinical effectiveness of one group of H1 antagonists decreases over time, how can you combat this?

A

change drug groups to restore effectiveness

Justin Lyle Cards (27 decks)

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