Ch.34: Antihistamines & Autacoids (Vickroy) Flashcards

1
Q

Name 2 H2 selective blockers

A

ranitidine

famotidine

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2
Q

therapeutic uses of antihistamines

A
  • acute/chronic allergic (anaphylactoid) or hypersensitivity reactions (target H1 receptors)
  • anti-ulcer therapy (target H2)
  • anti-motion sickness (target H1 or H3)
  • sedation-behavioral control (target H1 or H3)
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3
Q

what are autacoids

A

aka local hormones; a diverse group of substances that differ from traditional hormones or transmitters.
-2 main groups: those that are preformed/stored and those that are synthesized in response to stimuli

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4
Q

ex. of preformed autacoid

A

histamine

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5
Q

ex. of synthesized autacoid

A

arachidonic acid metabolites (PGs, LTs, TXs) and polypeptide autacoids

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6
Q

common targets of autacoid actions

A
  • smooth m.
  • secretory cells
  • blood coag components
  • immune system
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7
Q

does histamine cross BBB?

A

no

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8
Q

what is histamine

A

widely distributed highly polar endogenous decarboxylated amino acid stored and released from intracellular granules

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9
Q

2 major histamine pools

A

1) mast cell pool

2) non-mast cell pool (Gi mucosa, CNS neurons, epidermal cells

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10
Q

Which species has widest array of rxns to substances that produce histamine release

A

dogs

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11
Q

release of histamine is called

A

degranulation; contributes to allergic rxns and inflamm.

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12
Q

should pre-treat with anti-histamine when using which drugs?

A
morphine
amphotericin B
polymixin B
anti-cancer agents
succinylcholine (horses)
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13
Q

things that can trigger degranulation

A
  • Ag-Ab complex
  • drugs, toxins
  • elevation of Ca
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14
Q

cromolyn sodium

A

drug that blocks degranulation

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15
Q

non-mast cell pool chars.

A
  • faster turnover of HA stores
  • does NOT contribute to allergic/hypersensitivity rxns
  • insensitive to conventional HA-releasing agents**
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16
Q

H1 receptor locations and functions

A

smooth m. (constricts)
vascular endothelium (vasodilation)
sensory nn. (stimulant)
CNS (excitatory)

17
Q

H2 receptor locations and functions

A

GI tract (increases acid secretion)

18
Q

what are anti-histamines?

A

drugs that competitively block HA receptors (antagonists)

19
Q

can anti-histamines produce CNS effects?

A

Y (depression –> coma)

20
Q

only approved anti-histamine for dogs, cats, horses**

A

doxylamine (NOT for food animal or horses intended for food)

21
Q

Name 4 anti-histamines

A

doxylamine
diphenhydramine
famotidine
ranitidine

22
Q

disadvantage of older anti-histamine agents

A

are relatively non-specific and can act on a wide variety of receptors; can result in adverse effects

23
Q

therapeutic uses of diphenhydramine

A
  • acute allergic rxn
  • prevent anaphylaxis from antineoplastic agents
  • motion sickness, sedation, anti-tussive
  • OP poisoning
24
Q

how is diphenhydramine eliminated?

A

liver

25
Q

contraindications for diphenhydramine use

A
  • aspergillus
  • glaucoma
  • COPD
  • CV dz
26
Q

properties of newer anti-histamine agents

A
  • more selective for H1 receptors
  • more highly charged
  • less lipophilic
  • uncharacterized in most companion animals (not used much in vet med because we usually WANT the CNS/gastro-protective effects)
27
Q

efficacy for motion sickness depends of blockade of which receptors?

A

H1/H3 and/or mACh receptors

28
Q

full treatment of a SEVERE allergic rxn requires:

A
  • Epinephrine**
  • anti-histamines
  • Corticosteroid
  • Fluids, etc.
29
Q

EPI mech. of action in allergic rxn

A

antagonist of histamine actions on bronchiolar smooth m. (beta-2 receptors) and vascular smooth m. (alpha-1 receptors)

30
Q

cat-specific clinical signs (CS) of histamine (HA) release

A
*respiratory and GI signs:*
yawning
coughing
sneezing
labored breathing
31
Q

dog-specific CS of HA release

A

CV signs:
hypotension
white MM
CV collapse

32
Q

universal CS of HA release

A
restlessness
pruritis
anorexia
lacrimation
red/swollen eyes
salivation
33
Q

H1 receptors mediate most of the major detrimentral actions in which systems?

A

the CV system, respiratory, and GI tracts

34
Q

main CV actions of H1 receptors

A
  • relax arteriolar smooth m. via NO release –> dec. BP/shock**
  • increase capillary permeability (fluid loss) –> dec. BP/shock**
35
Q

respiratory actions of H1 receptors

A
  • constriction of bronchiolar smooth m.
  • inc. bronchial secretions
  • sensory n. ending irritation (coughing, sneezing)
  • all of the above lead to POOR VENTILATION*