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Pharmacology > Ch.19: Sedatives and Tranquilizers (Pablo) > Flashcards

Ch.19: Sedatives and Tranquilizers (Pablo) Flashcards

1
Q

Name 3 phenothiazines

A

acepromazine
promazine
chlorpromazine

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2
Q

Phenothiazine mech. of action

A
  • inhibit DA receptors in CNS–> sedation and tranquilization
  • block NE at alpha-adrenergic receptors in periphery
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3
Q

What kind of receptors are DA receptors?

A

G-protein coupled

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4
Q

phenothiazine indications

A
  • sedation/tranquil.

- prevention of nausea and vomiting

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5
Q

other phenothiazine PK effects

A
  • may see rigidity with high doses
  • may lower seizure threshold***
  • peripheral vasodilation
  • splenic engorgement
  • decreased afterload
  • low effect on motor activity
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6
Q

Why is Ace not safe for Boxers?

A

can result in bradycardia dn hypertension

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7
Q

Important contraindication for Ace***

A

can lower seizure threshold

-caution with horses and boxers

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8
Q

primary use of chlorpromazine

A

antiemetic in D/C

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9
Q

Ace available in what admin routes?

A

IV, IM, SC, oral

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10
Q

phenothiazines have low/high therapeutic index

A

very high when used in NONanesthetized animals (lowered during anesthesia)

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11
Q

contraindicatons of phenothiazines

A
  • dehydration
  • hypovolemia (dec. blood volume)
  • bleeding
  • coagulopathies
  • shock
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12
Q

3 major effects of alpha-2 agonists***

A

sedation
analgesia
master relaxation

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13
Q

basic structure of alpha-2 agonists

A

benzene ring with imidazole ring (exception = xylazine, which has a benzene + thiazole ring)

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14
Q

Name 6 alpha-2 agonists

A 
xylazine
detomidine
medetomidine
dexmedetomidine
romifidine
clonidine
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15
Q

most arrhythmogenic a2 agonist?**

A

xylazine (due to presence of thiazole ring)

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16
Q

mech. of action of a2 agonists (3 main parts)

A
  • mimic the action of NE, therefore inhibiting further release of NE –> sedation
  • also stimulates a1 receptor, which can result in adverse effects
  • imidazoline receptor stimulation –> mediates hyptoension, antiarrhythmogenesis. Not involved in sedation
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17
Q

notable feature of promazine

A

similar to acepromazine. popular use as oral med

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18
Q

Why do you want a2 agonist with high a2 selectivity and low a1 stimulation (high a2:a1 ratio)

A

will be more selective for sedation/analgesic effects and less adverse effects

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19
Q

Xylazine has high/low a2:a1 ratio***

A

low! It is the least potent and has more neg. side effects

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20
Q

most specific alpha-2 agonist that we use***

A

dexmedetomidine (even though medetomidine is even more specific)

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21
Q

Does xylazine have imidazoline receptor stimulation activity?

A

No, b/c it doesn’t have an imidazole ring

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22
Q

Indications for alpha-2 agonists

A
  • sedation
  • chem. restraint
  • preanesthetic
  • analgesia
  • emesis
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23
Q

CNS effects of alpha-2 agonists

A
  • profound sedation via locus coeruleus stim.
  • paradoxical excitement possible in less specific a2 agonists
  • anesthetic sparing effect
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24
Q

CV effects of alpha-2 agonists***

A

-biphasic response:
Phase 1:
-activation of central a2 receptors –> dec. sympathetic outflow, inc. parasym. tone.
-activation of peripheral a1 and a2 receptors –> vasoconstriction, hypertension, reflex bradycardia
Phase2:
-dec. HR and BP (due to dec. NE), dec. cardiac output
(May see 2nd degree AV block)

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25
Q

effect of combining a2 agonist with anticholinergic agent

A
  • increased risk of dysrhythmia
  • hypertension
  • cardiac output not normalized
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26
Q

Respiratory effects of alpha-2 agonists

A
  • mild resp. depression

- cyanosis

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27
Q

xylazine in sheep

A
  • can result in pulmonary edema and hypoxemia

- pulmonary macrophage activation –> damage endothelium

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28
Q

Musculoskeletal effects of alpha-2 agonists

A
  • muscle relax

- twitch possible if given IV

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29
Q

Gastrointestinal effects of a2 agonits

A
  • xylazine: vomiting

- reduced GI motility, acid secretion

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30
Q

Renal effects of a2 agonists

A
  • diuresis (inhibit ADH, inc. Na excretion)
  • dec. renin
  • dec. bladder capacity
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31
Q

endocrine effects of a2 agonists

A
  • dec. catecholamine lvls

- dec. stress response

32
Q

metabolic effects of a2 agonists

A

-hyperglycemia (due to decreased insulin release)

33
Q

Repro effects of a2 agonists

A

xylazine: premature parturition in cows
myometrial contraction in non-gravid uterus
decreased myometrial contraction at low doses only

34
Q

thermoregulation effects of a2 agonists

A

-dec. body temp

35
Q

a2 agonists help/hurt equine recovery from inhalation anesthesia

A

help

36
Q

a2 agonists and analgesia

A

-profound analgesia

37
Q

first a2 agonist used in vet med

A

xylazine

38
Q

which animals are sensitive to sedative effects of xylazine?

A

cattle, ruminants

39
Q

Why do different species have different sensitivity to xylazine

A

differences in G-protein signaling pathways

40
Q

important chars. of detomidine*

A
  • approved in horses**
  • longest duration of action**
  • higher a2:a1 ratio than xylazine
41
Q

important chars. of medetomidine*

A
  • can be used to tx emergence delirium in SA following anesthesia**
  • provides sedation, anxiolysis, analgesia
42
Q

important chars. of dexmedetomidine

A

-similar to medetomidine, but w/ higher HR/CO

43
Q

chars. of Romifidine*

A
  • produces less ataxia in horses than xylazine**

- longer duration of sedation than xylazine

44
Q

chars. of clonidine*

A
  • older human agent**

- not used in vet med

45
Q

adverse effects of a2 agonists

A
  • sudden arousal from sedation
  • vomiting
  • hyperglycemia
  • diuresis
46
Q

contraindications of a2 agonists

A

poor CO

47
Q

3 a2 antagonists

A

tolazole
yohimbine
atipamezole

48
Q

a2 antag. mech. of action

A

-REVERSAL of sedation, anxiolysis, analgesia, CV changes induced by a2 agonists

49
Q

yohimbine best reverses which drug?**

A

xylazine

50
Q

atipamezole best reverses which drug?**

A

dexmedetomidine and medetomidine

51
Q

tolazoline reverses what?*

A

xylazine in cattle and SR

52
Q

list yohimbine, tolazoline, and atipamezole in order of increasing selectiving for a2 receptors

A

tolazoline < yohimbine < atipamezole

53
Q

adverse effects of a2 antagonists

A
  • CNS excitement
  • vasodilation
  • tachycardia
  • CV collapse
  • delirium, aggression
54
Q

Benzodiazepine mech. of action

A

-enhance GABA receptor –> Cl channel opening –> hyperpolarization –> sedation

55
Q

indications of benzos*

A
  • preanesthetic
  • anticonvulsant
  • m. relaxant
  • phobia
56
Q

CNS effects of benzos*

A
  • paradoxical excitement**
  • dec. cerebral blood flow/O2 consumption
  • anticonvulsant
57
Q

CV effects of benzos*

A
  • minimal CV depression at clinical doses**

- high doses –> dec. MAP, inc. CO

58
Q

Resp. effects of benzos*

A

-mild resp. depression

59
Q

MS effects of benzos

A
  • m. relax
  • ataxia
  • can cause agitation in horses
60
Q

T/F: benzodiazepines can cause pain on admin*

A

T (due to propylene glycol vehicle)

61
Q

Do benzos cause analgesia?

A

NO

62
Q

Diazepam vs. midazolam***

A
  • diazepam is lipid soluble, short duration of action, w/ unpredictable absorption IM or SC, can be given rectally.
  • midazolam has ~2x potency of diazepam*, is water soluble due to presence of imidazole ring, has reliable bioavailability IM, IV, SC, has faster onset, and can be given nasally.
63
Q

potency and duration of lorazepam vs. diazepam

A

lorazepam 10x more potent, and longer duration of action than diazepam

64
Q

chars. of zolazepam*

A
  • similar to diazepam
  • only used in combo with tiletamine
  • cats recover slower and calmer than dogs
65
Q

benzo adverse effects

A
  • agitation, vocalization, aggression
  • hepatic failure in cats following repeated oral admin.
  • abstinence syndrome (tremors, etc.) w/ sudden stoppage of tx
66
Q

signs of benzo overdose

A
  • ataxia
  • depression
  • agitation
  • GI upset
  • weakness
  • tremors
  • vocal
  • tachycardia/pnea
  • hypothermia
67
Q

benzo antagonist drug

A

flumazenil

68
Q

flumazenil mech. of action

A

-competitively antagonizes benzos on GABA receptor –> prevents hyperpolarization of postsynaptic memb.

69
Q

PD Effects of flumazenil

A
  • reverses electroencephalographic changes of benzos
  • inc. BP
  • inc. minute vent. and tidal volume
70
Q

flumazenil adverse effects

A
  • seizure in chronically tx benzo patients
  • reduced activity in patients w/o benzo
  • inflamm./necrosis when administered perivascularly
  • dysrrhythmia
71
Q

name 2 butyrophenone derivs

A

azaperone and droperidol

72
Q

butyrophenone derivates mech. of action

A

-neuroleptic effect due to antagonism of D-2 receptors

73
Q

Only FDA drug for sedation in pigs***

A

azaperone

74
Q

indications for droperidol use

A
  • antiemetic

- preanesthetic med

75
Q

PD effects of butyrophenone derivs

A

-dec. HR, CO
-dec. Hb due to splenic sequestration of RBCs
-dec. m. tone
NO ANALGESIA**

76
Q

T/F: droperidol used to be in combo with fentanyl

A

T (due to aggressive behavior)

Pharmacology (21 decks)

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