Tranq and sedatives Flashcards
Two major types of sedatives/tranqs
Major (phenothiazines, butyrophenones, alpha-2’s); Minor- benzodiazepinesq
Phenothiazines- MOA
D2 dopaminergic receptor agonist and alpha receptor antagonist in periphery (blocking NE)
Phenothiazines- examples
acepromazine, promazine
Effects of 2 MOAs of phenothiazines
D2 antagonist- sedation/tranq; alpha-2 antagonist - vasodilation
Acepromazine- MOA
D2 antag, alpha2 antag
Acepromazine- uses
Sedation, tranq, anti-emetic, anti-arrhythmic
Acepromazine- SEs
Decreased myocardial contractility, vasodilation and decreased BP, dehydration, coagulopathy
Promazine- route
Inj or oral granules
Acepromazine- contraindications
Boxers (more sensitive), consumptive coagulopathies due to decreased platelet aggregation, hypotension, DCM!!!!!, liver/renal dz
Acepromazine- when to use in horses
Prolong alpha2 like xylazine, reverse alpha2 vasoconstriction
Benzodiazepines- MOA
a1, a1, gamma subunits of GABAa channel to increase GABA affinity and increase chlorine into cell
Benzodiazepines- effects
Sed, anxiolysis, muscle relax, anticonvulsive
Benzodiazepines- examples
diazepam, midazolam, zolazepam
Diazepam- MOA
a1, a1, gamma subunits of GABAa channel to increase GABA affinity and increase chlorine into cell
Diazepam- BBB?
Yes and placenta
Diazepam- route
No IM- pain, hemolysis
Diazepam- metabolism
Hepatic oxidative- nor- and oxa- metabolites
What causes persistent or permanent penile paralysis rarely in horses
Acepromazine
Midazolam- type
Benzo
Midazolam vs diazepam solubility
mid- h20, diaz- lipid
Midazolam vs diazepam advantages
mixes better with other drugs
Midazolam vs diazepam potency and duration
mid more potent, shorter
Midazolam- BBB
Yes, and placenta
Zolazepam- type
Benzo
Zolazepam- uses
Telazol- Anticonvulsant, muscle relaxant
Name a reversal agent for benzo
Flumazenil- benzo antagonist
Name the most potent benzo
Zolazepam
Describe MOA of alpha2agonists (a2A)
Act on sympathetic to mimic NE and EP to decrease NE
a2Ag- examples
Xylazine, detomidine, dexmedetomidine, romididine
Which a2Ag has lowest a2:a1 affinity
Xylazine
What effect does a1 agonism have
possible paradoxical aggression source
What class of drugs exibits reflex bradycardia
a2Ag
Describe a2:a1 affinity
higher ratio- more specific for sedation/tranq
Which drug in which class produces the least ataxia
Romifidine (a2Ag)
What is the most selective a2Ag
dexmedetomidine
Which a2Ag has highest HR and CO
dexmedetomidine
Which a2Ag has the longest duration of action
Detomidine (horses and cats)
What are the reversal drugs for a2Ag and what is their MOA
a2Antag’s : tolazoline, yohimbine, atipamezole
What kind of reversals are each of the a2Antags
Tolazoline and yohimbine are non-selective; atipamezole is selective for alpha2
Reverse xylazine
Yohimbine or tolazoline
Reverse dexmedetomidine
Atepamezole
Flumazenil- MOA
Benzo receptor antagonist- competitive; reversal for benzodiazepines