Sedatives / Tranquilizers Flashcards

(98 cards)

1
Q

Drugs acting on the CNS

A

Sedative & Tranquilizers - Alpha 2 agonists & antagonists - Opioids - Injectable anesthetics - Inhalant anesthetics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Tranquilizer aka..

A

Neuroleptic, anxiolytic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Tranquilizer effects

A

Induces state of behavioral change, anxiety relieved, patient is relaxed & aware of surroundings

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Sedative

A

CNS depression & drowsiness, decreased awareness of surroundings

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Hypnotic

A

Induces sleep

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Narcotic

A

Induces stupor bordering general anesthesia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Local/Regional anesthesia

A

Loss of sensation to a circumscribed body area

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

General anesthesia

A

Drug-induced unconsciousness with controlled, reversible CNS depression & analgesia. Patient cannot be aroused. Sensory, motor and autonomic reflexes reduced

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Dissociative anesthesia

A

Dissociate thalamacortic & limbic systems. Catatonic state with open eyes & swallowing reflexes remain functional. Skeletal muscles maintain tone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

4 parts of pain pathway

A

Transduction - Transmission - Modulation - Perception

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Transduction

A

Nociceptive Input (turn physical stimulus into electrical signal for nerves) - PGs, Substance P, K+, Bradykinin, increase peripheral sensitization (when light touch feels painful)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Transmission

A

Afferent nerve: A-delta fibers (sharp pain) & C fibers (dull pain)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Modulation

A

To spinal cord via Dorsal Horn - Enhanced/Diminished depending on neurotransmitters & drugs - “Spinal cord windup” at this level (sensitization of nerves)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Perception

A

In cerebral cortex - Experience/Be aware of the pain - Somatic=bones/muscles/joints

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Excitatory neurotransmitters

A

Glutamate (NMDA receptor) & ACH (acetylcholine)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Inhibitory neurotransmitters

A

GABA - Glycine (spinal cord)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Neurotransmitters metabolized by MAO

A

MAO=Monoamine Oxidase - Dopamine, NE, 5-HT (serotonin), Histamine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Goals of sedative use

A

What is signalment of patient? What is temperament of patient? What is the goal of drug use? Medical conditions/other drugs to consider?

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Phenothiazines -Drug list

A

Acepromazine - *Proclorperazine - *Chlorpromazine - *Trimeprazine w/prenisolone - Promethazine - Ethylisobutrazine - Triflupromazine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Phenothiazine uses

A

Sedative - Premed - Antiemetic - Antihistamine - Antipsychotic (human)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Phenothiazine mechanism

A

Block dopamine receptors in CNS!! (also- block H1/ A1/ ACH-muscarinic receptors)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Phenothiazine effects overview

A

Sedation - Some muscle relaxation - No analgesia - Hypotension & minimal effects on respiration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Phenothiazine Effects on CNS

A

Emotional quieting - Sedation - Decreased spontaneous motor activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Which Phenothiazines have less of a sedative effect?

A

Prochlorperazine / Chlorpromazine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
What can large doses of Phenothiazine cause
Extrapyramidal signs (rigidity, tremors, akinesia)
26
Other CNS mediated effects of Phenothiazine
Hypothermia (hypothalamus) - Antiemetic (CRTZ) - Hyperprolactinemia (hypothalamus)
27
Phenothiazine effects on ANS
Blocks Alpha-1 receptors - Weak anti-cholinergic (block M receptors)
28
Phenothiazine blocking Alpha 1
Vasodilation --> hypotension - "Epinephrine reversal" (Block A1, epinephrine still promoting vasodilation. It's vasoconstrictive effects are blocked)
29
Phenothiazine anticholinergic efect
Not usually clinically significant - Decreased tear production in cats & rabbits
30
Phenothiazine CV effects
Hypotension - Bradycardia - Anti-arrhythmic
31
Which dog breed is more susceptible to Phenothiazine
Boxers sensitive to CV effects
32
Phenothiazine Respiratory effects
Minimal @ therapeutic doses (may decrease rate, not oxygenation) - Depression possible @high doses or used with opioids (&other respiratory depressants)
33
Phenothiazine effects at skeletal muscle
Moderate muscle relaxation
34
Phenothiazine other effects
Reduced hematocrit (splenic sequestration) - H1 antagonist/ Antihistamine - Reduced platelet function - ADH inhibition causing mild diuresis? - Hyperglycemia? - Hyperprolactinemia?
35
Phenothiazine reduced platelet function
In vitro hanges in platelet aggregation - Not demonstrated with acepromazine in healthy dogs in vivo
36
Phenothiazine Administration
IV, IM, SQ, PO
37
Phenothiazine PO
Oral bioavailability low (~20%)
38
Phenothiazine bound in plasma?
Highly protein bound, unclear clinical significance when % varies
39
Phenothiazine distribution
High Vd - well distributed, crosses BBB into CNS
40
Phenothiazine Metabolism
In liver
41
Phenothiazine excretion
Metabolites excreted in urine
42
Phenothiazine duration of action variables
Depends on route of admin, species, breed, etc
43
Phenothiazine clinical uses
Preanesthetic (usually with opioids) - Tranquilizer - Chemical restraint - Antiemesis (motion sickness) - Antihistamine
44
Which Phenothiazines are used for antiemesis?
Chlorpromazine & Prochlorperazine
45
Phenothiazine Cautions
Boxer dogs sensitive - Stallions get penile prolapse & paraphimosis - MDR1 mutants have more, prolonged sedation - Aggressive dogs startle more easily & CNS stimulation sometimes (reduced sedative effect in excited patients)
46
Phenothiazine vasodilation contraindications
DON'T use if vasodilation is contraindicated (Cardiac dz, hypovolemia, dehydration etc)
47
Phenothiazine Toxin contraindication
Tetanus, strychnine, etc because of extrapyramidal effects
48
Phenothiazine contraindication in cattle
Not approved in food animals, ruminal regurgitation sometimes seen
49
Phenothiazine Other contraindications
Liver disease - concurrent Epinephrine dosing - epidurals
50
Drug interactions with acepromazine
Epinephrine/ephedrine - Other CNS depressants - Metoclopramide (& others that cause extrapyrimidal signs) - Cholinesterase inhibitors - Emetics - Opiates - Misc. other drugs
51
Miscellaneous other drugs that interact with acepromazine
Dopamine, phenytoin, procaine, propanolol, quinidine, antacids, acetaminophen, antidiarrheals
52
Butyrophenones main action
Dopamine antagonist!!
53
Butyrophenone dopamine antagonist effects
Antipsychotics in human med - Declining use in vet med - Very similar to phenothiazines (vasodilation, minimal analgesia, paraphimosis in boars) - No approved products in US
54
Azaperone / Stresnil
Labeled for IM in UK swine (reduce aggression during group mixing, control sow aggression) A in BAM (darting wild ungulates)
55
BAM
Butorphanol- Azaperone - Medetomidine - used for darting wild ungulates
56
Haloperidol
To birds for feather picking
57
Benzodiazepines - 3 categories
Agonists - Antagonist - Inverse agonist
58
Benzodiazepine - Agonists
*Diazepam (valium) - *Midazolam - *Alprazolam (xanax) - Lorazepam (ativan) - Oxazepam - Clonazepam - *Zolazepam/Tiletamine (telazol)
59
Benzodiazepine - antagonist
Flumazenil (romazicon)
60
Benzodiazepine - Inverse agonist
B-carboline
61
Review! Agonist/Inverse Agonist / Antagonist
Agonist (binds & causes effect of usual ligand) - Inverse Agonist (binds & causes opposite effect of agonist) - Antagonist (binds and does nothing but block, "neutral agonist")
62
Benzodiazepine mechanism of action
Bind site on GABAa receptors (Cl- channels) --> hyperpolarization of neurons
63
Benzodiazepine Overview of pharmacological effects
Some Sedation - Good Muscle relaxation - No Analgesia - Minimal Cardiorespiratory effects - Anticonvulsant - Appetite stimulant (unk mechanism)
64
Benzodiazepine CNS effects
Sedative-hypnotic (mild) - Anxiolytic - Centrally mediated muscle relaxation (supraspinal GABA) - Anticonvulsant -
65
Benzodiazepine CV & respiration effects
Minimal at therapeutic doses - Depression seen at larger doses
66
Benzodiazepine clinical uses
Anxiolytics/behavior modifier - Anticonvulsants (emergency seizure treatment) - Preanesthetic (in combo) - Sedation in ruminants - Muscle relaxation (anesthesia, urinary) - appetite stimulation
67
Benzodiazepine Administration types
Different products for different routes: Diazepam IV - Midazolam IM - Oral - Transmucosal/intranasal/rectal
68
Diazepam IV administration
Most common route - give slowly to avoid hypotension
69
Midazolam IM
Better IM choice than diazepam
70
Oral benzodiazepines
Generally good oral absorption - Diazepam=short duration - Alprazolam/lorazepam better
71
Problematic Diazepam administrations
Has slow & poor absorption IM & is painful from propylene glycol - Oral=short duration & hepatic necrosis in cats
72
What can oral diazepam cause in cats?
Hepatic necrosis
73
Transmucosal administration of diazepam
Decent bioavailability
74
Benzodiazepine Distribution
Lipid solube - wide distribution - cross BBB - protein bound
75
Benzodiazepine Metabolism
In liver into active metabolites
76
Benzodiazepine excretion
Primarily in urine
77
Benzodiazepine caution in cats
Hepatotoxicity with oral diazepam
78
Benzodiazepine caution in horses
Muscle fasciculations seen, ataxia @higher doses
79
Benzodiazepine benefits
Generally very safe bc lack of CV / respiratory depression (good in very young, old, sick)
80
Benzodiazepine paradoxical excitement
Sometimes seen - usually in combo with other animals or in fear-aggressive animals (disinhibition)
81
Benzodiazepine caution with diazepam injection
Propylene glycol causes pain IM - Hypotension with rapid IV injection - Hemolysis with large IV doses
82
Benzodiazepine caution in pregnancy
Maybe teratogenic (causes birth defects)
83
Benzodiazepine caution in liver/kidney disease
Altered metabolism / excretion
84
Benzodiazepine - Reversal
Flumazenil - Often unneccessary. B-carboline not used clinically
85
Most important phenothiazine for sedation
Acepromazine
86
Acepromazine + opioids = ?
Neuroleptanalgesia for chemical restraint - Or as pre-anesthetic
87
Acepromazine effects
Effective sedation - Some muscle relaxation - No analgesia
88
Acepromazine adverse effects
*Hypotension* - Always use with caution when hypotension is already a risk (*epidurals*)
89
What dog breed is sensitive to Acepromazine?
Boxers - Suffer worse cardiovascular effects
90
What happens to dogs with MDR1 mutations that are given Acepromazine
Have more profound clinical effects - Longer duration
91
What horrifying thing can happen to stallions on acepromazine?
May exhibit paraphimosis (can't put foreskin back over the head) can lead to penile injury #gladIdon'thaveone
92
Trimeprazine Use & formulation
Antihistamine effects - Often combined with prednisolone "Temeril-P" - May see some sedative side effects, but not main use
93
Acepromazine & seizures
Once thought to lower seizure threshold, now thought to pre-dispose patients to them.
94
Butyrophenones Uses
Similar to phenothiazines - Human med: antipsychotic - Use in Vet Med declining
95
Butyrophenones - Name them
Azaperone - Droperidol - Haloperidol
96
Azaperone use
Swine, in UK - Reduce aggression
97
What is BAM?
Butorphanol-Azaperone-Medetomidine for darting wild ungulates
98
Haloperidol uses
Sometimes to control feather-picking in birds (psitticines)