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Sedatives & Muscle Relaxants Part I SGU SVM Pharmacology I Flashcards | StudBud
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Sedatives & Muscle Relaxants Part I SGU SVM Pharmacology I
Sedatives & Muscle Relaxants Part I SGU SVM Pharmacology I
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Answers
1
Midazolam -- Facts
1/2 life longer in horses
BZDs are not for food-producing animals
No pain on injection
Intense pain on injection
2
Acepromazine maleate -- Route of Administration
SC
Oral
IM
IV
3
Physiological effects of phenothiazines: CVS Effects
Tachycardia
Increase hypotensive effects
Peripheral α1 blocker --> peripheral vasodilation
Acepromazine --> Decrease ventricular arrhythmias
4
Which are Major Tranquilizers?
α2-adrenergic receptor agonists
Butyrophenones
Phenothiazine derivatives
Benzodiazepines
5
Species sensitivity of Phenothiazines
Pigs -> prevent halothane-induced malignant hyperthermia
Horses have an increased tolerance so need a higher dose
Boxer dogs have an exaggerated response to acepromazine
Dogs w/ vagal tone -- Boxers/Bulldogs have greater morbidity or mortality
6
Benzodiazepines -- Clinical Indications
Muscle relaxation and sedation
Anti-anxiety & appetite stimulant
Anticonvulsants in emergencies
Adjuncts to anesthetic induction agents
7
Butyrophenones -- associated drugs -- Which is a sedative for swine and zoo/wildlife medicine?
Droperidol
Azaperone
Fluorone
Haloperidol
8
Flumazenil -- Adverse effects
Emergence delirium
Extravasation of flumazenil --> tissue inflammation + necrosis
Reverse tachycardia
Administration in chronically BZD administrated patients --> seizures
9
Diazepam has a shorter duration of action in dogs & cats when compared to horses
False
True
10
Phenothiazines-- Long acting drugs, how long?
3.1 hrs in horses
7.1 hrs in dogs
3.1 hrs in dogs
7.1 hrs in horses
11
Butyrophenones -- associated drugs which is antiemetic to prevent postoperative nausea and vomiting?
Haloperidol
Fluorone
Droperidol
Azaperone
12
Promazine hydrochloride -- FDA approved in which animals
Food animals
Cats
Horses
Dogs
13
Azaperone -- Route of Administration
IM
IV
Oral
SC
14
Azaperone -- Pharmacodynamic effects -- Respiratory effects
Tachypnea
Mild respiratory depression
Sloughing of tissue near injection site
Respiratory hyperactivity
15
Which are Minor Tranquilizers?
Butyrophenones
Benzodiazepines
Phenothiazine derivatives
α2-adrenergic receptor agonists
16
Diazepam is an appetite stimulant for cats
False
True
17
Benzodiazepines -- Pharmacodynamic effects -- Musculoskeletal effects
Can combine with other anesthetic drugs to mediate muscle relaxation
Hyper activates muscle contractions
Potentiate GABA mediated muscle relaxation at level of spinal cord
Not safe to use in myasthenia gravis patients
18
Azaperone -- Pharmacodynamic effects -- Musculoskeletal effects
Activation
Sloughing of tissue near injection site
Relaxation
No effect
19
Midazolam -- Route of Administration
Intranasal
SC
IM
IV
20
Flumazenil -- what does it actually do
Specifically inhibits binding of benzodiazepines to GABAD receptor
Specifically inhibits binding of benzodiazepines to GABAC receptor
Specifically inhibits binding of benzodiazepines to GABAB receptor
Specifically inhibits binding of benzodiazepines to GABAA receptor
21
Azaperone -- Pharmacodynamic effects -- CNS
Behavior modification -- chemical restraint
Paradoxical excitement in horses (IV)
Sloughing of tissue near injection site
Sedation
22
Phenothiazines -- Which one is commonly used?
Acepromazine
Chlorpromazine
Dipromazine
Promazine
23
Azaperone -- Onset of action
10 mins
>10 mins
<10 mins
24
Zolazepam -- Route of Administration
SC
Oral
IV
IM
25
Benzodiazepines -Respiratory effects - mild, dose-dependent respiratory depression but exaggerated when combined
True
False
26
Acepromazine maleate -- FDA approved in which animals
Horses
Dogs
Cats
Food animals
27
Physiological effects of phenothiazines: Respiratory & Musculoskeletal Effects
Good muscle relaxation, decrease in malignant hyperthermia
Bad muscle relaxation, increase in malignant hyperthermia
Mild respiratory effects; depressed, minute volume remains normal
Huge respiratory effects; depressed, minute volume remains not normal
28
Lorazepam -- Route of Administration
Rectal
IM
IV
Oral
29
Azaperone -- Pharmacodynamic effects -- CVS
Dec blood pressure
Hypotension
Tachycardia
Sloughing of tissue near injection site
30
Sedation causes CNS depression accompanied by drowsiness, but not unconsciousness
False
True
31
Zolazepam -- Route of Administration (Telazol)
IM & IV in dogs
IM & IV in cats
IM only in cats
IM only in dogs
32
BZD - overdose/acute toxicity
Vocalization, tachycardia, tachypnea, hypothermia
Respiratory depression, weakness, tremors
Ataxia/disorientation, CNS depression/agitation
Reversal with BZD antagonist -- Flumazenil
33
Azaperone -- Indications
Anesthetic adjunct
Calming effects to control maternal aggression
Sedative for wildlife
Analgesic effect
34
Azaperone -- Duration of action in pigs
1-4 hrs
2-4hrs
4-5hrs
3-6hrs
35
Flumazenil -- Route of Administration
Sublingual
Rectal in dogs
IM
IV
36
Phenothiazines-- Time to clinical effects
30 mins (IM)
10-15 mins (IV)
30 mins (IV)
10-15 mins (IM)
37
Azaperone -- Peak effect after administration
10 mins
20 mins
40 mins
30 mins
38
Azaperone (Stresnil) -- Used in swine
False
True
39
Benzodiazepines -- Pharmacodynamic effects -CVS -minimal cardiovascular depression; can be given to CVS disease patients
True
False
40
Flumazenil -- pharmacodynamic effects
CNS: reverses EEG changes in dogs/horses
Respiratory: tidal volume & minute ventilation restored to normal
CVS: reversal of fall in blood pressure (cats)
Musculoskeletal: reversal of muscle relaxation
41
Phenothiazines -- Clinical Indications
Pre anesthetic sedative
Decrease anxiety
Sedation & Antiemetic
Combo w/ opioids (Morphine) - neuroleptanalgesia- higher sedation+analgesia
42
Chlorpromazine hydrochlroide -- not recommended in horses due to extreme ataxia and altered mentation
False
True
43
BZDs -- Metabolism
After glucoronide conjugation, excreted in urine
Wide therapeutic index
Liver metabolism -- reduction or glucoronidation
Form active metabolites such as desmethyldiazepam, oxazepam, temazepam
44
Phenothiazine — What kind of drug is it?
Antipsychotic
Minor Tranquilizer
Antiemetic
Major Tranquilizer
45
Chlorpromazine hydrochlroide -- Mainly used as ___ in small animals?
Antipsychotic
Sedation
Antiemetic
Anxiolytic
46
Diazepam -- adverse effects
Kidney failure in cats
Pain on administration by IV/IM --> thrombophlebitis
Hepatic necrosis in cats
Hemolysis (cats)
47
Butyrophenones -- associated drugs
Droperidol
Haloperidol
Fluorone
Azaperone
48
BZDs -- Metabolism
Food producing animals get vertigo
Dogs get renal failure with midazolam
Cats get hepatic failure with diazepam
Horses - midazolam may not produce sedation (paddling, pacing + agitation)
49
Benzodiazepines -- Related drugs
Alprazolam
Midazolam & diazepam
Clonazepam
Zolazepam
50
Diazepam -- Route of Administration
IV
Rectal
IM
Oral
51
Promazine hydrochloride -- Route of Administration (more preferred for this type of administration)
IM
IV
SC
Oral
52
Benzodiazepines -- Pharmacodynamic effects -- CNS
Best sedative effects in neonates, geriatrics or critically ill patients
Sedation in pigs and rabbits > dogs
Paradoxical excitement, agitation, vocalization, & dysphoria
Reduction in cerebral blood flow and in oxygen consumption
53
Phenothiazines-- Is the ability to bind to protein bound high or low?
Low
High
54
Phentothiazines -- Mechanism of Action
Inhibits postsynaptic central dopaminergic receptors (D2)
Antiemetic- D2 anatagonism at CTZ
Peripheral - α1 antagonism - vasodilation
Dopamine receptors-GPCR- signal transduction
55
Phenothiazines -- There is an antagonist to reverse the effects
False
True
56
Physiological effects of phenothiazines: CNS Effects
Extrapyramidal symptoms (rigidity, tremors, amnesia)
Contraindicated for patients with seizures
Sedation (D2 anatagonism)
Decrease spontaneous motor activity
57
Therapeutic targets of sedatives and tranquilizers
NMDA receptor antagonist
α2 receptor agonist
GABA receptor agonist
D2 receptor antagonist
58
Diazepam is a lipid soluble benzodiazepine
True
False
59
Tranquilizers are used for their ability to reduce fear & anxiety & behavioral modification
False
True
60
Acepromazine -- Contraindications
Cautiously used in boxers, brachycephalic dogs, breeding stallions
Hypotension, shock, anemia, Icterus, Seizure history
Dehydrated, hypovolemic, CV disease
Liver disease, coagulopathy/thrombocytopenia
61
Which is/are Major Sedatives?
Benzodiazepines
Butyrophenones
Phenothiazine derivatives
α2-adrenergic receptor agonists
62
Butyrophenones -- associated drugs -- which is for antipsychotics
Fluorone
Droperidol
Haloperidol
Azaperone
63
Lorazepam -- Facts
Preferred for epilepsy
No analgesia
Pain on injection
Preferred for hyper anxiety
64
Midazolam is more or less potent than diazepam (True for more, false for less)
False
True
65
Benzodiazepines -- what does it do?
Sedation
Anxiolytic
Ability to cause sleep
Induce labor
66
Zolazepam -- Facts
Related drugs: Tilzolan and Telazol
Telazol is only FDA approved BZD for dogs and cats
Available in combo w/ tiletamine (NMDA antagonist)
Not used often
67
BZD -- Drug Interactions
W/ other CNS depressants -- produces synergistic CNS depressant effects
Dec in metabolism seen w/ co-admin of drugs that inhibit CYP450 enzymes
Increase in BZD metabolism w/ rifampin
Diazepam absorbed by polyvinyl chlroide
68
Diazepam is an induction agent to propofol, ketamine + etomidate
True
False
69
Azaperone -- Pharmacodynamic effects -- Miscellaneous
No analgesia
Thermoregulation - mild reduction in temperature
Sloughing of tissue near injection site
Decrease PCV
70
Azaperone -- Mechanism of action
Histamine antagonism
D1 & α1, antagonism
D2 antagonism
5-Ht antagonism
71
Phenothiazines -- Undergoes hepatic metabolism & excreted in urine
False
True
72
Phenothiazines -- Which are the drugs?
Chlorpromazine
Acepromazine
Promazine
Dipromazine
73
Sedatives and Tranquilizers: Indications
Not to be used in oxen
Chemical restraint
As an adjunct for general anesthesia
To produce calmness (anxiolytic, sedation)
74
Azaperone -- Adverse effects
Nausea, diarrhea
Salivation, sweating, muscle tremors, vocalization (horse)
Extrapyramidal signs tardive dyskinesia, muscle tremors, restlessness
Paraphimosis -- IM causes penile prolapse in boars (vasodilation)
