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Pharmacology > Sedative Hypnotics > Flashcards

Sedative Hypnotics Flashcards

1
Q

Define hypnotic

A

Drowsiness, promotes sleep, profound CNS depression

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2
Q

Define catalepsy

A

rigidity of the limbs, unresponsive to environmental stimuli

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3
Q

Define anxiolytic

A

anxiety relieving

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4
Q

Define sedative

A

ability to calm, reduce anxiety, mild depression of cerebral cortex

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5
Q

Define tranquilizer

A

neuroleptic, anxiety reduced w/ no loss of consciousness; hypothalamus and reticular formation fx depression

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6
Q

What is the difference in the mech of action between benzodiazepine and barbiturates?

A

BZ- binds GABA-a, Cl- influx, membrane hyperpolarization, decreased firing, ONLY in PRESENCE OF GABA

Barb- prolongs the duration of Cl- channels opening; inhibits NE, Ach and Glutamate. Does not req GABA

BOTH result in GABAnergic neurotransmission

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7
Q

What are the therapeutic effects of benzodiazepines?

A

anxiolytic, muscle relaxant, sedative-hypnotic

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8
Q

What are the pharmalogical effects of benzodiazepines?

A

dose dependent CNS depression, effects only in presence of GABA

low dose- sedative; high- hypnosis/anesthesia

anterograde amnesia; anti-convulsant

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9
Q

How does benzodiazepine cause muscle relaxation?

A

potentiation of GABAnergic neurotransmission in the spinal cord

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10
Q

What effects does BZ have on cardio, resp tract and uterus?

A

Cardio- collapse at toxic dose, but not significant in healthy animals

resp tract- PR and Tidal Volume minimally affected

uterine- crosses placenta, TERATOGENIC

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11
Q

T/F

Benzodiazepines do not induce CYP-40

A

TRUE

Barbiturates do

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12
Q

What are the 3 benzodiazepine agonists?

A

Diazepam

Midazolam

Zolazepam

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13
Q

Diazepam

A 
long T1/2
crosses BBB
relaxant, tranquilizer, anticonvulsant
minimal effect on cardio/resp
Neuroleptanalgesia
hapatoxic in cats
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14
Q

Midazolam

A

older animals neuroleptanalgesic
more potent than diazepam
water soluble at low pH
IM/IV

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15
Q

Zolazepam

A

telazol- uscle relaxation, exclusively used w/ tiletamine

induction agent

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16
Q

What is teh only BZ antagonist?

A

Flumazenil

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17
Q

Flumazenil

A

only reveral agent
competitive antagonist of GABA receptor
Counteract resp depression associated with IV diazepam
ONLY GIVE IV
must give repetitive doeses, can lead to toxicity
may cause seizures, arrhythmia , dizziness

18
Q

What are barbiturates used for?

A

anesthesia and seizure management

19
Q

Barbiturate activity largely depends on _____

A

lipid solubility

20
Q

Whataare the main 3 barbiturates, their duration of action and major clinical use?

A

Phenobarbital- long acting; seizures

Pentobarbital- short acting, induction, euthaniasia

Thiopental- ultra short; induction, neurosurgical procedures

21
Q

What are the 2 major classes of sedative hypnotics?

A

Phenothiazine derivatives; major tranquilizers

Butyrophenone derivitives

22
Q

What are the major pharm effects of phenothiazines?

A

sedation, antiemetic, anti- arrhythmia, anti histaminergic, hypotensice effect, hypothermic effect

23
Q

What are the 2 major phenothiazines?

A

chlorpromazine

acepromazine

24
Q

What are the 2 major butyrophenones?

A

droperidol

azaperone

25
Q

Droperidol

A

used for surgical neuroleptanalgesia in SA sx

psychomotor depression

26
Q

Azaperone

A

FDA approval for swine
sedative and premedicant
controls aggressive behavior
sedation in pigs prior to transport

27
Q

What is the mech of action of phenothiazines?

A

blockade of post synaptic mesolimbic dopaminergic receptors (D2)

blockade of alpha-1 adrenergic receptors, H1 histaminergic receptors, and serotonin receptors

28
Q

What is the site of action of phenothiazines?

A

basal ganglia, limbic system, thalamus, brain stem, hypothalamus, reticular activating system

29
Q

What effect do phenothiazines have on the CNS?

A

sedation

depression of brain stem and pathways linking to cerebral cortex

diminished arousal motility, decreased motor activity

extrapyramidal symptoms

anitemetic activity in dogs but not cats

30
Q

What are extrapyramidal effects?

A

rigidity, tremors, akinesia

31
Q

What cardiovascualr effects of phenothiazines

A

blocks alpha-1 receptor activation in peripheral vascualture- Net result is vasodilation

32
Q

what is reflex tachycardia?

A

phenothiazines block alpha-1 receptors, cause peripheral vasodialtion, interpreted by baroreceptors as hypotension, tachycardia develops as result

33
Q

What are the respiratort effects of phenothiazines

A

minimal effects

34
Q

What are the dermatological effects of phenothiazines

A

promethazine and trimeprazine block H1

35
Q

T/F phenothiazines produce profound analgesic effects

A

FALSE

they dont do this

36
Q

How do phenothiazines cause hypothermia?

A

depress thermoregualtion of the hypothalamus;

increased heat loss via vasodialtion

decrease heat pdx via decreased muscle activity

37
Q

What are butyrophenones used for?

A

sedative and pre-anesthetic agent

same mech of action as phenothiazines

38
Q

What CNS effects to butyrophenones have?

A

potent antiemetic effects

controls drug induced vomiting

39
Q

What are the cardiopulmonay effects of butyrophenones?

A

mild hypotension due to blockade of peripheral alpha-1 receptors

minimal effects on CO/resp depression compared to phenothiazines

40
Q

Adverse effects associated w/ phenothiazines:

A

accidental intracarotid administration in the horse leads to seizure/death

mimic/similar to clinical signs of organophosphate poisoning - Cholinesterase inhibitor

lower seizure threshold

NO REVERSAL AGENT

Contraindicated in hypovolemic administration

41
Q

Therapeutic uses of phenothiazines/butyrophenones

A

tranquilizers
pre-anesthetic in general anesthesia, allows dose reduction and amelioration of adverse effects associated w/ some anesthetic agents
antiemetics

Pharmacology (9 decks)

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