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Pharmacology > Sedative & Hypnotics > Flashcards

Sedative & Hypnotics Flashcards

1
Q

What are the 5 main types of CNS depressants?

A

Alcohol
General anesthetics
Barbiturates
Non - barbiturates
Benzodiazepines

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2
Q

Is ethanol a general CNS depressant w/ full spectrum?

A

Yes
-> from anti - anxiety to anesthesia / death

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3
Q

Where is ethanol absorbed?

A

Stomach
Intestine

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4
Q

Why is ethanol used to treat methanol intoxicated?

A

Compete with methanol for the enzyme
-> Alcohol dehydrogenase

Diuretic
-> promotes excretion of methanol

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5
Q

What are the mechanism of Disulfiram that allows it to be used as treat chronic alcoholism?

A

Disulfiram inhibits aldehyde dehydrogenase
-> increased acetaldehyde conc.
–> causes Acetaldehyde syndrome
—> extremely uncomfortable

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6
Q

Is thio - barbiturates longer acting than oxy - barbiturates in general?

A

No
Generally
-> oxy - barbiturates is longer acting than thio - barbiturates

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7
Q

If oxy - barbiturates is longer acting than thio - barbiturates, does that mean thiopental is shorter acting than methohexital?

A

No
-> Methohexital is kind of an exception

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8
Q

Provide 1 example of barbiturates with ultra short lasting, short lasting and long lasting effects

A

Ultra short lasting
-> Thiopental

Short lasting
-> Pentobarbital

Long lasting
-> Phenobarbital

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9
Q

What is the main function of Thiopental?

A

Anesthesia

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10
Q

What is the main function(s) of Pentobarbital?

A

Anesthetics
Hypnotic
Anticonvulsant

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11
Q

What is the main function(s) of Phenobarbital?

A

Anticonvulsant

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12
Q

What is the main neurotransmitter(s) for Presynaptic inhibition?

A

GABA
-> gamma - aminobutyric acid
–> (G)amma - (A)mino(B)utyric (A)cid

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13
Q

What is the main neurotransmitter(s) for Postsynaptic inhibition?

A

Glycine
Opioids
GABA

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14
Q

What type of channel is GABA(A) receptor?

A

Ligand - gated Cl- channel

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15
Q

How many subunits does GABA(A) receptor have?
What are they?
What could bind to it?

A

5 subunits
-> Alpha x 2
–> binding of GABA molecules for activation

-> Beta x 2
–> binding of Barbiturate

-> Gamma x 1
–> binding of Benzodiazepine

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16
Q

What happens when Barbiturate binds GABA(A) receptor?

A

Increases [Open time] of Cl- channel
High doses
-> directly activate GABA(A)
–> w/ or w/o GABA molecule on Alpha binding site for activation
—> causes CNS depression / death

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17
Q

What happens when Benzodiazepine binds to GABA(A) receptor?

A

Increases [Open frequency] of Cl- channel
Always requires GABA activation
-> does not cause severe CNS depression

18
Q

Is barbiturate a full spectrum drug?

A

Yes

19
Q

What is Therapeutic Index?

A

Ratio of
-> dose of a drug that produces a therapeutic effect
-> dose of a drug that produces toxicity

Equation
Median Lethal dose (LD50)
Therapeutic Index (TI) = —————————————–
Median Effective dose (ED50)

The lower the TI, the harder it is to grasp the amount of drugs needed to produce a therapeutic effect w/o causing toxicity

20
Q

Can phenobarbital be administered orally and still be well absorbed?

A

Yes

21
Q

What are the 3 main clinical uses of Barbiturates?

A

Anesthesia
Anticonvulsant
Euthanasia ( Small lab animals )

22
Q

Is Barbiturate IV anesthesia used for induction or maintenance, or both?

A

Induction only

23
Q

Can barbiturate used for pain control?

A

Nope
-> not analgesic

24
Q

How is Chloral hydrate administered?

A

IV
PO

25
Q

What is chloral hydrate mainly used for for large animals? and why?

A

Pre med
-> reduce dosage needed for anesthesia
-> smoother induction of general anesthesia

26
Q

Is Benzodiazepine full spectrum?

A

Nope
-> non anesthetic
-> at most hypnotic only

27
Q

Does BZD or barbiturate has less acute toxicity?

A

BZD has way less acute toxicity
-> LD50
–> Diazepam > Pentobarbital

28
Q

Which of the following means the same as “ Major tranquilizer “

a) Neuroleptics
b) Antipsychotics
c) Antischizophrenics
d) Benzodiazepine

A

a) Neuroleptics
b) Antipsychotics
c) Antischizophrenics

29
Q

Which of the following are clinical uses of BZD?

a) Insomnia
b) Anxiety disorder
c) Skeletal muscle relaxation
d) Alcohol withdrawal
e) Anticonvulsant
f) Pre med

A

All

30
Q

Is Diazepam long - acting, intermediate - acting or short - acting?

A

Long - acting

31
Q

What effects does it have in dogs & cats and are therefore used as behavior modification drugs?

A

Anxiolytic effects

32
Q

Can both BZD and barbiturate cause addiction?

A

Yes

33
Q

At hypnotic doses, does BZD affect respiration?

A

No

34
Q

Can pregnancy exposure to BZD cause prenatal toxicity?

A

Yes

35
Q

What happens to da babi if early pregnancy exposure to BZD in rodents?

A

Teratogenesis

36
Q

What happens to da babi if late pregnancy exposure to BZD in women?

A

Floppy baby syndrome

37
Q

Could diazepam cause serious hepatic necrosis in dogs due to toxic intermediate metabolites called nordiazepam?

A

No
-> cats though yes

38
Q

What are 3 examples of other drugs whose CNS depressant effect can be potentiated by BZD?

A

Barbiturates
Ethanol
Ketamine

39
Q

What are 4 difference between BZD and barbiturate?

A
  1. In terms of development of tolerance and addiction
    -> Barbiturate > BZD
  2. Barbiturate induces significant drug - drug interaction
    -> Cytochrome P450 induction
  3. Barbiturate could produce life - threatening withdrawal reactions
    -> regular use could lead to dependence
  4. In terms of pharmacological effects on CNS depression
    -> Barbiturate = full spectrum
    –> could cause death
    -> BZD
    –> hypnosis at most
40
Q

Is ‘BZD’ or ‘barbiturate’ in general a safer drug? And if so, in what occasion would we use the non safer drug?

A

BZD is generally a safer drug

Barbiturate is still used
-> Short - acting barbiturate
–> Anesthesia
-> Long - acting barbiturate
–> Anticonvulsant

41
Q

What is the BZD antagonist?
And its mechanism?

A

Flumazenil
-> competes for GABA(A) receptor
–> but no intrinsic efficacy
—> meaning it does not produce a pharmacological effect when bound to the receptor

42
Q

What is the non BZD anxiolytic drug that falls under the category of Azapirones?
And its mechanism?

A

Buspirone
-> Partial agonist 5-HT(1A) receptor
–> No side ( adverse ) effects at all

Pharmacology (5 decks)

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