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Pharmacology: CNS Drugs > Sedative-hypnotics > Flashcards

Sedative-hypnotics Flashcards

1
Q

Define sedative vs hypnotic

A

Sedative = anxiolytic; calms the patient

Hypnotic: promotes drowsiness and sleep

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2
Q

T/F: Sedative-hypnotics (SH) are lipid soluble

A

True. This allows them to cross BBB

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3
Q

Sedative-hypnotics are absorbed in ____

A

GIT

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4
Q

How are the CNS effects of sedative-hypnotics terminated?

A

by rapid REDISTRIBUTION of the drug from
brain to other highly perfused tissues

the higher rate of drug redistribution, the less its effect

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5
Q

All BDZs are absorbed completely, except

A

clorazepate

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6
Q

decarboxylated rapidly in gastric juice to N-desmethyldiazepam

A

nordiazepam

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7
Q

How are sedative-hypnotics metabolized?

A

via hepatic metabolism

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8
Q

Give examples of drugs that are converted initially to active metabolites with long half-lives

A

diazepam, flurazepam

Diazepam(28hrs) to Nordiazepam(60hrs) to Oxazepam(6hrs)

Flurazepam (2hrs) to N-desalkylflurazepam (50hours)

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9
Q

Undergo extrahepatic metabolism, and therefore do not form active metabolites

A

Lorazepam , tamezapam, and oxazepam

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10
Q

Main classes of drugs in sedative-hypnotics

A

Benzodiazepines

Barbiturates

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11
Q

Barbiturates are extensively metabolized Except

A

phenobarbital

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12
Q

Arrange the SH drugs in sequence based on increasing duration of action

A

zaleplon

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13
Q

It is a non-BDZ with biphasic release form

A

zolpidem

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14
Q

Examples of long-acting SH

A

chlordiazepoxide, clorazepate, diazepam, phenobarbital

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15
Q

Site of action of BDZ and barbiturates

A

GABA A receptor

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16
Q

Differentiate GABA A vs GABA B receptor

A

GABA A activation: ↑ Cl- influx; Ionotropic (fast)
GABA B activation: ↑ K+ efflux Metabotropic (slow)

Both mechanisms result in membrane hyperpolarization

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17
Q

GABA A receptor has how many subunits

A

5 subunits
o 4 transmembrane domains
o 2 α1, 2 β2, and 1 γ2 subunits

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18
Q

binding site for benzodiazepines is

A

between an α1 and the γ2

subunit

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19
Q

BDZ vs Barbiturates based on mechanism of action on GABA A receptor

A

BOTH increase the potency of GABA but by different mechanisms:

BDZ: increased FREQUENCY of opening of GABA receptor
Barb: increased DURATION of opening of GABA receptor

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20
Q

Is it okay to combine BDZ and Barbiturate?

A

No. they could have ADDITIVE effects. They can both stimulate the receptor. DO NOT MIX THESE DRUGS TOGETHER.

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21
Q

Antagonist of BDZ

A

Flumazenil

hence used as antidote for BDZ poisoning

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22
Q

Which has GABA-mimetic activity?

A

Barbiturates. They can mimic GABA esp at high doses

BDZ has NO GABA-mimetic activity.

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23
Q

Additional MOA of barbs

A

Inhibit complex I of the Electron Transport Chain

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24
Q

Give examples of SH that are neither BDZ or Barb

A

zolpidem, zaleplon, and esZopiclone

Z drugs

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25
Q

Adv of Z drugs

A

Less effect on cognitive function

Less tolerance and abuse liability

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26
Q

Give the dose-dependent effects of SH

A

Sedation (lowest dose)
Hypnosis
Anesthesia
Coma (highest dose)

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27
Q

What is paradoxical inhibtion?

A

Its a benzodiazepine induced hyper-reactive phenomenon. It takes the person to the extreme end of emotions, removes all inhibitory and suppressed signals resulting in extreme pychosis and agitation, paranoia and depression. Its a rare occurence in pts taking the drugs.

It is due to inhibition of inhibitory subcortical neurons during initial doses of BZ.

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28
Q

How does SH affect sleep?

A

Reduced REM duration

Increased of Non-REM (Stage II) duration (ex: Diazepam)

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29
Q

Used for anesthesia

A

Thiopental
Midazolam

Anesthesia can be produced by short acting barbiturates (eg,
thiopental) and certain benzodiazepines (eg,midazolam).

30
Q

Can cause anterograde amnesia

A

benzodiazepines

31
Q

Examples of SH with selective anticonvulsant action

A

Phenobarbital

Clonazepam

32
Q

Used in status epilepticus

A

diazepam, lorazepam, or phenobarbital

33
Q

Muscle Relaxation occurs only with high doses of most sedative-hypnotics Except

A

diazepam and Meprobamate (they can be used as muscle relaxant even at low doses)

34
Q

Can cause medullary depression

A

Alcohols and barbiturates

BDZs are safe and rarely cause medullary depression

35
Q

There is cross-tolerance between

A

BZ, barbituates, and ethanol

36
Q

T/F Benzodiazepines are less toxic compared to all sedatives.

A

T

37
Q

DOC for anxiety states

A

Alprazolam and clonazepam

38
Q

DOC for sleep disorders

A

estazolam, flurazepam, and triazolam

39
Q

T/F: Sedative hypnotic drugs recommended for breathing-related
sleep disorders

A

False. Sedative hypnotic drugs NOT recommended for breathing-related
sleep disorders

40
Q

Used for induction of anesthesia

A

thiopental

41
Q

components of anesthesia protocols

A

diazepam, midazolam

42
Q

used for seizure disorders

A

clonazepam, phenobarbital

43
Q

used for bipolar disorcer

A

clonazepam

44
Q

used for muscle spasticity

A

Diazepam

45
Q

used in management of withdrawal states

A

chlordiazepoxide, diazepam

46
Q

benzodiazepines that have active metabolites

with long half-lives

A

DIAZEPAM, FLURAZEPAM

47
Q

Barbiturates: Enzyme inducer or inhibitor?

A

Barbiturates are ENZYME INDUCERS

Mnemonic: PRC
Phenobarbital (barbiturates), phenytoin
Rifampicin
Carbamazepine, Chronic Alcohol use

48
Q

Adverse effect associated with barbiturates

A

Acute intermittent porphyria

49
Q

Mickey Finn is aka

A

Chloral hydrate

50
Q

May displace coumarins from plasma protein

A

chloral hydrate

51
Q

occasionally increases the incidence of nightmares

A

flurazepam

52
Q

Examples of ATYPICAL sedative-hypnotics

A

Buspirone

Ramelteon

53
Q

MOA of buspirone

A

Partial agonist of 5-HT1A serotonin receptors

54
Q

T/F Buspirone affects GABA

A

False. It is partial agonist of 5-HT1A serotonin receptors

55
Q

Use of buspirone

A

anxiolytic ONLY

it has NO anticonvulsant or muscle relaxant properties

56
Q

Disadvantage of using buspirone

A

slow onset of action (>1 week) since it is only partial agonist

57
Q

Advantage of using buspirone

A

Tolerance development is minimal with chronic use
little rebound anxiety or withdrawal symptoms on discontinuance
Minimal abuse

58
Q

Metabolism of buspirone is Increased or decreased by erythromycin?

A

Decreased metabolism (leading to increased plasma levels)

Enzyme inhibitors: MEDVICK-A
Metronidazole
Erythromycin
Valproic acid
Isoniazid
Cimetidine, ciprofloxacin
Ketoconazole
Acute Alcohol use
59
Q

Novel hypnotic drug

A

Ramelteon

60
Q

MOA Ramelteon

A

activates melatonin receptors in the suprachiasmatic nuclei

61
Q

Effect of Rifampin on metabolism of Ramelteon

A

Increased metabolism

ENZYME INDUCERS

Mnemonic: PRC
Phenobarbital (barbiturates), phenytoin
Rifampicin
Carbamazepine, Chronic Alcohol use

62
Q

Effect of fluconazole and fluvoxamine on ramelteon

A

Decreased metabolism
(azoles are enzyme inhibitors)

Enzyme inhibitors: MEDVICK-A
Metronidazole
Erythromycin
Valproic acid
Isoniazid
Cimetidine, ciprofloxacin
Ketoconazole
Acute Alcohol use
63
Q

Which one of the following statements is correct regarding
benzodiazepines?
A. Benzodiazepines directly open chloride
channels.
B. Benzodiazepines show analgesic actions.
C. Clinical improvement of anxiety requires 2 to 4
weeks of treatment with benzodiazepines.
D. All benzodiazepines have some sedative effects.
E. Benzodiazepines, like other CNS depressants,
readily produce general anesthesia.

A

Correct answer = D. Although all benzodiazepines can
cause sedation, the drugs labeled “benzodiazepines” in
Figure 9.1 are promoted for the treatment of sleep disorder.
Benzodiazepines enhance the binding of GABAA to its receptor,
which increases the permeability of chloride. The benzodiazepines
do not relieve pain but may reduce the anxiety
associated with pain. Unlike the tricyclic antidepressants and
the monoamine oxidase inhibitors, the benzodiazepines are
effective within hours of administration. Benzodiazepines do
not produce general anesthesia and, therefore, are relatively
safe drugs with a high therapeutic index.

64
Q 
Which one of the following is a short-acting hypnotic?
A. Phenobarbital.
B. Diazepam.
C. Chlordiazepoxide.
D. Triazolam.
E. Flurazepam.
A

Correct answer = D. Triazolam is a short-acting drug. It has

little dayt

65
Q

Which one of the following statements is correct regarding
the anxiolytic and hypnotic agents?
A. Phenobarbital shows analgesic properties.
B. Diazepam and phenobarbital induce the cytochrome
P450 enzyme system.
C. Phenobarbital is useful in the treatment of acute
intermittent porphyria.
D. Phenobarbital induces respiratory depression, which
is enhanced by the consumption of ethanol.
E. Buspirone has actions similar to those of the
benzodiazepines.

A

Correct answer = D. Barbiturates and ethanol are a potentially
lethal combination. Phenobarbital is unable to alter the
pain threshold. Only phenobarbital strongly induces the synthesis
of the hepatic cytochrome P450 drug-metabolizing
system. Phenobarbital is contraindicated in the treatment of
acute intermittent porphyria. Buspirone lacks the anticonvulsant
and muscle-relaxant properties of the benzodiazepines
and causes only minimal sedation.

66
Q

A 45-year-old man who has been injured in a car accident
is brought into the emergency room. His blood alcohol
level on admission is 275 mg/dL. Hospital records show a
prior hospitalization for alcohol-related seizures. His wife
confirms that he has been drinking heavily for 3 weeks.
What treatment should be provided to the patient if he
goes into withdrawal?
A. None.
B. Lorazepam.
C. Pentobarbital.
D. Phenytoin.
E. Buspirone.

A

Correct answer = B. It is important to treat the seizures
associated with alcohol withdrawal. Benzodiazepines, such
as chlordiazepoxide, diazepam, or the shorter-acting lorazepam,
are effective in controlling this problem. They are less
sedating than pentobarbital or phenytoin.

67
Q 
Which one of the following is a short-acting hypnotic
and better for sleep induction compared to sleep
maintenance?
A. Temazepam.
B. Flurazepam.
C. Zaleplon.
D. Buspirone.
E. Escitalopram.
A

Correct answer = C. Zaleplon has the shortest half-life and
duration of action. Buspirone and escitalopram are not
effective hypnotic agents. Temazepam and flurazepam have
longer durations of action and will reduce nighttime awakenings
but will have a greater risk of daytime sedation or
hangover effect compared to zaleplon.

68
Q

Which of the following agents has a rapid anxiolytic effect
and would be best for the acute management of anxiety?
A. Buspirone.
B. Venlafaxine.
C. Lorazepam.
D. Escitalopram.
E. Duloxetine

A

Correct answer = C. The benzodiazepines have same-dose,
first-dose efficacy for anxiety, whereas the other agents
require 2 to 8 weeks for clinically significant improvement
in anxiety.

69
Q 
Which of the following sedative–hypnotic agents utilizes
melatonin receptor agonism as the mechanism of action
to induce sleep?
A. Zolpidem.
B. Eszopiclone.
C. Estazolam.
D. Ramelteon.
E. Diphenhydramine.
A

Correct answer = D. Ramelteon is the only melatonin receptor
agonist to promote sleep, especially in sleep-phase
disrupted sleep. Zolpidem, eszopiclone, and estazolam all
utilize the benzodiazepine receptor, and diphenhydramine
is a histamine receptor antagonist.

70
Q 
All of the following agents for the management of
insomnia are controlled substances and may have a risk
for addiction or dependence except:
A. Zaleplon.
B. Flurazepam.
C. Doxepin.
D. Zolpidem.
E. Triazolam.
A

Correct answer = C. Only doxepin, a tricyclic agent with
significant antihistaminergic properties, is considered to
have no risk of addiction or dependence, whereas the other
agents listed all have DEA schedule IV designations with
some risk for addiction or dependence, especially when
used for extended periods.

71
Q 
All of the following agents may cause cognitive
impairment, including memory problems when used at
recommended doses except:
A. Diphenhydramine.
B. Zolpidem.
C. Alprazolam.
D. Phenobarbital.
E. Ramelteon.
A

Correct answer = E. All of the above listed agents, except
ramelteon, have been associated with cognitive impairments,
including memory impairment. Diphenhydramine
likely causes its cognitive problems from its anticholinergic
and antihistaminergic effects. Zolpidem, alprazolam, and
phenobarbital are well-known causes of cognitive impairment,
including anterograde amnesia. Ramelteon has
safety data extending to 6 months and is a noncontrolled
hypnotic agent acting as a melatonin receptor agonist. It is
not considered to have a risk for cognitive impairment as
compared to the other agents listed.

72
Q

Which agent is best used in the Emergency Room
setting for patients who are believed to have received
too much of a benzodiazepine drug or taken an
overdose of benzodiazepines?
A. Diazepam.
B. Ramelteon.
C. Flumazenil.
D. Doxepin.
E. Naloxone.

A

Correct answer = C. Flumazenil is only indicated to reverse
the effects of benzodiazepines via antagonizing the benzodiazepine
receptor. It should be used with caution due to a
risk of seizures if the patient has been a long time recipient
of benzodiazepines or if the overdose attempt was with
mixed drugs. Naloxone is an opioid receptor antagonist.
The other agents are not efficacious in reversing effects of
benzodiazepines.

Pharmacology: CNS Drugs (3 decks)

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