Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

House Pharmacology > Sedative and Hypnotics > Flashcards

Sedative and Hypnotics Flashcards

1
Q

SEDATIVES – reduce ______ and exert a ______ effect

HYPNOTICS - produces ______ and facilitates the onset and maintenance of _________________

A

anxiety; calming

drowsiness ;a state of sleep.

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

SEDATIVE/HYPNOTICS ANXIOLYTICS

Major therapeutic use is to relief _______(_______) or induce _______(_______)

A

anxiety (anxiolytics)

sleep (hypnotics).

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

Hypnotic effects can be achieved with most anxiolytic drugs

T/F

A

T

just by increasing the dose.

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

The distinction between a “pathological” and “normal” state of anxiety is easy to draw

T/F

A

F

hard

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

anxiolytics are among the most prescribed substances worldwide.

T/F

A

T

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

Manifestations of anxiety:

Verbal complaints. The patient says he/she is __________________

Somatic and autonomic effects: . The patient is _______ and _______, has ______cardia, _____eased sweating, weeping and often gastrointestinal disorders.

Social effects. Interference with _________________ activities.

A

anxious, nervous, edgy.

restless and agitated; tachycardia, incr

Normal productive

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

Pathological Anxiety

Generalized anxiety disorder (GAD): People suffering from GAD have general symptoms of ————, autonomic ______, etc. for at least ________

A

motor tension; hyperactivity

one month.

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

Pathological Anxiety

Phobic anxiety:
Simple phobias. Agoraphobia, fear of ______, etc. Social phobias.

.

A

animals

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

Pathological Anxiety

Panic disorders: Characterized by (acute or chronic ?) attacks of ___ as compared to the (acute or chronic?) presentation of GAD.

A

Acute ; fear

Chronic

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

Pathological Anxiety

Obsessive-compulsive behaviors: These patients show _________(obsessions) and ___________ (compulsions).

A

repetitive ideas

behaviors

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

Causes of Anxiety

______
_____-induced
Drug ______

A

Medical
Drug-induced
Drug withdrawal

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

Causes of Anxiety
1). Medical:
Respiratory Endocrine Cardiovascular Metabolic Neurologic.

T/F

A

T

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

Causes of Anxiety
2). Drug-Induced:

– Stimulants
_____,_______,_______,_______.

– Sympathomimetics
_______,________,______,________.

– Anticholinergics\Antihistaminergics
________,________,__________,_________

– Dopaminergics
________,________,________,__________

Miscellaneous:
• Baclofen, cycloserine, hallucinogens, indomethacin.

A

Amphetamines, cocaine, TCAs, caffeine

Ephedrine, epinephrine, pseudoephedrine phenylpropanolamine

Trihexyphenidyl, benztropine, meperidine diphenhydramine, oxybutinin.

Amantadine, bromocriptine, L-Dopa, carbid/levodopa.

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

Causes of Anxiety

Drug Withdrawal:
•____,________,_________, other ______,______

A

BDZs, narcotics, BARBs

sedatives, alcohol.

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

Strategy for treatment of anxiety

_______ anxiety without causing ________.

A

Reduce

sedation

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

Anxiolytics

Barbiturates e.g. ________,______,______,_____,_______

Benzodiazepines e.g._______ (Valium), _____ (Versed),_______ (Klonopin) ; ________ (Ormodon), ________ (Rohypnol)

Glutethimide : ____________

A

Methohexitone, Phenobarbital, Pentabarbital, Thiopentone,Thiamylal

Diazepam; Midazolam; Clonazepam

Nitrazepam; Flunitrazepam

Piperidinediones

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

Anxiolytics

Meprobamate : __________ _______

Alcohols : ______,_________,_________

Buspirone : _________

Zolpidem : _____________

Zaleplon : __________

A

Propanediol carbamates

Ethanol, Chloral hydrate, Paraldehyde

Azaspirodecanedione; Imidazopyridine

Pyrazolopyrimidine

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

BARBITURATES
Derivatives of ___________

–Hypnotic/anxiolytic effect discovered in the early 20th century (Veronal®, 1903)
– Until the 60s, it was the largest group of _________

– (low or high?) risk of dependence ((mild or severe?) withdrawal symptoms)

A

barbituric acid

hypnotics; high ; severe

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

BARBITURATES

– (mild or Strong?) depressant activity on the CNS => ________

– At higher doses it causes respiratory and cardiovascular ________ => very little use today as _______ (only for _______ and ________)

A

Strong ; anesthesia

hypnotics

epilepsy and anesthesia

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

Structure-Activity Relationship of Barbiturates

The ________ and ______ forms of barbituric acid with the sites of substitution in the hypnotically active barbiturates

A

keto and enol tautomeric

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

Structure-Activity Relationship of Barbiturates

Substitution at carbon 5 = *_____ activity is introduced

_______ chain >- greater hypnotic activity

______ group (like ________) -> Greater anticonvulsant activity

Presence of ______philic groups decreases lipophilicity so decreases activity

A

Hypnotic; Branched

Phenol; phenobarbital

hydro

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

Benzodiazepines

_____,_______,_______,_____, and _________ properties.

Treatment : _______

At low doses are useful _______ and high doses produce a ________ effect

A

sedative, hypnotic, anti-anxiety, anticonvulsant, and muscle relaxant

anxiety; sedatives; hypnotic

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

Benzodiazepines

Absorption and distribution: ___philic, are (slowly or rapidly?) and (completely or incompletely?) absorbed after _____ administration and distribute throughout the body.

Excreted in the urine as ________ or ______ metabolites.

A

lipo; rapidly ; completely

oral

glucuronides; oxidized

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

Benzodiazepines

Treatment : anxiety

It has (more or less?) side effects, dependence

It is (more or less?) effective

A

Less

More

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

What are the different types of benzodiazepines?

Several types with differences in potency, speed at which they are metabolized, and “half-life” and therapeutic use.

Vary mostly in their ________

A

duration of action

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Benzodiazepines

A substituent in the position _____, such as a _______, or ________ group, is required for sedative-hypnotic activity

A

7

halogen or a nitro

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

benzodiazepines

List 4

A

Clonazepam

Diazepam

Lorazepam

Flunitrazepam

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Anxiolytics

_______ (BZDs).
___________ (BARBs).
_________ receptor agonists.
_____,______, and ______ receptor
antagonists.

If ANS symptoms are prominent:

_______________ antagonists.
_________ agonists (clonidine).

A

Benzodiazepines (BZDs).
Barbiturates (BARBs).
5-HT1A receptor agonists.
5-HT2A, 5-HT2C & 5-HT3 receptor
antagonists.

ß-Adrenoreceptor
Alpha2-AR

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

Anxiolytics
Other Drugs with anxiolytic activity.

–_____(_______). Used for Obsessive compulsive Disorder.
–________. Used in panic attacks.
– Anti_____ agents. Present in over the counter medications.
– Anti________ (Ziprasidone).

A

TCAs (Fluvoxamine)

MAOIs; histaminic

psychotics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Anxiolytics
Other Drugs with anxiolytic activity.

Novel drugs. (Most of these are still on clinical trials).
-_____ (e.g. CCK4).
–______/_______ (e.g. HA966).

A

CCKB

EAA’s/NMDA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

Anxiolytics
Other Drugs with anxiolytic activity.
– TCAs (Fluvoxamine). Used for ________________

– MAOIs. Used in _______

A

Obsessive compulsive Disorder.

panic attacks.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

Sedative/Hypnotics

A hypnotic should produce, as much as possible, a state of _____ that resembles _______

A

sleep

normal sleep.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

Sedative/Hypnosis

By definition all sedative/hypnotics will induce sleep at _____ doses.

Normal sleep consists of distinct stages, based on three physiologic measures: ____________gram, ______gram, ____________gram.

A

high

electroencephalo; electromyo

electronystagmo

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

Sedative/Hypnosis

Two distinct phases are distinguished which occur cyclically over —— min:

1)___________(NREM). _____% of total sleep. Has _____ stages. Most sleep leads to stage ____.

2)__________ (REM). Recalled _____.

A

90

Non-rapid eye movement

70-75; 4; 2

Rapid eye movement; dreams

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

Properties of Sedative/Hypnotics in Sleep
1) The _______ of sleep onset is ____eased (time to ______).
2) The duration of stage ___ ——— sleep is increased.
3) The duration of _____ sleep is decreased.
4) The duration of ___-wave sleep is decreased.

Tolerance occurs after ______

A

latency; Decr; fall asleep

2 NREM; REM

slow; 1-2 weeks

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

slow-wave sleep , when ____________ and —————- occur

A

somnambulism and nightmares

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

Other Properties of Sedative/Hypnotics

Some sedative/hypnotics will depress the CNS to stage ______ of anesthesia.

Due to their (slow or fast?) onset of action and (short or long?) duration, barbiturates such as _______ and ________ are used as _____ in general anesthesia.

A

III ; fast ; short

thiopental and methohexital

adjuncts

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

Sedative/Hypnotics

All of the anxiolytics/sedative/hypnotics should be used only for __________
*****

All the drugs used alter the normal _____ and should be administered only for _______________, never for _________.

              ************ USE FOR \_\_\_\_\_\_\_-TERM TREATMENT ONLY!!
A

symptomatic relief.

sleep cycle

days or weeks; months

SHORT

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

Barbiturates

Long acting
___________

Short acting
___________ , ___________

Ultra-short acting
___________
___________

A

Phenobarbitone

Butobarbitone ,Pentobarbitone

Thiopentone
Methohexitone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

Benzodiazepines

Hypnotic
List 6

Antianxiety
List 5

Anticonvulsant
List 4

A

Diazepam Flurazepam Nitrazepam Alprazolam Temazepam Triazolam

Diazepam Chlordiazepoxide
Oxazepam Lorazepam Alprazolam

Diazepam Lorazepam
Clonazepam Clobazam

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

Non Benzodiazepine hypnotics
List 3

Miscellaneous
List 2

A

ZOLPIDEM
ZALEPLON
ZOPICLONE (ESZOPICLONE)

MELATONIN RAMELTEON

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
42
Q

GABA-A Receptor

Major player in ______ Synapses.

It is a ____ Channel.

Binding of GABA causes the channel to ____ and ____ to flow ____ the cell with the resultant membrane _____________.

A

Inhibitory

Cl- ; open

Cl- ; into

hyperpolarization

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
43
Q

GABA Receptor

Increase in Cl− permeability can depolarize the target cell under some conditions of ________________. This in turn potentially can _____________ or to activate _______ via voltage-gated channels and has been proposed as a physiologically relevant event, especially in embryonic neurons.

A

high intracellular Cl−

excite the cell to fire

Ca2+ entry

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
44
Q

GABA Receptor

GABAB receptors were identified by their __________ to the GABAA antagonist _______.

A

insensitivity; bicuculline

45
Q

GABA Receptor

The GABA analog (−) ________ was found to be a potent and selective GABA___ agonist.

A

baclofen

B

46
Q

GABA Receptor

Baclofen (__________________________________ acid)

A

β-(4-chloro-phenyl)-γ-aminobutyric

47
Q

GABAB receptors are coupled (directly or indirectly?) to ___ channels.

When activated, these receptors can ____ease _____conductance and ____ cAMP production via intracellular mechanisms mediated by G proteins.

A

Indirectly; K+

decr; Ca2+; inhibit

48
Q

GABAB receptors can mediate ___________________________________ inhibition.

A

both postsynaptic and presynaptic

49
Q

GabaB

Presynaptic inhibition may occur as a result of GABABreceptors on nerve terminals causing a ____ease in the influx of _____, thereby reducing the release of neurotransmitters.

it is known that these _________ increase the frequency of channel opening in response to GABA,

A

decr; Ca2+

benzodiazepines

50
Q

benzodiazepine site is coupled allosterically to the ______ and ______ sites.

Benzodiazepine receptors are _______geneous with respect to affinity for certain ligands.

A wide variety of nonbenzodiazepines, such as the _____,________, and ______, also bind to the benzodiazepine site.

A

barbiturate and picrotoxin

hetero

β- carbolines, cyclopyrrolones and imidazopyridines

51
Q

Barbiturates
• enhance the binding of GABA to ______ receptors
•Prolonging ________
•Only _____ (not ____ ) subunits are required for barbiturate action
•(wide or narrow?) therapeutic index
•in _____ doses, barbiturates increase reactions to painful stimuli.

A

GABAA; duration

α and β ; Υ

Narrow; small
Hence, they cannot be relied on to produce sedation or sleep in the presence of even moderate pain.

52
Q

Barbiturates can be relied on to produce sedation or sleep in the presence of moderate pain.

T/F

A

F

they cannot be relied on to produce sedation or sleep in the presence of even moderate pain.

53
Q

Bezodiazepines
• enhance the binding of GABA to ______ receptors

•Increasing the ________

•Unlike barbiturates, benzodiazepines do ___________

A

GABAA

frequency

not activate GABA

54
Q

BARBITURATES or BENZODIAZEPINES

Has a Respiratory depression steeper dose-response relationship than

BARBITURATES or BENZODIAZEPINES

A

BARBITURATES

BENZODIAZEPINES

55
Q

BARBITURATES
ACTIONS

  1. Depression of CNS: At _____ doses, the barbiturates produce _____ (——- effect, reducing ______).
  2. Respiratory depression: Barbiturates suppress the ______ and _______ response to CO2, and overdosage is followed by ———- and _________
  3. Enzyme induction: Barbiturates (induce or inhibit?) P450 microsomal enzymes in the liver.
A

low; sedation; calming ;excitement

hypoxic and chemoreceptor; respiratory depression and death.

induce

56
Q

BARBITURATES
ACTIONS
1. Depression of CNS: At low doses, the barbiturates produce sedation (calming effect, reducing excitement).
2. Respiratory depression: Barbiturates suppress the hypoxic and chemoreceptor response to CO2, and overdosage is followed by respiratory depression and death.
3. Enzyme induction: Barbiturates induce P450 microsomal enzymes in the liver.

A
57
Q

BARBITURATES PHARMACOKINETICS

All barbiturates redistribute in the body.
Barbiturates are metabolized in the ____, and inactive metabolites are excreted in the ________.

A

liver

urine

58
Q

BARBITURATES PHARMACOKINETICS

Toxicity: Extensions of CNS depressant effects
dependence liability (> or <?) benzodiazepines.

A

>

59
Q

BARBITURATES PHARMACOKINETICS

Interactions: Additive CNS depression with ________ and many other drugs (induction or inhibition?) of hepatic drug-metabolizing enzymes.

A

ethanol

induction

60
Q

Barbiturates readily cross the placenta and can depress the fetus.

T/F

A

T

61
Q

THERAPEUTIC USES
ANESTHESIA (THIOPENTAL, METHOHEXITAL)

Selection of a barbiturate is strongly influenced by the desired _________________________

The ultra______-acting barbiturates, such as thiopental, are used _______________ to induce anesthesia.

A

duration of action.

short; intravenously

62
Q

THERAPEUTIC USES
ANESTHESIA (THIOPENTAL, METHOHEXITAL)

ANXIETY
Barbiturates have been used as (mild or severe ?) sedatives to relieve anxiety, nervous tension, and insomnia.

When used as hypnotics, they suppress ________ more than other stages. However, most have been replaced by the _______________.

A

mild; REM sleep

benzodiazepines

63
Q

THERAPEUTIC USES
ANTICONVULSANT: (PHENOBARBITAL, MEPHOBARBITAL)

Phenobarbital is used in (short or long?) -term management of _______ seizures, status ___________, and eclampsia.

A

Long

tonic-clonic ; epilepticus

64
Q

THERAPEUTIC USES
ANTICONVULSANT: (PHENOBARBITAL, MEPHOBARBITAL)

However, phenobarbital can depress ____________ in children, and the drug should be used ______.

A

cognitive performance; cautiously

65
Q

THERAPEUTIC USES
ANTICONVULSANT: (PHENOBARBITAL, MEPHOBARBITAL)

Phenobarbital has specific _________ activity that is distinguished from the ___________ CNS depression.

A

anticonvulsant

nonspecific

66
Q

___________ has been regarded as the drug of choice for treatment of young children with recurrent febrile seizures.

A

Phenobarbital

67
Q

Adverse effects of Barbiturates

CNS: Barbiturates cause drowsiness, impaired _________

Drug hangover: Hypnotic doses of barbiturates produce a feeling of
_________ well after the patient wakes.

Barbiturates (induce or inhibit?) the P450 system.

A

concentration ; tiredness

Induce

68
Q

Adverse effects of Barbiturates

Drug hangover:

By inducing ___________________, barbiturates increase porphyrin synthesis, and are contraindicated in patients with ____________________

A

aminolevulinic acid (ALA) synthetase

acute intermittent porphyria.

69
Q

ADVERSE EFFECTS of Barbiturates

Physical dependence: Abrupt withdrawal from barbiturates may cause ______, anxiety, weakness, ________, nausea and vomiting, seizures, delirium, and _____________

Poisoning: Barbiturate poisoning has been a leading cause of death resulting from drug overdoses for many decades.
It may be due to ____________

A

tremors; restlessness; cardiac arrest.

automatism

70
Q

Barbiturates: adverse effects

Severe depression of _______ is coupled with _______________ depression, and results in a _____-like condition with shallow, infrequent breathing.

A

respiration

central cardiovascular

shock

71
Q

THE TREATMENT OF ACUTE BARBITURATE INTOXICATION

Treatment includes _______ and ________________________ if the drug has been recently taken.

A

artificial respiration ; purging the stomach of its contents

72
Q

Mention 2 specific barbiturate antagonist

A

No specific barbiturate antagonist is available.

73
Q

THE TREATMENT OF ACUTE BARBITURATE INTOXICATION

General supportive measures.
___________ or ___________ is necessary only rarely.

Use of CNS ______________ is contraindicated because they increase the mortality rate.

A

Hemodialysis or hemoperfusion

stimulants

74
Q

THE TREATMENT OF ACUTE BARBITURATE INTOXICATION

If renal and cardiac functions are satisfactory, and the patient is hydrated, __________ and ___________ of the urine will hasten the excretion of phenobarbital.

In the event of renal failure - _________

circulatory collapse is a major threat. So __________ must be corrected & blood pressure can be supported with ———.

Acute renal failure consequent to ______ and ________ accounts for perhaps one-sixth of the deaths.

A

forced diuresis and alkalinization

hemodialysis; hypovolemia; dopamine

shock and hypoxia

75
Q

Effects of benzodiazepine

On increasing the dose, sedation progresses to ______ and then to ________.

But the drugs do not cause a true general anesthesia because
- ________________________
-___________________ to allow surgery cannot be achieved.

However at “preanesthetic” doses, there is ________.

A

hypnosis; stupor

awareness usually persists

-immobility sufficient

amnesia

76
Q

Effects of benzodiazepines on the (EEG) and Sleep Stages

_____eased sleep latency
_____eased number of awakenings
_____eased time spent in stage 0, 1, 3, 4
_____eased time spent in REM sleep (_____eased number of cycles of REM sleep)
____eased total sleep time (largely by increasing the time spent in stage ___)

A

Decr; Decr

Decr; Decr

incr; Incr

2

77
Q

Respiration-Hypnotic doses of benzodiazepines are (with or without?) effect on respiration in normal subjects

CVS-In preanesthetic doses, all benzodiazepines ____ease blood pressure and ____ease heart rate

A

without

decr

incr

78
Q

PHARMACOKINETICS of benzodiazepines

A (short or long?) elimination half-life is desirable for hypnotics, although this carries the drawback of increased _____________ and ____________ after drug discontinuation.

Most of the BZDs are metabolized in the ____ to produce (active or inactive ?) products (thus long duration of action).

After metabolism these are ______ and are excreted via ________.

A

Short

abuse liability and severity of withdrawal

liver; active

conjugated; kidney

79
Q

ADVERSE EFFECTS of BZDs

Light-headedness, Fatigue
____eased reaction time
Motor _______
_______,__________ amnesia

A

Incr; incoordination

Confusion, Antero-grade

80
Q

Adverse effect of BZDs

________ appears to be affected less than ___________.

All of these effects can greatly impair _______ and other psychomotor skills, especially if combined with ———-.

A

Cognition

motor performance

driving; ethanol

81
Q

FLUMAZENIL: A BENZODIAZEPINE RECEPTOR ANTAGONIST

competitively antagonism

Flumazenil antagonizes both the electrophysiological and behavioral effects of agonist and inverse-agonist ___________ and _________.

Flumazenil is available only for ________ administration.

A

benzodiazepines and β -carbolines

intravenous

82
Q

FLUMAZENIL: A BENZODIAZEPINE RECEPTOR ANTAGONIST

On intravenous administration, flumazenil is eliminated almost entirely by hepatic metabolism to (active or inactive?) products with a t1/2 of ~________ ; the duration of clinical effects usually is only _________

A

Inactive

1 hour

30-60 minutes.

83
Q

FLUMAZENIL: A BENZODIAZEPINE RECEPTOR ANTAGONIST

PRIMARY INDICATIONS FOR THE USE OF FLUMAZENIL ARE:-

Management of suspected ________________

Reversal of _______ effects produced by benzodiazepines administered

The administration of _________ injections is preferred to ———— injection.

A

benzodiazepine overdose.

sedative

a series of small

a single bolus

84
Q

Novel Benzodiazepine Receptor Agonists
Z compounds

________,________,_________,____________

structurally (related or unrelated?) to each other and to benzodiazepines

A

zolpidem , zaleplon , zopiclone and eszopiclone

Unrelated

85
Q

Novel Benzodiazepine Receptor Agonists
Z compounds

therapeutic efficacy as hypnotics is due to agonist effects on the ______ site of the _____ receptor

A

benzodiazepine; GABAA

86
Q

Novel Benzodiazepine Receptor Agonists
Z compounds

Compared to benzodiazepines, Z compounds are
-(more or less?) effective as anticonvulsants or muscle relaxants
-which may be related to their relative selectivity for ______ receptors containing the ____ subunit.

A

Less

GABAA

α1

87
Q

The clinical presentation of overdose with Z compounds is similar to that of benzodiazepine overdose and can be treated with the ____________________

A

benzodiazepine antagonist flumazenil.

88
Q

Zaleplon and zolpidem are effective in relieving sleep-onset ______. Both drugs have been approved by the FDA for use for up to __________ at a time.

________ and _______ have sustained hypnotic efficacy without occurrence of rebound insomnia on abrupt discontinuation.

A

insomnia

7-10 days

Zaleplon and zolpidem

89
Q

RAMELTEON

Synthetic tricyclic analog of _________.

It was approved for the treatment of _______, specifically ________ difficulties.

A

MELATONIN; insomnia

sleep onset

90
Q

RAMELTEON

MECHANISM OF ACTION of melatonin

Melatonin levels in the _______ nucleus rise and fall in a circadian fashion

concentrations increasing in the _____ as an individual prepares for sleep, and then reaching a ______ and ultimately ____easing as the night progresses.

A

suprachiastmatic

evening; plateau

decr

91
Q

MELATONIN CONGENERS
Mechanism of Action

Two GPCRs for melatonin, MT1 and MT2, are found in the suprachiasmatic nucleus, each playing a different role in sleep.

RAMELTEON binds to both MT1 and MT2 receptors with (low or high?) affinity.

Binding of Melatonin to MT1 receptors promotes _____________

Binding of Melatonin to MT2 receptors _————- of the circadian system.

A

High; the onset of sleep.

shifts the timing

92
Q

RAMELTEON is efficacious in combating _____________ insomnia

A

both transient and chronic

93
Q

Management of Patients after Long-Term Treatment with Hypnotic Agents

If a benzodiazepine has been used regularly for >2 weeks, it should be ______ rather than ____________.

In some patients on hypnotics with a short t1/2, it is easier to switch first to a hypnotic with a ______ and then to _______.
The onset of withdrawal symptoms from medications with a long t1/2 may be _____.

Consequently, the patient should be warned about the symptoms associated with withdrawal effects.

A

tapered; discontinued abruptly

long t1/2(taper; delayed

94
Q

Atypical Anxiolytics

List 3

A

Buspiron
Ipsapirone Gepirone

95
Q

Buspirone relieves ______ without causing marked ______, hypnotic, or euphoric effects.

  • no _______ or _________ properties.

Buspirone does not interact directly with ________ systems.

A

anxiety; sedative

anticonvulsant or muscle relaxant

GABAergic

96
Q

Anxiolytic effects of buspirone is by acting as a _________ at brain ________ receptors.

A

partial agonist

5-HT1A

97
Q

Buspirone

the anxiolytic effects of buspirone may take more than ______

unsuitable for management of ______ states

____ rebound anxiety or withdrawal signs on abrupt discontinuance

A

a week; acute anxiety

no

98
Q

Buspirone

The drug is effective in blocking the acute withdrawal syndrome resulting from abrupt cessation of use of benzodiazepines or other sedative-hypnotics

A

F

The drug is not effective in blocking the acute withdrawal syndrome resulting from abrupt cessation of use of benzodiazepines or other sedative-hypnotics

99
Q

Buspirone has (minimal or maximal?) abuse liability

The drug is used in _______ states but is less effective in _____ disorders

A

Minimal

generalized anxiety

panic

100
Q

True statement about zolpidem:
A. Relieve sleep onset insomnia
B. Cause profound rebound insomnia
C. Cause profound REM suppression
D. Has strong anticonvulsant effect

A

A

101
Q

Which is NOT true about Flumazenil?
A. Acts on GABAA receptor
B. Specific antagonist of benzodiazepine C. Given intravenously
D. May be used in barbiturate poisoning

A

D

102
Q

Administration of barbiturate is contraindicated in:
A. Kernicterus
B. Anxiety
C. Epilepsy
D. Acute Intermittant porphyria

A

D

103
Q

Benzodiazepines act by:
A. Activating GABAA receptors directly
B. Modulating the effects of GABA on GABAA receptors
C. Antagonistic effect on GABAA receptors D. GABA mimetic effect

A

B

104
Q

Benzodiazepine antagonist is:
A. Naloxone
B. Zolpidem
C. Nalorphine
D. Flumazenil

A

D

105
Q

Beta carboline at benzodiazepine receptor act as:
A. Agonist
B. Inverse agonist
C. Antagonist
D. Partial agonist

A

B

106
Q

True statement about effect of bezodiazepines on sleep is:
A. Time spent in stage 2 is decreased
B. Time spent in stages 1, 3 and 4 is increased
C. Shortening of REM sleep
D. Increase sleep latency

A

C

107
Q

An ideal hypnotic drug should NOT have:
A. rapid onset of action
B. sustained effect throughout the night
C. without any residual effect in the following morning
D. increase in sleep latency

A

D

108
Q

Which one of the following effects is NOT seen with barbiturates?
A. Analgesic
B. Anticonvulsant
C. Induction and maintenance of anaesthesia
D. Sedation

A

A

109
Q

Sleep promoting effect of ramelteon is mediated by receptor:
A. GABAA receptor
B. Opiate receptors
C. GABAB receptor
D. Melatonin receptors MT1 and MT2

A

D

House Pharmacology (50 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions