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Neurology > Sedatives , Hypnotics, Anxiolytics > Flashcards

Sedatives , Hypnotics, Anxiolytics Flashcards

1
Q

What is a sedative drug

A

A drug that decreases activity moderate excitement and calms

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2
Q

What is a hypnotic drug

A

A drug that produces drowsiness facilitates I’m sets and maintenance of the state of sleep resembling natural sleep from which the recipients can be aroused easily

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3
Q

Two phases of sleep

A

Non-rapid movement sleep

Rapid eye movement sleep

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4
Q

How many stages of nonrapid eye movement sleep there is

A

4

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5
Q

In healthy sleep do you go fast into the first REM sleep Or do you first experience four stages of nonrapid eye movement sleep

A

Experience first four stages of nonrapid eye movement sleep

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6
Q

What part of the brain controls the nonrapid eye movement sleep

A

The basal forebrain
Area surrounding solitary Tracts in Medullal
Dorsal Raph’s nucleus

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7
Q

Decrease of that hormone reduces sleep

A

Serotonin

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8
Q

Destruction of this part of the brain that contains lots of serotonergic bodies reduces sleep

A

Dorsal raphe

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9
Q

What cells turns on the rapid eye movement sleep

A

cholinergics cells

Pontine gigantocellular celld

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10
Q

Hormone responsible for alertness and its decrease promote sleepiness

A

Dopamin

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11
Q

Mira chemicals involved in wakefulness

A 
Acetylcholine 
noradrenaline 
histamine 
Substance p , 
CRF
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12
Q

What is insomnia

A

Complaints of difficulty falling asleep
difficulty maintaining sleep
experiencing non restorative sleep

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13
Q

When is insomnia considered chronic

A

One last more than one month

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14
Q

E What is anxiety

A

Vague in present emotion experienced in anticipation of some future misfortune
State of apprehension and certainty of fear

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15
Q

Is anxiety always a medical condition

A

No it’s actually a normal adaptive function

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16
Q

What is anxiety disorders

A

Extreme of normal anxiety which occur in this regulation of six of system when there is apprehension even though there shouldn’t be

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17
Q

Types of anxiety disorders

A 
Généralised anxiety disorder
Panic disorder
Phobias
PTSD 
Ocd
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18
Q

What is generalized anxiety disorder

A

Excessive uncontrollable irrational worry

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19
Q

What is panic disorder

A

Unexpected repeated episodes of intense fear with physical reaction

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20
Q

What is phobia

A

Persistent fear of an object or situation

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21
Q

What is OCD

A

Repetitive unwanted obsession or compulsive act

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22
Q

Anxiety etiology

A 
Genetic 
neurotransmitter abnormalities - serotonin noradrenaline gabba
HPA DYSREGULATION
 social factors 
personality factors
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23
Q

What body mechanism is responsible for the action of sedative hypnotics

A

Central nervous system depression

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24
Q

Can you go over the state of hypnosis with new sedative hypnotic drugs as easily as it was with older sedative hypnotic drugs

A

No , much harder Requires very large doses

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25
Q

What is considered an ideal anxiolytic drug

A

Calm patients without causing daytime sedation

No physical or psychological

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26
Q

What is an ideal hypnotic drug

A

Patience fall asleep quickly

Sleep has sufficient quality and duration

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27
Q

What are the class of drug considered sedative hypnotic drugs

A 
Benzodiazepines
Barbiturates
Nonbenzodiazepine benzodiazepine receptor agonist
Sedative antihistamines
Melatonin receptor agonist
Herbals
Miscellaneous drug
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28
Q

The use of barbiturate is now confined to two specific uses ,what are they

A

Epilepsy

anesthesia

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29
Q

Examples of non-benzodiazepine benzodiazepine receptor agonist

A

Zaleplon
zopiclone
Eszopiclone
zolpidem

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30
Q

Examples of melatonin receptor agonist

A

Ramelteon

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31
Q

Example of sedative antihistamines

A

Diphenhydramine
Hydroxyzine
Promethazine

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32
Q

Examples of herbals

A

Valerian

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33
Q

Examples of miscellaneous drugs

A

Chloral hydrate
Meprobamate
Methaqualone

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34
Q

What substituent is necessary at the 7 position in the heterocyclic structure coupled to the benzene ring in benzodiazepines for sedative hypnotic activity to occur

A

A halogen or nitro group

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35
Q

What special structures do you find in triazolam and alprazolam which are benzodiazepines

A

Triazole ring at position one and two

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36
Q

Administration modes of benzodiazepine

A

Oral

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37
Q

Which Benzodiazepine have extremely rapid absorption

A

Triazolam
Diazepam
Clorazepate

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38
Q

What factor plays major role in determining rate at which a particular benzodiazepine will enter the central nervous system

A

The Lipids solubility profile

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39
Q

Can sedative hypnotics cross placental barrier during pregnancy

A

Yes

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40
Q

Can you find sedative hypnotics in breast milk

A

Yes

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41
Q

What is the metabolism of benzodiazepine

A

Hepatic - Microsomal oxidation with the alkylation and aliphatic hydroxylation
Conjugation with glucuronide

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42
Q

Metabolism of alprazolam and triazolam

A

Alfa hydroxylation. And then form inactive glucuronides

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43
Q

Are the effects of alprazolam and trialozam long lived or short lived

A

Short lived

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44
Q

How are benzodiazepine excreted

A

Through urine

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45
Q

The changes in renal function have it marked effect on elimination of parent benzodiazepine

A

No

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46
Q

In which type of disease do you see increased time of elimination

A

In old patients with severe liver disease

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47
Q

Which type of drugs when taken for a long term can cause increased hepatic microsomal activity of the enzyme

A

Barbiturates

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48
Q

Do benzodiazepine change hepatic drug metabolizing enzyme activity with continuous use

A

No

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49
Q

Where do benzodiazepine bind on GABA receptor

A

Between alpha 1 and gamma 2

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50
Q

Why do zolpidem zaleplon and eszopiclone buying bind more selectively to GABA receptors

A

Only interact with subunit containing alpha 1 subunit

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51
Q

Which part of the central nervous system do benzodiazepine potentiates GABA inhibition

A 
Spinal cord 
hypothalamus 
hippocampus 
substantial nigra
 cerebellar cortex 
cerebral cortex
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52
Q

Do benzodiazepines substitute or enhance gaba effects

A

Enhance rather than substitute

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53
Q

What are the action at the organ level of benzodiazepine

A

Sedation
Hypnosis
anticonvulsants
muscle relaxation

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54
Q

What are the clinical uses of benzodiazepine

A 
Anxiety states 
insomnia 
skeletal muscle relaxation 
premedication in anesthesia 
status epilepticus 
acute seizures 
Antero grade amnesia 
alcohol and sedative hypnotic withdrawal
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55
Q

What are the adverse effects of benzodiazepine

A

Toxic effects from overdosage
Unwanted effect wiith normal therapeutic use
Tolerance
dependence

56
Q

What are the side effects with therapeutic use in benzodiazepine used

A

Drowsiness
confusion
amnesia
impaired coordination

57
Q

Is chlordiazepoxide also known as Librium a long or short acting benzodiazepines

A

Long

58
Q

What is Librium mostly used for

A

Anxiety disorders
anesthetic premedication
alcohol withdrawal management
muscle relaxation

59
Q

Is clonazepam also known as clonopin a long acting or short acting benzodiazepine

A

Long acting

60
Q

When do you use clonazepam

A

Seizure disorders
adjunctive treatment in acute mania
movement disorders like Tourette syndrome

61
Q

Can clonazepam lead to tolerance in seizures disorders treatment

A

Yes

62
Q

Is Diazepam known as Valium a long or a short acting benzodiazepine

A

Long acting

63
Q

What are the main uses of diazepam

A

Anxiety disorders
seizures disorders like status epilepticus
anesthetic premedication
skeletal muscle relaxation

64
Q

Is flurazepam a long acting or short acting benzodiazepine

A

How long acting

65
Q

In which case is flurazepam used

A

Insomnia

anxiety disorders

66
Q

Alprazolam is long shorts or medium acting benzodiazepine

A

Medium acting

67
Q

Are withdrawal symptoms severe in alprazolam use

A

Yes

68
Q

When do you use alprazolam

A

Anxiety disorders

depressio

69
Q

Nitrazepam is a long short or medium acting benzodiaze

A

Medium

70
Q

When do you mostly use nitrazepam

A

Anxiety disorders

insomnia

71
Q

lorazepam a short long or medium acting benzodiazepine

A

Short acting

72
Q

Usage of lorazepam

A

Anxiety disorders
insomnia
preanesthetic medication

73
Q

Oxazepam short long or medium acting benzodiazepines

A

Short

74
Q

Use of oxazepam

A

Anxiety disorders

insomnia

75
Q

Is temazepam a short long or medium acting benzodiazepine

A

Short

76
Q

Use of temazepam

A

Insomnia

anxiety disorders

77
Q

Is midazolam a short medium long or ultra short acting benzodiazepine

A

Ultrashort

78
Q

Main uses of midazolam

A

Anxiety disorders
insomnia
preanesthetic medication

79
Q

Triazolam is a short ultrashort long or medium acting

A

Ultrashort

80
Q

Usage of triazolam

A

Insomnia

81
Q

Is clorazepate prodrug or active

A

Prodrug

82
Q

Use of clorazepate

A

Anxiety disorders seizures disorders

83
Q

Metabolism of clorazepate

A

Form nordazepam by decarboxylation

84
Q

What is an example of a specific benzodiazepine antagonists

A

Flumazenil

85
Q

Mode of administration of flumazenil

A

Iv

86
Q

What is the primary use of flumazenil

A

Management of benzodiazepine overdose

Reversal of sedative effect produced by benzodiazepine

87
Q

Is there a psychological and physical dependence with barbiturates

A

Yes

88
Q

Examples of barbiturates

A 
Phenobarbital 
Secobarbital 
Thiopental
Methohexital
Pentobarbital
Amobarbital
89
Q

What does action of barbiturates

A

Increase duration of gabba gated chloride channel openings

Can act like gabba mimetic at high concentration and activate directly chloride channels

90
Q

The barbiturate binds on the same site as benzodiazepine on GABA receptor

A

No

91
Q

What is the reason why barbiturates seem to have full surgical anesthesia ability and pronounced central depressants affect compared to benzodiazepine

A

Because of multiplicity of site of action

92
Q

Where is barbiturate absorbed

A

Small intestine
stomach
Because weakly acidic

93
Q

Is lipid profile important for central nervous system entry of barbiturates

A

Yes

94
Q

Which type of barbiturate are very lipid soluble and have a high entry and Rapid onset of action

A

Thiobarbiturates

95
Q

How are barbiturates cleared

A

Metabolized to more water soluble metabolites with conversion to alcohols and then conversion to glucuronides

96
Q

How are barbiturates excreted

A

By kidneys

97
Q

What method can be used to increase rate of elimination of barbiturates by kidneys

A

alkalinization of urine

98
Q

C clinical uses of barbiturates

A

Epilepsy
insomnia
general anesthesia

99
Q

Adverse effects of barbiturates

A 
Dizziness 
lightheadedness 
sedation 
headache 
nausea 
abdominal pain 
Tolerance 
 dependence 
cardiovascular depression 
respiratory depression
100
Q

What is an example of a non-benzodiazepine benzodiazepine receptor agonist

A

Zolpidem

Zaleplon

101
Q

Can flumazenil antagonize zolpidem

A

Yes

102
Q

Action an organ of zolpidem

A

Minimal Muscle relaxation

minimal anticonvulsant effect

103
Q

Does zolpidem have a Rapids aonset of action

A

Yes

104
Q

Which case can you have respiratory depression with zolpidem

A

If you take ethanol

105
Q

Metabolism of zolpidem

A

Oxidation and hydroxylation by liver

106
Q

Half life of zolpidem

A

1.5 hours to 3.5

107
Q

should you reduce the dosage of zolpidem in patients with hepatic dysfunction surgery patient and patient taking cimetidine

A

Yes

108
Q

Elimination half-life of Zaleplon

A

One hour

109
Q

Metabolism of zaleplon

A

Hepatic aldehyde oxidase and CYP3A4 in liver

110
Q

Which direction inhibits metabolism of zaleplon

A

Cimetidine

111
Q

What is the effect of zaleplon on sleep

A

Decrease sleep latency

no effect on sleep time or architecture

112
Q

Do you have rebound insomnia in zaleplon usage

A

Yes

113
Q

What is an example of a melatonin receptor agonist

A

Ramelteon

114
Q

Which receptor Ramelteon act

A

MT1

MT2

115
Q

Who should use Ramelteon

A

Patient will have difficulty falling asleep

116
Q

What is the goal of melatonin receptors

A

Maintain circadian rhythms

117
Q

Metabolism of Ramelteon

A

CYP1A2

Cyp2c9

118
Q

Which drug should you not give with Ramelteon

A 
Cyp1a2
Ciprofloxacin 
Fluvoxamine
Tacrine 
zileuton
Fluconazole (cyp2c9)
119
Q

Is there dependence or abuse with Ramelteon

A

Yes

120
Q

Should you pay attention in patients with liver dysfunction when administering Ramelteon

A

Yes

121
Q

Adverse effects of Ramelteon

A

‘Dizziness
somnolence
fatigue
Endocrine changes

122
Q

What is the function of histamine

A

Circadian pattern of release to activate neuron in day and silence them at night
Act on H1 receptors in cortex and reticular activating system for arousal and wakefulness

123
Q

Examples of antihistamine

A

Diphenhydramine
Chlorpheniramine
Hydroxyzine
Promethazine

124
Q

What is believed to be the mechanism of action of valerian which is an herbal remedy

A

May be involved in increasing concentration of gabba

125
Q

First line drugs for generalized anxiety disorders

A 
Duloxetine
Escitalopram 
Imipramine
PAroxetine
Sertraline 
Venlafaxine
126
Q

Secondly drugs for generalized anxiety disorders

A

Benzodiazepines
Busipirone
Buspirone
Imipramine

127
Q

First line drugs for panic disorders

A

SSRIs

venlafaxine

128
Q

Social anxiety disorder first line drugs

A 
Escitalopram
Fluvoxamine
Paroxetine 
sertraline 
venlafaxine
129
Q

Post traumatic stress disorder first line drugs

A

SSRI

130
Q

First example of a class of anxiolytic agents

A

Buspirone

131
Q

What is the mechanism of action of Buspirone

A

Serotonin receptor partial agonist

Inhibits activity of nor adrenergic nucleus Ceruleus neurons and interfere with arousal reaction

132
Q

Who is more effective buspirone or benzodiazepines for treatment of general anxiety

A

They are both equally effective

133
Q

Does Buspirone has sedative effect

A

No

134
Q

Can you call uses of Buspirone

A

Generalized anxiety disorder

Anxiety with depression

135
Q

Adverse effects of Buspirone

A

Dizziness
lightheadedness
headache
increased but blood pressure when taken with MAO inhibitors
can increase plasma levels of haloperidol
Abuse dependence and withdrawal symptoms

Neurology (31 decks)

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