Sedatives , Hypnotics, Anxiolytics Flashcards
1
Q
What is a sedative drug
A
A drug that decreases activity moderate excitement and calms
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
3
Q
Two phases of sleep
A
Non-rapid movement sleep
Rapid eye movement sleep
4
Q
How many stages of nonrapid eye movement sleep there is
A
4
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
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
7
Q
Decrease of that hormone reduces sleep
A
Serotonin
8
Q
Destruction of this part of the brain that contains lots of serotonergic bodies reduces sleep
A
Dorsal raphe
9
Q
What cells turns on the rapid eye movement sleep
A
cholinergics cells
Pontine gigantocellular celld
10
Q
Hormone responsible for alertness and its decrease promote sleepiness
A
Dopamin
11
Q
Mira chemicals involved in wakefulness
A
Acetylcholine noradrenaline histamine Substance p , CRF
12
Q
What is insomnia
A
Complaints of difficulty falling asleep
difficulty maintaining sleep
experiencing non restorative sleep
13
Q
When is insomnia considered chronic
A
One last more than one month
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
15
Q
Is anxiety always a medical condition
A
No it’s actually a normal adaptive function
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
17
Q
Types of anxiety disorders
A
Généralised anxiety disorder Panic disorder Phobias PTSD Ocd
18
Q
What is generalized anxiety disorder
A
Excessive uncontrollable irrational worry
19
Q
What is panic disorder
A
Unexpected repeated episodes of intense fear with physical reaction
20
Q
What is phobia
A
Persistent fear of an object or situation
21
Q
What is OCD
A
Repetitive unwanted obsession or compulsive act
22
Q
Anxiety etiology
A
Genetic neurotransmitter abnormalities - serotonin noradrenaline gabba HPA DYSREGULATION social factors personality factors
23
Q
What body mechanism is responsible for the action of sedative hypnotics
A
Central nervous system depression
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
25
What is considered an ideal anxiolytic drug
Calm patients without causing daytime sedation
| No physical or psychological
26
What is an ideal hypnotic drug
Patience fall asleep quickly
| Sleep has sufficient quality and duration
27
What are the class of drug considered sedative hypnotic drugs
```
Benzodiazepines
Barbiturates
Nonbenzodiazepine benzodiazepine receptor agonist
Sedative antihistamines
Melatonin receptor agonist
Herbals
Miscellaneous drug
```
28
The use of barbiturate is now confined to two specific uses ,what are they
Epilepsy
| anesthesia
29
Examples of non-benzodiazepine benzodiazepine receptor agonist
Zaleplon
zopiclone
Eszopiclone
zolpidem
30
Examples of melatonin receptor agonist
Ramelteon
31
Example of sedative antihistamines
Diphenhydramine
Hydroxyzine
Promethazine
32
Examples of herbals
Valerian
33
Examples of miscellaneous drugs
Chloral hydrate
Meprobamate
Methaqualone
34
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 halogen or nitro group
35
What special structures do you find in triazolam and alprazolam which are benzodiazepines
Triazole ring at position one and two
36
Administration modes of benzodiazepine
Oral
37
Which Benzodiazepine have extremely rapid absorption
Triazolam
Diazepam
Clorazepate
38
What factor plays major role in determining rate at which a particular benzodiazepine will enter the central nervous system
The Lipids solubility profile
39
Can sedative hypnotics cross placental barrier during pregnancy
Yes
40
Can you find sedative hypnotics in breast milk
Yes
41
What is the metabolism of benzodiazepine
Hepatic - Microsomal oxidation with the alkylation and aliphatic hydroxylation
Conjugation with glucuronide
42
Metabolism of alprazolam and triazolam
Alfa hydroxylation. And then form inactive glucuronides
43
Are the effects of alprazolam and trialozam long lived or short lived
Short lived
44
How are benzodiazepine excreted
Through urine
45
The changes in renal function have it marked effect on elimination of parent benzodiazepine
No
46
In which type of disease do you see increased time of elimination
In old patients with severe liver disease
47
Which type of drugs when taken for a long term can cause increased hepatic microsomal activity of the enzyme
Barbiturates
48
Do benzodiazepine change hepatic drug metabolizing enzyme activity with continuous use
No
49
Where do benzodiazepine bind on GABA receptor
Between alpha 1 and gamma 2
50
Why do zolpidem zaleplon and eszopiclone buying bind more selectively to GABA receptors
Only interact with subunit containing alpha 1 subunit
51
Which part of the central nervous system do benzodiazepine potentiates GABA inhibition
```
Spinal cord
hypothalamus
hippocampus
substantial nigra
cerebellar cortex
cerebral cortex
```
52
Do benzodiazepines substitute or enhance gaba effects
Enhance rather than substitute
53
What are the action at the organ level of benzodiazepine
Sedation
Hypnosis
anticonvulsants
muscle relaxation
54
What are the clinical uses of benzodiazepine
```
Anxiety states
insomnia
skeletal muscle relaxation
premedication in anesthesia
status epilepticus
acute seizures
Antero grade amnesia
alcohol and sedative hypnotic withdrawal
```
55
What are the adverse effects of benzodiazepine
Toxic effects from overdosage
Unwanted effect wiith normal therapeutic use
Tolerance
dependence
56
What are the side effects with therapeutic use in benzodiazepine used
Drowsiness
confusion
amnesia
impaired coordination
57
Is chlordiazepoxide also known as Librium a long or short acting benzodiazepines
Long
58
What is Librium mostly used for
Anxiety disorders
anesthetic premedication
alcohol withdrawal management
muscle relaxation
59
Is clonazepam also known as clonopin a long acting or short acting benzodiazepine
Long acting
60
When do you use clonazepam
Seizure disorders
adjunctive treatment in acute mania
movement disorders like Tourette syndrome
61
Can clonazepam lead to tolerance in seizures disorders treatment
Yes
62
Is Diazepam known as Valium a long or a short acting benzodiazepine
Long acting
63
What are the main uses of diazepam
Anxiety disorders
seizures disorders like status epilepticus
anesthetic premedication
skeletal muscle relaxation
64
Is flurazepam a long acting or short acting benzodiazepine
How long acting
65
In which case is flurazepam used
Insomnia
| anxiety disorders
66
Alprazolam is long shorts or medium acting benzodiazepine
Medium acting
67
Are withdrawal symptoms severe in alprazolam use
Yes
68
When do you use alprazolam
Anxiety disorders
| depressio
69
Nitrazepam is a long short or medium acting benzodiaze
Medium
70
When do you mostly use nitrazepam
Anxiety disorders
| insomnia
71
lorazepam a short long or medium acting benzodiazepine
Short acting
72
Usage of lorazepam
Anxiety disorders
insomnia
preanesthetic medication
73
Oxazepam short long or medium acting benzodiazepines
Short
74
Use of oxazepam
Anxiety disorders
| insomnia
75
Is temazepam a short long or medium acting benzodiazepine
Short
76
Use of temazepam
Insomnia
| anxiety disorders
77
Is midazolam a short medium long or ultra short acting benzodiazepine
Ultrashort
78
Main uses of midazolam
Anxiety disorders
insomnia
preanesthetic medication
79
Triazolam is a short ultrashort long or medium acting
Ultrashort
80
Usage of triazolam
Insomnia
81
Is clorazepate prodrug or active
Prodrug
82
Use of clorazepate
Anxiety disorders seizures disorders
83
Metabolism of clorazepate
Form nordazepam by decarboxylation
84
What is an example of a specific benzodiazepine antagonists
Flumazenil
85
Mode of administration of flumazenil
Iv
86
What is the primary use of flumazenil
Management of benzodiazepine overdose
| Reversal of sedative effect produced by benzodiazepine
87
Is there a psychological and physical dependence with barbiturates
Yes
88
Examples of barbiturates
```
Phenobarbital
Secobarbital
Thiopental
Methohexital
Pentobarbital
Amobarbital
```
89
What does action of barbiturates
Increase duration of gabba gated chloride channel openings
Can act like gabba mimetic at high concentration and activate directly chloride channels
90
The barbiturate binds on the same site as benzodiazepine on GABA receptor
No
91
What is the reason why barbiturates seem to have full surgical anesthesia ability and pronounced central depressants affect compared to benzodiazepine
Because of multiplicity of site of action
92
Where is barbiturate absorbed
Small intestine
stomach
Because weakly acidic
93
Is lipid profile important for central nervous system entry of barbiturates
Yes
94
Which type of barbiturate are very lipid soluble and have a high entry and Rapid onset of action
Thiobarbiturates
95
How are barbiturates cleared
Metabolized to more water soluble metabolites with conversion to alcohols and then conversion to glucuronides
96
How are barbiturates excreted
By kidneys
97
What method can be used to increase rate of elimination of barbiturates by kidneys
alkalinization of urine
98
C clinical uses of barbiturates
Epilepsy
insomnia
general anesthesia
99
Adverse effects of barbiturates
```
Dizziness
lightheadedness
sedation
headache
nausea
abdominal pain
Tolerance
dependence
cardiovascular depression
respiratory depression
```
100
What is an example of a non-benzodiazepine benzodiazepine receptor agonist
Zolpidem
| Zaleplon
101
Can flumazenil antagonize zolpidem
Yes
102
Action an organ of zolpidem
Minimal Muscle relaxation
| minimal anticonvulsant effect
103
Does zolpidem have a Rapids aonset of action
Yes
104
Which case can you have respiratory depression with zolpidem
If you take ethanol
105
Metabolism of zolpidem
Oxidation and hydroxylation by liver
106
Half life of zolpidem
1.5 hours to 3.5
107
should you reduce the dosage of zolpidem in patients with hepatic dysfunction surgery patient and patient taking cimetidine
Yes
108
Elimination half-life of Zaleplon
One hour
109
Metabolism of zaleplon
Hepatic aldehyde oxidase and CYP3A4 in liver
110
Which direction inhibits metabolism of zaleplon
Cimetidine
111
What is the effect of zaleplon on sleep
Decrease sleep latency
| no effect on sleep time or architecture
112
Do you have rebound insomnia in zaleplon usage
Yes
113
What is an example of a melatonin receptor agonist
Ramelteon
114
Which receptor Ramelteon act
MT1
| MT2
115
Who should use Ramelteon
Patient will have difficulty falling asleep
116
What is the goal of melatonin receptors
Maintain circadian rhythms
117
Metabolism of Ramelteon
CYP1A2
| Cyp2c9
118
Which drug should you not give with Ramelteon
```
Cyp1a2
Ciprofloxacin
Fluvoxamine
Tacrine
zileuton
Fluconazole (cyp2c9)
```
119
Is there dependence or abuse with Ramelteon
Yes
120
Should you pay attention in patients with liver dysfunction when administering Ramelteon
Yes
121
Adverse effects of Ramelteon
'Dizziness
somnolence
fatigue
Endocrine changes
122
What is the function of histamine
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
Examples of antihistamine
Diphenhydramine
Chlorpheniramine
Hydroxyzine
Promethazine
124
What is believed to be the mechanism of action of valerian which is an herbal remedy
May be involved in increasing concentration of gabba
125
First line drugs for generalized anxiety disorders
```
Duloxetine
Escitalopram
Imipramine
PAroxetine
Sertraline
Venlafaxine
```
126
Secondly drugs for generalized anxiety disorders
Benzodiazepines
Busipirone
Buspirone
Imipramine
127
First line drugs for panic disorders
SSRIs
| venlafaxine
128
Social anxiety disorder first line drugs
```
Escitalopram
Fluvoxamine
Paroxetine
sertraline
venlafaxine
```
129
Post traumatic stress disorder first line drugs
SSRI
130
First example of a class of anxiolytic agents
Buspirone
131
What is the mechanism of action of Buspirone
Serotonin receptor partial agonist
| Inhibits activity of nor adrenergic nucleus Ceruleus neurons and interfere with arousal reaction
132
Who is more effective buspirone or benzodiazepines for treatment of general anxiety
They are both equally effective
133
Does Buspirone has sedative effect
No
134
Can you call uses of Buspirone
Generalized anxiety disorder
| Anxiety with depression
135
Adverse effects of Buspirone
Dizziness
lightheadedness
headache
increased but blood pressure when taken with MAO inhibitors
can increase plasma levels of haloperidol
Abuse dependence and withdrawal symptoms
