Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

MBBS II HNNS > L17 - Sedatives and Hypnotics > Flashcards

L17 - Sedatives and Hypnotics Flashcards

1
Q

Compare the action of sedative and hypnotics?

A

Sedative = reduce anxiety + calming without motor or mental function effect

Hypnotics = Produce drowsiness, encourage onset and maintenance of a state of sleep close to natural sleep

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

Anxiety is only a psychiatric illness. T or F?

A

False

Can be both normal emotion (act as stimulant), or psychiatric illness when it becomes excessive and disproportional

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

Mental features of anxiety?

A 
Unpleasant emotional state consisting of: 
Tension, 
Apprehension (sense of dread) 
Uneasiness, 
Feelings of danger

Without a real / logical cause

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

List some physical symptoms of anxiety

A 
 Increased muscle tension 
 Shortness of breath / choking 
 Rapid heartbeat (tachycardia) 
 Dizziness / feel faint 
 Restlessness 
 Sweating 
 Trembling / shaky / wobbly legs 
 Difficulty concentrating 
 Insomnia 
 Nervousness
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

List the 4 Type of anxiety disorders?

A

 Generalized anxiety disorder (GAD)

 Obsessive-compulsive disorder (OCD)

 Panic disorder (panic attacks)

 Post-traumatic stress disorder (PTSD)

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

Define Generalized anxiety disorder (GAD)?

A

most common (50%)

Extreme feeling of anxiety about a wide variety of things

absence of any clear cause

on most days over a long period of time

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

Define OCD?

A

Obsessions: uncontrollable recurring anxiety-producing / intrusive thoughts

Compulsions: need to carry out certain rituals in order to feel less anxious

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

Define Panic disorder (panic attacks)?

A

Rapid-onset, frequent attacks of extreme fear

Feeling of heart palpitations, choking, shortness of breath

Encompass phobic anxiety:
i.e. social phobia

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

Define PTSD?

A

recurrent recollections of a traumatic event of unusual clarity

(e.g. traumatic delivery, sexual assault, violence, major disaster, car accidents)

which produce bursts of intense psychological distress

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

Criteria for insomnia?

A

 >30 min to fall asleep

 Waking up for >30 min at night

 Sleep disturbed >3 nights a week (e.g. for a month)

 Impairment of daytime functioning

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

List some causes of insomnia? Divide into Physical, Physiological, Psychological, Psychiatric and Pharmacological

A

 Physical disorders: cardiovascular system, obstructive sleep apnea, asthma

 Physiological disturbances: late heavy meals, noise, shift work

 Psychological: stress, tension, grief (e.g. death of relative)

 Psychiatric: anxiety, depression, mania, dementia

 Pharmacological: caffeine (e.g. coffee / tea), alcohol, nicotine (e.g. cigarette smoke), medicines (side effect)

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

2 principal chemical classes of sedatives and hypnotics?

A
  • Benzodiazepines

* Barbiturates

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

List other sedatives other than BDZ and barbiturate?

A

–Buspirone
–Antihistamines: e.g. hydroxyzine
–Antidepressants

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

List other hypnotics other than BDZ and barbiturate?

A

–Zolpidem/Zaleplon (Z-drugs)
–Ramelteon
–Chloral hydrate
–Antihistamines

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

List 2 short acting BDZ

A

t1/2: < 5 hr
Short lived or no active metabolites

–Midazolam
–Triazolam

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

List 3 intermediate acting BDZ

A

t1/2: 5-24 hr
Short lived or no active metabolites

–Alprazolam
–Lorazepam
–Temazepam

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

List 2 long acting BDZ

A

t1/2 > 24 hr
long-lived active metabolites

–Chlordiazepoxide
–Clonazepam *
–Diazepam * (Valium)
–Flurazepam

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

Describe the metabolism of BDZ?

A

All are lipid soluble, easily distributed, cross BBB

Short and intermediate acting&raquo_space; α-hydroxy-alprazolam&raquo_space; Glucuronidation

Long- acting&raquo_space; Lots of intermediates (some transform into intermediate acting BDZ)&raquo_space; Glucuronidation

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

List the BDZs that are Sedatives/ Anxiolytics?

A

–Diazepam * (Valium)

–Chlordiazepoxide * (Librium)

–Clonazepam *

–Alprazolam ^

–Lorazepam ^

^ = intermediate 
* = long
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

List the BDZs that are Hypnotics?

A

–Diazepam (Valium) (long)**
–Flurazepam (long)
–Temazepam (Inter)
–Triazolam (short)**

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

MoA of BDZ?

A

1) Selectively activate GABA- A receptors
» mediate fast inhibitory synaptic response produced by activity in GABAergic neurons

2) Bind allosterically to benzodiazepine receptor BZ1 and BZ2
» facilitate opening of GABA-activated chloride channels
» enhance response to GABA

> > Hyperpolrization, reduce neural excitability by increasing frequency of Cl channel opening

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

Describe the structure of the receptor that BDZ acts on?

A

GABA-A receptor-chloride ion channel complex

2α, 2β, γ subunits + BZ1 + BZ2

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

Indication of Alprazolam?

A

Panic disorders

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

Indication of Diazepam apart from anxiolytic/ sedative?

A

Skeletal muscle spasms

Spasticity from degenrative disorders: MS, Cerebral palsy

25
Indication of Midazolam apart from anxiolytic/ hypnotic?
Induction of anesthesia for unpleasant procedures i.e. bronchoscopy
26
BDZs used for seizures?
diazepam*,clonazepam*,lorazepam
27
BDZs used for sleep disorders?
triazolam
28
List some pharmacological effects of BDZ apart from hypnotic/ sedative? Side effects?
1) Temporarily impair memory >> ADR: Cognitive impairment and anterograde amnesia 2) Decrease hypoxic respiratory drive >> ADR: respiratory depression (lethal) 3) Decrease BP, Increase HR >> ADR: dizziness, light headedness 4) Motor ADR: Impaired motor coordination, Ataxia 5) Slurred speech, blur vision, mood swings **No Analgesic/ Antipsychotic effects**
29
BDZ antagonist name, action, admin, indication?
flumazenil: = competitive antagonist of benzodiazepines at the GABAA receptor - IV only - Reversal of BDZ overdose
30
Flumazenil ADR?
BDZ antagonist:  Dizziness, nausea, confusion  Withdrawal in dependent patients  Seizures, agitation
31
Compare the therapeutic index between BDZ and Barbituates.
BDZ = High therapeutic index: Increasing dose > sedation > hypnosis - High doses do not produce anesthesia, coma - patients can be aroused Barbituate = Low therapeutic index / margin of safety: - Effects of increasing dose > sedation >hypnosis > anesthesia > coma (loss of consciousness)
32
Compare physical dependence and tolerance between BDZ and Barbituate.
BDZ = Less physical dependence and withdrawal symptom Barbituate = More physical dependence, severe withdrawal symptoms Both induce tolerance, both induce some psychological dependence
33
Compare D/D interaction between BDZ and Barbituates?
BDZ = Do not induce hepatic microsomal enzyme (CYP450) = no drug-drug interaction Barbituates = Induce hepatic drug-metabolizing enzymes (CYP450) = drug-drug interaction
34
Compare the change in sleeping pattern between BDZ and Barbituates?
BDZ = Do not alter normal sleeping pattern or morning hangover, used as daytime anxiolytics Barbituates = esp. suppress REM sleep, cannot enter deep sleep, unacceptable drowsiness
35
Which has antagonist: BDZ or Barbituates?
BDZ Flumazenil
36
Example of Ultra-short-acting (10-20 min) Barbituates?
–Thiopental
37
Example of Short-acting (2 to 8 hr) barbituate?
–Pentobarbital –Amobarbital –Secobarbital
38
Example of Long- acting (1-2 days) Barbituate?
Phenobarbital
39
Contraindication of barbiturates? Explain why.
1) Induce cytochrome P450 = drug-drug interaction 2) Increase heme synthesis = contraindicated in porphyrias (hereditary disorder of hemoglobin metabolism), cause:  Mental disturbance  Extreme sensitivity to light  Excretion of dark pigments in urine)
40
Triple MoA of Barbituates?
1. Prolong duration (not frequency) of Cl- channel openings  >> potentiate GABA action on Cl- entry into neuron 2. Block excitatory glutamate AMPA receptors >> decreased glutamate-induced excitation 3. Anaesthetic / high concentrations of pentobarbital: also block high-frequency Na+ channels >> decreased neuronal activity (= analgesic)
41
Difference between Barbituate and BDZ action on Cl channels?
BDZ = increase frequency of Cl channel opening Barbituate = increase duration of chloride channel opening + block excitatory glutamata AMPA receptors
42
List some ADR of Barbituate at normal dose?
 Drowsiness  Decreased motor control  Induce hepatic cytochrome P450 system (drug-drug interaction can decrease the effect of other drugs metabolized by these enzymes)
43
List some ADR of Barbituate at high dose?
 High degree of tolerance, dependence  In high doses: respiratory depression, coma = death
44
MoA of Buspirone (BuSpar)?
multi-receptor: 1) partial agonist at 5-HT1A receptors: inhibits presynaptic serotonin release 2) Some affinity for (+)5-HT2A serotonin, (-)D2 dopamine receptors
45
Indication of Buspirone?
No anticonvulsant, muscle relaxant, hypnotic, sedative effects >> just treat anxiety, not hypnotic Indication: generalized anxiety disorder (GAD) (takes 1-2 weeks to exert anxiolytic effects)
46
D/D interactions of Buspirone?
Metabolism by CYP3A4 1) Shorter half-life if taken with rifampin (= inducer of the enzyme) 2) Longer half-life if taken with erythromycin (= inhibitor of the enzyme; macrolide)
47
ADR of Buspirone?
``` –Headaches –Dizziness –Nervousness –Hypothermia –Increase prolactin –Gastrointestinal distress ```
48
Indication of Hydroxyzine as anxiolytic/ hypnotic? ADR?
Antihistamine with antiemetic (H1) activity Indications: 1) Patients with anxiety + history of drug abuse 2) Sedation before dental procedures / surgery ADR: Drowsiness
49
Indication and 3 examples of antidepressants for anxiolytic?
managing long-term symptoms of chronic anxiety disorders:  Selective serotonin reuptake inhibitors (SSRIs)  Tricyclic antidepressants (TCAs)  Monoamine oxidase inhibitors (MAOIs)
50
MoA and indication of Propranolol to treat anxiety?
MoA: - Antagonizes B-adrenoceptors >> excessive catecholamine release does not produce sympathetic responses >> alleviate somatic manifestations of anxiety (e.g. tachycardia, palpitations, tremor, sweating)
51
MoA of Zolpidem/ Zaleplon?
 Binds selectively to BZ1 (= subtype of BZ receptor family)  Facilitates GABA-mediated neuronal inhibition (opens Cl- channel) >> No muscle-relaxing, anticonvulsant effects (pure sleeping pill)
52
Advantages of Zolpidem/Zaleplon as a hypnotic?
Little effect on stages of sleep (like BDZ) Less risk of developing tolerance, dependence with extended use Short duration of action, rapid onset
53
Metabolism of Zolpidem?
hepatic oxidation by cytochrome P450 ( unlike BDZ which doesnt induce P450 ) >> D/D interaction!! CAN BE ANTAGONIZED BY FLUMAZENIL (like BDZ)
54
List possible ADR of Zolpidem?
```  Daytime drowsiness (cf. benzodiazepines)  Ataxia (loss of full control of bodily movements)  Confusion  Nightmares  Agitation  Headache  Dizziness  Gastrointestinal upset ```
55
MoA, indication and ADR of Eszopiclone?
Z-drug Acts on BDZ receptor For Insomnia ADR: Anxiety, dry mouth, headache, peripheral edema, drowsiness, bad taste
56
MoA, indication and ADR of Ramelteon?
Selective agonist at MT1, MT2 subtypes of MELATONIN receptors in hypothalamus >> induce, promote sleep (act like endogenous hormone) Treat mild insomnia ``` ADR:  Dizziness  Fatigue  Drowsiness  Increased production of prolactin levels ```
57
Metabloism, Indication, ADR of Chloral hydrate?
= trichlorinated derivative of acetaldehyde: converted to trichloroethanol (= active metabolite) in the body effective sedative, hypnotic:  Induces sleep in ~30 minutes  Duration of sleep ~6 hr Adverse effects:  Gastrointestinal distress  Unpleasant taste
58
List 3 OTC antihistamines? ADR?
–Diphenhydramine (Unisom SleepGels) –Doxylamine –Promethazine ADR:  Dry mouth  Blurred vision  Drowsiness

MBBS II HNNS (57 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions