Brainscape's Knowledge GenomeTM

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


See full index

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
Q

Indication of Midazolam apart from anxiolytic/ hypnotic?

A

Induction of anesthesia for unpleasant procedures i.e. bronchoscopy

26
Q

BDZs used for seizures?

A

diazepam,clonazepam,lorazepam

27
Q

BDZs used for sleep disorders?

A

triazolam

28
Q

List some pharmacological effects of BDZ apart from hypnotic/ sedative? Side effects?

A

1) Temporarily impair memory&raquo_space; ADR: Cognitive impairment and anterograde amnesia
2) Decrease hypoxic respiratory drive&raquo_space; ADR: respiratory depression (lethal)
3) Decrease BP, Increase HR&raquo_space; ADR: dizziness, light headedness
4) Motor ADR: Impaired motor coordination, Ataxia
5) Slurred speech, blur vision, mood swings

No Analgesic/ Antipsychotic effects

29
Q

BDZ antagonist name, action, admin, indication?

A

flumazenil:

= competitive antagonist of benzodiazepines at the GABAA receptor

  • IV only
  • Reversal of BDZ overdose
30
Q

Flumazenil ADR?

A

BDZ antagonist:

 Dizziness, nausea, confusion
 Withdrawal in dependent patients
 Seizures, agitation

31
Q

Compare the therapeutic index between BDZ and Barbituates.

A

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
Q

Compare physical dependence and tolerance between BDZ and Barbituate.

A

BDZ = Less physical dependence and withdrawal symptom

Barbituate = More physical dependence, severe withdrawal symptoms

Both induce tolerance, both induce some psychological dependence

33
Q

Compare D/D interaction between BDZ and Barbituates?

A

BDZ = Do not induce hepatic microsomal enzyme (CYP450) = no drug-drug interaction

Barbituates = Induce hepatic drug-metabolizing enzymes (CYP450) = drug-drug interaction

34
Q

Compare the change in sleeping pattern between BDZ and Barbituates?

A

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
Q

Which has antagonist: BDZ or Barbituates?

A

BDZ

Flumazenil

36
Q

Example of Ultra-short-acting (10-20 min) Barbituates?

A

–Thiopental

37
Q

Example of Short-acting (2 to 8 hr) barbituate?

A

–Pentobarbital
–Amobarbital
–Secobarbital

38
Q

Example of Long- acting (1-2 days) Barbituate?

A

Phenobarbital

39
Q

Contraindication of barbiturates? Explain why.

A

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
Q

Triple MoA of Barbituates?

A
  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
Q

Difference between Barbituate and BDZ action on Cl channels?

A

BDZ = increase frequency of Cl channel opening

Barbituate = increase duration of chloride channel opening + block excitatory glutamata AMPA receptors

42
Q

List some ADR of Barbituate at normal dose?

A

 Drowsiness

 Decreased motor control

 Induce hepatic cytochrome P450 system
(drug-drug interaction can decrease the effect of other drugs metabolized by these enzymes)

43
Q

List some ADR of Barbituate at high dose?

A

 High degree of tolerance, dependence

 In high doses: respiratory depression, coma = death

44
Q

MoA of Buspirone (BuSpar)?

A

multi-receptor:

1) partial agonist at 5-HT1A receptors: inhibits presynaptic serotonin release
2) Some affinity for (+)5-HT2A serotonin, (-)D2 dopamine receptors

45
Q

Indication of Buspirone?

A

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
Q

D/D interactions of Buspirone?

A

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
Q

ADR of Buspirone?

A 
–Headaches 
–Dizziness 
–Nervousness 
–Hypothermia 
–Increase prolactin
–Gastrointestinal distress
48
Q

Indication of Hydroxyzine as anxiolytic/ hypnotic? ADR?

A

Antihistamine with antiemetic (H1) activity

Indications:

1) Patients with anxiety + history of drug abuse
2) Sedation before dental procedures / surgery

ADR:
Drowsiness

49
Q

Indication and 3 examples of antidepressants for anxiolytic?

A

managing long-term symptoms of chronic anxiety disorders:

 Selective serotonin reuptake inhibitors (SSRIs)
 Tricyclic antidepressants (TCAs)
 Monoamine oxidase inhibitors (MAOIs)

50
Q

MoA and indication of Propranolol to treat anxiety?

A

MoA:
- Antagonizes B-adrenoceptors

> > excessive catecholamine release does not produce sympathetic responses

> > alleviate somatic manifestations of anxiety (e.g. tachycardia, palpitations, tremor, sweating)

51
Q

MoA of Zolpidem/ Zaleplon?

A

 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
Q

Advantages of Zolpidem/Zaleplon as a hypnotic?

A

Little effect on stages of sleep (like BDZ)

Less risk of developing tolerance, dependence with extended use

Short duration of action, rapid onset

53
Q

Metabolism of Zolpidem?

A

hepatic oxidation by cytochrome P450 ( unlike BDZ which doesnt induce P450 )

> > D/D interaction!!

CAN BE ANTAGONIZED BY FLUMAZENIL (like BDZ)

54
Q

List possible ADR of Zolpidem?

A 
 Daytime drowsiness (cf. benzodiazepines) 
 Ataxia (loss of full control of bodily movements) 
 Confusion 
 Nightmares 
 Agitation 
 Headache 
 Dizziness 
 Gastrointestinal upset
55
Q

MoA, indication and ADR of Eszopiclone?

A

Z-drug

Acts on BDZ receptor

For Insomnia

ADR:
Anxiety, dry mouth, headache, peripheral edema, drowsiness, bad taste

56
Q

MoA, indication and ADR of Ramelteon?

A

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
Q

Metabloism, Indication, ADR of Chloral hydrate?

A

= 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
Q

List 3 OTC antihistamines? ADR?

A

–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.
© 2024 Bold Learning Solutions. Terms and Conditions