Anxiolytics & Hypnotics ✔️ Flashcards
(101 cards)
1
Q
What do anxiolytic drugs treat?
A
Acute anxiety.
2
Q
What do hypnotic drugs treat?
A
Sleep disorders
3
Q
Why are anxiolytics and hypnotics used interchangeably?
A
Because all anxiolytics have sedative effects
4
Q
What can high doses of sedative-hypnotics lead to?
A
Unconsciousness and death from respiratory and cardiovascular depression.
5
Q
What are the main drug groups of anxiolytics and hypnotics?
A
• Benzodiazepines (BZDs)
• Barbiturates
• 5-HT1A receptor agonists
• Other
6
Q
What is GABA (Gamma-Aminobutyric Acid)?
A
The major inhibitory neurotransmitter in the CNS.
7
Q
What is the role of GABA in the CNS?
A
It provides tonic control of excitatory transmission.
8
Q
What type of receptor is GABA-A, and what is its function?
A
It is an ion channel that mediates fast inhibitory synaptic transmission.
9
Q
What type of receptor is GABA-B?
A
A G-protein coupled receptor.
10
Q
What is the structure of the GABA-A receptor?
A
It is a multimeric ligand-gated ion channel
11
Q
What is the function of the GABA-A receptor?
A
It mediates fast postsynaptic inhibition via chloride influx, which hyperpolarizes the cell.
12
Q
Which drugs target the GABA-A receptor?
A
Benzodiazepines and barbiturates
13
Q
What are the main routes of administration for benzodiazepines?
A
Orally (mainly) and intravenously (I.V).
14
Q
Which benzodiazepine is used for status epilepticus?
A
Diazepam
15
Q
Which benzodiazepine is used for anesthesia?
A
Midazolam
16
Q
What is the most widely used class of anxiolytic drugs?
A
Benzodiazepines
(though their use is declining in favor of antidepressants and behavioral therapies in severe cases).
17
Q
Which older class of drugs have benzodiazepines replaced? Why?
A
Barbiturates, because benzodiazepines are more effective and safer.
18
Q
What is the mechanism of action of benzodiazepines (BZDs)?
A
Bind selectively to GABA-A modulatory site → enhance GABA receptor-mediated inhibition in the CNS by increasing GABA’s effect on opening chloride channels.
19
Q
What are the pharmacological effects of benzodiazepines (BZDs)?
A
• Reduction of anxiety and aggression
• Sedation and induction of sleep
• Reduction of muscle tone and coordination
• Anticonvulsant effects
• Anterograde amnesia
20
Q
Do benzodiazepines have antidepressant effects?
A
No, except for alprazolam.
21
Q
What is a possible side effect of short-acting benzodiazepines like triazolam?
A
They may increase irritability and aggression, likely due to withdrawal syndrome.
22
Q
Which benzodiazepine is long-acting and used for prolonged periods?
A
Diazepam
23
Q
Which benzodiazepine is used for panic disorders and suitable for short- and long-term treatment?
A
Alprazolam
24
Q
True or False:
Triazolam was withdrawn from the UK.
A
True
25
What are the two psychologically important types of sleep?
REM sleep (dreaming) and slow-wave sleep (deepest level of sleep)
26
What physiological changes occur during slow-wave sleep?
Metabolic rate and adrenal steroid secretion are at their lowest, and growth hormone secretion is at its highest.
27
What happens when REM sleep is artificially interrupted?
It leads to irritability and anxiety, even if the total amount of sleep is unaffected.
28
How do most hypnotics affect REM sleep?
reduce REM sleep proportion
29
Which hypnotic drugs affect REM sleep the least?
Benzodiazepines (BZDs) reduce REM sleep less than others, and zolpidem (non-BZD) reduces it the least.
30
How do BZDs affect slow-wave sleep (SW) and growth hormone secretion?
BZDs reduce SW sleep, but growth hormone secretion remains unaffected.
31
What is the short-term effect of BZDs on sleep?
They decrease the time taken to fall asleep and increase total sleep duration in patients who sleep less than 6 hours.
32
How long do the beneficial sleep effects of BZDs typically last?
1–2 weeks; after that, both effects decline
33
Why is long-term use of BZDs as sleeping pills not recommended?
Due to tolerance, dependence, and hangover effects.
34
For how long should BZDs be used as hypnotics?
Not more than 3 weeks, preferably only for one week.
35
What type of acting drug is Flurazepam; short-acting or long-acting?
Long acting.
36
What type of acting drug is Temazepam
Short , intermediate, or long acting?
Intermediate acting.
37
What happens to muscle tone during anxiety?
Muscle tone increases, leading to headaches, aches, and pains.
38
How do BZDs reduce muscle tone?
By central action independent of their sedative effect.
39
Can muscle tone be reduced without losing coordination?
Yes, reduction may be achievable without obvious loss of coordination.
40
What is Diazepam used for in relation to muscle tone?
Treating skeletal muscle spasms from muscle strain and spasticity from degenerative disorders (MS, CP).
41
Which benzodiazepine is selectively anticonvulsant?
Clonazepam
42
Which benzodiazepine is used in the treatment of status epilepticus?
Diazepam
43
What does anterograde amnesia mean in patients using benzodiazepines?
It is the obliteration of any memory experienced while under BZD influence, allowing minor surgical procedures without unpleasant memories.
44
Which benzodiazepine is used intravenously in anesthesia and causes anterograde amnesia?
Midazolam
45
Which benzodiazepine is known for misuse due to its amnesic effects?
Flunitrazepam (Rohypnol).
46
What is the duration of action of benzodiazepines (BZDs)?
BZDs have variable durations: short-, medium-, and long-acting.
47
What is the consequence of BZDs having active metabolites?
They can cause cumulative effects and long hangovers if taken regularly.
48
Give an example of a BZD with active metabolites and its half-life.
Nordazepam (N-desmethyldiazepam)
with a half-life of 60 hours.
49
Why is the duration of action important when considering BZD side effects?
Because both short- and long-acting BZDs can cause day-after impairment of job performance and driving skills.
(Like a hangover)
50
What are common side effects of benzodiazepines (BZDs)?
• Drowsiness
• Confusion
• Amnesia
• Impaired coordination
• Enhancement of depressant effects of other drugs (e.g., alcohol)
51
What types of dependence can BZDs cause?
Both psychological (not as severe as with drugs of abuse) and physical dependence.
52
What symptoms may occur if BZDs are abruptly discontinued after prolonged high-dose use?
Anxiety, restlessness, insomnia, and tension.
53
Why is BZD withdrawal syndrome slower and less intense than that of barbiturates?
Because most BZDs have a long plasma half-life.
54
Why do short-acting benzodiazepines cause more severe withdrawal reactions?
Because they lead to more abrupt and severe withdrawal than long-acting ones.
Example: Triazolam (very short-acting), can cause withdrawal symptoms a few hours after a single dose.
55
True or False:
Triazolam, a very short-acting benzodiazepine, can cause withdrawal symptoms a few hours after a single dose.
True
56
What is Flumazenil and what is its duration of action?
Flumazenil is a benzodiazepine (BZD) antagonist with a similar structure to BZDs; it counteracts overdose and is short-acting (2 hours).
57
True or False:
Flumazenil counteracts benzodiazepine overdose and is short-acting with a duration of 2 hours.
True
58
When is Flumazenil used?
• When severe respiratory depression occurs
• To reverse the effects of BZDs after minor surgical procedures
• In treating comatose patients suspected to have overdosed on BZDs, even before diagnosis is confirmed
59
Which neurotransmitter pathways, besides GABA-ergic, are involved in anxiety and panic disorders?
5-HT (serotonin), NA (noradrenaline), and CCK (cholecystokinin).
60
What is the role of 5-HT in the CNS?
It acts as a neurotransmitter
61
Does 5-HT have only inhibitory effects in the CNS?
No, 5-HT has both inhibitory and excitatory effects depending on the receptor it acts on.
62
What is the function of 5-HT1 receptors?
They are inhibitory and act on presynaptic receptors to inhibit transmitter release from nerve terminals.
63
What are the roles of 5-HT (serotonin) in the CNS?
Appetite control, sleep, mood, hallucinations, stereotyped behaviour, pain perception, and vomiting.
64
What conditions are associated with disturbed 5-HT function?
Migraine, carcinoid syndrome, mood disorders, and anxiety.
65
What type of receptor is the 5-HT1A receptor?
A G-protein-coupled inhibitory autoreceptor located in the CNS.
66
What are the main effects of 5-HT1A receptor activation?
Neuronal inhibition and behavioural effects such as sleep, feeding, thermoregulation, and ANXIETY.
67
What is the intracellular mechanism following activation of the 5-HT1A receptor?
Inhibition of adenylate cyclase → decreased cAMP → no activation of protein kinases → reduced release of 5-HT and other mediators → overall inhibition of neurotransmission.
68
How does 5-HT1A receptor activation affect arousal reactions?
It inhibits the activity of noradrenaline locus coeruleus (NA L.C.) neurons, interfering with arousal reactions.
69
What is Buspirone used to treat?
Generalised anxiety disorders.
70
Can Buspirone be used to manage acute anxiety? Why or why not?
No, because it takes more than a week for effects to show.
71
What is the proposed mechanism of action of Buspirone?
Possibly by activating inhibitory presynaptic 5-HT1A receptors, reducing 5-HT and other mediators’ release.
72
Why is the mechanism of action of Buspirone considered unclear?
Because its effects take days to weeks to appear.
73
What are the side effects of Buspirone?
Dizziness, nausea, headache, and restlessness
74
Why is Buspirone considered less troublesome than benzodiazepines (BZDs)?
It causes no sedation, no loss of coordination, and no withdrawal signs even after abrupt discontinuation.
75
Does Buspirone potentiate the effects of conventional sedative-hypnotics, alcohol, or TCAs?
No, it does not potentiate their effects
76
Are elderly patients more sensitive to Buspirone than the general population?
No, they are not more sensitive
77
What is the recommended duration for Z-drugs (Zolpidem, Zaleplon, Zopiclone) use?
They should be used for a maximum of 4 weeks; long-term use is not recommended.
78
What is the proposed mechanism of action of Z-drugs?
Thought to act on a subgroup of the GABA-A receptor family, acting like BZDs to enhance membrane hyperpolarization.
79
What are Z-drugs primarily used to treat?
Sleep disorders, especially when falling asleep is difficult.
80
What are the effects of Z-drugs?
Rapid onset of hypnosis with few amnesic effects or day-after psychomotor depression or somnolence.
81
What are the side effects of Zolpidem and Zaleplon?
Nightmares, agitation, headache, G.I. upset, and dizziness.
82
What are the side effects of Zopiclone?
Taste alteration, impairment of driving skills, and palpitations (following withdrawal after prolonged use).
83
Which Z-drugs are associated with anterograde amnesia more than Zaleplon?
Zolpidem and Zopiclone
84
What are the toxic effects associated with Z-drugs?
Extensions of CNS depressant effects and dependence.
85
What type of drug interactions occur with Z-drugs?
Additive CNS depression with ethanol and many other drugs.
86
Have addiction and tolerance been observed with Z-drugs?
Yes, despite being considered better than BZDs in this regard, addiction and tolerance have been seen recently.
87
What happens when light stimulates the retina?
It triggers a nerve pathway from the retina to the hypothalamus.
88
What is the role of the SCN in the hypothalamus?
The SCN sends signals to control hormones, body temperature, and functions that regulate sleepiness or wakefulness.
89
How does the SCN act like a biological clock?
It sets patterns of activity throughout the body in response to light.
90
What happens in the body when the SCN detects light?
It raises body temperature, releases stimulating hormones like cortisol, and delays melatonin release.
91
When is melatonin released?
When it gets dark, as the SCN stops suppressing its release.
92
What role do melatonin and its receptors play in the body?
They are thought to help maintain circadian rhythms that regulate the sleep-wake cycle.
93
What is Ramelteon?
A newer hypnotic drug taken orally
94
What is the mechanism of action of Ramelteon?
It acts as an agonist at MT₁ and MT₂ (melatonin) receptors in the SCN in the CNS.
95
What is Ramelteon used for?
Sleep disorders, especially in patients who have trouble falling asleep.
96
What are the effects of Ramelteon on sleep?
It causes rapid onset of sleep with minimal rebound insomnia, no withdrawal symptoms, and no effects on sleep architecture.
97
What are the side effects of Ramelteon?
Important: Dizziness, somnolence, fatigue, endocrine changes
Extra : increased prolactin, and decreased testosterone.
98
What is Doxepin and how does it help with sleep?
Doxepin is a tricyclic antidepressant that blocks monoamine (MA) uptake (5-HT, NA). It helps people who have trouble staying asleep, possibly by blocking histamine receptors.
99
What is Trazodone and how does it aid sleep?
Trazodone is an atypical (mild) antidepressant that is very sedating. It initiates sleep and is thought to increase 5-HT in synapses by blocking uptake, though its MOA is unknown.
100
What is Mirtazapine’s role as a sleep aid?
Mirtazapine is an atypical antidepressant. Its sedative effect is due to potent antihistaminic activity at H1 receptors.
101
What is the role of fluoxetine, SSRIs, and mixed 5-HT/NA uptake inhibitors in anxiety?
They are used as antidepressants and are also efficacious in treating anxiety disorders and panic attacks.
