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Pharma > MIDTERMS: Sedative Hypnotic, Anti-depressants, CNS > Flashcards

MIDTERMS: Sedative Hypnotic, Anti-depressants, CNS Flashcards

1
Q

What are the clinical uses of sedative-hypnotics?

A

Hypnosis (inducing sleep)
Sedation (calming or reducing agitation)
Anxiolysis (reducing anxiety)
Anti-seizures (seizure control)

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2
Q

How do older sedative-hypnotics differ from newer agents in terms of dose-response curves?

A

Older sedative-hypnotics like barbiturates have steeper dose-response curves, leading to higher risks of toxicity, while newer agents (e.g., benzodiazepines, melatonin receptor agonists) tend to have safer, more manageable dose-response profiles.

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3
Q

What are the six different types of sedative-hypnotics?

A

Benzodiazepines
Barbiturates
Melatonin Receptor Agonists
5-HT Receptor Agonists
New Hypnotics (e.g., Zolpidem, Zaleplon, Eszopiclone)
Other Agents

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3
Q

What is a key difference between barbiturates and benzodiazepines regarding enzyme induction?

A

Long-term use of barbiturates can induce enzyme activity, hastening their own metabolism and that of other drugs. This is not seen with benzodiazepines and newer agents.

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4
Q

What is important to consider when dosing newer hypnotics (e.g., Zolpidem, Zaleplon, Eszopiclone)?

A

Dose reductions are required in liver disease and elderly patients. Drug levels can be raised by CYP450 inhibitors and lowered by inducers.

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4
Q

What is a major kinetic feature of sedative-hypnotics that affects their absorption rate and CNS entry?

A

Lipophilicity is a major factor that influences the absorption rate and entry into the CNS.

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5
Q

Name the intermediate-acting benzodiazepines.

A

Alprazolam
Estazolam
Lorazepam
Temazepam

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5
Q

How are benzodiazepines metabolized?

A

Benzodiazepines undergo CYP3A4 oxidation followed by conjugation. Phase 1 metabolites are active and may have longer half-lives (e.g., Desmethyldiazepam).

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5
Q

What effect does Zolpidem have on sleep?

A

Decreases REM sleep
Minimal effect on slow wave sleep

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5
Q

What is unique about phenobarbital’s excretion compared to other barbiturates?

A

Phenobarbital has 25% excreted unchanged, and its elimination can be influenced by changes in urine pH.

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6
Q

List the long-acting benzodiazepines.

A

Diazepam
Clonazepam
Chlorazepate
Flurazepam
Quazepam

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6
Q

What are the effects of Eszopiclone on sleep?

A

Increases total sleep time, especially stage 2
Decreases REM sleep (at high doses)

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6
Q

Which sedative-hypnotics are classified as short-acting?

A

Midazolam
Oxazepam
Triazolam

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7
Q

What effects are associated with low doses of sedative-hypnotics?

A

Anxiolytic effects
Decreased cognitive and psychomotor functions
Behavioral disinhibition
Anterograde amnesia

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7
Q

How do higher doses of benzodiazepines and older drugs affect the sleep cycle?

A

Reduction of sleep onset latency
Increase in stage 2 NREM sleep
Decrease in duration of REM sleep and stage 4

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8
Q

What are the effects of Zaleplon on sleep?

A

Decreases sleep onset latency
Minimal effect on total sleep time, NREM, and REM

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9
Q

True or False: Zolpidem has anticonvulsant and muscle-relaxing effects similar to benzodiazepines.

A

False (Zolpidem has no anticonvulsant or muscle-relaxing effects)

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9
Q

True or False: Antihistamines such as hydroxyzine and diphenhydramine are commonly used as sedatives before surgery due to their ability to cross the blood-brain barrier.

A

True

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9
Q

True or False: Benzodiazepines at hypnotic doses are less likely to cause anterograde amnesia compared to newer agents.

A

False. Benzodiazepines at hypnotic doses can cause anterograde amnesia, which is less common with newer agents.

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9
Q

True or False: Benzodiazepines are recommended for long-term management of generalized anxiety disorder due to their low risk of tolerance and dependence.

A

False. Benzodiazepines are not recommended for long-term management due to the risk of tolerance, addiction, and dependence. SSRIs are considered safer for long-term use.

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10
Q

True or False: Long-term use of barbiturates can induce enzyme activity, accelerating their own metabolism and that of other drugs.

A

True. Long-term use of barbiturates can induce enzyme activity, leading to faster metabolism.

10
Q

True or False: Flumazenil is a benzodiazepine agonist that is used to reverse the effects of benzodiazepine overdose.

A

False (Flumazenil is a benzodiazepine antagonist)

11
Q

True or False: Buspirone has a high potential for dependence and significant sedative effects.

A

False (Buspirone has minimal sedation and low risk of dependence)

11
Q

T or F
Benzodiazepines bind to the GABA 𝐴
Areceptor and increase the frequency of opening of chloride ion channels, leading to hyperpolarization.

A

True

12
Q

True or False: Barbiturates can induce liver enzymes, leading to a decrease in the concentration of certain drugs.

A

True

12
Q

True or False: Barbiturates increase the duration of chloride ion channel opening, leading to CNS depression.

A

True

13
Q

Match the drug to its primary effect:

Zolpidem
Diazepam
Flumazenil
Buspirone
a) Muscle relaxation and anticonvulsant activity
b) Competitive antagonist at the GABA-A receptor
c) Hypnotic effect with minimal withdrawal
d) Partial serotonin receptor agonist

A

Zolpidem → c) Hypnotic effect with minimal withdrawal
Diazepam → a) Muscle relaxation and anticonvulsant activity
Flumazenil → b) Competitive antagonist at the GABA-A receptor
Buspirone → d) Partial serotonin receptor agonist

13
Q

True or False: Benzodiazepines are indicated for long-term management of generalized anxiety disorder.

A

False (Benzodiazepines are not recommended for long-term use due to the risk of tolerance, dependence, and addiction)

13
Q

True or False: Zolpidem causes significant withdrawal effects and develops a high level of tolerance with prolonged use.

A

False (Zolpidem has minimal withdrawal effects and little or no tolerance development)

13
Q

True or False: First-generation antihistamines like diphenhydramine can cause sedation due to their ability to cross the blood-brain barrier.

A

True

13
Q

Which drug is commonly used to reverse the CNS depressant effects of benzodiazepine overdose?
a) Zolpidem
b) Flumazenil
c) Buspirone
d) Diazepam

A

b) Flumazenil

13
Q

Buspirone binds to serotonin and dopamine receptors and acts as a partial __________ receptor agonist.

A

serotonin

13
Q

What is the primary difference between sedative agents and hypnotic agents?

A

Sedative agents reduce anxiety and exert a calming effect, while hypnotic agents produce drowsiness and encourage the onset and maintenance of sleep. Hypnotic agents cause more pronounced CNS depression than sedative agents.

14
Q

Which of the following is an adverse effect associated with Monoamine Oxidase Inhibitors (MAOIs)?
a) Orthostatic hypotension
b) Weight gain
c) Increased seizure threshold
d) None of the above

A

a) Orthostatic hypotension

14
Q

Which of the following drugs binds to the GABA-A receptor and increases the frequency of chloride channel opening?
a) Barbiturates
b) Zolpidem
c) Benzodiazepines
d) Buspirone

A

c) Benzodiazepines

14
Q

The adverse effect known as “serotonin syndrome” can occur when two or more __________ are taken concurrently.

A

antidepressants

15
Q

The main inhibitory neurotransmitter in the central nervous system is __________.

A

GABA (gamma-aminobutyric acid)

15
Q

Which of the following is an advantage of Zolpidem compared to traditional benzodiazepines?
a) It has anticonvulsant properties.
b) It causes significant dependence.
c) It has minimal withdrawal effects.
d) It induces microsomal liver enzymes.

A

c) It has minimal withdrawal effects.

16
Q

Why should rehabilitation sessions be carefully scheduled for patients taking sedative-hypnotics or anxiolytic agents?

A

Rehabilitation sessions should be scheduled to avoid the period several hours after taking these medications, as they may increase the risk of falls and trauma (e.g., hip fractures) due to sedation and impaired coordination.

17
Q

T or F
Tricyclic antidepressants (TCAs) can be used for prolonged treatment of depression without losing efficacy.

A

True

17
Q

Which theory suggests that depression results from a deficiency of monoamines?
a) Cognitive-behavioral theory
b) Amine theory
c) Dopamine hypothesis
d) Serotonin syndrome

A

b) Amine theory

17
Q

Which class of antidepressant drugs works by inhibiting the neuronal reuptake of norepinephrine and serotonin, while also blocking serotonergic, α-adrenergic, histamine, and muscarinic receptors?
a) Selective serotonin reuptake inhibitors (SSRIs)
b) Tricyclic antidepressants (TCAs)
c) Monoamine oxidase inhibitors (MAOIs)
d) Lithium salts

A

b) Tricyclic antidepressants (TCAs)

18
Q

Selective Serotonin Reuptake Inhibitors (SSRIs) selectively inhibit __________ reuptake.

A

serotonin

19
Q

Match the drug to its adverse effect:

Tricyclic Antidepressants (TCAs)
Monoamine Oxidase Inhibitors (MAOIs)
Selective Serotonin Reuptake Inhibitors (SSRIs)
Lithium salts
a) Hypertension when combined with tyramine
b) Sedation and muscle weakness
c) Sexual dysfunction and weight loss
d) Orthostatic hypotension and reflex tachycardia

A

Tricyclic Antidepressants (TCAs) → d) Orthostatic hypotension and reflex tachycardia
Monoamine Oxidase Inhibitors (MAOIs) → a) Hypertension when combined with tyramine
Selective Serotonin Reuptake Inhibitors (SSRIs) → c) Sexual dysfunction and weight loss
Lithium salts → b) Sedation and muscle weakness

19
Q

What is the mechanism of action of Monoamine Oxidase Inhibitors (MAOIs) in treating depression?

A

MAOIs work by inhibiting the enzyme monoamine oxidase, which deaminates and inactivates excess neurotransmitters (NT), allowing NTs like serotonin and norepinephrine to remain active in the synaptic cleft for longer periods, leading to an antidepressant effect.

19
Q

T or F
Lithium salts are commonly used in the prophylaxis of manic-depressive episodes but have a very wide therapeutic window.

A

False (They have a very narrow therapeutic window.)

19
Q

What nonpharmacological interventions can be beneficial for patients with depression?

A

Regular exercise, counseling, support groups, and cognitive-behavior specialists.

20
Q
A
21
Q
A
22
Q
A

Pharma (13 decks)

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