Anxiolytic and Hypnotic Drugs

Question 1

Define anxiety.

Answer 1

An unpleasant emotional state consisting of apprehension, tension, and feelings of danger without a real or logical cause.

Question 2

What are the physical symptoms seen with anxiety?

Answer 2

Tachycardia.
Tachypnea.
Sweating.
Trembling.
Weakness.

Question 3

How do benzodiazepines work, including details on their receptor subtypes and mechanism of action?

Answer 3

Benzodiazepines target GABA receptors.

Two benzodiazepine (BZ) receptor subtypes are commonly found in the CNS, designated as BZ1 and BZ2 receptors, depending on whether their composition includes the α1 subunit or the α2 subunit, respectively.

The binding of the benzodiazepine to its site on the GABA-A receptor increases the affinity of GABA to bind to the receptor. The BZ receptor locations in the CNS are parallel to those of the GABA neurons.

Binding of GABA to its receptor triggers an opening of a chloride channel, i.e., an increase in chloride influx, resulting in a hyperpolarization that moves the postsynaptic ptoential away from its firing threshold, thereby inhibiting the formation of action potentials.

So, in other words, benzodiazepines amplify the effect of GABA by increasing the frequency at which chloride channels open, thus enhancing GABA’s inhibitory action on neuronal activity.

Question 4

Do benzodiazepines bind on the same site on the GABA receptors as gaba itself?

Answer 4

No. Instead, BZs attach to a distinct allosteric binding site on the GABA receptor, which enhances the affinity of the inhibitory neurotransmitter GABA for the receptor, thus amplifying its inhibitory effect.

Question 5

Do benzodiazepines have antipsychotic activity or affect the autonomic nervous system?

Answer 5

No, benzodiazepines do not have antipsychotic activity, nor do they affect the autonomic nervous system.

Question 6

Where are GABA-A receptors found in the human body, and what are their subunits?

Answer 6

GABA-A receptors are present in the human body in various isforms, and each one contains a particular type of subunit: α1, α2, α3, and α5.

Question 7

What effects are produced upon the activation of different GABA-A receptor subunits?

Answer 7

The α1 subunit is associated with sedation, amnesia, and hypnosis.
The α2 and α3 subunits are associated with anxiolytic and muscle relaxant effects.
The α5 subunit is associated with memory impairment.

Question 8

How does the effect of benzodiazepines vary?

Answer 8

The effect of benzodiazepines depends mainly on the dose and subsequent selectivity.

Question 9

What is the primary effect of benzodiazepines at low doses, and which subunit do they act upon?

Answer 9

At low doses, benzodiazepines are anxiolytic, primarily acting on the α2 subunit.

Question 10

What type of amnesia is associated with benzodiazepine use and which subunit does it affect?

Answer 10

Benzodiazepines can cause anterograde amnesia, which is a temporary impairment of memory formation. This effect is linked to the α1 subunit.

Question 11

What are the sedative and hypnotic effects associated with benzodiazepines, and how do these effects change with higher dosages?

Answer 11

Benzodiazepines are known for their sedative and hypnotic actions; they all possess some sedative properties, and at higher doses, some can produce hypnosis, which is an artificially induced sleep. These effects are associated with the α1 subunit.

Question 12

In addition to their sedative and hypnotic effects, what role do benzodiazepines play in the treatment of seizure disorders, and which receptor subunit is primarily involved in this action?

Answer 12

Several benzodiazepines have anticonvulsant activity and are utilized in the treatment of epilepsy, including status epilepticus, as well as other seizure disorders.

This therapeutic effect is due to their affinity for the α1 subunit of the GABA-A receptor.

Question 13

What is the effect of high doses of benzodiazepines on skeletal muscle, and which GABA-A receptor subunit do they primarily interact with to produce this effect?

Answer 13

At high doses, benzodiazepines act as muscle relaxants, alleviating spasticity of skeletal muscle. This effect is primarily mediated through the α2 subunit of the GABA-A receptor.

Question 14

How are benzodiazepines classified based on their duration of action?

Answer 14

Benzodiazepines are classified into three categories based on the duration of their action:
1. Long-acting.
2. Intermediate-acting.
3. Short-acting.

Question 15

Why is the half-life of benzodiazepines clinically important?

Answer 15

The half-lives of benzodiazepines are very important clinically because the duration of action of the drug may determine its therapeutic usefulness.

Different durations of action are suitable for different clinical situations and treatment goals.

Question 16

Do individual benzodiazepines differ significantly in their therapeutic effects?

Answer 16

The individual benzodiazepines exhibit small differences in their relative anxiolytic, anticonvulsant, and sedative properties, which can influence their specific therapeutic uses.

Question 17

In what types of anxiety disorders are benzodiazepines indicated?

Answer 17

Benzodiazepines should not be used to alleviate normal everyday stress because they are intended for the treatment of severe and continuous anxiety disorders and are not appropriate for the normal fluctuations in stress that people experience regularly.

Benzodiazepines are indicated for severe and continuous anxiety, including generalized anxiety disorder, social anxiety, performance anxiety, and post-traumatic stress disorder (PTSD).

Question 18

Why should benzodiazepines not be used for long durations?

Answer 18

Benzodiazepines should not be used for long durations because they may cause addiction and lead to dependence.

Question 19

Why are longer-acting benzodiazepines, such as clonazepam, diazepam, often preferred for prolonged treatment of anxiety disorders?

Answer 19

Longer-acting agents like clonazepam and diazepam are often preferred for prolonged treatment because they are less addictive than short-acting benzodiazepines and are less likely to lead to tolerance.

Question 20

Why are the anti-anxiety effects of benzodiazepines less subject to tolerance than their sedative and hypnotic effects?

Answer 20

The anti-anxiety effects of benzodiazepines are less subject to tolerance than the sedative and hypnotic effects because a lower dose is typically sufficient to alleviate anxiety, reducing the risk of tolerance development.

Question 21

What happens when benzodiazepines are used for more than two weeks?

Answer 21

When benzodiazepines are used for more than two weeks, tolerance can occur due to a decrease in GABA receptor density.

Question 22

What is cross-tolerance in the context of benzodiazepines?

Answer 22

Cross-tolerance exists among benzodiazepines and other central nervous system depressants like ethanol, chlordiazepoxide, meaning tolerance to one can lead to tolerance to the others.

Question 23

How do benzodiazepines interact with alcohol?

Answer 23

Benzodiazepines potentiate the effects of alcohol, leading to additive central nervous system depression.

Question 24

What is the efficacy of alprazolam for panic disorders, and what is a notable risk?

Answer 24

Alprazolam is effective for short-term and long-term treatment of panic disorders but may cause withdrawal reactions in about 30 percent of sufferers.

Question 25

What is diazepam's role in the treatment of muscular disorders?

Answer 25

Diazepam is useful in the treatment of skeletal muscle spams, which may occur in conditions like muscle strain. It is also used in treating spasticity resulting from degenerative disorders, such as multiple sclerosis and cerebral palsy.

Question 26

What is the purpose of using shorter-acting benzodiazepines in medical procedures?

Answer 26

Shorter-acting benzodiazepines are used before unpleasant medical procedures, such as endoscopic, bronchoscopic, and certain dental procedures like angioplasty, to induce conscious sedation, helping patients to relax while still being able to respond to stimuli.

Question 27

Which benzodiazepine is commonly used for the induction of anesthesia and how is it administered?

Answer 27

Midazolam, which is an injectable-only benzodiazepine, is commonly used for the induction of anesthesia.

Question 28

Which benzodiazepines are considered the drugs of choice for terminating grand-mal epileptic seizures and status epilepticus?

Answer 28

Diazepam and lorazepam.

Question 29

How do certain benzodiazepines contribute to the treatment of alcohol and barbiturate withdrawal?

Answer 29

Due to cross-tolerance, benzodiazepines such as chlordiazepoxide, clorazepate, diazepam, and oxazepam are useful in the acute treatment of alcohol and barbiturate withdrawal and in reducing the risk of withdrawal-related seizures.

Question 30

How does an organism's sleep cycle alternate, and what are the characteristics of REM sleep?

Answer 30

In the sleep cycle, an organism alternates between deep sleep (which has slow, large brain waves) and rapid eye movement (REM) sleep (which has faster brain waves). REM sleep is a unique phase of mammalian sleep characterized by: 1. Random movement of the eyes. 2. Low muscle tone throughout the body. 3. A propensity for the sleeper to dream vividly. 4. Quickly changing and often irregular heart rate, blood pressure, cardiac output, arterial pressure, and breathing rate.

Question 31

Are all benzodiazepines effective as hypnotic agents for sleep disorders?

Answer 31

Not all benzodiazepines are useful as hypnotic agents, although they all have sedative or calming effects, which is an important consideration for their use in sleep disorders.

Question 32

What effects do benzodiazepines tend to have on the sleep cycle?

Answer 32

A. Decrease the latency to sleep onset, meaning they help individuals fall asleep more quickly. B. Increase stage II of non-rapid eye movement (NREM) sleep. However, the duration of both REM sleep and slow-wave sleep are decreased.

Question 33

Why is it important to balance the sedative effects of benzodiazepines at bedtime with their effects upon waking?

Answer 33

It is important to balance the sedative effect needed at bedtime with the hangover effect upon waking because long-acting benzodiazepines can lead to more pronounced hangover effects, which may impair cognitive and motor functions the following day.

Question 34

Why might non-benzodiazepine hypnotic drugs be preferred for treating sleep disorders?

Answer 34

Non-benzodiazepine hypnotic drugs such as zolpidem and zaleplon are preferable as hypnotics for sleep disorders because they do not significantly alter sleep stages, thereby reducing the likelihood of hangover effects and preserving the natural structure of sleep.

Question 35

Which benzodiazepines are commonly prescribed for sleep disorders and what is their mechanism of action?

Answer 35

Commonly prescribed benzodiazepines for sleep disorders include the long-acting flurazepam, intermediate-acting temazepam, and short-acting triazolam. Their mechanism of action involves targeting the BZ1 receptor, which contributes to their sedative effects.

Question 36

Why is flurazepam considered a long-acting benzodiazepine for sleep disorders?

Answer 36

Flurazepam is considered a long-acting benzodiazepine for sleep disorders due to its active metabolite, which has a long half-life. This pharmacological feature contributes to its effects on sleep, such as reducing sleep-induction time, decreasing the number of awakenings, and increasing the total duration of sleep.

Question 37

What are the potential advantages and disadvantages of using flurazepam?

Answer 37

The potential advantages of using flurazepam include its ability to reduce sleep-induction time and the number of awakenings, as well as increasing the duration of sleep, with little rebound insomnia reported. However, a disadvantage may be daytime sedation and the accumulation of the drug due to its long half-life, which can lead to hangover effects or cumulative sedation.

Question 38

For which type of sleep disorder is temazepam particularly useful?

Answer 38

Temazepam is particularly useful for patients who experience frequent awakening, as it has an intermediate duration of action. It is beneficial for insomnia characterized by the inability to stay asleep.

Question 39

When should temazepam be administered in relation to bedtime, and why?

Answer 39

Temazepam should be administered 1 to 2 hours before the desired bedtime. This timing is recommended because the peak sedative effect occurs 1 to 3 hours after an oral dose. However, it is noted that temazepam delays the onset of action and does not decrease the latency to fall asleep.

Question 40

What characteristic of triazolam's action makes it suitable for treating certain sleep disorders?

Answer 40

Triazolam has a relatively short duration of action, making it suitable for inducing sleep (decreasing sleep latency) in patients with recurring insomnia, particularly those who have difficulty falling asleep.

Question 41

What should be considered when prescribing triazolam due to its potency and the risk of tolerance?

Answer 41

When prescribing triazolam, it's important to consider that tolerance to this potent drug can develop quickly, often within a few days. Withdrawal from the drug can result in rebound insomnia. To avoid tolerance, triazolam should be prescribed for intermittent rather than daily use and should not be used for more than two weeks.

Question 42

How are benzodiazepines absorbed and distributed in the body?

Answer 42

Benzodiazepines are lipophilic, meaning they can easily dissolve in fats, which allows them to be rapidly and completely absorbed after oral administration and distributed throughout the body.

Question 43

What is the fate of most benzodiazepines in terms of metabolism?

Answer 43

Most benzodiazepines are metabolized by the hepatic microsomal enzyme system, including cytochrome P450 isozymes, to compounds that are also active, contributing to a longer duration of action.

Question 44

Why are lorazepam and oxazepam preferred in patients with liver dysfunction?

Answer 44

In patients with liver dysfunction, lorazepam and oxazepam, which are metabolized extrahepatically (outside the liver), are less likely to cause excessive central nervous system (CNS) depression and are therefore preferred for use as preanesthetic sedation in these patients.

Question 45

How is the effect of benzodiazepines terminated in the body?

Answer 45

The effect of benzodiazepines is not terminated solely by excretion but also by redistribution within the body. This is why sometimes the clinical effect is not directly correlated with the half-life of the drug.

Question 46

Can benzodiazepines be used during pregnancy and lactation?

Answer 46

Benzodiazepines cross the placenta and are excreted in breast milk, which is why they are generally not recommended for use by pregnant individuals or breastfeeding women.

Question 47

What can result from the administration of high doses of potent benzodiazepines over a prolonged period?

Answer 47

Administration of high doses of potent benzodiazepines over a prolonged period can lead to both psychological (such as restlessness, headache, insomnia) and physical dependence (which includes more serious disturbances).

Question 48

What are the symptoms of withdrawal after abrupt discontinuation of benzodiazepines?

Answer 48

Symptoms of withdrawal from benzodiazepines can include confusion, anxiety, agitation, restlessness, insomnia, tension, and rarely, seizures.

Question 49

How do the withdrawal reactions of benzodiazepines with short half-lives compare to those with long half-lives?

Answer 49

Benzodiazepines with short half-lives, like triazolam (one of the most potent benzodiazepines), can induce more abrupt and severe withdrawal reactions than those seen with drugs that are slowly eliminated, such as flurazepam. More potent and rapidly eliminated drugs are associated with more frequent and severe withdrawal problems.

Question 50

What are some common adverse effects associated with benzodiazepines?

Answer 50

At high doses, benzodiazepines can cause ataxia, which affects activities that require fine motor coordination, such as driving. Benzodiazepines can lead to cognitive impairment, including decreased long-term recall of new knowledge.

Question 51

What precautions should be considered when prescribing benzodiazepines?

Answer 51

When prescribing benzodiazepines, the following precautions should be considered: Patients with liver disease, as their ability to metabolize the drug may be impaired. Acute narrow-angle glaucoma, because benzodiazepines can exacerbate this condition. Concurrent use with alcohol and other central nervous system depressants should be avoided due to the risk of enhanced sedative effects, which can be dangerous.

Question 52

What is flumazenil and what is its primary use?

Answer 52

Flumazenil is a GABA-A receptor antagonist that can rapidly reverse the effects of benzodiazepines. It is used intravenously and has a rapid onset of action. It's typically used in acute care settings to reverse benzodiazepine sedation, often in cases of overdose.

Question 53

Why is flumazenil not used as a treatment for benzodiazepine dependency?

Answer 53

Flumazenil has a short duration of action and most benzodiazepines have intermediate to long durations of action. Due to its short-lived effect, flumazenil is not suitable as a treatment for benzodiazepine dependency but can be used in diagnosis.

Question 54

What are the risks associated with the use of flumazenil?

Answer 54

Flumazenil may precipitate withdrawal in dependent patients or cause seizures if a benzodiazepine is used to control seizure activity, because it can rapidly reverse the effects of benzodiazepines.

Question 55

Which antidepressants are used to treat chronic anxiety?

Answer 55

Selective serotonin reuptake inhibitors (SSRIs), such as escitalopram or paroxetine, and selective serotonin and norepinephrine reuptake inhibitors (SNRIs), such as venlafaxine or duloxetine, are alternative agents used in the long-term management of chronic anxiety.

Question 56

Why should SSRIs and SNRIs be considered as first-line treatments for anxiety?

Answer 56

SSRIs and SNRIs should be considered as first-line treatments for anxiety, especially in patients with concerns for addiction or dependence, as they have a lower potential for abuse compared to benzodiazepines.

Question 57

What is the mechanism of action of buspirone?

Answer 57

Buspirone acts primarily through the activation of the serotonin receptor 5HT1A and has some affinity for the dopamine DA2 receptor.

Question 58

For what condition is buspirone typically used?

Answer 58

Buspirone is used in the treatment of generalized anxiety disorder and is intended for chronic use.

Question 59

How does the efficacy of buspirone as an anxiolytic compare to benzodiazepines?

Answer 59

The efficacy of buspirone as an anxiolytic agent is comparable to that of benzodiazepines, although it has a different mode of action.

Question 60

Is buspirone effective for short-term or "as-needed" treatment of anxiety?

Answer 60

No, buspirone is not effective for short-term or "as-needed" treatment of acute anxiety states due to its slow onset of action.

Question 61

What are the advantages of buspirone compared to benzodiazepines?

Answer 61

The advantages of buspirone over benzodiazepines include: Minimal sedation, psychomotor, and cognitive dysfunction. Unlikelihood of developing dependence. Minimal tolerance. Lack of potentiation of the central nervous system (CNS) depression of alcohol.

Question 62

What are the disadvantages of using buspirone?

Answer 62

The disadvantages of buspirone are: Its slow onset of action makes it ineffective for the acute treatment of anxiety. It lacks the anticonvulsant and muscle-relaxant properties of benzodiazepines.

Question 63

How do barbiturates interact with GABA receptors?

Answer 63

Barbiturates interact with GABA receptors, specifically enhancing GABAergic transmission. This interaction increases the duration of chloride channel opening, which results in an increased influx of chloride ions and greater neuronal inhibition.

Question 64

How is the binding site of barbiturates related to that of benzodiazepines on GABA receptors?

Answer 64

The binding site for barbiturates on GABA receptors is distinct from that of benzodiazepines. While benzodiazepines bind to their own specific site on the GABA_A receptor, barbiturates bind to a separate site, and their binding leads to different effects on the receptor function.

Question 65

Apart from affecting GABA receptors, what other action do barbiturates have?

Answer 65

Barbiturates can also block excitatory glutamate receptors. Additionally, at anesthetic concentrations, drugs like pentobarbital can block high-frequency sodium channels, contributing to their overall CNS depressant effects.

Question 66

In what ways are barbiturates considered stronger and more effective than benzodiazepines, and what are their safety concerns?

Answer 66

Barbiturates are considered stronger and more effective than benzodiazepines in their sedative and hypnotic effects. However, they have a lower safety profile compared to benzodiazepines, which includes a higher risk of overdose and lower therapeutic index.

Question 67

Why have barbiturates been replaced by benzodiazepines in clinical practice?

Answer 67

Barbiturates have been replaced by benzodiazepines because they induce rapid and more significant tolerance, stimulate the production of drug-metabolizing enzymes, leading to variable levels of drug in the blood, are associated with a higher risk of physical dependence, can cause more severe withdrawal symptoms upon discontinuation, and have the potential to produce coma at toxic doses, posing a higher risk of fatal overdose.

Question 68

What are the differences in the duration of action among barbiturates, and for what purposes are they used?

Answer 68

Barbiturates are categorized based on their duration of action into long-acting, short-acting, and ultra-short-acting. Long-acting barbiturates like phenobarbital have effects that last for 1-2 days and are useful in the treatment of seizures. Short-acting barbiturates such as pentobarbital, secobarbital, and amobarbital last for 3-8 hours and are useful as sedatives and hypnotics but are not typically used as anxiolytics. Ultra-short-acting barbiturates like thiopental have an action lasting around 20 minutes and are used intravenously for the induction of anesthesia; they are commonly used barbiturates for this purpose.

Question 69

How does the effect of barbiturates on the central nervous system (CNS) vary with dosage?

Answer 69

The effect of barbiturates on the CNS depends on the dose. At low doses, barbiturates produce sedation, calming the individual and reducing excitation. At higher doses, they induce hypnosis followed by anesthesia, resulting in a loss of sensation. Even higher doses can lead to coma and death.

Question 70

What are the consequences of chronic use of barbiturates?

Answer 70

Chronic use of barbiturates leads to the development of tolerance, and they can produce stronger dependence compared to benzodiazepines.

Question 71

Do barbiturates have analgesic properties?

Answer 71

No, barbiturates do not have analgesic properties, which is similar to benzodiazepines.

Question 72

What impact do barbiturates have on respiration?

Answer 72

Barbiturates can cause respiratory depression by suppressing the hypoxic and chemoreceptor response to CO2. An overdose can lead to significant respiratory depression and death.

Question 73

What is the effect of barbiturates on liver enzymes?

Answer 73

Barbiturates induce the activity of cytochrome P450 (CYP450) enzymes, which increases the metabolism of other drugs that are metabolized by CYP450, potentially decreasing the effects of these other drugs.

Question 74

For what purposes are ultra-short-acting barbiturates used?

Answer 74

Ultra-short-acting barbiturates, such as thiopental, are used intravenously to induce anesthesia.

Question 75

What are the therapeutic uses of phenobarbital?

Answer 75

Phenobarbital is used for the long-term management of tonic-clonic seizures, status epilepticus, eclampsia, and febrile seizures. It is the drug of choice for treating young children with recurrent febrile seizures.

Question 76

Why should phenobarbital be used with caution in children and adults?

Answer 76

Phenobarbital should be used with caution in children and adults because it can suppress cognitive development in children and cognitive performance in adults.

Question 77

How do barbiturates relieve anxiety?

Answer 77

Barbiturates can relieve anxiety, nervous tension, and insomnia because they act as mild sedatives.

Question 78

What effects do barbiturates have as hypnotics on sleep?

Answer 78

As hypnotics, barbiturates suppress REM sleep more than other stages of sleep. They decrease sleep latency (the time it takes to fall asleep), the number of awakenings, and the duration of REM sleep.

Question 79

How are barbiturates absorbed and distributed in the body?

Answer 79

Barbiturates are absorbed orally and distributed widely throughout the body.

Question 80

What does the redistribution of barbiturates from the brain to other tissues indicate?

Answer 80

The redistribution of barbiturates from the brain to other tissues leads to a decrease in the duration of action. This is one reason why thiopental, for instance, has a short duration of action despite its potent effects.

Question 81

Why should barbiturates not be used during pregnancy?

Answer 81

Barbiturates should not be used during pregnancy because they can cross the placenta and may depress the fetus, potentially causing respiratory depression.

Question 82

How are barbiturates metabolized and excreted?

Answer 82

Barbiturates are metabolized in the liver, and the inactive metabolites are excreted in the urine.

Question 83

What are the central nervous system (CNS) adverse effects of barbiturates?

Answer 83

The CNS adverse effects of barbiturates include drowsiness, impaired concentration, and mental and physical sluggishness. Barbiturates also have a synergistic CNS depressant effect with alcohol.

Question 84

What is the 'drug hangover' effect associated with barbiturates?

Answer 84

The 'drug hangover' effect refers to the feeling of tiredness after the patient awakes from the hypnotic doses of barbiturates.

Question 85

Why should precautions be taken with chronic use of phenobarbital, especially in women who take oral contraceptives?

Answer 85

Chronic use of phenobarbital increases the activity of hepatic drug-metabolizing enzymes, including CYP450, which may decrease the duration of action of other drugs, including oral contraceptives. Therefore, extra protective procedures must be taken by women on anti-epileptic phenobarbital who use oral contraceptives.

Question 86

Why are barbiturates contraindicated in patients with acute intermittent porphyria?

Answer 86

Barbiturates are contraindicated in patients with acute intermittent porphyria because they increase the synthesis of porphyrin precursors. Barbiturates induce other enzymes, notably δ-aminolevulinic acid (ALA) synthetase, which is involved in porphyrin production. An increased amount of porphyrin can cause dysfunction of the CNS and potentially lead to coma and death.

Question 87

How does physical dependence on barbiturates compare to that on benzodiazepines?

Answer 87

Physical dependence on barbiturates is generally more severe than on benzodiazepines.

Question 88

What are the symptoms associated with abrupt withdrawal from barbiturates?

Answer 88

Abrupt withdrawal from barbiturates may cause tremors, anxiety, weakness, restlessness, nausea and vomiting, seizures, delirium, and in severe cases, cardiac arrest.

Question 89

What is the leading cause of death from barbiturate overdose?

Answer 89

The leading cause of death from barbiturate overdose is poisoning due to severe respiratory and central cardiovascular depression, leading to a shock-like condition with shallow, infrequent breathing.

Question 90

How is barbiturate poisoning treated?

Answer 90

Treatment of barbiturate poisoning includes: 1. Hemodialysis to remove the drug from the bloodstream. 2. Artificial respiration to support breathing and purging of the stomach to remove any unabsorbed drug. 3. Alkalization of the urine with sodium bicarbonate to enhance the excretion of the drug.

Question 91

Is zolpidem a benzodiazepine?

Answer 91

No, zolpidem is not a benzodiazepine. It does not have the same chemical structure as benzodiazepines.

Question 92

How does zolpidem act pharmacologically?

Answer 92

Zolpidem acts on a subset of the benzodiazepine receptor family, specifically the BZ1 receptor.

Question 93

What are the onset and duration of action for zolpidem?

Answer 93

Zolpidem has a rapid onset of action, which decreases the latency of getting sleep, and it is known for its long duration of action.

Question 94

Does zolpidem have anticonvulsant or muscle-relaxing properties?

Answer 94

No, zolpidem does not have anticonvulsant or muscle-relaxing properties.

Question 95

Does zolpidem affect REM sleep?

Answer 95

Zolpidem does not significantly suppress REM sleep, meaning it has minimal effect on sleep architecture.

Question 96

What are the withdrawal effects of zolpidem?

Answer 96

Zolpidem has few withdrawal effects and exhibits minimal rebound insomnia and little or no tolerance.

Question 97

How does the risk of tolerance and dependence with zolpidem compare to benzodiazepines?

Answer 97

The risk of tolerance and dependence with zolpidem is less than with benzodiazepines.

Question 98

What are the adverse effects of zolpidem?

Answer 98

Adverse effects of zolpidem include nightmares, agitation, headache, gastrointestinal upset, dizziness, and ataxia.

Question 99

How does zaleplon compare to zolpidem?

Answer 99

Zaleplon is very similar to zolpidem in its hypnotic effects.

Question 100

Why does zaleplon cause fewer residual effects on psychomotor and cognitive functions than zolpidem or benzodiazepines?

Answer 100

Zaleplon causes fewer residual effects on psychomotor and cognitive functions because of its rapid elimination from the body due to its short half-life.

Question 101

What is the half-life of zaleplon, and how does it influence tolerance?

Answer 101

Zaleplon has a short half-life, which contributes to minimal tolerance when used over a 5-week period.

Question 102

What type of medication is Eszopiclone?

Answer 102

Eszopiclone is a non-benzodiazepine hypnotic medication.

Question 103

How does Eszopiclone work?

Answer 103

Eszopiclone works by acting on the benzodiazepine binding site situated on GABA neurons as an agonist, similar to the mechanism of zolpidem and zaleplon.

Question 104

What is Eszopiclone used to treat?

Answer 104

Eszopiclone is used for treating sleeping problems, specifically symptoms such as difficulty falling asleep and difficulty staying asleep during the night.

Question 105

What is the elimination half-life of Eszopiclone?

Answer 105

The elimination half-life of Eszopiclone is approximately 6 hours.

Question 106

What are the adverse effects of Eszopiclone?

Answer 106

Adverse effects of Eszopiclone can include anxiety, dry mouth, headache, peripheral edema, somnolence (sleepiness), and an unpleasant taste. Eszopiclone may cause drowsiness or dizziness and can potentiate the alcohol effect, meaning it can increase the effects of alcohol.

Question 107

Is there a development of tolerance with the use of Eszopiclone?

Answer 107

Minimal tolerance was observed with the use of Eszopiclone over a 6-month period.

Question 108

What is Ramelteon?

Answer 108

Ramelteon is a selective agonist at the MT1 and MT2 subtypes of melatonin receptors.

Question 109

Where do Ramelteon's targeted receptors reside?

Answer 109

The MT1 and MT2 receptors that Ramelteon targets are located in the suprachiasmatic nucleus (SCN) of the brain.

Question 110

What role does melatonin play in relation to Ramelteon?

Answer 110

Melatonin is known as the hormone of sleep. It stimulates MT1 and MT2 receptors, which Ramelteon also targets, to induce sleep and is involved in maintaining the circadian rhythms that regulate the sleep-wake cycle.

Question 111

How is melatonin produced in the body?

Answer 111

Melatonin is produced by the pineal gland during periods of darkness.

Question 112

Does Ramelteon have any direct effect on GABAergic neurotransmission?

Answer 112

No, Ramelteon does not have a direct effect on GABAergic neurotransmission.

Question 113

What is Ramelteon used to treat?

Answer 113

Ramelteon is used in the treatment of insomnia, particularly when the primary complaint is difficulty falling asleep, which is known as increased sleep latency.

Question 114

Why can Ramelteon be administered for a long time?

Answer 114

Ramelteon can be administered for an extended period because it has minimal potential for abuse, withdrawal, dependence, and tolerance, and it does not cause rebound insomnia.

Question 115

What effect does Ramelteon have on prolactin levels and ovulation?

Answer 115

Ramelteon can increase prolactin levels from the pituitary gland, which may inhibit the menstrual cycle and consequently ovulation.