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Questions and Answers
What is a common side effect of anxiolytics related to sleep?
What is a common side effect of anxiolytics related to sleep?
- Enhanced alertness
- Improved memory retention
- Increased energy
- Daytime sedation (correct)
Which classification of drugs primarily act on the GABA receptors to produce sedative effects?
Which classification of drugs primarily act on the GABA receptors to produce sedative effects?
- Beta-blockers
- Antidepressants
- Stimulants
- Benzodiazepines (correct)
What does the 'D' in ADME stand for in pharmacology?
What does the 'D' in ADME stand for in pharmacology?
- Diffusion
- Distribution (correct)
- Dosage
- Degradation
The mechanism of action of GABA involves which of the following?
The mechanism of action of GABA involves which of the following?
Which of the following represents a common use for anticonvulsant medications?
Which of the following represents a common use for anticonvulsant medications?
What is a primary effect of sedative-hypnotics on the central nervous system?
What is a primary effect of sedative-hypnotics on the central nervous system?
How are benzodiazepines commonly classified?
How are benzodiazepines commonly classified?
What is a key consideration in the metabolism of drugs classified as sedative-hypnotics?
What is a key consideration in the metabolism of drugs classified as sedative-hypnotics?
What mechanism underlies the action of GABA as a neurotransmitter?
What mechanism underlies the action of GABA as a neurotransmitter?
When treating insomnia related to psychological conditions, which approach is most effective?
When treating insomnia related to psychological conditions, which approach is most effective?
Which of the following conditions is most likely to require the use of benzodiazepines?
Which of the following conditions is most likely to require the use of benzodiazepines?
Which drug classification could be effectively used for the management of narcolepsy?
Which drug classification could be effectively used for the management of narcolepsy?
Which statement best describes an effective hypnotic drug?
Which statement best describes an effective hypnotic drug?
What is the mechanism of action of benzodiazepines?
What is the mechanism of action of benzodiazepines?
Which benzodiazepine has the fastest onset of action when administered intravenously?
Which benzodiazepine has the fastest onset of action when administered intravenously?
What is the duration of effect for alprazolam?
What is the duration of effect for alprazolam?
Which of the following benzodiazepines is primarily excreted through urine as inactive glucuronide conjugates?
Which of the following benzodiazepines is primarily excreted through urine as inactive glucuronide conjugates?
Which benzodiazepine is indicated for use as an anticonvulsant during status epilepticus?
Which benzodiazepine is indicated for use as an anticonvulsant during status epilepticus?
Which factor primarily affects the absorption of oxazepam?
Which factor primarily affects the absorption of oxazepam?
What is the half-life of lorazepam in adults?
What is the half-life of lorazepam in adults?
Which of the following benzodiazepines is noted for having an active metabolite?
Which of the following benzodiazepines is noted for having an active metabolite?
Which benzodiazepine has a longer duration of action than the others listed?
Which benzodiazepine has a longer duration of action than the others listed?
What is the primary site of action for benzodiazepines in the brain?
What is the primary site of action for benzodiazepines in the brain?
Which option represents the metabolic pathway for lorazepam?
Which option represents the metabolic pathway for lorazepam?
What is a common use for midazolam?
What is a common use for midazolam?
Which of the following is the primary route of administration for diazepam?
Which of the following is the primary route of administration for diazepam?
Which of these benzodiazepines is most effective for inducing hypnosis?
Which of these benzodiazepines is most effective for inducing hypnosis?
What is a significant adverse effect associated with the use of barbiturates?
What is a significant adverse effect associated with the use of barbiturates?
Which of the following best describes how buspirone works as an anxiolytic?
Which of the following best describes how buspirone works as an anxiolytic?
What is a contraindication for the use of barbiturates?
What is a contraindication for the use of barbiturates?
Which statement is true regarding the onset of action for buspirone?
Which statement is true regarding the onset of action for buspirone?
Which of the following is a disadvantage of using buspirone compared to barbiturates?
Which of the following is a disadvantage of using buspirone compared to barbiturates?
What is a potential adverse effect of benzodiazepines related to CNS activity?
What is a potential adverse effect of benzodiazepines related to CNS activity?
Which benzodiazepine is specifically indicated for status epilepticus?
Which benzodiazepine is specifically indicated for status epilepticus?
What is a clinical application of benzodiazepines in treating anxiety disorders?
What is a clinical application of benzodiazepines in treating anxiety disorders?
What attribute distinguishes benzodiazepines from barbiturates regarding overdose risk?
What attribute distinguishes benzodiazepines from barbiturates regarding overdose risk?
Which benzodiazepine is considered to have a preference as a general anesthetic due to its properties?
Which benzodiazepine is considered to have a preference as a general anesthetic due to its properties?
What is a common mechanism through which benzodiazepines exert their effects?
What is a common mechanism through which benzodiazepines exert their effects?
What is the role of flumazenil in the context of benzodiazepine administration?
What is the role of flumazenil in the context of benzodiazepine administration?
Which statement is true regarding the withdrawal from long-acting benzodiazepines?
Which statement is true regarding the withdrawal from long-acting benzodiazepines?
What is a primary advantage of non-benzodiazepine hypnotics compared to older sedative-hypnotics?
What is a primary advantage of non-benzodiazepine hypnotics compared to older sedative-hypnotics?
Suvorexant functions by targeting which receptor type?
Suvorexant functions by targeting which receptor type?
Which of the following statements is true regarding the adverse effects of ramelteon?
Which of the following statements is true regarding the adverse effects of ramelteon?
Which medication could pose a contraindication due to its interaction with strong CYP3A4 inhibitors?
Which medication could pose a contraindication due to its interaction with strong CYP3A4 inhibitors?
What is a characteristic of non-benzodiazepine hypnotics like Zolpidem?
What is a characteristic of non-benzodiazepine hypnotics like Zolpidem?
Which adverse effect is commonly associated with both suvorexant and non-benzodiazepine hypnotics?
Which adverse effect is commonly associated with both suvorexant and non-benzodiazepine hypnotics?
What distinguishes ramelteon from other hypnotics in terms of dependency?
What distinguishes ramelteon from other hypnotics in terms of dependency?
What is a major mechanism by which non-benzodiazepine hypnotics exert their effects?
What is a major mechanism by which non-benzodiazepine hypnotics exert their effects?
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Study Notes
Sleep Disorders
- Sleep disorders can be characterized by altered consciousness and changes in brainwave activity, as seen in the electroencephalogram (EEG)
- Insomnia can be caused by physiological issues, mental issues, or other medical conditions
- Insomnia due to a medical condition is often treated with benzodiazepines or other sedative-hypnotic drugs
- Insomnia due to psychological and psychiatric issues is best managed with a combination of psychotherapy and sedative-hypnotic drugs
- Hypersomnia is another type of sleep disorder
- Sleep disorders like narcolepsy, enuresis, somnambulism, nightmares, and night terrors, can be managed with a combination of psychotherapy and antidepressant drugs or CNS stimulants
- Sleep apnea is also a common sleep disorder
Sedative-hypnotics
- Sedative-hypnotic drugs are effective in reducing anxiety and calming patients
- These drugs can encourage sleep onset and maintenance of a state of sleep
- Some sedative-hypnotics, like barbiturates, can depress respiratory and vasomotor centers leading to coma and death
Benzodiazepines
- Benzodiazepines are a class of sedative-hypnotics that bind to GABA receptors
- Benzodiazepines increase the affinity of GABA for these receptors, increasing the frequency of channel opening
- This mechanism enhances the effects of GABA, which is an inhibitory neurotransmitter, leading to sedative and anxiolytic effects
- The effect of benzodiazepines on sleep and consciousness is achieved by facilitating GABA activity in the brain
- Common examples of benzodiazepines include: oxazepam, alprazolam, midazolam, clonazepam, lorazepam, diazepam, triazolam, and famil
Benzodiazepine Pharmacokinetics
- Oxazepam
- Oral administration
- Onset of action: 30-60 minutes
- Duration of action: 6-8 hours
- Well absorbed from the gastrointestinal tract
- Metabolized by hepatic glucuronide conjugation to produce an inactive metabolite
- Eliminated in the urine
- Alprazolam
- Oral administration
- Onset of action: 30-60 minutes
- Duration of action: ~6 hours
- Clonazepam
- Oral, IV, IM, rectal
- Onset of action: 6 to 8 hours in children; ≤12 hours in adults.
- Duration of action: 8 to 12 hours
- Well absorbed, with an active metabolite (clorazepate) that is more rapidly absorbed
- Metabolized by N-demethylation to form N-desmethyldiazepam (active metabolite)
- Triazolam
- Oral
- Onset of action: 15 to 30 minutes for hypnotic effect, 6 to 7 hours for duration.
- Duration of action: 6 to 7 hours
- Midazolam
- IM, IV, oral, nasal, buccal, rectal
- Onset of action: 3-5 minutes for IV, 10-20 minutes for oral.
- Duration of action: Up to 6 hours for IM, 2 hours for IV.
- Rapidly absorbed from the IM route
- Metabolized by hepatic conjugation to form inactive metabolites
- Diazepam
- Oral, IV, IM, rectal
- Onset of action: 1 to 3 minutes for IV (status epilepticus), 20 to 30 minutes for IM (hypnosis), 2 to 10 minutes for rectal.
- Duration of action: 15-30 minutes (status epilepticus), 6 to 8 hours (anesthesia premedication)
- Rapid and complete absorption from the IM route
- Metabolized by CYP3A4 and CYP2C19 to form N-desmethyldiazepam (active metabolite)
- Lorazepam
- Oral, IV, IM, SC, rectal
- Onset of action: Within 2-3 minutes for IV (sedation), 60-120 minutes for pediatrics
- Duration of action: 12-18 hours for adults
- Rapidly absorbed from the IM route
- Metabolized by hepatic conjugation to form lorazepam glucuronide (inactive metabolite)
- Diazepam has a long half-life (33 to 72 hours) due to the active metabolite desmethyldiazepam, which has a half-life of 71 to 174 hours.
Anxiety Disorders
- Anxiety can be normal and adaptive, helping individuals cope with life challenges
- Signs of anxiety can include:
- Changes in mood (apprehension and fear)
- *Sympathetic nervous system arousal
- *Hypervigilance
- Chronic anxiety can impair daily living
- Signs of chronic anxiety can include:
- Gastrointestinal problems (diarrhea)
- Cardiovascular problems (tachycardia)
- Neurologic problems (tremor, dizziness)
- *Sweating
- Chronic anxiety can lead to:
- Self-medication
- Substance abuse
- Treatment for anxiety disorders can include pharmacologic agents, psychotherapy, or both.
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