Anxiolytics, Hypnotics and Barbiturates
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Questions and Answers

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?

  • Beta-blockers
  • Antidepressants
  • Stimulants
  • Benzodiazepines (correct)

    • 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?

    <p>Enhancing inhibitory neurotransmission</p> Signup and view all the answers

    Which of the following represents a common use for anticonvulsant medications?

    <p>Treating anxiety disorders</p> Signup and view all the answers

    What is a primary effect of sedative-hypnotics on the central nervous system?

    <p>Decrease respiratory function</p> Signup and view all the answers

    How are benzodiazepines commonly classified?

    <p>Long-acting and short-acting</p> Signup and view all the answers

    What is a key consideration in the metabolism of drugs classified as sedative-hypnotics?

    <p>They generally have a high first-pass effect</p> Signup and view all the answers

    What mechanism underlies the action of GABA as a neurotransmitter?

    <p>It facilitates chloride ion influx</p> Signup and view all the answers

    When treating insomnia related to psychological conditions, which approach is most effective?

    <p>Combination of psychotherapy and sedative-hypnotics</p> Signup and view all the answers

    Which of the following conditions is most likely to require the use of benzodiazepines?

    <p>Severe insomnia caused by medical conditions</p> Signup and view all the answers

    Which drug classification could be effectively used for the management of narcolepsy?

    <p>Stimulants</p> Signup and view all the answers

    Which statement best describes an effective hypnotic drug?

    <p>It should produce drowsiness and support sleep onset</p> Signup and view all the answers

    What is the mechanism of action of benzodiazepines?

    <p>Bind in the chloride ion channel between α1 and γ subunits to increase GABA affinity</p> Signup and view all the answers

    Which benzodiazepine has the fastest onset of action when administered intravenously?

    <p>Midazolam</p> Signup and view all the answers

    What is the duration of effect for alprazolam?

    <p>6 to 8 hours</p> Signup and view all the answers

    Which of the following benzodiazepines is primarily excreted through urine as inactive glucuronide conjugates?

    <p>Oxazepam</p> Signup and view all the answers

    Which benzodiazepine is indicated for use as an anticonvulsant during status epilepticus?

    <p>Lorazepam</p> Signup and view all the answers

    Which factor primarily affects the absorption of oxazepam?

    <p>Slow gastrointestinal absorption</p> Signup and view all the answers

    What is the half-life of lorazepam in adults?

    <p>$12$ hours</p> Signup and view all the answers

    Which of the following benzodiazepines is noted for having an active metabolite?

    <p>Diazepam</p> Signup and view all the answers

    Which benzodiazepine has a longer duration of action than the others listed?

    <p>Clonazepam</p> Signup and view all the answers

    What is the primary site of action for benzodiazepines in the brain?

    <p>GABA receptors</p> Signup and view all the answers

    Which option represents the metabolic pathway for lorazepam?

    <p>Rapidly conjugated to an inactive metabolite</p> Signup and view all the answers

    What is a common use for midazolam?

    <p>Anesthesia premedication</p> Signup and view all the answers

    Which of the following is the primary route of administration for diazepam?

    <p>Oral and IV</p> Signup and view all the answers

    Which of these benzodiazepines is most effective for inducing hypnosis?

    <p>Triazolam</p> Signup and view all the answers

    What is a significant adverse effect associated with the use of barbiturates?

    <p>Dependence and withdrawal symptoms</p> Signup and view all the answers

    Which of the following best describes how buspirone works as an anxiolytic?

    <p>It partially stimulates the 5-HT1A receptor.</p> Signup and view all the answers

    What is a contraindication for the use of barbiturates?

    <p>Cardiovascular disease</p> Signup and view all the answers

    Which statement is true regarding the onset of action for buspirone?

    <p>It takes 1–2 weeks to begin taking effect.</p> Signup and view all the answers

    Which of the following is a disadvantage of using buspirone compared to barbiturates?

    <p>Less effective for generalized anxiety disorders</p> Signup and view all the answers

    What is a potential adverse effect of benzodiazepines related to CNS activity?

    <p>Dependence</p> Signup and view all the answers

    Which benzodiazepine is specifically indicated for status epilepticus?

    <p>Lorazepam</p> Signup and view all the answers

    What is a clinical application of benzodiazepines in treating anxiety disorders?

    <p>Rapid relief of acute anxiety</p> Signup and view all the answers

    What attribute distinguishes benzodiazepines from barbiturates regarding overdose risk?

    <p>Less risk of respiratory depression</p> Signup and view all the answers

    Which benzodiazepine is considered to have a preference as a general anesthetic due to its properties?

    <p>Midazolam</p> Signup and view all the answers

    What is a common mechanism through which benzodiazepines exert their effects?

    <p>Facilitating GABAA receptor action</p> Signup and view all the answers

    What is the role of flumazenil in the context of benzodiazepine administration?

    <p>To treat benzodiazepine overdose</p> Signup and view all the answers

    Which statement is true regarding the withdrawal from long-acting benzodiazepines?

    <p>It can precipitate acute seizures.</p> Signup and view all the answers

    What is a primary advantage of non-benzodiazepine hypnotics compared to older sedative-hypnotics?

    <p>They have a lower risk of dependency.</p> Signup and view all the answers

    Suvorexant functions by targeting which receptor type?

    <p>Orexin receptors</p> Signup and view all the answers

    Which of the following statements is true regarding the adverse effects of ramelteon?

    <p>Dizziness and fatigue are common side effects.</p> Signup and view all the answers

    Which medication could pose a contraindication due to its interaction with strong CYP3A4 inhibitors?

    <p>Suvorexant</p> Signup and view all the answers

    What is a characteristic of non-benzodiazepine hypnotics like Zolpidem?

    <p>They provide rapid onset of sleep with a short duration.</p> Signup and view all the answers

    Which adverse effect is commonly associated with both suvorexant and non-benzodiazepine hypnotics?

    <p>Headaches</p> Signup and view all the answers

    What distinguishes ramelteon from other hypnotics in terms of dependency?

    <p>It has no known risk of dependency.</p> Signup and view all the answers

    What is a major mechanism by which non-benzodiazepine hypnotics exert their effects?

    <p>They act as GABA receptor agonists.</p> Signup and view all the answers

    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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    Description

    This quiz covers various sleep disorders such as insomnia, hypersomnia, and sleep apnea, along with their treatment options. It also delves into the role of sedative-hypnotic drugs in managing anxiety and promoting sleep. Test your knowledge on the classification, symptoms, and therapeutic approaches related to these conditions.

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