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Pharmacology: Sedative-Hypnotic Drugs
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Pharmacology: Sedative-Hypnotic Drugs

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Questions and Answers

What is the primary use of sedative-hypnotic drugs?

  • To treat anxiety and insomnia (correct)
  • To treat depression and ADHD
  • To treat schizophrenia and bipolar disorder
  • To treat pain and inflammation

    • Which of the following drugs is classified as a hypnotic?

  • Benzodiazepines
  • Buspirone
  • Chloral hydrate (correct)
  • Ramelteon (correct)

    • What is the mechanism of action of benzodiazepines?

  • They directly activate GABA receptors
  • They block the release of GABA
  • They cause allosteric modulation of GABA action on GABAA receptors (correct)
  • They inhibit the reuptake of GABA

    • Which of the following benzodiazepines is short-acting?

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

    What is the advantage of using lorazepam and oxazepam in patients with liver dysfunction?

    <p>They are less likely to cause excessive CNS depression</p> Signup and view all the answers

    What is the primary difference between short-acting and long-acting benzodiazepines?

    <p>Their metabolism and elimination half-life</p> Signup and view all the answers

    What is the effect of benzodiazepines on Cl- conductance?

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

    Why do long-acting benzodiazepines have a longer duration of action?

    <p>They are metabolized by oxidation into active metabolites</p> Signup and view all the answers

    What is the primary effect of BDZ receptors in small doses?

    <p>Anxiolytic effect</p> Signup and view all the answers

    Which of the following is NOT a therapeutic use of BDZ receptors?

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

    What is a common side effect of BDZ receptors in high doses?

    <p>Headache and muscle pain</p> Signup and view all the answers

    Which BDZ receptor subtype is most widely expressed and mediates most of the effects of BDZ?

    <p>Subtype 1</p> Signup and view all the answers

    What is a potential consequence of long-term use of BDZ receptors?

    <p>Physical dependence</p> Signup and view all the answers

    Which of the following anxiety disorders is NOT typically treated with BDZ receptors?

    <p>Post-traumatic stress disorder</p> Signup and view all the answers

    Benzodiazepines are classified based on their chemical structure rather than their clinical uses.

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

    Ramelteon is a drug with a main use as a sedative.

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

    Barbiturates are known for their great margin of safety over previously available sedative-hypnotic agents.

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

    The long-acting benzodiazepine, diazepam, is metabolized by conjugation into inactive metabolites.

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

    The main mechanism of action of benzodiazepines is to block the action of GABA on GABAA receptors.

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

    Buspirone is a type of barbiturate.

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

    The oral absorption of benzodiazepines is poor and slow.

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

    Benzodiazepines have a direct effect on the GABA receptors.

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

    Six BDZ receptor subtypes have been discovered, where subtype 2 is the most widely expressed and mediates most of the effects of BDZ.

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

    BDZ receptors produce a calming effect in animals and a taming effect in humans.

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

    Central skeletal muscle relaxation is a common feature in anxiety and may lead to headache and muscle pain.

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

    Acute amnesia is a long-term effect of BDZ receptors.

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

    BDZ receptors are only effective for the long-term management of anxiety disorders.

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

    Social phobia is not a type of anxiety disorder that can be treated with BDZ receptors.

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

    What impact do lipid solubility and half-life have on the therapeutic use of benzodiazepines?

    <p>Lipid solubility affects the onset of action, while half-life determines the duration of therapeutic effects.</p> Signup and view all the answers

    How do the metabolic pathways differ between short-acting and long-acting benzodiazepines?

    <p>Short-acting benzodiazepines are metabolized by conjugation into inactive metabolites, while long-acting ones are oxidized into active metabolites.</p> Signup and view all the answers

    What role does GABA play in the mechanism of action of benzodiazepines?

    <p>Benzodiazepines enhance GABA's effect by allosterically modulating GABAA receptors, increasing chloride conductance.</p> Signup and view all the answers

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

    <p>They are metabolized extrahepatically, reducing the risk of excessive CNS depression in these patients.</p> Signup and view all the answers

    Describe the classification of benzodiazepines based on their duration of action.

    <p>Benzodiazepines are classified as short-acting (t½ &lt; 5h), intermediate-acting (t½ 5-24 h), and long-acting (t½ &gt; 24 h).</p> Signup and view all the answers

    Can you explain the importance of active metabolites in the pharmacology of long-acting benzodiazepines?

    <p>Active metabolites extend the pharmacological effects of long-acting benzodiazepines beyond their initial half-life.</p> Signup and view all the answers

    What distinguishes buspirone from traditional benzodiazepines in treating anxiety?

    <p>Buspirone is a non-benzodiazepine anxiolytic that does not have the sedation or dependency risks associated with benzodiazepines.</p> Signup and view all the answers

    What is the significance of allosteric modulation in the effects of benzodiazepines on the CNS?

    <p>Allosteric modulation by benzodiazepines enhances the inhibitory effects of GABA, leading to increased sedation and anxiolysis.</p> Signup and view all the answers

    What is the anxiolytic effect of benzodiazepines associated with in small doses?

    <p>It is associated with a calming effect in humans and a taming effect in animals.</p> Signup and view all the answers

    Describe the therapeutic use of BDZs in acute anxiety situations.

    <p>BDZs provide effective short-term management of acute anxiety episodes.</p> Signup and view all the answers

    What muscle-related benefit do benzodiazepines provide to anxiety patients?

    <p>They offer central skeletal muscle relaxation, which can alleviate muscle tension associated with anxiety.</p> Signup and view all the answers

    Identify the primary receptor subtype associated with most benzodiazepine effects.

    <p>BDZ receptor subtype 1 is the most widely expressed and mediates most effects.</p> Signup and view all the answers

    What is one of the significant acute effects of high doses of benzodiazepines?

    <p>Acute amnesia can occur after the administration of high doses.</p> Signup and view all the answers

    What is a notable complication of using benzodiazepines for long-term anxiety management?

    <p>Long-term use may lead to dependence and withdrawal symptoms.</p> Signup and view all the answers

    Benzodiazepines are primarily used to treat anxiety and __________.

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

    Benzodiazepines have a great margin of safety over previously available sedative–hypnotic agents like __________.

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

    Short acting benzodiazepines have a half-life of less than __________ hours.

    <p>5</p> Signup and view all the answers

    The process by which long acting benzodiazepines are metabolized is called __________.

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

    Benzodiazepines act on special receptors in the __________ and peripheral tissue.

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

    BDZ cause allosteric modulation of GABA action on __________ receptors.

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

    Drugs with main use as __________ include barbiturates and ramelteon.

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

    Oral absorption of benzodiazepines is described as good and __________.

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

    The most widely expressed BDZ receptor subtype is subtype ______.

    <p>1</p> Signup and view all the answers

    In small doses, BDZ produce a calming effect and a ______ effect in animals.

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

    One of the pharmacological effects of BDZ at high doses is the ______ effect.

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

    BDZ are effective in managing acute anxiety and ______ anxiety disorders.

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

    A common consequence of anxiety is increased muscle tension leading to headaches and ______.

    <p>muscle pain</p> Signup and view all the answers

    After high doses of BDZ, acute ______ can occur.

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

    Match the BDZ receptor subtypes with their primary effects:

    <p>Subtype 1 = Mediates most effects of BDZ Subtype 2 = Less widely expressed Subtype 3 = Associated with anticonvulsant effects Subtype 4 = Involved in skeletal muscle relaxation</p> Signup and view all the answers

    Match the therapeutic uses of benzodiazepines with the corresponding anxiety disorders:

    <p>Acute Anxiety = Short-term management of anxiety Generalized Anxiety Disorder (GAD) = Chronic management of anxiety Social Phobia = Treatment of avoidance behavior Panic Disorder = Immediate relief for panic attacks</p> Signup and view all the answers

    Match the pharmacological effects of benzodiazepines with their descriptions:

    <p>Anxiolytic effect = Calming effect in small doses Hypnotic effect = Sedative effect at higher doses Muscle relaxation = Reduces muscle tension and pain Anticonvulsant effect = Prevention of seizure activity</p> Signup and view all the answers

    Match the common side effects of high doses of benzodiazepines with their corresponding effects:

    <p>Acute Amnesia = Memory loss after high doses Drowsiness = Excessive sleepiness and sedation Confusion = Disorientation and cognitive impairment Headaches = Pain possibly related to muscle relaxation</p> Signup and view all the answers

    Match the statements regarding benzodiazepines with their correct attributes:

    <p>Increased muscle relaxation = Common feature in anxiety disorders Short-term management = Effective for acute anxiety interventions BDZ receptor subtypes = Six identified, subtype 1 is the most prevalent Therapeutic use = Primarily for anxiety and sleep disorders</p> Signup and view all the answers

    Match the types of anxiety disorders with their characteristics relevant to benzodiazepine treatment:

    <p>Acute Anxiety = Immediate onset of excessive fear Generalized Anxiety Disorder = Chronic state of worry Social Anxiety Disorder = Fear of social interactions Panic Disorder = Recurrent panic attacks</p> Signup and view all the answers

    Match the following benzodiazepines with their classification based on duration of action:

    <p>Midazolam = Short acting Lorazepam = Intermediate acting Diazepam = Long acting Triazolam = Short acting</p> Signup and view all the answers

    Match the following sedative-hypnotic drugs with their main use:

    <p>Ramelteon = Hypnotic Chloral hydrate = Hypnotic Buspirone = Anxiolytic Barbiturates = Sedative</p> Signup and view all the answers

    Match the following pharmacokinetic properties with the corresponding type of benzodiazepine:

    <p>Metabolized by oxidation = Long acting Rapid onset of action = Highly lipid soluble Conjugation metabolism = Short acting Active metabolites = Long acting</p> Signup and view all the answers

    Match the following characteristics of benzodiazepines with their impact:

    <p>Allosteric modulation of GABA = Increased Cl- conductance Highly lipid soluble drugs = Fast onset of action Long half-life = Extended duration of action Short half-life = Rapid clearance from body</p> Signup and view all the answers

    Match the following terms related to benzodiazepines with their definitions:

    <p>Anxiolytics = Drugs that relieve anxiety Sedatives = Drugs that induce calmness Hypnotics = Drugs that induce sleep CNS receptor = Target site for benzodiazepines</p> Signup and view all the answers

    Match the following mechanisms of action with the corresponding effects of benzodiazepines:

    <p>GABA action enhancement = CNS depression Hyperpolarization = Reduced neuronal excitability Chloride ion influx = Sedative effects Fast onset due to lipid solubility = Quick therapeutic response</p> Signup and view all the answers

    Match the following statements regarding benzodiazepines with their characteristics:

    <p>Less likely to cause CNS depression in liver dysfunction = Lorazepam and Oxazepam Short-acting drugs are cleared rapidly = Conjugation metabolism Long-acting drugs metabolized by oxidation = CYP450 pathway Similar therapeutic actions, differing pharmacokinetics = Benzodiazepines</p> Signup and view all the answers

    Match the following properties of sedative-hypnotic drugs with their general classifications:

    <p>Barbiturates = Sedative Buspirone = Anxiolytic Ramelteon = Hypnotic Diazepam = Anxiolytic</p> Signup and view all the answers

    Study Notes

    Sedative-Hypnotic Drugs

    • Drugs that induce sedation or sleep and relieve anxiety.
    • Primarily used for anxiety and insomnia treatment.
    • Classified based on clinical uses rather than chemical structures.
    • Sedatives include benzodiazepines and buspirone.
    • Hypnotics include barbiturates, ramelteon, and chloral hydrate.

    Benzodiazepines

    • Have a higher margin of safety compared to barbiturates.
    • Therapeutic actions are similar, but vary in lipid solubility, metabolism, and half-life.

    Classification

    • Short acting (half-life < 5h): midazolam, triazolam
    • Intermediate acting (half-life 5-24h): alprazolam, lorazepam, clonazepam
    • Long acting (half-life > 24h): diazepam, clorazepate, flurazepam

    Pharmacokinetics

    • Good and rapid oral absorption.
    • Lipid-soluble drugs (midazolam, triazolam) have a fast onset of action.
    • Long-acting drugs, like diazepam, are metabolized by oxidation (CYP450) into active metabolites.
    • Short-acting drugs are metabolized by conjugation into inactive metabolites for renal clearance.
    • Lorazepam and oxazepam (metabolized extrahepatically) are preferred in liver dysfunction to avoid excessive CNS depression.

    Mechanism of Action

    • Benzodiazepines act on specific receptors in the CNS and peripheral tissues.
    • Cause allosteric modulation of GABA action on GABAA receptors, increasing Cl- conductance and resulting in hyperpolarization.
    • Six receptor subtypes identified; subtype 1 mediates most effects.

    Pharmacological Effects

    • Reduction of anxiety with small doses (anxiolytic effect).
    • High doses induce hypnosedative effects.
    • Central skeletal muscle relaxation useful for alleviating muscle tension and headaches.
    • Exhibit anticonvulsant properties.
    • Potential for acute amnesia at high doses.

    Therapeutic Uses

    • Effective in treating anxiety disorders, including:
      • Acute anxiety
      • Generalized anxiety disorder (GAD)
      • Social phobia (social anxiety disorder)
    • Primarily used for short-term management of anxiety symptoms.

    Sedative-Hypnotic Drugs

    • Drugs that induce sedation or sleep and relieve anxiety.
    • Primarily used for anxiety and insomnia treatment.
    • Classified based on clinical uses rather than chemical structures.
    • Sedatives include benzodiazepines and buspirone.
    • Hypnotics include barbiturates, ramelteon, and chloral hydrate.

    Benzodiazepines

    • Have a higher margin of safety compared to barbiturates.
    • Therapeutic actions are similar, but vary in lipid solubility, metabolism, and half-life.

    Classification

    • Short acting (half-life < 5h): midazolam, triazolam
    • Intermediate acting (half-life 5-24h): alprazolam, lorazepam, clonazepam
    • Long acting (half-life > 24h): diazepam, clorazepate, flurazepam

    Pharmacokinetics

    • Good and rapid oral absorption.
    • Lipid-soluble drugs (midazolam, triazolam) have a fast onset of action.
    • Long-acting drugs, like diazepam, are metabolized by oxidation (CYP450) into active metabolites.
    • Short-acting drugs are metabolized by conjugation into inactive metabolites for renal clearance.
    • Lorazepam and oxazepam (metabolized extrahepatically) are preferred in liver dysfunction to avoid excessive CNS depression.

    Mechanism of Action

    • Benzodiazepines act on specific receptors in the CNS and peripheral tissues.
    • Cause allosteric modulation of GABA action on GABAA receptors, increasing Cl- conductance and resulting in hyperpolarization.
    • Six receptor subtypes identified; subtype 1 mediates most effects.

    Pharmacological Effects

    • Reduction of anxiety with small doses (anxiolytic effect).
    • High doses induce hypnosedative effects.
    • Central skeletal muscle relaxation useful for alleviating muscle tension and headaches.
    • Exhibit anticonvulsant properties.
    • Potential for acute amnesia at high doses.

    Therapeutic Uses

    • Effective in treating anxiety disorders, including:
      • Acute anxiety
      • Generalized anxiety disorder (GAD)
      • Social phobia (social anxiety disorder)
    • Primarily used for short-term management of anxiety symptoms.

    Sedative-Hypnotic Drugs

    • Drugs that induce sedation or sleep and relieve anxiety.
    • Primarily used for anxiety and insomnia treatment.
    • Classified based on clinical uses rather than chemical structures.
    • Sedatives include benzodiazepines and buspirone.
    • Hypnotics include barbiturates, ramelteon, and chloral hydrate.

    Benzodiazepines

    • Have a higher margin of safety compared to barbiturates.
    • Therapeutic actions are similar, but vary in lipid solubility, metabolism, and half-life.

    Classification

    • Short acting (half-life < 5h): midazolam, triazolam
    • Intermediate acting (half-life 5-24h): alprazolam, lorazepam, clonazepam
    • Long acting (half-life > 24h): diazepam, clorazepate, flurazepam

    Pharmacokinetics

    • Good and rapid oral absorption.
    • Lipid-soluble drugs (midazolam, triazolam) have a fast onset of action.
    • Long-acting drugs, like diazepam, are metabolized by oxidation (CYP450) into active metabolites.
    • Short-acting drugs are metabolized by conjugation into inactive metabolites for renal clearance.
    • Lorazepam and oxazepam (metabolized extrahepatically) are preferred in liver dysfunction to avoid excessive CNS depression.

    Mechanism of Action

    • Benzodiazepines act on specific receptors in the CNS and peripheral tissues.
    • Cause allosteric modulation of GABA action on GABAA receptors, increasing Cl- conductance and resulting in hyperpolarization.
    • Six receptor subtypes identified; subtype 1 mediates most effects.

    Pharmacological Effects

    • Reduction of anxiety with small doses (anxiolytic effect).
    • High doses induce hypnosedative effects.
    • Central skeletal muscle relaxation useful for alleviating muscle tension and headaches.
    • Exhibit anticonvulsant properties.
    • Potential for acute amnesia at high doses.

    Therapeutic Uses

    • Effective in treating anxiety disorders, including:
      • Acute anxiety
      • Generalized anxiety disorder (GAD)
      • Social phobia (social anxiety disorder)
    • Primarily used for short-term management of anxiety symptoms.

    Sedative-Hypnotic Drugs

    • Drugs that induce sedation or sleep and relieve anxiety.
    • Primarily used for anxiety and insomnia treatment.
    • Classified based on clinical uses rather than chemical structures.
    • Sedatives include benzodiazepines and buspirone.
    • Hypnotics include barbiturates, ramelteon, and chloral hydrate.

    Benzodiazepines

    • Have a higher margin of safety compared to barbiturates.
    • Therapeutic actions are similar, but vary in lipid solubility, metabolism, and half-life.

    Classification

    • Short acting (half-life < 5h): midazolam, triazolam
    • Intermediate acting (half-life 5-24h): alprazolam, lorazepam, clonazepam
    • Long acting (half-life > 24h): diazepam, clorazepate, flurazepam

    Pharmacokinetics

    • Good and rapid oral absorption.
    • Lipid-soluble drugs (midazolam, triazolam) have a fast onset of action.
    • Long-acting drugs, like diazepam, are metabolized by oxidation (CYP450) into active metabolites.
    • Short-acting drugs are metabolized by conjugation into inactive metabolites for renal clearance.
    • Lorazepam and oxazepam (metabolized extrahepatically) are preferred in liver dysfunction to avoid excessive CNS depression.

    Mechanism of Action

    • Benzodiazepines act on specific receptors in the CNS and peripheral tissues.
    • Cause allosteric modulation of GABA action on GABAA receptors, increasing Cl- conductance and resulting in hyperpolarization.
    • Six receptor subtypes identified; subtype 1 mediates most effects.

    Pharmacological Effects

    • Reduction of anxiety with small doses (anxiolytic effect).
    • High doses induce hypnosedative effects.
    • Central skeletal muscle relaxation useful for alleviating muscle tension and headaches.
    • Exhibit anticonvulsant properties.
    • Potential for acute amnesia at high doses.

    Therapeutic Uses

    • Effective in treating anxiety disorders, including:
      • Acute anxiety
      • Generalized anxiety disorder (GAD)
      • Social phobia (social anxiety disorder)
    • Primarily used for short-term management of anxiety symptoms.

    Sedative-Hypnotic Drugs

    • Drugs that induce sedation or sleep and relieve anxiety.
    • Primarily used for anxiety and insomnia treatment.
    • Classified based on clinical uses rather than chemical structures.
    • Sedatives include benzodiazepines and buspirone.
    • Hypnotics include barbiturates, ramelteon, and chloral hydrate.

    Benzodiazepines

    • Have a higher margin of safety compared to barbiturates.
    • Therapeutic actions are similar, but vary in lipid solubility, metabolism, and half-life.

    Classification

    • Short acting (half-life < 5h): midazolam, triazolam
    • Intermediate acting (half-life 5-24h): alprazolam, lorazepam, clonazepam
    • Long acting (half-life > 24h): diazepam, clorazepate, flurazepam

    Pharmacokinetics

    • Good and rapid oral absorption.
    • Lipid-soluble drugs (midazolam, triazolam) have a fast onset of action.
    • Long-acting drugs, like diazepam, are metabolized by oxidation (CYP450) into active metabolites.
    • Short-acting drugs are metabolized by conjugation into inactive metabolites for renal clearance.
    • Lorazepam and oxazepam (metabolized extrahepatically) are preferred in liver dysfunction to avoid excessive CNS depression.

    Mechanism of Action

    • Benzodiazepines act on specific receptors in the CNS and peripheral tissues.
    • Cause allosteric modulation of GABA action on GABAA receptors, increasing Cl- conductance and resulting in hyperpolarization.
    • Six receptor subtypes identified; subtype 1 mediates most effects.

    Pharmacological Effects

    • Reduction of anxiety with small doses (anxiolytic effect).
    • High doses induce hypnosedative effects.
    • Central skeletal muscle relaxation useful for alleviating muscle tension and headaches.
    • Exhibit anticonvulsant properties.
    • Potential for acute amnesia at high doses.

    Therapeutic Uses

    • Effective in treating anxiety disorders, including:
      • Acute anxiety
      • Generalized anxiety disorder (GAD)
      • Social phobia (social anxiety disorder)
    • Primarily used for short-term management of anxiety symptoms.

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    Learn about sedative-hypnotic drugs, their uses, classification, and pharmacokinetics, including benzodiazepines and their properties.

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