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Benzodiazepines
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Benzodiazepines

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Questions and Answers

Which drug is the most commonly used benzodiazepine in the perioperative period?

  • Midazolam (correct)
  • Diazepam
  • Flumazenil
  • Lorazepam

    • Which of the following statements about benzodiazepines is true?

  • They have a longer context-sensitive half-time than barbiturates (correct)
  • They are structurally different from barbiturates
  • They produce enzyme induction
  • They activate the GABAA receptors

    • Which GABAA receptor subtype is important for sedation?

  • β
  • α1 (correct)
  • α5
  • α2

    • What is the mechanism of action of benzodiazepines?

    <p>Enhancement of GABA affinity for GABAA receptors</p> Signup and view all the answers

    Which drug is a specific pharmacologic antagonist for benzodiazepines?

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

    Which drug is associated with decreases in the plasma concentrations of cortisol?

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

    What is the principal pharmacologic effect of benzodiazepines?

    <p>Anticonvulsant actions</p> Signup and view all the answers

    Which type of amnesia is longer lasting for benzodiazepines?

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

    Do benzodiazepines produce adequate skeletal muscle relaxation for surgical procedures?

    <p>No</p> Signup and view all the answers

    What percentage of the population uses hypnotics for more than a year?

    <p>0.4%</p> Signup and view all the answers

    Which class of drugs is commonly used for detoxication from alcohol?

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

    What is the mechanism that limits the effect of benzodiazepines on GABAergic neurotransmission?

    <p>Built-in ceiling effect</p> Signup and view all the answers

    Which factor influences the onset and duration of action of benzodiazepines?

    <p>Lipid solubility</p> Signup and view all the answers

    What may increase the clinical effects produced by benzodiazepines?

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

    Which side effect is most commonly observed in patients treated chronically with benzodiazepines?

    <p>Fatigue and drowsiness</p> Signup and view all the answers

    Which benzodiazepine is known for its enhanced suppression of the hypothalamic-pituitary-adrenal axis?

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

    Dependence on benzodiazepines may occur after how long of use?

    <p>More than 6 months</p> Signup and view all the answers

    Which benzodiazepines are preferentially selected in elderly patients due to their metabolism?

    <p>Lorazepam, oxazepam, and temazepam</p> Signup and view all the answers

    Which group of patients may experience accelerated cognitive decline with long-term benzodiazepine administration?

    <p>Elderly patients</p> Signup and view all the answers

    Benzodiazepines may inhibit platelet-activating factor–induced aggregation, but their effect on hemorrhagic complications in patients with severe, chemotherapy-induced thrombocytopenia is

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

    Which factor influences the binding affinity of benzodiazepines to plasma proteins?

    <p>Lipid solubility</p> Signup and view all the answers

    Which of the following is a physiological effect of adenosine that is terminated through reuptake into cells?

    <p>Decreased cardiac oxygen demand</p> Signup and view all the answers

    Which area of the brain experiences a shift from alpha to beta activity with benzodiazepines?

    <p>Frontal and rolandic areas</p> Signup and view all the answers

    Which of the following is a common side effect of chronic benzodiazepine use?

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

    Which drug class exerts synergistic sedative effects with benzodiazepines?

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

    Which of the following is NOT a characteristic of benzodiazepines compared to barbiturates?

    <p>Induction of hepatic microsomal enzymes</p> Signup and view all the answers

    Which benzodiazepine is commonly used for prolonged administration when prompt recovery is desired?

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

    What is the mechanism of action of benzodiazepines?

    <p>Enhancement of GABAA receptor affinity for GABA</p> Signup and view all the answers

    Which GABAA receptor subtype is important for sedation?

    <p>α1-containing receptors</p> Signup and view all the answers

    Which of the following drugs can produce synergistic effects with benzodiazepines to increase GABAA receptor-mediated inhibition in the CNS?

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

    Which of the following is NOT a principal pharmacologic effect of benzodiazepines?

    <p>Anticonvulsant actions</p> Signup and view all the answers

    What is the estimated percentage of the population that uses hypnotics for more than a year?

    <p>0.4%</p> Signup and view all the answers

    Which of the following is true about the effect of benzodiazepines on skeletal muscle relaxation for surgical procedures?

    <p>Benzodiazepines do not produce adequate skeletal muscle relaxation</p> Signup and view all the answers

    Which drug is more likely to evoke histamine release compared to etomidate?

    <p>Neuromuscular blocking drugs</p> Signup and view all the answers

    Which of the following is true about the amnestic potency of benzodiazepines?

    <p>The amnestic potency of benzodiazepines is greater than their sedative effects</p> Signup and view all the answers

    Which benzodiazepine is metabolized only by glucuronidation and has no active metabolites?

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

    Which symptom is commonly observed in elderly long-term benzodiazepine users?

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

    Which benzodiazepine produces dose-dependent inhibition of adrenocorticotrophic hormone and cortisol secretion?

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

    Which benzodiazepine has replaced diazepam for use in aqueous solutions and rapid metabolism?

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

    Which factor affects glucuronidation less than oxidative metabolic pathways?

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

    True or false: Etomidate is associated with decreases in the plasma concentrations of cortisol.

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

    True or false: The incidence of allergic reactions following administration of etomidate is high.

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

    True or false: Benzodiazepines produce adequate skeletal muscle relaxation for surgical procedures.

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

    True or false: Benzodiazepines exert anterograde amnesia but do not affect retrograde amnesia.

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

    True or false: The amnestic potency of benzodiazepines is greater than their sedative effects.

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

    True or false: Benzodiazepines are commonly used for the treatment of chronic insomnia.

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

    True or false: Benzodiazepines have a greater margin of safety compared to barbiturates.

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

    True or false: Benzodiazepines induce hepatic microsomal enzymes.

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

    True or false: Benzodiazepines are more addicting than opioids, cocaine, amphetamines, or barbiturates.

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

    True or false: Midazolam is the most commonly used benzodiazepine in the perioperative period.

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

    True or false: Benzodiazepines can suppress cortisol levels in treated patients?

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

    True or false: Dependence on benzodiazepines can occur even with therapeutic doses?

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

    True or false: Benzodiazepine withdrawal symptoms have a time of onset that reflects the elimination half-time of the drug?

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

    True or false: Aging and liver disease affect glucuronidation more than oxidative metabolic pathways?

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

    True or false: Long-term benzodiazepine administration may accelerate cognitive decline in elderly patients?

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

    True or false: Benzodiazepines have a built-in ceiling effect that prevents them from exceeding the physiologic maximum of GABA inhibition.

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

    True or false: Benzodiazepines are highly absorbed from the gastrointestinal tract following oral administration.

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

    True or false: Chronic administration of benzodiazepines adversely affects systemic blood pressure, heart rate, or cardiac rhythm.

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

    True or false: Benzodiazepines may interact with other medications to have adverse effects on patients with chronic lung disease characterized by hypoventilation and/or decreased arterial oxygenation.

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

    True or false: Benzodiazepines exert synergistic sedative effects with opioids.

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

    Study Notes

    Benzodiazepines Overview

    • Midazolam is the most commonly used benzodiazepine in the perioperative period.
    • Commonly used for detoxication from alcohol.
    • Dependence may occur after prolonged use, typically beyond a few weeks.

    Mechanism of Action

    • Benzodiazepines enhance GABAergic neurotransmission by binding to GABAA receptors, specifically the alpha2 subtype for sedation.
    • They exhibit a ceiling effect, preventing excessive GABA inhibition.
    • Mechanism of action involves increasing frequency of chloride channel opening.

    Pharmacological Effects

    • Principal effects include sedation, anxiolysis, muscle relaxation, and amnesia.
    • Anterograde amnesia is more prominent than retrograde amnesia; longer-lasting effects observed with anterograde amnesia.
    • Chronic use may lead to side effects such as cognitive decline, particularly in elderly patients.

    Specific Drugs and Effects

    • Flumazenil is the specific pharmacologic antagonist for benzodiazepines.
    • Etomidate is associated with decreased cortisol levels but has a relatively low incidence of allergic reactions.
    • Diazepam has been replaced by other benzodiazepines for certain uses, like midazolam, which offers rapid metabolism and intravenous formulation.

    Patient Factors and Clinical Implications

    • Factors influencing onset and duration of action include lipid solubility and metabolism.
    • Elderly patients may be prescribed benzodiazepines with less active metabolites to reduce risk.
    • Long-term use may accelerate cognitive decline in elderly patients, often observable as memory side effects.
    • Approximately 10% of the population uses hypnotics for more than a year.

    Drug Interactions and Side Effects

    • Benzodiazepines can exert synergistic effects with opioids, leading to increased sedation.
    • Chronic administration can adversely affect blood pressure and heart rhythm.
    • Interactions with other drugs may pose risks in patients with chronic lung disease.

    Miscellaneous Facts

    • The binding affinity of benzodiazepines to plasma proteins can be influenced by factors like drug concentration and patient metabolism.
    • They may inhibit platelet-activating factor-induced aggregation, without notable impact on hemorrhagic complications in thrombocytopenia.
    • Psychological side effects are commonly seen with long-term benzodiazepine use, including dependence and withdrawal symptoms upon cessation.

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    Description

    "Understanding the Synergy and Cross-Tolerance of Benzodiazepines in Alcohol Detoxication" - Test your knowledge on the pharmacologic relationship between benzodiazepines and alcohol, including cross-tolerance and the role of GABA inhibition. Explore the clinical use of benzodiazepines and their built-in ceiling effect.

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