Podcast
Questions and Answers
Which drug is the most commonly used benzodiazepine in the perioperative period?
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?
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?
Which GABAA receptor subtype is important for sedation?
- β
- α1 (correct)
- α5
- α2
What is the mechanism of action of benzodiazepines?
What is the mechanism of action of benzodiazepines?
Which drug is a specific pharmacologic antagonist for benzodiazepines?
Which drug is a specific pharmacologic antagonist for benzodiazepines?
Which drug is associated with decreases in the plasma concentrations of cortisol?
Which drug is associated with decreases in the plasma concentrations of cortisol?
What is the principal pharmacologic effect of benzodiazepines?
What is the principal pharmacologic effect of benzodiazepines?
Which type of amnesia is longer lasting for benzodiazepines?
Which type of amnesia is longer lasting for benzodiazepines?
Do benzodiazepines produce adequate skeletal muscle relaxation for surgical procedures?
Do benzodiazepines produce adequate skeletal muscle relaxation for surgical procedures?
What percentage of the population uses hypnotics for more than a year?
What percentage of the population uses hypnotics for more than a year?
Which class of drugs is commonly used for detoxication from alcohol?
Which class of drugs is commonly used for detoxication from alcohol?
What is the mechanism that limits the effect of benzodiazepines on GABAergic neurotransmission?
What is the mechanism that limits the effect of benzodiazepines on GABAergic neurotransmission?
Which factor influences the onset and duration of action of benzodiazepines?
Which factor influences the onset and duration of action of benzodiazepines?
What may increase the clinical effects produced by benzodiazepines?
What may increase the clinical effects produced by benzodiazepines?
Which side effect is most commonly observed in patients treated chronically with benzodiazepines?
Which side effect is most commonly observed in patients treated chronically with benzodiazepines?
Which benzodiazepine is known for its enhanced suppression of the hypothalamic-pituitary-adrenal axis?
Which benzodiazepine is known for its enhanced suppression of the hypothalamic-pituitary-adrenal axis?
Dependence on benzodiazepines may occur after how long of use?
Dependence on benzodiazepines may occur after how long of use?
Which benzodiazepines are preferentially selected in elderly patients due to their metabolism?
Which benzodiazepines are preferentially selected in elderly patients due to their metabolism?
Which group of patients may experience accelerated cognitive decline with long-term benzodiazepine administration?
Which group of patients may experience accelerated cognitive decline with long-term benzodiazepine administration?
Benzodiazepines may inhibit platelet-activating factor–induced aggregation, but their effect on hemorrhagic complications in patients with severe, chemotherapy-induced thrombocytopenia is
Benzodiazepines may inhibit platelet-activating factor–induced aggregation, but their effect on hemorrhagic complications in patients with severe, chemotherapy-induced thrombocytopenia is
Which factor influences the binding affinity of benzodiazepines to plasma proteins?
Which factor influences the binding affinity of benzodiazepines to plasma proteins?
Which of the following is a physiological effect of adenosine that is terminated through reuptake into cells?
Which of the following is a physiological effect of adenosine that is terminated through reuptake into cells?
Which area of the brain experiences a shift from alpha to beta activity with benzodiazepines?
Which area of the brain experiences a shift from alpha to beta activity with benzodiazepines?
Which of the following is a common side effect of chronic benzodiazepine use?
Which of the following is a common side effect of chronic benzodiazepine use?
Which drug class exerts synergistic sedative effects with benzodiazepines?
Which drug class exerts synergistic sedative effects with benzodiazepines?
Which of the following is NOT a characteristic of benzodiazepines compared to barbiturates?
Which of the following is NOT a characteristic of benzodiazepines compared to barbiturates?
Which benzodiazepine is commonly used for prolonged administration when prompt recovery is desired?
Which benzodiazepine is commonly used for prolonged administration when prompt recovery is desired?
What is the mechanism of action of benzodiazepines?
What is the mechanism of action of benzodiazepines?
Which GABAA receptor subtype is important for sedation?
Which GABAA receptor subtype is important for sedation?
Which of the following drugs can produce synergistic effects with benzodiazepines to increase GABAA receptor-mediated inhibition in the CNS?
Which of the following drugs can produce synergistic effects with benzodiazepines to increase GABAA receptor-mediated inhibition in the CNS?
Which of the following is NOT a principal pharmacologic effect of benzodiazepines?
Which of the following is NOT a principal pharmacologic effect of benzodiazepines?
What is the estimated percentage of the population that uses hypnotics for more than a year?
What is the estimated percentage of the population that uses hypnotics for more than a year?
Which of the following is true about the effect of benzodiazepines on skeletal muscle relaxation for surgical procedures?
Which of the following is true about the effect of benzodiazepines on skeletal muscle relaxation for surgical procedures?
Which drug is more likely to evoke histamine release compared to etomidate?
Which drug is more likely to evoke histamine release compared to etomidate?
Which of the following is true about the amnestic potency of benzodiazepines?
Which of the following is true about the amnestic potency of benzodiazepines?
Which benzodiazepine is metabolized only by glucuronidation and has no active metabolites?
Which benzodiazepine is metabolized only by glucuronidation and has no active metabolites?
Which symptom is commonly observed in elderly long-term benzodiazepine users?
Which symptom is commonly observed in elderly long-term benzodiazepine users?
Which benzodiazepine produces dose-dependent inhibition of adrenocorticotrophic hormone and cortisol secretion?
Which benzodiazepine produces dose-dependent inhibition of adrenocorticotrophic hormone and cortisol secretion?
Which benzodiazepine has replaced diazepam for use in aqueous solutions and rapid metabolism?
Which benzodiazepine has replaced diazepam for use in aqueous solutions and rapid metabolism?
Which factor affects glucuronidation less than oxidative metabolic pathways?
Which factor affects glucuronidation less than oxidative metabolic pathways?
True or false: Etomidate is associated with decreases in the plasma concentrations of cortisol.
True or false: Etomidate is associated with decreases in the plasma concentrations of cortisol.
True or false: The incidence of allergic reactions following administration of etomidate is high.
True or false: The incidence of allergic reactions following administration of etomidate is high.
True or false: Benzodiazepines produce adequate skeletal muscle relaxation for surgical procedures.
True or false: Benzodiazepines produce adequate skeletal muscle relaxation for surgical procedures.
True or false: Benzodiazepines exert anterograde amnesia but do not affect retrograde amnesia.
True or false: Benzodiazepines exert anterograde amnesia but do not affect retrograde amnesia.
True or false: The amnestic potency of benzodiazepines is greater than their sedative effects.
True or false: The amnestic potency of benzodiazepines is greater than their sedative effects.
True or false: Benzodiazepines are commonly used for the treatment of chronic insomnia.
True or false: Benzodiazepines are commonly used for the treatment of chronic insomnia.
True or false: Benzodiazepines have a greater margin of safety compared to barbiturates.
True or false: Benzodiazepines have a greater margin of safety compared to barbiturates.
True or false: Benzodiazepines induce hepatic microsomal enzymes.
True or false: Benzodiazepines induce hepatic microsomal enzymes.
True or false: Benzodiazepines are more addicting than opioids, cocaine, amphetamines, or barbiturates.
True or false: Benzodiazepines are more addicting than opioids, cocaine, amphetamines, or barbiturates.
True or false: Midazolam is the most commonly used benzodiazepine in the perioperative period.
True or false: Midazolam is the most commonly used benzodiazepine in the perioperative period.
True or false: Benzodiazepines can suppress cortisol levels in treated patients?
True or false: Benzodiazepines can suppress cortisol levels in treated patients?
True or false: Dependence on benzodiazepines can occur even with therapeutic doses?
True or false: Dependence on benzodiazepines can occur even with therapeutic doses?
True or false: Benzodiazepine withdrawal symptoms have a time of onset that reflects the elimination half-time of the drug?
True or false: Benzodiazepine withdrawal symptoms have a time of onset that reflects the elimination half-time of the drug?
True or false: Aging and liver disease affect glucuronidation more than oxidative metabolic pathways?
True or false: Aging and liver disease affect glucuronidation more than oxidative metabolic pathways?
True or false: Long-term benzodiazepine administration may accelerate cognitive decline in elderly patients?
True or false: Long-term benzodiazepine administration may accelerate cognitive decline in elderly patients?
True or false: Benzodiazepines have a built-in ceiling effect that prevents them from exceeding the physiologic maximum of GABA inhibition.
True or false: Benzodiazepines have a built-in ceiling effect that prevents them from exceeding the physiologic maximum of GABA inhibition.
True or false: Benzodiazepines are highly absorbed from the gastrointestinal tract following oral administration.
True or false: Benzodiazepines are highly absorbed from the gastrointestinal tract following oral administration.
True or false: Chronic administration of benzodiazepines adversely affects systemic blood pressure, heart rate, or cardiac rhythm.
True or false: Chronic administration of benzodiazepines adversely affects systemic blood pressure, heart rate, or cardiac rhythm.
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.
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.
True or false: Benzodiazepines exert synergistic sedative effects with opioids.
True or false: Benzodiazepines exert synergistic sedative effects with opioids.
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.
