Exam (elaborations) NURS 5220

What are benzodiazepines?️️A class of drugs used for anxiety and other purposes. What are the uses of benzodiazepines?️️Sedation, hypnosis, muscle relaxation, anxiolysis, anticonvulsant, amnesia, insomnia, alcohol withdrawal. What is the structure of benzodiazepines?️️Benzodiazepine ring with 2 nitrogen atoms at positions 1 & 4, phenyl group at position 5, and an electronegative group at position 7. How do benzodiazepines work?️️They promote the binding of GABA to the GABAA receptor, enhancing GABA-induced chloride currents and inhibiting neuronal cell excitation. How are benzodiazepines metabolized?️️They are oxidized in the liver via CYP enzymes, primarily CYP3A4. What are the active metabolites of benzodiazepines?️️Diazepam (with a half-life exceeding 100 hours) and midazolam (rapidly metabolized to an α-hydroxylated compound with biologic activity). Which benzodiazepines have no active metabolites?️️Oxazepam, lorazepam, and temazepam. What factors can alter the metabolism of benzodiazepines?️️Disease and age. What is the duration of action of benzodiazepines primarily determined by?️️The α phase (distribution-redistribution from CNS) dynamics rather than the rate of elimination. What are the pharmacodynamic effects of benzodiazepines on the CNS?️️CNS depressant effects including anxiolysis, sedation, sleep, anticonvulsant, amnesia, muscle relaxation, and inhibition of alcohol withdrawal symptoms. What effect do high doses of benzodiazepines have on CMR02 & CBF?️️They reduce CMR02 & CBF. What effect do benzodiazepines have on the threshold to local anesthetic-induced seizures?️️They increase the threshold to local anesthetic-induced seizures. What is the dose-related effect of benzodiazepines on anterograde amnesia?️️They cause anterograde amnesia at high doses. What are the potential drawbacks of benzodiazepine use?️️Awareness regarding addiction, withdrawal, recreational abuse, and the development of other drug classes has led to a decline in their use. Which CYP enzyme is primarily responsible for the metabolism of benzodiazepines?️️CYP3A4. Which benzodiazepine has a half-life exceeding 100 hours?️️Diazepam. Which benzodiazepine is rapidly metabolized to an α-hydroxylated compound with biologic activity?️️Midazolam. Which benzodiazepines have no active metabolites?️️Oxazepam, lorazepam, and temazepam. What is the primary factor determining the duration of action of benzodiazepines?️️The α phase dynamics of distribution-redistribution from the CNS. What are the CNS depressant effects of benzodiazepines?️️Anxiolysis, sedation, sleep, anticonvulsant, amnesia, muscle relaxation, and inhibition of alcohol withdrawal symptoms. What effect do high doses of benzodiazepines have on CMR02 & CBF?️️They reduce CMR02 & CBF. What effect do benzodiazepines have on the threshold to local anesthetic-induced seizures?️️They increase the threshold to local anesthetic-induced seizures. What is the dose-related effect of benzodiazepines on anterograde amnesia?️️They cause anterograde amnesia at high doses. What does midazolam achieve at low doses?️️Rapid onset, short duration of action, and halflife How long does the effect of midazolam usually last?️️20-30 minutes Does midazolam produce reliable retrograde amnesia?️️No What is midazolam commonly used for?️️Preoperative sedation, anxiolysis, sedation, and amnesia What are the cardiovascular effects of midazolam?️️Minimal effects in commonly used doses, decrease in blood pressure when combined with opioids in patients with heart disease or the elderly What are the respiratory effects of midazolam?️️Dose-dependent respiratory depression, increased when combined with other CNS depressants, most respiratory depressing benzodiazepine How do hypnotic doses of benzodiazepines affect sleep-related breathing disorders?️️Worsen by adversely affecting control of upper airway muscles and decreasing ventilatory response to CO2 What are the adverse effects of midazolam?️️Prolonged sedation, impaired cognition and psychomotor performance, unwanted amnesia, potential for delirium, increased risk of accidents and falls, dependence and withdrawal effects What are the withdrawal effects of benzodiazepines?️️Delirium, anxiety, panic, seizures, insomnia, muscle spasm What are the drug interactions of benzodiazepines?️️Potential for cross-tolerance to nonbenzodiazepine GABA anesthetic agents, augmentation of CNS depressant effects of other sedative-hypnotic anesthetics and opioids What is the most prescribed psychiatric medication in the US?