Pharm - Benzodiazepines Flashcards
- Give the recommendation from the guidelines for benzodiazepine use for what to prescribe to patients who do not respond to any particular hypnotic agent.
It is recommended that, because of the lack of compelling evidence to distinguish between zaleplon, zolpidem, zopiclone or the shorter-acting benzodiazepine hypnotics, the drug with the lowest purchase cost (taking into account daily required dose and product price per dose) should be prescribed
Patients who have not responded to one of these hypnotic drugs should not be prescribed any of the others.
- Apply the indications for alprazolam to clinically-relevant case scenario.
Alprazolam is a benzodiazepine
Alprazolam is for panic disorders
- Apply the indications for meprobamate to clinically-relevant case scenario.
Meprobamate is a benzodiazepines
Meprobamate is for short-term anxiety and a sedative-hypnotic. Meprobamate is used for the management of anxiety disorders or for the short-term relief of the symptoms of anxiety.
- Apply three sedation settings, including the primary sedative agents, to clinically-relevant case scenarios.
Monitored anesthesia care (superficial) - Use regional or local anesthesia combined with midazolam, propofol or opioids. Pre-midazolam IV followed by propofol or ketamine or opioids.
Conscious sedation –IV diazepam, midazolam, propofol; pt. responsive verbally.
Deep sedation – pt needs breathing help, difficult to arouse; IV-thiopental, midazolam, propofol, opioid analgesics and ketamine.
- Describe the efficacy of oral midazolam as a premedicant to sedate and calm pediatric patients.
preoperatively relieves anxiety, provides sedation, light anesthesia, anterograde amnesia of perioperative events.
More than 90% of treated patients achieved satisfactory sedation and anxiolysis at least one timepoint within 30 minutes post-treatment and 70% within 10 minutes
Apply the advantages in the use of buspirone as opposed to benzodiazepines to a clinically-relevant case scenario.
Buspirone acts on 5HT1A receptors, perhaps to inhibit 5HT release.
Effective relief of persistent anxiety within 2 to 4 weeks
No potential for abuse, dependence or withdrawal syndrome
Patients maintain cognitive skills (e.g. memory function) and psychomotor skills (e.g ability to drive a car)
Can be used with alcohol and other CNS agents
Modulates serotonin at specific receptors (5HT1A)
Apply the disadvantages in the use of buspirone as opposed to benzodiazepine
s to a clinically-relevant case scenario.
Disadvantages:
May be less effective in recent benzodiazepine users
Gradual onset of action (2 to 4 weeks for effect)
Not effective in panic disorder (better with generalize anxiety disorder (GAD)
- Explain what the FDA recommended in 2007, in response to demonstrated occurrences of sleep-driving, that manufacturers of hypnotic agents should do with respect to consumers.
FDA notified healthcare professionals of its request that all manufacturers of sedative-hypnotic drug products, a class of drugs used to induce and/or maintain sleep, strengthen their product labeling to include stronger language concerning potential risks.
These risks include severe allergic reactions and complex sleep-related behaviors, which may include sleep-driving.
Sleep driving is defined as driving while not fully awake after ingestion of a sedative-hypnotic product, with no memory of the event.
- Give a benzodiazepine that is recommended by the Guidelines for Pain Management for use with nocturnally predominant pain.
Clonazepam, a benzodiazepine, is used by many providers for nocturnally predominant pain.
- Discuss the receptor site of action for barbiturates (be prepared to discuss how this differs for BZs).
Barbiturates are agonists at GABA receptor site. Act as an agonist at the GABAA receptor. Activation of the GABAA receptor causes sedation. A direct agonist Barbiturates differ from Benzodiazepines in that BZs enhance activation of GABA.
- Apply the indications for phenobarbital and secobarbital to a clinically-relevant case scenario.
Phenobarbital is used to provide sedation preoperatively.
Secobarbital is used in short-term (<2 weeks) treatment for insomnia and acute phsycosis. Typically, barbiturates lose effectiveness after two weeks
- Draw a diagram showing a GABA receptor with sites of BZ and barbiturate action. Discuss how stimulation at these sites alters cell function and how this influences the overdose potential of benzodiazepines.
Benzodiazepines acts at a site on GABAA receptors that is separate from the GABA site itself. From this site the action of GABA in opening chlorine ion channels is increased, but no effect without GABA, therefore body can compensate.
The body has the capacity to shut down the release of GABA. Overloading the body on benzodiazepems does not continously create a response. This creates a wider therapeutic window for benzodiazepines compares to barbituates.
- Describe BZ withdrawal and give symptoms. Apply the appropriate withdrawal paradigm to a clinically-relevant case scenario.
When used for prolonged periods (>2-3 weeks) the chance of physical dependence is great.
Withdrawal may occur when BZ are out of the system (I.e. Soon after for short-acting, longer for longer half-lives), with symptoms of restlessness, anxiety, weakness, and generalized seizures.
Taper 25% per week to 50% of dose, then 1/8th dose every 4-7 days.
Week 1: down to 75%
Week 2: down to 50%
Week 3: 1/8th of 50%
Week 4: 1/8th of 43.75%
- Describe the general receptor type upon which zolpidem and zaleplon act.
The Z-hypnotics for sleep aids
Zolpidem (Ambien) Acts at GABAA type 1(type 1 means a specific combination of subunits) only, I.e. less anti-convulsant effect. Non-benzodiazepine agent used as sedative hypnotic. Rapid onset, given before retiring.
Zaleplon (Sonata) Short-acting sedative, non-BZ, pyrazolopyrimidine acts at type1 GABA receptors (omega1). Fast onset and short terminal elimination half-life.
May have anxiolytic actions.
- Describe the particular MOA for propofol.
Propofol stimulates GABA release (like EtOH). Agent of choice for ambulatory surgery, no nausea and sense of well-being, given IV.
Has a rapid recovery.
