Sedatives, Anxiolytics, and Hypnotics Flashcards
Sedative Hypnotics
Barbs, BZDs, Z-hypnotics, Propofol, Etomidate
Barbiturates receptor sight of action.
GABAa to open Cl- channel
Phenobarbital clinical indications
preoperative sedation
Secobarbital clinical indications
short term <2 week treatment of insomnia, or acute psychosis
Amnesia
occurs at low doses of anesthetics.
GABA vs Glycine
Brain vs Spinal chord
Barbiturates
Affect GABAa receptors to allow flow of Cl-. Narrow therapeutic window. Loes effectiveness after 2 weeks.
Phenobarbital
Barbiturate. Slow onset, not used as an oral hypnotic. Produces hyperactivity in children.
Secobarbital
short term <2 week treatment of insomnia, or acute psychosis. Only Oral admin.
Benzodiazepines
Acts at GABAa at a different binding site than the GABA. Increase efficacy of GABA. Body can buffer effects – larger therapeutic window. Hypnotics and Anxialytics/Sedatives. When used >2 weeks, risk of physical dependence is great.
Zolpidem acts on what receptor type?
Non-BZ, hypnotic. Acts at GABAa Type 1 only.
Zaleplon acts on what receptor type?
non-BZ, hypnotic. Acts at GABAa Type 1 only.
Propofol MOA?
Stimulates GABA release, similar to EtOH – induces depression. DOC in ambulatory surgery. Monitored anesthesia care. Not for children – acidosis. Pain at sight of injection.
Fospropofol
same as propofol, minus pain at the injection site.
Etomidate is clinically useful in which population?
Patients with a limited CV reserve. Elderly. - does not lower BP. Not analgesic – administered with opioids. Slower recovery to propofol. Steroid and GC effects, pain on injection, myoclonus, post-op N/V.
Describe BZ withdrawal and give symptoms.
occurs when out of system. Restlessness, anxiety, weakness, and generalized seizures. Potential for abuse is only found in drug dependent populations.
Appropriate BZ withdrawal paradigm.
Taper 25%/week until 50% of dose, then 1/8th of dose every 4-7 days.
Alprazolam
Panic, anxiety disorders and PMS. Useful in elderly. Exacerbates ventilatory failure. Not for use in the pulmonary compromised.
Advantage to using BZ for persistent anxiety.
Rapid onset of action. Safe in overdose. Effective for acute treatment.
Disadvantage to using BZ for persistent anxiety.
Cognitive impairment – sedation and memory, psychomotor impairment, Respiratory depression, potentiation of CNS depressants, abuse and dependence, withdrawal syndrome.
Advantage to using Buspirone for persistent anxiety.
Acts on 5HT1a receptors – to inhibit 5HT release. Only for long term anxiety not short term panic attacks.
Disadvantage to using Buspirone for persistent anxiety.
Not cross tolerant with Bzs.
How to switch a patient from a BZ to Buspirone.
Completely taper BZ, prior to initiation of Buspirone.
Two advantages of using Ramelteon as a hypnotic agent.
Shortens latency to sleep with no rebound insomnia or withdrawal symptoms. Melatonin receptor agonist at both MT1&2 in the suprachiasmatic nucleus. No effect in Teens.
Propanolol
performance anxiety, reduces visceral activity
Zopiclone
similar to Bzs
Abecarnil
some specificity for omega 1 GABA receptor
Bretazenil
slightly less locomotor disruption than
SSRIs
GAD, panic disorder, PTSD, social and other phobias
Mirtazapine
comorbidity of Depression and Anxiety.
Recommendation from the guidelines to BZ use for what to prescribe to those who do not respond to any particular hypnotic agent.
Patients who have not responded to any one of these hypnotic drugs, should not be prescribed any of the others.
Indications for Alprazolam.
Panic disorders.
Indications for Meprobamate.
Short-term anxiety symptom relief and sedative-hypnotic.
Three sedation settings, and primary agents.
Monitored anesthesia care, conscious sedation, deep sedation
Monitored anesthesia care
superficial, use local anesthesia combined with Midazolam, Propofol, or Opioids. - pre-midazolam followed by Propofol, Ketamine, opioids
Conscious sedation
patient is verbally responsive. IV Diazepam, Midazolam, or Propofol.
Deep sedation
patient requires assisted respiration, difficult to arouse. IV Thiopental, Midazolam, Propofol, Opioids and Ketamine.
efficacy of oral Midazolam as a premed to sedate and calm pediatric patients.
Best results when given 1mg/Kg up to 20mg. Only significant difference between upper and lower dosage.
One advantage to using Buspirone over BZ.
No potential for abuse, dependence or withdrawal syndrome. Patients maintain cognitive and psychomotor skills. Can be used with EtOH and other CNS agents. Effective relief of persistent anxiety.
One disadvantage to using Buspirone over BZ.
Less effective in recent BZ users. Gradual onset of action 2-4 weeks. Not effective in panic disorder.
2007 FDA recommendation in response to demonstrated occurances of sleep-driving, that manufacturers should do with respect to consumers.
Strengthen product labeling to include stronger language concerning potential risks. Letters to Health Care Providers to inform them about new warnings. Patient Medication Guides to inform about drugs.
BZ that is recommended by Guidlines for Pain Management for use with nocturnally predominant pain.
Clonazepam
