Sedatives, Anxiolytics, and Hypnotics

Question 1

Sedative Hypnotics

Answer 1

Barbs, BZDs, Z-hypnotics, Propofol, Etomidate

Question 2

Barbiturates receptor sight of action.

Answer 2

GABAa to open Cl- channel

Question 3

Phenobarbital clinical indications

Answer 3

preoperative sedation

Question 4

Secobarbital clinical indications

Answer 4

short term <2 week treatment of insomnia, or acute psychosis

Question 5

Amnesia

Answer 5

occurs at low doses of anesthetics.

Question 6

GABA vs Glycine

Answer 6

Brain vs Spinal chord

Question 7

Barbiturates

Answer 7

Affect GABAa receptors to allow flow of Cl-. Narrow therapeutic window. Loes effectiveness after 2 weeks.

Question 8

Phenobarbital

Answer 8

Barbiturate. Slow onset, not used as an oral hypnotic. Produces hyperactivity in children.

Question 9

Secobarbital

Answer 9

short term <2 week treatment of insomnia, or acute psychosis. Only Oral admin.

Question 10

Benzodiazepines

Answer 10

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.

Question 11

Zolpidem acts on what receptor type?

Answer 11

Non-BZ, hypnotic. Acts at GABAa Type 1 only.

Question 12

Zaleplon acts on what receptor type?

Answer 12

non-BZ, hypnotic. Acts at GABAa Type 1 only.

Question 13

Propofol MOA?

Answer 13

Stimulates GABA release, similar to EtOH – induces depression. DOC in ambulatory surgery. Monitored anesthesia care. Not for children – acidosis. Pain at sight of injection.

Question 14

Fospropofol

Answer 14

same as propofol, minus pain at the injection site.

Question 15

Etomidate is clinically useful in which population?

Answer 15

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.

Question 16

Describe BZ withdrawal and give symptoms.

Answer 16

occurs when out of system. Restlessness, anxiety, weakness, and generalized seizures. Potential for abuse is only found in drug dependent populations.

Question 17

Appropriate BZ withdrawal paradigm.

Answer 17

Taper 25%/week until 50% of dose, then 1/8th of dose every 4-7 days.

Question 18

Alprazolam

Answer 18

Panic, anxiety disorders and PMS. Useful in elderly. Exacerbates ventilatory failure. Not for use in the pulmonary compromised.

Question 19

Advantage to using BZ for persistent anxiety.

Answer 19

Rapid onset of action. Safe in overdose. Effective for acute treatment.

Question 20

Disadvantage to using BZ for persistent anxiety.

Answer 20

Cognitive impairment – sedation and memory, psychomotor impairment, Respiratory depression, potentiation of CNS depressants, abuse and dependence, withdrawal syndrome.

Question 21

Advantage to using Buspirone for persistent anxiety.

Answer 21

Acts on 5HT1a receptors – to inhibit 5HT release. Only for long term anxiety not short term panic attacks.

Question 22

Disadvantage to using Buspirone for persistent anxiety.

Answer 22

Not cross tolerant with Bzs.

Question 23

How to switch a patient from a BZ to Buspirone.

Answer 23

Completely taper BZ, prior to initiation of Buspirone.

Question 24

Two advantages of using Ramelteon as a hypnotic agent.

Answer 24

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.

Question 25

Propanolol

Answer 25

performance anxiety, reduces visceral activity

Question 26

Zopiclone

Answer 26

similar to Bzs

Question 27

Abecarnil

Answer 27

some specificity for omega 1 GABA receptor

Question 28

Bretazenil

Answer 28

slightly less locomotor disruption than

Question 29

SSRIs

Answer 29

GAD, panic disorder, PTSD, social and other phobias

Question 30

Mirtazapine

Answer 30

comorbidity of Depression and Anxiety.

Question 31

Recommendation from the guidelines to BZ use for what to prescribe to those who do not respond to any particular hypnotic agent.

Answer 31

Patients who have not responded to any one of these hypnotic drugs, should not be prescribed any of the others.

Question 32

Indications for Alprazolam.

Answer 32

Panic disorders.

Question 33

Indications for Meprobamate.

Answer 33

Short-term anxiety symptom relief and sedative-hypnotic.

Question 34

Three sedation settings, and primary agents.

Answer 34

Monitored anesthesia care, conscious sedation, deep sedation

Question 35

Monitored anesthesia care

Answer 35

superficial, use local anesthesia combined with Midazolam, Propofol, or Opioids. - pre-midazolam followed by Propofol, Ketamine, opioids

Question 36

Conscious sedation

Answer 36

patient is verbally responsive. IV Diazepam, Midazolam, or Propofol.

Question 37

Deep sedation

Answer 37

patient requires assisted respiration, difficult to arouse. IV Thiopental, Midazolam, Propofol, Opioids and Ketamine.

Question 38

efficacy of oral Midazolam as a premed to sedate and calm pediatric patients.

Answer 38

Best results when given 1mg/Kg up to 20mg. Only significant difference between upper and lower dosage.

Question 39

One advantage to using Buspirone over BZ.

Answer 39

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.

Question 40

One disadvantage to using Buspirone over BZ.

Answer 40

Less effective in recent BZ users. Gradual onset of action 2-4 weeks. Not effective in panic disorder.

Question 41

2007 FDA recommendation in response to demonstrated occurances of sleep-driving, that manufacturers should do with respect to consumers.

Answer 41

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.

Question 42

BZ that is recommended by Guidlines for Pain Management for use with nocturnally predominant pain.

Answer 42

Clonazepam