Pharm: Sedatives + Hypnotics

Question 0

What are the indications for phenobarbital?

Answer 0

Pre-operative sedation

Question 1

What is the receptor for barbiturates?

Answer 1

GABA receptor agonist - opens a chloride channel

Question 2

What is the indication for secobarbital?

Answer 2

Short term treatment of Insomnia

Used in acute psychosis

Question 3

How do benzodiazepines function?

Answer 3

Bind to a site on GABA-a receptors that is separate from GABA. The function is to allow more chloride ions flow in once GABA binds for increased efficacy.

Question 4

What are symptoms of benzodiazepine withdrawal and how is this prevented?

Answer 4

Restlessness, anxiety, weakness, generalized seizures

To avoid withdrawal:

• Taper 25% / week down to 50% of the dose
• Then once you’ve reached 50% of the original dose, drop to 1/8 the dose every 4-7 days

Question 5

What kind of drugs are zolpidem and zaleplon? On what kind of receptor type do they act?

Answer 5

They are Z-hypnotics that act on the GABA-a type 1 receptors which are rapid onset for hypnosis or sleep.

Question 6

Describe the MOA for propofol.

Answer 6

Acts on presynaptic cells to stimulate GABA release.

Question 7

What population is etomidate a useful drug?

Answer 7

Good for patients with limited cardiovascular reserve.

It doesn’t lower blood pressure and is not analgesic.

Question 8

What is important to remember when switching between a BZ and buspirone?

Answer 8

Buspirone is not cross tolerant with benzodiazepines, which means that it cannot replace a BZ and prevent withdrawal symptoms of BZs. It acts on serotonin 1A receptors NOT GABA receptors.

Question 9

What are two advantages of using ramelteon as a hypnotic agent?

Answer 9

Melatonin receptor agonist.

Shortens latency to sleep with no rebound insomnia
No withdrawal symptoms.

Question 10

What are the recommended guidelines for BZ use in patients with insomnia that do not respond to hypnotics?

Answer 10

• The hypnotic should be used for short term use
• for its specific indications
• the cheapest one should be prescribed
• no switching between similar class hypnotics unless there is an allergy to a specific one
• patients that do not respond to these should NOT be prescribed another one

Question 11

What are indications for alprazolam?

Answer 11

Panic disorders

Question 12

What are indications for meprobamate?

Answer 12

Short-term anxiety and sedative hypnotic

Question 14

Describe the efficacy of oral midazolam as a premedicant to sedate and calm peds patients.

Answer 14

Given orally in peds patients. 90% achieved satisfactory sedation and axiolysis and ease of separation from parents or guardians within 30 minutes of administration.

Question 15

What are advantages and disadvantages to using buspirone in stead of BZ?

Answer 15

Adv.

• relief of anxiety within 2-4 weeks
• no addiction, abuse, or withdrawal
• used with alcohol or other CNS agents
• modulates 5HT at certain receptors

Dis.

• less effective than BZ
• not effective in panic disorders

Question 16

What did the FDA recommend to hypnotic manufacturers due to increased amount of sleep-driving?

Answer 16

Labels should include stronger language concerning potential risks like sleep driving or allergies.
They also recommended letter be sent to healthcare providers to inform them of the risks in the hope that the providers create guidelines for patients when prescribing these meds.

Question 17

What benzodiazepine is prescribed for management of nocturnally predominant pain?

Answer 17

Clonazepam

Question 20

What are the 3 sedation settings and the primary sedative agents for each?

Answer 20

1. Monitored anesthesia care: midazolam, propofol, opioids
2. Conscious sedation: IV diazepam, midazolam, propofol
3. Deep Sedation: IV thiopental, midazolam, propofol, opioids, ketamine