Anxiolytics: Slattery

Question 1

What does an anxiolytic do to a patient?

Answer 1

Relaxed, unconcerned with surroundings, fully functional.

Question 2

What does a sedative do?

Answer 2

Decreases activity, calms, patient is still awake.

Question 3

What does a hypnotic do?

Answer 3

Drowsiness, facilitates the onset and maintenance of sleep, patient may be easily aroused.

Question 4

What does a general anesthetic do?

Answer 4

Loss of consciousness. Patient cannot be aroused.

Question 5

What is the difference between Barbiturates and Benzodiazepines in terms of dose?

Answer 5

Barbiturates can be increased to higher than what is needed for hypnosis and may lead to a state of general anesthesia or coma.

Benzodiazepines require proportionately greater dosage to achieve depression beyond hypnosis.

Question 6

Name the barbiturates.

Answer 6

Phenobarbital, Thiopental, Pentobarbital.

Question 7

How do barbiturates work?

Answer 7

They increase the time that the chloride channel is open on a GABA A receptor, Hyperpolarizing the cell.

Question 8

Why is it easy to push barbiturates into the coma and death stage?

Answer 8

They aren’t very selective. They also depress the excitatory actions of Glutamate by binding to the AMPA receptor.

Question 9

Which Barbiturate is really lipid soluble so it works fast?

Answer 9

Thiopental.

Question 10

What accounts for short duration of action of barbiturates that is useful in recovery from anesthesia?

Answer 10

Rapid tissue redistribution.

Question 11

How are barbiturates metabolized and how does this make you take dosing into account?

Answer 11

Metabolized by the liver SLOWLY. The half life can be up to 5 days (Phenobarbital) so multiple dosing can lead to cumulative effects.

Question 12

How are barbiturates excreted? Is it ever in an unchanged form?

Answer 12

Via the kidney. For some, significant percentage of the drug is excreted unchanged (Phenobarbital 25 %).

Question 13

How do you treat an overdose of a Barbiturate?

Answer 13

IV Sodium bicarbonate (Increase urinary pH)

Question 14

Describe the pharmacokinetics of Barbiturates.

Answer 14

Barbiturates have the ability to increase CYP450: this can decrease its own function and gives it potential for other drug interactions.

Question 15

What effects do barbituates and benzodiazapines have on sleep?

Answer 15

Decrease time it takes to fall asleep and increase the duration of stage 2 non-REM sleep. The duration of REM and stage 4 non-Rem sleep go down.

Question 16

Which barbiturate is an effective treatment for tonic-clonic seizures?

Answer 16

Phenobarbital.

Question 17

Name the Benzodiazepines.

Answer 17

Diazepam, Lorazepam, Triazolam, Alprazolam.

Question 18

How do benzodiazepines work?

Answer 18

Bind GABA A receptor! Increase the frequency of the chloride channels opening.

Question 19

Do bentos increase CYP450 like barbituates?

Answer 19

No

Question 20

How would you describe the tolerance to benzodiazepines.

Answer 20

Primarly pharmacodynamic. Due to down regulation of GABA A receptors.

Question 21

Sedation from benzodiazepines exerts dose-dependent Anterograde amnestic effects, what does this mean?

Answer 21

Inability to remember events occurring during drug’s duration of action.

Question 22

How do you reverse persistent post-anesthetic respiratory depression from a benzodiazepine?

Answer 22

Flumazenil (Benzo binding site antagonist)

Question 23

Which benzodiazepine has a short half-life so you may see signs of withdrawal between doses?

Answer 23

Triazolam.

Question 24

What are the effects of Benzodiazepines and Barbituates on CV and respiratory function?

Answer 24

No adverse effects unless an underlying issue.

At toxic doses, myocardial contractility and vascular tone may be depressed but it is reversible.

Question 25

Describe Zolpidem (Ambien).

Answer 25

Agonist to benzodiazepine binding site on GABA A receptor (selective to certain receptor subtypes).

Rapid onset, promotes sleep, no anxiolytic properties.

Question 26

Clinically, what are barbituates used for?

Answer 26

Hypnosis, seizure control, anesthesia induction.

Question 27

Clinically, what are benzodiazepines used for?

Answer 27

Anxiety, Insomnia, Seizures, Muscle relaxation, Pre-anesthetic.

Question 28

How does Buspirone work?

Answer 28

Relieves anxiety by being a partial agonist at 5-HT-1a receptors and D2 receptors.
CYP3A4 metabolized.
Less psychomotor effects than benzos so the patient can drive.

Question 29

What is Ramelteon used for and how does it work?

Answer 29

It helps people fall asleep.
It is an agonist of the MT1 and MT2 melatonin receptors in the suprachiasmatic nuclei of the brain.
*No rebound insomnia if you go off of it.