Axiolytics, Sedatives, Hypnotics

Question 1

What are the benzos used to treat anxiety?

Answer 1

diazepam and clonazaepam (all the zepams)

Question 2

What is the mechanism of action for the benzos?

Answer 2

increases frequency of chloride channels by activating GABA receptor, leading to reduced action potentials

Question 3

What are the uses for benzos?

Answer 3

reduces anxiety (LOW doses), sedative and hypnotic, anterograde amnesia (take before colonoscopy), anticonvulsant, muscle relaxant (HIGH doses)

Question 4

How do benzos help sleeping

Answer 4

reduce sleep latency, increase Stage II of non-REM sleep, decrease nocturnal awakenings, increase sleep duration

Question 5

Which benzo is used for panic disorders?

Answer 5

ALPrazolam

Question 6

What happens when you mix benzos and ethanol?

Answer 6

cross tolerance

Question 7

Describe the differences in Flurazepam, Temazepam, and Triazolam as sleep aids.

Answer 7

Flurazepam is long lasting, sleep hangovers are an issue
Temazepam give 1-2 hours before bad and prevents frequent awakening
Trizolam - induces sleep, short sleep latency

Question 8

In which patients should benzos be avoided?

Answer 8

pregnant and nursing mothers

Question 9

How are benzos metabolized?

Answer 9

hepatic system, metabolized into active components

Question 10

Which types of benzos have a more severe withdrawal (short, intermediate, or long-term)

Answer 10

Benzos with a short half-life

Question 11

What is a benzodiazepine antagonist?

Answer 11

Flumazenil

Question 12

What is Buspirone used for?

Answer 12

Generalized Anxiety Disorder

Question 13

Which receptor does Buspirone act on?

Answer 13

Seratonin receptor

Question 14

What are side effects of Buspirone?

Answer 14

Seratonin receptor, partial agonist

Question 15

What is the mechanism of action of the barbiturates?

Answer 15

Bind to GABA alpha receptor, prolong duration of open chloride channels

Question 16

What are the names of the barbiturates?

Answer 16

Pentobarbital, Phenobarbital, Thiopentone, Secobarbital, Amobarbital

Question 17

What are the three actions of barbiturates?

Answer 17

Depress CNS (low doses - sedation, high doses - hypnosis, anesthesia, coma, death); Central respiratory depression; Enzyme induction of P450 system increases inactivation or increases activation

Question 18

What are the therapeutic uses of Barbiturates?

Answer 18

Anesthesia, Anticonvulsant (tonic clonic, status epilepticus, and eclampsia), Anxiety (mild sedative, suppresses REM)

Question 19

Should barbiturates be given to pregnant women?

Answer 19

NO, crosses placenta and can depress fetus

Question 20

What are the adverse effects of barbiturates?

Answer 20

drug hangover - feeling of tiredness long after waking
CI in patients with acute intermittent porphyria
Severe W/D can result in death
overdose can cause respiratory and cardiovascular depression

Question 21

What are Zolpidem, Zaleplon, and Eszopiclone used for?

Answer 21

sleeping

Question 22

What are the omega benzodiazepene agonists (BZ1 receptor agonists)?

Answer 22

Zolpidem, Zaleplon, and Eszopiclone

Question 23

What are adverse effects of Zolpidem, Zaleplon, and Eszopiclone?

Answer 23

dry mouth, nightmares, GI upset, unpleasant taste, but DO NOT alter stages of sleep

Question 24

How are the BZI receptor agonists metabolized?

Answer 24

hepatic oxidation by 450 to inactive products

Question 25

What receptors does Ramelteon act on?

Answer 25

agonist at MT1 and MT2 receptors (melatonin receptors)

Question 26

What are the adverse effects of melatonin?

Answer 26

somnolence (drowsiness), increased prolactin levels

Question 27

Why is ethanol a bad sleep aid?

Answer 27

Takes high doses to get sleep aid effect, synergistic with other sedatives, CNS depression with sedatives/depressants.