Anxiolytic-sedative-hypnotic Drugs

Question 0

What does sedation mean?

Answer 0

Decreases activity, calm, although awake

Question 1

What does anxiolytic mean?

Answer 1

Px is relaxed, unconcerned with surroundings and is fully functional

Question 2

What does hypnosis mean?

Answer 2

Drowsiness and leads to sleep (noise hey wake up)

Question 3

What does anesthesia mean?

Answer 3

Not wake up if noise

Question 4

What factors determine the duration of action and clinical utility of barbiturates?

Answer 4

Linear slope of dose and effects

Question 5

What is the action of barbiturates on electrically excitable tissue?

Answer 5

• Extends duration of GABA channel opening
• At high levels may open the channel
• reversible depression on all excitatory tissue

Question 6

What is meant by pharmacokinetic/metabolic tolerance?

Answer 6

Increased rate of drug metabolism

Question 7

What is meant by pharmacodynamic tolerance?

Answer 7

Changes in responsiveness of the CNS

Question 8

What is the mechanism of barbiturates?

Answer 8

• increases the duration of the opening of GABA channels

- termination of action is by redistribution of ultra fast acting drugs (thiopental) outside the CNS

Question 9

What is the mechanism of benzodiazepines?

Answer 9

• ups the frequency of the opening of GABA a receptor chloride channel

Question 10

What is changing the urinary pH useful in treating an overdose of phenobarbital?

Answer 10

• phenobarbital is a weak acid
• weak acids are re absorbed at a low pH
• increasing the pH can lead to increased drug excretion
• treat and overdose with sodium bicarbonate
• only works with phenobarbital
• DNW with high lipid soluble barbs

Question 11

What are possible benefits of non-benzodiazepine benzodiazepine receptor agonists?

Answer 11

A

Question 12

What do sedative-hypnotic drugs do at low and high doses?

Answer 12

Low: relief anxiety and cause sedation (a few don’t)
High: encourage sleep, general anesthetics, death

Question 13

What do the benzos and barbs follow for there dose-effect curve?

Answer 13

Barbs - linear, easy to overdose

Benzos - non linear, harder to overdose

Question 14

What is Valium?

Answer 14

Diazepam

Question 15

What do barbiturates end with?

Answer 15

-tal

Question 16

Why are there secondary effects of barbiturates (anesthesia and bad effects)?

Answer 16

• Antagonist of the AMPA glutamate receptor
• non synaptic membrane effects other than glu and GABA
• this is the reason it is a good CNS depressant

Question 16

How are barbiturates excreted?

Answer 16

• metabolized and excreted
• liver
• exceptions: phenobarbital is excreted as is and around 4-5 day. Thiobarbiturates is the only fast excreted one

Question 17

What do barbs do for metabloism of other drugs?

Answer 17

• effect cyt P450

- effect metabolism of other Drugs and itself

Question 18

What is unique about phenobarbital in relation to tolerance?

Answer 18

Both pharmacodynamic and pharmacokinetic tolerance

Question 19

What do the barbs and benzos do to sleep?

Answer 19

• stage 2 sleep is increased (rapid onset)
• REM sleep duration is decreased
• stage 4 - slow wave sleep is decreased

Question 20

What is the main reason barbs are a anesthetic?

Answer 20

High lipid solubility

Other as mentioned

Question 21

What is metharbital?

Answer 21

Prodrug form of phenobarbital

Question 22

What other random thing is phenobarbital used to treat?

Answer 22

Tonic-clonic seizures

Question 23

What are the adverse effects of barbs?

Answer 23

CV (only a problem clinically if there is a disorder)
Respiratory depression
Reversible depression of all excitable tissue

Question 24

What is significant of the dependance of barbs?

Answer 24

Anxiety relief, euphoria is good and addictive

- continuous drug administration is required to prevent withdrawal

Question 25

What is absorption/distribution of benzos related to?

Answer 25

Lipophilicity

Question 26

What benzos are extremely rapid onset wise?

Answer 26

Triazolam followed by diazepam

Question 27

What is significant with benzos biotransformation?

Answer 27

Metabolized by the liver

• metabolite have effects
• long half lives
• do not effect cyt P450

Question 28

What is the main mechanism of tolerance for benzos?

Answer 28

Pharmacodynamic

Question 29

What is an interesting side effect of benzos?

Answer 29

Dose-dependent anterograde amnesic

Can’t remember events occuring while on the drug

Question 30

What happens when large doses of benzos are used for anesthesia?

Answer 30

A persistent postanesthetic respiratory depression

Question 31

What can treat postanesthetic respiratory depression caused by benzodiazepines?

Answer 31

Flumazenil

Question 32

What are more useful for anti-convulsants effects?

Answer 32

Benzos, lees CV and respiratory depression

Question 33

What are some non-benzo benzo receptor agonists?

Answer 33

Zolpidem - ambien
Zaleplom - sonata
Eszoplicone - lunesta

Question 34

What do non benzo benzo receptor agonist do?

Answer 34

Specific GABA subunits

- only for sedation

Question 35

What are advantages of non benzo benzo receptor agonists?

Answer 35

• rapid onset
• short duration of action
• slow tolerance dependance

Question 36

What is Buspirone?

Answer 36

• no sleep
• only anxiolytic effects
• disconnect between levels in the body and effects, take a week to have an effect
• do effects on driving
• maybe patial agonist of serotonin 1 a
• extensive first pass metabolism in the liver

Question 37

What does Buspirone inhibit?

Answer 37

CYP3A4

Question 38

What is Ramelteom (Rozerem)?

Answer 38

• melatonin receptor agonist 1 and 2 in suprachiasmic nucleus
• no rebound

Question 39

What can propranolol do for sleep?

Answer 39

Beta blocker

No sleep, chronic anxiety