Thursday 1 - Slattery - anxiolytics/hypnotics

Question 1

hypnotics

what do they do at low doses
medium
high

Answer 1

anti anxiety (anxiolytic)

decreases activity/promotes sleep

sedation/anesthesia

Question 2

newer hypnos: are the dose/effect curves linear or nonlinear?

why?

Answer 2

nonlinear

then you don’t hit the more dangerous Sx as easily.

there effects start to “level off” at higher doses

Question 3

barbiturates

3 kinds
mech
solubility

Answer 3

phenobarbital - less lipid soluble
pentobarbital
Thiopental - highly lipid soluble

Binds to the GABAa receptor, which is a component of a chloride channel. Chloride is let into the cell and the cell hyperpolarizes

increases the DURATION of of the GABA-gated chloride channels

(at huge doses, it might also be GABA mimetic)

Question 4

most common benzodiazepine

Answer 4

diazepam (vallium)

Question 5

Z’s drugs

Answer 5

zoplidem

zapelon

Question 6

Tx for phenobarbitol overdose

Answer 6

increase pH of urine via IV sodium bicarbonate

this doesn’t work for the other barbs

Question 7

what happens when you build up a tolerance to barbiturates

Answer 7

as the effect of the barbs decreases, so does the actual plasma concentrations.

phenobarbitol induces the activity of the enzymes that are breaking it down

aka pharmacokinetic tolerance

Question 8

pharmacokinetic tolerance vs pharmacodynamic tolerance

Answer 8

pharmacokinetic tolerance - plasma levels of the drug decrease as the effect decreases (drugs induce the activity of the enzymes that break it down)

pharmacodynamic tolerance - some sort of disconnect between receptor binding and functional output of the signal

Question 9

barbs general effect of patterns of sleep

Answer 9

can induce sleepiness, but causes less deep and REM sleep

Question 10

Benzodiazepines

4 types

Answer 10

diazepam - rapid
lorazepam
triazolam - very rapid
alprazolam

Question 11

Benzodiazepines

mech

Answer 11

Bind GABAa

release Cl

enhance GABA’s effects allosterically without directly activating GABAa or opening the associated chloride channels

increases the frequency of the chloride channel-opening events.

Question 12

Benzodiazepines

metabolism occurs where in body
why is the metabolizm noteworthy

Answer 12

liver metabs them

have many pharmacologically active metabolites:
desmethyldiazepam for example is a product of diazepam and has a half life of like 48 hours or some biz

Question 13

what kind of tolerance is exhibited in benzos

Answer 13

primarily pharmacodynamic tolerance (drug in plasma doesn’t go down when tolerance is built up)

there is some sort of disconnect between the drug hitting the receptor and the message getting through (most likely decrease in GABA receptors by the body)

Question 14

what type of amnesia does benzos cause

Answer 14

anterograde amnesia (cannot remember what happened when you were on the drug)

Question 15

flumazonil

Answer 15

displaces benzodiazepines from GABAa

Question 16

barbs or benzos for treating convulsions? why?

Answer 16

benzos:

they have less effect on the CNS

Question 17

non-benzo benzo receptor agonists

1 main one

used for

Answer 17

zolpidem (ambien)

bind GABAa

benzos bind all GABAa’s, but these only bind to SOME GABAa’s

only used to promote sleep, rapid onset, short duration of action, slow tolerance development.

Question 18

buspirone

Answer 18

anxiolytic effects without the muscle relaxant or anticonvulsant properties.

anxiolytic effects may take weeks to establish

doesn’t effect driving skills

Question 19

ramelteon

Answer 19

novel hypnotic used for patients who have trouble falling asleep

acts on melatonin receptors