Chapter 8 - Depressants Flashcards

1
Q

What is a depressant?

A

drug that diminishes physiological activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Therapeutic uses of depressants

A

anxiety, sleep management, seizures, anesthesia
-most produce positive subjective effects (activate reward pathways); high abuse liability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What are some common depressants?

A

alcohol, barbiturates, benzodiazepines, opioids

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Most depressants act through increased activity of ____

A

GABA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Depressants and GABAA receptor

A

Ionotropic receptor that allows entry of Cl- ions; hyperpolarizes neurons which decreases their firing rate; five subunits; two binding sites for GABA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

There are ____ sites on the GABAA receptor that enhance GABA transmission

A

allosteric

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are barbiturates?

A

became available after development of barbital from barbituric acid; became widely used for insomnia, nervousness, sedation, anesthesia; first effective anti-seizure medication

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Barbiturates are ____ depressants and are sometimes referred to as ____

A

CNS; sedatives

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

barbiturates are classified by their…

A

speed of onset and duration of action

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

speeds and durations of barbiturates

A

ultra-shortacting: effects in 20-30s, lasts ~30min ex. thiopental
short-acting/intermediate: ex. pentobarbital
long-acting: effects in ~1hr, last ~12hr ex. phenobarbital

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Barbiturate as a drug of abuse

A

positive reinforcing effects; reduce feelings of stress and anxiety; produce feelings of well-being and lower inhibitions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

depressants enhance GABA inhibition at sites of action such as…

A

cerebral cortex, amygdala, thalamus, and medulla
HOWEVER as doses increase the effects reach deeper into brain cortex>amygdala>medulla
cortex: disinhibition
amygdala: red. anxiety
medulla: resp. depression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Inhibition of ____ accounts for
the effects on seizures, memory, attention, and other cognitive functions

A

cortical activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

the ____ effects of barbiturates are due to the inhibition of the amygdala

A

anti anxiety

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

The effects on ____ result from inhibition of the medulla

A

respiratory function

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

overdose potential of barbiturates

A

main concern is respiratory depression; memory blocking effects (forgetting if they took a dose); long term use can lead to shrinking therapeutic index

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

chronic use of barbiturates causes tolerance to the ____ but not to the ____

A

therapeutic effects: respiratory depressant effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

withdrawling from barbiturates

A

Withdrawal should be done gradually; abrupt withdrawal causes a Barbiturate Abstinence Syndrome (anxiety, muscle weakness, abdominal pain seizures)
-think of it like the opposite of what theyre used for

19
Q

What are benzodiazepines?

A

produces less drowsiness and cognitive inhibition than barbiturates; relatively common for anxiety disorders

20
Q

short-acting benzodiazepines are used as..

A

“as needed” acute anxiety situations

21
Q

intermediate/long-lasting benzodiazepines are used as…

A

relief for or to prevent generalized anxiety disorder

22
Q

Long-lasting benzodiazepines produce ____

A

active metabolites

23
Q

Benzodiazepines abuse

A

High abuse potential; positive subject effects but less than barbiturates

24
Q

Benzodiazepine withdrawal syndrome

A

Characterized by depression, anxiety, mania; can last several months; avoiding withdrawal could be main reason to continue use

25
Q

Risks of using benzodiazepines

A

Accidental injury; poor decision making; most misuse is from combining with alcohol;

26
Q

Benzodiazepines serve as positive modulators by ____

A

binding to an allosteric site known as the benzodiazepine site (separate from barbiturate site)

27
Q

What are the two types of benzodiazepine sites?

A

BZI site: high affinity
BZII site: low affinity

28
Q

What are Z-drugs?

A

non-benzodiazepine hypnotics (sleep aids); generic names typically start w Z; high binding affinity for GABAA receptors

29
Q

Risks of Z-drugs

A

Sleep-related complex behaviours (walking, driving, cooking, eating, conversing while asleep); recommends 8hrs of sleep for effects to wear off

30
Q

What is Gamma-Hydroxybutyrate (GHB)?

A

a drug (white, tasteless, dissolves in water) and a NT; used instrumentally (narcolepsy, schedule II) and recreationally (abused, schedule I); associated with sexual assault

31
Q

What two precursor drugs is GHB easily produced from?

A

GBL (gamma-butyrolactone, immediate precursor of GHB); 1,4 butanediol (readily converted to GHB); biotransformation occurs in “alcohol” metabolic pathway in liver

32
Q

GHB is also produced naturally in the brain from ____

A

GABA
-GHB is stored and released with GABA; GABA is the product of GHB metabolism

33
Q

How many GHB receptors are there?

A

one, with evidence of another
-G-protein-coupled receptor
-inhibitory effects on hippocampus, cerebral cortex, & basal ganglia

34
Q

Pharmacokinetics of GHB

A

concentrated within 45 mins, onset of effects after about 15-20; metabolized into GABA in liver and brain; about 30min half life

35
Q

Pharmacological effects of GHB

A

longer time in deep sleep; subjective effects are time dependent (similar to alcohol; good at first but later effects mood, memory, drowsiness, etc)

36
Q

Overdosing on GHB

A

nausea; decreased BP; decreased HR; unconsciousness
-most emergency room visits related to GHB involve polydrug use, often alcohol

37
Q

What are inhalants?

A

vaporous chemicals with psychoactive effects

38
Q

What are some compounds of inhalants?

A

amyl nitrate (“poppers,” warmth, enhances sexual experiences); nitrous oxide (laughing gas, aerosol spray cans, euphorogenic but can also be a depressant); volatile solvents (hydrocarbon chemicals, toluene, gasoline, acetone)

39
Q

Who uses inhalants?

A

mainly adolescents; mainly bc none of the compounds are legal (easily accessible) and wear off quickly

40
Q

Ways to administer inhalants

A

sniffing (direct inhalation); huffing (soaking a cloth); bagging (inhaling from a bag)

41
Q

Pharmacological actions of inhalants

A

most are depressants (share some mechanisms of actions with alcohol); After several days of use there is an upregulation of NMDA receptors to compensate for this antagonism (tolerance to subjective effects); positive modulation of GABAA receptors

42
Q

4 stages of inhalant effects

A
  1. stimulant like positive subj effects
  2. behaviours resembling alcohol intoxication
  3. enhanced depressant effects
  4. overdose (unconsciousness, seizures, cardiac arrest)
43
Q

How is inhalant overdose dangerous?

A

cardiac arrest is the primary cause of sudden sniffing death syndrome due to poor oxygen availability (occurs when vapors complete with oxygen inhalation and absorption)
-Chronic use of inhalants can lead to loss of brain tissue: ventricular enlargement and white matter degeneration