Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Psychopharmacology > Final: Anxiolytics > Flashcards

Final: Anxiolytics Flashcards

1
Q

What are the differences between GABAA and GABA-B Receptors?

A 
GABA-A: 
Axodendritic/somal
Ionotropic 
Postsynpatic inhibition
Cl- influx 
IPSP (hyperpolarization)
decrease AP 
target of depressants

GABA-B:
AxoAXONAL, metabotropic, presynaptic. Decrase Ca2+ influx, decrease transmitter release. GHB is example, so if Baclofen.

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

What 3 factors affect the onset/duration of barbiturates?

A
  1. lipid solubility
  2. Plasma protein binding
  3. rate of excretion
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

How do you synthesize barbiturate

A

Malonic acid (apple ester) + Urea (urine) –> Barbituric Acid –> Barbiturate

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

Short acting Barbiturates

A

1) Thiopental = anesthetic
Rapid enter, slow to leave. Why? Lipid soluble. Cross BBB to get in fast, then absorbed in fat.
2) Methohexital

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

Intermediate-to-short acting barbiturates

A 
These are the ones getting abused
1) Secobarbitals (red)
2) Pentobarbital (yellow)
3) Amobarbital (blue)
(SPA, or RYB)

*Use: Anesthesia, hypnosis, anti-anxiety

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

Long-acting barbiturates

A

1) phenobarbital (Luminal)- lasts 10-12 hours
2) Therapeutically useful in epilepsy

*Use: seizures, sedation

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

Are barbiturates GABA agonists/antagonists?

A

NO!

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

Are barbiturates GABA agonists/antagonists? If not, then wtf is going on?

A

NO! They are neither!

They bind to increase receptor affinity for GABA.

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

Barbiturate Mechanisms of Action

A

1) Increases affinity of GABA-A receptor
2) facilitates coupling of GABA-A receptor to Cl- channel.
3) Opens Cl- Channel directly

More: Block AMPA, bind to various ionotropic receptors [N], in high doses

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

*Barbiturate Mechanisms of Action

A

1) Increases affinity of GABA-A receptor
2) facilitates coupling of GABA-A receptor to Cl- channel.
3) Opens Cl- Channel directly

More: Block AMPA, bind to various ionotropic receptors [N], in high doses

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

GABA-A receptors

Alpha Subunit
Beta Subunit
Gamma Subunit

Where are the barbiturates?

A

1) Alpha- picrotoxin?, ethanol
2) Beta- neurosteroids, barbiturates, GABA
3) Gamma- Benzodiazepines

Barbiturates site near middle of channels, can open ion channel on their own

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

What is a GABA agonist?

A

Muscimol

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

Allosteric regulation of GABA binding to Gaba-A receptor by depressants

A

1) depressant increases affinity of gaba for receptor
2) Allosteric effect
3) Binding of regulatory site that is not active site changes shape of active site

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

Benzodiazepines:

1) Admin
2) Absorption
3) Action
4) Distribution
5) biotransformation

A

1) Admin- oral, apenteral
2) WEAK BASE, GI Tract
3) 6-24 hr. depends onrate, biotranformation, ppb
4) Cross BBB
5) Converted by lier to active/inactive metabolites

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

*What 3 factors affect onset/duration of BENZODIAZEPINe action?

A

1) BIOTRANSFORMATION
2) ppb
3) rate of excretion

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

Short Acting Benzodiazepines

A

1) *Alprazolam (Xanax)

2) Triazolam (halcion)

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

Intermediate-acting BENZ

A

Clonazepam (Clonopin)

*Iorazepam (Ativan)

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

Long-Acting BENZ

A

Diazepam (valium) (20-100 hr.)

Chlordiazepoxide (libruim) (50-100 hr; chlorazepate)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

The idea behind short acting benzodiazepines is that they make better tolerance, so less addictive. Problem?

A

More dependence

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Long Acting Benzodiazepines biotransformation

A

Phase 1 –> Active metabolism,

Phase 2–> BDZ + UDP-O-carbon conjugation to inactive metabolite for excretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Short Acting Benzodiazepines biotransformation

A

Phase 2–> BDZ + UDP-O-carbon conjugation to inactive metabolite for excretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

*Benzodiazipine mechanisms of action

A

1) Increase affinity for GABA-A receptor for GABA
2) Couple GABA-A to Cl- channel

BUT: need GABA in system to work

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

*Benzodiazepines and Barbituates: Which is more potent?

A

Barbiturates are more potent

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Benzoiazepine increases the ____ of Cl- channel opening

A

FREQUENCY

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Barbituates increase the ___ of Cl- channel opening.

A

DURATION

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Picotoxin

A

Blocks Cl- Channel

Can cause seizures and act as stimulant

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Once neurosterioids bind, they are converted to

A

allopregnanolone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

GABA + BDZ

A

increase CL- Influx

enhances inhibition of NS

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

GABA + BDZ + BDZ blocker

A

normal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

GABA + BDZ + GABA blocker

A

barely any influx

31
Q

GABA

A

hyperpolarization

32
Q

GABA + Diazepam

A

increased magnitude of hyperpolarization

33
Q

BDZ agonists

A

Midazolam
Clonazeplam
Flunitrazepam
Diazepam

34
Q

BDZ competitive antagonist

A

Flumazenil

35
Q

Beta-Carboline inverse agonists

A

DMCM, Beta-CCM, beta-CCE

36
Q

Acute effects of BDZ and Barbituates

A

Mock ADHD: decrease arousal/altert, decrease anxiety, disinhibition, decrease concentration

DrunK: sedation, mild euphoria, intoxication, hypnosis, impaired memory, suppress REM, decreased activity impaired motor

37
Q

Barbituates vs. BDZ, which like alcohol in terms of intoxication

A

Barbituates

38
Q

TOXIC effects of barbiturates and BZD

A

Suppressed respiration
stupor
Coma

Barbiturates: death, unlikely for BDZ unless combined with other depressants

39
Q

Barbiturate OD

A

no safe antidote

Therapy, vital monitoring, respiratory assistance,

activated charcoal to prevent GI absorption, increasing renal pH NOT recommended

40
Q

What are APPROVED therapeutic uses of BARBITURATES?

A

Anesthesia - short term (thiopental)

Anti-Seizure (phenobarbital)

41
Q

What are APPROVED therapeutic uses of BARBITURATES?

A

Anesthesia (thiopental)

Anti-Seizure (phenobarbital)

42
Q

UNAPPROVED therapeutic uses of BARBITURATES?

A

Anti-anxiety (secobarbital)

hyponosis (amobarbital)

43
Q

Non-Benzodiazepines Hyponosis

A

Ambien (Zolpidem), Lunesta (Eszopiclone), and Sonata (Zalepion)

Selective for BZ1 subtype link to sleep, selective for hypnotic effect

Report induce sleep, no hangover, fewer side effect, less likely to induce dependence

44
Q

Non-Benzodiazepines Hyponosis

A

Ambien (Zolpidem), Lunesta (Eszopiclone), and Sonata (Zalepion)

Selective for BZ1 subtype link to sleep, selective for hypnotic effect

Report induce sleep, no hangover, fewer side effect, less likely to induce dependence

45
Q

Cellular tolerance of Barbiturates/BDZ

A

Decrease GABA receptors

46
Q

Metabolic tolerance of Barbiturates/BDZ

A

Increases metabolism

47
Q

Behavioral tolerance of Barbiturates/BDZ

A

Functioning in presence of drug

48
Q

Cross tolerance

A

across depressants

49
Q

Tolerance of barbituates reduces…

A

Therapeutic index, bring desired effect dangerously close to toxic effect

50
Q

BDZ dependence

A

mild, but discomforting
NOT life threatening
Anxiety, irritability, sweating, vertigo, insomnia, cramps, sensitivity, tachycardia

positive reinforcement: weak reinforcer

51
Q

Abuse model of BDZ

A

patients with history of drug abuse more likely to escalate dosage and abuse

52
Q

Therapeutic model

A

patients use recommended doses, many no escalate and under medicate

53
Q

Non barbiturate depressants

A

Gamm hydoxy… (GHB)
Flunitrazepam (Rohypnol)
Methaqualone (Quaalude)

All not marketed in US

54
Q

GHB

A

Not barbiturate

Powerful depressant
Structure similar to GABA

Liquid Ecstasy, Liquid X or E, Soap

Disinhibition, drunkenness, amnesia

Acute overdose (stupor, coma)

Predatory Drug

55
Q

Rohypnol- memory blocking

A

Powerful benzodiazepine

Not marketed in U.S.

Roofies, Roachies, Rope, Ruffies

Potent long-acting amnesic

Predatory drug

56
Q

Psychological Symptoms of Anxiety

A

Apprehension, worry, nervousness, agitation

57
Q

Physical Symptoms

A

increase bp, heart rate, erratic respiration rate, decreased salivary flow, GI disturbance, muscle tension

58
Q

Barbiturate risks

A

Acute toxicity
lethal od
varying rate of tolerance
physical/psychological dependence

59
Q

BDZ risks

A

OD when combined with other drugs (opiods)

prolong physical dependence

Psychological dependence if susceptible

60
Q

How do you treat BDZ dependence?

A

Tapering dosage over time, replace with longer acting DBZ, initiate psychotherapy

61
Q

Buspirone (Buspar)

A

Partial 5HT1A agonist
no tolerance/dependence

no rebound anxiety upon termination

Weak side effect: sedation, memory, motor

no interaction with other depressants

But: action requires several weeks, and less effective as treatment

62
Q

SSRIs

A

Most popular treatment of anxiety and depression

inhibit reuptake of 5-HT primarily

fewer risks compared to depressants

Fewer side effects than TCAs or MAOIs

63
Q

Vilazodone (Viibryd)

A

Partial agonist at 5HT1A receptors

selective serotonin reuptake inhibitor

64
Q

Amygdala hypothesis of anxiety

A

Sensory input via thalamus

Lateral N. of Amygdala

Center/Basolateral N. of amygdala

(Output is CRH)

Stria terminalis

Projection to CNS/ANS

65
Q

Cortical Releasing hormone (CRH)

A

41 amino acid peptide

Hormone regulating ACTH release from anterior pituitary, which induces cortisol release from adrenal cortex

Neurotransmitter released in anxiety circuits

66
Q

LC neurons: BDZ

A

enhances inhibitory function of GABA on LC

67
Q

LC neurons: SSRIS

A

reuptake block of 5-HT enhances 5-HT inhibition of LC

68
Q

LC Neurons: CRH

A

has anxiety producing excitatory effect on LC

69
Q

DREADD Experiment

A

Designer receptors exclusively activated by designer drugs

HM3/HM4 dye

1) inject virus in brain
2) CNO ligand in water, binds to receptor

hM4Di- inhibition
hM3Dq= excitation

LC neurons activated by stress

More time in open field maze

70
Q

Fear vs. anxiety

A

Anxiety- apprehension about possible future events

Fear- emotional response to clear and current danger

71
Q

BENZO agonist

A

increase GABAA affinity, helps GABA work, increase attraction, allows more Cl- into neurons, more inhibition

72
Q

BENZO antagonist

A

binds to the same sight of benzodiazepine, block benzodiazepine BUT The problem is, the only drug used is one antagonist and some get seizure from that.

73
Q

BENZO inverse agonists

A

increase anxiety

reduction in Cl- influx

Angiogenic: produce anxiety. Experiment only.

Bind to BENZO site

Psychopharmacology (16 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions