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Psychopharmacology > Final: Anxiolytics > Flashcards

Final: Anxiolytics Flashcards

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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.

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2
Q

What 3 factors affect the onset/duration of barbiturates?

A
  1. lipid solubility
  2. Plasma protein binding
  3. rate of excretion
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3
Q

How do you synthesize barbiturate

A

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

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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

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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

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6
Q

Long-acting barbiturates

A

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

*Use: seizures, sedation

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7
Q

Are barbiturates GABA agonists/antagonists?

A

NO!

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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.

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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

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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

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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

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12
Q

What is a GABA agonist?

A

Muscimol

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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

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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

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15
Q

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

A

1) BIOTRANSFORMATION
2) ppb
3) rate of excretion

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16
Q

Short Acting Benzodiazepines

A

1) *Alprazolam (Xanax)

2) Triazolam (halcion)

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17
Q

Intermediate-acting BENZ

A

Clonazepam (Clonopin)

*Iorazepam (Ativan)

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18
Q

Long-Acting BENZ

A

Diazepam (valium) (20-100 hr.)

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

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19
Q

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

A

More dependence

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20
Q

Long Acting Benzodiazepines biotransformation

A

Phase 1 –> Active metabolism,

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

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21
Q

Short Acting Benzodiazepines biotransformation

A

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

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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

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23
Q

*Benzodiazepines and Barbituates: Which is more potent?

A

Barbiturates are more potent

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24
Q

Benzoiazepine increases the ____ of Cl- channel opening

A

FREQUENCY

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25
Barbituates increase the ___ of Cl- channel opening.
DURATION
26
Picotoxin
Blocks Cl- Channel | Can cause seizures and act as stimulant
27
Once neurosterioids bind, they are converted to
allopregnanolone
28
GABA + BDZ
increase CL- Influx enhances inhibition of NS
29
GABA + BDZ + BDZ blocker
normal
30
GABA + BDZ + GABA blocker
barely any influx
31
GABA
hyperpolarization
32
GABA + Diazepam
increased magnitude of hyperpolarization
33
BDZ agonists
Midazolam Clonazeplam Flunitrazepam Diazepam
34
BDZ competitive antagonist
Flumazenil
35
Beta-Carboline inverse agonists
DMCM, Beta-CCM, beta-CCE
36
Acute effects of BDZ and Barbituates
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
Barbituates vs. BDZ, which like alcohol in terms of intoxication
Barbituates
38
TOXIC effects of barbiturates and BZD
Suppressed respiration stupor Coma Barbiturates: death, unlikely for BDZ unless combined with other depressants
39
Barbiturate OD
no safe antidote Therapy, vital monitoring, respiratory assistance, activated charcoal to prevent GI absorption, increasing renal pH NOT recommended
40
What are APPROVED therapeutic uses of BARBITURATES?
Anesthesia - short term (thiopental) | Anti-Seizure (phenobarbital)
41
What are APPROVED therapeutic uses of BARBITURATES?
Anesthesia (thiopental) | Anti-Seizure (phenobarbital)
42
UNAPPROVED therapeutic uses of BARBITURATES?
Anti-anxiety (secobarbital) hyponosis (amobarbital)
43
Non-Benzodiazepines Hyponosis
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
Non-Benzodiazepines Hyponosis
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
Cellular tolerance of Barbiturates/BDZ
Decrease GABA receptors
46
Metabolic tolerance of Barbiturates/BDZ
Increases metabolism
47
Behavioral tolerance of Barbiturates/BDZ
Functioning in presence of drug
48
Cross tolerance
across depressants
49
Tolerance of barbituates reduces...
Therapeutic index, bring desired effect dangerously close to toxic effect
50
BDZ dependence
mild, but discomforting NOT life threatening Anxiety, irritability, sweating, vertigo, insomnia, cramps, sensitivity, tachycardia positive reinforcement: weak reinforcer
51
Abuse model of BDZ
patients with history of drug abuse more likely to escalate dosage and abuse
52
Therapeutic model
patients use recommended doses, many no escalate and under medicate
53
Non barbiturate depressants
Gamm hydoxy… (GHB) Flunitrazepam (Rohypnol) Methaqualone (Quaalude) All not marketed in US
54
GHB
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
Rohypnol- memory blocking
Powerful benzodiazepine Not marketed in U.S. Roofies, Roachies, Rope, Ruffies Potent long-acting amnesic Predatory drug
56
Psychological Symptoms of Anxiety
Apprehension, worry, nervousness, agitation
57
Physical Symptoms
increase bp, heart rate, erratic respiration rate, decreased salivary flow, GI disturbance, muscle tension
58
Barbiturate risks
Acute toxicity lethal od varying rate of tolerance physical/psychological dependence
59
BDZ risks
OD when combined with other drugs (opiods) prolong physical dependence Psychological dependence if susceptible
60
How do you treat BDZ dependence?
Tapering dosage over time, replace with longer acting DBZ, initiate psychotherapy
61
Buspirone (Buspar)
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
SSRIs
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
Vilazodone (Viibryd)
Partial agonist at 5HT1A receptors selective serotonin reuptake inhibitor
64
Amygdala hypothesis of anxiety
Sensory input via thalamus Lateral N. of Amygdala Center/Basolateral N. of amygdala (Output is CRH) Stria terminalis Projection to CNS/ANS
65
Cortical Releasing hormone (CRH)
41 amino acid peptide Hormone regulating ACTH release from anterior pituitary, which induces cortisol release from adrenal cortex Neurotransmitter released in anxiety circuits
66
LC neurons: BDZ
enhances inhibitory function of GABA on LC
67
LC neurons: SSRIS
reuptake block of 5-HT enhances 5-HT inhibition of LC
68
LC Neurons: CRH
has anxiety producing excitatory effect on LC
69
DREADD Experiment
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
Fear vs. anxiety
Anxiety- apprehension about possible future events Fear- emotional response to clear and current danger
71
BENZO agonist
increase GABAA affinity, helps GABA work, increase attraction, allows more Cl- into neurons, more inhibition
72
BENZO antagonist
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
BENZO inverse agonists
increase anxiety reduction in Cl- influx Angiogenic: produce anxiety. Experiment only. Bind to BENZO site

Psychopharmacology (16 decks)

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