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Addictions: PSYC 3304 A > Lecture 4: Sedative-Hypnotic and Anxiolytic Medications > Flashcards

Lecture 4: Sedative-Hypnotic and Anxiolytic Medications Flashcards

1
Q

What are barbiturates, when were they introduced?

What are the mechanisms (effects) of the drug? Is it dose dependent?

A

Phenobarbital was introduced as sedative in 1912 (originally mechanism was unknown)
Classified by chemical structure

Mechanism: non-selective neuronal depression (reducing overall firing of neurons), depress polysynaptic diffuse brain-stem neuronal pathways (reduce activity between synapses) in the brain stem and cerebral cortex
Yes - dose dependent

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2
Q

From a metabolic standpoint what are the mechanisms of barbiturates? What can u do to measure sugar-use in brain?

A

Reduce electrical and metabolic activity (what you are doing, brain is running lower/using less energy)
Decreases in whole-brain glucose metabolism (cant break down or use sugars)
Reduction of excitatory activity or increased inhibitory

Give someone shot of radioactive traced glucose to see where it is being consumed in brain during tasks

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3
Q

What is the involvement of GABAa receptors in barbiturate interaction?
What can be a problematic result of interaction?

Hint: Cl-

A

Enhancement of GABA transmission - applying more breaks, depressing brain activity
Increased Cl- influx accounts for sedative-hypnotic actions, anesthetic properties

Can open Cl- channel in the absence of GABA - not good, GABA is key receptor is lock but barbituates push open the door without GABA
increases toxicity of B (inhibition without control)
High doses can produce amnesia and state of dementia
Therapeutic index is super skinny

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4
Q

What are the components present is demented states?

A 
Sensorium - time and place
Affect - expression of feelings
Mental content - fund of knowledge
Intellectual function - ability to reason
Insight and judgement
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5
Q

What are the pharmacokinetics of barbiturates?

What are the differences between short-acting and long-acting barbiturates?

A

wide range of half-lives (3m - 120hr), after 6 half lives drug is removed
Rapidly and completely absorbed

Short-acting versions are very lipid soluble (BBB, induce sleep)
Long-lasting versions are more water soluble (blood/urine residues) - do not diffuse easily and last longer

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6
Q

What are the pharmacological effects of barbiturates?

Hint: unlike mechanism, think laymen effects or visible

A 
Low degree of selectivity - acts like a big mallet, hits a ton of other receptors 
Suppression of REM sleep
Cognitive inhibition (little dumb)
Combination of barbiturates-alcohol can affect respiration, overdose
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7
Q

What are the psychological effects of barbiturates? What happens when combined with alc?

A

Similar to alc-induced inebriation
Low doses remove anxiety
High doses cause general behavioral depression and sleep

Affects respiration and can cause overdose

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8
Q

What are the principle properties of barbiturates?

A

Lethal in overdose
Narrow therapeutic range (v little doses allot)
Potential for tolerance, dependence and abuse
possible dangerous interactions
Teratogenic potential (unconfirmed)
“truth serum” - increases suggestibility

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9
Q

How can you distinguish a nonbarbiturate and what are some examples?

A

Different chemical structure but same effects
Soma, Quaalude (v popular in the 70-80), Paraldehyde
- used as date rape drug but is acc a anaphrodisiac
- banned in 1984 in the US

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10
Q

What are general anesthetics, how are they used? how are they administered? provide some examples

A 
Potent CNS depressants, unconsciousness 
Low analgesic or euphoriant activity 
Used in medical settings
Administered via inhalation or intravenous injection
Nitrous oxide, isoflurane, halothane
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11
Q

Provide 4 examples of injectable anesthetics?

A

Pentothal, brevital, diprivan, amidate

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12
Q

What is Gamma Hydroxybutyrate (GHB)? what is a similarity? What are some characteristics/uses of the drug?
Is it found in the body?

A

W: Potent CNS depressant (inhibitory)
Structurally similar to GABA, derived from GABA
GHB increases DA levels in the brain, activates DA reward system
C: Easily crosses the BBB, high abuse potential, foreign availability
Synergistic effects with EtOh - two together are worse than both apart
U: Used as anesthetic, to treat sleep disorders, EtOH detox, also date rape drug
Used to treat narcolepsy (inappropriate levels of da in brain)

Normally found endogenously - body does produce it but not in dosage concentrations

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13
Q

How is GHB classified by the FDA?

A

both a schedule I and III drug - it is allowed for therapeutic uses but can be illegal if found outside of that context

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14
Q

What is the purpose of antiepileptic drugs? what is an important consideration pertinent to this drug?

A

Help deal with epileptic seizures
Treatment of bipolar disorders
Neuromodulators: wide array of applications
Chemically belongs to either - barbiturates (phenobarbital), hydantoins (phenytoin)

This drug has teratogenic effects, its important to weigh this against the pro of seizure control - a way to control for this is daily low doses

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15
Q

What is/what are the characteristics of a benzodiazepene? what is the mechanism of action?

A

next generation barbiturate, anxiolytic, sedative, anticonvulsant
Most widely used psychotherapeutic drug (valium, librium, xanax)

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16
Q

What are the mechanisms of action of a benzodiazepine? Where is the site of action? where are the side effects?

A

Potent GABA agonist - facilitate GABA binding
Causes influx of Cl- hyperpolarization

Site of action: limbic system
Side effects: ceberal cortex and brain stem

17
Q

Where do the anxiety, panic, and behavioral responses to fear occur?

A

amygdala, orbitofrontal cortex and insula

experimented on via stimulation and lesions

18
Q

In terms of benzos mechanism of A, where does a blockade occur? How does this potentially effect fear levels?

A

Blockade of GABAergic function in amygdala (blocks GABAs effect on amygdala) - increases amygdala functioning = anxiogenic responses to stimuli (overly scared)

BZ may increase threshold for responsiveness in amygdala - priming fear

19
Q

How many kinds of bz are available and what are the primary differences between them?

A

Over 20
Rates of metabolism, active metabolites, plasma half-lives
Peak BAC occurs in 1hr

20
Q

What is an active metabolite?

A

results when a drug is metabolized by the body into a modified form which continues to produce effects in the body. Usually these effects are similar to those of the parent drug but weaker, although they can still be significant

21
Q

What benzos produce active metabolites? what is a metabolite of V?

A

Valium, librium, centrax

Nordiazepam - half life of 60hrs

22
Q

What is significant about the use of benzos by the elderly?

A

Elderly have trouble metabolizing long-acting BZ and their metabolites (blood plasma concentration of the drug can persist)
Lower dosage required (50%) at shorter-acting BZ
Long term use can result in severe cognitive dysfunction

23
Q

What are the pharmacological effects of benzos?

A

Mental confusion and amnesia - cerebral cortex and hippocampus
Muscle relaxant effect - spinal cord, cerebellum and brainstem
Antiepileptic actions - cerebellum and hippocampus
Behavioral rewarding effects - ventral tegmentum & nucleus accumbens

24
Q

What are the clinical uses and issues associated with the use of benzos as treatment?

A

acts as cognitive inhibitor - may interfere with cognitive therapies
effective at producing anterograde amnesia - can be helpful for surgery sedation (lorazepam)
Typically used for short-term alleviation of anxiety or insomnia

25
Q

What is rohypnol? uses/characteristics

A

used in 70s for deep sedation
up to 80% is absorbed by oral application
detectability lost after 72hrs

26
Q

What are the overall advantages and disadvantages to benzos?

A

Good: rapid onset, anxiolysis, low-level side effects, good patient acceptance

Bad: impaired psychomotor performance, impaired learning and cognition, reduced alertness, paradoxical agitation, potential for dependence and abuse

27
Q

What are the fetal effects of benzos?

A

infant dependence, floppy infant syndrome (low muscle tone)

28
Q

What is the relevance of flumazenil to bzs?

A

Binds with high affinity to BZ site on GABAa receptor
Once bound it exhibits no intrinsic activity - once bound it stops doing things
Blocks BZ ability to interact with BZ site
Short half-life (1hr) - good for overdose situations

29
Q

What are the characteristics of a 2nd generation anxiolytics? what are some examples?

A

Nonbenzobenzos (not classical structure)

Zolpidem (ambien) - partial agonist (not a tight fit) binds to GABA1a receptor
Used for insomnia, acts as sedative, not an anxiolytic (not for anxiety)
Fine tuned and rapidly absorbed by GI

Zaleplon (sonata)
Hypnotic agent 
Bind to GABA1a receptor 
very short half-life (1hr)
only 30% reaches blood plasma, sleep onset
30
Q

What is a serotonergic anxiolytic? where is the second focus located?

A

Attention on presynaptic 5-HT transporter and postsynaptic 5-HT1a receptor

5-HT1a receptor: hippocampus, septum, amygdala, dorsal raphe nucleus

31
Q

What is busporin? what does the activation of 5-HT1a do?

A

Anxiolytic with little hypnotic action
Low levels of amnesia
No additive effects with EtOH
Low dependence

Activation of 5-HT1a keeps anxiolytic balance

Addictions: PSYC 3304 A (6 decks)

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