Lecture 10: Sedatives & Hypnotics Flashcards

(74 cards)

1
Q

sedative definition

A

a drug that reduces anxiety & produces a calming effect
- causes CNS depression

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2
Q

anxiolytic definition

A

drugs used to treat anxiety

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3
Q

hypnotic definition

A

a drug that should produce drowsiness & encourage onset & maintenance of sleep
- produces more pronounced CNS depression than just sedation

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4
Q

generalized anxiety disorder

A

an ongoing state of excessive anxiety lacking any clear reason

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5
Q

panic disorder

A

attacks of overwhelming fear occurring in association w/ somatic symptoms (sweating, tachycardia, etc)

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6
Q

phobias

A

fears of specific things or situations

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7
Q

PTSD

A

anxiety triggered by recall of stressful experiences

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8
Q

what manner do anxiety reactions occur in an anxiety disorder?

A

in an anticipatory manner, independent of external events

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9
Q

what is the distinction b/w pathological & a normal state of anxiety

A

not clear, but likely the point at which the symptoms interfere w/ normal productive activities

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10
Q

which areas of the brain undergo changes in activity for anxiety?

A
  • heightened activity in the amygdala (associated w/ fear)
  • reduced activity in prefrontal cortex (executive function & emotional regulation0
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11
Q

anxiety scale tests

A

generalized anxiety disorder questionnaire, hamilton anxiety rating scale, beck anxiety inventory

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12
Q

somatic & autonomic measures of anxiety

A

galvanic skin response

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13
Q

psychological treatments for anxiety disorders

A
  • cognitive behavioral therapy
  • exposure therapy
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14
Q

cognitive behavioral therapy

A
  • identifies & challenges negative though patterns & replaces w/ more balanced ones
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15
Q

exposure therapy

A

gradual & repeated exposure to feared situations or objects
- acceptance & commitment therapy, mindfulness, humanistic therpies

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16
Q

gut-brain axis treatment of anxiety

A

reduced Lactobacillus or Bifidobacterium levels have been linked to higher anxiety scores

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17
Q

benzodiazepine examples

A

diazepam, lorazepam, midazolam, alprazolam

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18
Q

barbiturate examples

A

thiopental, pentobarbital, phenobarbital

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19
Q

orexin antagonist function

A

improves sleep duration

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20
Q

melatonin receptor agonist function

A

aids in sleep onset
- no direct effect on GABAergic neurotransmission
- don’t affect sleep architecture or have rebound insomnia or withdrawal

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21
Q

buspirone function

A

slow onset anxiolytic w/ no action on GABAergic neurotransmission
- minimal abuse liability
- used for general anxiety disorders but not panic attacks

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22
Q

buspirone mechanism of action

A

5HT1A agonist & D2 receptor agonist

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23
Q

antihistamine drugs function

A

produce sedation (via peripheral that affects autonomic nervous system)

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24
Q

beta-adrenergic agonist used to treat anxiety

A

propranolol

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25
when is propranolol used to treat anxiety
when physical symptoms (sweating) are troublesome - no effect on the affectiv ecomponent
26
how do benzos work to treat anxiety
- reduce excessive activity by enhancing the effect of GABA - alprazolam, lorazepam
27
which benzos treat insomnia
temazepam
28
which benzos control seizures
clonazepam or diazepam
29
which drugs are useful for treating alcohol withdrawal
benzos
30
which benzo is used to treat muscle spasms
diazepam
31
how does diazepam treat muscle spasms
by a central action independent of their sedative effect; increased muscle tone is a common feature of anxiety states & may contribute to aches & pains
32
what drug can be used to manage acute panic attacks
fast-acting benzos
33
first line of treatment for insomnia
avoiding stimulannts
34
how do benzos affect sleep
- change sleep architecture - reduces REM & slow-wave (deep) sleep - abrupt cessation of benzos can cause rebound insomnia
35
what is REM important for
emotional regulation, learning, & memory consolidation
36
what is deep sleep necessary for
clearing metabolic waste
37
general function of barbiturates
reversibly depress the activity of all excitable tissues
38
what occurs from acute barbiturate intoxication
severe deficits in cardiovascular & other peripheral functions
39
what kind of CNS depression do barbiturates cause
all degrees, ranging from mild sedation to general anaesthesia - may have euphoric effects
40
what barbiturate is used as an anasethetic
thiopental
41
what barbiturate is used as an anticonvulsant
phenobarbital
42
why do people misuse barbiturates
- euphoric high - enhance the effects of other drugs - self-medicate for anxiety, stress, or insomnia - escape psychological pain or trauma
43
difference between central nervous system effects b/w benzos & barbiturates
barbiturates can cause medullary depression & coma, benzos only cause anaesthesia by themselves
44
what is medulla crucial for
heart rate regulation & BP control, rhythm & depth of breathing, reflexes for coughing, swallowing, vomiting, cranial nerve nuclei
45
GABA-A receptor function
mediates fast inhibitory synaptic transmission in the CNS
46
how do GABA-A receptor mediate synaptic inhibition
increasing Cl- conductance, which hyperpolarizes the cell
47
how do benzos enhance response to GABA
increasing the frequency of the opening of GABA-activated Cl- channels - do not open the channel by themselves
48
benzos binding site
specific site (distinct from GABA on GABA-A receptor/ion channel complex - positive allosteric modulators, increasing the affinity of GABA for its receptor
49
do benzos change the conductance or mean opening time
no
50
do benzos affect receptors for other amino acids
no
51
when does bicarbonate efflux through GABA-A receptors become significant
in some neurons during developmental stages or in certain pathological conditions
52
when is GABA-A receptor activation depolarizing rather than inhibitory
early in development
53
why are GABA-A receptors depolarizing early in development
due to a high intracellular Cl- concentration in immature neurons - when GABA binds to GABA-A receptors, Cl- ions exit the cell instead of entering
54
what is the function of the excitatory actions of GABA
supporting neurogenesis, synapse formation, neuronal migration, & dendritic & axonal growth
55
what is disruption of the excitatory - to inhibitory switch of GABA-A receptors linked to
- epilepsy - autism spectrum disorders - schizophrenia
56
barbiturates binding activity
bind to the GABA-A receptor & increase the duration of GABA-gated channel openings - different site than benzos
57
how does barbiturate binding activity change at high concentrations
becomes GABA-mimetic, directly activating Cl- channels
58
short term effects of barbiturates
euphoria, fatigue, shallow breathing, trouble coordinating movements, paranoia, aggression, easily agitated, difficulty remembering, irritability
59
long term effects of barbiturates
- rebound effects - tolerance - withdrawal
60
rebound effects of barbiturates
- reversal effect - seizures can occur, calm & relaxed feelings dissipate
61
tolerance of barbiturates
- must have more & more of the drug to feel a minor effect - higher risk of overdose
62
what happens in overdose of benzos alone
prolong sleep, w/o serious depression of respiratory or cardiovascular function
63
what happens in overdose of benzos plus other CNS depressants
can be life-threatening
64
benzo antagonist
flumazenil - reverses effects of acute overdose
65
side effects of benzos
drowsiness, confusion, amnesia, impaired coordination
66
what causes the tolerance of benzos
down-regulation of benzodiazepine receptor binding sites
67
how can benzo withdrawal symptoms be minimized
gradually reducing the dose - rapid withdrawal & drug cessation is life threatening due to seizures
68
withdrawal symptoms of benzos
- tachycardia - severe headaches - restlessness, dizziness, reduced concentration - panic attacks, irritability - tremors, insomnia, psychoses - changes in perception - weight loss parasthesias
69
what kind of metabolism do benzos undergo
hepatic - rely on CYP3A4 enzyme (phase 1 reaction), followed by glucoronidation that allows excretion in the urine (phase 2 reaction)
70
clonazepam use
seizure disorders - tolerance develops to anticonvulsant doses
71
diazepam use
anxiety disorders, life threatening seizures - prototypical benzo
72
flurazepam use
insomnia, anxiolytic - active metabolites accumulate w/ chronic use
73
lorazepam use
anxiety disorder, hypnotic - metabolized solely by conjugation
74
how is barbiturate overdose managed
supportive care