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Pharm Exam 3 > 32: Anxiolytics and Sedative Hypnotics > Flashcards

32: Anxiolytics and Sedative Hypnotics Flashcards

1
Q

sensory and motor function, cognition, short-term memory, speech, etc..

A

cerebral cortex

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2
Q

area of brain that encloses the 3rd ventricle

A

diencephalon

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3
Q

integration of sensory relays

A

thalamus

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4
Q

temperature, appetite, emotional and hormonal regulation

A

hypothalalmus

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5
Q

bridge between cerebrum/diencephalon and the brainstem

A

mesencephalon

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6
Q

the thalamus and hypothalamus are part of the…

A

diencephalon

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7
Q

the pons, medulla oblongata, and reticular formation are part of the…

A

brainstem

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8
Q

involved in control of respiration and cardiovascular function (vasomotor center)

A

pons and medulla oblongata

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9
Q

control of consciousness, arousal and alertness

A

reticular formation

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10
Q

planning and coordination of motor movements and motor patterns including maintenance of balance and posture

A

cerebellum

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11
Q

striatum =

A

caudate nucleus and putamen

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12
Q

basal ganglia =

A

striatum
globus pallidus
lentiform nucleus
substantia nigra

primarily involved in control of motor activites

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13
Q

amygdala, hippocampus, cingulate gyrus, prefrontal cortex, hypothalamuc, thalamic nuclei, mamillary bodies,, etc…

A

limbic system

primarily involved in control of emotional and behavioral activity

ex: stress responses, fear, mood control, etc

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14
Q

formation of tight junctions between endothelial cells on CNS capillaries

A

blood-brain barrier

selective filter - prevents many substances from entering the brain and the spinal cord, especially polar and lipophobic compounds

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15
Q

excitatory or inhibitory: Acetylcholine

A

excitatory

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16
Q

excitatory or inhibitory: DA, NE, 5HT

A

mostly inhibitory, but the overall effect is often general excitation of the brain (disinhibition)

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17
Q

excitatory or inhibitory:GABA

A

inhibitory

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18
Q

excitatory or inhibitory: glycine

A

inhibitory

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19
Q

excitatory or inhibitory: glutamate

A

excitatory

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20
Q

excitatory or inhibitory: aspartate

A

excitatory

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21
Q

excitatory or inhibitory: substance P

A

excitatory nt involved in spinal pain processing

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22
Q

excitatory or inhibitory: endogenous opiods (endorphins, enkephalins and dynorphins)

A

excitatory - inhibit pain sensation

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23
Q

decreased neuronal excitability

A

CNS depression

24
Q

agents that are mainly used to treat anxiety states and sleep disorders

A

CNS depressants

25
selective depressants/ sedative hypnotics include...
benzodiazepines barbiturates ethanol
26
non-selective/ general depressants include..
antihistamines | opiod analgesics
27
exert a calming effect or sedation with concomitant relief or anxiety at relatively low doses
sedative anxiolytics depressant effects on psychomotor and cognitive functions
28
agents that produce drowsiness adn encourage the onset and maintenance of a state of sleep
hypnotics general hypnotic effects 1) more rapid onset of sleep 2) increased duration of stage 2 NREM sleep 3) decreased duration of REM and stage 4 NREM sleep
29
overwhelming and continuous worrying about life events
anxiety symptoms include anxiousness, nervousness, apprehension, fear, panic, mental disintegration
30
linear slope drugs (barbiturates and alcohols) at doses higher than needed for hypnosis may lead to a state of ...
general anesthesia at even higher doses: depression of respiratory and vasomotr centers in the medulla resulting in coma and death
31
non-linear slope drugs (benzodiazepines) are generally safer to use than linear because...
reach plateau in CNS depression greater dose increments are needed to achieve hypnosis
32
what is required for benzodiazepine sedative-hypnotic activity?
electronegative substituent in the 7 position is required for sedative-hypnotic activity
33
where are benzodiazepines meatabolized?
liver via P450s, mainly CYP3A4 + glucoronidation
34
which benzos are inactive water-soluble glucornides with metabolism? weakly active? active?
inactive = lorazepam and oxazepam weakly active = alprazolam and triazolam long-lived = all the rest
35
what 4 pharmacodynamic changes occur with aging?
1. >65 hepatic processing slows 2. decreased lean body mass 3. increased Vd for many lipid soluble drugs 4. decreased rate of elimination
36
which benzos are affected by age? which are not?
oxazepam and lorazepam are not influenced by age diazepam is age dependent
37
MOA benzodiazepines
increase the frequency of opening and conductance of the GABA Cl- channels ---> inhibition binds to BZ sites to facilitate channel opening
38
side effects and toxicity of benzodiazepines:
- drowsiness and sedation - ataxia - respiratory depression - anterograde amnesia - tolerance and dependence
39
date rape drug
flunitrazepam -- anterograde amnesia
40
contraindications for benzodiazepines
- pregnancy - elderly - substance abuse - sleep disorders - required alertness (surgery, driving, etc)
41
major drug interaction for benzodiazepines
additive CNS depression with ethanol, opiods, etc...
42
therapeutic uses for benzodiazepines
anxiolytic (relief of anxiety) and sedative hypnotic ( relief of insomnia)
43
MOA flumazenil
competitive inhibitor that binds to the BZ receptor ----> REVERSE the effects of benzodiazepines
44
uses for flumazenil
- terminate benzodiazepine-induced sedation | - diagnosis and treatment of benzodiazepine toxicity
45
MOA of the Z drugs
selectively bind to BZ receptros on GABA and act as an agonist only to alpha1 subunits
46
clinical uses for barbiturates
- anesthesia - sedative/hypnotic - anticonvulsant - medically induced coma 3+4 = phenobarbital
47
which of the discussed drugs are NO active metabolites?
barbitruates unlike benzodiazepines slow meatbolism of the barbiturates by the lier
48
MOA of barbiturates
increase the duration of the GABA-gated chloride channel opening
49
MOA barbiturates v. benzos
barbiturates: increase duration benzos: increase frequency
50
MOA ramelteon
melatonin receptor agonist MT1 - sleep onset MT2- circadian pattern
51
does using ramelteon have a dependence risk for sleeping?
no regular use does not result in dependence - not a controlled substance
52
non-sedating anxiolytic
buspirone causes less psychomotor impairment than benzodiazepines and does not affect driving skills but delayed response is not suitable for acute anxiety or panic
53
MOA buspirone
partial agonist at 5HT 1a receptors | autoreceptors - activation of 5HT1a receptor reduces neuronal excitability, firing frequency and 5HT release
54
adverse effects buspirone
``` nonspecific chest pain tachycardia palpitations dizziness nervousness tinnitus GI distress ```
55
not an anxiolytic, but diminishes some of the somatic manifestations of anxiety (stage fright, performance anxiety)
propanolol
56
oldest and most commonly used anxiolytic
alcohol via a sedative action

Pharm Exam 3 (11 decks)

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