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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
Q

selective depressants/ sedative hypnotics include…

A

benzodiazepines
barbiturates
ethanol

26
Q

non-selective/ general depressants include..

A

antihistamines

opiod analgesics

27
Q

exert a calming effect or sedation with concomitant relief or anxiety at relatively low doses

A

sedative anxiolytics

depressant effects on psychomotor and cognitive functions

28
Q

agents that produce drowsiness adn encourage the onset and maintenance of a state of sleep

A

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
Q

overwhelming and continuous worrying about life events

A

anxiety

symptoms include anxiousness, nervousness, apprehension, fear, panic, mental disintegration

30
Q

linear slope drugs (barbiturates and alcohols) at doses higher than needed for hypnosis may lead to a state of …

A

general anesthesia

at even higher doses: depression of respiratory and vasomotr centers in the medulla resulting in coma and death

31
Q

non-linear slope drugs (benzodiazepines) are generally safer to use than linear because…

A

reach plateau in CNS depression

greater dose increments are needed to achieve hypnosis

32
Q

what is required for benzodiazepine sedative-hypnotic activity?

A

electronegative substituent in the 7 position is required for sedative-hypnotic activity

33
Q

where are benzodiazepines meatabolized?

A

liver via P450s, mainly CYP3A4 + glucoronidation

34
Q

which benzos are inactive water-soluble glucornides with metabolism? weakly active? active?

A

inactive = lorazepam and oxazepam

weakly active = alprazolam and triazolam

long-lived = all the rest

35
Q

what 4 pharmacodynamic changes occur with aging?

A
  1. > 65 hepatic processing slows
  2. decreased lean body mass
  3. increased Vd for many lipid soluble drugs
  4. decreased rate of elimination
36
Q

which benzos are affected by age? which are not?

A

oxazepam and lorazepam are not influenced by age

diazepam is age dependent

37
Q

MOA benzodiazepines

A

increase the frequency of opening and conductance of the GABA Cl- channels —> inhibition

binds to BZ sites to facilitate channel opening

38
Q

side effects and toxicity of benzodiazepines:

A
  • drowsiness and sedation
  • ataxia
  • respiratory depression
  • anterograde amnesia
  • tolerance and dependence
39
Q

date rape drug

A

flunitrazepam – anterograde amnesia

40
Q

contraindications for benzodiazepines

A
  • pregnancy
  • elderly
  • substance abuse
  • sleep disorders
  • required alertness (surgery, driving, etc)
41
Q

major drug interaction for benzodiazepines

A

additive CNS depression

with ethanol, opiods, etc…

42
Q

therapeutic uses for benzodiazepines

A

anxiolytic (relief of anxiety) and sedative hypnotic ( relief of insomnia)

43
Q

MOA flumazenil

A

competitive inhibitor that binds to the BZ receptor —-> REVERSE the effects of benzodiazepines

44
Q

uses for flumazenil

A
  • terminate benzodiazepine-induced sedation

- diagnosis and treatment of benzodiazepine toxicity

45
Q

MOA of the Z drugs

A

selectively bind to BZ receptros on GABA and act as an agonist only to alpha1 subunits

46
Q

clinical uses for barbiturates

A
  • anesthesia
  • sedative/hypnotic
  • anticonvulsant
  • medically induced coma

3+4 = phenobarbital

47
Q

which of the discussed drugs are NO active metabolites?

A

barbitruates

unlike benzodiazepines

slow meatbolism of the barbiturates by the lier

48
Q

MOA of barbiturates

A

increase the duration of the GABA-gated chloride channel opening

49
Q

MOA barbiturates v. benzos

A

barbiturates: increase duration
benzos: increase frequency

50
Q

MOA ramelteon

A

melatonin receptor agonist

MT1 - sleep onset

MT2- circadian pattern

51
Q

does using ramelteon have a dependence risk for sleeping?

A

no

regular use does not result in dependence - not a controlled substance

52
Q

non-sedating anxiolytic

A

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
Q

MOA buspirone

A

partial agonist at 5HT 1a receptors

autoreceptors - activation of 5HT1a receptor reduces neuronal excitability, firing frequency and 5HT release

54
Q

adverse effects buspirone

A 
nonspecific chest pain
tachycardia
palpitations
dizziness
nervousness
tinnitus
GI distress
55
Q

not an anxiolytic, but diminishes some of the somatic manifestations of anxiety (stage fright, performance anxiety)

A

propanolol

56
Q

oldest and most commonly used anxiolytic

A

alcohol via a sedative action

Pharm Exam 3 (11 decks)

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