32: Anxiolytics and Sedative Hypnotics Flashcards Preview

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

Flashcards in 32: Anxiolytics and Sedative Hypnotics Deck (56):
1

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

cerebral cortex

2

area of brain that encloses the 3rd ventricle

diencephalon

3

integration of sensory relays

thalamus

4

temperature, appetite, emotional and hormonal regulation

hypothalalmus

5

bridge between cerebrum/diencephalon and the brainstem

mesencephalon

6

the thalamus and hypothalamus are part of the...

diencephalon

7

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

brainstem

8

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

pons and medulla oblongata

9

control of consciousness, arousal and alertness

reticular formation

10

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

cerebellum

11

striatum =

caudate nucleus and putamen

12

basal ganglia =

striatum
globus pallidus
lentiform nucleus
substantia nigra

primarily involved in control of motor activites

13

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

limbic system

primarily involved in control of emotional and behavioral activity

ex: stress responses, fear, mood control, etc

14

formation of tight junctions between endothelial cells on CNS capillaries

blood-brain barrier

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

15

excitatory or inhibitory: Acetylcholine

excitatory

16

excitatory or inhibitory: DA, NE, 5HT

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

17

excitatory or inhibitory:GABA

inhibitory

18

excitatory or inhibitory: glycine

inhibitory

19

excitatory or inhibitory: glutamate

excitatory

20

excitatory or inhibitory: aspartate

excitatory

21

excitatory or inhibitory: substance P

excitatory nt involved in spinal pain processing

22

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

excitatory - inhibit pain sensation

23

decreased neuronal excitability

CNS depression

24

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

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