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Pharmacology 2 > 2.2 Sedatives, hypnotics, anxiolytics > Flashcards

2.2 Sedatives, hypnotics, anxiolytics Flashcards

(69 cards)

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1
Q

Sedatives fn

A

decrease activity,
moderate excitement and
calm the recipient

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2
Q

Hypnotics fn

A

produce drowsiness and facilitate the onset and maintenance of a state of sleep that resembles natural sleep and from which the recipient can be aroused easily

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3
Q

anxiety is cahracterized by

A

heightened arousal (i.e. physical symptoms such as tachycardia)

accompanied by apprehension, fear, and obsession

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4
Q

anxiety disorders include

A

phobia/panic disorder,
generalized anxiety disorder,
obsessive compulsive disorder,
post traumatic stress disorder

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5
Q

older anxiolytics and hypnotics like barbiturates fn

A

depress the CNS in a dose dependent manner, progressively producing sedation, unconsciousness, surgical anesthesia, coma, fatal respiratory cardiac depression

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6
Q

a normal sleep consists of

A

alternating NREM and REM sleep

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7
Q

NREMstages

A

4

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8
Q

Sleep cycle

A

90 min – 4NREM,1REM

– repeats several times during the night

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9
Q

NREM stage 0

A

awake –from lying down to falling asleep.

Constitutes 1-2% of sleep time

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10
Q

NREM stage 1

A

dozing–the first stage of NREM seep is drifting off,

it lasts 10 minutes and takes up about 2-5% of normal night sleep

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11
Q

NREM stage 2

A

the sleeper can be wakened easily,

stage 2 sleep occupies approximately 50% of sleep time

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12
Q

NREM stage 3

A

much more difficult to awaken,

larger slower delta brain waves are generated

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13
Q

NREM stage 4

A

during this stage of sleep the body gets its most rest,
very difficult to be awakeng and
sometimes sleep walking (somnabulism) occurs

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14
Q

slow wave sleep (SWS)

A

stages 3 and 4

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15
Q

during stages 2, 3, and 4

A

heart rate, BP, and respiration are steady and

muscles are relaxed

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16
Q

REM sleep

A

brain is extremely active,
brain waves are small and fast with bursts of activity,
REM sleep is characterized by “rapid eye movemt”, and is
the phase when dreams occur most often and intensely
(but dreams can occur at other stages too)

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17
Q

% of sleep in stage 1

A

5%

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18
Q

% of sleep in stage 2

A

40-50% — longest

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19
Q

% of sleep in stage 3

A

12%

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20
Q

% of sleep in stage 4

A

12%

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21
Q

% of sleep in REM

A

25%

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22
Q

A hypnotic, at a lower dose

A

becomes a sedative

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23
Q

classification of these drugs

A

benzodiazepines,
barbiturates,
benzo receptor agonists,
5HT1A receptor agonist

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24
Q

benzodizepines structure

A

benzene ring, diazepine ring

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25
benzo TI
high
26
benzo and anesthsia
cannot induce a state of surgical anesthesia
27
benzo dependance liablity
low
28
benzo antidote
flumazenil
29
benzo and induction
does not induce P450
30
benzos act by
interacting with the inhibitory GABA a receptors, has Cl channles, bind at a distinct site on the receptor
31
gaba binding to gabaA rec
opening of chlride channel, leading to hyperpolarization, increasing the firing threshold, and decrease generation of action potential
32
gaba and benzos
binding of gaba is enhanced by benzos resulting in a greater entry of chlroide ion due to greater freq of opening of the channels, reducing neural excitablity
33
benzo action
does not directly activate GABA-a rec but REQUIRES GABA to express their effects
34
GABA facilitatory
Benzodiazepines
35
benzo and Cl channels
inc frequency of opening of Cl channels
36
BZD receptors
bzd binds to alpha and gamma subunits in gaba receptor but NOT with beta subunit
37
Benzo receptor tyeps
BZ1 BZ2
38
BZ1
associated with alpha1 subunit. Mediates sedation (higher dose), anterograde amnesia, anticonvulsant action. Tolerance.
39
BZ2
associated with alpha2 subunit. Mediates antianxiety action, (low doses), muscle relaxation. No tolerance.
40
long acting benzo (1-3d)
flur azepam, di azepam, chlordi azepoxide, chlor azepate
41
intermediate acting benzo (20-20h)
alpr azolam, lor azepam, tem azepam
42
short acting benzo (3-8hrs)
Tri azolam, Mid azolam, Ox azepam
43
Actions of benzos
selective depressant actions, NOT general depressants like barbiturates
44
Benzo on CNS
reduction of anxiety (anxiolytic) and aggression at low dose, sedation and induction of sleep (sedative and hypnotic), reduction of muslce tone and co-ordination (muslce relaxant), anti-convulsant effect, anterograde amnesia (an impairment of memory and recall of envents occuring after the dose is taken)
45
reduction of anxiety and aggression by benzo
at low doses, benzos are anxiolytics, reduce anxiety by selectivley inhibiting neuronal circuits in the limbic system of the brain (BZ2 rec mediate antianxiety and impairment of cognitive functions)
46
at the the benzo receptor
flumazenil (antagonist) and zolpidem (sedatives) can bind
47
Alprazolam also has
antidepressant actions
48
Triazolam is reported to produce
agression
49
tolerance depvelps to
sedative hypnotic property, and anticonvulsant property, NOT to anxiolytic property
50
benzo and sedation and induction of sleep
benzo decreases time taken to get to sleep (dec sleep latency and hasten onset of sleep), increase duration of stage 2 NREM, dec duration of REM sleep, red intermittent awakening and increase total sleep time, most subjects wake up with a feeling of refresing sleep, sedative action is mediated through BZ1R
51
benzo receptor for sedation
BZ1R
52
benso receptor for anxiolytic
BZ2R
53
benzo as a muscle relaxant
BZDs relax the spasticity of skeletal muscle, probably by increasing presynaptic inhibition in the spinal cord. At high dose, BZDs depress neuromuscular transmission, BZDs muscle relaxant effect is independent of sedative action
54
benzo muscle relaxants
clon azepam, flunitr azepam, di azepam
55
Anticonvulsant effects of benzos
ihibit the development and spread of epileptic seizures in the CNS, can exert anticonvulsant effects without marked CNS depression, so that mentation and physiologic activity are unaffected, tolerance develops to anticonvulsant action
56
anticonvulsant benzos
clon azepam, di azepam, nitr azepam, and flur azepam
57
respiratory effects of benzos
respiratory suppression occurs at high dose, | however no effect on normal subjects at hypnotic dose
58
caution of benzos
COPD and asthmatic patients are more prone to respiratory depression, also caution should be used in pts with cardiac complications
59
overdose of benzos can cause
death due to depression of medullary respiration center
60
CVS and Benzo
hypnotic dose in normal subjects will have no CVS effect, pre-anesthetic dose reduces BP and HR, Toxic dose leads to circulatory collapse due to depression in myocardial contractility (neg inotropic effect) and vascular tone
61
GIT and Benzo
decrease nocturnal gastric secretion
62
Structure of BZDs
lipophilic
63
bzd and pregancy
benzos cross placental barrier - FLOPPY BABY SYNDROME, | and secreted in the milk
64
most enzymes are metabolized by
hepatic cyp450 enzyme system to active compunds | -- some undergo enterohepatic circulation
65
bzds that do not have active metabolites and involve only conjugation, preferred in elderly
lor azepam, ox azepam, tem azepam
66
dealkylation and hydroxylation of bzds give rise to
many metabolites, some of which may be active, so biological effects may be much longer than plasma half-life
67
adverse effects of benzos
relatively safer drug, ``` monitor incoordination, impairment of mental and motor fn (driving machinery should be avoided), confusion, anterograde amnesia; ``` increased reaction time, cognitive performance appears to be affected less than motor performance
68
contraindication of benzos
pregnancy, substance abuse, sleep apnea
69
chronic use of benzos leadst to
tolerance and | dependance

Pharmacology 2 (12 decks)

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