Sedative - Hypnotic - Anxiolytic Drugs

Sedative Hypnotic Drugs :

that calms
• Sedative in a
drug a
person .
whereas
Hypnotics
induces
sleep .

used sedation
•

Drugs for ,
sleep & Anxiety can came

Dependent depression that extends sedation

Dose - Cms
from
to anesthesia to
Respiratory depression and even Death .

Benzodiazepines ( 132s) reach a

plateau in CNS
depression .

while barbiturates and alcohol

do not .

Others
classification : te

"
"
-

"
Sedative Hypnotic Drugs Zolpijdem
Benzodiazepine !
Barbiturates

typnotic Antianxiety Anticonvulsant .

Ultra
-
-

Clonazepam
Long Acting Short
short
Diazepam Oxazepam cllobazam
a
Pheno barbitone Acting Acting
Flurazepam Clonazepam f. te

Fria 201am Diazepam Bato barbitone Thiopen

Alprazolam -

tone
Pen to barbitone
 GABAA
-

BZD a Channel
Complex
-
-

•
It is anion channel ,
which on

increases the conductance

opening y
-

U ion
resulting in CNS

Depression
.

•
GABA increases the duration

of ,
Channel
opening by
binding to GABAA Receptor
site .

Barbiturates &
Benzodiazepines increase GABA
Binding
•

( GABA
facilitatory Action) .

So these
drugs increases the
frequency of channel
-
•

acts
opening .

Fluzamenil
competitive antagonist at
•
as a

BZD site and therefore inhibits its action .

Barbiturates
These derivatives Barbi toric Acid
of
•

are .

Causes increased flow through chloride Channel

•

(a)
By helping GABA to inhibit the Y subunit .

(b)
Prolong GABA
Activity
e) Increase the duration
of Ci channel
Opening .

(d) Binds of a
&
p units
 Adverse effects :

•
Distortion
of sleep ( Decrease duration g
REM )

Learning &
Memory impairment
•
.

Contradicted
•
in Acute intermittent
porphyria .

doses acute
•
At
high ,
poisoning may
occur -

(
is Coma

Iii , Depressed Respiration

eiiis
Hypotension
in Cardiovascular Collapse .

in Barbiturate Blisters .

Important Examples :

Induction
of Anesthesia :
•

cat
thiopental
(b) Midazolam
Diazepam
&

• Seizure Control :

(a) Phenobarbital .

② Med Notes
( www.mednol-es.in)
 Benzodiazepines ( BZP ,
BZD.BZ )

act action
• These
drugs by GABA
facilitatory .

°
Also
posses Anxiolytic anticonvulsant
,
and skeletal
relaxant
muscle
Properties .

132s
Receptors in Brain :

(a) Cerebral Cortese -

( Confusion ,
Amnesia)

(b) Thalamus ( Disinhibition .

Sedation .
Motor Inhibition )
structures Sedation )
(c) Limbic ( Anxiolysis ,

Functions :

• Potentiate GABA

Opening frequency
Increases channel
-

•
U
.

Have GABA mimetic

Activity
•
no
.

Act through Bz
Receptor
•
132 ,
mediates sedation .

mediates
1322
Antianxiety &
Impairment of cognitive
•

functions .

:-#
 •
Flumazenil ( Anexate "
) is an
antagonist to

Benzodiazepines .

Used Overdoses
Reversal Agent in
-

as a .

Binds at a similar site to BZD .

Adverse Effects :

Benzodiazepines are much

safer than Barbiturates .

•
But these
drugs can also :

is
Impair learning &
Memory .

dis Amnesia

(
iii. Paranoia &
Psychiatric disturbances
(
in Ataxia

in
Nightmares ( Withdrawal effects )
•

Flunitrazepam Tasteless BZD and is

implicated as

Date
rape dnep due to its Amnesia

Effects .
 Non - BZ Drugs ( Atypical Drugs )
•

Zolpidem &
Zaleplon :
[ Acting through Benzodiazepine
Receptor ]
Iii BZ , Receptor Agonist
.

cii , less
effect on
Cognitive function ( 1322 mediated )
-

Overdose
(Iii , Reversed
by Flumazenil .

in Used in Steed disorders

less tolerance
in &
Abuse liability ( sleepwalking ) .

•
Bus pirone [ Acting through serotonin
Receptor ]
ii. No
effect on GABA

(
ii , 5- HT , acoerotonin Rec .

) Partial
Agonist
Used disorder
iiiii for generalised Anxiety .

(in Non sedative

in Takes 1 to 2 weeks for effects .

 Melatonin
"

Rame Heon [ Acting through Receptor ]

( is Melatonin
agonist in
suprachiasmatic nuclei

( Ii ,
Used in Insomnia
Low Risk abuse addictive )
Liii , of ( ✗ ess
in Metabolised to
Active Metabolite and
by
( an CYP 1- A2

2cg .

•
Suxorexant ( Belsomra ) [ Acting through Orexin
Receptor ]
Iii Orexin receptor Antagonist
( Ii , Hypnotic Properties .
} (Newly discovered )

safety Profile
iii,
( - UNKNOWN

② Med Notes (www.mednotes.in)

Med Notes med notes ebooks
☒
full : .

company
. site

[ App Available ]