ANXIOLYTIC AND

HYPNOTIC DRUGS

.
 anxiolytic agents

An anxiolytic or antianxiety
agent is a drug prescribed
for the treatment of
symptoms of anxiety.
 Anxiety disorders as
recognised clinically include
• generalised anxiety disorder (excessive
anxiety lacking any clear reason)
• panic disorder (sudden attacks of
overwhelming fear occur in association with
marked somatic symptoms, such as sweating,
tachycardia, chest pains, trembling and
choking).
• phobias (strong fears of specific objects or
situations, e.g. snakes, open spaces, flying,
social interactions)
• post-traumatic stress disorder (recall of past
stressful experiences)
• obsessive compulsive disorder (e.g. fear of
contamination).
 
 CLASSIFICATION OF
ANXIOLYTIC AND HYPNOTIC
DRUGS
• Benzodiazepines.
• Buspirone.
• Barbiturates
• β-Blockers
• Sedative antihistamines
• Antidepressants
• antiepileptic drugs
• Zolpidem.( for insomnia)
 Benzodiazepines
Act by binding to GABAA receptor, thus
enhancing the inhibitory effect of
GABA.

Anxiolytic effects are mediated by

GABAA receptors containing the α2
subunit, while sedation occurs
through those with the α1 subunit.
 Effects of
Benzodiazepines
Benzodiazepines cause:
1. reduction of anxiety and aggression
2. sedation, leading to improvement of
insomnia Although { long-term use of
benzodiazepines as sleeping pills is
undesirable, owing to tolerance,
dependence and 'hangover' effects}
 Effects of
Benzodiazepines
• Benzodiazepines decrease the time taken
to get to sleep, and increase the total
duration of sleep, Both effects tend to
decline when benzodiazepines are taken
regularly for 1-2 weeks. Long-acting
drugs such as nitrazepam are no longer
used as hypnotics.
• muscle relaxation and loss of motor
coordination ( clonazepam)
• suppression of convulsions (antiepileptic
effect) (e.g. Clonazepam ,
 Side effects of
benzodiazepines
These may be divided into:
• toxic effects resulting from acute
overdosage
• unwanted effects occurring during
normal therapeutic use
• tolerance and dependence
• the appearance of a benzodiazepine
withdrawal syndrome when the
benzodiazepines are stopped or the
dose is reduced after long-term usage
 
 withdrawal symptoms of
benzodiazepines
• The withdrawal symptoms may
include anxiety & irritability
• sweating
• tremor
• sleep disorders
 Side effects of
benzodiazepines
1. Drowsiness & confusion
2. amnesia
3. impaired coordination, which
considerably affects manual skills
such as driving performance.
 BUSPIRONE
 
Buspirone is a partial agonist at 5-
HT1A receptors is used to treat
various anxiety disorders. It also
binds to dopamine receptors (e.g.
ipsapirone).
However, buspirone takes days or
weeks to produce its effect in
humans,. Buspirone is ineffective in
controlling panic attacks or severe
anxiety states.
side effects of Buspirone
• Buspirone has side effects quite
different from those of
benzodiazepines. It does not cause
sedation or motor
incoordination, nor have
withdrawal effects been reported.
 
• side effects are nausea, dizziness,
headache and restlessness, which
generally seem to be less
troublesome than the side effects of
 Barbiturates
Barbiturates are Non-selective central
nervous system depressants (Act
partly by enhancing action of
GABA)that produce effects ranging
from sedation and reduction of
anxiety to unconsciousness and
death from respiratory and
cardiovascular failure-therefore
dangerous in overdose
 Barbiturates
use as sedative/hypnotic agents is
no longer recommended.
Barbiturates that remain in clinical
use include:
• phenobarbital , to treat
epilepsy
• thiopental, used as an
intravenous anaesthetic agent .
 Barbiturates
Barbiturates induce a high degree of
tolerance and dependence.
They also strongly induce the
synthesis of hepatic cytochrome
P450 and conjugating enzymes, and
thus increase the rate of metabolic
degradation of many other drugs.
Sedative antihistamines
Sedative antihistamines such as
diphenhydramine &
promethazine, are sometimes used
as sleeping pills, intended to improve
children's sleep patterns.they have
antagonistic effect on H1 –receptor in
the brain.
 Antidepressants
Antidepressants as Selective
serotonin reuptake inhibitors such as
fluoxetine and sertraline are used
to treat certain anxiety
disorders.Their action in this context
appears to be independent of their
antidepressant effects.
 antiepileptic drugs
• Various drugs that enhance the
effects of GABA, developed primarily
as antiepileptic drugs ,may also be
effective in treating anxiety disorders
,They include gabapentin , and
valproate.
 zolpidem
• Zolpidem It is a short-acting
nonbenzodiazepine hypnotic that
potentiates inhibitory
neurotransmitter GABA, by binding to
GABAA receptors. It works quickly
(usually within 15 minutes)
• It was recommended that zolpidem
be used for short periods of time
using the lowest effective dose for
improving sleep quality.
Side effects of zolpidem
• zolpidem is associated with drug
tolerance, drug dependence,
rebound insomnia and CNS related
adverse effects.
• amnesia
• Hallucinations
• motor coordination
 Drug interaction with
anxiolytic or hypnotic drugs
• Cimetidine metabolism of
benzodiazepines inhibited by
cimetidine
• Rifampicin metabolism of
benzodiazepines possibly
accelerated by rifampicin
• Theophylline effects of
benzodiazepines possibly reduced by
theophylline
• enhanced hypotensive effect when
anxiolytics and hypnotics given with
 Drug interaction with
anxiolytic or hypnotic drugs
• Anaesthetics, General /increased
sedative effect when anxiolytics and
hypnotics given with general
anaesthetics
• Digoxin\ alprazolam increases plasma
concentration of digoxin (increased risk
of toxicity)
• Valproate \clobazam possibly increases
plasma concentration of valproate
• Omeprazole /metabolism of diazepam
possibly inhibited by omeprazole
 Drug interaction with
anxiolytic or hypnotic drugs
barbiturates accelerate the
metabolism of some drugs
including
• Chloramphenicol
• Corticosteroids
• Coumarins
• Digitoxin
• Doxycycline
 Drug interaction with
anxiolytic or hypnotic drugs
barbiturates accelerate the
metabolism of some drugs
including:
• Metronidazole
• Progestogens &oestrogenes
• Propranolol
• Clonazepam
• Rifampicin

 
 Drug interaction with
anxiolytic or hypnotic drugs
• Folates
plasma concentration of phenobarbital possibly
reduced by folates

• Valproate
plasma concentration of phenobarbital increased by
valproate (also plasma concentration of valproate
reduced)
• Alcohol
increased sedative effect when barbiturates given
with alcohol
 sedatives and dental
procedures

• The benefits of using sedatives befor

dental procedures involves
performing dental treatment on a
patient in an environment that’s
stress- and anxiety-free
 sedatives and dental procedures…cont.

• Some anxious patients may benefit

from the use of a hypnotic for 1 to 3
nights before the dental
appointment. Hypnotics do not
relieve pain, and if pain interferes
with sleep an appropriate analgesic
should be given. Diazepam ,
nitrazepam or temazepam are
used at night for dental patients.
 sedatives and dental procedures…cont.

• Benzodiazepines can alleviate

anxiety at doses that do not
necessarily cause excessive
sedation and they are of particular
value during short procedures or
during operations under local
anaesthesia ...
 sedatives and dental procedures…cont.

• In children anxiolytic treatment

should be used only to relieve
acute anxiety (and related
insomnia) caused by fear (e.g.
before surgery).