SEDATIVE-

HYPNOTICS AND
ANTI-ANXIETY
DRUGS
Dr. Zoya Mehmood
Lecturer STMU
Sleep Disorders

 Insomnia
 Insomnia affects between 10-15 percent of the general
population
Sedation and Hypnosis

 Drugs that are classified as Sedative-hypnotics

are used both to relax the patient and to promote
sleep.
 Sedation: Calming effect
 Hypnosis: At higher doses the same drug can
induce drowsiness and relatively a normal state of
sleep
 Anesthesia
Sedative-Hypnotics

Benzodiazepines

Non-Benzodiazepines
Benzodiazepines
GABA

 Gamma aminobutyric acid (GABA) is probably the most

important inhibitory transmitter in the CNS.
 GABA-ergic neurons are distributed widely in the CNS. GABA
controls the state of excitability in all brain areas and the balance
between excitatory inputs and the inhibitory GABA-ergic activity.
 If the balance swings in favour of GABA -> sedation, amnesia, and
muscle relaxation is induced. Nervousness and anxiety are
reduced.
 The mildest reduction of GABA-ergic activity elicits -> arousal,
anxiety, rest-lessness, insomnia and exaggerated reactivity.
Mechanism of Action

 Benzodiazepines exert their effects by

increasing the inhibitory effects at CNS synapses
that use GABA. These synapses contain a
membrane protein complex with 3 primary
components:
1. Binding site for GABA
2. Binding site for BD
3. An ion channel specific for chloride ions
Cont..

 GABA-A-increase Cl entry
 GABA-B –increase K exit
 GABA-C

 Bzd act primarily on GABA-A

 GABA-A  alpha, beta, gamma
Non-Benzodiazepines
(end with barbital)

(end with barbital)

Cont..

 Common chemical origin: Barbituric acid

 Small Therapeutic Index; Overdose can be fatal
 Occasionally used for Hypnosis
 Mechanism of Action: Exact mechanism unclear
 GABA-A receptor (different site)
 Very addictive; prolong use is often a problem in
terms of drug abuse
 At higher doses  also depress neuronal excitability
in other areas of the brain and spinal cord
 General anaesthetics
Other Non-Benzodiazepines
Cont..

 Promote relaxation and sleep via depressing the

CNS
 Mechanisms poorly understood
 Lipid soluble substances dissolve in the lipid
bilayer and inhibit neuronal excitability by
disrupting membrane structures in the pre
synaptic and post synaptic regions of CNS neurons
 Zaleplon
 Zolpidem
Pharmacokinetics

 Mostly Oral administration

 Lipid soluble, absorbed easily and completely
from the GI tract
 Metabolized by the oxidative enzymes of the liver
 Often sequestered in adipose and other peripheral
tissues  hang over like feelings when
redistributed to brain
 Polar metabolite excreted by the kidney
Problems and Adverse effects

 Residual Effects
 Anterograde Amnesia
 Zolpidem and Zaleplon- newer agents with milder
side effects
 Physical dependence and tolerance: onset of
withdrawal symptoms if drug administration is
ceased abruptly (rebound Insomnia)
 GI discomfort, nausea, dry mouth, sore throat and
muscular incoordination
What is anxiety?
 Fear or apprehension over a situation or event that an
individual feels is threatening

 An anxiety state consists of feelings of tension,

apprehension, nervousness, worry and activation of the
autonomic nervous system

 Physiological manifestations generally include increased

blood pressure, rapid heart rate, sweating, dryness of mouth,
vertigo, irregularities in breathing, and muscular skeletal
disturbances
Normal VS. Abnormal Anxiety
 Anxiety is ‘normal’ in any situation in which an immediate danger
may result in physical harm

 Anxiety is also a normal reaction to social-evaluative situations

that pose threats to self-esteem or psychological well-being

 Neurotic, clinical, or abnormal anxiety occurs in situations in

which there is no real physical or psychological danger, or when
the emotional reaction is disproportionate in intensity to the
actual danger
Anxiety disorders

 Panic disorder
 Generalized anxiety disorder
 Social Anxiety disorder
 Performance anxiety
 Post-traumatic stress disorder
 Obsessive compulsive disorder
 Extreme anxiety associated with phobias
Anti anxiety Drugs
Benzodiazepines

Buspirone

Anti depressants
Benzodiazepines

 BDZ are typically the front-line drugs used to treat many forms of anxiety.
 Diazepam (Valium) is the prototypical antianxiety BDZ
 When prescribed in anxiolytic dosage  decrease anxiety without major
sedative effects
 Potentiate GABAergic transmission
Cont..

 BDZ also increase inhibition in the spinal cord, which

produces some degree of skeletal muscle relaxation,
which may contribute to their antianxiety effects by
making the individual feel more relaxed.
Buspirone
 Belong to drug class known as the Azapirones

 Serotonin agonist that stimulates certain serotonin receptors,

especially the 5-HT1A serotonin receptor subtype to treat many
anxiety disorders influenced by CNS serotonin levels

 Less sedation and psychomotor impairment than BDZ

 Less risk of developing tolerance and dependence

 Buspirone has only moderate efficacy; may not take effect as

quickly in patients with severe anxiety

 Safer for prolong use; less potential for drug abuse

Use of Antidepressants in
Anxiety
 Many patients with anxiety have symptoms of depression
 Patients with a combination of anxiety and depression are
given  benzodiazepine along with an antidepressant
 Some antidepressants have direct anxiolytic effects e.g.
paroxetine (Paxil) or venlafaxine (Effexor) are used as the
primary treatment for several forms of anxiety in people
who cannot tolerate side effects of traditional anxiolytics
Other anti-anxiety
drugs
 Beta-adrenergic antagonists (i.e beta
blockers) e.g propranolol:
 can reduce situational anxiety without producing
sedation
 seen to be used by musicians/ performing artists
to control palpitations, hyperventilation, muscle
tremors
Problems and Adverse Effects
 Sedation (X)
 Psychomotor impairment, especially during activities that
require people to remain especially alert, such as driving a
car
 Addiction and abuse are problems with chronic
benzodiazepine use, and withdrawal from these drugs can be
a serious problem causing  rebound anxiety. It is important
to follow psychological counseling too along with medicines
 Associated with buspirone include dizziness, headache,
nausea and restlessness
Special Considerations in
Rehabilitation
 Hospitalized patients and out patients  high
level of anxiety
 Administration of anti-anxiety and sedative
hypnotics have direct implications for the
rehabilitation session  patient cooperation
 Bzd reach peak levels 2-4 hours  Schedule OT
/PT session accordingly
 Sedative-Hypnotics  active participation, gait
training useless and hazardous
 Falls
 Balance training, environmental modifications
 Non-pharmacological interventions to decrease
anxiety and improve sleep
CASE STUDY