ANXIOLYTICS

Dr Neelam Joshi
Department of Psychiatry
 CONTENTS
• ANXIETY
• DEFINITIONS
• TYPES OF ANXIOLYTICS AND HYPNOTICS
• BENZODIAZEPINES
• Z COMPOUNDS AND BUSPIRONES
 Anxiety

Normal adaptive response Pathological/disorder if:

- fear -chronic
-flight or fright -without identifiable stimuli
-disproportionate
-impairment in work
 Definitions

• Anxiolytic: A drug that reduces anxiety and causes calm and quietness in a patient
• Sedative : A drug that decreases activity and calms the recipient
• Hypnotic : A drug that produces drowsiness and facilitates the onset and maintenance
of a state of sleep that resembles normal sleep
• Anxiety→Drowsiness→Sleep→Anaesthesia→Coma→Death
• Lower dose: calming effect
• Higher dose: cause sleep
• Newer anxiolytic without sedation -Buspirone
 Benzodiazepines

MOA:
• Acts on GABA, the predominant inhibitory neurotransmitter in human
brain.
• Binds to GABA-A receptor increase influx of calcium ions
hyperpolarization of neuronal membrane excitability
 Pharmacological effects

• Reduction of anxiety and aggression: associated with psychiatric disorders

Paradoxical effect: hyperexcitability talkativeness excitement aggression anger
• Sleep induction: reduce sleep latency,increase sleep time,reduce the no. of
awakenings, overall increase the quality of sleep
• Anterograde amnesia: esp. useful in minor surgeries and invasive procedures
• Anticonvulsant effect: used to control seizures
• Reduction in muscle tone and co ordination: by central action on GABA A
receptors
• Effect on respiration: decreases respiratory drive
• Effect on CVS: decreases blood pressure
 Pharmacokinetics
• Well absorbed after oral administration
• Metabolized extensively by hepatic CYPs
• Excreted in urine
 Commonly used benzodiazepines

• Diazepam
• Chlordiazepoxide
• Lorazepam
• Clonazepam
• Clorazepate
• Flurazepam
• Prazepam
• Quazepam
• Halazepam
 Indications
• Insomnia
• Anxiety disorders
• Agitation and anxiety associated with Bipolar disorders,Schizophrenia
• Management of alcohol withdrawal
• Management of catatonia
 Adverse effects
• Sedation
• Ataxia
• Anterograde amnesia
• Confusion
• Muscle weakness
 Z Compounds
• Eg, Zolpidem, Zopiclone, Zaleplon
• Structurally unrelated to BDZ
• MOA: Agonist on GABA-A receptors
• Rapidly and well absorbed after oral administration.
• Indications: short term treatment of insomnia
• Adverse effects:
Sedation, dizziness, ataxia, dry mouth, loss of appetite, constipation
 BUSPIRONE
• Anxiolytic
• MOA: partial agonist for 5HT 1A receptors
• ADVANTAGES: No physical dependence, no abuse potential
• Less sedation and psychomotor impairment
• DISADVANTAGES: slow onset of action
• Short half life, more frequent administration
Indications:
• Generalized anxiety disorders
Adverse effects:
• Headache, nausea, dizziness, and rarely, insomnia.
THANK YOU