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ANTI-ANXIETY
DRUGS
VIJAY SALVEKAR
DEPT. OF PHARMACOLOGY
GRY INSTITUTE OF PHARMACY
Anxiety
 Unpleasant state of tension,
apprehension[fear]or uneasiness
[discomfort] that seems to arise
from an unknown source.
 Usually associated with somatic
symptoms tachycardia, sweating,
tremor, palpitation, hyper apnea,
etc
ANXIETY DISORDERS
o Panic Disorder- sudden periods of
intense fear that may include
palpitations, sweating, shaking,
shortness of breath, numbness, or a
feeling that something terrible is going
to happen.
2.Generalized Anxiety Disorder- a disorder
characterized by excessive or unrealistic
anxiety about two or more aspects of life
(work, social relationships, financial matters,
etc.), often accompanied by symptoms such
as palpitations, shortness of breath, or
dizziness
Phobic Disorders- intense, persistent,
and recurrent fears of certain objects
(such as snakes, spiders, or blood) or
situations (like heights, speaking in front
of a group, and public places).
Stress Disorders-
mental health disorders that are a result of an
atypical response to both short and long-term
anxiety due to physical, mental, or
emotional stress. These disorders can include,
but are not limited to
obsessive-compulsive disorder and
posttraumatic stress disorder.
oObsessive-Compulsive Disorder-
A psychiatric disorder characterized by obsessive thoughts
and compulsive actions, such as cleaning, checking,
counting, or hoarding. (OCD), one of the anxiety disorders,
is a potentially disabling condition that can persist
throughout a person's life. The individual who suffers
from OCD trapped in a pattern of repetitive thoughts and
behaviors that are senseless and distressing but extremely
difficult to overcome. OCD occurs in a spectrum from mild
to severe, but if severe and left untreated, can destroy a
person's capacity to function at work, at school, or even in
the home.Treatment includes talk therapy, medication or
both.
Anti anxiety drugs
o Mostly mild CNS depressants
o Control the symptoms of anxiety,
produce a restful state of mind
without interfering with normal
mental or physical functions.
Classification
1. Benzodiazepines: Diazepam ,Chlordiazepoxide
Oxazepam, Lorazepam, Alprazolam, Flurazepam
2) Azapirones :Buspirone ,Gepirone, Ipsapirone
3) Sedative Antihistaminic: Hydroxyzine
4) Beta blockers :Propranolol
5) Others: selective serotonin reuptake inhibitor[SSRIs]
6) tricyclic antidepressant. [TCA]
7) MAO- inhibitors
8) Serotonin-norepinephrine reuptake inhibitos [SNRI]
(venlafaxine)
 Meprobamate , Clonidine,
Benzodiazepines
Site of action: mid brain ,ascending
reticular formation ,&limbic system
MOA:
By post synaptic inhibition through
BZD receptor
PK of Benzodiazepines
 Given orally ,iv & im (lorazepam & temazepam)
 Oral absorption good
 Phase I & phase II metabolism
 Lorazepam & Oxazepam  no active metabolite 
short acting
ADR
 Sedation
 Light headedness
 Cognitive impairment
 Vertigo
 Confusion
 Appetite & Wt gain
 Alter in sexual function
 Dependence
Advantages of BZD
 High therapeutic index
 Do not affect respiration or cardiovascular
function
 No microsomal induction
 Specific BZD antagonist Flumazenilis
available
CHLORDIAZEPOXIDE
 First BZD used as an antianxiety
agent
 Produce smooth long lasting effect
 Preferred in chronic anxiety states
 T1/2 :5-15 hours
 Dose : 20-100 mg
OXAZEPAM
 Hepatic metabolism is less significant
 It is preferred in the elderly and those with
liver disease
 Short duration of action
 Used in short lasting anxiety state
LORAZEPAM
 Oral & IM administration
 No active mtb
 Short acting  preferred in elderly
 Used in short lasting anxiety ,Panic, OCD,
tension syndrome
 Dose: 1 - 6mg/day
ALPRAZOLAM
Anxiolytic + antidepressant
High potency anxiolytic
Useful in anxiety associated with
depression
Less drowsiness
Dose : 0.25-0.5mg BD or TDS
AZAPIRONES
 Buspirone , Gepirone, Ipsapirone
MOA:
Selective agonistic action on 5HT-1A
receptor
Weak D2 blocking action – no
antipsychotic or extrapyramidal S/E
Site of action:
Dorsal raphe seretoninergic neurones
Azapirones
Advantages:
 No sedation
 No tolerance or physical
dependence
 No abuse liability
 Less psychomotor
impairment
 Does not potentiate the
effect of other CNS drugs
Disadvantages
 Slow onset of action
 not suitable for acute
anxiety
 Requires thrice daily
admin
PK
 given orally, rapidly absorbed
 Extensive first pass metabolism
 Excreted through urine and faeces
ADR
 Dizziness ,headache, Nausea
 Tachycardia , Pupillary Constriction
DOSE: 5-10mg OD-TDS
SSRI in Anxiety
 Preferred in chronic anxiety states
 Started in low dose
 Slow onset of action
 Started along with BZD
Beta blockers
o Propranolol :reduce the symptoms of
anxiety
o They do not affect the psychological
symptoms (worry ,tension, anxiety)
o Used for performance/situational anxiety
o Dose: 20-40mg 2hr before the
performance
Different type of anxiety and its and
its management
 Generalized Anxiety Disorder: persistent excessive,
unrealistic worry associated with somatic symptoms.
 Acute phase – Benzodiazepines are preferred
 Rapid onset of action
 Eg: lorazepam, Oxazepam
 Not ideal for long term treatment due to abuse
liability & development of tolerance
 For long term use : Buspirone ,SSRIs .
Obsessive-Compulsive Disorder
 Obsessive thoughts and compulsive behaviors that impair
everyday functioning
 Treatment
o TCA (clomipramine) poorly tolerated
o SSRI
• Fluoxetine (5–60 mg/d),
• fluvoxamine (25–300 mg/d),
• sertraline (50–150 mg/d)
o Buspirone
o BZD
Panic Disorder:
Recurrent and unpredictable panic
attacks, with intense discomfort and fear
of impending doom or death.
Treatment
• SSRIs low doses
• Eg: 5–10 mg fluoxetine, 25–50 mg sertraline,
10 mg paroxetine
Phobic Disorders
 Persistent fear of objects or situations, exposure to
which results in an immediate anxiety reaction. The
patient avoids the phobic stimulus, and this
avoidance usually impairs occupational or social
functioning.
 Treatment
o Beta blockers : Propranolol 20–40 mg orally 2 h before
the event (performance anxiety)
o SSRIs
o MAO inhibitors
Stress Disorders
 Anxiety following exposure to extremetraumatic events.
The reaction may occur shortly after the trauma (acute
stress disorder) or be delayed and subject to recurrence
(PTSD) . In both syndromes, individuals experience
associated symptoms of detachment and loss of
emotional responsivity.
 Treatment
o Benzodiazepines and supportive/expressive
psychotherapy
o SSRI
o MAO inhibitors
Future prospects
 Cholecystokinin (CCK) antagonists
 Alpiderm: partial agonist on BZD
receptor
 Corticotropin-releasing factor (CRF)
antagonists
 Neuroactivesteroids
THANK YOU

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Anti-Anxiety drugs

  • 1. ANTI-ANXIETY DRUGS VIJAY SALVEKAR DEPT. OF PHARMACOLOGY GRY INSTITUTE OF PHARMACY
  • 2. Anxiety  Unpleasant state of tension, apprehension[fear]or uneasiness [discomfort] that seems to arise from an unknown source.  Usually associated with somatic symptoms tachycardia, sweating, tremor, palpitation, hyper apnea, etc
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  • 4. ANXIETY DISORDERS o Panic Disorder- sudden periods of intense fear that may include palpitations, sweating, shaking, shortness of breath, numbness, or a feeling that something terrible is going to happen.
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  • 6. 2.Generalized Anxiety Disorder- a disorder characterized by excessive or unrealistic anxiety about two or more aspects of life (work, social relationships, financial matters, etc.), often accompanied by symptoms such as palpitations, shortness of breath, or dizziness
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  • 8. Phobic Disorders- intense, persistent, and recurrent fears of certain objects (such as snakes, spiders, or blood) or situations (like heights, speaking in front of a group, and public places).
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  • 10. Stress Disorders- mental health disorders that are a result of an atypical response to both short and long-term anxiety due to physical, mental, or emotional stress. These disorders can include, but are not limited to obsessive-compulsive disorder and posttraumatic stress disorder.
  • 11.
  • 12. oObsessive-Compulsive Disorder- A psychiatric disorder characterized by obsessive thoughts and compulsive actions, such as cleaning, checking, counting, or hoarding. (OCD), one of the anxiety disorders, is a potentially disabling condition that can persist throughout a person's life. The individual who suffers from OCD trapped in a pattern of repetitive thoughts and behaviors that are senseless and distressing but extremely difficult to overcome. OCD occurs in a spectrum from mild to severe, but if severe and left untreated, can destroy a person's capacity to function at work, at school, or even in the home.Treatment includes talk therapy, medication or both.
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  • 17. Anti anxiety drugs o Mostly mild CNS depressants o Control the symptoms of anxiety, produce a restful state of mind without interfering with normal mental or physical functions.
  • 18. Classification 1. Benzodiazepines: Diazepam ,Chlordiazepoxide Oxazepam, Lorazepam, Alprazolam, Flurazepam 2) Azapirones :Buspirone ,Gepirone, Ipsapirone 3) Sedative Antihistaminic: Hydroxyzine 4) Beta blockers :Propranolol 5) Others: selective serotonin reuptake inhibitor[SSRIs] 6) tricyclic antidepressant. [TCA] 7) MAO- inhibitors 8) Serotonin-norepinephrine reuptake inhibitos [SNRI] (venlafaxine)  Meprobamate , Clonidine,
  • 19. Benzodiazepines Site of action: mid brain ,ascending reticular formation ,&limbic system MOA: By post synaptic inhibition through BZD receptor
  • 20.
  • 21. PK of Benzodiazepines  Given orally ,iv & im (lorazepam & temazepam)  Oral absorption good  Phase I & phase II metabolism  Lorazepam & Oxazepam  no active metabolite  short acting
  • 22. ADR  Sedation  Light headedness  Cognitive impairment  Vertigo  Confusion  Appetite & Wt gain  Alter in sexual function  Dependence
  • 23. Advantages of BZD  High therapeutic index  Do not affect respiration or cardiovascular function  No microsomal induction  Specific BZD antagonist Flumazenilis available
  • 24. CHLORDIAZEPOXIDE  First BZD used as an antianxiety agent  Produce smooth long lasting effect  Preferred in chronic anxiety states  T1/2 :5-15 hours  Dose : 20-100 mg
  • 25. OXAZEPAM  Hepatic metabolism is less significant  It is preferred in the elderly and those with liver disease  Short duration of action  Used in short lasting anxiety state
  • 26. LORAZEPAM  Oral & IM administration  No active mtb  Short acting  preferred in elderly  Used in short lasting anxiety ,Panic, OCD, tension syndrome  Dose: 1 - 6mg/day
  • 27. ALPRAZOLAM Anxiolytic + antidepressant High potency anxiolytic Useful in anxiety associated with depression Less drowsiness Dose : 0.25-0.5mg BD or TDS
  • 28. AZAPIRONES  Buspirone , Gepirone, Ipsapirone MOA: Selective agonistic action on 5HT-1A receptor Weak D2 blocking action – no antipsychotic or extrapyramidal S/E Site of action: Dorsal raphe seretoninergic neurones
  • 29. Azapirones Advantages:  No sedation  No tolerance or physical dependence  No abuse liability  Less psychomotor impairment  Does not potentiate the effect of other CNS drugs Disadvantages  Slow onset of action  not suitable for acute anxiety  Requires thrice daily admin
  • 30. PK  given orally, rapidly absorbed  Extensive first pass metabolism  Excreted through urine and faeces ADR  Dizziness ,headache, Nausea  Tachycardia , Pupillary Constriction DOSE: 5-10mg OD-TDS
  • 31. SSRI in Anxiety  Preferred in chronic anxiety states  Started in low dose  Slow onset of action  Started along with BZD
  • 32. Beta blockers o Propranolol :reduce the symptoms of anxiety o They do not affect the psychological symptoms (worry ,tension, anxiety) o Used for performance/situational anxiety o Dose: 20-40mg 2hr before the performance
  • 33. Different type of anxiety and its and its management  Generalized Anxiety Disorder: persistent excessive, unrealistic worry associated with somatic symptoms.  Acute phase – Benzodiazepines are preferred  Rapid onset of action  Eg: lorazepam, Oxazepam  Not ideal for long term treatment due to abuse liability & development of tolerance  For long term use : Buspirone ,SSRIs .
  • 34. Obsessive-Compulsive Disorder  Obsessive thoughts and compulsive behaviors that impair everyday functioning  Treatment o TCA (clomipramine) poorly tolerated o SSRI • Fluoxetine (5–60 mg/d), • fluvoxamine (25–300 mg/d), • sertraline (50–150 mg/d) o Buspirone o BZD
  • 35. Panic Disorder: Recurrent and unpredictable panic attacks, with intense discomfort and fear of impending doom or death. Treatment • SSRIs low doses • Eg: 5–10 mg fluoxetine, 25–50 mg sertraline, 10 mg paroxetine
  • 36. Phobic Disorders  Persistent fear of objects or situations, exposure to which results in an immediate anxiety reaction. The patient avoids the phobic stimulus, and this avoidance usually impairs occupational or social functioning.  Treatment o Beta blockers : Propranolol 20–40 mg orally 2 h before the event (performance anxiety) o SSRIs o MAO inhibitors
  • 37. Stress Disorders  Anxiety following exposure to extremetraumatic events. The reaction may occur shortly after the trauma (acute stress disorder) or be delayed and subject to recurrence (PTSD) . In both syndromes, individuals experience associated symptoms of detachment and loss of emotional responsivity.  Treatment o Benzodiazepines and supportive/expressive psychotherapy o SSRI o MAO inhibitors
  • 38. Future prospects  Cholecystokinin (CCK) antagonists  Alpiderm: partial agonist on BZD receptor  Corticotropin-releasing factor (CRF) antagonists  Neuroactivesteroids