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ANTI-ANXIETY DRUGS
DR. RENJU.RAVI MD
Anxiety
 Unpleasant state of tension,
apprehension or uneasiness that
seems to arise from an unknown
source.
 Usually as...
ANXIETY DISORDERS
oPanic Disorder
oGeneralized Anxiety Disorder
oPhobic Disorders
oStress Disorders
oObsessive-Compulsive ...
Anti anxiety drugs
o Mostly mild CNS depressants
o Control the symptoms of anxiety,
produce a restful state of mind withou...
Classification
1. Benzodiazepines: Diazepam ,Chlordiazepoxide
Oxazepam, Lorazepam, Alprazolam, Flurazepam
2) Azapirones :B...
Benzodiazepines
 Site of action: mid brain ,ascending
reticular formation ,&limbic system
MOA:
By post synaptic inhibiti...
PK of Benzodiazepines
 Given orally ,iv & im (lorazepam & temazepam)
 Oral absorption good
 Phase I & phase II metaboli...
ADR
 Sedation
 Light headedness
 Cognitive impairment
 Vertigo
 Confusion
 Appetite & Wt gain
 Alt in sexual functi...
Advantages of BZD
 High therapeutic index
 Do not affect respiration or cardiovascular
function
 No microsomal inductio...
CHLORDIAZEPOXIDE
 First BZD used as an antianxiety
agent
 Produce smooth long lasting effect
 Preferred in chronic anxi...
OXAZEPAM
 Hepatic metabolism is less significant
 It is preferred in the elderly and those
with liver disease
 Short du...
LORAZEPAM
 Oral & IM administration
 No active mtb
 Short acting  preferred in elderly
 Used in short lasting anxiety...
ALPRAZOLAM
Anxiolytic + antidepressant
High potency anxiolytic
Useful in anxiety associated with
depression
Less drows...
AZAPIRONES
 Buspirone , Gepirone, Ipsapirone
MOA:
Selective agonistic action on 5HT-1A
receptor
Weak D2 blocking action...
Azapirones
Advantages:
 No sedation
 No tolerance or physical
dependence
 No abuse liability
 Less psychomotor
impairm...
PK
 given orally, rapidly absorbed
 Extensive first pass metabolism
 Excreted through urine and faeces
ADR
 Dizziness ...
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 ,tensio...
Different type of anxiety and its and
its management
 Generalized Anxiety Disorder: persistent excessive,
unrealistic wor...
Obsessive-Compulsive Disorder
 Obsessive thoughts and compulsive behaviors that impair
everyday functioning
 Treatment
o...
Panic Disorder:
Recurrent and unpredictable panic
attacks, with intense discomfort and fear
of impending doom or death.
...
Phobic Disorders
 Persistent fear of objects or situations, exposure to which
results in an immediate anxiety reaction. T...
Stress Disorders
 Anxiety following exposure to extreme traumatic events. The
reaction may occur shortly after the trauma...
Future prospects
 Cholecystokinin (CCK) antagonists
 Alpiderm: partial agonist on BZD
receptor
 Corticotropin-releasing...
THANK YOU
Anti-anxiety drugs
Anti-anxiety drugs
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Anti-anxiety drugs

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Anti-anxiety drugs

  1. 1. ANTI-ANXIETY DRUGS DR. RENJU.RAVI MD
  2. 2. Anxiety  Unpleasant state of tension, apprehension or uneasiness that seems to arise from an unknown source.  Usually associated with somatic symptoms tachycardia, sweating, tremor, palpitation, hyper apnea, etc
  3. 3. ANXIETY DISORDERS oPanic Disorder oGeneralized Anxiety Disorder oPhobic Disorders oStress Disorders oObsessive-Compulsive Disorder
  4. 4. 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.
  5. 5. Classification 1. Benzodiazepines: Diazepam ,Chlordiazepoxide Oxazepam, Lorazepam, Alprazolam, Flurazepam 2) Azapirones :Buspirone ,Gepirone, Ipsapirone 3) Sedative Antihistaminic: Hydroxyzine 4) Beta blockers :Propranolol 5) Others: SSRIs, TCA, MAO- inhibitors, SNRI (venlafaxine)  Meprobamate , Clonidine,
  6. 6. Benzodiazepines  Site of action: mid brain ,ascending reticular formation ,&limbic system MOA: By post synaptic inhibition through BZD receptor
  7. 7. PK of Benzodiazepines  Given orally ,iv & im (lorazepam & temazepam)  Oral absorption good  Phase I & phase II metabolism  Lorazepam & Oxazepam  no active metabolite  short acting
  8. 8. ADR  Sedation  Light headedness  Cognitive impairment  Vertigo  Confusion  Appetite & Wt gain  Alt in sexual function  Dependence
  9. 9. Advantages of BZD  High therapeutic index  Do not affect respiration or cardiovascular function  No microsomal induction  Low abuse liability  Specific BZD antagonist Flumazenil is available
  10. 10. 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
  11. 11. 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
  12. 12. 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
  13. 13. ALPRAZOLAM Anxiolytic + antidepressant High potency anxiolytic Useful in anxiety associated with depression Less drowsiness Dose : 0.25-0.5mg BD or TDS active mtb
  14. 14. 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
  15. 15. 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
  16. 16. 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
  17. 17. SSRI in Anxiety  Preferred in chronic anxiety states  Started in low dose  Slow onset of action  Started along with BZD
  18. 18. 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
  19. 19. 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 .
  20. 20. 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
  21. 21. 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
  22. 22. 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
  23. 23. Stress Disorders  Anxiety following exposure to extreme traumatic 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
  24. 24. Future prospects  Cholecystokinin (CCK) antagonists  Alpiderm: partial agonist on BZD receptor  Corticotropin-releasing factor (CRF) antagonists  Neuroactive steroids
  25. 25. THANK YOU

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