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AntiAnxiety Drugs .pptx

About antianxiety drugs in psychiatry

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Anti-Anxiety Drugs
By DHANIK MK
Anxiety
● Anxiety: Unpleasant state of tension,
apprehension or uneasiness that seems to
arise from an unknown source.
● Usually associated with somatic symptoms
● We can see tachycardia, sweating, tremor,
palpitation, hyper apnea, etc as the symptom.
ANXIETY DISORDERS
1. Panic Disorder
2. Generalized Anxiety Disorder
3. Phobic Disorders
4. Stress Disorders
5. Obsessive-Compulsive Disorder
Anti anxiety drugs
- Mostly mild CNS depressants
- 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: SSRIs, TCA, MAO- inhibitors, SNRI (venlafaxine)
i) Benzodiazepines
Site of action: midbrain ,ascending reticular formation & limbic system.
MOA: By postsynaptic 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.
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.
Adverse Reaction: Sedation, Lightheadedness , Cognitive impairment, Vertigo, Confusion,
Appetite & Weight gain, Alt in sexual function, Dependence.
1) CHLORDIAZEPOXIDE
- First Benzodiazepines used as an antianxiety agent.
- Produce smooth long lasting effect.
- Preferred in chronic anxiety states.
- T1/2 :5-15 hours.
- Dose : 20-100 mg
2) 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.

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AntiAnxiety Drugs .pptx

  • 2. Anxiety ● Anxiety: Unpleasant state of tension, apprehension or uneasiness that seems to arise from an unknown source. ● Usually associated with somatic symptoms ● We can see tachycardia, sweating, tremor, palpitation, hyper apnea, etc as the symptom.
  • 3. ANXIETY DISORDERS 1. Panic Disorder 2. Generalized Anxiety Disorder 3. Phobic Disorders 4. Stress Disorders 5. Obsessive-Compulsive Disorder
  • 4. Anti anxiety drugs - Mostly mild CNS depressants - 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: SSRIs, TCA, MAO- inhibitors, SNRI (venlafaxine)
  • 5. i) Benzodiazepines Site of action: midbrain ,ascending reticular formation & limbic system. MOA: By postsynaptic 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. 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. Adverse Reaction: Sedation, Lightheadedness , Cognitive impairment, Vertigo, Confusion, Appetite & Weight gain, Alt in sexual function, Dependence.
  • 6. 1) CHLORDIAZEPOXIDE - First Benzodiazepines used as an antianxiety agent. - Produce smooth long lasting effect. - Preferred in chronic anxiety states. - T1/2 :5-15 hours. - Dose : 20-100 mg 2) 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.
  • 7. 3) LORAZEPAM - Oral & IM administration. - No active metabolism. - Short acting - preferred in elderly - Used in short lasting anxiety ,Panic, OCD, tension syndrome. - Dose: 1 - 6mg/day 4) ALPRAZOLAM - Anxiolytic + antidepressant. - High potency anxiolytic. - Useful in anxiety associated with depression. - Less drowsiness. - Dose : 0.25-0.5mg BD or TDS. - Active metabolism.
  • 8. ii) AZAPIRONES - Buspirone , Gepirone, Ipsapirone. - MOA: Selective agonist action on 5HT-1A receptor. - Weak D2 blocking action – no antipsychotic or extrapyramidal S/E - PK: given orally, rapidly absorbed, Extensive first pass metabolism, Excreted through urine and faeces. - Site of action: Dorsal raphe serotonergic neurons. - 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 administration. - Adverse effects: Dizziness ,headache, Nausea Tachycardia , Pupillary Constriction. - Dosage: 5-10mg OD-TDS
  • 9. ● SSRI in Anxiety: - Preferred in chronic anxiety states. - Started in low dose. - Slow onset of action. - Started along with Benzodiazepines. ● Beta blockers Propranolol : reduce the symptoms of anxiety. - They do not affect the psychological symptoms (worry ,tension, anxiety). - Used for performance/situational anxiety. - Dose: 20-40mg 2hr before the performance.
  • 10. Different type of anxiety and its and its management 1. 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 . 2. Obsessive-Compulsive Disorder: Obsessive thoughts & compulsive behaviors that impair everyday functioning. Treatment: TCA (clomipramine) poorly tolerated SSRI • Fluoxetine (5–60 mg/d), fluvoxamine (25–300 mg/d), sertraline (50–150 mg/d), Buspirone & Benzodiazepines.
  • 11. 3) 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). 4) 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: 1) Beta blockers : Propranolol 20–40 mg orally 2 h before the event (performance anxiety) 2) SSRIs 3) MAO inhibitors
  • 12. 5) 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: Benzodiazepines and supportive/expressive psychotherapy; SSRI; MAO inhibitors. Future prospects ● Cholecystokinin (CCK) antagonists ● Alpiderm: partial agonist on Benzodiazepine receptor ● Corticotropin-releasing factor (CRF) antagonists ● Neuroactive steroids