Anxiolytics med chem Lecture
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Lecture for B pharm, Medicinal chemistry of Purbanchal University of Nepal

Lecture for B pharm, Medicinal chemistry of Purbanchal University of Nepal

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  • Why delayed onset of action?

Anxiolytics med chem Lecture Presentation Transcript

  • 1. Psychotropic Agents These are drugs that cure mental disorders. Mental disorders includes abnormal changes in how a person feels, acts, thinks or perceives which degrades ability to function in ordinary life or socialize with others – Anxiolytic – Antidepressents – Antiphycotics
  • 2. Anxiolytics Drugs that cause mental clamness
  • 3. Anxiety • Anxiety is a normal fear response to stress or threats. It helps us to prepare for a “fight or flight” action • Too much or unnecessary anxiety can cause stress related disorders ranging from cognitive block to pain and heart palpitations (abnormal heart beat)
  • 4. Types of Anxiety • General Anxiety • Obsessive Compulsive Disorder • Panic Disorder • Post Traumatic Stress Disorder • Specific Phobias • Social Anxiety
  • 5. Is anxiety really a disease? Yes Clinical effects of General Anxiety • Constant worrying or obsession about small or large concerns • Restlessness and feeling on edge • Fatigue • Difficulty concentrating or your mind "going blank" • Irritability • Muscle tension or muscle aches • Trembling, feeling twitchy or being easily startled • Trouble sleeping • Sweating, nausea or diarrhea • Shortness of breath or rapid heartbeat
  • 6. Drugs used to treat Anxiety are 1) Benzodiazepines: – Chordiazepoxide, Clonazepam, – Alprazolam, Diazepam*, Lorazepam 2) Azapirones - Buspirone
  • 7. Chlordiazepoxide • It is a long acting benzodiazepam • It has amnestic, anticonvulsant, anxiolytic, hypnotic and skeletal muscle relaxant properties • It has an intermediate onset of action (15-30 mins), with a peak blood level occurring two to four hours after oral administration. It has active metabolite • Used for the short-term (2–4 weeks) treatment of anxiety • It’s long term use can cause depression, tolerance and dependence with withdrawal effects similar to alcohol • MOA- Anxiolytic effect is due to CNS depression caused by stimulation of GABAA receptors
  • 8. Clonazepam • It is a intermediate acting benzodiazepam • It has amnestic, anticonvulsant, anxiolytic, hypnotic and skeletal muscle relaxant properties • It has an intermediate onset of action (15-30 mins), with a peak blood level occurring one to four hours after oral administration • Used for the short-term (2-4) treatment of panic disorder (recurring panic attacks- palpitations, shaking and chest pain) • It’s long term use can cause depression, tolerance and dependence with withdrawal effects similar to alcohol • MOA- Anxiolytic effect is due to CNS depression caused by stimulation of GABAA receptors
  • 9. Azapirones: Buspirone • Azapirones are a class of drugs having both anxiolytics and antipsychotics activity • Anxiolytic action due to agonism at serotonin (5-HT]) type 1A receptor • antipsychotics activity is due to antagonism at D2 receptor • It has delayed onset of action but • As potent as diazepam with no tolerance and addictiveness and no sedative effects, no cognitive or motor impairment • They are very especially safe and effective in elderly patients • Used limited for mild to moderate anxiety and not useful in severe cases like panic attack
  • 10. Thanks
  • 11. Review How to they point out SAR of drugs?
  • 12. Comparative oral doses of various Benzodiazepams
  • 13. • SAR is developed by analyzing activity of a series of drugs with a small alteration made around a common structure • These alteration must be planned carefully so that effective comparisons can be made • We can judge in above compounds that – Substituting Nitrogen decreses activity (1st and 2nd) – Removing hydroxyl group improves activity (1st and 4th) – Having an extra aromatic nitrogen ring is good and compensates lack of Chlorine in lower ring(6th and 7th) – We know that for diazepams, having electronegative groups at specific positions is essential for activity and it reflected in these 8 marketed compounds but to include it as a valid SAR we need to compare it’s activity with those structures that lack those electronegative groups • But these small alteration have big changes in ADME
  • 14. Assignment • Refer the given research article and point out SAR of drugs called HDAC inhibitors • European Journal of Medicinal Chemistry 44 (2009) 1067e1085 • Key skill gained: • Knowledge on various structural diversity that can be implemented for drug design