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     1
2
3
In simple words, “Study of the effects of drugs on the function of living systems”




Drug: a chemical substance of known structure, which, when administered to a living
                                                                                        4
                      organism, produces a biological effect.
5
6
In Simple words, “Study of how drugs act on living body”




  –   General principles

  –   Molecular aspects

  –   Cellular aspects




                                                      7
• The Binding Postulate

• Paul Ehrlich: “Corpora non agunt nisi fixata” i.e.
  'A drug will not work unless it is bound’


                        Cellular Binding Sites
                           (Drug Targets)


                                             Carrier
                           Ion
Receptors   Enzymes                        molecules      Miscellenous
                         channels
                                         (transporters)



                                                                    8
9
•   The cellular assembly which recognizes one or more chemical mediators




                                             Chain of           Physiological
Binding              Activation
                                            reactions              action




Affinity              Efficacy




                                                                                10
Affinity              Affinity         Affinity


                                                   Less
           Efficacy                               Efficacy




                                             Partial
     Agonist              Antagonist
                                             agonist




                                                             11
Antagonism




  Competitive                      Non-competitive




Reversible          Irreversible




                                                 12
13
14
15
Liberation     Absorption      Distribution   Metabolism   Excretion




             Bioavailability

                                                                  16
17
Lipid:water     Gastrointestinal
 pH partition
                     Partition         motility


                                    Physicochemical
Gastrointestinal
                    Particle size   interaction with
      pH
                                      gut contents



First Pass effect                       Prodrug

                                                       18
19
Lipid:Water
                 partition

                               Plasma
 Volume of      Blood Brain
                               Protein
distribution   barrier (BBB)
                               binding

                Placental
                 barrier
                                         20
21
22
23
Glomerular filtration



Active tubular secretion


Passive diffusion across
  tubular epithelium.
                           24
25
26
27
EC50                                      IC50
• Represents the concentration of an     • Represents the concentration of an
  agonist compound where 50% of its        antagonist compound where 50%
  maximal agonistic effect is observed     of its maximal antagonistic effect is
                                           observed




                                                                            28
Therapeutic
        ED50                         LD50                    Index
• Represents the             • Represents the dose     • Represents the ratio
  minimum required             required to kill half     of LD50 to ED50 i.e.
  dose to show desired         the members of a
  activity of drug in half     tested population         LD50
  the members of a             after a specific                     Therapeutic
  tested population            duration of time                        Index
  after a specific                                       ED50
  duration of time
                                                       • Safety parameter


                                                                            29
In vitro   Animal    Clinical
studies     trials    trials


                            30
31
32
• Pharmacology : It’s all about drugs

• Highly interdisciplinary applied science

• Different subdivisions – In overall, core of drug
  discovery

• One of the most important divisions of pharmaceutical
  sciences



                                                          33
34
35

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Effects of Drugs on Living Systems

  • 1. By 1
  • 2. 2
  • 3. 3
  • 4. In simple words, “Study of the effects of drugs on the function of living systems” Drug: a chemical substance of known structure, which, when administered to a living 4 organism, produces a biological effect.
  • 5. 5
  • 6. 6
  • 7. In Simple words, “Study of how drugs act on living body” – General principles – Molecular aspects – Cellular aspects 7
  • 8. • The Binding Postulate • Paul Ehrlich: “Corpora non agunt nisi fixata” i.e. 'A drug will not work unless it is bound’ Cellular Binding Sites (Drug Targets) Carrier Ion Receptors Enzymes molecules Miscellenous channels (transporters) 8
  • 9. 9
  • 10. The cellular assembly which recognizes one or more chemical mediators Chain of Physiological Binding Activation reactions action Affinity Efficacy 10
  • 11. Affinity Affinity Affinity Less Efficacy Efficacy Partial Agonist Antagonist agonist 11
  • 12. Antagonism Competitive Non-competitive Reversible Irreversible 12
  • 13. 13
  • 14. 14
  • 15. 15
  • 16. Liberation Absorption Distribution Metabolism Excretion Bioavailability 16
  • 17. 17
  • 18. Lipid:water Gastrointestinal pH partition Partition motility Physicochemical Gastrointestinal Particle size interaction with pH gut contents First Pass effect Prodrug 18
  • 19. 19
  • 20. Lipid:Water partition Plasma Volume of Blood Brain Protein distribution barrier (BBB) binding Placental barrier 20
  • 21. 21
  • 22. 22
  • 23. 23
  • 24. Glomerular filtration Active tubular secretion Passive diffusion across tubular epithelium. 24
  • 25. 25
  • 26. 26
  • 27. 27
  • 28. EC50 IC50 • Represents the concentration of an • Represents the concentration of an agonist compound where 50% of its antagonist compound where 50% maximal agonistic effect is observed of its maximal antagonistic effect is observed 28
  • 29. Therapeutic ED50 LD50 Index • Represents the • Represents the dose • Represents the ratio minimum required required to kill half of LD50 to ED50 i.e. dose to show desired the members of a activity of drug in half tested population LD50 the members of a after a specific Therapeutic tested population duration of time Index after a specific ED50 duration of time • Safety parameter 29
  • 30. In vitro Animal Clinical studies trials trials 30
  • 31. 31
  • 32. 32
  • 33. • Pharmacology : It’s all about drugs • Highly interdisciplinary applied science • Different subdivisions – In overall, core of drug discovery • One of the most important divisions of pharmaceutical sciences 33
  • 34. 34
  • 35. 35