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“In the name of Allah the most
 beneficent and merciful”.
 Presented to:
                   Sir Amir Rashid



 Presented by:
                   Syed Usman Farooq Gilani
                                       Bpd01093202
 Semester:
                   5th C




   DEPARTMENT OF PHARMACY
       The University Of Lahore
USE DEPENDENT &
VOLTAGE DEPENDENT
 Sodium Channels
GENERATION OF ACTION POTENTIAL
LOCAL ANESTHETICS
MECHANISM OF LOCAL ANESTHETICS
USE DEPENDENT
VOLTAGE DEPENDENT
Sodium Channels

   Excitable tissues possess special voltage-gated sodium
    channels. These voltage-gated sodium channels can
    exist in three functional states.


  1)   Closed channel(resting)
  2)   Open channel (activated)
  3)   Blocked channel (inactivated)
Sodium Channels




 Sodium channels consist of two gates;
        h-gates
        m-gates
Sodium Channels




 At the RMP, most h-gates are open and the m-gates
  are closed (closed channel).
Sodium Channels




 Depolarization causes the m-gates to open (open
  channels).
Sodium Channels




 but intense depolarization of the action potential
  then causes the h-gates to close the channel
  (inactivation).
GENERATION OF ACTION POTENTIAL

 Phase (0) Rapid depolarization;
  generation of action potential


 Phase (1) Partial re-polarization; slight
  re-polarization


 Phase (2) The plateau; potassium
  efflux, balanced by calcium influx


 Phase (3) Re-polarization; if
  potassium efflux is not balanced by
  sodium influx


 Phase (4) Resting membrane potential
  (RMP)
LOCAL ANESTHETICS

 Local anesthetics bind reversibly to a specific
  receptor site within the pore of the sodium
  channels in nerves and block ion (i.e. sodium)
  movement through this pore.


 When applied locally, local anesthetics can
  act on any part of the nervous system and on
  every type of nerve fiber, reversibly blocking
  the action potentials responsible for nerve
  conduction.
MECHANISM OF LOCAL
ANESTHETICS
 Local anesthetics penetrate into the interior of the
  axon in the form of the lipid-soluble free base.
MECHANISM OF LOCAL
ANESTHETICS
 There, protonated molecules are formed, which then
  enter and plug the sodium channels after binding to a
  ‘receptor’.
MECHANISM OF LOCAL
ANESTHETICS
 Local anesthetics blocks the sodium channel, largely by
  preventing the opening of h-gates (i.e. by increasing
  the inactivation).
MECHANISM OF LOCAL
ANESTHETICS
 Eventually, so many channels are inactivated that their
  number falls below the minimum necessary for
  depolarization to reach threshold and, because action
  potential cannot be generated, nerve block occurs.
MECHANISM OF LOCAL
ANESTHETICS
 Local anesthetics block sodium channels by physically
  plugging the trans-membrane pore. Their activity is
  strongly dependent upon pH(i.e. highest at basic pH and
  lowest at acidic pH).
MECHANISM OF LOCAL
ANESTHETICS
 At basic pH most of the molecules are unionized, so can
  easily penetrate in membrane to reach the inner and of
  sodium channel where the local anesthetic binding site
  resides.
USE DEPENDENT

 Local anesthetics are ‘use dependent’ (i.e. the degree of
  block is proportional to the rate of nerve stimulation).


 This indicates that more drug molecules (in their
  protonated form) enter the sodium channels when they
  are open and cause more inactivation.
USE DEPENDENT

 Use dependent means more of the channels are       open;
  the greater will be the block becomes.

 Because molecules can easily cross the channel, in open
  state.


 Local anesthetics have affinity for blocking channels in
  open and block state.
VOLTAGE DEPENDENT
 The site of anesthetic action is at the inner surface of
  the cell membrane.


 At tissue pH the drug is in the form of
  lipophilic, uncharged, secondary or tertiary amines and
  thus diffuses across cell membrane where it is ionized to
  a charged cation (+ve).
VOLTAGE DEPENDENT

 The cation form is the active form that blocks the action
  potential.


 Due to the ionic nature of anesthetic drugs, it poorly
  penetrates out of the cell and hence, prolongs the
  duration of action potential.
Use dependent & voltage dependent

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Use dependent & voltage dependent

  • 1. “In the name of Allah the most beneficent and merciful”.
  • 2.  Presented to:  Sir Amir Rashid  Presented by:  Syed Usman Farooq Gilani  Bpd01093202  Semester:  5th C DEPARTMENT OF PHARMACY The University Of Lahore
  • 3. USE DEPENDENT & VOLTAGE DEPENDENT  Sodium Channels GENERATION OF ACTION POTENTIAL LOCAL ANESTHETICS MECHANISM OF LOCAL ANESTHETICS USE DEPENDENT VOLTAGE DEPENDENT
  • 4. Sodium Channels  Excitable tissues possess special voltage-gated sodium channels. These voltage-gated sodium channels can exist in three functional states. 1) Closed channel(resting) 2) Open channel (activated) 3) Blocked channel (inactivated)
  • 5. Sodium Channels  Sodium channels consist of two gates;  h-gates  m-gates
  • 6. Sodium Channels  At the RMP, most h-gates are open and the m-gates are closed (closed channel).
  • 7. Sodium Channels  Depolarization causes the m-gates to open (open channels).
  • 8. Sodium Channels  but intense depolarization of the action potential then causes the h-gates to close the channel (inactivation).
  • 9. GENERATION OF ACTION POTENTIAL  Phase (0) Rapid depolarization; generation of action potential  Phase (1) Partial re-polarization; slight re-polarization  Phase (2) The plateau; potassium efflux, balanced by calcium influx  Phase (3) Re-polarization; if potassium efflux is not balanced by sodium influx  Phase (4) Resting membrane potential (RMP)
  • 10. LOCAL ANESTHETICS  Local anesthetics bind reversibly to a specific receptor site within the pore of the sodium channels in nerves and block ion (i.e. sodium) movement through this pore.  When applied locally, local anesthetics can act on any part of the nervous system and on every type of nerve fiber, reversibly blocking the action potentials responsible for nerve conduction.
  • 11. MECHANISM OF LOCAL ANESTHETICS  Local anesthetics penetrate into the interior of the axon in the form of the lipid-soluble free base.
  • 12. MECHANISM OF LOCAL ANESTHETICS  There, protonated molecules are formed, which then enter and plug the sodium channels after binding to a ‘receptor’.
  • 13. MECHANISM OF LOCAL ANESTHETICS  Local anesthetics blocks the sodium channel, largely by preventing the opening of h-gates (i.e. by increasing the inactivation).
  • 14. MECHANISM OF LOCAL ANESTHETICS  Eventually, so many channels are inactivated that their number falls below the minimum necessary for depolarization to reach threshold and, because action potential cannot be generated, nerve block occurs.
  • 15. MECHANISM OF LOCAL ANESTHETICS  Local anesthetics block sodium channels by physically plugging the trans-membrane pore. Their activity is strongly dependent upon pH(i.e. highest at basic pH and lowest at acidic pH).
  • 16. MECHANISM OF LOCAL ANESTHETICS  At basic pH most of the molecules are unionized, so can easily penetrate in membrane to reach the inner and of sodium channel where the local anesthetic binding site resides.
  • 17. USE DEPENDENT  Local anesthetics are ‘use dependent’ (i.e. the degree of block is proportional to the rate of nerve stimulation).  This indicates that more drug molecules (in their protonated form) enter the sodium channels when they are open and cause more inactivation.
  • 18. USE DEPENDENT  Use dependent means more of the channels are open; the greater will be the block becomes.  Because molecules can easily cross the channel, in open state.  Local anesthetics have affinity for blocking channels in open and block state.
  • 19. VOLTAGE DEPENDENT  The site of anesthetic action is at the inner surface of the cell membrane.  At tissue pH the drug is in the form of lipophilic, uncharged, secondary or tertiary amines and thus diffuses across cell membrane where it is ionized to a charged cation (+ve).
  • 20. VOLTAGE DEPENDENT  The cation form is the active form that blocks the action potential.  Due to the ionic nature of anesthetic drugs, it poorly penetrates out of the cell and hence, prolongs the duration of action potential.