Wednesday 15 June 2011

Cardiac and Renal Pharmacology Fundamental Concepts

CARDIAC ACTION POTENTIAL

Fast -Response Fibers: Cardiac Muscle, His-Purkinje System



Phase 0

Na+ channels open-sodium enters the cell down its concentration gradient  (fast INa)  causing
membrane depolarization. Rate of depolarization depends on number of Na+ channels open,  which in turn depends on resting membrane potential of the cell.

Class I antiarrhythmic drugs can slow or block phase 0 in fast-response fibers.

Phase  1

Na+ channels are inactivated. In some His-Purkinje cells, transient  outward K+  currents  and
inward C1-  currents contribute to the  "notch" and overshoot.

Antiarrhythmic drugs have no significant effects on these transient currents.

Phase 2

Plateau phase in which a slow influx of  ca2+  (ICa_L)  is "balanced" by a late-appearing outward
K+ current (the delayed rectifier current IK).

Antiarrhythmic  drugs have  no significant  effects on  these  currents during  this  phase of  the
action potential (AP).

Phase 3

Repolarization phase in which the delayed rectifier K+  current rapidly increases  as the Ca2+ cur-
rent dies out because of  time-dependent channel inactivation.

Class 111 antiarrhythrnic drugs slow this repolarization phase.

Note that during phases 0 through 3 a slow Na'  current ("window current") occurs, which can
help prolong the duration of  the action potential.

Phase 4

Return of membrane to resting potential-maintained by activity of  the Na+/K+-ATPase.

Responsiveness

Capacity of a cell to depolarize, associated with the number of Na'  channels in a ready state (see
Na channel below). This in turn depends on resting membrane potential:  the more negative the
resting potential (RP),  the faster the response.

Conductance

Rate of spread of an impulse, or conduction velocity-three major determinants:

- Rate of phase 0 depolarization-as Vmax  decreases, conduction velocity decreases and
vice versa.
- Threshold potential-the less negative, the slower the conduction velocity.
    Resting potential-the more negative the RP,  the faster the conduction.

Slow-Response Fibers (SA  and AV Nodes, Specialized Cells):




Fig: Cardiac Action Potentials  in Slow-Response Fibers

 

Relative Refractory Period (RRP) 

A strong stimulus can elicit a response, but the timing will be out of  sync with  the rest of  the
heart, and arrhythmias may occur.


Ratio of ERP to the action potential duration (APD) is a measure of refractoriness,  as illustrated
below. Decreases in ERP favor the formation and propagation of premature impulses.


 
          Fig: Relationship of ERP to APD


     Fig:   Mechanism of Action of Voltage-Gated Na+ Channels

This voltage-gated channel, which  is  responsible for the  fast Na  current  (INa),  exists in  three
conformations:
  • resting or ready state , open or active state 
  •  inactivated or refractory state                        
The channel has two gates: M  (activating) and h (inactivating), both of which are sensitive to
voltage changes. Inactivation  of  the h gate is slower; therefore, it stays open longer, and the Na
channel is active.

Recovery

Rate of  recovery of  the Na channel is dependent on resting potential (RP).  Fastest rate of  recov-
ery occurs at normal RP, and recovery  slows as membrane voltage increases. Rate of  recovery is
slower in ischemic tissue because cells may be partly depolarized at rest. This reduces the num-
ber of channels able to participate in  the next depolarization, which leads to a decrease in con-
duction rate in ischemic tissue. Na channel blockers also slow the rate of recovery  in such tissues.

ANS REGULATION OF HEART RATE

Nodal tissue, especially  that  of  the SA  node, is  heavily innervated  by  both PANS and SANS
fibers activating M2  and Beta1 receptors, respectively. Phase 4 slope is increased by an increase in CAMP  resulting from PI  receptor activation and slowed by a decrease in CAMP  resulting from
M,  receptor activation.

Increase in CAMP  will:

-  increase upstroke velocity  in pacemakers by increase of ICa-=
-  shorten AP duration by increase of  I,
-  increase HR by increase of If,  thus increasing slope of phase 4

Decrease  in CAMP:

- Does the opposite plus produces a K+ current  (IK/ACh),  which slows the rate of diastolic
depolarization and thus decreases HR
- Beta blockers prevent CAMP  formation, with primary effects on SA and AV  nodal tissues.

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