Elimination rate constant

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Elimination rate constant is a value used in pharmacokinetics to calculate the rate at which drugs are removed from the system.[1]

It is often abbreviated K or Ke. It is equivalent to the fraction of a substance that is removed per unit time measured at any particular instant and has units of T-1 This can be expressed mathematically as C_{t+dt} = C_t - C_t * K_e*dt, where C_t is the concentration of drug in the system at a given point in time, dt is an infinitely small change in time, and C_{t+dt} is the concentration of drug in the system after the infinitely small change in time.

It is useful in calculating the change in plasma concentration after the administration of a single dose of drug:

C = C_{0} e^{-Kt} \,
  • Ct is concentration after time t
  • C0 is the initial concentration (t=0)
  • k is the elimination rate constant

[edit] Sample values and equations

Characteristic Description Example value Abbreviation(s) Formula
Dose Loading dose (LD), or steady state / maintenance dose (MD). 500 mg \textstyle D design parameter
τ Dosing interval. 24 h \textstyle \tau design parameter
Volume of distribution The apparent volume in which a drug is distributed immediately after it has been injected intravenously and equilibrated between plasma and the surrounding tissues. 6.0 L \textstyle V_d \textstyle = D / C_0
Concentration Initial or steady-state concentration of drug in plasma. 83.3 µg/mL \textstyle C_{0} \ or \ C_{ss} \textstyle = D / V_d
Biological half-life The time required for the concentration of the drug to reach half of its original value. 12 h \textstyle t_{1/2} \textstyle = ln (2) / k_{e}
Elimination rate constant The rate at which drugs are removed from the body. 0.0578 h-1 \textstyle k_e \textstyle = ln (2) / t_{1/2} = CL / V_{d}
Elimination rate Rate of infusion required to balance elimination. 50 mg/h \textstyle k_{in} \textstyle = C_{ss} \cdot CL
Area under the curve The integral of the concentration-time curve (after a single dose or in steady state). 1320 µg/mL×h \textstyle AUC_{0-\infty}

\textstyle AUC_{\tau,ss}
= \int_{0}^{\infty}C\, dt
= \int_{t}^{t+\tau}C\, dt
Clearance The volume of plasma cleared of the drug per unit time. 0.38 L/h \textstyle CL \textstyle= V_{d} \cdot k_{e} = D/AUC
Bioavailability The fraction of drug that is absorbed. 0.8 \textstyle f = \frac{AUC_{po}\cdot D_{iv}}{AUC_{iv}\cdot D_{po}}
Cmax The peak plasma concentration of a drug after oral administration. 60.9 µg/mL \textstyle C_{max} direct measurement
tmax Time to reach Cmax. 3.9 h \textstyle t_{max} direct measurement
Cmin The lowest (trough) concentration that a drug reaches before the next dose is administered. 27.7 µg/mL \textstyle C_{min,ss} direct measurement
Fluctuation Peak trough fluctuation within one dosing interval at steady state 41.8 % \textstyle %PTF \textstyle =100 \cdot \frac{(C_{max,ss} - C_{min,ss})}{C_{av,ss}}
where
\textstyle C_{av,ss}=\frac{AUC_{\tau,ss}}{\tau}
edit


[edit] References

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