Lecture 33: Clinical Pharmocokinetics 2 Flashcards
RATIONAL DOSAGE REGIMEN
-Plan for drug administration over time
(Shouldn’t exceed minimum toxic [ ])
Based on
1) Theraputic window (Range of [ ] helping pt)
2) Clearance (Amount excreting body)
3) Vd (Volume of distribution)
Theraputic Window
-Range of acceptable plasma levels
- Trough plasma [ ] = minimum effective [ ]
- Minimum toxic [ ] = peak plasma [ ]
Maintenance Dose
-Used to obtain desired plasma [ ] over long periods of time and maintain steady state of drug in the body
Maintenance dose = dosing rate x dosing interval
(CLx TC/how many times a day)
Loading Dose
-Used to obtain desired plasma [ ] rapidly
Loading dose = Vd X TC / F
Vd= Volume of distribution TC = Target Plasma [ ] F = Bioavailability (Always 1 with IV)
Dosing rate
CL X TC / F
CL X C
CL= Clearance TC = Target Plasma [ ] F = Bioavailability (Always 1 with IV)
How do fixed doses effect plasma level of drugs
fluctuations in the plasma level of the drug
Single IV Injection
Graph
The plasma level will peak and decrease exponentially with time
Multiple IV Injections
Graph
The plasma [ ] increases until a steady state is reached
-plasma [ ] fluctuates (Up and down and pointy at peak))
Oral admission
Graphs
Types of release
Graph:
- Round peak
- upward climb (bc needs to be absorbed first)
Slow release = lower/delayed peak, higher levels @ later time, take it less, short half lives
Rapid release = higher/immediate peak, lower levels @ later time
Describe steady state (Css)
- Amount given over time = amount eliminated over time
- Reached after 4 half-lives
Dosing rate-ss = rate of elimination-ss = CL X C/F
CL= Clearance C= Concentration F= Bioavailability
Continuous IV Infusion
- Rate of drug entry: Constant
- Plasma [ ] increases until rate of input and output are equal (Steady state)
Css= Infusion rate/CL
(Steady state plasma [ ] = proportional to Infusion rate)
-Infusion stops = plasma [ ] declines to 0 (takes same amount of time to get to 0 that it took to reach steady state)
Percentage of Steady state (Css) achieved after 1-4 half-lives
1 = 50% 2= 75% 3= 87.5% 4= 93.75% (all)
Half-life equation
t 1/2 = 0.693 x Vd / CL
PH Equation
PH - PK = log [unprotonated form]/[protonated form]
Continuous IV
-plasma [ ] increases and levels off when reaches steady state (hump looking)