L9 Pharmacokinetic parameters Flashcards
I. pharmacokinetics
- Absorption
- Distribution
- Metabolism
- Excretion
……………….. assumes primary importance in oral, inhalation, and dermal exposures.
Absorption
The two kinetic parameters of concern are:
1- The rate of absorption
2- The extent of absorption (or bioavailability).
is a measure of the body’s ability to completely clear a drug from blood.
Clearance(CL):
Clearance is the rate of …………….
excretion
CL = ………………………………………..
Rate of elimination of drug / Plasma drug conc.
The time taken to reduce the plasma drug concentration by half:
Half-Life (t1/2)
(t1/2)= (0.693) x (v) over CL
• V= Volume of distribution
• CL= Clearance
………. does is an ………. ……… ………. of a drug given at the onset of therapy if a therapeutic concentration must be achieved rapidly.
Loading, initial high dose
Loading dose (LD) = (v) x (Desired C) over F
• V= VOLUME OF DISTRIBUTION • F= BIOAVAILABILTY
…………… dose is the dose of the drug required per unit time to maintain a desired steady state level in plasma to sustain a specific therapeutic effect
Maintenance
Maintenance dose ( MD) = (Desired Css) x (CI) over F
•CL= CLEARANCE
•F= BIOAVAILABILTY
A normal volunteer will receive a new drug in a phase I clinical trial. The clearance and volume of distribution of the drug in this subject are 1.386 L/h and 80 L, respectively. The half-life of the drug in this subject will be approximately…………….
• t1\2= 0.693X 80 L / 1.386 L/h
• = 40 HR
Estimate the oral loading dose of digoxin for a 70 kg man, which would be necessary to attain a plasma level of 1.5 μg/L (microgram/L)?
Vd of digoxin is 420 L, F for tablet is 0.62.
• Oral Loading Dose= 420 L X 1.5 μg/L / 0.62
• = 1016.129 μg
• = 1.016 mg
Estimate the IV loading dose of a drug, which would be necessary to attain a plasma level of 2 μg/L (microgram/L)?
Its Vd is 100 L, F for iv is one.
• Loading Dose= 2 X 100 = 200 microgram
……………. ……………… is the process that side effects of drugs are misdiagnosed as symptoms of another problem, resulting in further prescriptions and further side effects and unanticipated drug interactions, which itself may lead to further symptoms and further misdiagnoses.
Prescription cascade
is the use of numerous medications at the same time.
Polypharmacy
POLYPHARMACY MORE THAN .. ………….. AT THE SAME TIME
5 MEDICATION