What are the pharmacokinetic variables represented by the acronym ADME?
A- Absorption
D- Distribution
M- Metabolism
E- Excretion
Name the four ways a drug gets across barriers during absorption.
What is aqueous diffusion?
Diffusion via concentration gradient.Drug has to be aqueous and hydrophilic, allowing it to pass through aquaporins
What type of drugs typically use lipid diffusion to cross cell membranes?
Small and uncharged or mostly uncharged drugs, such as steroids.
What drugs use special carriers in drug absorption?
drugs that are large and charged (utilizing active transport and facilitated diffusion )
What is bulk transport?
endocytosis and exocytosis (endocytosis-herceptin, exocytosis-acetylcholine)
Define Volume of Distribution (Vd).
*amount of the drug leaving the blood.
*higher Vd indicates more drug leaving the blood.
*Lowed Vd, means the mmore likely it is to stay in the blood.
*Dose=VdxTC
What is Clearance (CL)?
Ability of the body to eliminate a drug
* main removal mechanism is in the urine.
*Cl=ROE/C
What does concentration (C) refer to in pharmacokinetics?
*measured in ml or L
*the amount of a drug in a given volume
What is the Rate of Elimination (ROE)?
How much of the drug is leaving the body per time, measured in mg/min, mg/hr, or ng/min.
ROE= Cl x C
What is the difference between first-order and zero-order elimination? And what determines which order a drug uses?
*First-order: clearance is constant, rate of elimination varies with concentration. *Zero-order: rate of elimination is constant, clearance varies.
*the order of elimination depends on how a drug is eliminated from the body
What is target concentration?
*The specific amount of drug clinicians aim for, to achieve therapeutic effect
And what is Half-life?
*the amount of time it takes to eliminate 1/2 of concentration
How do you get to target concentration from Half-life
4(T1/2) = Vd x TC
How do find how long it will take to effectively eliminate a drug from the body?
Take half-life and muliply by 4.
What is bioavailability (F)?
How much of the drug reaches systemic circulation
What is a maintenance dose?
The dose given to maintain steady state of a drug by replacing eliminated drug.
What is the significance of therapeutic drug monitoring? (Peak and Trough)
Used for monitoring concentration in the blood for very toxic drugs and adjusting for patient-specific factors.
What tests are used to determine kidney function?
Creatinine clearance test, which monitors creatinine levels in serum and urine.
What does a high Volume of Distribution (Vd) indicate?
More drug is leaving the blood.
What does a high Clearance (CL) indicate?
The body is able to eliminate the drug efficiently.
What is capacity limited elimination also known as?
Zero-order elimination
What are the extraction rations? What will get high clearance?
*0.7-1=high
*0.3-0.7=intermediate
*<0.3=low
*high clearance needs high extraction ration and high blood flow
What does a high extraction ratio mean?
A high extraction ratio will be eliminated more quickly than a low extraction drug