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Enzymes, which are proteins, are usually responsible for? The biotransformation of medications
Where does the vast majority of drug metabolism take place? in the liver
What is the most important group of enzymes for drug metabolism? cytochrome P450 enzymes
Biotransformation metabolizes active drug to one of three things. What are the three things the drug could be metabolized to? Less active compound, Inactive compound, or Another active compound.
What is a prodrug? a medication that is pharmacologically inactive when administered, but is quickly metabolized to an active form.
What are two examples of prodrugs? Cortisone and prednisone
What is the first-pass effect? a phenomenon of drug metabolism whereby the concentration of a drug is greatly reduced before it reaches the systemic circulation.
Clearance of a medication refers to? the volume of blood that is completely cleared of the drug per unit time
Renal elimination/excretion involves one or more of three processes....what are they? Filtration, Active secretion, and reabsorption
The passage of active, unchanged drug from the blood stream through the glomerulus into the urine is called? Filtration
The secretion of active, unchanged drug into the filtrate (and eventually into the urine) is called? Active secretion
The process of the drug returning to the blood stream before reaching the urine is known as what? reabsorption
What is Half-life? the amount of time it takes for the plasma concentration or the amount of a drug in the body (after absorption and distribution) to be reduced by 50 percent.
What is half-life dependent upon? clearance
How would a decrease in clearance affect the half-life of a drug, and how will that affect the drug concentration in the blood? It will increase the half-life, drug concentration will be increased as well.
A decrease in clearance and an increase in half-life could lead to what? toxicity (in some cases)
When does a drug reach steady state? when the amount of drug being administered equals the amount being eliminated.
In general how many half lives does it take for a drug to reach steady state? 5
In general, medications with a long half-life will have a dosing interval of what? once per day
In general, medications with a shorter half-life will have a dosing interval of what? twice per day or three to four times per day
What is the definition of pharmakokinetics? the effects of the body on drugs
What are the four components of pharmakokinetics? absorption, distribution, metabolism, and excretion
What is bioavailability? the amount - stated as a percentage - of a drug that reaches the systemic circulation after extra-vascular administration.
What would the bioavailability of an IV drug be? 100% (all of the drug reaches systemic circulation)
Which will have an affect on the bioavailability of a drug, reduced rate of absorption or reduced extent of absorption? reduced extent of absorption
Drugs "exist" in one of two "forms" while they are in the body....what are they? free(unbound,not protein bound) or protein bound
Drugs must be in which form to be active and have a therapeutic effect? free(unbound)
What is the primary protein that drugs may bind to and where is it made? albumin, in the liver
Created by: txst spr 2009
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