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