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Pharm1Pkin
Pharm1 Pharmacokinetics
| Question | Answer |
|---|---|
| What is clearance? | The removal of a drug in units of volume/time. |
| Intensity of effect related... | To drug concentration at receptor sites. |
| Duration of action related to... | How long drug conc. at receptor site remains high enough to provide response. |
| One-compartment model easiest to use, and many drugs follow this scheme. | Assumes a single compartment which is in equilibrium which accounts for drug in plasma, and various tissues. |
| Two (or more) compartment models more difficult to model. | Seen when drug moves into tissues and is handled at different rates than central plasma compartment. |
| Two compartment model... | Involves both distributive and elimination phases normally.I |
| Describe log plot of two compartment model: | Log plot does not give a single straight line, but instead shows two phases. |
| What is zero-order kinetics? | The rate is independent of the concentration. |
| What happens if a process (ex.- elimination) is dependent on a carrier or enzyme that may become saturated? | Rate now no longer dependant on concentration, but instead becomes constant, at least until concentration falls below saturation. (Zero-order kinetics) |
| Bioavailability: | Percentage of a drug or drug product that enters the general systemic circulation. Includes not only amount entering body, but also rate of entry. |
| What is the volume of distribution? | The volume of distribution, Vd, is the apparent or “virtual” volume into which a drug distributes. |
| Can Vd be larger than the total plasma volume in the body? | heparin = 5 liters (plasma only) chlordiazepoxide = 28 liters (extracellular water) imipramine = 1600 liters (highly lipid soluble) |
| Knowledge of the Vd is also important in estimating the... | Loading dose. |
| About how many half-lives to reach steady-state? | Five. |
| Drugs with a t1/2 less than 6 hours require a <blank> to use them in repeated doses. | Very wide therapeutic window. |
| Drugs with narrow therapeutic windows should be given by... | Continuous infusion. |
| First pass may be saturable, and like all liver metabolism may increase due to... | Enzyme induction. |
| High Extraction Ratio: | ClH controlled by blood flow rate, Strong first-pass effect, Plasma protein binding may facilitate clearance |
| Low Extraction Ratio: | ClH controlled by intrinsic clearance, Biotransformation limited by diffusion, Plasma protein binding reduces clearance, Sensitive to enzyme inhibition and induction |
| Rate of renal excretion = | Rate of filtration + Rate of secretion – Rate of reabsorption |
| For Biliary Excretion: | ClB = (Conc. in bile / Conc. In plasma) Bile flow |
| What is normal bile flow? | Bile flow normally 0.5 – 0.8 ml/min. |
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