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NUR 613 Ch. 4
Term | Definition |
---|---|
4 phases of pharmacokinetics | |
All phases of pharmacokinetics depend upon.. | drug crossing membrane |
P-gylcoprotein | transmembrane protein that transports a wide variety of drugs out of cells |
To directly penetrate membranes, a drug must be.... | Lipophilic (lipid soluble) |
Factors affecting drug absorption | •Rate of dissolution •Surface area • Blood flow •Lipid solubility •pH partitioning •Site of administration |
Drug distribution is determined by these three factors: | • Blood flow to tissues • Exiting the vascular system • Entering cells |
Tight junctions | prevent drug passage |
Blood Brain Barrier is poorly developed in ? | babies -> sensitive to drugs that act on the brain |
Ion trapping | - the fetal compartment is more acidic than the mother - non-ionized substances that cross can become ionized in lower pH environments and then get "trapped" in the fetal compartment |
Protein binding | |
Bound vs. Unbound drugs | -Bound= inactive -Unbound= active/free |
Dynamic state | - between inactive and active form of drug-molecules -always leaving and attaching to the transport molecule |
Disorders that decrease or increase albumin production will... | change the free and bound concentrations of drugs |
Metabolism ( aka biotransformation) | Drug is converted to a less active or more active form |
First pass effect | drugs absorbed from the intestine are transported to the liver where the drug is metabolized to either decrease or increase the amount of active drug |
Induction of drug-metabolizing enzymes | - Certain drugs may induce liver enzymes that speed the metabolism of the inducing drug as well as other drugs - Ex: - Cytochrome P450 |
- Cytochrome P450 | |
Metabolic Competition | -if two drugs are metabolized by the same system, one will compete with the other - drug levels may not be predictable |
Steps in renal drug excretion | • Glomerular filtration • Passive tubular reabsorption • Active tubular secretion |
Factors that modify renal drug excretion | • pH-dependent ionization • Competition for active tubular transport • Age |
Single-dose Time Course | • Latent phase: time from administration to minimal effective concentration (MEC) • Duration of action: time from MEC to MEC |
• Duration of action: time from MEC to MEC | |
Drug Half-life (t1/2) | • the time required for the amount of drug in the body to decrease by 50% •T½ is independent of the amount of drug given |
plateau | When the amount of drug eliminated between doses equals the dose administered, average drug levels will remain constant |
plateau is reached in approximately ..... | 4 half lives |
when drug is discontinued... | 94% reduction in plasma level occurs in four half-lives |
Peak vs. Trough | Peak= Highest level Trough= Lowest level |
The "peak" drug concentration during the plateau phase is | approximately twice the peak of the first dose |
The "trough" drug concentration during the plateau phase is | approximately the same as the peak of the first dose |
foods that decreased absorption | milk, fiber |
foods that increase absorption | high calorie meal |
Pharmacokinetics definition | Impact of the BODY ON THE DRUG: |