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27 Cards in this Set
- Front
- Back
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Drug Administration Blood Levels: the highest blood levels are achieved by ____, then _____, and then _____
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IV
IM Orally |
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Drug Administration Blood Levels
Blood Level = _____ + _____ Total Drug Concentration = _____ + _____ Is there any difference between the blood level and the total drug concentration? |
Drugs Dissolved in plasma water ("free drug") + drug bound to plasma proteins
Free + Bound |
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Only the _____ drug can be pharmacologically active
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Free
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What's the graph that we use?
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Plasma or serum concentration verses time graph
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_____ = the concentration on the graph that is the greatest.
_____ = the time after the dose when the Cmax occurs. |
Cmax
Tmax |
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time when the concentration of drug is rising.
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absorption phase
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time while drug is distributing throughout the body.
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Distribution Phase
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_____ time when drug is primarily being lost from the body.
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Elimination phase
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The distribution of drugs within then body depends on
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Tissue permeability
Blood flow Binding to plasma proteins Binding to subcellular components and receptors |
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The _____ is a major determinant of how often a drug is given in clinical studies, and therefore the approved drug dose.
How do you calculate a half life? |
half-life
Evaluating the elimination phase of a drug on a concentration verses time graph |
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The percentage of a non-IV dose that reaches the bloodstream
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Bioavailability
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Bioavailability = _____ of absorption, but not the _____ of absorption
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extent
rate How much of the drug gets absorbed...not how fast |
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The bioavailability for an IV dose is
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100%
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Bioavailability equation
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AUC (Oral)/AUC (IV)
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Oral administration – immediate release vs. sustained release:
Sustained release: _____ drug disintegration and dissolution – _____ absorption and _____ compared to immediate release dosage forms. Advantage of sustained release is _____ doses per day – but Cmax values are usually _____ than immediate release, so low blood levels must be effective for sustained release forms to work. |
slowed
proloned later Tmax fewer lower |
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the process whereby a drug molecule is modified in such a way to enhance its elimination from the body
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Drug Metabolism
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Active versus inactive metabolites: most metabolites are _____, because their structure no longer matches that of the receptor. However, some metabolites remain active because they still have some _____ for the parent drug receptor
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inactive
affinity |
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Most drug metabolism occurs in the _____ by oxidation and conjugation reactions that _____ of the metabolite. Once the metabolite forms within liver cells, it can be secreted back into the blood circulating through the liver, or into the _____, which then empties the metabolite into the _____.
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liver
increase the water solubility bile GI tract |
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Renal Elimination:
Kidneys eliminate drugs from the blood by two processes: _____: these drugs (_____ molecules, not protein bound) move through the renal glomerulus and into the renal tubule and are eliminated in the urine. _____: renal tubular cells can uptake certain drugs from the blood, and directly secrete the drug into the renal tubule and thus urine. |
Filtration
small Secretion |
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Renal Elimination The Impact of Renal Failure:
Filtration and secretion functions _____. Drug elimination is _____, and drug half-life _____. Without dosage adjustment, slowed elimination results in _____ drug levels. Higher drug levels in the blood can then potentially lead to drug _____. |
decrease
slowed increases higher toxicity |
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Variations in Drug Response and metabolism
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Sex, Age, Diet, Disease
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Benefits of sublingual
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It bypasses the liver
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Benefits of IM injection
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Slow, prolonged administration
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_____ protein binding drugs typically have _____ effects.
It's only the _____ drug that exerts its pharmaological effect Changes in protein binding _____ the drug's effect |
High
Faster...think of a pothead free increases |
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Most drugs have first order _____, which means linear. That is, we will have a linear elmination on a _____
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elimination
Log-linear graph (concentration being the log) |
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Daily pills: it takes about _____ half lives with consistent doses for the drug to get to a steady state. The amount in = _____. If a drug has a short half life, you get to steady _____.
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3-5
the amount out. faster |
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Extended release = _____ phases of absorption
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Longer
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