| Hint | Answer | % Correct |
|---|---|---|
| what is ADME? | absorption, distribution, metabolism, elimination | 75%
|
| what reactions are included in Phase I, and what enzyme does this normally involve? | oxidation | 75%
|
| what happens if the drug is sufficiently polar after Phase I? | it may be eliminated without undergoing further metabolism | 50%
|
| reduction | 50%
| |
| what is first-pass metabolism? | the first pass of the substance through the liver, being metabolised by the hepatic enzymes | 50%
|
| what is Vd? | volume of distribution - the degree to which the substance is taken up by the tissues rather than staying in the blood | 50%
|
| what is Phase I M? | where the substance is converted to a more polar metabolite by adding or changing a functional group | 50%
|
| ability of the substance to bind to plasma proteins | 25%
| |
| what is the A in ADME? | absorption: the process of the substance being taken up into the circulation | 25%
|
| what does Phase I do to the drug? | activates or deactivates the original substance | 25%
|
| what is Phase II catalysed by? | a family of non-specific transferases that require endogenous co-factors in order for the reaction to proceed | 25%
|
| how do we calculate Vd? | amount of drug in the body/concentration in the blood | 25%
|
| how do you calculate bioavailability? | AUC oral/AUC iv (area under the curve of the oral dose of drug/area under the curve of the intravenous dose of the drug) | 25%
|
| what are the 5 factors that affect this? | blood flow | 25%
|
| breast milk | 25%
| |
| how are products of Phase II & III removed from the cell? | by various transporter proteins, which allows the products to now be eliminated | 25%
|
| cytochrome P450 enzyme system | 25%
| |
| deactivates the substance if Phase I did not | 25%
| |
| what does the plasma concentration of each of these models do over time? | decrease exponentially over time | 25%
|
| decrease in a linear fashion over time | 25%
| |
| what is the D in ADME? | distribution: the transfer of the substance from the bloodstream to the tissues | 25%
|
| what curve do we use to measure toxicodynamics? | dose-effect curve | 25%
|
| what is the E in ADME? | elimination: removal of the substance from the body by the kidneys, gut, lungs, or skin | 25%
|
| exhaled breath | 25%
| |
| feces | 25%
| |
| what are the 2 models of E? | first-order elimination (the most common): the elimination rate of the substance is directly proportional to its concentration | 25%
|
| hydrolysis | 25%
| |
| increases the hydrophilicity | 25%
| |
| what does Phase II do? | increases the molecular weight | 25%
|
| what is toxicokinetics? | interaction between the body & the substance - what does the body do to the substance? | 25%
|
| what is toxicodynamics? | interactions between a substance & its biological target - what does the substance do to the body? | 25%
|
| lipid solubility of the substance | 25%
| |
| what does this do to reabsorption? | makes it less likely to be reabsorbed by the kidneys as it is bigger | 25%
|
| makes it more likely to be excreted by the kidneys as it is more water soluble | 25%
| |
| what is the M in ADME? | metabolism: the conversion of the substance by enzymes into metabolites, which can either activate or deactivate the substance | 25%
|
| what is Phase III M? | metabolites that could not be eliminated after Phase I & II are further processed, such as by acetylation | 25%
|
| perfusion rate of the tissue | 25%
| |
| sweat | 25%
| |
| what is the LD50? | the dose of a substance that is required to kill 50% of the population | 25%
|
| what is the ED50? | the dose of a substance that produces the desired effect in 50% of the population | 25%
|
| what is bioavailability? | the fraction of a substance that reaches the systemic circulation (after first-pass metabolism) | 25%
|
| what is Phase II M? | the metabolite is conjugated with a charged compound such as glutathione | 25%
|
| what is the therapeutic index? | the therapeutic window of safety of the substance (LD50/ED50) | 25%
|
| what does this do to reabsorption? | this reduces the reabsorption of the metabolite back into the renal tubules, as it is less lipid soluble | 25%
|
| what is the goal of M? | to convert the substance into a more hydrophilic compound, which speeds up the rate of excretion by the kidneys | 25%
|
| what are the mechanisms of E of the substance? | urine | 25%
|
| vascular permeability | 25%
| |
| zero-order elimination: the elimination rate of the substance is independent of the concentration | 25%
|