Hint | Answer | % Correct |
---|---|---|
what is ADME? | absorption, distribution, metabolism, elimination | 100%
|
what happens if the drug is sufficiently polar after Phase I? | it may be eliminated without undergoing further metabolism | 100%
|
what reactions are included in Phase I, and what enzyme does this normally involve? | oxidation | 100%
|
reduction | 100%
| |
what is Phase I M? | where the substance is converted to a more polar metabolite by adding or changing a functional group | 100%
|
ability of the substance to bind to plasma proteins | 50%
| |
what is the A in ADME? | absorption: the process of the substance being taken up into the circulation | 50%
|
what does Phase I do to the drug? | activates or deactivates the original substance | 50%
|
what is Phase II catalysed by? | a family of non-specific transferases that require endogenous co-factors in order for the reaction to proceed | 50%
|
how do we calculate Vd? | amount of drug in the body/concentration in the blood | 50%
|
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) | 50%
|
what are the 5 factors that affect this? | blood flow | 50%
|
breast milk | 50%
| |
how are products of Phase II & III removed from the cell? | by various transporter proteins, which allows the products to now be eliminated | 50%
|
cytochrome P450 enzyme system | 50%
| |
deactivates the substance if Phase I did not | 50%
| |
what does the plasma concentration of each of these models do over time? | decrease exponentially over time | 50%
|
decrease in a linear fashion over time | 50%
| |
what is the D in ADME? | distribution: the transfer of the substance from the bloodstream to the tissues | 50%
|
what curve do we use to measure toxicodynamics? | dose-effect curve | 50%
|
what is the E in ADME? | elimination: removal of the substance from the body by the kidneys, gut, lungs, or skin | 50%
|
exhaled breath | 50%
| |
feces | 50%
| |
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 | 50%
|
hydrolysis | 50%
| |
increases the hydrophilicity | 50%
| |
what does Phase II do? | increases the molecular weight | 50%
|
what is toxicokinetics? | interaction between the body & the substance - what does the body do to the substance? | 50%
|
what is toxicodynamics? | interactions between a substance & its biological target - what does the substance do to the body? | 50%
|
lipid solubility of the substance | 50%
| |
what does this do to reabsorption? | makes it less likely to be reabsorbed by the kidneys as it is bigger | 50%
|
makes it more likely to be excreted by the kidneys as it is more water soluble | 50%
| |
what is the M in ADME? | metabolism: the conversion of the substance by enzymes into metabolites, which can either activate or deactivate the substance | 50%
|
what is Phase III M? | metabolites that could not be eliminated after Phase I & II are further processed, such as by acetylation | 50%
|
perfusion rate of the tissue | 50%
| |
sweat | 50%
| |
what is the LD50? | the dose of a substance that is required to kill 50% of the population | 50%
|
what is the ED50? | the dose of a substance that produces the desired effect in 50% of the population | 50%
|
what is first-pass metabolism? | the first pass of the substance through the liver, being metabolised by the hepatic enzymes | 50%
|
what is bioavailability? | the fraction of a substance that reaches the systemic circulation (after first-pass metabolism) | 50%
|
what is Phase II M? | the metabolite is conjugated with a charged compound such as glutathione | 50%
|
what is the therapeutic index? | the therapeutic window of safety of the substance (LD50/ED50) | 50%
|
what does this do to reabsorption? | this reduces the reabsorption of the metabolite back into the renal tubules, as it is less lipid soluble | 50%
|
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 | 50%
|
what are the mechanisms of E of the substance? | urine | 50%
|
vascular permeability | 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%
|
zero-order elimination: the elimination rate of the substance is independent of the concentration | 50%
|
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