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20 Cards in this Set
- Front
- Back
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What factors influence drug delivery? |
• Molecular structure - medicinal chemistry • Product formulation - pharmaceutics • Route of administration - pharmacokinetics |
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What controls drug absorption? |
Epithelial cell layer |
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What does a high Log P value indicate? |
The higher the Log P value, the more lipophilic the drug, I.e. more of the drug dissolved in the octanol (oil) phase |
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What does a lower Log P value indicate? |
The lower the Log P value, the more hydrophilic the drug, I.e. more of the drug dissolves in the water phase. |
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What is the optimal range of Log P values for oral drugs? |
0 to 3 |
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What does a very high Log P result in? |
Bioaccumulation e.g. the environmental contaminant Polychlorinated biphenyls (PCBs) with Log P > 5 |
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What does a low Log P result in? |
Poor Lipid Bilayer Permeability |
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Name the basic functional groups |
Amines (-NH2, NHR, NR2) |
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Name the acidic functional groups |
Carboxylic acids (-CO2H), sulphonic acids (-SO3H), and phenols (Ar-OH) |
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What is an example of a basic drug? |
Lignocaine (anime group) |
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What is an example of an acidic drug? |
Ibuprofen (carboxylic acid) |
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What is pKa a measure of? |
Acid strength- the higher the value, the weaker the acid |
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What happens if the pH is one unit more than the pKa value? |
91% of the drug is ionized |
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What happens if the pH is one unit less than the pKa value? |
91% of the drug is unionized |
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How does Log D relate to pH/pKa? |
In general, an ionized drug has a lower Log D value (less lipophilic) than its unionized form and so absorption is affected by pH |
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What is bioavailability? |
The amount of the drug absorbed |
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What aspects of an active pharmaceutical ingredient can affect a drug’s bioavailability? |
Morphology and particle size |
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Why are excipients used in pharmaceutics? |
The dosages of many drugs are very small (milligrams) so it would be impossible to administer them without a carrier. Can also be used to control drug absorbance |
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What does a bioequivalence study do? |
Compares the bioavailability of a drug for two or more products. Plasma/serum drug concentrations following administration are used to calculate the pharmacokinetics parameters which are then compared. |
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What is a pro-drug? |
A compound that becomes pharmacologically active through metabolism |
