17335112
Description
Flashcards by Simeon Crane, updated more than 1 year ago
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Created by Simeon Crane
about 5 years ago
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| Question | Answer |
| What are the 7 steps in the modern drug discovery process? | - Target identification - Target validation - Lead discovery - Lead optimisation - Pharmacological and toxicological profiling - Formulation development - Marketing authorisation |
| Name 3 methods for identifying drug targets | DNA microarrays Proteomics RNA knockdown |
| What are isosteres? | Molecules or ions of similar size containing the same number of atoms and valence electrons |
| Name 2 tests that are used to detect genotoxicity of a new drug | - Bacterial reverse mutation (Ames) test - COMET assay |
| What is meant by lead discovery in drug discovery process? | The process of identifying active new chemical entities, which by subsequent modification may be transformed into a clinically useful drug |
| What is the Easson-Stedman Hypothesis? | If two enantiomers demonstrate different activities at the same target, then three sites on the molecule must be involved in the interaction between drug and target |
| What is combinatorial synthesis? | A process used to prepare large sets of organic compounds by combining sets of building blocks |
| Name 4 drug related factors that affect the transport of drugs across biological membranes | - Concentration - RMM - Lipophilicity - Chemical structure and functional groups |
| According to Lipinkski's rule of five, what 4 factors affect drug absorption? | - Number of H-bond acceptors - Number of H-bond donors - Log P - Molecular Weight |
| What is the most commonly encountered reason for using pro-drugs for the delivery of therapeutic agents? | To reduce the toxicity of a drug |
| What does QSAR stand for? | Quantitative structure-activity relationships |
| What is a prodrug? | A biologically inactive molecule that is metabolised to produce the active drug |
| Name 4 types of drug degradation | - Hydrolysis - Oxidation/Reduction - Photolysis - Trace metal catalysis |
| What 5 factors will the particle size of a drug affect? | - Solubility and dissolution rate - Content uniformity in the final dosage form - Flow characteristics - Sedimentation rate - Bioavailability |
| What are the 3 basic rules of formulation design? | - Select excipients based on formulation type - Determine excipient compatibility - Use minimal number of excipients |
| What 3 factors determine if a drug should be formulated as a SVP or a LVP? | - Route of administration - Onset/duration of action - Concentration of drug in the product |
| What are the 8 components of a Target Product Profile? | - Business plan - Drug Discovery - Drug product development - Pre-clinical investigations - Phase 1 clinical trial - Phase 2 clinical trial - Exit strategy - IND/NDA application |
| What is Pharmacoeconomics? | The comparison of VALUE of one drug product or drug therapy over one that is already available to the patient |
| What two properties do class 2 drugs in the biopharmaceutical classification system have? | Low solubility High permeability |
| What characteristics of a drug has the greatest effect on the rate of passage through a biological membrane via passive diffusion? | Polarity of the drug molecule |
| What is the role of propylene glycol in a transdermal formulation? | Penetration enhancer |
| A drug molecule has high aqueous solubility and low permeability. What class in the biopharmaceutical classification system would it belong to? | Class 3 |
| What is a pharmacophore? | A part of a molecule structure that is responsible for a particular biological or pharmacological interaction that it undergoes |
| What is the most commonly used measurement of lipophilicity? | LogP |
| What is the most common type of drug target? | Enzymes |
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