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24 Cards in this Set
- Front
- Back
- 3rd side (hint)
Helpful drug? Harmful drug? |
Medicine Poison |
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Definition of a drug? |
Medicinal agent used for diagnosis, prevention,treatment of symptoms, and cure of diseases. |
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What are adverse drug responses appearing at therapeutic doses? |
Side effects |
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What are toxic effects? |
Adverse drug effects appearing at extreme drug doses. |
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What are the sites of drug interaction? |
1) Enzymes=inhibition 2) Drug receptors eg. Receptor sites on cell membrane 3) Non-specific eg. Physical means Outside of cells membranes |
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Explain Increasing resistance to chemical or enzymatic degradation? |
Uses steric shields or electronic modifications |
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What is potency? |
The amount of drug required for its specific effect to occur The inverse of the EC50 for that drug |
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What is efficacy? |
Measurement of the maximum strength of the effect itself at saturating drug concentrations |
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What are the different properties of drugs? |
Physical, chemical, physiological etc. |
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What are the different mechanisms of drug action? |
Physical properties Chemical properties Through Enzymes Through receptors |
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What are the steps of the drug development process? |
1) Target Identification 2) Target Validation 3) Designing 4)HTS 5)Lead Selection 6)Lead Optimization Pre-clinical trials Clinical trials |
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What is target Identification? |
Identifying a drug target such as an enzyme/DNA/receptor/ion channels that are involved in a metabolic or signalling pathway specific to a disease condition or pathology, or the infectivity or survival of a microbial pathogen. |
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What is target validation? |
Validation techniques : In vitro - whole animal models - diseased humans |
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Explain the Designing step? |
Synthesis of compounds effective against target. Straight forward,safe,cheap,effective , minimum number of steps,high quality,high purity. Subjected to biological screening to test activity and potency. |
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Explain HTS? |
Uses robotics,data processing,control software,liquid handling devices and sensitive detectors. Identifies active compound, antibodies, or genes which modulate a particular biomolecular pathway. |
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What is lead selection? |
A lead compound is a chemical compound that has pharmacological or biological activity and whose structure is used as a starting point for chemical modifications to improve potency, selectivity or pharmacokinetic parameters. |
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What is lead Optimization? |
Chemical modification of the hit structure Loos at structure activity analysis and structure based design--> can discover which parts of the molecule are important to biological activity and identify the pharmacophore |
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What is a pharmacophore? |
Collection of the important binding groups required for biological activity and their relative positions in space with respect to each other |
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What is the main objective of lead Optimization? |
To modify the lead compound to increase its activity, decrease it's side effects and provide easy and efficient administration to he patient. |
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What are the two main strategies of lead Optimization? |
1) strategies to improve the interaction with the target 2) strategies to increase the access of the drug to the target |
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What are the strategies to improve the interaction with the target? |
1) Simplification of the structure 2) Extension of the structure 3)Ring expansions/contractions 4) Variation of the substituents 5)Isosteres 6)Chain extensions/contractions 7)Ring variations 8)Rigidification of the structure |
SERVIC-RR |
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Simplification of the structure? |
Essential parts are retained. Advantage:much easier and cheaper to synthesize in the laboratory |
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Rvv |
Gggg |
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Ftvgvf |
Cf vrcrctc |
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