22085454
Description
Flashcards by Evian Chai, updated more than 1 year ago
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Created by Evian Chai
about 4 years ago
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| Question | Answer |
| Most drugs mimic or block cell function through these three things | 1. Pumps 2. Receptors 3. Enzymes |
| Chemotherapeutic agents act on what? | Cancer/microorganisms |
| How does lipid solubility impact absorption of a drug? What else impacts absorption? | Uncharged proteins are more lipid soluble, and are more easily absorbed 1. Bioavailability 2. Administration method (inhalation, nasal, rectal, IV, topical) |
| Agonists ... the target when bound Antagonists ... the target bound | Activate Don't activate |
| What is the difference between a drug with high affinity and efficacy? | High affinity means it has a high tendency to bind High efficacy indicates high tendency to bind AND activate |
| What does KD measure? On a graph, where is KD? | Affinity The concentration of drug needed to occupy 50% of the receptor Where graph reaches 50% |
| What does EC50 measure? | Efficiency Percentage of drug needed for 50% of max effect |
| Reversible antagonist drugs can be overcome by what? How do they impact the agonist-response curve? | Increasing the concentration of agonist They shift the graph to the right, so a higher concentration of agonist is needed for the same response |
| Irreversible antagonists impact the graph by | Lowering the max effect on the graph |
| Concentration of drug plotted against %of receptor occupied produces a graph with a ... shape While log[D] produces a .... shape |
X axis is [D] or log[D]
Y is Proportion of drugs
Image:
Plots (binary/octet-stream)
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| What 3 factors increase drug potency? | 1. High efficiency 2. High affinity 3. Slow to metabolise |
| Pharmacokinetics measures what ... does to .... While Pharmacodynamics measures what ... does to .... | 1. Organism does to drug - absorption, distribution, metabolism, excretion 2. Drug does to organism (PharmacoDynamics so drug) |
| How can drugs interact with each other? | 1. Activate/inhibit enzymes needed for other drugs 2. Mutual slowing of excretion |
| Where does metabolism of drugs occur? What are the two phases? | In the liver 1. Catabolic (SER, using enzymes) 2. Synthesis (chemical groups added to drug to make it more water soluble) |
| Where do drugs get excreted? What is t1/2? | Kidneys via glomerular filtration in the renal nephrons The half-life of the drug |
| Which type of drugs are excreted more slowly? | Lipid soluble ones |
| What are the 4 phases of clinical trials a drug must undergo? | 1. Small scale (20-80 healthy, test pharmacokinetics, side effects ) 2. Medium scale (patient volunteers, test efficacy, dosage) 3. Large scale (patient volunteers, optimise dosage, side effect incidence, compare w current) 4. Post-licensing (surveillance) |
| What is a physiological antagonist? | Two drugs bind to different receptors and cause effects that oppose each other |
| What does the agonist response curve measure? What is on the X and Y and what shape? | Measures how much agonist needed for max response X: Log of Concentration of agonist Y: % Max response Sigmoidal shape |
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