Question | Answer |
Define EC50 | The concentration of drug required to produce 50% of that drugs maximum response |
Define Kd | The concentration of drug required to occupy 50% of the receptors |
What are the 4 receptor superfamilies? | Metabotropic, Ionotropic, Tyrosine Kinase and DNA-linked |
Which enzymes are targeted by aspirin? | COX 1 and COX 2 |
What are the 5 stages of drug action | Absorption, Distribution, Exertion of pharmacological effects, Metabolism and Excretion |
9 methods of drug administration | Topical, Transdermal patch, Inhalation, Oral, Sub-lingual, Sub-cutaneous (SC), Intravenous (IV), Intra-muscular (IM), Suppository |
Define pharmacokinetics | The way the body responds to drugs |
Define pharmacodynamics | The effects of the drug on the body and their mechanism of action |
When does EC50=Kd | In the case of partial agonists |
Which pathways are linked to G-protein coupled receptors | Adenylate cyclase - cAMP
Phospholipase C - IP3, DAG |
Define affinity | How well a drug binds to its receptor |
Define efficacy | How good the drug is at activating the receptor once it has bound |
Is efficacy linked to occupancy? Explain. | No because lower concentrations than the Kd may cause 50% of the maximum response due to signal amplification |
On a graph what does the relationship between EC50 and Kd tell you? | EC50 and Kd will be closer together if the efficacy is low, they will be farther apart if the efficacy is high |
What is receptor reserve? | The number of free receptors once a drug has produced its maximum response |
When would a drug produce a high receptor reserve? | When it has a high efficacy, lower [D] required so more receptors would be left over |
Explain the importance of the receptor reserve in terms of safety and economy | Safety - giving too high a dose could be toxic
Economy - money isn't wasted producing a drug of higher concentration than is necessary |
Which compounds were used in Langley's experiment to provide evidence of receptors? | Nicotine and curare |