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Pharmacology 1

Receptors

QuestionAnswer
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
Created by: sallyelphick
 

 



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