Drug receptor interactions

Law of Mass Action ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],www.freelivedoctor.com

SATURATION CURVE Log [Drug] Drug-Receptor Complex [Drug] nM DR www.freelivedoctor.com

SATURATION CURVE [DR] [Drug] nM R T = Bmax R T = Total number of receptors Bmax = Maximal number of receptors Bound ,[object Object],[object Object],[DR] max www.freelivedoctor.com

TIME COURSE [DR] Equilibrium K D = Equilibrium Dissociation Constant ,[object Object],[object Object],[D] + [R] = [DR] 0 10 20 30 40 50 60 Time (min) www.freelivedoctor.com

SATURATION CURVE [Drug] nM [DR] K D At equilibrium, the dissociation constant is K D and the affinity is K A = 1/K D Thus when [D] = K D , half the total number of receptors will be occupied. www.freelivedoctor.com

Agonists and Antagonists ,[object Object],[object Object],[object Object],+ + + + + - - - - + - - www.freelivedoctor.com - - - + + +

Agonists and Antagonists ,[object Object],[object Object],[object Object],www.freelivedoctor.com

Agonists and Antagonists ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],www.freelivedoctor.com

Agonists and Antagonists ,[object Object],[object Object],[object Object],Glucocorticoid Hormones  Blood Sugar Insulin  Blood Sugar www.freelivedoctor.com

Agonists and Antagonists ,[object Object],[object Object],[object Object],Heparin , an anticoagulant, acidic If there is too much  bleeding and haemorrhaging Protamine sulfate is a base. It forms a stable inactive complex with heparin and inactivates it. www.freelivedoctor.com

Competition Binding Log [I] nM IC50 Binding of Drug D I = Competitor www.freelivedoctor.com

Competition Binding RANK ORDER OF POTENCY: A > B > C > D www.freelivedoctor.com Log [I] nM IC50 A B C D Four drugs

Drug Concentration Response SEMILOG DOSE-RESPONSE CURVE Effect or www.freelivedoctor.com

Drug Concentration Response SEMILOG DOSE-RESPONSE CURVE www.freelivedoctor.com ED50 50% Effect Maximal Effect Effect or

SEMILOG DOSE-RESPONSE CURVE www.freelivedoctor.com EFFECT POTENCY EFFICACY ED50 Maximal Effect Log [Dose]

SEMILOG DOSE-RESPONSE CURVE RANK ORDER OF POTENCY: A > B > C > D www.freelivedoctor.com A B C D EFFECT Log [Dose]

SEMILOG DOSE-RESPONSE CURVE RANK ORDER OF POTENCY: A > B > C > D RANK ORDER OF EFFICACY: A = C > B > D ED50 www.freelivedoctor.com A B C D RESPONSE

Agonists and Antagonists ,[object Object],[object Object],[object Object],fraction of the receptors thus, the higher the concentration of antagonist used, the more drug you need to get the same effect. www.freelivedoctor.com

Agonists and Antagonists ,[object Object],[object Object],[object Object],[object Object],www.freelivedoctor.com

Drug Concentration LINEWEAVER-BURKE PLOT 1 www.freelivedoctor.com 1 K D 1 Effect 1 Bmax K D Bmax 1 [D]

Quantal Dose-response Curves ,[object Object],[object Object],www.freelivedoctor.com 1 10 20 30 40 50 60 70 80 90 100 Dose (mg/kg) % population responding

Quantal Dose-response Curves ,[object Object],1 10 100 Dose (mg/kg) log scale % population responding ED50 ED90 ED10 www.freelivedoctor.com

Therapeutic Index Toxic effect www.freelivedoctor.com

Therapeutic index ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],www.freelivedoctor.com

Therapeutic Index Toxic effect ED99 ED13 ED1 www.freelivedoctor.com

APPENDIX www.freelivedoctor.com

Law of Mass Action ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],www.freelivedoctor.com

Law of Mass Action ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],www.freelivedoctor.com

Law of Mass Action ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],www.freelivedoctor.com

Law of Mass Action ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],www.freelivedoctor.com

Drug receptor interactions

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Drug receptor interactions