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

Empfohlen

Empfohlen

Weitere ähnliche Inhalte

Was ist angesagt?

Was ist angesagt? (20)

Ähnlich wie Drug receptor interactions

Ähnlich wie Drug receptor interactions (20)

Mehr von raj kumar

Mehr von raj kumar (20)

Drug receptor interactions