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Adrenergic Drugs II Aims To understand the actions and side effects of major adrenergic drugs, and their clinical applications Read:  Chapter 8, Rang and Dale comments to Dr Ian Musgrave (336S) Email:  Ian.Musgrave@adelaide.edu.au
Sympathomimetics: Types ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Amphetamine - indirect agonist ,[object Object],[object Object],[object Object],[object Object]
Amphetamine - indirect agonist
Ephedrine ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Tyramine ,[object Object],[object Object],[object Object],[object Object]
Cocaine ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Close up of Adrenergic terminal NA NA NA NA Tyrosine Dopamine DOPA NA MAO NA NA Metabolites Uptake 1 Vesicular transporter TH DDC D  H Vesicular  transporter Cocaine
Sympathomimetic Uses ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Sympatholytics: Types ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Directly acting sympatholytics - antagonists ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Adrenergic antagonists ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Non-selective alpha antagonists ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Non-selective alpha antagonists - structure Phentolamine Tolazoline Phenoxybenzamine Active intermediate (ethyleneimonium)
Effect of tolazoline and phenoxybenzamine on noradrenergic contraction in cat splenic strips + Tolazoline + Phenoxybenzamine Competitive vs non-competitive antagonism
Problems with non-selective alpha antagonists  ,[object Object],[object Object],[object Object],[object Object],[object Object]
Selective alpha antagonists Prazosin ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Adrenaline “reversal” adrenaline adrenaline Prazosin Blood Presure Blockade of vasoconstrictor   1 -adrenoceptors reveals vasodilator   -adrenoceptors Time Time Blood pressure recordings in anaesthetised dog
Alpha antagonists: Uses ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Beta antagonists: Types ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Beta antagonists - structure Propranolol (non-selective) Atenolol (  1 -selective) ICI 118551 (  2 -selective) Pindolol (intrinsic activity)
Effect of a beta-antagonist on heart rate
Non-selective   -antagonist Propranolol ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Adrenaline with and without propranolol adrenaline adrenaline propranolol Blodd Pressure Blockade of vasodilator   -adrenoceptors reveals vasoconstrictor   -adrenoceptors  Time Time
Propranolol Bioavailability Peripheral  Circulation propranolol Intestine Portal vein liver 100 % 30 % metabolites 70 %
Selective    -antagonist Atenolol ,[object Object],[object Object],[object Object],[object Object],[object Object]
Effects of Beta Blockade ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Relative Contraindications ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Antagonists with Intrinsic Sympathomimetic Activity Pindolol ,[object Object],[object Object],[object Object],[object Object],[object Object]
Clinical uses of   -antagonists ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Clinical uses of   -antagonists (cont) ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Agonist structure-activity relationships ,[object Object],[object Object],[object Object],[object Object]
Cartoon of adrenergic receptors  showing the 7 transmembrane spanning domains G S Family G i/o Family Adenylyl cyclase +ve -ve ATP cAMP  -adrenoceptors  2 -adrenoceptors Biological response cAMP dependent protein kinase
Structure-activity relationships Looking down on the   -adrenoceptor from outside the membrane  with adrenaline in the binding site between transmembrane domains 3,5 and 6 (model based on rhodopsin crystal structure) TM3 TM5 TM6
Structure-activity relationships  close up of binding site with adrenaline TM6 TM6 TM3
Agonist structure-activity relationships
Antagonist structure-activity relationships
Indirect sympatholytics NA NA NA MeNA Tyrosine Dopamine DOPA NA NA NA Uptake 1 Vesicular transporter TH DDC D  H Reserpine -ve Guanethidine -ve MethylDOPA  -Methyl tyrosine -ve
Indirect sympatholytics: ,[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]
Indirect sympatholytics: ,[object Object],[object Object],[object Object],[object Object]

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Adrenergic Drugs II

  • 1. Adrenergic Drugs II Aims To understand the actions and side effects of major adrenergic drugs, and their clinical applications Read: Chapter 8, Rang and Dale comments to Dr Ian Musgrave (336S) Email: Ian.Musgrave@adelaide.edu.au
  • 2.
  • 3.
  • 5.
  • 6.
  • 7.
  • 8. Close up of Adrenergic terminal NA NA NA NA Tyrosine Dopamine DOPA NA MAO NA NA Metabolites Uptake 1 Vesicular transporter TH DDC D  H Vesicular transporter Cocaine
  • 9.
  • 10.
  • 11.
  • 12.
  • 13.
  • 14. Non-selective alpha antagonists - structure Phentolamine Tolazoline Phenoxybenzamine Active intermediate (ethyleneimonium)
  • 15. Effect of tolazoline and phenoxybenzamine on noradrenergic contraction in cat splenic strips + Tolazoline + Phenoxybenzamine Competitive vs non-competitive antagonism
  • 16.
  • 17.
  • 18. Adrenaline “reversal” adrenaline adrenaline Prazosin Blood Presure Blockade of vasoconstrictor  1 -adrenoceptors reveals vasodilator  -adrenoceptors Time Time Blood pressure recordings in anaesthetised dog
  • 19.
  • 20.
  • 21. Beta antagonists - structure Propranolol (non-selective) Atenolol (  1 -selective) ICI 118551 (  2 -selective) Pindolol (intrinsic activity)
  • 22. Effect of a beta-antagonist on heart rate
  • 23.
  • 24. Adrenaline with and without propranolol adrenaline adrenaline propranolol Blodd Pressure Blockade of vasodilator  -adrenoceptors reveals vasoconstrictor  -adrenoceptors Time Time
  • 25. Propranolol Bioavailability Peripheral Circulation propranolol Intestine Portal vein liver 100 % 30 % metabolites 70 %
  • 26.
  • 27.
  • 28.
  • 29.
  • 30.
  • 31.
  • 32.
  • 33. Cartoon of adrenergic receptors showing the 7 transmembrane spanning domains G S Family G i/o Family Adenylyl cyclase +ve -ve ATP cAMP  -adrenoceptors  2 -adrenoceptors Biological response cAMP dependent protein kinase
  • 34. Structure-activity relationships Looking down on the  -adrenoceptor from outside the membrane with adrenaline in the binding site between transmembrane domains 3,5 and 6 (model based on rhodopsin crystal structure) TM3 TM5 TM6
  • 35. Structure-activity relationships close up of binding site with adrenaline TM6 TM6 TM3
  • 38. Indirect sympatholytics NA NA NA MeNA Tyrosine Dopamine DOPA NA NA NA Uptake 1 Vesicular transporter TH DDC D  H Reserpine -ve Guanethidine -ve MethylDOPA  -Methyl tyrosine -ve
  • 39.
  • 40.