protease inhibitors 2 0.0 / 5 ? PharmacyMedicinal substancesUniversityNone Created by: RscottqubCreated on: 10-03-20 17:33 major sucesses ACE inhibitors , Gliptins 1 of 31 Renin acts on angiotensinogen, converted it into Angiotensin 1 2 of 31 ACE acts on angiotensin converting enzyme, acts on Ang I converting to Ang II 3 of 31 where does renin cleave , and what type of peptidase is it Leu-Leu , endopeptidase 4 of 31 ACE inhibitors prevent the conversion of Ang I --> Ang II 5 of 31 the 1st ACE inhibitor was captopril - but it was short acting - so required multiple daily dosing 6 of 31 better once daily ACE inhibitors were developed Enalapril, Lisinopril , perindopril . 7 of 31 captopril had many side effects , why do the newer inhibitors have fewer side effects? slower acting - less side effects 8 of 31 other ways of managing high BP other than ACE inhibitors renin inhibitors 9 of 31 what type of protease is renin aspartyl protease , produced in the kidneys 10 of 31 renin release is stimulated by hypotension in renal artery, sympathetic nerve activation , decreased sodium delivery in the DTubule 11 of 31 renin has less what compared to ACE inhibitors side effects 12 of 31 examples of renin inhibitors aliskeren , 3 generations of it - the 3rd is the best 13 of 31 type 1 diabetes autoimmune disease - B cell destruction, insulin requiring 14 of 31 type II diabetes lifestyle disease. treated 1st - lifestykle and diet change 2. metformin/gliptins 15 of 31 after a meal what does the pancreas secrete incretin hormones 16 of 31 incretin hormones work to lower blood glucose - they control insulin scretion, glucagon secretion, rate of gastric emptying 17 of 31 DPP - IV Dipeptidyl peptidase 4- enzyme which hydrolyses these incretin hormones - 18 of 31 DPP IV inhibitors give incretin hormomes longer to lower blood glucose 19 of 31 examples of DPP inhibitors Gliptins - sitagliptin, alogliptin, linagliptin 20 of 31 All gliptins obey lipinskis rule of 5 , and bind reversibly 21 of 31 many gliptins are available ... in combo with metformin 22 of 31 what type of protease is DPP exopeptidase - cleaves of depeptide at end of chain - this is enough to inactive the incretin 23 of 31 where does DPP cleave after the penultimate proline - therefore gliptins mimic this 24 of 31 sucess _ HIV protease inhibitors HIV protease responsible for maturation - gives virions ability to infect other host cells 25 of 31 HIV protease inhibitors prevent HIV maturation 26 of 31 1st gen IHV proteases Ritonavir - no longer used, v short T1/2 , 27 of 31 2nd generation HIV proteases lopinavir, Atazanavir , Tipranavir 28 of 31 lopinavir improved version of ritonavir - but cant be used on its own - used in combo with ritonavir 29 of 31 atazanavir once daily dose , longer t1/2, 30 of 31 Tipranavir potent vs some resistant strains of HIV protease 31 of 31
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