2016 7 14 7 Central South Pharmacy. July 2016, Vol. 14 No.7 R96A 1672-2981(2016)07-0673-11 doi:10.7539/j.issn.1672-2981.2016.07.001 proton pump inhibitor PPI PPI 75.5% PPI PPI PPI PPI FDA PPI PPI PPI PPI PPI 25% 70% PPI PPI 30% 50% PPI PPI PPI 2016 5 28 proton pump inhibitor PPI PPI GERD GERD PPI PPI PPI PPI PPI ph 1 H H /K -ATP α H /K -ATP PPI 1 24 h PPI H 2 H 2 -RA 20% 1988 PPI 8 PPI 6 PPI PPI 673
Central South Pharmacy. July 2016, Vol. 14 No.7 2016 7 14 7 PPI CYP450 PPI 1 PPI P450 CYP2C19 CYP3A4 CYP2C19 2 extensive metabolite EM poor metabolite PM 12% 22% PM 3% PM PM CYP2C19 PM EM 7 PPI 2 PPI 24 h 20 mg ph 3 14 h ph 9 h 1 15 60 min PPI 3 PPI PPI 4 PPI 3 d 5 nocturnal acid breakthrough NAB PPI 3 d GERD 24 h ph GERD 2 NAB PPI 2 ph 4 60 min PPI PPI NAB H 2 -RA NAB 1omeprazole PPI 2 0.5 3.5 h 0.5 1 h 35% 60% 2 h 42% 96 h 83% H 2 -RA 20 mg/ 1 2 d 1 4 6 8-60 mg/ 1 d 1 90% 20 120 mg d 1 80 mg d 1 2 20 60 mg/ 1 2 d 1 4 8 40 mg/ 12 h 1 3 d 100% 1 40% 80% 5% 3% P4501A2 P4501A1 B 12 2lansoprazole 4 F3 3 1 30% 1.3 1.7 h 674
2016 7 14 7 Central South Pharmacy. July 2016, Vol. 14 No.7 24 h 13% 14% 3pantoprazole H /K -ATP H /K -ATP 5 6 2 7 75% 1.18 h P450 P450 P450 20 mg 40 mg - 40 mg PPI GERD GERD 24 h NAB CYP2C19 1rabeprazole H /K -ATP H /K -ATP 4 pka PPI ph PPI CYP2C19 CYP2C19 EM PM ph 4.0 PPI PPI HP HP 1.57 3.13 mg ml 1 HP HP HP 2 esomeprazole R S 2 1 1 S R 60% 4 PPI R S R CYP2C19 CYP3A4 P450 R 2 R CYP2C19 675
Central South Pharmacy. July 2016, Vol. 14 No.7 2016 7 14 7 S CYP3A4 CYP2C19 R 1 2 h 2 h INR 97% 3haprazole PPI H /K -ATP H /K -ATP 4 d ph CYP3A4 CYP3A4 PPI PPI PPI PPI PPI PPI ph PPI PPI PPI PPI ph PPI G PPI PPI GERD - - β 90% 95% PPI PPI ph 3 18 20 h 4 PPI 1 1 6 8 4 90% PPI HP HP HP PPI PPI 676
2016 7 14 7 Central South Pharmacy. July 2016, Vol. 14 No.7 PPI HP 2 10 14 d 1 PPI 40 mg/60 mg * Qd 40 mg/80 mg * Qd 30 mg Qd 40 mg Qd / 40 mg Qd 10 mg Qd 10 mg Qd / 10 mg/20 mg * Qd / 30 mg Qd / 30 mg Qd 20 mg Qd 10 mg Qd * - H 2 -RA PPI PPI 2014 GERD 1. PPI GERD PPI PPI PPI PPI H 2 -RA GERD PPI PPI PPI 2 PPI 2 1 PPI ph 2. PPI 8 3. GERD PPI PPI GERD PPI PPI 4. GERD NERD PPI NERD GERD GERD 5. PPI PPI PPI GERD Barrett PPI 6. GERD PPI PPI - - PPI G H 2 -RA PPI 2 BAO 10 mmol h 1 stress ulcer SU stress related mucosal disease SRMD SU SU SU 4 677
Central South Pharmacy. July 2016, Vol. 14 No.7 2016 7 14 7 SU Cushing 3 10 d 1 ICU 24 h 1 3 d 75% 100% SU 1% 17% 8% SU 1% 50% 80% ICU 1. SU 2015 Cushing 30% Curling MODS 2. SU 48 h ARDS SU SU SU SU 1. 2. 3. TRH 5-5-HT SU ICU ICU ICU ICU SU 2252 OR 25.5 OR 9.5 OR 7.3 OR 6.5OR 5.0 OR 4.6 OR 3.8OR 3.7 OR 3.6 OR 3.3 OR 15.6 OR 4.3 SU ICU 1. 1 1 48 h 2 [ INR 1.5 50 10 9 L 1 2 ] 3 1 4 10 5 30% 6 16 7 3 h 8 9 ARDS 10 30 min 90 mmhg 1 mmhg 0.133 kpa 40 mmhg 11 12 13 2. 2 1 ICU 1 2 3 d 3 250 mg d 1 4 ICU ICU SU SU Herzig 2013 75 723 SU 678
2016 7 14 7 Central South Pharmacy. July 2016, Vol. 14 No.7 1.16% 3.24% 2 2 60 2 2 2 a 2 b 2 c 2 d 3 e 3 7 8 9 10 11 12 a. b. c. 60 mg d 1 d. 50 10 9 L 1 INR 1.5 APTT 2 60 mg d 1 e. 1. 2. ph 24 h ph 3. SU 4. SU 5. ph 4 PPI ph 6 SU H 2 -RA PPI SU PPI H 2 -RA PPI SU H 2 -RA 2014 meta PPI H 2 -RA 1 H 2 -RA 20 mg 150 mg 400 mg 1 d 1 12 h 2 H 2 -RA 20 mg 150 mg 400 mg 2 d 1 PPI 20 40 mg qd 40 mg qd 30 mg qd 10 20 mg qd 20 40 mg qd 3 2 40 mg q12 h 80 mg qd 40 mg q12 h 30 mg q12 h 40 mg q12 h 4 ICU 2 5 ICU PPI ph 4 3 6 SU PPI 80 mg 8 mg h 1 SU SU [1]. 2015 [J]. 2015 35 7 728-730. [2]. 2015 [J]. 2015 95 20 1555-1557. [3] Cook DJ Fuller HD Guyatt GH et al. Risk factors for gastrointestinal bleeding in critically ill patients. Canadian Critical Care Trials Group [J]. N Engl J Med 1994 330 6 377-381. [4] Herziq SJ Roehberg MB Feinbloom DB et al. Risk factors for nosocomial gastrointestinal bleeding and use of acid-suppressive medication in non-critically ill patients [J]. J Gen Intern Med 2013 28 5 683-690. [5] GrubeRR MayDB. Stress ulcer prophylaxis in hospital- 679
Central South Pharmacy. July 2016, Vol. 14 No.7 2016 7 14 7 ized patients not in intensive care units [J]. Am J Health Syst Pharm 2007 64 13 1396-1400. [6] Spirt MJ Stanley S. Update on stress ulcer prophylaxis in critically ill patients [J]. Crit Care Nurse 2006 26 1 18-20 22-28. [7] EAST practice management guidelines committee. Practice management guidelines for stress ulcer prophylaxis [EB/ OL].www.east.org /Content/documents /practice management guidelines /stress-ulcer-prophylaxis. [8] Messori A Fadda V Maratea D et al. Intravenous proton pump inhibitors for stress ulcer prophylaxis in critically ill patients determining statistical equivalence according to evidence-based methods [J]. Int J Clin Pharmacol Ther 2014 52 10 825-829. 1 1 Hp PPI H 2- RA H 2 1. ACS 1 6 3 5 d PPI 24 h PPI 2. PPI 3. PPI H 2 -RA PPI PPI 25% Hb 80 g L 1 PPI H 2 -RA 4. Hp Hp PPI 10 14 d 1. H 2 -RA 20 mg 150 mg 400 mg 2 d 1 2. PPI 20 40 mg qd 40 mg qd 30 mg qd 10 20 mg qd 20 40 mg qd PPI 6 PPI 6 H 2 -RA PPI [1] 2012 [J]. 2013 52 3 264-268. 15% 30% NSAID 2% 4% NSAID 2009 NSAID NSAID 3 680
2016 7 14 7 Central South Pharmacy. July 2016, Vol. 14 No.7 3 NSAID 1. 2. 2 NSAID COX-2 PPI 1 2 1. 65 2. NSAID COX-2 2 NSAID PPI NSAID 3. 4. NSAID NSAID NSAID COX-2-2 1. PPI NSAID 2. PG NSAID 3. H 2 -RA 20 mg 150 mg 400 mg 2 d 1 20 40 mg qd 40 mg qd 30 mg qd 10 20 mg qd 20 40 mg qd NSAID COX-2 PPI HP NSAID PPI H 2 -RA COX-2 NSAID COX 1% 3% COX-2 PPI PPI 4 8 NSAID PPI PPI H 2 -RA [1]. 2013 [J]. 2014 34 2 73-76. [2]. [M]. 2013. PPI NSAID PPI 0.5 mg/ kg d 2.5 15.0 mg d 1 PPI PPI 1. H 2 -RA 20 mg 150 mg 400 mg 2 d 1 2. PPI 20 40 mg qd 40 mg qd 30 mg qd 10 20 mg qd 20 40 mg qd [1]. [M]. 1. 2013. 1 PPI 2 3 A D E K 3 4 80 681
Central South Pharmacy. July 2016, Vol. 14 No.7 2016 7 14 7 mg 40 mg q12 h 80 mg qd 40 mg q12 h 40 mg q12 h 40 mg/ 1 2 d 1 40 80 mg/ 1 2 d 1 20 40 mg/ qd [1]. [J]. 2007 1 10 37-48. [2]. [J]. 2010 22 12 186-187. [3]. 2013 [J]. 2013 33 4 217-222. [4]. 2014 [J]. 2015 35 1 4-7. [5]. 2014 [J]. 2015 35 3 277-282. [6]. [M]. 2013 88-93. [7]. 20 [J]. 2013 19 20 3826-3827. [8]. [J]. 2015 31 10 1695-1698. [9]. [J]. 2014 15 25 3495-3496. [10] Youssef SS Iskandar SB Scruggs J et al. Acute pancreatitis associated with omeprazole [J]. Int J Clin Pharmacol Ther 2005 43 12 558-561. [11] Das Ganguly Ghosh et al. Oral pantoprazole-induced acute pancreatitis in an 11-Year-Old Child [J]. Ther Drug Monit 2012 34 3 242-244. [12] Concept-SÖ MK AEY Design-SÖ EA Supervision-HS RA et al. Lansoprazole-induced acute pancreatitis [J]. Turk J Gastroenterol 2014 25 5 582-583. 1. SU PPI SU PPI 2. SU PPI SU ph 3. PPI SU 3 5 d 2 SU 4. SU PPI 1. PPI ph 24 h 3 SU H 2 -RA 2. PPI PPI 3. PPI SU 5.0% H 2 -RA 4.3% 1. 60 3.9% 18.8% O 2. PPI 40 mg d 1 20 mg d 1 20 mg d 1 3. 2 6 12 2 3 6 PPI 1. PPI 2. SU SU PPI 1. 17.4% 20 mg d 1 682
2016 7 14 7 Central South Pharmacy. July 2016, Vol. 14 No.7 14 d 2. 0.4% PPI 1. H 2 -RA 20 mg 150 mg 400 mg 2 d 1 2. PPI 20 40 mg qd 40 mg qd 30 mg qd 10 20 mg qd 20 40 mg qd PPI SU ph 4 [1] Hata M Shiono M Sekino H et al. Prospective randomized trial for optimal prophylactic treatment of the upper gastrointestinal complications after open heart surgery [J]. Circ J 2005 69 3 331-334. [2] Fujita K Hata M Sezai A et al. Is prophylactic intravenous administration of a proton pump inhibitor necessary for perioperative management of cardiac surgery? [J]. Heart Surg Forum 2012 15 5 E277-279. [3] Bateman BT Bykov K Choudhry NK et al. Type of stress ulcer prophylaxis and risk of nosocomial pneumonia in cardiac surgical patients cohort study [J]. BMJ 2013 347 f5416. [4] Fisher L Fisher A Pavli P et al. Perioperative acute upper gastrointestinal haemorrhage in older patients with hip fracture incidence risk factors and prevention [J]. Aliment Pharmacol Ther 2007 25 3 297-308. [5] Lalmohamed A Vestergaard P Javaid MK et al. Risk of gastrointestinal bleeding in patients undergoing total hip or knee replacement compared with matched controls a nationwide cohort study [J]. Am J Gastroenterol 2013 108 8 1277-1285. [6] Takeuchi T Ota K Harada S et al. The postoperative bleeding rate and its risk factors in patients on antithrombotic therapy who undergo gastric endoscopic submucosal dissection [J]. BMC Gastroenterol 2013 13 136. [7] Chen C Shi Y Zhang XP et al. Risk factors associated with stress ulcer bleeding in postoperative rectal cancer patients [J]. Zhonghua Wei Chang Wai Ke Za Zhi 2012 15 12 1277-1281. [8] Stephenson KA Fagan JJ. Effect of perioperative proton pump inhibitors on the incidence of pharyngocutaneous fistula after total laryngectomy a prospective randomized controlled trial [J]. Head Neck 2015 37 2 255-259. [9] Han JB Keller EE Grothe RM. Postoperative gastrointestinal bleeding in orthognathic surgery patients its estimated prevalence and possible association to known risk factors [J]. J Oral Maxillofac Surg 2014 72 10 2043-2051. [10] Guillamondegui OD Gunter OL Bonaides JA et al. Practice management guidelines for stress ulcer prophylaxis [J]. Eastern Association for the surgery of Trauma 2008 1-24. [11] Daley RJ Rebuck JA Welage LS et al. Prevention of sress ulceration current trends in critical care [J]. Crit Care Med 2004 32 10 2008-2013. [12] Hurt RT Frazier TH McClave SA et al. Stress prophylaxis in intensive care unit patients and the role of enteral nutrition [J]. J Parenter Enteral Nutr 2012 36 6 721-731. [13] Pisegna JR Sostek MB Monyak JT et al. Intravenous esomeprazole 40 mg vs. intravenous lansoprazole 30 mg for controlling intragastric acidity in healthy adults [J]. Aliment Pharmacol Ther 2008 27 6 483-490. [14] Wilder-Smith CH Röhss K Bondarov P et al. Esomeprazole 40 mg i.v. provides faster and more effective intragastric acid control than pantoprazole 40 mg i.v. results of a randomized study [J]. Aliment Pharmacol Ther 2004 20 10 1099-1104. 2016-05-282016-06-20 683