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P H R M A C O L O G Y - NOTE 3 - Treatment of Peptic Ulcer

                                                                         DRUGS FOR PEPTIC ULCER



                  Drugs Affecting                                                   Mucosal                                                Drugs erdicate
                       HCL                                                      Protictive Agents                                            H. Pylori


                                                                                                      Colloidal Bismuth                                  Quadruple
     Antacids                 H2 Blocker          Sucralfate                      Misoprostol                                 Triple Therapy
                                                                                                        compounds                                         Therapy


                                                                                                                          Omeprazole OR                     Omeprazole OR
                                                                                                      Bismuth
         AL(OH)3                    Cimetidine                                                                             Lansoprazole                      Lansoprazole
                                                                                                    Subsalycilate
                                                                                                                               (PPI)                             (PPI)


                                                                                                      Bismuth                                                  Bismuth
         Mg(OH)2                    Ranitidine                                                                            Clarithromycin
                                                                                                     Sobcitrate                                              Subsalycilate


                                                                                                                          Amoxycillin OR
                                    Famotidine                                                                                                              Metronidazole
                                                                                                                          Metronidazole


   Proton Pump
                            Anti-muscarinic                                                                                                                  Tetracycline
     Inhibitors



       Omeprazole                   Pirenzepine
                                                                    (GU & DU)
                                                     Peptic Ulcer




                                                                                • It is caused by imbalance between:
                                                                                  • Protective Factors
       Lansoprazole                                                              •      (Mucus & Bicharbonate).
                                                                                 • Dameging Factors                                                                          8
                                                                                 •      (HCL & pepsin).
                                                                                • So, it is caused by either  DF or PF.

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P H R M A C O L O G Y - NOTE 3 - Treatment of Peptic Ulcer
                                               Drugs Affecting Gastric (HCL) Acid
                  DRUGS                            PHARMACOKINETIC                                      ACTION                             USES                       SIDE EFFECT
                  AL(OH)3            Weak bases (-OH).                                    1) Neutralize         Slowly          Used for symptomatic        Constipation.
                                     Taken 30 min in empty stomach.                          already                            relife of dyspepsia         In renal failure,
                                     Taken 2 hrs after meal.                                 secreted acid.                                                      Aluminum toxicity
Antacid




                                     Relieve heart burn immediatly.                       2) Inhibit                                                             Encephalopathy
                 MG(OH)2             If it take with other drugs,                            formation of       Fast                                        Diarrhoea
                                          It form insoluble com;ex that adsorb on            pepsin
                Combination                                                                                      Fast &                                      Constipation + Diarrhoea = nothing
                                              GIT wall not absorb.                                               sustained
                                    So, it take 2 hrs after or before other druds
                Simethicone             They are added to antacid either it combined or     surface tension                      Anti-flatulent.
Additives




                                         no.                                                    So, reduce buble                   To prevent reflux.
                                                                                                     formation.
                 Alginates                                                                  Form a layer of foam on the          Reduce reflux
                                                                                             top of gastric content.
    H2                                 Potency      T1/2     Duration     Inhibition of    Cyto-450 is an enzyme that                                        H2 antagonist cross placenta & are
antagonist                                                     (hrs)        Cyto-450       metabolizes drugs.                                                also secreted in breast milk.
 (blokers)       Cimetidine              1          1.5 –         6             1                                                Not used by elderly         Gynecomastia.
                                                     2.3                                                                         male because it is anti-    Galactorrhea.
 Extremly                                                                                                                        androgenic                  Inhibition of Cyto-450
save drugs                                                                                                                                                       So, conc. of Theophyline &
                                                                                                                                                                     Warfine.
                 Ranitidine            5 -10       1– 2.4        8             0.1


                Famotidine              32         2.5 - 4      12             0
                Omeprazole                  Average T1/2= 1.5 hrs.                        Irreversible inhibitors for
                                                                                             + +
                Lansoprazole                Need acidic media, So                          H /K ATPase
PPI




                                              Taken 1 hr befor meal.
                                              Don’t take with other acid suppressing
                                                  agent.
                Pirenzepine                                                                Inhibit gastric acid by blocking M3    Used in refractory
                                                                                           receptor                                cases that is not
muscarinic




                                                                                                                                   responding to other
  Anti-




                                                                                                                                   drugs.
                                                                                                                                  Used in nocturnal
                                                                                                                                   pain.




                                                                                                                                                                                                   9




 ‫ـــــألكم الدعاء‬
                ‫نس‬
P H R M A C O L O G Y - NOTE 3 - Treatment of Peptic Ulcer


                                                   Muocosal protective Agents
                          DRUGS                         PHARMACOKINETIC                                       ACTION                          USES                     SIDE EFFECT
                         Sucralfate             It is salt of ( socrose + AL(OH)3 ).              1) In acidic pH, it become
                                                Taken 1 hr befor meal.                               viscous gell & protect ulcer.
                                                Work in acidic pH                                 2) Stimulate PG production.
                                                       Not used with antacid or H 2 antagonist.
                        Misoprostol         It is a PGE1 analogue                                  1)   Gastric acid inhibition.      Used with NSAID to      Diarrhoea
                                                                                                   2)   Stimulate secretion of        prevent peptic ulcer    Abdominal pain.
                                                                                                        mucus & bicarbonate.                                  Abortion?
                                                                                                   3)   Enhance mucusal blood
                                                                                                        flow.
                    Bismuth subsalicylate                                                          1)   Coat the ulcer                                        Stain stools & tongue with black
                                                                                                   2)   stimulate secretion of                                 color.
                     Bismuth sobcitrate                                                                 mucus & bicarbonate.                                  Cause bismuth toxicity with long
                                                                                                   3)    PG synthesis.                                        used.
                                                   Drugs erdicate Helicobacter pylori
                          DRUGS                         PHARMACOKINETIC                                       ACTION                          USES                     SIDE EFFECT
                        Omeprazole             It is combination of ONE acid suppressant + 2
                              Or                antibiotics.
                     Lansoprazole (PPI)        Given for 14 days.
Triple Therapy




                       Clarithromycin          Then, followed by PPI for 4 - 6 wks.

                        Amoxycillin
                            or
                       Metronidazole
                        Omeprazole             It is combination of ONE acid suppressant + 3
                            Or                  antibiotics.
                     Lansoprazole (PPI)        Given when triple therapy fails.
Quadruple Therapy




                    Bismuth Subsalicylate
                       Metronidazole
                        Tetracycline




                                                                                                                                                                                                  10




  ‫ـــــألكم الدعاء‬
                 ‫نس‬

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Pharmacology.. Treatment of Peptic Ulcer

  • 1. P H R M A C O L O G Y - NOTE 3 - Treatment of Peptic Ulcer DRUGS FOR PEPTIC ULCER Drugs Affecting Mucosal Drugs erdicate HCL Protictive Agents H. Pylori Colloidal Bismuth Quadruple Antacids H2 Blocker Sucralfate Misoprostol Triple Therapy compounds Therapy Omeprazole OR Omeprazole OR Bismuth AL(OH)3 Cimetidine Lansoprazole Lansoprazole Subsalycilate (PPI) (PPI) Bismuth Bismuth Mg(OH)2 Ranitidine Clarithromycin Sobcitrate Subsalycilate Amoxycillin OR Famotidine Metronidazole Metronidazole Proton Pump Anti-muscarinic Tetracycline Inhibitors Omeprazole Pirenzepine (GU & DU) Peptic Ulcer • It is caused by imbalance between: • Protective Factors Lansoprazole • (Mucus & Bicharbonate). • Dameging Factors 8 • (HCL & pepsin). • So, it is caused by either  DF or PF. ‫ـــــألكم الدعاء‬ ‫نس‬
  • 2. P H R M A C O L O G Y - NOTE 3 - Treatment of Peptic Ulcer  Drugs Affecting Gastric (HCL) Acid DRUGS PHARMACOKINETIC ACTION USES SIDE EFFECT AL(OH)3  Weak bases (-OH). 1) Neutralize Slowly Used for symptomatic  Constipation.  Taken 30 min in empty stomach. already relife of dyspepsia  In renal failure,  Taken 2 hrs after meal. secreted acid.  Aluminum toxicity Antacid  Relieve heart burn immediatly. 2) Inhibit  Encephalopathy MG(OH)2  If it take with other drugs, formation of Fast  Diarrhoea  It form insoluble com;ex that adsorb on pepsin Combination Fast &  Constipation + Diarrhoea = nothing GIT wall not absorb. sustained  So, it take 2 hrs after or before other druds Simethicone  They are added to antacid either it combined or   surface tension  Anti-flatulent. Additives no.  So, reduce buble  To prevent reflux. formation. Alginates  Form a layer of foam on the  Reduce reflux top of gastric content. H2 Potency T1/2 Duration Inhibition of Cyto-450 is an enzyme that H2 antagonist cross placenta & are antagonist (hrs) Cyto-450 metabolizes drugs. also secreted in breast milk. (blokers) Cimetidine 1 1.5 – 6 1 Not used by elderly  Gynecomastia. 2.3 male because it is anti-  Galactorrhea. Extremly androgenic  Inhibition of Cyto-450 save drugs  So, conc. of Theophyline & Warfine. Ranitidine 5 -10 1– 2.4 8 0.1 Famotidine 32 2.5 - 4 12 0 Omeprazole  Average T1/2= 1.5 hrs. Irreversible inhibitors for + + Lansoprazole  Need acidic media, So H /K ATPase PPI  Taken 1 hr befor meal.  Don’t take with other acid suppressing agent. Pirenzepine Inhibit gastric acid by blocking M3  Used in refractory receptor cases that is not muscarinic responding to other Anti- drugs.  Used in nocturnal pain. 9 ‫ـــــألكم الدعاء‬ ‫نس‬
  • 3. P H R M A C O L O G Y - NOTE 3 - Treatment of Peptic Ulcer  Muocosal protective Agents DRUGS PHARMACOKINETIC ACTION USES SIDE EFFECT Sucralfate  It is salt of ( socrose + AL(OH)3 ). 1) In acidic pH, it become  Taken 1 hr befor meal. viscous gell & protect ulcer.  Work in acidic pH 2) Stimulate PG production.  Not used with antacid or H 2 antagonist. Misoprostol It is a PGE1 analogue 1) Gastric acid inhibition. Used with NSAID to  Diarrhoea 2) Stimulate secretion of prevent peptic ulcer  Abdominal pain. mucus & bicarbonate.  Abortion? 3) Enhance mucusal blood flow. Bismuth subsalicylate 1) Coat the ulcer  Stain stools & tongue with black 2) stimulate secretion of color. Bismuth sobcitrate mucus & bicarbonate.  Cause bismuth toxicity with long 3)  PG synthesis. used.  Drugs erdicate Helicobacter pylori DRUGS PHARMACOKINETIC ACTION USES SIDE EFFECT Omeprazole  It is combination of ONE acid suppressant + 2 Or antibiotics. Lansoprazole (PPI)  Given for 14 days. Triple Therapy Clarithromycin  Then, followed by PPI for 4 - 6 wks. Amoxycillin or Metronidazole Omeprazole  It is combination of ONE acid suppressant + 3 Or antibiotics. Lansoprazole (PPI)  Given when triple therapy fails. Quadruple Therapy Bismuth Subsalicylate Metronidazole Tetracycline 10 ‫ـــــألكم الدعاء‬ ‫نس‬