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    Antiulcer Drugs ANDC

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    jutttoxic

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    Antiulcer Drugs ANDC

    Uploaded by

    jutttoxic
    5 views25 pages

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    © © All Rights Reserved

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    Copyright:

    © All Rights Reserved
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    Download as pptx, pdf, or txt
    5 views25 pages

    Antiulcer Drugs ANDC

    Uploaded by

    jutttoxic

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    of 25

    Drugs for acid-peptic disease

    Symptoms of acid peptic disease

    • Indigestion/Heartburn
    • Epigastric pain
    • Nausea
    • Mouth ulcers
    • Anorexia, loss of appetite
    • Weight loss
    Learning
    Objectives
    • Classify drugs used for the treatment of acid peptic
    disease

    • Summerize the role of Proton pump inhibitor, H2


    receptor antagonist, antacid, misoprostol & antibiotics
    in acid peptic disease

    • Enumerate major adverse effects of these drugs

    .
    Acid-peptic disease includes

     Gastroesophageal reflux disease


    (GERD)

     Peptic ulcer
    Gastric ulcer
    Deudenal ulcer
     Stress ulcers.
    What is stress ulcer?
    • Stress ulcers are multiple, superficial
    erosions which occur mainly in the fundus
    and body of the stomach. They develop due
    to decrease perfusion after shock, sepsis,
    and trauma and are often found in patients
    with chronic medical illness.
    Gastric
    Glands
    • Secrete gastric juice:
    • Goblet cells: mucus.
    • Parietal cells: HCl and intrinsic factor.
    • Chief cells: pepsinogen.
    • Enterochromaffin-like cells (ECL):
    histamine , serotonin.
    • G cells: gastrin.
    Causes of gastric ulcer
    formation
    • Imbalance between mucosal defense mechanisms
    and acid producing mechanism
    • Stress
    • H-Pylori bacteria
    • Drugs; NSAIDS, Steroids
    TREATMENT GOAL

     Relieve ulcer pain.

     Promote healing.

    HOW?

     Reducing secretion of Gastric acid or neutralizing it.

     Providing agent that protect Gastric mucosa

     Eradicating H-Pylori.
    Classification
    Drugs that reduce Drugs that improve
    intragastric acidity mucosal defense
    • H2 receptor blockers,
    •Cimetidine…Ranitidine…Famotidine •Sucralfate
    •Antacids… •Misoprostol
    •Aluminum hydroxide, Magnesium
    hydroxide,Calcium carbonate(CaCo3),
    …Sodium bicarbonate(NaHCO3)

    •Proton pump inhibitors


    (PPI's)
    •Omeprazole…Esoperazole…
    Pantoperazole
    H2 Blockers
    Cimetidine,Ranitidne,Famotidine
    • Adverse Effects:
    • MOA: • Cimetidine:
    • Competitive inhibition of histamine at
    H2 receptors at gastric parietal • Cimetidine (Antiandrogen)
    cells,subsequently inhibit gastric acid
    secretion • Menstrual irregularities
    • Hirsuitism
    • Inhibit basal,food stimulated and
    nocturnal secretion of gastric acid. • Gynecomastia
    • Clinical Uses: • Oligospermia
    • Gastroesophageal reflux • Inhibit CYP-450
    disease(GERD)
    • Peptic ulcer disease
    • Drug interactions with
    Warfarin,Phenytoin,theop
    • Non-ulcer dyspepsia
    hyline
    • Prevention of bleeding from stress
    ulcers
    Proton Pump Inhibitors
    Omeprazole,Lanzoprazole,Esomeprazole,Pantoperazole
    • USES:
    • Erosive esophagitis
    • MOA: • Active duodenal ulcer
    • Prodrugs • Zollinger-Ellison Syndrome (gastrin
    • Enteric coated formulations producing tumor)
    • Weak base ----- accumulate • NSAID induced gastric ulcer e,g
    in canaliculi of parietal cell ------ Aspirin
    converted into active drug and • Part of Regimen to eradicate
    forms a stable covalent bond with H.Pylori. Triple therapy
    H/K ATPase enzyme
    • It takes about 18 hours for • Adverse Effects:
    enzyme to resynthesize and acid • Atrophy of gastric mucosa.
    secretion is inhibited during this • B12 deficiency
    time.
    • Increased risk of fractures due to
    • Omeprazole + sodium
    bicarbonate has fast absorption calcium malabsorption
    in case of high acid levels and • Diarrhea, colitis
    gastric ulcerations • Hypo-magnesemia
    • Should be taken empty
    stomach ,before meals.
    TRIPLE Therapy for H.Pylori
    eradication
    1. PPIs: Omeprazole, 40mg +
    2. Clarithromycin...500mgx BD +
    3. Amoxicillin...1gm x BD
    OR
    Metronidazole 500mg x BD If allergy to
    penicillin
    These drugs are given for 14 days(2 Weeks)
    Sucralfate
    MOA:
    • Adverse Effects:
    • Complex of aluminium • It binds with other drugs and interfere
    hydroxide and sulphated with their absorption
    sucrose • PRECAUTION :
    • In acidic environment of • Sucralfate should not
    stomach sucralfate binds to be administered with
    the positively charged
    proteins of necrotic mucosa H2-antagonist or
    and create a physical barrier antacid
    that protects the ulcer
    • It does not heal but buys time
    healing of gastric ulcer. WHY?
    MISOPROSTOL
    • MECHANISM OF ACTION: • ADVERSE
    EFFECTS:
    • Prostaglandin analogue
    • Intestinal cramps, Pain
    • Increases mucosal blood abdomen
    flow,bicarbonate and mucus • Abortion and uterine bleeding in
    secretions and protect gastric pregnancy
    mucosa • Contraindicated in pregnancy

    • CLINICAL USES:

    • Prevention of NSAIDs
    induced ulcers
    Antacids
    MECHANISM OF ACTION: • ADVERSE EFFECTS:
    • Abdominal distension,belching
    • Promote healing of ulcer • Milk alkali syndrome with calcium
    • Alkaline substances, Neutralize salts
    acid • Milk-Alkali Syndrome:
    • React with HCL in the stomach. ...... Headache, weakness,
    Produce neutral, less acidic, or anorexia, constipation,nausea,
    poorly absorbed salts vomiting,abdominal pain and
    polyuria.
    • Should be taken just after meals for
    • Impair absorption of other drugs by
    maximum effectiveness
    binding to them; tetracyclines
    • Acid base imbalance with sodium
    • Clinical uses containing antacids
    • Hyperacidity including GERD • Aluminium antacids cause
    • Indigestion constipation
    • Magnesium antacids cause diarrhea
    • MgOH + HCl -------- MgCl + H2O
    (stomach)

    • ALOH3 + HCl ----------- AlCl +H2O


    (stomach)

    • CaCO3 + 2HCl ------------ CaCl2 +CO2 + H2O

    • NaHCO3 +HCl ------------- NaCl+ CO2 +H2O


    Assignment

    • Describe MOA & enlist adverse effects of misoprostol?

    • Describe MOA & enlist adverse effects of cimetidine?

    • Describe mechanism of action of Proton pump inhibitors & enlist


    adverse effects of PPI’s?

    • Describe Triple therapy for H-Pylori eradication?


    Drug MOA USES A/E
    ANTACIDS: Neutralize gastric acid Heartburn,dyspeps Mg-antacids-diarrhea
    Al,Mg,Ca,Na salts into salts ia,indigestion,GERD Al-Antacids-Constipation
    Ca and Na antacids- acid base disterbance

    H2 BLOCKERS: Block histamine H2 GERD,Acid peptic Cimetidine causes androgenic adverse


    Cimetidine,Ranitidin receptors and acid disease,Gastric effects,gynecomastia & oligospermia in
    e production ulcer males,hirsuitism,menstrual irregularities in
    females, inhibit CYP-450 and causes drug
    interactions with
    warfarin,phenytoin,theophylline.

    Proton pump Block H/K ATPase pump GERD,Acid peptic Atrophy of gastric mucosa,Acid rebound
    Inhibitors: and acid production in disease,Gastric phenomenon,B12 deficiency
    Omeprazole,lanzopr parietal cells ulcer,Zollinger megaloblastic anemia,Increased risk of
    azole Ellison syndrome, fractures due to calcium malabsorption,
    H-Pylori
    eradication therapy Diarrhea, colitis, Hypo-magnesemia

    Sucralfate In the presence of gastric Gastric ulcer Not effective in combination with acid
    acid it binds with inhibitors.
    positively charged Must be a gap of 2 hours between acid
    proteins of necrotic inhibiting drugs
    mucosa and forms a
    viscous paste which coats
    ulcers.
    Drug MOA USES A/E
    Misoprostol Prostaglandin E1 NSAID Induced Abortion,Heavy
    analogue gastric ulcer uterine
    Increases mucosal Off label use to bleeding,contraindica
    blood flow,mucus induce abortion ted in pregnancy
    production
    Protects gastric
    mucosa

    TRIPLE THERAPY-H-PYLORI ERADICATION

    PPI: Omeprazole Clarithromycin Amoxacillin 1g For 14 days


    40mg OD 500mg BD BD OR
    Metronidazole
    400mg BD

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