Gastrointestinal drugs .ppt

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    Farmakoterapi

    Pada Gangguang Sistem Pencernaan

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    Classification

    Drugs for treatment of peptic ulcers

    Drugs for adjusting the function of

    digestion

    Drugs promoting gastrointestinal motility

    Antiemetic drugs

    laxatives

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    Drugs for peptic ulcers

    Classification of peptic ulcer:

    Duodenal (DU) Gastric (GU)

    Role of pepsin in peptic ulcer disease:

    Secreted gastric acid plus effects ofpepsin promote tissue injury

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    Peptic ulcer disease: an imbalance between

    aggressive factors (gastric acid pepsin bacteria)

    and protective factors (gastric mucus,bicarbonate, prostaglandins)

    Regulation of gastric acid secretion-- many

    factors (chemical, neural, hormonal)

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    Stimulation:

    Gastrin-most potent stimulant

    Activation of postganglionic

    vagal fibers

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    Drugs for peptic ulcers-----antacids

    Action

    Neutralize secreted acid

    Reduce gastric acidity

    Pepsin inactive

    Reduce destroy factors

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    Drugs for peptic ulcers-----antacids

    A magnesium hydroxide

    B magnesium trislilicate

    C aluminum hydrocide

    D Calcium carbonate F Sodium bicarbonate

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    1 NaHCO3+HCl NaCl+H2O+CO2

    2 AlOH3 aluminium hydroxide

    Al

    OH

    3+3HCl AlCl3 +3H2O 3 MgOH2 magnesium hydroxide

    MgOH2+2HCl MgCl2 +2H2 O

    4 Mg2Si3O8 magnesium trisilicate

    Mg2Si3O8+4HCl 2MgCl2+3SiO2+2H2O

    5 CaCO3 calcium carbonate

    CaCO3+2HCl CaCl2+H2O+CO2

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    Gastric antisecretory drugs

    antagonisit of H2 receptor

    decrease the H+ secretion

    Basal gastric acid

    food-stimulated gastric acid

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    H2 Receptor Antagonists

    A cimetidine +

    B ranitidine ++

    C famotidine +++

    Effective inhibitor of stimulated and non-

    stimulated gastric acid secretion Healing rates: similar between antacids and H2

    receptor antagonists

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    Effective inhibitor of stimulated and

    non-stimulated gastric acid secretion

    Healing rates: similar between

    antacids and H2 receptor

    antagonists

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    Mucosal protective agents

    Prostaglandins

    reduction in basal and stimulated gastric

    acid secretion;

    enhanced mucosa resistance to injury

    (PGE1/PGE2).

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    Mucosal protective agents

    Bismuth compounds

    Mechanism of Action

    cytoprotective effects compounds bind to the ulcer base, stimulating

    mucus and prostaglandin production

    antibacterial effect

    inhibition of proteolytic, lipolytic, and ureaseactivities

    Coating and protecting the ulcer crater

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    Clinical use of Bismuth compounds

    In monotherapy:

    ------- eradicate H. pylori in

    about 20 of patients

    combination with antibiotics

    -------eradicate H. pylori in up to 95%

    of patients.

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    Sucralfate

    binds to ulcer bed (granulation tissue, not to

    gastric or duodenal mucosa)

    decreases proton diffusion to the ulcer base

    may increase endogenous tissue prostaglandins

    and may bind epidermal growth factors andother growth factors-- improving mucosal

    defense

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    antimicrobials

    activity against H.pylori

    clarithromycin, amoxicillin, tetracycline

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    Drugs for adjusting the function of

    digestion

    drugs of aid digestive

    A pepsin

    B pancreatin

    C lactasin

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    antiemetic drugs and drugs promoting

    gastrointestinal motility

    antiemetic drugs:

    H-1 receptor blocker : diphenhydramine

    Chloropromazine

    M-receptor blocker : scopolamine

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    drugs promoting gastrointestinal motility

    Metoclopramide

    domperidone blocking D2-receptor

    Cisapride

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    Metoclopramide

    1) Blocking the DA2 receptor in

    CTZ

    2)

    Blocking the DA2 receptor inGastrointestinal

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    domperidone

    blocking DA2-receptor in

    Gastrointestinal

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    Cisapride

    Increase release of the Ach

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