Gastrointestinal Agents Pharmaceutical Chemistry.pptx

Gastro intestinal agents definition, drugs, important topic for D pharmacy pharmaceutical chemistry

1. 10/17/2016 2:07:42 PM 1 GASTROINTESTINAL AGENTS

2. GIT Agents Acidifying Agents Antacids Protective & Adsorbents Saline Cathratics 10/17/2016 2:07:42 PM 2 GASTROINTESTINAL AGENTS Def: The agents which are used to treat gastrointestinal disorders are called gastrointestinal agents.

3. 1. Acidifying Agents: e.g. Dilute Hydrochloric Acid Glutamic Acid 2. Antacid : E.G.: = Calcium Carbonate = Magnesium Carbonate = Sodium Bicarbonate = Magnesium Hydroxide = Aluminum Hydroxide Gel 10/17/2016 2:07:42 PM 3

4. 3. Protectives & Adsorbent Eg .: Bismuth Subcarbonate Bismuth Subgallate Kaoline Milk Of Bismuth 4. Saline Cathratics E.G. Magnesium Sulphate Sodium Potassium Tartrate . 10/17/2016 2:07:42 PM 4

5. Def: The substances which increase the acidity in stomach are called acidifying agents. Role of HCl : Kills the micro-organism in ingested food and drinks. Softens the ingested food materials 1. Acidifying agents 10/17/2016 2:07:42 PM 5

6. Definition: When the secretion of gastric acid is totally absent, the condition is called Achlorhydria . Two Groups Those who remain free of gastric hydrochloric acid after stimulation with histamine. Those in whom there is normally a lack of gastric HCL but who respond to stimulation by histamine. Symptoms : Abdominal pains, loss of appetite, mild diarrhea, Confusion . ACHLORHYDRIA 10/17/2016 2:07:42 PM 6

7. Mechanism of Action : These substances increase the acidity in stomach by one of the following mechanisms: They increase acidic concentration due to acidic nature. They increase the acidity in stomach by stimulating the secretary cells of GIT. Promote formation of proteolytic enzyme pepsin. 1. Acidifying agents 10/17/2016 2:07:42 PM 7

8. Standard: It contains 10% w/w of HCl . Properties: It is a clear, colourless , tasteless, odourless liquid. It is miscible with water and organic solvents. Acidic to litmus. Reacts with iron to change its colour . Storage: It is stored in well closed, insert glass container below 30°C. Uses: As an acidifying agent. In achlorhydria and hypochlorhydria . In anemia with iron therapy. 1. Dil. Hydrochloric Acid 10/17/2016 2:07:42 PM 8

9. 1. Dil. Hydrochloric Acid Chemical Properties: It turns moist blue litmus to red Hydrochloric acid gas forms dense white fumes of ammonium chloride with ammonia. HCl + NH 3 NH 4 Cl HCl decomposes salts of weaker acids such as carbonates, bicarbonates, sulphides , etc. NaHCO 3 + HCl NaCl + CO 2 + H 2 O It react with metals & their salts to form chlorides of metals. 10/17/2016 2:07:42 PM 9

10. Def: Antacids are t he compounds used to neutralize excess of gastric hydrochloric acid in stomach. Antacids used, when 1) uncomfortable feeling 2) Heartburn, Abdominal pain 3)A growing hungry feeling between meals Therapy: These are alkaline (basic) comp. used to neutralize the excess gastric hydrochloric acid associated with gastritis & peptic ulcers. 2. Antacids 10/17/2016 2:07:42 PM 10

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12. I deal Properties of Antacid : It should neutralize excessive acidity. It should not interfere with digestion. It should be exert its effect rapidly & over a long period of time. It should be buffer in the pH 4-6 range. It should probably inhibit pepsin. It should be stable, nontoxic and nonirritant . It should not cause constipation or act as laxative . It should be insoluble in water. It should not be absorbed through GIT. It should not cause systemic alkalosis . 10/17/2016 2:07:42 PM 12

13. Combination of antacid preparations: There is no single antacid which is ideal. Single antacids produces side effects. Therefore, combinations of antacids are used which reduce side effects and give more benefits. 10/17/2016 2:07:42 PM 13

14. Most of the antacids commonly used today raise the gastric pH to 4-5, which greatly reduces pepsin’s proteolytic action, the result is that an excess of acid is secreted into the stomach, leading to possible hyperacidity Systemic alkalosis due to antacid Sodium content of antacid. Local effect in GI tract (laxative & Constipation Effect) Which Side effects Produced by Antacid when given alone 10/17/2016 2:07:42 PM 14

15. Sodium bicarbonate - Systemic alkalosis . Sodium containing antacids - Hypertension. Magnesium compounds - contraindicated in patients with renal disorders. Calcium compounds : are contraindicated in patients suffering from renal and cardiac disorders . Aluminum and calcium compounds : produce constipation. 10/17/2016 2:07:42 PM 15

16. Combination of antacid is used because: Combination reduces constipation effect of antacids. Combination reduces laxative action. Some combinations produce specific action and are used for specific purpose . Combination also reduces the dose of drug required to produce action. Examples : [AC CM MA] Aluminium hydroxide gel + Calcium Carbonate Calcium Carbonate + Magnesium trisilicate. Magnesium trisilicate + Aluminium hydroxide.   10/17/2016 2:07:42 PM 16

17. Combination antacid preparation Aluminium hydroxide- magnesium carbonate co-dried gel Aluminium hydroxide gel-magnesium trisilicate combinations Algicon tablet: Chewable tablets prepared by Aluminium hydroxide-magnesium carbonate co-dried gel (360 mg), Magnesium alginate (250 mg), magnesium carbonate (320 mg) & potassium Bicarbonate (100 mg) Magaldrate : combination of Aluminium hydroxide & magnesium hydroxide. Alginic acid sodium bicarbonate- containing antacid mixtures. 10/17/2016 2:07:42 PM 17

18. 1. Sodium bicarbonate (NaHCO 3 ) Synonym: Baking soda, Mitha soda Sodium hydrogen carbonate Standard: 99 to 100.5% w/w of NaHCO 3 Properties: Colour ; White crystalline powder, Odour : odourless , Taste: saline taste. Solubility: Soluble in water and insoluble in alcohol. Aqueous solution is alkaline. On heating produces CO 2 10/17/2016 2:07:42 PM 18

19. Chemical Reactions o f Sod. Bicarbonate When it is heated in a dry state, it decomposes giving Sod. carbonate, CO 2 & water 2NaHCO 3 Na 2 CO 3 + H 2 O + CO 2 Sod. Bicarbonate is reacted with acids, salts formed & CO 2 is liberated NaHCO 3 + HCl NaCl + H 2 O + CO 2 10/17/2016 2:07:42 PM 19

20. Storage: store in well closed, air tight containers. Incompatibility: with acid, acid salts, aspirin etc. Uses As an antacid, As a carminative ( prevent formation of gas) . In treatment of renal acidosis, crystaluria . In treatment of systemic acidosis. In poisoning cases . Used in spray sol In irrigation of eyes. 3.5% sol as a eye lotion, 5% as ear drops In effervescent powders and bath soaps . 10/17/2016 2:07:42 PM 20

21. 2. Aluminium Hydroxide Gel: Al(OH) 3 Aluminium Hydroxide gel is aq. suspension of hydrated , aluminium oxide together with varying quantities of basic aluminium carbonate . Properties: White , Viscous suspension , translucent in thin layers , small amounts of clear liquid may separate on standing . It is Odourless & tasteless Practically insoluble in water & alcohol Storage: Store in air tight container & avoid freezing. Incompatibility : it interferes with or reduces the absorption of no. of drugs like barbituretes , quinine, tetracyclines & Vitamins. Uses: Used as Antacids Mild Astringent & demulcent ( forms a soothing film over a mucous membrane, relieving minor pain and inflammation of the membrane .) used in peptic ulcer and hyperchlorhydria . 10/17/2016 2:07:42 PM 21

22. 3. Calcium carbonate CaCO3: Mol. Wt: 100 It s found in nature as limestone, marble, aragonite, calcite, dolomite & shells of sea animals . Properties: It is white, odourless , tasteless microcrystalline powder. It is practically insoluble in water. It produces constipation effect so it is given with magnesium antacid. It is rapid acting & non systemic antacid Storage: S tore in well closed, air tight containers. Incompatibility: with tetracycline. Uses As antacids As a calcium supplement, as a polishing agent in tooth powders, as a chalk As a food additive & in homeopathic medicine Used in dentifrices, insecticides, cosmetics, antibiotics & diarrhoea . 10/17/2016 2:07:42 PM 22

23. 4. Aluminium Phosphate (A l PO 4) Properties: It is aq . suspension of aluminium orthophosphate. It is white, viscous suspension. It contains peppermint oil 0.01% as flavouring agent & saccharin sodium as a sweetening agent It is a non absorbable antacid. Storage : store in air tight containers at a temp. not exceeding 30° C & avoid freezing. Uses: It is used as a slow acting antacid It is also used as adjuvant in adsorbed vaccines. 10/17/2016 2:07:42 PM 23

24. 5. Magnesium Carbonate (MgCO 3 ) Properties: It is white, odourless, tasteless, powder It is practically insoluble in water & alcohol It occurs in the form of light & heavy variety. Storage: store in air tight containers Incompatibility: with tetracycline. Uses: used as a weak antacid & mild laxative. Heavy Mg. carbonate Used in powders & Tablets. Light Mg. carbonate used in mixtures & dispersing volatile oil in inhalations 10/17/2016 2:07:42 PM 24

25. 6. Magnesium Trisilicate (2MgO.3SiO 2 ) Properties: It contains 29 to 32% MgO & 65 to 68.5% SiO 2 It is a white, odourless, tasteless fine powder free from grittiness It is slightly hygroscopic in nature It is practically insoluble in water & alcohol. Storage: S tore in air tight containers Uses: Used as mild antacid Also used as adsorbent & protective agent Also used in gastric & duodenal ulcers. 10/17/2016 2:07:42 PM 25

26. 7. Magnesium Oxide ( MgO ) Properties: It is white odourless powder, with slight alkaline taste It is practically insoluble in water & alcohol. It reacts with acid to form Mg. hydroxide. Storage: Store in air tight containers. Uses: It is used as potent antacid & mild laxative. Light MgO used in dentifrices. Heavy MgO used in powders & Tablets. 10/17/2016 2:07:42 PM 26

27. Protective's: These are the substances which protect the GIT surfaces from harmful stimuli, e.g. kaolin, bismuth carbonate. It should be water insoluble, chemically inert. Adsorbents: The substances which are used to adsorb the gases, toxins and bacteria are called adsorbents, e.g. kaolin, activated charcoal. It should be fine powder. Protective's & Adsorbent 10/17/2016 2:07:42 PM 27

28. Mechanism of action These substances are water insoluble and also insoluble in dilute HCl, alkali. These substances form a protective layer on innermost wall of GIT. Therefore, contact of bacterial toxins is prevented. Thus, stimulation of peristalsis by bacteria is prevented and they are used in diarrhea. Adsorbents have a property to adsorb the bacterial toxins and also gases thus prevent attack of toxins on GIT. Frequent elimination of watery stools in diarrhea can be prevented by protective adsorbents. Examples Bismuth sub carbonate, kaolin, activated charcoal. 10/17/2016 2:07:42 PM 28

29. Application of Protective's and Adsorbents They are useful in the treatment of diarrhea. They are useful in poisoning cases to adsorb the poison. They prevent GIT irritation . They prevent entry of microbes in the body by forming protective layer, over the surfaces of the body. Bismuth Compounds used as Protective's: Bismuth sub carbonate. Bismuth subgallate . Kaoline Milk of bismuth. 10/17/2016 2:07:42 PM 29

30. Bismuth Subcarbonate {( BiO ) 2 CO 3 } H 2 O Synonym: Bismuth Oxycarbonate , Bismuth Carbonate It contains equivalent of 80 to 82.5% of bismuth. Properties: White or creamy white powder. odourless , tasteless Insoluble in water and alcohol. Dissolves completely in HNO3. Affected by light but stable in air. 10/17/2016 2:07:42 PM 30

31. Bismuth Subcarbonate Storage: Store in well closed air tight & light resistant container. Uses: It is used as protective & adsorbent. Used as antidiarrhoeal. Mild antiseptic and astringent. In treatment of gastric and duodenal ulcers. As a mild antacid. Used in cosmetics (lotions and face Powder). 10/17/2016 2:07:42 PM 31

32. 2 . Kaolin Synonym: China clay, hydrated aluminium silicate Al 2 O 3 . 2SiO 2 ,2H 2 O Properties: White odorless, tasteless powder. Insoluble in water, dilute alkali and acids. It is free from gritty particles, unctuous & soapy to touch. Available in two forms- heavy and light kaolin. Impure forms of kaolin contain gritty particles. 10/17/2016 2:07:42 PM 32

33. Storage: It is stored in well closed air tight containers. Incompatibility: I t absorbs certain vitamins, enzymes, alkaloids & minerals leading failure of medication. Uses: In treatment of dysentery and diarrhea. In treatment of alkaloid poisoning. Used as adsorbent. In food-poisoning cases. In dusting powders & in cosmetic preparations. As a main ingredient of kaolin poultice. 10/17/2016 2:07:42 PM 33

34. 4. SALINE CATHARTICS (Osmotic Laxatives, Hydrophilic Cathartics, Purgatives) These are the agents that fasten and stimulate or facilitate evacuation of the bowels. Laxatives are mild cathartics that are used for short term therapy. Laxatives may be used for evacuation bowel, which are of Four types: Stimulant Laxative Bulk forming Laxative Emollient Laxative Saline Laxative 10/17/2016 2:07:42 PM 34

35. C onstipation In this condition fecal material becomes dry & hard due to ignoring the evacuation from bowels. Difficult evacuation of the feces is known as constipation. Causes: Weakness of intestine. Intestinal spasm. Injury or use of certain drugs & diet. Treatment: Laxatives, Cathartics 10/17/2016 2:07:42 PM 35

36. Types of Laxatives Stimulant Laxatives They act by local irritation on the intestinal tract which increases peristaltic activity. MOA: they act by local irritation on the intestinal tract, which stimulate peristaltic activity. 2. Bulk forming Laxatives : Bulk forming laxatives are the agents which increases bulk of intestinal content. MOA: these are made up of cellulose & other non-digestive polysaccharides. They swell when wet, with the increased bulk stimulation peristalsis. 10/17/2016 2:07:42 PM 36

37. 3. Emollient Laxatives : Emollient laxatives acts either as lubricant or as stool softner . MOA: they act either as lubricants facilitating the passage of compacted fecal material or as stool softeners. 4. Saline Laxatives: They acts by increasing the osmotic load of intestine by absorbing large quantity of water. MOA: They act by increasing the osmotic load of the GIT They are poorly absorbable anions & sometimes cations . The body relives the hyper-tonicity of the gut by secreting additional fluids into intestinal tract, it result in to increased bulk stimulates peristalsis. 10/17/2016 2:07:42 PM 37

38. 1. sodium Potassium tartrate C 4 H 4 KNaO 6 ;4H 2 O; 282.23 Rochelle salt, seignette’s salt Properties: It is colourless or white crystalline powder Cooling, saline in taste. Freely soluble in water & practically insoluble in alcohol . Uses: Used as saline cathartic As additive in food industry,where it acts as sequestrant , emulsifier, stabilizer, buffer and antioxidant in cheese products, margarine, jellies, jams, minced meat, and sausage casings. As a antidote in some cases. 10/17/2016 2:07:42 PM 38

39. 2. Magnesium Sulphate (M g so 4 .7h 2 o) Epsons Salt Properties: It is colourless, odourless needle like crystalline powder. With a cooling, saline bitter taste. It is freely soluble in water. Storage: Store in cool place in well closed air tight containers. Incompatibility: with sod. & pot. Tartrate, alkali carbonate. Uses: Used as saline cathartics. Used parenterally as an anticonvulsant. Used orally as antidote for heavy metal poisoning Used as cholagogue .   (a medicinal agent which promotes the discharge of bile from the system) 10/17/2016 2:07:42 PM 39

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