Antidiarrhoeals: Adsorbents

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Chapter: Medicinal Chemistry : Antidiarrhoeals

Drugs Acting on Digestive System : Antidiarrhoeals: 1. Diphenoxylate HCl (Lemotil) 2. Loperamide - Synthesis and Drug Profile


Drugs Acting on Digestive System

Antidiarrhoeals

Adsorbents

These substances have the power of adsorbing gases, bacteria, and toxins without undergoing any chemical reaction. They also posses the protective property apart from their adsorbent action. They form a coating over the intestinal mucosa to reduce its irritation, example of this category are kaolin, calcium carbonate, magnesium trisilicate, and aluminium hydroxide, pectin, bismuth subsalicylate and polycarbophill and various psyllium seed derivatives.

 

1. Diphenoxylate HCl (Lemotil)


Synthesis


Properties and uses: It is a weak meperidine congener lacking analgesic activity. It is used for the symptomatic activity of diarrhoea in patients with mild chronic inflammatory bowel disease and for infectious gastroenteritis.

Dose: The usual adult dose orally is 5 mg four times a day.

 

2. Loperamide


Properties and uses: It is a synthetic meperidine congener devoid of sedative or respiratory depressant actions. It is orally used as an antidiarrhoeal agent. Loperamide exerts spasmolytic effect on the gastrointestinal tract (GIT) muscle by depressing slow cholinergic phase and rapid prostaglandin mediated phase of smooth muscle contraction. It may act on the intestinal nerve endings or on the ganglia.

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