Cimetidine Raw Materials Powder

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CimetidineRaw Materials Powder Usage and Synthesis.

Cimetidine, marketed in 1975, is the first selective H2 receptor antagonist for the treatment of peptic ulcer. It mainly has the effect of inhibiting the secretion of gastric acid and making it less acidic, and has a preventive and protective effect on corrosive gastritis due to chemical irritation, as well as significant efficacy in stress gastric ulcers and upper gastrointestinal haemorrhage.

Histamine H2 receptor antagonist. It can inhibit gastric acid secretion caused by histamine stimulation and gastric acid secretion induced by food, pentagastrin, caffeine and insulin, etc. It can also inhibit basal gastric acid secretion. It is used for gastric and duodenal ulcers, peptic oesophagitis, and Droe-Ayer syndrome.

Uses and functions of CimetidinePowder.

1. For stomach pain and acidity. This product is good at controlling acid and relieving pain, and also has the function of dispersing the liver, regulating qi and stomach, it is a common medicine for liver-stomach disharmony, excessive acidity, stomach pain, belching and acid swallowing.

2. Used for stomach muscle breakage. This product also has good effect of protecting stomach and removing decay, astringent and muscle growth, used for stomach pain caused by broken stomach muscle, it can not only protect stomach muscle, but also can harmonise the stomach and relieve pain.

3. Used for vomiting blood, blood in stool. This product has the effect of astringency and stopping bleeding, and is suitable for spitting blood and bleeding in stool caused by injury of stomach lining.

Pharmacological Effects of Cimetidine Raw Powder.

Cimetidine is a histamine H2 receptor antagonist, which can reversibly inhibit the action of histamine on H2 receptors. Therefore, it can inhibit the secretion of basic gastric acid and gastric acid caused by various stimuli, and prevent peptic ulcer.

It can enhance cellular immune function, inhibit the activity of suppressor T cells, and have immunostimulatory effect on lymphocytes. It also has anti-androgen effect, can block the binding of dihydrotestosterone and hair follicle receptor, and inhibit the secretion of skin glands. There are also antiviral effects, local anaesthesia and analgesia, and anti-itching effect.

Cimetidine is rapidly absorbed after oral administration, and the blood concentration reaches the peak in 60～90 minutes after administration, with a biological half-life of about 2 hours. The biological half-life is about 2 hours. Taking the drug with meals will significantly delay the peak time and prolong the half-life. Fasting dose of 0.4g, the effective blood concentration can be maintained for more than 4 hours, acid inhibition effect lasts 5-6 hours.

Cimetidine can pass the blood-brain barrier, the concentration in cerebrospinal fluid is about 1/4 of that in blood; it can also pass the placental barrier, and can be secreted into breast milk. 80% of the drug in its original form is excreted through the kidneys within 24 hours. Excretion is reduced in patients with renal insufficiency and the duration of drug action is prolonged. This information was compiled and edited by Squire Yan.

Production method of Cimetidine.

Reaction of intermediate (I) and 2-aminoethyl mercaptan hydrochloride, in the presence of hydrogen bromide, followed by neutralisation with potassium carbonate gave compound (II). This was followed by reaction with the corresponding thiourea to give cimetidine.

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