Definition
A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.
Description
A histamine congener, it competitively inhibits histamine binding to histamine H2 receptors. Cimetidine has a range of pharmacological actions. It inhibits gastric acid secretion, as well as pepsin and gastrins output. It also blocks the activity of cytochrome P-450 which might explain proposals for use in neoadjuvant therapy.
Top Gene Interactions
Related Pathways
General Information
- Metabolism:
Hepatic Route of Elimination: The principal route of excretion of cimetidine is the urine. Half Life: 2 hours
- Uses/Sources:
For the treatment and the management of acid-reflux disorders (GERD), peptic ulcer disease, heartburn, and acid indigestion.
- Symptoms:
Symptoms of overdose include nausea, vomiting, diarrhea, increased saliva production, difficulty breathing, and a fast heartbeat.
- Treatment:
The usual measures to remove unabsorbed material from the gastrointestinal tract, clinical monitoring and supportive therapy should be employed. (L1712)
- Route of Exposure:
Oral, rapid 60-70%
Mechanism of Action
| Target Name | Mechanism of Action | References |
|---|---|---|
|
Multidrug resistance protein 1 Cytochrome P450 2D6 Multidrug and toxin extrusion protein 1 |
16248836 23241029 12699389 |
|
|
Histamine H2 receptor Putative renal organic anion transporter 1 |
Cimetidine binds to an H2-receptor located on the basolateral membrane of the gastric parietal cell, blocking histamine effects. This competitive inhibition results in reduced gastric acid secretion and a reduction in gastric volume and acidity. |
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