Pirenzepine

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Pirenzepine

Chemical structure of Pirenzepine

Pirenzepine is a muscarinic receptor antagonist that is primarily used in the treatment of peptic ulcer disease. It is a selective M1 receptor antagonist, which means it preferentially blocks the M1 subtype of muscarinic receptors. This selectivity is beneficial in reducing gastric acid secretion without significantly affecting other systems that are regulated by muscarinic receptors.

Mechanism of Action

Pirenzepine works by inhibiting the action of acetylcholine on the M1 receptors located on parietal cells in the stomach. This inhibition leads to a decrease in the secretion of gastric acid, which is a key factor in the development and exacerbation of peptic ulcers. By reducing acid secretion, pirenzepine helps in the healing of ulcers and provides symptomatic relief.

Clinical Uses

Pirenzepine is primarily used in the management of:

It is not commonly used in the United States but has been used in other countries for its gastric acid-reducing properties.

Side Effects

The side effects of pirenzepine are generally mild due to its selectivity for M1 receptors. However, some patients may experience:

These side effects are typical of anticholinergic agents but are less pronounced with pirenzepine compared to non-selective anticholinergics.

Pharmacokinetics

Pirenzepine is administered orally and is absorbed from the gastrointestinal tract. It undergoes hepatic metabolism and is excreted primarily in the urine. The drug has a relatively long half-life, allowing for less frequent dosing compared to other anticholinergic agents.

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Contributors: Prab R. Tumpati, MD