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Pirenzepine | CAS No: 28797-61-7 | GMP-certified suppliers
A medication that treats peptic, gastric, and duodenal ulcers by reducing gastric acid secretion and supporting ulcer healing with a well-tolerated antimuscarinic profile.
Therapeutic categories
Primary indications
- For the treatment of peptic ulcer, gastric ulcer, and duodenal ulcer
Product Snapshot
- Pirenzepine is formulated as oral tablets and capsules
- It is indicated for the treatment of peptic, gastric, and duodenal ulcers
- The product is approved in the Canadian market
Clinical Overview
Pharmacologically, pirenzepine acts as a muscarinic acetylcholine receptor antagonist, binding specifically to these receptors to modulate downstream cellular signaling. The muscarinic receptor mediates inhibition of adenylate cyclase, phosphoinositide hydrolysis, and potassium channel activity through G-protein-coupled mechanisms. By blocking muscarinic receptors in gastric parietal cells, pirenzepine reduces acid secretion, which aids in ulcer healing and contributes to its cytoprotective effects. Additionally, pirenzepine enhances the therapeutic efficacy of other antiulcer agents, such as cimetidine and ranitidine, through pharmacodynamic potentiation.
The compound belongs structurally to the class of 1,4-benzodiazepines, characterized by a benzene ring fused to a 1,4-azepine ring. Pirenzepine’s therapeutic profile extends to antispasmodic effects, helping alleviate gastrointestinal cramps and spasms, and it may be co-administered with antacids or other medications targeting acid-related disorders. It is also sometimes used in the prevention of nausea, vomiting, and motion sickness, although its principal approved indication remains ulcer treatment.
Key ADME parameters indicate selective action with minimal impact on non-gastrointestinal parasympathetic functions at therapeutic doses. Pirenzepine is generally well tolerated, with a safety profile that reflects its receptor selectivity. However, as with other anticholinergics, potential side effects may include dry mouth, tachycardia, and blurred vision.
For formulation scientists and sourcing specialists, pirenzepine’s API quality should be verified against pharmacopeial standards for purity, residual solvents, and polymorphic form due to its influence on bioavailability and stability. Reliable suppliers should provide comprehensive documentation, including certificates of analysis and evidence of Good Manufacturing Practice (GMP) compliance, to ensure consistent API quality for use in anti-ulcer formulations.
Identification & chemistry
| Generic name | Pirenzepine |
|---|---|
| Molecule type | Small molecule |
| CAS | 28797-61-7 |
| UNII | 3G0285N20N |
| DrugBank ID | DB00670 |
Pharmacology
| Summary | Pirenzepine is a muscarinic acetylcholine receptor antagonist with selectivity for the M1 subtype. It modulates gastrointestinal motility and acid secretion by inhibiting receptor-mediated signaling pathways involving G proteins. This mechanism underlies its use in managing peptic and gastric ulcers through antispasmodic and antisecretory effects. |
|---|---|
| Mechanism of action | Pirenzepine is a muscarinic receptor antagonist and binds to the muscarinic acetylcholine receptor. The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. |
| Pharmacodynamics | Pirenzepine belongs to a group of medications called antispasmodics/anticholinergics. These medications are used to relieve cramps or spasms of the stomach, intestines, and bladder. Pirenzepine is used to treat duodenal or stomach ulcers or intestine problems. It can be used together with antacids or other medicine in the treatment of peptic ulcer. It may also be used to prevent nausea, vomiting, and motion sickness. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Muscarinic acetylcholine receptor M1 | Humans | antagonist |
Formulation & handling
- Pirenzepine is a small molecule suitable for oral administration in tablet and capsule forms.
- Formulation should consider its moderate water solubility and lipophilicity (LogP 0.97) for bioavailability optimization.
- Administering on an empty stomach is necessary to avoid food interactions and enhance absorption.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) is marketed in Canada with patent protection recently expired, allowing for generic entry and increased market competition. The product is currently in a mature phase with established clinical use. |
|---|
| Markets | Canada |
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Supply Chain
| Supply chain summary | Pirenzepine is marketed in Canada with branded products such as Gastrozepin tablets available at a 50 mg dosage. The presence of branded formulations indicates established originator companies, though the limited market data suggests a regional focus rather than broad global distribution. Given the availability of branded products and lack of recent patent data, generic competition may already exist or emerge, reflecting typical post-patent market dynamics. |
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Pirenzepine is a type of Anticholinergics/Parasympathemimetics
Anticholinergics/Parasympathomimetics are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) widely used in the medical field. These compounds exhibit specific pharmacological actions by targeting the cholinergic system in the body.
Anticholinergics are drugs that block the action of acetylcholine, a neurotransmitter that regulates various bodily functions. By inhibiting the activity of acetylcholine, anticholinergics can have diverse therapeutic effects, including reducing muscle spasms, decreasing gastrointestinal motility, and alleviating symptoms associated with certain respiratory conditions.
On the other hand, parasympathomimetics, also known as cholinomimetics, mimic the action of acetylcholine by stimulating cholinergic receptors. These compounds enhance the parasympathetic nervous system, which is responsible for the "rest and digest" functions of the body. Parasympathomimetics are commonly used to treat conditions such as glaucoma, urinary retention, and Alzheimer's disease.
The use of anticholinergics/parasympathomimetics requires careful consideration and medical supervision due to their potential side effects, which can include dry mouth, blurred vision, urinary retention, constipation, and cognitive impairment. These medications are available in various forms, including tablets, capsules, patches, and inhalers, and their dosage is determined by the specific medical condition being treated.
Overall, anticholinergics/parasympathomimetics play a vital role in modern medicine, providing targeted therapeutic effects by modulating the cholinergic system. Their usage has significantly improved patient outcomes in various medical conditions and continues to be an important category of pharmaceutical APIs.
Pirenzepine (Anticholinergics/Parasympathemimetics), classified under Autonomic Nervous System Agents
Autonomic Nervous System Agents are a crucial category of pharmaceutical active ingredients (APIs) that target the autonomic nervous system (ANS). The ANS plays a vital role in regulating essential bodily functions such as heart rate, blood pressure, digestion, and respiratory rate. This category of pharmaceutical APIs encompasses a wide range of drugs designed to modulate the activity of the ANS.
One subcategory within Autonomic Nervous System Agents is the Sympathomimetic agents, which mimic the effects of the sympathetic nervous system. These drugs are often used to treat conditions such as asthma, nasal congestion, and hypotension by stimulating specific adrenergic receptors.
Conversely, Sympatholytic agents act to inhibit or block the sympathetic nervous system. They are employed to treat hypertension, anxiety, and certain cardiac conditions by reducing sympathetic activity.
Another subcategory is Parasympathomimetic agents, which mimic the effects of the parasympathetic nervous system. These drugs are commonly used to treat glaucoma, urinary retention, and certain gastrointestinal disorders by stimulating cholinergic receptors.
Parasympatholytic agents, on the other hand, act to block the parasympathetic nervous system. They find applications in the treatment of conditions such as overactive bladder and irritable bowel syndrome by inhibiting cholinergic receptors.
The Autonomic Nervous System Agents API category includes various drugs with distinct mechanisms of action that enable healthcare professionals to fine-tune the balance of the autonomic nervous system. By targeting specific receptors and pathways, these pharmaceutical APIs provide valuable therapeutic options for managing a wide range of medical conditions related to autonomic dysfunction.
Pirenzepine API manufacturers & distributors
Compare qualified Pirenzepine API suppliers worldwide. We currently have 3 companies offering Pirenzepine API, with manufacturing taking place in 3 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| AGC Pharma Chemicals | Distributor | Spain | Spain | BSE/TSE, CoA, GMP, MSDS | 4 products |
| Euticals | Producer | Italy | Unknown | CoA, USDMF | 48 products |
| LGM Pharma | Distributor | United States | World | CEP, USDMF | 441 products |
When sending a request, specify which Pirenzepine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Pirenzepine API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
