Nizatidine is a synthetic histamine H2-receptor antagonist (H2 blocker) used as an active pharmaceutical ingredient in medicines for acid-related gastrointestinal disorders. It works by reducing gastric acid secretion through selective antagonism of histamine H2 receptors on gastric parietal cells.
Nizatidine is chemically classified as a substituted thiazole-containing nitroethenediamine and is structurally related to other H2-receptor antagonists such as ranitidine and famotidine. PubChem identifies Nizatidine as a histamine H2-receptor antagonist used for the treatment of acid-peptic disease.
Nizatidine is a specialized gastrointestinal pharmaceutical API used in formulation development, pharmaceutical manufacturing, analytical research and quality-control applications.
Important quality attributes for pharmaceutical-grade Nizatidine include:
The USP-NF monograph provides a defined assay range for Nizatidine, making the pharmacopoeial numerical value preferable to a generic assumed API purity range.
Product Name: Nizatidine
Synonyms: Nizatidinum; Nizatidina; N-[2-[[[2-[(Dimethylamino)methyl]-4-thiazolyl]methyl]thio]ethyl]-N′-methyl-2-nitro-1,1-ethenediamine
CAS Number: 76963-41-2
Molecular Formula: C12H21N5O2S2
Molecular Weight: 331.46 g/mol
IUPAC Name: (E)-1-N-[2-[[2-[(dimethylamino)methyl]-1,3-thiazol-4-yl]methylsulfanyl]ethyl]-1-N-methyl-2-nitroethene-1,1-diamine
Drug Class: Histamine H2-Receptor Antagonist
Therapeutic Class: Antiulcer / Acid-Suppressing Agent
Therapeutic Area: Gastroenterology
Molecule Type: Synthetic Small Molecule
PubChem lists Nizatidine under CAS 76963-41-2, with molecular formula C12H21N5O2S2 and molecular weight approximately 331.5 g/mol. The USP monograph reports the molecular weight as 331.46.
Nizatidine selectively blocks histamine H2 receptors located on gastric parietal cells.
Its pharmacological action results in:
Nizatidine is classified by FDA-related substance information as a histamine type-2 receptor antagonist.
Nizatidine API is relevant to:
Nizatidine has been used in the management of duodenal ulcers and other acid-related gastrointestinal conditions. Its pharmacological action is based on suppression of gastric acid secretion.
Because the regulatory status and approved indications of medicines can vary by market, formulation claims should be aligned with the applicable national regulatory authorization.
Nizatidine is a synthetic sulfur- and nitrogen-containing organic pharmaceutical compound. Its molecular structure incorporates:
PubChem reports a calculated topological polar surface area of 140 Ų, hydrogen-bond donor count of 2, and hydrogen-bond acceptor count of 8. These are calculated molecular descriptors rather than API release specifications.
Nizatidine has appreciable solubility characteristics compared with many highly lipophilic drug substances, but quantitative solubility varies with pH, solvent, temperature and experimental methodology.
For an API CMS, a numerical solubility value should only be entered when supported by the applicable pharmacopoeial or validated technical specification.
A controlled Nizatidine API manufacturing process may involve:
The exact commercial synthesis route should be based on the manufacturer's validated manufacturing process and regulatory documentation.
Typical pharmaceutical-grade Nizatidine testing may include:
The USP-NF monograph establishes a specific assay requirement for Nizatidine and therefore provides a stronger basis for CMS specifications than an arbitrary generic API range.
The USP-NF monograph specifies:
Nizatidine: 98.0%–101.0%, calculated on the dried basis.
This is the appropriate numerical assay value to use when representing the API against the cited USP-NF specification.
Nizatidine related-substance control is important because the molecule can generate process-related and degradation impurities.
Known Nizatidine-related substances include N-desmethylnizatidine and Nizatidine N2-oxide. PubChem identifies N-desmethylnizatidine as a metabolite and separately records Nizatidine N2-oxide as a chemically related substance.
For the CMS, individual and total impurity limits should be taken from the current approved API specification or applicable pharmacopoeial monograph rather than assigning unsupported generic limits.
Nizatidine has been associated with regulatory attention concerning N-nitroso-related impurities, including N-nitroso-nizatidine and N-nitroso-desmethyl-nizatidine. PubChem separately identifies these nitrosamine-related substances.
Consequently, a commercial Nizatidine API quality system should include an appropriate nitrosamine risk assessment and control strategy consistent with applicable regulatory requirements.
Elemental impurities should be assessed and controlled according to applicable pharmaceutical requirements, including ICH Q3D where applicable.
A generic heavy-metal numerical limit should not be inserted unless it is specifically supported by the current approved API specification.
Nizatidine is represented with a defined E configuration around its nitroethenediamine double bond, but it does not contain a conventional chiral stereogenic center.
Therefore:
Specific Rotation: Not applicable as a routine stereochemical release parameter.
Enantiomeric Purity: Not applicable.
Geometrical Isomer Control: May be relevant and should be controlled according to the applicable validated specification.
Nizatidine API should be stored in a tightly closed container under controlled pharmaceutical storage conditions, protected from excessive moisture, heat and direct light as required by the applicable stability and packaging specification.
Final storage conditions should be based on validated stability data.
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 101.0 |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.1% |
| Individual Impurity | NMT 0.3% |
| Water Content | NMT 1.0% |
| Melting Point | 130–134°C |