Nizatidine

Nizatidine is a histamine H2 receptor antagonist that inhibits stomach acid production, and is commonly used in the treatment of peptic ulcer disease and gastroesophageal reflux disease.[1]

Nizatidine
Clinical data
Trade namesAxid, Tazac
AHFS/Drugs.comMonograph
MedlinePlusa694030
License data
Pregnancy
category
    Routes of
    administration    		By mouth
    ATC code
    Legal status
    Legal status
    • AU: S4 (Prescription only)
    • UK: POM (Prescription only)
    • US: OTC / Rx-only
    Pharmacokinetic data
    Bioavailability>70%
    Protein binding35%
    MetabolismLiver
    Elimination half-life1–2 hours
    ExcretionKidney
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard100.155.683
    Chemical and physical data
    FormulaC12H21N5O2S2
    Molar mass331.45 g·mol−1
    3D model (JSmol)
     NY (what is this?)  (verify)

    It was patented in 1980 and approved for medical use in 1988.[2][3] It was developed by Eli Lilly. Brand names include Tazac and Axid.

    Medical use
    Main article: H2 antagonist

    Nizatidine is used to treat duodenal ulcers, gastric ulcers, and gastroesophageal reflux disease (GERD/GORD), and to prevent stress ulcers.[4]

    Adverse effects

    Side effects are uncommon, usually minor, and include diarrhea, constipation, fatigue, drowsiness, headache, and muscle aches.[4]

    History and development

    Nizatidine was developed by Eli Lilly, and was first marketed in 1988.[2] It is considered to be equipotent with ranitidine and differs by the substitution of a thiazole ring in place of the furan ring in ranitidine. In September 2000, Eli Lilly announced they would sell the sales and marketing rights for Axid to Reliant Pharmaceuticals.[5] Subsequently, Reliant developed the oral solution of Axid, marketing this in 2004, after gaining approval from the U.S. Food and Drug Administration (FDA).[6] However, a year later, they sold rights of the Axid Oral Solution (including the issued patent[7] protecting the product) to Braintree Laboratories.[8]

    Nizatidine proved to be the last new histamine H2 receptor antagonist introduced prior to the advent of proton pump inhibitors.

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    See also
    • Famotidine (Pepcid) — another popular H2 receptor antagonist

    References
    1. Romero M, Franzosi MG (1989). "[Nizatidine]". Medicina (Florence, Italy) (in Italian). 9 (1): 93–6. PMID 2567957.
    2. "Nizatidine: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Retrieved 20 March 2020.
    3. Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 44. ISBN 9783527607495.
    4. "Nizatidine". LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. NCBI Bookshelf. 25 January 2018. PMID 31643707. NBK548387. Retrieved 19 March 2020.
    5. "Eli Lilly and Company and Reliant Pharmaceuticals Announce Agreement for U.S. Sales and Marketing Rights to Axid(R)". High Beam Encyclopedia. 7 September 2000. Archived from the original on May 26, 2008.
    6. "Reliant Pharmaceuticals to Launch AxidŽ Oral Solution". Reliant Pharmaceuticals, LLC. 26 July 2004.
    7. US 6930119, Bobotas G, Fawzy AA, "Liquid pharmaceutical composition", issued 24 June 2005, assigned to Reliant Pharmaceuticals, LLC
    8. "Reliant Pharmaceuticals Announces the Sale of Axid® Oral Solution to Braintree Laboratories". Reliant Pharmaceuticals, LLC. Archived from the original on August 14, 2007.
    • "Nizatidine". Drug Information Portal. U.S. National Library of Medicine.
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