Nizatidine

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Nizatidine
Nizatidine structure.png
Systematic (IUPAC) name
N-(2-[(2-[(dimethylamino)methyl]thiazol-4-yl)methylthio]ethyl)-N-methyl-2-nitroethene-1,1-diamine
Clinical data
Trade names Axid
AHFS/Drugs.com monograph
MedlinePlus a694030
Licence data US FDA:link
Pregnancy cat.
Legal status
Routes Oral
Pharmacokinetic data
Bioavailability >70%
Protein binding 35%
Metabolism Hepatic
Half-life 1-2 hours
Excretion Renal
Identifiers
CAS number 76963-41-2 YesY
ATC code A02BA04
PubChem CID 3033637
DrugBank DB00585
ChemSpider 2298266 YesY
UNII P41PML4GHR YesY
KEGG D00440 YesY
ChEBI CHEBI:7601 YesY
ChEMBL CHEMBL653 YesY
Chemical data
Formula C12H21N5O2S2 
Mol. mass 331.46 g/mol
 YesY (what is this?)  (verify)

Nizatidine is a histamine H2-receptor antagonist that inhibits stomach acid production, and commonly used in the treatment of peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD). It was developed by Eli Lilly and is marketed under the brand names Tazac and Axid.

Clinical use[edit]

Certain preparations of nizatidine are now available over the counter in various countries including the United States. Nizatidine has been used experimentally to control weight gain associated with some antipsychotic medication. [2]

Adverse effects[edit]

Antacid preparations such as nizatidine work by suppressing acid mediated break down of proteins, leads to an elevated risk of developing food or drug allergies. This happens due to undigested proteins then passing into the gastrointestinal tract where sensitisation occurs. It is unclear whether this risk occurs with only long-term use or with short-term use as well.[3]

History and development[edit]

Nizatidine was developed by Eli Lilly, and was first marketed in 1987. 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. [4] Subsequently, Reliant developed the oral solution of Axid, marketing this in 2004, after gaining approval from the U.S. Food and Drug Administration (FDA). [5] However, a year later they sold rights of the Axid Oral Solution (including the issued patent US6,930,119 protecting the product) to Braintree Laboratories.[6]

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

See also[edit]

  • Famotidine, aka Pepcid AC, Pepcidine: another popular H2-receptor antagonist

References[edit]

  1. ^ Nizatidine
  2. ^ Atmaca M, Kuloglu M, Tezcan E, Ustundag B, Kilic N (January 2004). "Nizatidine for the treatment of patients with quetiapine-induced weight gain". Hum Psychopharmacol 19 (1): 37–40. doi:10.1002/hup.477. PMID 14716710. 
  3. ^ Pali-Schöll I, Jensen-Jarolim E (April 2011). "Anti-acid medication as a risk factor for food allergy". Allergy 66 (4): 469–77. doi:10.1111/j.1398-9995.2010.02511.x. PMID 21121928. 
  4. ^ Eli Lilly and Company and Reliant Pharmaceuticals Announce
  5. ^ Reliant Pharmaceuticals : Press Releases
  6. ^ Reliant Pharmaceuticals : Press Releases

External links[edit]