Nizatidine

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Nizatidine
Names
Trade namesAxid, Tazac, others
  • (E)-1-N'-[2-[[2-[(dimethylamino)methyl]-1,3-thiazol-4-yl]methylsulfanyl]ethyl]-1-N-methyl-2-nitroethene-1,1-diamine
Clinical data
Drug classH2 antagonist[1]
Main usesStomach ulcers, gastroesophageal reflux disease[1]
Side effectsHeadache, dizziness[1]
Pregnancy
category
  • AU: B3
Routes of
use		By mouth
Typical dose75 to 300 mg/day[1]
External links
AHFS/Drugs.comMonograph
MedlinePlusa694030
Legal
License data
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: OTC / Rx-only
Pharmacokinetics
Bioavailability>70%
Protein binding35%
MetabolismLiver
Elimination half-life1–2 hours
ExcretionKidney
Chemical and physical data
FormulaC12H21N5O2S2
Molar mass331.45 g·mol−1
3D model (JSmol)
  • [O-][N+](=O)\C=C(/NC)NCCSCc1nc(sc1)CN(C)C
  • InChI=1S/C12H21N5O2S2/c1-13-11(6-17(18)19)14-4-5-20-8-10-9-21-12(15-10)7-16(2)3/h6,9,13-14H,4-5,7-8H2,1-3H3/b11-6+ checkY
  • Key:SGXXNSQHWDMGGP-IZZDOVSWSA-N checkY

Nizatidine, sold under the brand name Axid, is a medication used to treat stomach ulcers and gastroesophageal reflux disease.[1] It may be take for 4 to 12 weeks.[2] It is taken by mouth.[1]

Common side effects include headache and dizziness.[1] Other side effects may include pneumonia.[1] No harm has been found in pregnancy, but such use has not been well studied.[3] Use when breastfeeding appears safe.[2] It is a histamine H2 receptor antagonist that inhibits stomach acid production.[1]

Nizatidine was patented in 1980 and approved for medical use in 1987.[4] It was approved in the United States in 1988.[1] It is available as a generic medication and over the counter.[2] In the United Kingdom a month of medication costs the NHS about £18 as of 2021.[2] In the United States this costs about 20 USD.[5]

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.[6]

Dosage

It is used at a dose of 75 to 150 mg by mouth once or twice per day.[1]

Side effects

Side effects are uncommon, usually minor, and include diarrhea, constipation, fatigue, drowsiness, headache, and muscle aches.[6]

History

Nizatidine was developed by Eli Lilly, and was first marketed in the United States in 1988.[7] 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.[8] Subsequently, Reliant developed the oral solution of Axid, marketing this in 2004, after gaining approval from the U.S. Food and Drug Administration (FDA).[9] However, a year later, they sold rights of the Axid Oral Solution (including the issued patent[10] protecting the product) to Braintree Laboratories.[11]

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

Axid (nizatidine) drug recalled due to presence of NDMA

See also

  • Famotidine (Pepcid) — another H2 receptor antagonist

References

  1. ↑ 1.00 1.01 1.02 1.03 1.04 1.05 1.06 1.07 1.08 1.09 1.10 "Nizatidine Monograph for Professionals". Drugs.com. Archived from the original on 7 August 2020. Retrieved 13 November 2021.
  2. ↑ 2.0 2.1 2.2 2.3 BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 81. ISBN 978-0857114105.
  3. ↑ "Nizatidine Use During Pregnancy". Drugs.com. Archived from the original on 26 October 2020. Retrieved 13 November 2021.
  4. ↑ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 44. ISBN 9783527607495. Archived from the original on 2020-07-29. Retrieved 2021-02-13.
  5. ↑ "Nizatidine Prices, Coupons & Savings Tips - GoodRx". GoodRx. Retrieved 13 November 2021.
  6. ↑ 6.0 6.1 "Nizatidine". LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. NCBI Bookshelf. 25 January 2018. PMID 31643707. NBK548387. Archived from the original on 28 October 2021. Retrieved 19 March 2020.
  7. ↑ "Nizatidine: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Archived from the original on 4 August 2020. Retrieved 20 March 2020.
  8. ↑ "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.
  9. ↑ "Reliant Pharmaceuticals to Launch AxidŽ Oral Solution". Reliant Pharmaceuticals, LLC. 26 July 2004. Archived from the original on 26 December 2013. Retrieved 13 February 2021.
  10. ↑ US 6930119, Bobotas G, Fawzy AA, "Liquid pharmaceutical composition", issued 24 June 2005, assigned to Reliant Pharmaceuticals, LLC 
  11. ↑ "Reliant Pharmaceuticals Announces the Sale of Axid® Oral Solution to Braintree Laboratories". Reliant Pharmaceuticals, LLC. Archived from the original on August 14, 2007.

External links

External sites:
Identifiers:
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