Terlipressin

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Terlipressin
Terlipressin.png
Clinical data
Trade names Terlivaz
AHFS/Drugs.com International Drug Names
Routes of
administration 		Intravenous
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding ~30%
Identifiers
  • 1-{[(4R,7S,10S,13S,16S,19R)-19-{[({[(aminoacetyl)amino]acetyl}amino)acetyl]amino}-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-benzyl-16-(4-hydroxybenzyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosan-4-yl]carbonyl}-L-prolyl-N-(2-amino-2-oxoethyl)-L-lysinamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
ECHA InfoCard 100.035.149 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C52H74N16O15S2
Molar mass 1227.38 g·mol−1
3D model (JSmol)
  • O=C(N)CNC(=O)[C@@H](NC(=O)[C@H]4N(C(=O)[C@H]1NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)CNC(=O)CN)CSSC1)Cc2ccc(O)cc2)Cc3ccccc3)CCC(=O)N)CC(=O)N)CCC4)CCCCN
  • InChI=1S/C52H74N16O15S2/c53-17-5-4-9-31(45(76)60-23-41(57)72)63-51(82)38-10-6-18-68(38)52(83)37-27-85-84-26-36(61-44(75)25-59-43(74)24-58-42(73)22-54)50(81)65-34(20-29-11-13-30(69)14-12-29)48(79)64-33(19-28-7-2-1-3-8-28)47(78)62-32(15-16-39(55)70)46(77)66-35(21-40(56)71)49(80)67-37/h1-3,7-8,11-14,31-38,69H,4-6,9-10,15-27,53-54H2,(H2,55,70)(H2,56,71)(H2,57,72)(H,58,73)(H,59,74)(H,60,76)(H,61,75)(H,62,78)(H,63,82)(H,64,79)(H,65,81)(H,66,77)(H,67,80)/t31-,32-,33-,34-,35-,36-,37-,38-/m0/s1 Yes check.svgY
  • Key:BENFXAYNYRLAIU-QSVFAHTRSA-N Yes check.svgY
   (verify)

Terlipressin, sold under the brand name Terlivaz among others, is an analogue of vasopressin used as a vasoactive drug in the management of low blood pressure. It has been found to be effective when norepinephrine does not help. Terlipressin is a vasopressin receptor agonist. [2]

Contents

Terlipressin was approved for medical use in the United States in 2022. [2] [4] [5] The US Food and Drug Administration (FDA) considers it to be a first-in-class medication. [5] [6]

Medical uses

Terlipressin is indicated to improve kidney function in adults with hepatorenal syndrome with rapid reduction in kidney function. [2]

Indications for use include norepinephrine-resistant septic shock [7] although, 2021 Surviving Sepsis Guidelines recommend against its use for adults with septic shock [8] and hepatorenal syndrome. [9] In addition, it is used to treat bleeding esophageal varices. [10]

Contraindications

Terlipressin is contraindicated in people experiencing hypoxia or worsening respiratory symptoms and in people with ongoing coronary, peripheral or mesenteric ischemia. [2] Terlipressin may cause fetal harm when used during pregnancy. [2]

Society and culture

Terlipressin is available in United States, [11] New Zealand, [12] Australia, the European Union, [13] India, Pakistan & UAE. It is sold under various brand names including Glypressin and Terlivaz.

References

  1. ↑ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA . Retrieved 22 Oct 2023.
  2. 1 2 3 4 5 6 "Terlivaz- terlipressin injection, powder, lyophilized, for solution". DailyMed. 19 September 2022. Archived from the original on 28 September 2022. Retrieved 27 September 2022.
  3. ↑ "Drug Approval Package: Terlivaz". U.S. Food and Drug Administration (FDA). 7 October 2022. Retrieved 4 December 2022.
  4. ↑ "Drug Approval Package: Terlivaz". U.S. Food and Drug Administration (FDA). 7 October 2022. Retrieved 23 January 2023.
  5. 1 2 "Advancing Health Through Innovation: New Drug Therapy Approvals 2022". U.S. Food and Drug Administration (FDA). 10 January 2023. Retrieved 22 January 2023.PD-icon.svg This article incorporates text from this source, which is in the public domain .
  6. ↑ New Drug Therapy Approvals 2022 (PDF). U.S. Food and Drug Administration (FDA) (Report). January 2024. Archived from the original on 14 January 2024. Retrieved 14 January 2024.PD-icon.svg This article incorporates text from this source, which is in the public domain .
  7. ↑ O'Brien A, Clapp L, Singer M (April 2002). "Terlipressin for norepinephrine-resistant septic shock". Lancet. 359 (9313): 1209–1210. doi:10.1016/S0140-6736(02)08225-9. PMID   11955542. S2CID   38463837.
  8. ↑ Evans L, Rhodes A, Alhazzani W, Antonelli M, Coopersmith CM, French C, et al. (November 2021). "Surviving Sepsis Campaign: International Guidelines for Management of Sepsis and Septic Shock 2021". Critical Care Medicine. 49 (11): e1063 –e1143. doi: 10.1097/CCM.0000000000005337 . PMID   34605781.
  9. ↑ Uriz J, Ginès P, Cárdenas A, Sort P, Jiménez W, Salmerón JM, et al. (July 2000). "Terlipressin plus albumin infusion: an effective and safe therapy of hepatorenal syndrome". Journal of Hepatology. 33 (1): 43–48. doi:10.1016/S0168-8278(00)80158-0. PMID   10905585.
  10. ↑ Ioannou G, Doust J, Rockey DC (2003). Ioannou GN (ed.). "Terlipressin for acute esophageal variceal hemorrhage". The Cochrane Database of Systematic Reviews (1): CD002147. doi:10.1002/14651858.CD002147. PMC   7017851 . PMID   12535432.
  11. ↑ "FDA approves treatment to improve kidney function in adults with hepatorenal syndrome". FDA. 14 September 2022. Archived from the original on 2023-02-10. Retrieved 2023-02-21.
  12. ↑ "GLYPRESSIN 1mg/8.5mL Solution for Injection; Terlipressin acetate" (PDF). Medsafe, New Zealand Medicines and Medical Devices Safety Authority. New Zealand Ministry of Health. Archived from the original (PDF) on 2021-12-20.
  13. ↑ "Terlipressin". Drugs.com. Archived from the original on 2019-06-26. Retrieved 2018-01-23.
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