TERLIPRESSIN ACETATE

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/022231s000lbl.pdf|https://www.ncbi.nlm.nih.gov/pubmed/27586252 | http://www.nps.org.au/__data/cmi_pdfs/CMR10462.pdf

Terlipressin (Glypressin) is indicated for the treatment of bleeding oesophageal varices and in some countries for the treatment of hepatorenal syndrome type 1. It is a prodrug and is converted to the lysine vasopressin in the circulation after the N-triglycyl residue is cleaved by endothelial peptidases. This results in a ‘slow release’ of the vasoactive lysine vasopressin. Terlipressin exerts its action by activating V1a, V1b and V2 vasopressin receptors. On September 14, 2022, the FDA granted approval to terlipressin (Terlivaz) for the treatment of adults hospitalized with hepatorenal syndrome with rapid reduction in kidney function (HRS-1). Prior to the approval, no approved treatment for this condition existed in the United States.

Approval Year

Targets

Primary Target	Pharmacology	Potency
Vasopressin V1a receptor 18 Target ID: P37288 Gene ID: 552.0 Gene Symbol: AVPR1A Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/27586252\|https://pubmed.ncbi.nlm.nih.gov/29302194/	Partial Agonist 297	852.0 nM [Ki]
Vasopressin V1b receptor 7 Target ID: P47901 Gene ID: 553.0 Gene Symbol: AVPR1B Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/27586252\|https://pubmed.ncbi.nlm.nih.gov/29302194	Agonist 2752	1115.0 nM [Ki]
Vasopressin V2 receptor 16 Target ID: P30518 Gene ID: 554.0 Gene Symbol: AVPR2 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/27586252\|https://pubmed.ncbi.nlm.nih.gov/29302194	Agonist 2752	1580.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hepatorenal syndrome 3 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/022231s000lbl.pdfhttps://www.old.health.gov.il/units/pharmacy/trufot/alonim/Glypressin_dr_1293447055647.pdf	Primary		Approved 8583	TERLIVAZ Approved Use TERLIVAZ is a vasopressin receptor agonist indicated to improve kidney function in adults with hepatorenal syndrome with rapid reduction in kidney function. Launch Date 2022
Bleeding oesophageal varices 3 Sources: https://www.medicines.org.uk/emc/files/pil.6551.pdfhttps://www.medsafe.govt.nz/profs/datasheet/g/Glypressin01mgmlFerringinj.pdf	Primary		Approved 8583	GLYPRESSIN Approved Use GLYPRESSIN is used to treat Bleeding Oesophageal Varices (BOV), bleeding veins inthe lower end of the food-pipe in people with serious liver disease. GLYPRESSIN is also used to treat hepatorenal syndrome, type 1 (HRS-1).

C_max

Value	Dose	Co-administered	Analyte	Population
70.5 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=49 \| https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/022231s000lbl.pdf#page=8	1 mg 4 times / day multiple, intravenous dose: 1 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:		TERLIPRESSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.16 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=49 \| https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/022231s000lbl.pdf#page=8	1 mg 4 times / day multiple, intravenous dose: 1 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:		LYPRESSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
123 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=49 \| https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/022231s000lbl.pdf#page=8	1 mg 4 times / day multiple, intravenous dose: 1 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:		TERLIPRESSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
11.2 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=49 \| https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/022231s000lbl.pdf#page=8	1 mg 4 times / day multiple, intravenous dose: 1 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:		LYPRESSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
0.9 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=49 \| https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/022231s000lbl.pdf#page=8	1 mg 4 times / day multiple, intravenous dose: 1 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:		TERLIPRESSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
3 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=49 \| https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/022231s000lbl.pdf#page=8	1 mg 4 times / day multiple, intravenous dose: 1 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:		LYPRESSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
3 mg 4 times / day steady, intravenous Highest studied dose Dose: 3 mg, 4 times / day Route: intravenous Route: steady Dose: 3 mg, 4 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf	Disc. AE: Death... AEs leading to discontinuation/dose reduction: Death (17.4%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf
1 mg 4 times / day steady, intravenous Studied dose Dose: 1 mg, 4 times / day Route: intravenous Route: steady Dose: 1 mg, 4 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf	Disc. AE: Death... Other AEs: Hepatic disorders, Respiratory failure... AEs leading to discontinuation/dose reduction: Death (50.8%) Other AEs: Hepatic disorders (33.3%) Respiratory failure (5.1%) Gastrointestinal hemorrhage (4.0%) Abdominal pain (1.0%) Haemodynamic edema, effusions and fluid overload (2.0%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf
1 mg 4 times / day steady, intravenous Studied dose Dose: 1 mg, 4 times / day Route: intravenous Route: steady Dose: 1 mg, 4 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000RiskR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000RiskR.pdf	Disc. AE: Death... Other AEs: Respiratory failure, Hemodynamic edema... AEs leading to discontinuation/dose reduction: Death (4.5%) Other AEs: Respiratory failure (14.0%) Hemodynamic edema (4.6%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000RiskR.pdf

AEs

AE	Significance	Dose	Population
Death	17.4% Disc. AE	3 mg 4 times / day steady, intravenous Highest studied dose Dose: 3 mg, 4 times / day Route: intravenous Route: steady Dose: 3 mg, 4 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf
Abdominal pain	1.0%	1 mg 4 times / day steady, intravenous Studied dose Dose: 1 mg, 4 times / day Route: intravenous Route: steady Dose: 1 mg, 4 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf
Haemodynamic edema, effusions and fluid overload	2.0%	1 mg 4 times / day steady, intravenous Studied dose Dose: 1 mg, 4 times / day Route: intravenous Route: steady Dose: 1 mg, 4 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf
Hepatic disorders	33.3%	1 mg 4 times / day steady, intravenous Studied dose Dose: 1 mg, 4 times / day Route: intravenous Route: steady Dose: 1 mg, 4 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf
Gastrointestinal hemorrhage	4.0%	1 mg 4 times / day steady, intravenous Studied dose Dose: 1 mg, 4 times / day Route: intravenous Route: steady Dose: 1 mg, 4 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf
Respiratory failure	5.1%	1 mg 4 times / day steady, intravenous Studied dose Dose: 1 mg, 4 times / day Route: intravenous Route: steady Dose: 1 mg, 4 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf
Death	50.8% Disc. AE	1 mg 4 times / day steady, intravenous Studied dose Dose: 1 mg, 4 times / day Route: intravenous Route: steady Dose: 1 mg, 4 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf
Respiratory failure	14.0%	1 mg 4 times / day steady, intravenous Studied dose Dose: 1 mg, 4 times / day Route: intravenous Route: steady Dose: 1 mg, 4 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000RiskR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000RiskR.pdf
Death	4.5% Disc. AE	1 mg 4 times / day steady, intravenous Studied dose Dose: 1 mg, 4 times / day Route: intravenous Route: steady Dose: 1 mg, 4 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000RiskR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000RiskR.pdf
Hemodynamic edema	4.6%	1 mg 4 times / day steady, intravenous Studied dose Dose: 1 mg, 4 times / day Route: intravenous Route: steady Dose: 1 mg, 4 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000RiskR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000RiskR.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252 inducer 1087	inhibitor 2438 inducer 440	inhibitor 2507 inducer 109

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
BCRP 910 P-gp 1741 CYP2A6 879 CYP2E1 1060 CYP1A2 2153 CYP2B6 926 CYP2C8 1057 CYP2C19 2057 MATE2-K 77 MATE1 415 OCT2 779 OAT3 747 OAT1 725 OATP1B3 961 OATP1B1 1079	P-gp 2052 OAT3 391 BCRP 697 OATP1B1 503 OAT1 395 OATP1B3 435 OCT2 434 MATE1 182 MATE2-K 33	CYP1A2 832 CYP2E1 131 CYP2B6 669 CYP2A6 86 CYP2C19 329

Drug as perpetrator

Target	Modality	Activity
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50 \| 256 \| 278	no [IC50 >=5000 uM]
CYP2A6 911	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=255 Page: 255 \| 256 \| 278	no [IC50 >=5000 uM]
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50 \| 256 \| 278	no [IC50 >=5000 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50 \| 256 \| 278	no [IC50 >=5000 uM]
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50 \| 256 \| 278	no [IC50 >=5000 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50 \| 256 \| 278	no [IC50 >=5000 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50 \| 256 \| 278	no [IC50 >=5000 uM]
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=255 Page: 255 \| 256 \| 278	no [IC50 >=5000 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50 \| 256 \| 278	no [IC50 >=5000 uM]
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50 \| 257 \| 258 \| 279	no
CYP2A6 911	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=257 Page: 257 \| 258 \| 279	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50 \| 257 \| 258 \| 279	no
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=257 Page: 257 \| 258 \| 279	no
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=257 Page: 257 \| 258 \| 279	no
CYP2D6 2546	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=257 Page: 257 \| 258 \| 279	no
CYP2E1 1146	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=257 Page: 257 \| 258 \| 279	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50 \| 257 \| 258 \| 279	no
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
MATE2-K 77	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no

Drug as victim

Target	Modality	Activity
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
MATE1 182	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
MATE2-K 33	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
OAT1 395	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
OAT3 391	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/022231Orig1s000IntegratedR.pdf#page=50 Page: 50.0	no

PubMed

Title	Date	PubMed
Terlipressin for treating intraoperative hypotension: can it unmask myocardial ischemia?	2001 Jul	11429338
Portal hypertension.	2001 May	11385974
New method of cardiac output measurement using ultrasound velocity dilution in rats.	2001 Sep	11509526
Terlipressin-ephedrine versus ephedrine to treat hypotension at the induction of anesthesia in patients chronically treated with angiotensin converting-enzyme inhibitors: a prospective, randomized, double-blinded, crossover study.	2002 Apr	11916781
Terlipressin in patients with cirrhosis and type 1 hepatorenal syndrome: a retrospective multicenter study.	2002 Apr	11910344
Terlipressin for norepinephrine-resistant septic shock.	2002 Apr 6	11955542
Renal failure in cirrhotic patients: role of terlipressin in clinical approach to hepatorenal syndrome type 2.	2002 Dec	12468959
Terlipressin-induced vasoconstriction reversed with N-acetylcysteine: a case for combined use in hepatorenal syndrome?	2002 Dec	12454887
Effect of terlipressin (Glypressin) on hepatorenal syndrome in cirrhotic patients: results of a multicentre pilot study.	2002 Feb	11981339
Terlipressin inhibits in vivo aortic iNOS expression induced by lipopolysaccharide in rats with biliary cirrhosis.	2002 Nov	12395316
Terlipressin for haemodynamic support in septic patients: a double-edged sword?	2002 Oct 19	12401276
[Comparison of Doppler ultrasonography and hepatic venous pressure gradient in assessing portal hypertension in liver cirrhosis].	2002 Sep	12499783
Management of acute variceal bleeding.	2003	12837994
Portal hypertensive bleeding.	2003 Dec	14696298
Effects of the V1a vasopressin agonist F-180 on portal hypertension-related bleeding in portal hypertensive rats.	2003 Dec	14647048
Systematic review: terlipressin in acute oesophageal variceal haemorrhage.	2003 Jan	12492732
When endoscopic therapy or pharmacotherapy fails to control variceal bleeding: what should be done? Immediate control of bleeding by TIPS?	2003 Jul	12728322
Cyclooxygenase expression in splanchnic hyposensitivity to glypressin of bleeding portal hypertensive rats.	2003 Jun	12795648
Terlipressin infusion in catecholamine-resistant shock.	2003 Oct	14601280
[Vasoconstrictive Therapies for Bleeding Esophageal Varices and their Mechanisms of Action].	2003 Oct	14562199
[Vasopressin and its analogues in the therapy of shock].	2004	15305765
Vasopressors for shock.	2004	15266497
Effects of terlipressin on systemic and regional haemodynamics in catecholamine-treated hyperkinetic septic shock.	2004 Apr	14673520
Effects of treatment of hepatorenal syndrome before transplantation on posttransplantation outcome. A case-control study.	2004 Jan	14672625
Clinical review: influence of vasoactive and other therapies on intestinal and hepatic circulations in patients with septic shock.	2004 Jun	15153235
[Refractory hypotension during anesthesia in a patient treated with angiotensin receptor blockers].	2004 Jun-Jul	15303535
Effect of terlipressin on blood volume distribution in patients with cirrhosis.	2004 May	15180188

Sample Use Guides

In Vivo Use Guide

Recommended Dosage Regimen: (2.2) • Days 1 to 3 administer TERLIVAZ 0.85 mg (1 vial) intravenously every 6 hours. • Day 4: Assess serum creatinine (SCr) versus baseline. • If SCr has decreased by at least 30% from baseline, continue TERLIVAZ 0.85 mg (1 vial) intravenously every 6 hours. • If SCr has decreased by less than 30% from baseline, dose may be increased to TERLIVAZ 1.7 mg (2 vials) intravenously every 6 hours.

Route of Administration: Intravenous

In Vitro Use Guide

Terlipressin also non-selectively interacted with all the vasopressin receptors but with an affinity reduced by at least 710 folds (Ki in nM: 852 for hV1A-R; 1115 for hV1B-R; and 1580 for hV2-R)

Substance Class	Protein Created by `admin` on `Mon Mar 31 20:36:51 GMT 2025` Edited by `admin` on `Mon Mar 31 20:36:51 GMT 2025`
Protein Sub Type
Sequence Type	COMPLETE
Record UNII	4U092XZF0K
Record Status	`FAILED`
Record Version

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Name

Type

Language

TERLIPRESSIN DIACETATE PENTAHYDRATE

Preferred Name

English

TERLIPRESSIN ACETATE

Common Name

English

TERLIPRESSIN ACETATE [JAN]

Common Name

English

TERLIVAZ

Brand Name

English

TERLIPRESSIN ACETATE [MART.]

Common Name

English

Terlipressin acetate [WHO-DD]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C80212