Terlivaz (terlipressin acetate)
Antidiuretic Hormone Intravenous Vial (EA)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Terlipressin acetate is a synthetic vasopressin analogue.
Terlipressin is a synthetic vasopressin analogue with twice the selectivity for vasopressin V1 receptors versus V2 receptors. Terlipressin acts as both a prodrug for lysine-vasopressin, as well as having pharmacologic activity on its own. Terlipressin is thought to increase renal blood flow in patients with hepatorenal syndrome by reducing portal hypertension and blood circulation in portal vessels and increasing effective arterial volume and mean arterial pressure (MAP).
After administration, increases of diastolic, systolic, and MAPs were observed within 5 minutes and were maintained for at least 6 hours. The maximum change in blood pressure and heart rate occurred at 1.2-2 hours after dosing. The estimated maximum effects on MAP and heart rate were an increase of 16.2 mm Hg and a decrease of 10.6 beats per minute, respectively.
Terlipressin and lysine-vasopressin exhibit linear pharmacokinetics in healthy subjects. Plasma concentrations of terlipressin demonstrate proportional increases with the dose administered. In patients with hepatorenal syndrome-1, body weight increased clearance of terlipressin, but had no effect on the clearance of lysine-vasopressin.
The terminal half-life was 0.9 hours for terlipressin and 3.0 hours for lysine-vasopressin. Terlipressin is metabolized by various tissue peptidases, resulting in release of the pharmacologically active metabolite lysine-vasopressin. Lysine-vasopressin is metabolized by various tissue peptidase-mediated routes.
Terlipressin is not metabolized in blood or plasma. Less than 1% of terlipressin and <0.1% of lysine-vasopressin is excreted in urine in healthy subjects. Clearance of terlipressin and lysine-vasopressin appears to be unaffected by gender, age, creatinine clearance, Child-Pugh score, serum alkaline phosphatase, ALT, AST, and total bilirubin.
Generic name: terlipressin acetate
Drug class: Antidiuretic Hormone
Therapeutic class: Endocrine
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Terlivaz
Indications
The following indications are listed for Terlivaz:
- Hepatorenal Syndrome
Also known as: Hepatorenal Disease, Heyd's Syndrome, Urohepatic Syndrome.
Dosing
Dosage of terlipressin acetate is expressed in terms of terlipressin. Each 1 mg of terlipressin acetate is equivalent to terlipressin 0.85 mg.
Terlipressin is administered by slow IV bolus injection (over 2 minutes). Administer terlipressin through a peripheral or central line. A dedicated central line is not required. Flush the line after terlipressin administration.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Terlivaz 0.85 Mg Vial | Maintenance | Inject 0.85 mg over 2 minute(s) by intravenous route every 6 hours. |
No dosing information is available for this tab.
Drug interactions
In vitro studies in human liver microsomes demonstrated little or no evidence that terlipressin was an inhibitor and inducer of any of the cytochrome P-450 (CYP) enzymes evaluated. In addition, there was little or no evidence that terlipressin is an inhibitor and substrate of human adenosine triphosphate-binding cassette (ABC) and solute carrier (SLC) transporters. No significant drug-drug interactions are anticipated with terlipressin.
Due to the ubiquitous nature of the tissue peptidases that metabolize the terlipressin parent compound and its active metabolize, it is unlikely that the metabolism of terlipressin will be affected by other disease states or drugs.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Patients experiencing hypoxia or worsening respiratory symptoms.
*Patients with ongoing coronary, peripheral, or mesenteric ischemia.
- Cerebral ischemia
- Myocardial ischemia
- Atherosclerotic cardiovascular disease
- Congenital long QT syndrome
- Hypokalemia
- Hypomagnesemia
- Hyponatremia
- Hypoxia
- Pregnancy
- Prolonged QT interval
- Torsades de pointes
- Hypertension
- Lower seizure threshold
- Respiratory depression
- Seizure disorder
- Ventricular arrhythmias
Adverse reactions
The most common adverse reactions (>=10%) include abdominal pain, nausea, respiratory failure, diarrhea, and dyspnea.
More Frequent
- Acute respiratory failure
- Bradycardia
Less Frequent
- Pleural effusions
- Sepsis
Rare or Very Rare
- Acute myocardial infarction
- Cerebral ischemia
- Dermal necrosis
- Gangrene
- Hyponatremia
- Intestinal ischemic necrosis
- Myocardial ischemia
- Pulmonary edema
More Frequent
- Acute abdominal pain
- Diarrhea
- Dyspnea
- Nausea
Less Frequent
- Hypervolemia
Rare or Very Rare
- Headache disorder
Precautions
No enhanced messaging available.
Safety and effectiveness of terlipressin have not been established in pediatric patients.
Based on findings from the published literature and its mechanism of action, terlipressin may cause fetal harm when administered to pregnant patients. In small, published studies, administration of a single IV dose of terlipressin to pregnant females during the first trimester induced uterine contractions and endometrial ischemia. The limited published data are not sufficient to determine a drug-associated risk for major birth defects or miscarriage. If terlipressin is used during pregnancy, inform the patient of the potential risk to the fetus.
In published reproductive toxicity animal studies, administration of terlipressin to pregnant guinea pigs at doses lower than the maximum recommended human dose of 4 mg/day caused a marked decrease in blood flow to the uterus and placenta. In rabbits, terlipressin is both embryotoxic and teratogenic.
There are no data on the presence of terlipressin in human or animal milk, the effects on the breast-fed infant, or the effect on milk production. Consider the developmental and health benefits of breastfeeding along with the mother's clinical need for terlipressin and any potential adverse effects on the breast-fed child from the drug or underlying maternal condition.
The manufacturer makes no specific dosage recommendations for geriatric patients.
Of the total number of patients in clinical studies treated with terlipressin, 55 (16%) were >=65 years of age. No overall differences in safety or effectiveness were observed between these subjects and younger subjects; other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.
ICD codes
| Code | Type | Description |
|---|---|---|
| Hepatorenal syndrome | ||
| K76.7 | ICD10CM | Hepatorenal syndrome |
| K91.83 | ICD10CM | Postprocedural hepatorenal syndrome |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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