Terlipressin


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : IV Acute oesophageal variceal haemorrhage As powder and solvent for solution for inj: Initial: 1-2 mg, then 1 mg 4-6 hourly. Max duration: 72 hours. As solution for inj: Initial: 2 mg 4 hourly, maintain until bleeding is controlled for 24 hours or up to max of 48 hours, may reduce to 1 mg 4 hourly if needed. Hepatorenal syndrome type 1 Initial: 1 mg 6 hourly, may be increased up to max 2 mg 4-6 hourly if serum creatinine has not been reduced by at least 25% after 3 days. Max duration: 2 weeks.
Dosage Details
Intravenous
Acute oesophageal variceal haemorrhage
Adult: As powder and solvent for solution for inj: Initially, 1-2 mg, then 1 mg 4-6 hourly. Max duration of treatment: 72 hours. As solution for inj: Initially, 2 mg 4 hourly, maintain until bleeding is controlled for 24 hours or up to max of 48 hours. Subsequent doses may be reduced to 1 mg 4 hourly in patients weighing <50 kg or if adverse reaction occur.

Intravenous
Hepatorenal syndrome type 1
Adult: Initially, 1 mg 6 hourly via slow bolus inj, may be increased up to max 2 mg 4-6 hourly if serum creatinine has not been reduced by at least 25% after 3 days. Max duration of treatment: 2 weeks.
Reconstitution
Powder for solution for inj: Slowly add the contents of the solvent ampoule to the powder vial and roll gently until completely dissolved. Dilute further with 10 mL NaCl 0.9% solution for inj.
Contraindications
Unstable angina, recent MI, septic shock with low cardiac output. Pregnancy.
Special Precautions
Patient with uncontrolled hypertension, severe asthma or COPD, cardiac disease, arrhythmias, atherosclerosis, vascular disease (cerebral or peripheral), electrolyte and fluid disturbances. Renal impairment (especially chronic renal failure). Lactation.
Adverse Reactions
Significant: QT interval prolongation, ventricular arrhythmias (including Torsade de pointes), cutaneous ischaemia and necrosis.
Cardiac disorders: Tachycardia, bradycardia, pulmonary oedema, dyspnoea.
Gastrointestinal disorders: Intestinal ischaemia, abdominal cramps, diarrhea, nausea, vomiting.
Metabolism and nutrition disorders: Rarely, hyponatraemia, hyperglycaemia.
Nervous system disorders: Convulsion, headache.
Reproductive system and breast disorders: Uterine ischaemia.
Respiratory, thoracic and mediastinal disorders: Bronchospasm, respiratory failure.
Vascular disorders: Hypertension, hypotension, pallor.
MonitoringParameters
Monitor blood pressure, heart rate, serum creatinine, and electrolytes (e.g. Na/K concentrations) daily.
Overdosage
Symptoms: Acute hypertensive crisis, bradycardia. Management: Symptomatic and supportive treatment with a vasodilator-type α-blocker (e.g. clonidine) and atropine.
Drug Interactions
Increases the hypotensive effect of non-selective β-blockers. Concomitant use of drugs known to induce bradycardia (e.g. propofol, sufentanil) may lower heart rate and cardiac output. May trigger ventricular arrhythmias, including Torsade de pointes, when used with drugs that can prolong QT interval (e.g. class IA and III antiarrhythmics, erythromycin, certain antihistamines and TCAs), or with drugs that may cause hypokalaemia or hypomagnesaemia.
Action
Description: Terlipressin, an inactive prodrug, is converted via enzymatic cleavage to lysine-vasopressin. The active vasopressin selectively causes splanchnic and extrarenal vasoconstriction by stimulation of V1 receptors on vascular smooth muscle, thereby reducing splanchnic blood flow and portal pressure. It also increases systemic mean arterial pressure and decrease heart rate. It has minimal action on V2 receptors responsible for its antidiuretic effects.
Duration: 4-6 hours.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: Approx 2 hours.
Distribution: Volume of distribution: Approx 0.5 L/kg.
Metabolism: Almost completely metabolised in the liver and kidneys by endo- and exopeptidases.
Excretion: Via urine (<1% as unchanged drug and <0.1% as lypressin). Elimination half-life: 50-80 minutes.
Chemical Structure

Chemical Structure Image
Terlipressin

Source: National Center for Biotechnology Information. PubChem Database. Terlipressin, CID=72081, https://pubchem.ncbi.nlm.nih.gov/compound/Terlipressin (accessed on Jan. 23, 2020)

Storage
Solution for inj: Store between 2-8°C. Powder for solution for inj: Store below 25°C. Protect from light.
MIMS Class
ATC Classification
H01BA04 - terlipressin ; Belongs to the class of vasopressin and analogues. Used in posterior pituitary lobe hormone preparations.
References
Anon. Terlipressin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 27/10/2017.

Buckingham R (ed). Terlipressin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/10/2017.

Joint Formulary Committee. Terlipressin Acetate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/10/2017.

Disclaimer: This information is independently developed by MIMS based on Terlipressin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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