Glypressin

Glypressin

terlipressin

Manufacturer:

Ferring

Distributor:

DCH Auriga - Universal
/
Four Star
Full Prescribing Info
Contents
Terlipressin.
Description
Each vial of powder contains terlipressin acetate 1 mg, corresponding to terlipressin 0.86 mg. It also contains the following excipients: Mannitol (E421) and hydrochloric acid (for pH-adjustment).
Each ampoule of solvent contains sodium chloride, hydrochloric acid (for pH-adjustment) and water for injection.
Action
Pharmacotherapeutic Group: Posterior pituitary lobe hormones (vasopressin and analogues). ATC Code: H01B A04.
Pharmacology: Pharmacodynamics: Glypressin may be regarded as a circulating depot of lysine vasopressin. Following IV injection, 3 glycyl moieties are enzymatically cleaved from the N-terminal to release lysine vasopressin.
The slowly released vasopressin reduces blood flow in the splanchnic circulation in a prolonged manner, thereby helping to control bleeding from ruptured oesophageal varices.
Pharmacokinetics: Glypressin is administered by bolus IV injection. It shows a biphasic plasma level curve which indicates that a 2 compartment model can be applied. The half-life of distribution (T½α) is about 8-10 min. The half-life of elimination (T½β) is about 50-70 min.
Lysine vasopressin reaches maximum plasma levels about 1-2 hrs following IV administration and has a duration of activity of 4-6 hrs.
Indications/Uses
Treatment of bleeding oesophageal varices.
Emergency treatment of type 1 hepatorenal syndrome, as defined by International Ascites Club (IAC) criteria.
Dosage/Direction for Use
Bleeding Oesophageal Varices: Adults: Initially, an IV injection of 2 mg every 4 hrs. The treatment should be maintained until bleeding has been controlled for 24 hrs, but up to a maximum of 48 hrs. After the initial dose, the dose can be adjusted to 1 mg IV every 4 hrs in patients with body weight <50 kg or if adverse effects occur.
Type 1 Hepatorenal Syndrome: 3-4 mg every 24 hrs as 3 or 4 administrations.
In the absence of any reduction of the serum creatinine after 3 days of treatment, cessation of Glypressin treatment is advised.
In the other cases, Glypressin treatment is to be pursued until the obtaining either of a serum creatinine <130 micromol/L or of a drop of at least 30% in the serum creatinine with respect to the value measured at the time of diagnosis of hepatorenal syndrome.
The standard average duration of treatment is 10 days.
Overdosage
The recommended dose (terlipressin acetate 2 mg/4 hrs) should not be exceeded as the risk of severe circulatory adverse effects is dose-dependent.
Elevated blood pressure in patients with hypertension can be controlled with clonidine 150 mcg IV. Severe bradycardia should be treated with atropine.
Contraindications
Hypersensitivity to terlipressin or to any other excipients of Glypressin.
Use in pregnancy & lactation: Treatment with Glypressin during pregnancy is contraindicated.
Glypressin has been shown to cause uterine contractions and increased intrauterine pressure in early pregnancy and may decrease uterine blood flow. Glypressin may have harmful effects on pregnancy and foetus.
Spontaneous abortion and malformation have been shown in rabbits after treatment with Glypressin.
Information on transfer of Glypressin to breast milk is insufficient. Glypressin should not be used in breastfeeding women.
Special Precautions
Blood pressure, heart rate and fluid balance should be monitored during treatment.
Caution should be exercised in treating patients with hypertension, recognised heart disease, renal dysfunction, cerebral or peripheral vascular disease, asthma or respiratory failure.
To avoid local necrosis at the injection site, the injection must be administered IV.
In patients with septic shock with a low cardiac output, terlipressin should not be used.
Prior to use of terlipressin for hepatorenal syndrome, it must be ascertained that the patient has an acute functional renal failure and this functional renal failure does not respond to a suitable plasma expansion therapy.
Effects on the Ability to Drive or Operate Machinery: No studies on the effects on the ability to drive and use machines have been performed.
Use in children and the elderly: Particular caution should be exercised in the treatment of children and elderly patients, as experience is limited in these groups.
There is no data available regarding dosage recommendation in these special patient categories.
Use In Pregnancy & Lactation
Treatment with Glypressin during pregnancy is contraindicated.
Glypressin has been shown to cause uterine contractions and increased intrauterine pressure in early pregnancy and may decrease uterine blood flow. Glypressin may have harmful effects on pregnancy and foetus.
Spontaneous abortion and malformation have been shown in rabbits after treatment with Glypressin.
Information on transfer of Glypressin to breast milk is insufficient. Glypressin should not be used in breastfeeding women.
Adverse Reactions
The most commonly reported adverse reactions in clinical trials (frequency 1-10%) are paleness, increased blood pressure, abdominal pain, nausea, diarrhoea and headache. (See table.)

Click on icon to see table/diagram/image
Drug Interactions
The hypotensive effect of nonselective β-blockers on the portal vein is increased with terlipressin. Concomitant treatment with medicinal products with a known bradycardic effect (eg, propofol, sufentanil) may lower the heart rate and cardiac output. These effects are due to reflexogenic inhibition of cardiac activity via the vagus nerve due to the elevated blood pressure.
Incompatibilities: In the absence of compatibility studies, Glypressin must not be mixed with other medicinal products.
Storage
Store at 15-25°C. Protect from light.
The reconstituted solution must be used immediately after reconstitution.
Shelf-Life: 3 years.
MIMS Class
ATC Classification
H01BA04 - terlipressin ; Belongs to the class of vasopressin and analogues. Used in posterior pituitary lobe hormone preparations.
Presentation/Packing
Inj 1 mg (vial, lyophilized powder) + 5 mL (diluent) x 1's.
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