Glypressin Injection

1. Name Of The Medicinal Product

Glypressin^® Injection

2. Qualitative And Quantitative Composition

Each vial contains 1mg Terlipressin Acetate

For excipients, see 6.1

3. Pharmaceutical Form

Powder and solvent for solution for injection

Vial contains white, freeze-dried powder.

Ampoule contains solvent.

4. Clinical Particulars

4.1 Therapeutic Indications

Glypressin^® is indicated in the treatment of bleeding oesophageal varices.

4.2 Posology And Method Of Administration

In acute variceal bleeding, 2mg Glypressin^® should be administered by intravenous bolus, followed by 1 - 2mg every 4 - 6 hours until bleeding is controlled, up to a maximum of 72 hours.

Administration is by intravenous injection.

4.3 Contraindications

Pregnancy

4.4 Special Warnings And Precautions For Use

Since Glypressin^® has antidiuretic and pressor activity it should be used with great caution in patients with hypertension, atherosclerosis, cardiac dysrhythmias or coronary insufficiency. Constant monitoring of blood pressure, serum sodium and potassium and fluid balance is essential.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

None known

4.6 Pregnancy And Lactation

Glypressin^® may stimulate contraction of smooth muscle and is therefore contraindicated in pregnancy. There is no data concerning its use in lactation.

4.7 Effects On Ability To Drive And Use Machines

Not applicable

4.8 Undesirable Effects

Glypressin^® is only recommended for the short-term treatment of bleeding oesophageal varices, so few side effects have been reported. Those noted have included abdominal cramps, headache, transient blanching and increased arterial blood pressure.

4.9 Overdose

Increase in blood pressure in patients with known hypertension has been controlled with clonidine, 150mcg iv.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

Glypressin^® may be regarded as a circulating depot of lysine vasopressin. Following intravenous injection, three glycyl moieties are enzymatically cleaved from the N-terminus 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.

5.2 Pharmacokinetic Properties

Glypressin^® is administered by bolus iv injection. It shows a biphasic plasma level curve which indicates that a two compartment model can be applied.

The half-life of distribution is about 8 -10 minutes.

The half-life of elimination is about 50 -70 minutes.

Lysine vasopressin reaches maximum plasma levels about 1 - 2 hours following iv administration and has a duration of activity of 4 - 6 hours.

5.3 Preclinical Safety Data

There are no pre-clinical data of relevance to the prescriber which are additional to that already included in other sections of the SPC.

6. Pharmaceutical Particulars

6.1 List Of Excipients

Vial:

Mannitol

Hydrochloric Acid 1M

Solvent Ampoule:

Sodium Chloride

Hydrochloric Acid 1M

Water for Injection

6.2 Incompatibilities

None known

6.3 Shelf Life

36 months

6.4 Special Precautions For Storage

Do not store above 25ºC. Keep container in the outer carton.

6.5 Nature And Contents Of Container

Powder: Type I glass vial

Solvent: Type I glass ampoule

Pack size: Cartons containing 5 packs, each with one vial of powder and one ampoule of 5ml solvent.

6.6 Special Precautions For Disposal And Other Handling

Prior to injection, the powder should be reconstituted with the solvent provided. Use immediately after reconstitution.

7. Marketing Authorisation Holder

Ferring Pharmaceuticals Limited, The Courtyard, Waterside Drive, Langley, Berkshire SL3 6EZ (UK)

8. Marketing Authorisation Number(S)

PL 3194/0018

9. Date Of First Authorisation/Renewal Of The Authorisation

18^th July 2001

10. Date Of Revision Of The Text

June 2002

11. Legal Category

POM