GLUKO

CHARACTERISTICS’ SUMMARY OF PRODUCT/

SCIENTIFIC INFORMATION DATA SHEET

1. DENOMINATION OF MEDICAL SPECIALITY:

GLUKO
“300mg/3ml powder and solvent for injectable solution” 10 powder vials 300 mg + 10 solvent vials 3 ml
“600mg/4ml powder and solvent for injectable solution” 10 powder vials 600 mg + 10 solvent vials 4 ml

Glutathione

2. QUALITATIVE AND QUANTITATIVE COMPOSITION

10 VIALS OF LYOPHILIZED POWDER 300 MG + 10 SOLVENT VIALS 3 ML

1 vial of lyophilized contains:

Active principle:
Reduced Glutathione g 0,3
Excipients:
Sodium hydroxide mg 40

1 solvent vial contains:

Water for injectable preparations ml 3

10 VIALS OF LYOPHILIZED POWDER 600 MG + 10 SOLVENT VIALS 4 ML

1 vial of lyophilized contains:

Active principle:
Reduced Glutathione g 0,6
Excipients:
Sodium hydroxide mg 80

1 solvent vial contains:

Water for injectable preparations ml 4

3. PHARMACEUTICAL FORM

Lyophilized powder + solvent.

4. CLINICAL INFORMATION

4.1 Therapeutic indications

Prophylaxis of neuropathy resulting from chemotherapy treatment with cisplatin or similar.

4.2 Recommended dosage and method of administration

In mild cases: 1-2 vials daily of Gluko 300 intramuscularly or slow intravenous or according to different medical pre-
scription.
In most challenging cases: 1-2 vials daily of Gluko 600 intramuscularly or slow intravenous or added to drip or accor-
ding to medical prescription.
4.3 Contraindications

Individual ascertained hypersensitivity to the drug.

4.4 Special warnings and precautions

Keep out of reach of children.

4.5 Interactions with other medicines and other interaction forms

In literature are not described cases of medicinal interactions and specific incompatibility with glutathione.

4.6 Pregnancy and lactation

Although experimental research hasn’t shown embryo-fetal toxicity for the glutathione, is not recommended its use
during pregnancy and lactation.

4.7 Effects on ability to drive and use machines

None.

4.8 Side effects

May occur very rarely skin rashes that disappear by suspending therapy.

4.9 Overdose

In literature are not described cases of overdose.

5. PHARMACOLOGICAL PROPERTIES

5.1 Pharmacodynamic properties

Il glutathione is a tripeptide widely distributed in nature; at the cellular level is present in the cytosol. It’s linked to a
wide variety of cellular biochemical functions.
The sulphydryl group of glutathione’s cysteinyl part is strongly nucleophilic and therefore it represents a primary
target of electrophilic attack by chemical substances or their reactive metabolites with consequent protection of vital
nucleophilic sites, which attack would begin a process of cellular damage. In fact, glutathione reacts with a big variety
of oxidized organic metabolites, giving rise to less toxic conjugates compounds which can be more easily and further
metabolized and eliminated as mercapturic acids. Various factors can modify and decrease the cellular levels of gluta-
thione, like malnutrition, various diseases, as well chemical substances and medicines. Glutathione has been shown to
have protective effects in animals and humans on the cellular toxicity of many substances, like salicylic, paracetamol,
diethylmaleate, ethacrynic acid, phenobarbital, organo-phosphate insecticides, antineoplastic, ethyl alcohol, acid pe-
nicillata and others. Glutatihone hasn’t shown in animals in vivo effects on intestinal mobility, sistemic blood pression,
breath and electrocardiogram.
5.2 Pharmacokinetic properties

Glutathione S35 administered intravenously in the rat presents the maximum concentration in plasma at the 5th hour:
it’s present, especially in the 1st hour, in kidneys, liver, muscles and in small amounts in the brain. At the 24th hour the
quantities present are halved.

5.3 Preclinical safety data

Acute toxicity: In rats and mice, doses of 5000 mg/kg of glutathione sodiun by slow intravenous infusion (5 ml/minu-
te) do not cause death. In rabbit, doses of 3000 mg/kg are well tolerated. By intraperitoneal, in mice and rat doses of
7500 mg/kg do not cause death.
Subacute and chronic toxicity: Doses of 500 mg/kg/die and 1000 mg/kg/die by intravenous for 28 days in the rabbit
didn’t induce any particular symptoms. Rats treated for 120 days at doses of 43,86 and 129 mg/kg intraperitoneally
have not suffered any adverse effect on both the biochemical constants and various parenchyma. Dogs treated for 90
days at doses of 86 and129 mg/kg/die by intravenous at the end of the experiment showed no particular symptoms or
variations of biochemical constants or defects in the major parenchyma from the histomorphological point of view.
Teratogenicity: From tests conducted on the Wister rat and New Zealand rabbit at the dose of 86 mg/kg/die, glutathio-
ne did not affect negatively the reproductive function, growth and lactation of births.
Local tolerability: during the intravenous and intraperitoneal injections, or during instillations into the conjunctival
sac (eyewash) there were no facts of irritation, even after chronic administration.

6. PHARMACEUTICAL INFORMATION

6.1 List of excipients

Sodium hydroxide, water for injectable preparation.

6.2 Incompatibility

None.

6.3 Validity

3 years in unopened box.

6.4 Special precautions for the conservation

None.

6.5 Nature and content of container and price

For the active principle: glass vials with chlorobutyl rubber undercap and aluminium cap containing 300 and 600 mg
of active principle in lyophilized powder form.
For the excipients: glass vials containing 3 and 4 ml of water for injectable preparation.
- Pack of 10 FL LIOF. 300 MG + 10 F SOLV. 3 ML
- Pack of 10 FL LIOF. 600 MG + 10 F SOLV. 4 ML

6.6 Instructions for use

Please see item 4.2

7. HOLDER OF THE AUTORIZATION FOR THE MARKETING

TRENDFARMA Srl – Rome

8. NUMBER OF AUTORIZATION FOR THE MARKETING

GLUKO 300 - AIC n.: 028403032

GLUKO 600 - AIC n.: 028403044

9. DATE OF FIRT AUTORIZATION / AUTORIZATION RENOWAL

01-04-1993 / 01-04-2008

10. DATE OF TEXT REVIEW:

01-04-2008
www.trendfarma.it