INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo LEUCOVORIN-FAULDING 3 MG/ML (Injection)
LEUCOVORIN-FAULDING 10 MG/ML (Injection)

SCHEDULING STATUS:
S1

PROPRIETARY NAME
(and dosage form)

LEUCOVORIN-FAULDING 3 MG/ML (Injection)
LEUCOVORIN-FAULDING 10 MG/ML (Injection)

COMPOSITION
LEUCOVORIN-FAULDING 3 MG/ML: Each 1 mL contains
leucovorin 3,0 mg (as leucovorin calcium 3,24 mg).
LEUCOVORIN-FAULDING 10 MG/ML: Each 1 mL contains leucovorin 10,0 mg as (leucovorin calcium 10,8 mg)

PHARMACOLOGICAL CLASSIFICATION
A 8.3 Erythropoietics (haematinics)

PHARMACOLOGICAL ACTION
Leucovorin is the 5-formyl derivate of tetrahydrofolic acid, the active form of folic acid, which is a coenzyme for various metabolic processes, including the synthesis of purine and pyrimidine nucleotides and thymidylate and hence in the synthesis of DNA.

INDICATIONS
Calcium Leucovorin Rescue: Calcium leucovorin may be used in conjunction with folic acid antagonists, e.g. methotrexate and pyrimethamine to circumvent the action of inhibitors of dihydrofolate reductase. Leucovorin is also used in cases of inadvertent overdosage of the folic acid antagonists.
Megaloblastic anaemia due to folate deficiency.
Leucovorin is also used to enhance the cytotoxic effect of fluorouracil in advanced colorectal cancer.

CONTRA-INDICATIONS
Hypersensitivity to leucovorin.
Calcium leucovorin is contra-indicated in the treatment of pernicious anaemia or other megaloblastic anaemias secondary to a deficiency of vitamin B12.

WARNINGS
Leucovorin enhances the toxicity of 5-fluorouracil. When these two agents are administered concurrently in the palliative therapy of advanced colorectal cancer, the dosage of 5-fluorouracil must be lower than usually administered. Although the toxicities observed in patients treated with the combination of leucovorin and 5-fluorouracil are qualitatively similar to those observed in patients treated with 5-fluorouracil alone, gastrointestinal toxicities are observed more commonly and may be more severe and of prolonged duration in patients treated with the combination.
Therapy with leucovorin/5-fluorouracil must not be initiated or continued in patients who have symptoms of gastrointestinal toxicity of any severity, until those symptoms have completely resolved. Patients with diarrhoea must be monitored with particular care until the diarrhoea has resolved, as rapid clinical deterioration leading to death can occur. Elderly or debilitated colorectal cancer patients are at increased risk of severe toxicity.

DOSAGE AND DIRECTIONS FOR USE
Leucovorin can be administered intramuscularly or by intravenous injection or infusion. The dosage and route will often depend on the circumstances it is being employed for.

In cases of inadvertent overdosage of a folic acid antagonist, leucovorin should be administered as soon as possible and preferably within the first hour; if a period of more than 4 hours intervenes, the treatment may not be effective. Leucovorin may be given by intravenous infusion in a dose equivalent to 75 mg of folinic acid within 12 hours, followed by 12 mg intramuscularly every 6 hours for 4 doses. In less severe overdosage 6 to 12 mg of leucovorin intramuscularly every 6 hours for 4 doses may be adequate.

When used in conjunction with methotrexate to reduce the toxicity of the methotrexate: leucovorin is given after an appropriate interval usually of up to 24 hours has elapsed for methotrexate to exert its antineoplastic effect. Doses of up to 150 mg have been given over 12 to 24 hours, by intramuscular injection or intravenous injection or infusion, followed by 12 to 15 mg intramuscularly every six hours for the next 48 hours.

Leucovorin is also used to enhance the cytotoxic effect of fluorouracil in advanced colorectal cancer. Suggested doses are 200 mg per m2body-surface by slow intravenous injection over at least 3 to 5 minutes followed by fluorouracil at an initial dose of 370 mg per m2intravenously; the treatment is given daily for 5 consecutive days and may be repeated at intervals of 21 to 28 days.

For the treatment of folate-deficient megaloblastic anaemia, doses of not greater than 1 mg intramuscularly have been suggested.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS
Hypersensitivity reactions have been reported, pyrexia has occurred.
Leucovorin should not be administered simultaneously with a folic acid antagonist as this may nullify the effect of the antagonist.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
See “SIDE-EFFECTS AND SPECIAL PRECAUTIONS”.
Treatment is symptomatic and supportive.

IDENTIFICATION
LEUCOVORIN-FAULDING 3 MG/ML: Clear, straw to pale yellow solution, free from particulate matter.
LEUCOVORIN-FAULDING 10 MG/ML: Clear, straw to pale yellow solution, free from particulate matter.

PRESENTATION
LEUCOVORIN-FAULDING 3 MG/ML: 1 mL amber glass ampoules.
LEUCOVORIN-FAULDING 10 MG/ML: 5 mL clear glass vials.

STORAGE INSTRUCTIONS
Store between 2°C and 8°C. Refrigerate, do not freeze. Protect from light.
KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBER
LEUCOVORIN-FAULDING 3 MG/ML: 29/8.3/0358
LEUCOVORIN-FAULDING 10 MG/ML: 29/8.3/0359

NAME AND BUSINESS ADDRESS OF APPLICANT
Pharmaplan (Pty) Ltd
106 16thRoad
Midrand

DATE OF PUBLICATION OF THIS PACKAGE INSERT
9 January 1996

New addition to this site: May 2014
Source: Pharmaceutical Industry

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