LEXPEC 2.5 MG / 5ML ORAL SOLUTION - summary of medicine characteristics

1 NAME OF THE MEDICINAL PRODUCT

Lexpec 2.5mg/5ml Oral Solution

2. QUALITATIVE AND QUANTITATIVE COMPOSITION

Folic Acid 2.5mg/5ml

Excipient(s) with known effect:

Methyl hydroxybenzoate (E218) 3.5mg/5ml

Ethyl hydroxybenzoate (E214) 2.2mg/5ml

Propyl hydroxybenzoate (E216) 0.7mg/5ml

Propylene glycol (E1520) 14.5mg/5ml

Sodium 10.4mg/5ml

For excipients see section 6.1

3 PHARMACEUTICAL FORM

Oral Solution

4 CLINICAL PARTICULARS

4.1 Therapeutic indications

1. Folate deficient megaloblastic anaemia

2. Folate deficient megaloblastic anaemia in infants

3. Malabsorption syndromes

3.1 Tropical sprue

3.2 Coeliac disease

3.3 Non-tropical sprue

4. Megaloblastic anaemia in pregnancy

5. Megaloblastic anaemia associated with alcoholism

6. Megaloblastic anaemia associated with anti-convulsant therapy

7. Haemolytic anaemias e.g. Sickle Cell Anaemia

4.2 Posology and method of administration

For oral administration only.

Children:

May be given 5mg to 15mg daily, in divided doses, according to the severity of the deficiency state.

Adults:

Initial dose of 10mg to 20mg daily, in divided doses, for 14 days or until a haemopotoietic response has been obtained.

Maintenance dose is 2.5mg to 10mg daily.

Prophylactic dose in pregnancy 0.5mg (1ml) daily.

Elderly:

As for adults.

4.3 Contraindications

Known hypersensitivity to folic acid.

Known hypersensitivity to hydroxybenzoate esters.

Patients with folate dependent tumours.

Patients with malignant disease, unless megaloblastic anaemia due to folic acid deficiency.

4.4. Special warnings and precautions for use

If folic acid is used indiscriminately, there is a danger that patients with pernicious anaemia and other B12 deficiency states, despite a haematological remission, may develop irreparable neurological lesions. Therefore a full clinical diagnosis should be made before initiating treatment.

Folic acid is removed by haemodialysis.

Excipients in the Formulation

– Methyl and propyl hydroxybenzoates are contained in this product which may cause allergic reactions (possibly delayed).

– Propylene glycol (E1520) 14.5 mg in each 5ml. Co-administration with any substrate for alcohol dehydrogenase such as ethanol may induce serious adverse effects in neonates.

– This medicinal product contains 10.4 mg sodium per 5ml, equivalent to 0.5% of the WHO recommended maximum daily intake of 2 g sodium for an adult.

4.5 Interaction with other medicinal products and other forms of interaction

Antiepileptics – if folic acid supplements are given to treat folate deficiency, which can be caused by the use of antiepileptics (phenytoin, phenobarbital and primidone), the serum antiepileptic levels may fall, leading to decreased seizure control in some patients.

Antibacterials – chloramphenicol and co-trimoxazole may interfere with folate metabolism.

Sulfasalazine – can reduce the absorption of folic acid.

Folic acid may interfere with the toxic and therapeutic effects of methotrexate.

4.6 Fertility, pregnancy and lactation

There are no known hazards to the use of folic acid, indeed folic acid supplements are often necessary in pregnancy.

Folic acid is excreted in breast milk.

4.7 Effects on ability to drive and use machines

There are no known effects of this preparation on the ability to drive or use machines.

4.8. Undesirable effects

Allergic reactions to folic acid have been reported. Frequency not known: anaphylactic reaction.

Mild gastro-intestinal upsets are rare but may occur.

4.9 Overdose

No cases of acute overdosage appear to have been reported, but even extremely high doses are unlikely to cause harm to patients.

5 PHARMACOLOGICAL PROPERTIES

5.1 Pharmacodynamic properties

ATC Code: B03B B

After conversion into co-enzyme forms it is concerned in single carbon unit transfers in the synthesis of purines, pyrimidines and methionine.

5.2 Pharmacokinetic properties

About 70–80% of a 2mg oral solution of folic acid is absorbed. Larger doses are probably equally well absorbed. It is distributed into plasma and extracellular fluid. In plasma, folate is bound weakly to albumin (70%). There is a further high affinity binder for folate but this has a very low capacity and is barely detectable in normal sera. About 70% of small doses of folate (about 1mg) are retained and the rest excreted into the urine. With larger doses most is excreted into the urine. With a 5mg dose of folate, urinary excretion will be complete in about 5 hours. There is an enterohepatic circulation of folate. The retained folate is taken into cells and reduced by dihydrofolate to tetrahydrofolate. Folic acid is a relatively poor substrate for folate reduction, the normal substrate being dihydrofolate.

Folic acid itself does not occur in natural materials, it is entirely a pharmacological form of the compound. Once reduced, folate has additional glutamic acid residues added, a folate pentaglutamate being the dominant intracellular analogue. These polyglutamates are the active co-enzymes.

5.3 Preclinical safety data

Folic Acid is a drug on which extensive clinical experience has been obtained. Relevant information for the prescriber is provided elsewhere in the Summary of Product Characteristics.

6 PHARMACEUTICAL PARTICULARS

6.1 List of excipients

Mannitol (E421), glycerol (E422), methyl hydroxybenzoate (E218), ethyl hydroxybenzoate (E214), propyl hydroxybenzoate (E216), sodium dihydrogen phosphate, disodium hydrogen phosphate (E339), disodium ethylene diamine tetra acetic acid, strawberry flavour (containing propylene glycol E1520) and purified water

6.2 Incompatibilities

None stated

6.3 Shelf life

18 months

6.4 Special precautions for storage

Do not store above 25°C

6.5 Nature and contents of container

Bottle: Amber (Type III) glass with 150ml capacity

Closure: HDPE, EPE wadded, tamper evident, child resistant