Lexpec 2.5mg/5ml Oral Solution
SUMMARY OF PRODUCT CHARACTERISTICS
1 NAME OF THE MEDICINAL PRODUCT
Lexpec 2.5mg/5ml Oral Solution
2 QUALITATIVE AND QUANTITATIVE COMPOSITION
Folic Acid 2.5mg/5ml
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
This product contains hydroxybenzoate esters, which may cause allergic reactions (possibly delayed).
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.
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.
6.1 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
6.6 Special precautions for disposal
Not applicable
7 MARKETING AUTHORISATION HOLDER
Rosemont Pharmaceuticals Ltd
Rosemont House
Yorkdale Industrial Park
Braithwaite Street
Leeds
LS11 9XE
UK
8 MARKETING AUTHORISATION NUMBER(S)
PL 00427/0034
9 DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION
30/10/74
10 DATE OF REVISION OF THE TEXT
29/07/2013