1. Name Of The Medicinal Product
Emeside Syrup (Blackcurrant)
2. Qualitative And Quantitative Composition
Ethosuximide 5% (250 mg/5 mL)
3. Pharmaceutical Form
Elixir for oral use.
4. Clinical Particulars
4.1 Therapeutic Indications
Emeside gives selective control of absence seizures (petit mal) even when complicated by grand-mal. It is also indicated for myoclonic seizures.
4.2 Posology And Method Of Administration
Adults, the Elderly and Children over 6 Years : Start with a small dose - 500mg daily with increments of 250mg every five to seven days until control is achieved with 1000 - 1500 mg daily. Occasionally 2000 mg in divided doses may be necessary.
Children and Infants under 6 years : Begin with a daily dose of 250 mg ( 5 ml ) and increase the dose gradually by small increments every few days until control is achieved. The optimal dose in most children is 20mg/Kg/day. The maximum dose should be 1000 mg.
Effective plasma levels of ethosuximide normally lie between 40 and 100 mcg per ml, but the clinical response should be the criteria for the regulation of the dosage. The half-life of ethosuximide in the plasma is more than 24 hours but the daily dose if large is more comfortably divided between morning and evening.
Larger children and adults will normally take Emeside in capsule form.
4.3 Contraindications
Known hypersensitivity to succinimides. Porphyrias.
4.4 Special Warnings And Precautions For Use
Use with caution in hepatic or renal impairment. Monitor liver/renal function and ethosuximide concentrations.
If Emeside is being substituted for another anti-epileptic drug the latter must not be withdrawn abruptly but the replacement made gradually with overlap of the preparations otherwise petit mal may break through.
Emeside should always be withdrawn slowly.
It is advisable to brush the teeth or rinse the mouth after taking Emeside syrup.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
The plasma concentrations of ethosuximide may be reduced by carbamazepine, primidone, phenobarbitone and lamotrigine and increased by isoniazide. No consistent changes in levels of ethosuximide occur when used in combination with phenytoin or sodium valproate.
Phenytoin levels however are increased by concomitant ethosuximide.
4.6 Pregnancy And Lactation
Ethosuximide may be excreted into breast milk. Mothers receiving the drug should not breast feed. There is a recognised small increase in the incidence of congenital malformations in children born to mothers receiving anti-convulsants. For women planning pregnancy or who are already pregnant the risk should be weighed carefully against the benefit of treatment.
4.7 Effects On Ability To Drive And Use Machines
Patients should be cautioned that ethosuximide may cause drowsiness and if this occurs should avoid driving or operating machinery.
4.8 Undesirable Effects
Blood dyscrasias (leucopoenia, agranulocytosis, aplastic anaemia, and pancytopaenia) have been reported, some with fatal outcome. In most cases of leucopoenia the blood picture has returned to normal on reduction of dose or discontinuation. In some instances, patients who become leucopenic on other anticonvulsant therapy have been satisfactorily treated with ethosuximide alone. Elevated neutrophil, monocyte and eosinophil counts have also been noted. Patients should be advised to seek immediate medical attention, for full blood count tests, if symptoms such as fever, sore throat, mouth ulcers, bruising or bleeding develop.
Ethosuximide when used alone in mixed types of epilepsy may increase the frequency of generalised tonic-clonic (grand mal) seizures in some patients.
Other adverse reactions reported include: weight loss, diarrhoea, abdominal pain, gum hypertrophy, swelling of the tongue, hiccoughs, irritability, hyperactivity, sleep disturbances, night terrors, inability to concentrate, aggressiveness, paranoid psychosis, increased libido, myopia, and vaginal bleeding.
Mild side effects, common at first but generally transient, include apathy, euphoria, fatigue, drowsiness, dizziness, headache, ataxia, dyskinesia, photophobia, depression and nausea, vomiting, anorexia, and gastric upset.
Psychotic states thought to be induced or exacerbated by anticonvulsant therapy have been reported.
Rarely cases of skin rash and isolated cases of erythema nodosum have been reported. Lupus-like reactions have occasionally been reported in children given ethosuximide, varying from severe systemic immunological disorders, eg the nephrotic syndrome generally with complete recovery on drug withdrawal, to the detection of antinuclear antibodies without clinical features. Stevens Johnson syndrome has also been reported.
4.9 Overdose
Where more than 2g has been thought to be ingested gastric lavage may be employed, if the time lapse is less than four hours. Routine observation of respiration and circulation will indicate the need for supportive measures.
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
Ethosuximide gives selective control of absence seizures (petit-mal) even when complicated by grand-mal. It is also indicated for myoclonic seizures. Compared to other anti-convulsants, ethosuximide is more specific for pure petit-mal.
The reduction of seizure frequency is thought to be achieved by depression of the motor cortex and elevation of the threshold to convulsive stimuli as seen by the suppression of the characteristic spike and wave EEG pattern.
5.2 Pharmacokinetic Properties
Ethosuximide is readily absorbed from the gastro-intestinal tract and extensively metabolised in the liver. It is excreted in the urine mainly in the form of its metabolites. It is widely distributed throughout the body but is not significantly bound to plasma proteins so saliva concentrations may be useful for monitoring. Peak serum levels occur 1 to 7 hours after single oral dose. Therapeutic levels are between 40 and 100 mcg/ml. It has a long elimination half-life: adults: 40 – 60 hours; children 30 hours.
5.3 Preclinical Safety Data
None stated.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Other Substances
Sucrose |
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Colouring, Flavouring and Perfume Compounds
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6.2 Incompatibilities
Carbamazepine, phenytoin, sodium valproate, or isoniazid.
6.3 Shelf Life
5 years.
6.4 Special Precautions For Storage
Store at ambient temperature.
6.5 Nature And Contents Of Container
200 ml amber glass bottle with plastic cap with polycone liner.
6.6 Special Precautions For Disposal And Other Handling
No special instructions
7. Marketing Authorisation Holder
Laboratories for Applied Biology Ltd
91, Amhurst Park
London
N 16 5 DR ML (UK) 0118/01
8. Marketing Authorisation Number(S)
UK PL 0118/5004R
9. Date Of First Authorisation/Renewal Of The Authorisation
Granted 01.11.90.
Renewed until 26.02.06
10. Date Of Revision Of The Text
05.10 99 Changes to 5.6 Interactions
19.09.00 Rearranged to current format
06.02.2001 Corrected and expanded: 4. Clinical Particulars and 5.2 Pharmacokinetics.
14.06.2001 Changes to 4.2 and 4.8.
11. Legal Category
Prescription only medicine.
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