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ESKAZOLE TABLETS 200MG

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SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
Eskazole Tablets 200 mg

2

QUALITATIVE AND QUANTITATIVE COMPOSITION
Albendazole 200 mg

3

PHARMACEUTICAL FORM
Tablet

4

CLINICAL PARTICULARS

4.1

Therapeutic indications
Eskazole is a benzimidazole carbamate anthelmintic for use in the treatment of
hydatid cysts caused by:
Echinococcosis
Eskazole shows greatest efficacy in the treatment of liver, lung and peritoneal
cysts. Experience with bone cysts and those in the heart and central nervous
system is limited.
Cystic Echinococcosis (caused by Echinococcus granulosus)
Eskazole is used in patients with cystic echinococcosis:
1. where surgical intervention is not feasible.
2. prior to surgical intervention.
3. post-operatively if pre-operative treatment was too short, if spillage has
occurred or if viable material was found at surgery.
4. following percutaneous drainage of cysts for diagnostic or therapeutic
reasons.
Alveolar Echinococcosis (caused by Echinococcus multilocularis)
Eskazole is used in patients with alveolar echinococcosis:
1. in inoperable disease, particularly in cases of local or distant
metastasis.
2. following palliative surgery.

3. following radical surgery or liver transplantation.

4.2

Posology and Method of Administration
Route of administration: Oral.
Dosage: Dosages are dependent on the parasite involved, the weight of the
patient, and the severity of the infection:
Cystic Echinococcosis
Patients weighing >60 kg
Total daily dose: 800 mg given in two divided doses of 400 mg for a total of
28 days.
Patients weighing <60 kg
Total daily dose: 12 mg/kg given in two equally divided doses (maximum
dose 800 mg/day) as above.
This 28-day treatment period may be repeated after a 14-day period without
treatment for a total of three cycles.
Alveolar Echinococcosis
Patients weighing >60 kg
Total daily dose: 800 mg given in two equally divided doses for cycles of 28
days with 14 days between cycles.
Patients weighing <60 kg
Total daily dose: 12 mg/kg given in two equally divided doses (maximum
dose 800 mg/day) as above.
Treatment may need to be prolonged for months or years. Continuous
treatment at the same dose has been used for periods of up to 20 months.
Method of administration
Albendazole should be taken with meals. Some people, particularly young
children, may experience difficulties swallowing the tablets whole and should
be encouraged to chew the tablets with a little water, alternatively tablets may
be crushed.

Cystic Echinococcosis
1. Inoperable and multiple cysts
Up to three 28-day cycles of albendazole may be given for the
treatment of liver, lung and peritoneal cysts. More prolonged
treatment may be required for sites such as bone and brain.
2. Pre-operative
Two 28-day cycles should be given where possible prior to surgery.

Where surgical intervention is necessary before completion of two
cycles, albendazole should be given for as long as possible.
3. Post-operative
Where only a short pre-operative course has been given (less than 14
days) and in cases where emergency surgery is required, albendazole
should be given post-operatively for two 28-day cycles separated by 14
drug-free days.
Additionally, where cysts are found to be viable following pre-surgical
treatment or where spillage has occurred, a full two-cycle course
should be given.
4. After percutaneous cyst drainage.
Treatment as for post-surgery above.
Alveolar Echinococcosis
Treatment is normally given in 28 day cycles as for cystic echinococcosis. It
may have to be continued for months or even years. Current follow up
suggests that survival times are substantially improved following prolonged
treatment. Continuous treatment has been shown in a limited number of
patients to lead to apparent cure.
Special Populations
Children
There has been limited experience to date with the use of albendazole in
children under six years of age; therefore, usage in children less than six years
is not recommended. The recommended dose for older children is 12 mg/kg
body weight/day in divided doses.
Elderly
Experience in patients 65 years of age or older is limited. Reports indicate that
no dosage adjustment is required; however, albendazole should be used with
caution in elderly patients with evidence of hepatic dysfunction (see ‘Hepatic
impairment’ below and ‘5.2 Pharmacokinetic Properties’).
Renal impairment
Since renal elimination of albendazole and its primary metabolite, albendazole
sulfoxide, is negligible, it is unlikely that clearance of these compounds would
be altered in these patients. No dosage adjustment is required; however,
patients with evidence of renal impairment should be carefully monitored.
Hepatic impairment
Since Albendazole is rapidly metabolised by the liver to the primary
pharmacologically active metabolite, albendazole sulfoxide, hepatic
impairment would be expected to have significant effects on the
pharmacokinetics of albendazole sulfoxide. Patients with abnormal liver
function test results (transaminases) prior to commencing albendazole therapy
should be carefully evaluated and therapy should be discontinued if liver

enzymes are significantly increased or full blood count decreased by a
clinically significant level (see ‘4.4 Special Warnings and Precautions for Use’
and ‘4.8 Undesirable Effects’).

4.3

Contraindications
Albendazole should not be administered during pregnancy or in women
thought to be pregnant. Women of childbearing age should be advised to take
effective precautions, with non hormonal contraceptive measures, against
conception during and within one month of completion of treatment with
Eskazole.
Albendazole is contra-indicated in patients with a known history of
hypersensitivity to Eskazole (albendazole or constituents).

4.4

Special Warnings and Precautions for Use
Albendazole has been associated with mild to moderate elevations of hepatic
enzymes. Hepatic enzymes generally normalise on discontinuation of
treatment. Case reports of hepatitis have also been received (see ‘4.8
Undesirable Effects’). Liver function tests should be obtained before the start
of each treatment cycle and at least every two weeks during treatment. If
hepatic enzymes are significantly increased (greater than twice the upper limit
of normal), albendazole should be discontinued. Treatment may be restarted
when hepatic enzymes have returned to normal limits, but patients should be
carefully monitored for recurrence.
Albendazole has been shown to cause bone marrow suppression and therefore
blood counts should be performed at the start and every two weeks during
each 28-day cycle. Patients with liver disease, including hepatic
echinococcosis, appear to be more susceptible to bone marrow suppression
leading to pancytopenia, aplastic anaemia, agranulocytosis and leucopenia and
therefore warrant closer monitoring of blood counts. Albendazole should be
discontinued if clinically significant decreases in blood cell counts occur (see
‘4.2 Posology and Method of Administration’ and ‘4.8 Undesirable Effects’).
Precautions:
In order to avoid administering albendazole during early pregnancy, women of
childbearing age should:
- initiate treatment only after a negative pregnancy test. These tests should
be repeated at least once before initiating the next cycle.
- be advised to take effective precautions against conception during and
within one month of completion of treatment with albendazole for a
systemic infection.

Symptoms associated with an inflammatory reaction following death of the
parasite may occur in patients receiving albendazole treatment for
neurocysticercosis (e.g. seizures, raised intracranial pressure, focal signs).
These should be treated with appropriate steroid and anticonvulsant therapy.
Oral or intravenous corticosteroids are recommended to prevent cerebral
hypertensive episodes during the first week of treatment.
Pre-existing neurocysticercosis may also be uncovered in patients treated with
albendazole for other conditions, particularly in areas with high taenosis
infection. Patients may experience neurological symptoms e.g. seizures,
increased intracranial pressure and focal signs as a result of an inflammatory
reaction caused by death of the parasite within the brain. Symptoms may
occur soon after treatment, appropriate steroid and anticonvulsant therapy
should be started immediately.

4.5

Interactions with other Medicaments and other Forms of Interactions
Albendazole has been shown to induce liver enzymes of the cytochrome P450
system responsible for its own metabolism.
Drugs that can reduce the effectiveness of albendazole – monitor effect - other
dose regimens or therapies may be required.
• Anticonvulsants (eg phenytoin: fosphenytoin: carbamazepine:
phenobarbital: primidone)
• Levamisole
• Ritonavir
Drugs that may increase levels of the active metabolite of albendazole –
monitor to possible increased albendazole adverse effects.
• Cimetidine
• Dexamethasone (continuous use raises albendazole levels by 50%)
• Praziquantel
Grapefruit juice also increases the plasma levels of albendazole sulfoxide.
Other possible interactions
Because of possible alterations in cytochrome P450 activity, there is a
theoretical risk of an interaction with the following
• Oral contraceptives
• Anticoagulants
• Oral hypoglycaemics
• Theophylline
Care should be exercised when albendazole is given to patients taking these
medicines.

4.6

Pregnancy and lactation
Pregnancy:
Eskazole should not be administered during pregnancy or in women thought to
be pregnant (see contra-indications).
Lactation:
It is not known whether albendazole or its metabolites are secreted in human
breast milk. Thus Eskazole should not be used during lactation unless the
potential benefits are considered to outweigh the potential risks associated
with treatment.

4.7

Effects on ability to drive and use machines
Dizziness is reported as a common reaction. Patients should be advised that if
affected they should not drive, operate machinery or take part in activities
where this could put them or others at risk.

4.8

Undesirable effects
Data from large clinical studies were used to determine the frequency of very
common to rare undesirable reactions. The frequencies assigned to all other
undesirable reactions (i.e. those occurring at < 1/1000) were mainly
determined using post-marketing data and refer to a reporting rate rather than a
true frequency.
The following convention has been used for the classification of frequency:
Very common
≥1/10
Common
≥1/100 and <1/10
Uncommon
≥ 1/1000 and < 1/100
Rare
≥ 1/10,000 and < 1/1000
Very rare
< 1/10,000
Blood and the lymphatic system disorders
Uncommon:
Leucopenia
Very rare:
Pancytopenia, aplastic anaemia, agranulocytosis
Patients with liver disease, including hepatic echinococcosis, appear to be
more susceptible to bone marrow suppression (see ‘4.2 Posology and Method
of Administration’ and ‘4.4 Special Warnings and Precautions for Use’).
Immune system disorders
Uncommon:
Hypersensitivity reactions including rash, pruritus and
urticaria
Nervous system disorders
Very common: Headache
Common:
Dizziness

Gastrointestinal disorders
Common:
Gastrointestinal disturbances (abdominal pain, nausea,
vomiting)
Gastrointestinal disturbances have been associated with albendazole when
treating patients with echinococcosis.
Hepato-biliary disorders
Very common: Mild to moderate elevations of hepatic enzymes
Uncommon:
Hepatitis
Skin and subcutaneous tissue disorders
Common:
Reversible alopecia (thinning of hair, and moderate hair loss)
Very rare:
Erythema multiforme, Stevens-Johnson syndrome
General disorders and administrative site conditions
Common:
Fever

4.9

Overdose
In case of overdosage, symptomatic therapy (gastric lavage) and general
supportive measures should be undertaken.

5

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties
Albendazole is a benzimidazole carbamate with anthelmintic effects against
tissue parasites.
Albendazole exhibits larvicidal, ovicidal and vermicidal activity, and it is
thought to exert its anthelmintic effect by inhibiting tubulin polymerisation.
This causes the disruption of the helminth metabolism, including energy
depletion, which immobilises and then kills the susceptible helminth.
Albendazole is effective in the treatment of tissue parasites including cystic
echinococcosis and alveolar echinococcosis caused by infestation of
Echinococcus granulosus and Echinococcus multilocularis, respectively.
In the treatment of cysts due to E. multilocularis, a minority of patients were
considered to be cured and a majority had an improvement or stabilisation of
disease due to albendazole.

5.2

Pharmacokinetic properties
Absorption and metabolism
In man, albendazole is poorly absorbed (<5%) following oral administration.
Albendazole rapidly undergoes extensive first-pass metabolism in the liver,
and is generally not detected in plasma. Albendazole sulfoxide is the primary
metabolite, which is thought to be the active moiety in effectiveness against
systemic tissue infections. The plasma half-life of albendazole sulfoxide is 8½
hours.
Following oral administration of a single dose of 400 mg albendazole, the
pharmacologically active metabolite, albendazole sulfoxide, has been reported
to achieve plasma concentrations from 1.6 to 6.0 micromol/litre when taken
with breakfast. The systemic pharmacological effect of albendazole is
augmented if the dose is administered with a fatty meal, which enhances the
absorption by approximately 5-fold.
Excretion
Albendazole sulfoxide and its metabolites appear to be principally eliminated
in bile, with only a small proportion appearing in the urine. Elimination from
cysts has been shown to occur over several weeks following high and
prolonged dosing.
Special Patient Populations
Elderly
Although no studies have investigated the effect of age on albendazole
sulfoxide pharmacokinetics, data in 26 hydatid cyst patients (up to 79 years)
suggest pharmacokinetics similar to those in young healthy subjects. The
number of elderly patients treated for either hydatid disease or
neurocysticercosis is limited, but no problems associated with an older
population have been observed.
Renal Impairment
The pharmacokinetics of albendazole in patients with impaired renal function
have not been studied.
Hepatic Impairment
The pharmacokinetics of albendazole in patients with impaired hepatic
function have not been studied.

5.3

Preclinical safety data
There are no pre-clinical data of relevance to the prescriber which are
additional to that already included in other sections of the SPC.

6

PHARMACEUTICAL PARTICULARS

6.1

List of excipients
Lactose
Maize starch
Polvinylpyrrolidone
Sodium lauryl sulphate
Sodium starch glycollate
Microcrystalline cellulose
Sodium saccharin
Magnesium stearate
Hydroxypropylmethylcellulose
Propylene glycol
Purified water

6.2

Incompatibilities
None

6.3

Shelf life
60 months

6.4

Special precautions for storage
No special storage precautions.

6.5

Nature and contents of container
Polypropylene 'Securitainer' with polyethylene lid, each pack containing 120
tablets

6.6

Special precautions for disposal
No special instructions

7

MARKETING AUTHORISATION HOLDER
Smith Kline & French Laboratories Ltd.

980 Great West Road
Brentford
Middlesex TW8 9GS

8

MARKETING AUTHORISATION NUMBER(S)
PL 00002/0201

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
13 August 2003

10

DATE OF REVISION OF THE TEXT
02/08/2011

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Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

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