QUALITATIVE AND QUANTITATIVE COMPOSITION
ZENTEL tablets 200mg
ZENTEL 100mg/5mL (2% liquid suspension)
Tablet: Circular, off white film – coated with pyramid shaped structure on both sides.
Suspension: A white homogeneous liquid suspension with a characteristic odour and flavour.
ZENTEL is a benzimidazole carbamate with anthelmintic and anti-protozoal activity against the following intestinal and tissue parasites: Roundworm (Ascaris lumbricoides), pinworm (Enterobius vermicularis), hookworm (Necator americanus, Ancylostoma duodenale), whip-worm (Trichuris trichiura), threadworm (Strongyloides stercoralis), tapeworm (Taenia spp and Hymenolepis nana only in the case of associated parasitism), Chlonorchiasis (Chlonorchis sinensis), Opisthorchiasis (Opisthorchis viverrini) and cutaneous larva migrans; Giardiasis (G.lambIia, G.duodenalis, G.intestinalis, Lamblia intestinalis) in children.
DOSAGE AND ADMINISTRATION
|Adults and children over 2 years of age||400 mg (two 200 mg or 20 mL 2% suspension]#||Single dose.|
|Children 1-2 years of age||200 mg (0ne 200 mg tablet or 10 mL 2% suspension)||Single dose|
|Adults and children over 2 years of age||400 mg (#see above)||Two doses per day for 3 days|
|Adults and children
over 2 years of age.
|400 mg (#see above)||Two doses per day for 3 days.|
|– Cutaneous larva migrans||Adults and children
over 2 years of age.
|400 mg (#see above)||One dose per day for 1 to 3 days.|
|– Giardiasis||Children 2 – 12 years of age only.||400 mg (#see above)||One dose per day for 5 days.|
*ln order to obtain a complete cure in the case of pinworm infestation, prescribe strict measures of hygiene, also treat the relatives and individuals sharing the same housing.
In cases of proven Hymenolepiasis, retreatment in 10 to 21 days is recommended.
Method of Administration
If the patient is not cured after three weeks, a second course of treatment is indicated.
No special procedures, such as fasting or purging, are required.
The tablets can be chewed or taken with water. 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 the tablets may be crushed.
Special Patient Populations
• Elderly: Experience in patients 65 years of age or older is limited. Reports indicate that no dosage adjustment is required, however, ZENTEL should be used with caution in elderly patients with evidence of hepatic dysfunction (see Hepatic Impairment and Pharmacokinetics).
• Renal Impairment: Since renal elimination of albendazole and its primary metabolite, azole 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 monitored.
ZENTEL should not be administered during pregnancy, or in women thought to be pregnant.
ZENTEL is contraindicated in patients with a known history of hypersensitivity to the drug (albendazole or constituents).
Warnings and Precautions
In order to avoid administering ZENTEL during early pregnancy, women of childbearing age should initiate treatment during the first week of menstruation or after a negative pregnancy test.
Treatment with ZENTEL may uncover pre-existing neurocysticercosis, 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.
ZENTEL suspension contains benzoic acid which is a mild irritant to the skin, eyes and mucous membrane. It may increase the risk of jaundice in newborn babies.
Praziquantel has been reported to increase the plasma levels of the albendazole active metabolite.
Ritonavir, phenytoin, carbamazepine and phenobarbital may have the potential to reduce plasma concentrations of the active metabolite of albendazole; albendazole sulfoxide. The clinical relevance of this is unknown, but may result in decreased efficacy, especially in the treatment of systemic helminth infections. Patients should be monitored for efficacy and may require alternative dose regimens or therapies.
Pregnancy and Lactation
Pregnancy: ZENTEL should not be administered during pregnancy or in women thought to be pregnant (see Contraindications).
Lactation: It is not known whether albendazole or its metabolites are secreted in human breast milk. Thus ZENTEL should not be used during lactation unless the potential benefits are considered to outweigh the potential risks associated with treatment.
Effects on Ability to Drive and Use Machines
Adverse effects on the ability to drive or operate machinery have not been observed.
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 to <1/10
Uncommon ≥1/1000 to < 1/100
Rare ≥1/10,000 to < 1/1000
Very rare < 1/10,000
Immune system disorders
Rare: Hypersensitivity reactions including rash, pruritis and urticaria.
Nervous system disorders
Uncommon: Headache and dizziness.
Uncommon: Upper gastrointestinal symptoms (e.g. epigastric or abdominal pain, nausea, vomiting) and diarrhoea.
Rare: Elevations of hepatic enzymes.
Skin and subcutaneous tissue disorders
Very rare: Erythema multiforme, Stevens-Johnson syndrome.
Treatment: Further management should be as clinically indicated or as recommended by the national poisons centre, where available.
Mechanism of Action
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, incIuding energy depletion, which immobilises and then kills the susceptible helminth.
In man, albendazole is poorly absorbed (less than 5%) following oral administration.
The-systemic pharmacological effect of albendazole is augmented if the dose is administered with a fatty meal, which enhances the absorption by approximately five fold.
Following oral administration of a single dose of 400 mg albendazole, the pharmacoIogical active metabolite, albendazole sulfoxide, has been reported to achieve plasma concentrations from 1.6 to 6.0 micromol/L when taken with breakfast.
Albendazole rapidly undergoes extensive first-pass metabolism in the liver, and is generally not detected in plasma. Albendazole suIfoxide is the primary metabolite, which is thought to be the active moiety in effectiveness against systemic tissue infections.
The plasma haIf-life of albendazole sulfoxide is 8.5 hours.
Albendazole suIfoxide and its metabolites appear to be principally eliminated in bile, with only a small proportion appearing in the urine.
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 has not been studied.
• Hepatic impairment: The pharmacokinetics of albendazole in patients with impaired hepatic function have not been studied.
List of Excipients
lactose, starch, povidone, sodium Iauryl sulphate, microcrystalline cellulose, sodium starch glycollate, trusil vanilla special, trusil orange special and magnesium
Film coating: HPMC 15, HPMC 5, diehloromethane, isopropyl alcohol and propylene glycol.
Sodium Iauryl sulphate, glycerol, methyl hydroxybenzoate, carmellose sodium, sorbitol (70%), orange flavor, passion fruit flavour, vanilla extra strong and purified water.
Use before the expiry date clearly indicated on the packaging.
Special Precautions for Storage
Tablets: Store below 30°C.
Suspensions: Store below 25°C and protect from direct sunlight.
Nature and Contents of Container
Albendazole tablets: 2’s in blister strips comprising a laminate of clear PVC and aluminium foil.
Albendazole suspension: Albendazole suspension 100mg/5mL packed in 28mL PVC resin bottle fitted with 22mm red colour PP cap.
Instructions for Use and Handling
Suspensions: Shake well before use.
Not all presentations are available in every country
KEEP OUT OF REACH OF CHILDREN
Further information is available on request.
Smithkline Beecham Pharmaceuticals
SmithKline Beecham SB House,
Brentford, TW8 9GS, U.K
ZENTEL is the trademark of GlaxoSmithKline Group of Companies
Pack insert Leaflet revised 23 April 2014. Version GA03
© 2014 GlaxoSmithKline
Avalahalli, Bangalore – 560 062, INDIA.