Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/562
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ALBENZA (Tablet)
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Dosing of ALBENZA will vary, depending upon which
of the following parasitic infections is being treated. In young children,
the tablets should be crushed or chewed and swallowed with a drink
of water. Patients being treated for neurocysticercosis
should receive appropriate steroid and anticonvulsant therapy as required.
Oral or intravenous corticosteroids should be considered to prevent
cerebral hypertensive episodes during the first week of treatment.
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dailymed-instance:descripti... |
ALBENZA (albendazole) is an orally administered
broad-spectrum anthelmintic. Chemically, it is methyl 5-(propylthio)-2-benzimidazolecarbamate.
Its molecular formula is CHNOS. Its molecular weight is 265.34. It has the following
chemical structure: Albendazole
is a white to off-white powder. It is soluble in dimethylsulfoxide,
strong acids, and strong bases. It is slightly soluble in methanol,
chloroform, ethyl acetate, and acetonitrile. Albendazole is practically
insoluble in water. Each white to off-white, film-coated tablet contains
200 mg of albendazole. Inactive ingredients
consist of: carnauba wax, hypromellose, lactose monohydrate, magnesium
stearate, microcrystalline cellulose, povidone, sodium lauryl sulfate,
sodium saccharin, sodium starch glycolate, and starch.
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dailymed-instance:clinicalP... |
Pharmacokinetics:<br/>Absorption and Metabolism: Albendazole is poorly absorbed from the gastrointestinal
tract due to its low aqueous solubility. Albendazole concentrations
are negligible or undetectable in plasma as it is rapidly converted
to the sulfoxide metabolite prior to reaching the systemic circulation.
The systemic anthelmintic activity has been attributed to the primarymetabolite, albendazole sulfoxide. Oral bioavailability appears to
be enhanced when albendazole is coadministered with a fatty meal (estimated
fat content 40 g) as evidenced by higher (up to 5-fold on average)
plasma concentrations of albendazole sulfoxide as compared to the
fasted state. Maximal plasma concentrations
of albendazole sulfoxide are typically achieved 2 to 5 hours
after dosing and are on average 1.31 mcg/mL (range 0.46 to 1.58 mcg/mL)
following oral doses of albendazole (400 mg) in 6 hydatid disease
patients, when administered with a fatty meal. Plasma concentrations
of albendazole sulfoxide increase in a dose-proportional manner over
the therapeutic dose range following ingestion of a fatty meal (fat
content 43.1 g). The mean apparent terminal elimination half-life
of albendazole sulfoxide typically ranges from 8 to 12 hours
in 25 normal subjects, as well as in 14 hydatid and 8 neurocysticercosis
patients. Following 4 weeks of treatment with
albendazole (200 mg three times daily), 12 patients' plasma
concentrations of albendazole sulfoxide were approximately 20% lower
than those observed during the first half of the treatment period,
suggesting that albendazole may induce its own metabolism.<br/>Distribution: Albendazole sulfoxide is 70% bound to plasma protein
and is widely distributed throughout the body; it has been detected
in urine, bile, liver, cyst wall, cyst fluid, and cerebral spinal
fluid (CSF). Concentrations in plasma were 3- to 10-fold and 2- to
4-fold higher than those simultaneously determined in cyst fluid and
CSF, respectively. Limited in vitro and clinical data suggest
that albendazole sulfoxide may be eliminated from cysts at a slower
rate than observed in plasma.<br/>Metabolism and Excretion: Albendazole is rapidly converted in the liver to
the primary metabolite, albendazole sulfoxide, which is further metabolized
to albendazole sulfone and other primary oxidative metabolites that
have been identified in human urine. Following oral administration,
albendazole has not been detected in human urine. Urinary excretion
of albendazole sulfoxide is a minor elimination pathway with less
than 1% of the dose recovered in the urine. Biliary elimination presumably
accounts for a portion of the elimination as evidenced by biliary
concentrations of albendazole sulfoxide similar to those achieved
in plasma.<br/>Special Populations:<br/>Patients with Impaired Renal Function: The pharmacokinetics of albendazole in patients
with impaired renal function have not been studied. However, 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.<br/>Biliary Effects: In patients with evidence of extrahepatic obstruction
(n = 5), the systemic availability of albendazole sulfoxide
was increased, as indicated by a 2-fold increase in maximum serum
concentration and a 7-fold increase in area under the curve. The rate
of absorption/conversion and elimination of albendazole sulfoxide
appeared to be prolonged with mean Tand serum elimination
half-life values of 10 hours and 31.7 hours, respectively. Plasma
concentrations of parent albendazole were measurable in only 1 of
5 patients.<br/>Pediatrics: Following single-dose administration of 200 mg
to 300 mg (approximately 10 mg/kg) albendazole to 3 fasted
and 2 fed pediatric patients with hydatid cyst disease (age range
6 to 13 years), albendazole sulfoxide pharmacokinetics were similar
to those observed in fed adults.<br/>Elderly Patients: 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.<br/>Microbiology: The principal mode of action for albendazole is
by its inhibitory effect on tubulin polymerization which results in
the loss of cytoplasmic microtubules. In the
specified treatment indications albendazole appears to be active against
the larval forms of the following organisms: Echinococcus granulosus Taenia solium
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ALBENZA is contraindicated in patients with known
hypersensitivity to the benzimidazole class of compounds or any components
of ALBENZA.
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dailymed-instance:supply |
ALBENZA is supplied as 200 mg, white to off-white,
circular, biconvex, bevel-edged, film-coated TILTAB tablets in bottles
of 112. NDC 0007-5500-40 Bottles of 112 Store between 20��and 25��C (68��and 77��F). GlaxoSmithKline Research Triangle
Park, NC 27709 ALBENZA and TILTAB are registered
trademarks of GlaxoSmithKline. ��2007, GlaxoSmithKline.
All rights reserved. August 2007 ALB:6PI
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dailymed-instance:inactiveI... |
dailymed-ingredient:carnauba_wax,
dailymed-ingredient:hypromellose,
dailymed-ingredient:lactose_monohydrate,
dailymed-ingredient:magnesium_stearate,
dailymed-ingredient:microcrystalline_cellulose,
dailymed-ingredient:povidone,
dailymed-ingredient:sodium_lauryl_sulfate,
dailymed-ingredient:sodium_saccharin,
dailymed-ingredient:sodium_starch_glycolate,
dailymed-ingredient:starch
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dailymed-instance:precautio... |
General: Patients being treated for neurocysticercosis should
receive appropriate steroid and anticonvulsant therapy as required.
Oral or intravenous corticosteroids should be considered to prevent
cerebral hypertensive episodes during the first week of anticysticeral
therapy. Cysticercosis may, in rare cases,
involve the retina. Before initiating therapy for neurocysticercosis,
the patient should be examined for the presence of retinal lesions.
If such lesions are visualized, the need for anticysticeral therapy
should be weighed against the possibility of retinal damage caused
by albendazole-induced changes to the retinal lesion.<br/>Information for Patients: Patients should be advised that:<br/>Laboratory Tests:<br/>White Blood Cell Count: Albendazole has been shown to cause occasional (less
than 1% of treated patients) reversible reductions in total white
blood cell count. Rarely, more significant reductions may be encountered
including granulocytopenia, agranulocytosis, or pancytopenia. Blood
counts should be performed at the start of each 28-day treatment cycle
and every 2 weeks during each 28-day cycle in all patients. Patients
with liver disease, including hepatic echinococcosis, appear to be
more at risk of bone marrow suppression and warrant closer monitoring
of blood counts (see WARNINGS). Albendazole should be discontinued
in all patients if clinically significant decreases in blood cell
counts occur.<br/>Liver Function: In clinical trials, treatment with albendazole has
been associated with mild to moderate elevations of hepatic enzymes
in approximately 16% of patients. These elevations have generally
returned to normal upon discontinuation of therapy. There
have also been case reports of acute liver failure of uncertain causality
and hepatitis (see ADVERSE REACTIONS). Liver function tests (transaminases) should be performed before
the start of each treatment cycle and at least every 2 weeks during
treatment. If hepatic enzymes exceed twice the upper limit of normal,
consideration should be given to discontinuing albendazole therapy
based on individual patient circumstances. Restarting albendazole
treatment in patients whose hepatic enzymes have normalized off treatment
is an individual decision that should take into account the risk/benefit
of further albendazole usage. Laboratory tests should be performed
frequently if albendazole treatment is restarted. Patients with abnormal liver function test results are at increased
risk for hepatotoxicity and bone marrow suppression (see WARNINGS).
Therapy should be discontinued if liver enzymes are significantly
increased or if clinically significant decreases in blood cell counts
occur.<br/>Theophylline: Although single doses of albendazole have been shown
not to inhibit theophylline metabolism (see Drug Interactions), albendazole
does induce cytochrome P450 1A in human hepatoma cells. Therefore,
it is recommended that plasma concentrations of theophylline be monitored
during and after treatment with ALBENZA.<br/>Drug Interactions:<br/>Dexamethasone: Steady-state trough concentrations of albendazole
sulfoxide were about 56% higher when 8 mg dexamethasone was coadministered
with each dose of albendazole (15 mg/kg/day) in 8 neurocysticercosis
patients.<br/>Praziquantel: In the fed state, praziquantel (40 mg/kg) increased
mean maximum plasma concentration and area under the curve of albendazole
sulfoxide by about 50% in healthy subjects (n = 10) compared
with a separate group of subjects (n = 6) given albendazole
alone. Mean Tand mean plasma elimination half-life
of albendazole sulfoxide were unchanged. The pharmacokinetics of praziquantel
were unchanged following coadministration with albendazole (400 mg).<br/>Cimetidine: Albendazole sulfoxide concentrations in bile and
cystic fluid were increased (about 2-fold) in hydatid cyst patients
treated with cimetidine (10 mg/kg/day) (n = 7) compared
with albendazole (20 mg/kg/day) alone (n = 12). Albendazole
sulfoxide plasma concentrations were unchanged 4 hours after dosing.<br/>Theophylline: The pharmacokinetics of theophylline (aminophylline
5.8 mg/kg infused over 20 minutes) were unchanged following
a single oral dose of albendazole (400 mg) in 6 healthy subjects.<br/>Carcinogenesis, Mutagenesis, Impairment of Fertility: Long-term carcinogenicity studies were conducted
in mice and rats. In the mouse study, albendazole was administered
in the diet at doses of 25, 100, and 400 mg/kg/day (0.1, 0.5,
and 2 times the recommended human dose based on body surface area
in mg/m, respectively) for 108 weeks. In the rat
study, albendazole was administered in the diet at doses of 3.5, 7,
and 20 mg/kg/day (0.04, 0.08, and 0.21 times the recommended
human dose based on body surface area in mg/m, respectively)
for 117 weeks. There was no evidence of increased incidence of tumors
in the treated mice and rats when compared to the control group. In genotoxicity tests, albendazole was found negative
in an Ames Salmonella/Microsome Plate mutation assay with and without
metabolic activation or with and without pre-incubation, cell-mediated
Chinese Hamster Ovary chromosomal aberration test and in vivo
mouse micronucleus test. In the in vitro BALB/3T3 cells transformation
assay, albendazole produced weak activity in the presence of metabolic
activation while no activity was found in the absence of metabolic
activation. Albendazole did not adversely affect
male or female fertility in the rat at an oral dose of 30 mg/kg/day
(0.32 times the recommended human dose based on body surface area
in mg/m).<br/>Pregnancy:<br/>Teratogenic Effects: Pregnancy Category C. Albendazole has been shown
to be teratogenic (to cause embryotoxicity and skeletal malformations)
in pregnant rats and rabbits. The teratogenic response in the rat
was shown at oral doses of 10 and 30 mg/kg/day (0.10 times and
0.32 times the recommended human dose based on body surface area in
mg/m, respectively) during gestation days 6 to 15 and
in pregnant rabbits at oral doses of 30 mg/kg/day (0.60 times
the recommended human dose based on body surface area in mg/m) administered during gestation days 7 to 19. In the rabbit
study, maternal toxicity (33% mortality) was noted at 30 mg/kg/day.
In mice, no teratogenic effects were observed at oral doses up to
30 mg/kg/day (0.16 times the recommended human dose based on body
surface area in mg/m), administered during gestation days
6 to 15. There are no adequate and well-controlled
studies of albendazole administration in pregnant women. Albendazole
should be used during pregnancy only if the potential benefit justifies
the potential risk to the fetus (see WARNINGS).<br/>Nursing Mothers: Albendazole is excreted in animal milk. It is not
known whether it is excreted in human milk. Because many drugs are
excreted in human milk, caution should be exercised when albendazole
is administered to a nursing woman.<br/>Pediatric Use: Experience in children under the age of 6 years
is limited. In hydatid disease, infection in infants and young children
is uncommon, but no problems have been encountered in those who have
been treated. In neurocysticercosis, infection is more frequently
encountered. In 5 published studies involving pediatric patients as
young as 1 year, no significant problems were encountered, and the
efficacy appeared similar to the adult population.<br/>Geriatric Use: Experience in patients 65 years of age or older
is limited. The number of patients treated for either hydatid disease
or neurocysticercosis is limited, but no problems associated with
an older population have been observed.
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Significant toxicity and mortality were shown in
male and female mice at doses exceeding 5,000 mg/kg; in rats,
at estimated doses between 1,300 and 2,400 mg/kg; in hamsters,
at doses exceeding 10,000 mg/kg; and in rabbits, at estimated
doses between 500 and 1,250 mg/kg. In the animals, symptoms were
demonstrated in a dose-response relationship and included diarrhea,
vomiting, tachycardia, and respiratory distress. One overdosage has been reported with ALBENZA in a patient who took
at least 16 grams over 12 hours. No untoward effects were
reported. In case of overdosage, symptomatic therapy (e.g., gastric
lavage and activated charcoal) and general supportive measures are
recommended.
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albendazole
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ALBENZA (Tablet)
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The adverse event profile of albendazole differs
between hydatid disease and neurocysticercosis. Adverse events occurring
with a frequency of���1% in either disease are described in
the table below. These symptoms were usually
mild and resolved without treatment. Treatment discontinuations were
predominantly due to leukopenia (0.7%) or hepatic abnormalities (3.8%
in hydatid disease). The following incidence reflects events that
were reported by investigators to be at least possibly or probably
related to albendazole. The following adverse events were observed at
an incidence of<1%:<br/>Blood and Lymphatic System Disorders: Leukopenia. There have been rare reports of granulocytopenia,
pancytopenia, agranulocytosis, or thrombocytopenia (see WARNINGS).
Patients with liver disease, including hepatic echinococcosis, appear
to be more at risk of bone marrow suppression (see WARNINGS and PRECAUTIONS).<br/>Immune System Disorders: Hypersensitivity reactions, including rash and urticaria.<br/>Postmarketing Adverse Reactions: In addition to adverse events reported from
clinical trials, the following events have been identified during
world-wide post-approval use of ALBENZA. Because they are
reported voluntarily from a population of unknown size, estimates
of frequency cannot be made. These events have been chosen for inclusion
due to a combination of their seriousness, frequency of reporting,
or potential causal connection to ALBENZA.<br/>Blood and Lymphatic System Disorders: Aplastic anemia, bone marrow suppression, neutropenia.<br/>Hepatobiliary Disorders: Elevations of hepatic enzymes, hepatitis, acute
liver failure.<br/>Skin and Subcutaneous Tissue Disorders: Erythema multiforme, Stevens-Johnson syndrome.<br/>Renal and Urinary Disorders: Acute renal failure.
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Rare fatalities associated with the use of ALBENZA
have been reported due to granulocytopenia or pancytopenia (see PRECAUTIONS).
Albendazole has been shown to cause bone marrow suppression, aplastic
anemia, and agranulocytosis in patients with and without underlying
hepatic dysfunction. Blood counts should be monitored at the beginning
of each 28-day cycle of therapy, and every 2 weeks while on therapy
with albendazole in all patients. Patients with liver disease, including
hepatic echinococcosis, appear to be more at risk for bone marrow
suppression leading to pancytopenia, aplastic anemia, agranulocytosis,
and leukopenia attributable to albendazole and warrant closer monitoring
of blood counts. Albendazole should be discontinued in all patients
if clinically significant decreases in blood cell counts occur. Albendazole should not be used in pregnant women except
in clinical circumstances where no alternative management is appropriate.
Patients should not become pregnant for at least 1 month following
cessation of albendazole therapy. If a patient becomes pregnant while
taking this drug, albendazole should be discontinued immediately.
If pregnancy occurs while taking this drug, the patient should be
apprised of the potential hazard to the fetus.
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dailymed-instance:indicatio... |
ALBENZA is indicated for the treatment of the following
infections:<br/>Neurocysticercosis: ALBENZA is indicated for the treatment of parenchymal
neurocysticercosis due to active lesions caused by larval forms of
the pork tapeworm, Taenia solium. Lesions considered responsive to albendazole
therapy appear as nonenhancing cysts with no surrounding edema on
contrast-enhanced computerized tomography. Clinical studies in patients
with lesions of this type demonstrate a 74% to 88% reduction in number
of cysts; 40% to 70% of albendazole-treated patients showed resolution
of all active cysts.<br/>Hydatid Disease: ALBENZA is indicated for the treatment of cystic
hydatid disease of the liver, lung, and peritoneum, caused by the
larval form of the dog tapeworm, Echinococcus
granulosus. This indication is based
on combined clinical studies which demonstrated non-infectious cyst
contents in approximately 80-90% of patients given ALBENZA for 3 cycles
of therapy of 28 days each (see DOSAGE AND ADMINISTRATION). Clinical
cure (disappearance of cysts) was seen in approximately 30% of these
patients, and improvement (reduction in cyst diameter of���25%)
was seen in an additional 40%. NOTE: When medically
feasible, surgery is considered the treatment of choice for hydatid
disease. When administering ALBENZA in the pre- or post-surgical setting,
optimal killing of cyst contents is achieved when 3 courses of therapy
have been given. NOTE: The efficacy of albendazole
in the therapy of alveolar hydatid disease caused by Echinococcus multilocularis has not
been clearly demonstrated in clinical studies.
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ALBENZA
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