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Albendazole, also known as albendazolum,
Common side effects include nausea, abdominal pains, and headaches.
Albendazole was developed in 1975.
Contents
1 Medical uses
1.1 Pregnancy
2 Contraindications
3 Side effects
4 Overdose
5 Interactions
6 Pharmacology
6.1 Mechanism of action
6.2 Pharmacokinetics
7 History
8 Society and culture
8.1 Brand names
8.2 Cost
9 Veterinary use
9.1 Meat
10 See also
11 References
12 External links
Medical uses
Albendazole is an effective treatment for:
Flatworms
Fasciolosis
Cestodes (tapeworms), as an alternative to praziquantel or niclosamide for adult beef tapeworms ( Taenia saginata ) and as an alternative to praziquantel for pork tapeworms ( T. solium ).
Cysticercosis
Hydatic disease (aka echinococcosis)
Nematodes
Ascariasis, which can be cured with a single dose of albendazole.
Baylisascariasis, caused by the raccoon roundworm. Corticosteroids are sometimes added in cases of eye and CNS infections.
Enterobiasis ( pinworm infection)
Filariasis ; since albendazole’s disintegration of the microfilarie (“pre-larva”) can cause an allergic reaction, antihistamines or corticosteroids are sometimes added to treatment. In cases of lymphatic filariasis (elephantiasis) caused by Wuchereria bancrofti or Brugia malayi, albendazole is sometimes given as an adjunct to ivermectin or diethylcarbamazine in order to suppress microfilaremia. It can also be given for loa loa filariasis as an adjunct or replacement to diethylcarbamazine.
Gnathostomiasis when caused by Gnathostoma spinigerum.
Gongylonemiasis
Hookworm infections,
Intestinal capillariasis,
Mansonelliasis when caused by Mansonella perstans. Albendazole works against the adult worms but not against the younger microfilariae.
Oesophagostomumiasis, when caused by Oesophagostomum bifurcum
Strongyloidiasis,
Toxocariasis, also called “visceral larva migrans”, when caused by the dog roundworm Toxocara canis or cat roundworm T. catis. Corticosteroids can be added in severe cases, and surgery might be required to repair secondary damage.
Trichinosis, when caused by Trichinella spiralis
Trichostrongyliasis, as an alternative to pyrantel pamoate.
Trichuriasis (whipworm infection),
Giardiasis, as an alternative or adjunct to metronidazole, especially in children
Microsporidiosis, including ocular microsporidiosis caused by Encephalitozoon hellem or E. cuniculi, when combined with topical fumagillin
Granulomatous amoebic encephalitis, when caused by the ameba Balamuthia mandrillaris, in combination with miltefosine and fluconazole
Arthropods
Crusted scabies, when combined with topical crotamiton and salicylic acid
Head lice infestation, though ivermectin is much better
Intestinal myiasis
Though albendazole is effective in treating many diseases, it is only FDA-approved for treating hydatid disease caused by dog tapeworm larvae and neurocysticercosis caused by pork tapeworm larvae.
Pregnancy
Albendazole is a pregnancy class D drug in Australia and pregnancy class C in the United States. It is contraindicated in the first trimester of pregnancy, and should be avoided up to one month before conception. While studies in pregnant rats and rabbits have shown albendazole to be teratogenic,
In pregnant dogs, albendazole use has led to puppies with reduced weight and with cleft palates. Birds have lower rates of laying eggs and hatching when given albendazole.
Albendazole sulfoxide is secreted into breast milk at around 1.5% of the maternal dose, though oral absorption is poor enough that it is unlikely to affect nursing infants.
Contraindications
Hypersensitivity to the benzimidazole class of compounds contraindicates its use.
Side effects
Close-up of a pork tapeworm cyst. Destruction of these cysts can cause inflammation.
The most common side effects by albendazole are, experienced by over 10% of people, headache and abnormal liver function.
Side effects can be different when treating for hydatid disease versus neurocysticercosis; for example, those being treated for the former are more likely to experience elevated liver enzymes and abdominal pain; those being treated for the latter are more likely to experience headache.
Overdose
Because of its low solubility, albendazole often cannot be absorbed in high enough quantities to be toxic.
Interactions
The antiepileptics carbamazepine, phenytoin, and phenobarbital lower the plasma concentration and the half life of albendazole sulfoxide’s R(+) enantiomer.
Antiepileptics and pharmacokinetics of albendazole sulfoxide
Drug
Change in AUC
Change in C max
Carbamazepine
49% decrease
50–63% decrease
Phenobarbitol
61% decrease
50–63% decrease
Phenytoin
66% decrease
50–63% decrease
The antacid cimetidine heightens serum albendazole concentrations, increases the half life of albendazole, and doubles albendazole sulfoxide levels in bile.
Several other interactions exist. Corticosteroids increase the steady-state plasma concentration of albendazole sulfoxide;
Pharmacology
A microtubule is composed of polymers of α- and β-tubulin.
Mechanism of action
As a vermicide, albendazole causes degenerative alterations in the intestinal cells of the worm by binding to the colchicine -sensitive site of β-tubulin, thus inhibiting its polymerization or assembly into microtubules (it binds much better to the β-tubulin of parasites than that of mammals). Due to diminished ATP production, the parasite is immobilized and eventually dies.
Some parasites have evolved to have some resistance to albendazole by having a different set of acids comprising β-tubulin, decreasing the binding affinity of albendazole.
Pharmacokinetics
Oral absorption of albendazole varies among species, with 1–5% of the drug being successfully absorbed in humans, 20–30% in rats, and 50% in cattle.
The absorption also largely depends on gastric pH. People have varying gastric pHs on empty stomachs, and thus absorption from one person to another can vary wildly when taken without food.
Absorption is also affected by how much of the albendazole is degraded within the small intestine by metabolic enzymes in the vili.
General metabolism of albendazole and its sulfoxides.
The pharmacokinetics of albendazole differ slightly between men and women: women have a lower oral clearance and volume of distribution, while men have a lower serum peak concentration.
Albendazole undergoes very fast 1st-pass metabolism in all species, such that the unchanged drug is undetectable in plasma.
While oxidation to albendazole sulfoxide by FMO produces R(+) enantiomers, while oxidation the cytochromes and by some enzymes in the gut epithelium produce S(-). Different species produce the R(+) and S(-) enantiomers in different quantities; humans, dogs, and most other species
For systemic parasites, albendazole acts as a prodrug, while albendazole sulfoxide reaches systemic circulation and acts as the real antihelminthic.
Albendazole sulfoxide is converted to the inactive albendazole sulfone by cytochrome P450 oxidases, thought to include CYP3A4
methyl carbamate,
methyl carbamate,
methyl carbamate,
5-(n-propylsulfonyl)-1H-benzimidazole-2-yl amine, and
5-(n-propysulfinyl)-1H-benzimidazole-2-yl amine.
There are also some minor hydroxylated sulfated or glucuronidated derivatives.
In humans, the metabolites mostly excreted in the bile, with only a small amount being excreted in the urine (less than 1%) and feces.
Like all benzimidazoles, albendazole has no residual effect, and thus does not protect well against reinfestations.
History
Albendazole, patented in 1975, was invented by Robert J. Gyurik and Vassilios J. Theodorides and assigned to SmithKline Corporation.
Society and culture
Discarded bottles of albendazole distributed in Africa
Brand names
Brand names include: Albenza, Alworm, Andazol, Eskazole, Noworm, Zentel, Alben-G, ABZ, Cidazole, Wormnil etc.
Cost
In many areas of the world it costs between US$0.01 and US$0.06 per dose.
In Raleigh, North Carolina, the brand-name prescription cost was around US$800, and US$540 for the generic. The pharmaceutical company Amedra increased the price after purchasing the rights to the drug, instead of lowering it as generics are predicted to do, drawing criticism from patients’ rights advocates and US Democratic Party leaders.
In 2013, GlaxoSmithKline donated 763 million albendazole tablets for the treatment and prevention of parasitic infections in developing countries, bringing the total to over 4 billion tablets donated since 1998.
Veterinary use
Albendazole is mainly used in cattle and sheep, but has found some use in cats and dogs as well;
Albendazole use in animals
Cattle
Sheep
Others
Platyhelminthes (flatworms)
Trematodes
Dicrocoelium (liver flukes)
D. dendriticum (lancet liver fluke)
D. dendriticum
Fasciola (liver flukes)
F. hepatica
F. hepatica
For F. hepatica and F. gigantica in people
Fascioloides (liver flukes)
F. magna
F. magna
Also for F. magna in South American camelids (ex. llama and alpaca)
Paragonimus (lung flukes)


For P. kellicotti in cats and dogs
Platynosomum


For Platynosomum infections in cats
Opisthorchiidae


For Opisthorchiidae infections in cats
Cestodes (tapeworms)
Echinococcus


For Echinococcus cysts in horses and humans
Moniezia
M. expansa M. benedini
M. expansa  
Taenia
T. saginata larvae

For T. saginata, T. solium, and T. crassiceps in humans
Thysanosoma

T. actinoides
Nematodes (roundworms)
Ancylostoma


For Ancylostoma infections in dogs, cats, and humans
Bunostomum
B. phlebotomum

Capillaria


For causative agents of various forms of capillariasis in cats and dogs (including C. philippinensis, C. hepatica, C. aerophila, and C. plica ) and intestinal capillariasis ( C. philippinensis ) in humans.
Chabertia

C. ovina
Cooperia
C. oncophora C. punctata
C. oncophora  
Dictyocaulus (lungworm)
D. viviparus
D. filaria
For D. amfieldi infections in horses
Filaroides (lungworm)


For F. hirthi and F. osleri in dogs
Haemonchus
H. contortus H. placei
H. contortus  
Marshallagia

M. marshalli
Metastrongylus


For M. apri in swine
Nematodirus
N. spathiger N. helvetianus
N. spathiger N. filicollis
Parascaris


For P. equorum in horses
Ostertagia
O. ostertagi
O. circumcincta
For O. bifurcum in humans
Oesophagostomum
O. radiatum
O. columbianum
Strongyloides


For S. stercoralis in dogs and humans
Strongylus


For S. equinus in horses
Toxocara


For T. canis infections in dogs and toxocariasis in humans (caused by T. canis and T. cati )
Trichostrongylus
T. axei T. colubriformis
T. axei T. colubriformis
For any Trichostrongylus infection in humans
Trichuris (whipworm)
Most species, but those usually found in cattle are: T. discolor T. globulosa T. ovis
Most species, but those usually found in sheep are: T. discolor T. globulosa T. ovis
Albendazole is also used for Trichuris infections in humans (usually T. trichiura, causative agent of trichuriasis), dogs (usually T. vulpis and T. campanula ), cats (usually T. serrata and T. campanula ), pigs (usually T. suis ), and other ruminants (same species as those found in cattle and sheep).
Other
Encephalitozoon


For E. cuniculi infections (microsporidiosis) in humans and rabbits
Giardia
G. lamblia (causative agent of giardiasis )

Also treats giardiasis in humans, dogs, and small mammals
Leishmania


Treats leishmaniasis, caused by various species of Leishmania, in dogs
Albendazole has been used as an anthelminthic and for control of flukes in a variety of animal species, including cattle, sheep, goats, swine, camels, dogs, cats, elephants, poultry, and others.
It is extensively used for ruminant livestock in Latin America.
Albendazole has greater bioavailability in ruminants: some albendazole sulfoxide, when released back into the rumen, is reduced to albendazole by the resident microbiota, with a preference of the (+) enantiomer being the substrate.
Meat
This section needs additional citations for verification. Please help improve this article by adding citations to reliable sources. Unsourced material may be challenged and removed. (August 2017) ( Learn how and when to remove this template message )
The limitations in early pregnancy are due to a limited period during which teratogenic effects may occur. Summarized research data relating to the durations of these preslaughter and early pregnancy periods when albendazole should not be administered are found in US FDA NADA 110-048 (cattle) and 140-934 (sheep). Some data and inferences regarding goats are found in US FDA Supplemental NADA 110-048 (approved January 24, 2008).
Maximum residue limits (MRLs) for albendazole in food, adopted by the FAO/WHO Codex Alimentarius in 1993, are 5000, 5000, 100, and 100 micrograms per kilogram of body weight (μg/kg) for kidney, liver, fat, and muscle, respectively, and 100 μg/L for milk. For analysis purposes, MRLs of various nations may pertain to concentration of a marker substance which has been correlated with concentrations of the administered substance and its metabolized products. For example, in Canada, the marker substance specified by Health Canada is albendazole-2-aminosulfone, for which the MRL in liver of cattle is 200 μg/kg.
There is a 27 days cattle withdrawal time for meat.
See also
Mebendazole
Eradication of infectious disease
Neglected tropical diseases

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