Albendazole
Encyclopedia
Albendazole, marketed as Albenza, Eskazole, Zentel and Andazol, is a member of the benzimidazole
compounds used as a drug
indicated for the treatment
of a variety of worm
infestations. Although this use is widespread in the United States
, the U.S. Food and Drug Administration (FDA) has not approved albendazole for this indication. It is marketed by Amedra Pharmaceuticals. Albendazole was first discovered at the SmithKline Animal Health Laboratories in 1972. It is a broad spectrum anthelmintic
, effective against: roundworms, tapeworms, and flukes
of domestic animals and human
s.
, albendazole (donated by GlaxoSmithKline
) is being used to treat lymphatic filariasis as part of efforts to stop transmission
of the disease
. In sub-Saharan Africa, albendazole is used in conjunction with ivermectin, and elsewhere in the world, the medicine
is used in combination with diethylcarbamazine
.
In Brazil
and other countries it is used against giardiasis
.
and intestinal cells of the worm by binding to the colchicine
-sensitive site of tubulin
, thus inhibiting its polymerization or assembly into microtubules. The loss of the cytoplasmic microtubules leads to impaired uptake of glucose by the larval and adult stages of the susceptible parasites, and depletes their glycogen
stores. Degenerative changes in the endoplasmic reticulum
, the mitochondria of the germinal layer, and the subsequent release of lysosome
s result in decreased production of adenosine triphosphate
(ATP), which is the energy required for the survival of the helminth. Due to diminished energy production, the parasite is immobilized and eventually dies.
Albendazole also has been shown to inhibit the enzyme fumarate reductase
, which is helminth-specific. This action may be considered secondary to the effect on the microtubules due to the decreased absorption of glucose. This action occurs in the presence of reduced amounts of nicotinamide-adenine dinucleotide in reduced form (NADH), which is a coenzyme involved in many cellular oxidation-reduction reactions.
Albendazole has larvicidal effects in necatoriasis and ovicidal effects in ascariasis
, ancylostomiasis
, and trichinosis
.
NOTE: When administering albendazole in the pre- or post-surgical setting, optimal killing of cyst contents is achieved when 3 courses of therapy have been given.
Note: 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.
In rare cases it may cause persistent sore throat, severe headache, seizures, vision problems, yellowing eyes or skin, dark urine, stomach pain, easy bruising, mental/mood changes, very stiff neck, change in amount of urine. Elevation of liver enzymes during treatment is a common side effect, but in rare cases there have also been reports of acute liver failure. Allergic reactions are also possible.
Rarely Albendazole has been reported to cause marrow suppression, agranulocytosis or aplastic anemia
which may be permanent. The risk of developing this side effect seems to be increased in patients with liver disease, including echinococcal cysts.
Because of this dangerous side effect it is important to regularly monitor complete blood count
s.
, phenytoin
and phenobarbital
lower the plasmatic concentration and the half life of albendazole.
heightens serum
albendazole concentrations, and increases the half life of albendazole.
This might be a helpful interaction on more severe cases, because it boosts the potency
of albendazole.
have shown that trace amounts of albendazole appears in semen
. Given this potential for teratogenicity
, the manufacturers advise that the male sexual partner should also use adequate protection.
Benzimidazole
Benzimidazole is a heterocyclic aromatic organic compound. This bicyclic compound consists of the fusion of benzene and imidazole. The most prominent benzimidazole compound in nature is N-ribosyl-dimethylbenzimidazole, which serves as an axial ligand for cobalt in vitamin B12. Benzimidazole, in...
compounds used as a drug
Medication
A pharmaceutical drug, also referred to as medicine, medication or medicament, can be loosely defined as any chemical substance intended for use in the medical diagnosis, cure, treatment, or prevention of disease.- Classification :...
indicated for the treatment
Pharmacotherapy
Pharmacotherapy is the treatment of disease through the administration of drugs. As such, it is considered part of the larger category of therapy....
of a variety of worm
Worm
The term worm refers to an obsolete taxon used by Carolus Linnaeus and Jean-Baptiste Lamarck for all non-arthropod invertebrate animals, and stems from the Old English word wyrm. Currently it is used to describe many different distantly-related animals that typically have a long cylindrical...
infestations. Although this use is widespread in the United States
United States
The United States of America is a federal constitutional republic comprising fifty states and a federal district...
, the U.S. Food and Drug Administration (FDA) has not approved albendazole for this indication. It is marketed by Amedra Pharmaceuticals. Albendazole was first discovered at the SmithKline Animal Health Laboratories in 1972. It is a broad spectrum anthelmintic
Anthelmintic
Anthelmintics or antihelminthics are drugs that expel parasitic worms from the body, by either stunning or killing them. They may also be called vermifuges or vermicides .-Pharmaceutical classes:...
, effective against: roundworms, tapeworms, and flukes
Trematoda
Trematoda is a class within the phylum Platyhelminthes that contains two groups of parasitic flatworms, commonly referred to as "flukes".-Taxonomy and biodiversity:...
of domestic animals and human
Human
Humans are the only living species in the Homo genus...
s.
Main uses
It is effective first line of treatment against:- Flatworms
- Flukes/trematodes
- Fasciolosis
- Tapeworm/cestodes
- CysticercosisCysticercosisCysticercosis refers to tissue infection after exposure to eggs of Taenia solium, the pork tapeworm. The disease is spread via the fecal-oral route through contaminated food and water, and is primarily a food borne disease. After ingestion the eggs pass through the lumen of the intestine into the...
- EchinococcosisEchinococcosisEchinococcosis, which is often referred to as hydatid disease or echinococcal disease, is a parasitic disease that affects both humans and other mammals, such as sheep, dogs, rodents and horses. There are three different forms of echinococcosis found in humans, each of which is caused by the larval...
- Cysticercosis
- Flukes/trematodes
- Nematodes
- EnterobiasisEnterobiasisA pinworm infection or enterobiasis is a human parasitic disease and one of the most common childhood parasitic worm infections in the developed world. It is caused by infestation with the parasitic roundworm Enterobius vermicularis, commonly called the human pinworm...
(pinworm infection) - Trichuriasis (whipwormTrichurisThe roundworm family Trichuridae includes as type genus Trichuris, often referred to as whipworms...
infection) - AscariasisAscariasisAscariasis is a human disease caused by the parasitic roundworm Ascaris lumbricoides. Perhaps as many as one quarter of the world's people are infected, with rates of 45% in Latin America and 95% in parts of Africa. Ascariasis is particularly prevalent in tropical regions and in areas of poor...
- HookwormHookwormThe hookworm is a parasitic nematode that lives in the small intestine of its host, which may be a mammal such as a dog, cat, or human. Two species of hookworms commonly infect humans, Ancylostoma duodenale and Necator americanus. A. duodenale predominates in the Middle East, North Africa, India...
- Cutaneous larva migransCutaneous larva migransCutaneous larva migrans is a skin disease in humans, caused by the larvae of various nematode parasites of the hookworm family...
(caused by AncylostomaAncylostomaAncylostoma is a genus that includes some species of hookworm.Species include:Ancylostoma is a genus that includes some species of hookworm.Species include:Ancylostoma is a genus that includes some species of hookworm....
) - FilariasisFilariasisFilariasis is a parasitic disease and is considered an infectious tropical disease, that is caused by thread-like nematodes belonging to the superfamily Filarioidea, also known as "filariae"....
- Enterobiasis
Other uses
In AfricaAfrica
Africa is the world's second largest and second most populous continent, after Asia. At about 30.2 million km² including adjacent islands, it covers 6% of the Earth's total surface area and 20.4% of the total land area...
, albendazole (donated by GlaxoSmithKline
GlaxoSmithKline
GlaxoSmithKline plc is a global pharmaceutical, biologics, vaccines and consumer healthcare company headquartered in London, United Kingdom...
) is being used to treat lymphatic filariasis as part of efforts to stop transmission
Transmission (medicine)
In medicine and biology, transmission is the passing of a communicable disease from an infected host individual or group to a conspecific individual or group, regardless of whether the other individual was previously infected...
of the disease
Disease
A disease is an abnormal condition affecting the body of an organism. It is often construed to be a medical condition associated with specific symptoms and signs. It may be caused by external factors, such as infectious disease, or it may be caused by internal dysfunctions, such as autoimmune...
. In sub-Saharan Africa, albendazole is used in conjunction with ivermectin, and elsewhere in the world, the medicine
Medication
A pharmaceutical drug, also referred to as medicine, medication or medicament, can be loosely defined as any chemical substance intended for use in the medical diagnosis, cure, treatment, or prevention of disease.- Classification :...
is used in combination with diethylcarbamazine
Diethylcarbamazine
Diethylcarbamazine is an anthelmintic drug that does not resemble other antiparasitic compounds. It is a synthetic organic compound which is highly specific for several parasites and does not contain any toxic metallic elements.-Uses:...
.
In Brazil
Brazil
Brazil , officially the Federative Republic of Brazil , is the largest country in South America. It is the world's fifth largest country, both by geographical area and by population with over 192 million people...
and other countries it is used against giardiasis
Giardiasis
Giardiasis or beaver fever in humans is a diarrheal infection of the small intestine by a single-celled organism Giardia lamblia. Giardiasis occurs worldwide with a prevalence of 20–30% in developing countries. In the U.S., 20,000 cases are reported to the CDC annually, but the true annual...
.
Mode of action
As a vermicidal, albendazole causes degenerative alterations in the tegumentTegument
Tegument may refer to:* Integumentary system* Tegument * Viral tegument...
and intestinal cells of the worm by binding to the colchicine
Colchicine
Colchicine is a medication used for gout. It is a toxic natural product and secondary metabolite, originally extracted from plants of the genus Colchicum...
-sensitive site of tubulin
Tubulin
Tubulin is one of several members of a small family of globular proteins. The most common members of the tubulin family are α-tubulin and β-tubulin, the proteins that make up microtubules. Each has a molecular weight of approximately 55 kiloDaltons. Microtubules are assembled from dimers of α- and...
, thus inhibiting its polymerization or assembly into microtubules. The loss of the cytoplasmic microtubules leads to impaired uptake of glucose by the larval and adult stages of the susceptible parasites, and depletes their glycogen
Glycogen
Glycogen is a molecule that serves as the secondary long-term energy storage in animal and fungal cells, with the primary energy stores being held in adipose tissue...
stores. Degenerative changes in the endoplasmic reticulum
Endoplasmic reticulum
The endoplasmic reticulum is an organelle of cells in eukaryotic organisms that forms an interconnected network of tubules, vesicles, and cisternae...
, the mitochondria of the germinal layer, and the subsequent release of lysosome
Lysosome
thumb|350px|Schematic of typical animal cell, showing subcellular components. [[Organelle]]s: [[nucleoli]] [[cell nucleus|nucleus]] [[ribosomes]] [[vesicle |vesicle]] rough [[endoplasmic reticulum]]...
s result in decreased production of adenosine triphosphate
Adenosine triphosphate
Adenosine-5'-triphosphate is a multifunctional nucleoside triphosphate used in cells as a coenzyme. It is often called the "molecular unit of currency" of intracellular energy transfer. ATP transports chemical energy within cells for metabolism...
(ATP), which is the energy required for the survival of the helminth. Due to diminished energy production, the parasite is immobilized and eventually dies.
Albendazole also has been shown to inhibit the enzyme fumarate reductase
Fumarate reductase
Fumarate reductase is the enzyme that converts fumarate to succinate, and is important in microbial metabolism as a part of anaerobic respiration.Succinate + acceptor fumarate + reduced acceptor...
, which is helminth-specific. This action may be considered secondary to the effect on the microtubules due to the decreased absorption of glucose. This action occurs in the presence of reduced amounts of nicotinamide-adenine dinucleotide in reduced form (NADH), which is a coenzyme involved in many cellular oxidation-reduction reactions.
Albendazole has larvicidal effects in necatoriasis and ovicidal effects in ascariasis
Ascariasis
Ascariasis is a human disease caused by the parasitic roundworm Ascaris lumbricoides. Perhaps as many as one quarter of the world's people are infected, with rates of 45% in Latin America and 95% in parts of Africa. Ascariasis is particularly prevalent in tropical regions and in areas of poor...
, ancylostomiasis
Ancylostomiasis
Ancylostomiasis is the condition of infection by Ancylostoma hookworms. The name is derived from Greek ancylos αγκυλος "crooked, bent" and stoma στομα "mouth."...
, and trichinosis
Trichinosis
Trichinosis, also called trichinellosis, or trichiniasis, is a parasitic disease caused by eating raw or undercooked pork or wild game infected with the larvae of a species of roundworm Trichinella spiralis, commonly called the trichina worm. There are eight Trichinella species; five are...
.
Hydatid disease (Echinococcosis)
- Patients 60 kg or greater: 400 mg twice daily, with meals.
- Patients less than 60 kg: 15 mg/kg/day given in divided doses twice daily with meals (maximum total daily dose 800 mg).
- Treatment interval: 28-day cycle followed by a 14-day albendazole-free interval, for a total of 3 cycles.
NOTE: When administering albendazole in the pre- or post-surgical setting, optimal killing of cyst contents is achieved when 3 courses of therapy have been given.
Neurocysticercosis
- Patients 60 kg or greater: 400 mg twice daily, with meals.
- Patients less than 60 kg: 15 mg/kg/day given in divided doses twice daily with meals (maximum total daily dose 800 mg).
- Treatment interval: 8–30 days.
Note: 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.
Filaria
Single dose of 400 mg. For Filariaris, note that Albendazole kills the adult worms. Filariasis, albendazole and/or disintegrating filariae can affect the lymphatic system.Side effects
Albendazole may cause dizziness, headache, fever, nausea, vomiting, or temporary hair loss.In rare cases it may cause persistent sore throat, severe headache, seizures, vision problems, yellowing eyes or skin, dark urine, stomach pain, easy bruising, mental/mood changes, very stiff neck, change in amount of urine. Elevation of liver enzymes during treatment is a common side effect, but in rare cases there have also been reports of acute liver failure. Allergic reactions are also possible.
Rarely Albendazole has been reported to cause marrow suppression, agranulocytosis or aplastic anemia
Aplastic anemia
Aplastic anemia is a condition where bone marrow does not produce sufficient new cells to replenish blood cells. The condition, per its name, involves both aplasia and anemia...
which may be permanent. The risk of developing this side effect seems to be increased in patients with liver disease, including echinococcal cysts.
Because of this dangerous side effect it is important to regularly monitor complete blood count
Complete blood count
A complete blood count , also known as full blood count or full blood exam or blood panel, is a test panel requested by a doctor or other medical professional that gives information about the cells in a patient's blood...
s.
Antiepileptics
The drugs carbamazepineCarbamazepine
Carbamazepine is an anticonvulsant and mood-stabilizing drug used primarily in the treatment of epilepsy and bipolar disorder, as well as trigeminal neuralgia...
, phenytoin
Phenytoin
Phenytoin sodium is a commonly used antiepileptic. Phenytoin acts to suppress the abnormal brain activity seen in seizure by reducing electrical conductance among brain cells by stabilizing the inactive state of voltage-gated sodium channels...
and phenobarbital
Phenobarbital
Phenobarbital or phenobarbitone is a barbiturate, first marketed as Luminal by Friedr. Bayer et comp. It is the most widely used anticonvulsant worldwide, and the oldest still commonly used. It also has sedative and hypnotic properties but, as with other barbiturates, has been superseded by the...
lower the plasmatic concentration and the half life of albendazole.
Antacids/histamine H2 antagonists
The drug cimetidineCimetidine
Cimetidine INN is a histamine H2-receptor antagonist that inhibits the production of acid in the stomach. It is largely used in the treatment of heartburn and peptic ulcers. It is marketed by GlaxoSmithKline under the trade name Tagamet...
heightens serum
Blood serum
In blood, the serum is the component that is neither a blood cell nor a clotting factor; it is the blood plasma with the fibrinogens removed...
albendazole concentrations, and increases the half life of albendazole.
This might be a helpful interaction on more severe cases, because it boosts the potency
Potency (pharmacology)
In the field of pharmacology, potency is a measure of drug activity expressed in terms of the amount required to produce an effect of given intensity. A highly potent drug evokes a larger response at low concentrations, while a drug of lower potency evokes a small response at low concentrations...
of albendazole.
Pregnancy class
D (Australia) - Do not take when pregnant, and do not become pregnant for one month after taking this drug. Pharmacokinetic studiesPharmacokinetics
Pharmacokinetics, sometimes abbreviated as PK, is a branch of pharmacology dedicated to the determination of the fate of substances administered externally to a living organism...
have shown that trace amounts of albendazole appears in semen
Semen
Semen is an organic fluid, also known as seminal fluid, that may contain spermatozoa. It is secreted by the gonads and other sexual organs of male or hermaphroditic animals and can fertilize female ova...
. Given this potential for teratogenicity
Teratology
Teratology is the study of abnormalities of physiological development. It is often thought of as the study of human birth defects, but it is much broader than that, taking in other non-birth developmental stages, including puberty; and other non-human life forms, including plants.- Etymology :The...
, the manufacturers advise that the male sexual partner should also use adequate protection.
See also
- MebendazoleMebendazoleMebendazole or MBZ is a benzimidazole drug developed by Janssen Pharmaceutica and marketed as Vermox, Ovex, Antiox, and Pripsen...
- Eradication of infectious disease
- Neglected diseasesNeglected DiseasesThe neglected diseases are a group of tropical infections which are especially endemic in low-income populations in developing regions of Africa, Asia, and the Americas. Different organizations define the set of diseases differently...