Clinical data | |
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Trade names | Vermox, [1] Ovex, others |
Other names | MBZ |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682315 |
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Routes of administration | By mouth |
ATC code | |
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Pharmacokinetic data | |
Bioavailability | 2–10% |
Protein binding | 95% |
Metabolism | Extensive liver |
Elimination half-life | 3–6 hours |
Excretion | Feces, urine (5–10%) |
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CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.046.017 |
Chemical and physical data | |
Formula | C16H13N3O3 |
Molar mass | 295.298 g·mol−1 |
3D model (JSmol) | |
Melting point | 288.5 °C (551.3 °F) |
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Mebendazole (MBZ), sold under the brand name Vermox among others, is a medication used to treat a number of parasitic worm infestations. [5] This includes ascariasis, pinworm infection, hookworm infections, guinea worm infections, hydatid disease, and giardia, among others. [5] It is taken by mouth. [5]
Mebendazole is usually well tolerated. [5] Common side effects include headache, vomiting, and ringing in the ears. [5] If used at large doses it may cause bone marrow suppression. [5] It is unclear if it is safe in pregnancy. [5] [2] Mebendazole is a broad-spectrum antihelminthic agent of the benzimidazole type. [5]
Mebendazole came into use in 1971, after it was developed by Janssen Pharmaceutica in Belgium. [6] It is on the World Health Organization's List of Essential Medicines. [7] Mebendazole is available as a generic medication. [8]
Mebendazole is a highly effective, broad-spectrum antihelmintic indicated for the treatment of nematode infestations, including roundworm, hookworm, whipworm, threadworm (pinworm), and the intestinal form of trichinosis prior to its spread into the tissues beyond the digestive tract. Other drugs are used to treat worm infections outside the digestive tract, as mebendazole is poorly absorbed into the bloodstream. [9] Mebendazole is used alone in those with mild to moderate infestations. It kills parasites relatively slowly, and in those with very heavy infestations, it can cause some parasites to migrate out of the digestive system, leading to appendicitis, bile duct problems, or intestinal perforation. To avoid this, heavily infested patients may be treated with piperazine, either before or instead of mebendazole. Piperazine paralyses the parasites, causing them to pass in the feces. [10] It is also used rarely in the treatment of cystic echinococcosis, also known as hydatid disease. Evidence for effectiveness for this disease, however, is poor. [11]
Mebendazole and other benzimidazole antithelmetics are active against both larval and adult stages of nematodes, and in the cases of roundworm and whipworm, kill the eggs, as well. Paralysis and death of the parasites occurs slowly, and elimination in the feces may require several days. [9]
Mebendazole has been shown to cause ill effects in pregnancy in animal models, and no adequate studies of its effects in human pregnancy have been conducted. [2] Whether it can be passed by breastfeeding is unknown. [12] [2]
Mebendazole sometimes causes diarrhea, abdominal pain, and elevated liver enzymes. In rare cases, it has been associated with a dangerously low white blood cell count, low platelet count, and hair loss, [12] [13] with a risk of agranulocytosis in rare cases.
Carbamazepine and phenytoin lower serum levels of mebendazole. Cimetidine does not appreciably raise serum mebendazole (in contrast to the similar drug albendazole), consistent with its poor systemic absorption. [14] [15]
Stevens–Johnson syndrome and the more severe toxic epidermal necrolysis can occur when mebendazole is combined with high doses of metronidazole. [16]
Mebendazole works by selectively inhibiting the synthesis of microtubules via binding to the colchicine binding site of β-tubulin, thereby blocking polymerisation of tubulin dimers in intestinal cells of parasites. [17] Disruption of cytoplasmic microtubules leads to blocking the uptake of glucose and other nutrients, resulting in the gradual immobilization and eventual death of the helminths. [9]
Poor absorption in the digestive tract makes mebendazole an efficient drug for treating intestinal parasitic infections with limited adverse effects. However mebendazole has an impact on mammalian cells, mostly by inhibiting polymeration of tubulin dimers, thereby disrupting essential microtubule structures such as mitotic spindle. [18] Disassembly of the mitotic spindle then leads to apoptosis mediated via dephosphorylation of Bcl-2 which allows pro-apoptotic protein Bax to dimerize and initiate programmed cell death. [19]
Mebendazole is available as a generic medication. [8] Mebendazole is distributed in international markets by Johnson and Johnson and a number of generic manufacturers. [20]
In the United States, mebendazole is sometimes sold at about 200 times the price of the same medication in other countries. [21] [22] [23]
Several studies show mebendazole exhibits potent antitumor properties. mebendazole significantly inhibited cancer cell growth, migration, and metastatic formation of adrenocortical carcinoma, both in vitro and in vivo . [24] Treatment of lung cancer cell lines with mebendazole caused mitotic arrest, followed by apoptotic cell death with the feature of caspase activation and cytochrome c release. [25] Mebendazole induced a dose- and time-dependent apoptotic response in human lung cancer cell lines, [26] and apoptosis via Bcl-2 inactivation in chemoresistant melanoma cells. [27] The anti-cancer effect of mebendazole comes from preclinical studies and case reports. [28]
Trichuriasis, also known as whipworm infection, is an infection by the parasitic worm Trichuris trichiura (whipworm). If infection is only with a few worms, there are often no symptoms. In those who are infected with many worms, there may be abdominal pain, fatigue and diarrhea. The diarrhea sometimes contains blood. Infections in children may cause poor intellectual and physical development. Low red blood cell levels may occur due to loss of blood.
Ascariasis is a disease caused by the parasitic roundworm Ascaris lumbricoides. Infections have no symptoms in more than 85% of cases, especially if the number of worms is small. Symptoms increase with the number of worms present and may include shortness of breath and fever in the beginning of the disease. These may be followed by symptoms of abdominal swelling, abdominal pain, and diarrhea. Children are most commonly affected, and in this age group the infection may also cause poor weight gain, malnutrition, and learning problems.
Tubulin in molecular biology can refer either to the tubulin protein superfamily of globular proteins, or one of the member proteins of that superfamily. α- and β-tubulins polymerize into microtubules, a major component of the eukaryotic cytoskeleton. Microtubules function in many essential cellular processes, including mitosis. Tubulin-binding drugs kill cancerous cells by inhibiting microtubule dynamics, which are required for DNA segregation and therefore cell division.
Bcl-2, encoded in humans by the BCL2 gene, is the founding member of the Bcl-2 family of regulator proteins that regulate cell death (apoptosis), by either inhibiting (anti-apoptotic) or inducing (pro-apoptotic) apoptosis. It was the first apoptosis regulator identified in any organism.
Albendazole is a broad-spectrum antihelmintic and antiprotozoal agent of the benzimidazole type. It is used for the treatment of a variety of intestinal parasite infections, including ascariasis, pinworm infection, hookworm infection, trichuriasis, strongyloidiasis, taeniasis, clonorchiasis, opisthorchiasis, cutaneous larva migrans, giardiasis, and gnathostomiasis, among other diseases.
Necator americanus is a species of hookworm commonly known as the New World hookworm. Like other hookworms, it is a member of the phylum Nematoda. It is an obligatory parasitic nematode that lives in the small intestine of human hosts. Necatoriasis—a type of helminthiasis—is the term for the condition of being host to an infestation of a species of Necator. Since N. americanus and Ancylostoma duodenale are the two species of hookworms that most commonly infest humans, they are usually dealt with under the collective heading of "hookworm infection". They differ most obviously in geographical distribution, structure of mouthparts, and relative size.
Echinococcus multilocularis, the fox tapeworm, is a small cyclophyllid tapeworm found extensively in the northern hemisphere. E. multilocularis, along with other members of the Echinococcus genus, produce diseases known as echinococcosis. Unlike E. granulosus,E. multilocularis produces many small cysts that spread throughout the internal organs of the infected animal. The resultant disease is called Alveolar echinococcosis, and is caused by ingesting the eggs of E. multilocularis.
Docetaxel, sold under the brand name Taxotere among others, is a chemotherapy medication used to treat a number of types of cancer. This includes breast cancer, head and neck cancer, stomach cancer, prostate cancer and non-small-cell lung cancer. It may be used by itself or along with other chemotherapy medication. It is given by slow injection into a vein.
Vinblastine (VBL), sold under the brand name Velban among others, is a chemotherapy medication, typically used with other medications, to treat a number of types of cancer. This includes Hodgkin's lymphoma, non-small-cell lung cancer, bladder cancer, brain cancer, melanoma, and testicular cancer. It is given by injection into a vein.
The p53 upregulated modulator of apoptosis (PUMA) also known as Bcl-2-binding component 3 (BBC3), is a pro-apoptotic protein, member of the Bcl-2 protein family. In humans, the Bcl-2-binding component 3 protein is encoded by the BBC3 gene. The expression of PUMA is regulated by the tumor suppressor p53. PUMA is involved in p53-dependent and -independent apoptosis induced by a variety of signals, and is regulated by transcription factors, not by post-translational modifications. After activation, PUMA interacts with antiapoptotic Bcl-2 family members, thus freeing Bax and/or Bak which are then able to signal apoptosis to the mitochondria. Following mitochondrial dysfunction, the caspase cascade is activated ultimately leading to cell death.
A mitotic inhibitor, microtubule inhibitor, or tubulin inhibitor, is a drug that inhibits mitosis, or cell division, and is used in treating cancer, gout, and nail fungus. These drugs disrupt microtubules, which are structures that pull the chromosomes apart when a cell divides. Mitotic inhibitors are used in cancer treatment, because cancer cells are able to grow through continuous division that eventually spread through the body (metastasize). Thus, cancer cells are more sensitive to inhibition of mitosis than normal cells. Mitotic inhibitors are also used in cytogenetics, where they stop cell division at a stage where chromosomes can be easily examined.
Ancylostomiasis is a hookworm disease caused by infection with Ancylostoma hookworms. The name is derived from Greek ancylos αγκύλος "crooked, bent" and stoma στόμα "mouth".
Necatoriasis is the condition of infection by Necator hookworms, such as Necator americanus. This hookworm infection is a type of helminthiasis (infection) which is a type of neglected tropical disease.
Tubulin alpha-8 chain is a protein that in humans is encoded by the TUBA8 gene.
Tubulin alpha-1C chain is a protein that in humans is encoded by the TUBA1C gene.
Pyrantel is a medication used to treat a number of parasitic worm infections. This includes ascariasis, hookworm infections, enterobiasis, trichostrongyliasis, and trichinellosis. It is taken by mouth.
Eribulin, sold under the brand name Halaven among others, is an anti-cancer medication used to treat breast cancer and liposarcoma.
Follicular dendritic cell sarcoma (FDCS) is an extremely rare neoplasm. While the existence of FDC tumors was predicted by Lennert in 1978, the tumor wasn't fully recognized as its own cancer until 1986 after characterization by Monda et al. It accounts for only 0.4% of soft tissue sarcomas, but has significant recurrent and metastatic potential and is considered an intermediate grade malignancy. The major hurdle in treating FDCS has been misdiagnosis. It is a newly characterized cancer, and because of its similarities in presentation and markers to lymphoma, both Hodgkin and Non-Hodgkin subtypes, diagnosis of FDCS can be difficult. With recent advancements in cancer biology better diagnostic assays and chemotherapeutic agents have been made to more accurately diagnose and treat FDCS.
Pinworm infection, also known as enterobiasis, is a human parasitic disease caused by the pinworm, Enterobius vermicularis. The most common symptom is itching in the anal area. The period of time from swallowing eggs to the appearance of new eggs around the anus is 4 to 8 weeks. Some people who are infected do not have symptoms.
Anthelmintics or antihelminthics are a group of antiparasitic drugs that expel parasitic worms (helminths) and other internal parasites from the body by either stunning or killing them and without causing significant damage to the host. They may also be called vermifuges or vermicides. Anthelmintics are used to treat people who are infected by helminths, a condition called helminthiasis. These drugs are also used to treat infected animals.