Mebendazole

P02C - Antinematodal agents ATC P02CA01 Small molecule approved 1974 Oral Natural product

JFDA label: Vermazol

Mechanism of Action

Inhibitor of Tubulin — Tubulin inhibitor

Target	Action	Gene / class
Tubulin efficacy	INHIBITOR

Indications

Approved

Intestinal nematode infection

Off-label

Capillariasis
Echinococcosis, cystic (Echinococcus granulosus)
Toxocariasis
Trichinellosis (Trichinella spiralis)
Trichostrongyliasis

Antimicrobial Spectrum

Expected / intrinsic spectrum (EUCAST breakpoints & labels) — not local resistance. Source: openfda-label.

Helminths

Organism	Activity	MIC
Ascaris lumbricoides	Active	—
Trichuris trichiura	Active	—

Contraindications

Source: Lexicomp

Hypersensitivity to mebendazole or any component of the formulation Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Hepatobiliary disorders (1)

Not Known Hepatitis

Gastrointestinal disorders (6)

Not Known Abdominal pain · anorexia · diarrhea · flatulence · nausea · vomiting

Dosing

Source: Lexicomp

Ancylostoma duodenale or Necator americanus (hookworm): Oral: Manufacturer’s labeling: 100 mg twice daily for 3 days; repeat in 3 weeks if not cured with initial treatment Alternate dosing: 500 mg as a single dose (Parasitic Infections 2013) Ascariasis (roundworm): Oral: Manufacturer’s labeling: 100 mg twice daily for 3 days; repeat in 3 weeks if not cured with initial treatment. Alternate dosing: 500 mg as a single dose (Parasitic Infections 2013) Enterobiasis (pinworm): Oral: 100 mg as a single dose; repeat in 3 weeks if not cured with initial treatment. Trichuriasis (whipworm): Oral: 100 mg twice daily for 3 days; repeat in 3 weeks if not cured with initial treatment. Capillariasis (off-label use): Oral: 200 mg twice daily for 20 days (CDC 2012). Additional data may be necessary to further define the role of mebendazole in this condition. Echinococcus, cystic (off-label use): Oral: 40 to 50 mg/kg/day in 3 divided doses for 3 to 6 months (CDC 2014; Franchi 1999). Additional data may be necessary to further define the role of mebendazole in this condition. Trichinellosis (Trichinella spiralis) (off-label use): Oral: 200 to 400 mg 3 times daily for 3 days, followed by 400 to 500 mg 3 times daily for 10 days (CDC 2016b). Additional data may be necessary to further define the role of mebendazole in this condition. Trichostrongyliasis (off-label use): Oral: 100 mg twice daily for 3 days (Farahmandian 1977) Toxocariasis (off-label use): Oral: 100 to 200 mg twice daily for 5 days (CDC 2013). Additional data may be necessary to further define the role of mebendazole in this condition.

(For additional information see "Mebendazole: Pediatric drug information") Intestinal nematode infection (hookworm, pinworm, roundworm, whipworm): Children ≥2 years and Adolescents: Oral: Refer to adult dosing. Capillariasis (off-label use): Limited data available: Children and Adolescents: Oral: Refer to adult dosing. Trichinellosis (off-label use): Limited data available: Children and Adolescents: Oral: Refer to adult dosing. Toxocariasis (off-label use): Children and Adolescents: Oral: Refer to adult dosing.

Refer to adult dosing.

There are no dosage adjustments provided in the manufacturer's labeling.

There are no dosage adjustments provided in the manufacturer's labeling; however, undergoes extensive hepatic metabolism; use with caution as systemic exposure may be increased.

Warnings & Precautions

Source: Lexicomp

Bone marrow suppression

Neutropenia and agranulocytosis have been reported with high doses and prolonged use. Monitor CBC if used at higher doses or for a prolonged duration. Disease-related concerns:

Hepatic impairment

Use with caution; systemic exposure may be increased with hepatic impairment. Concurrent drug therapy issues:

Drug-drug interactions

Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information. Special populations:

Pediatric

Experience with use in children

Pregnancy & Lactation

Pregnancy

Untreated soil transmitted helminth infections during pregnancy are associated with adverse outcomes (eg, maternal iron deficiency anemia, low birth weight, neonatal and maternal death). Treatment of pinworm in pregnancy with mebendazole may be considered; however, the CDC suggests postponing therapy until the third trimester when possible (CDC 2016a).

Lactation

Mebendazole is present in breast milk. According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should take into account the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother. Current guidelines note that breastfeeding does not need to be withheld during therapy (CDC 2016a).

Monitoring

Clinical pearl	Periodic hematologic, hepatic, and renal function; check for helminth ova in feces within 3-4 weeks following the initial therapy

Chemistry & Properties

Formula	C16H13N3O3
Molecular weight	295.3 g/mol
IUPAC name	methyl N-(6-benzoyl-1H-benzimidazol-2-yl)carbamate
CAS	31431-39-7
PubChem CID	4030
InChIKey	`OPXLLQIJSORQAM-UHFFFAOYSA-N`
logP	2.97 (XLogP 2.8)
Polar surface area	84.08 Å²
H-bond acceptors / donors	4 / 2
Drug-likeness (QED)	0.73
Lipinski violations	0

SMILES

COC(=O)Nc1nc2cc(C(=O)c3ccccc3)ccc2[nH]1

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	No

Enzyme interactions

Enzyme	Role	Detail
CYP1A2	Inhibitor	—
CYP1A2	Substrate	—
CYP2C8	Inhibitor	—

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MDR1 (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)MDR1 (Substrate)P-gp (Substrate)

Drug–drug interactions (10, DDInter)

Interacting drug	Severity	Management
Carbamazepine	moderate
Fosphenytoin	moderate
Iodide I-123	moderate
Iodide I-131	moderate
Metronidazole	moderate
Phenobarbital	moderate
Phenytoin	moderate
Primidone	moderate
Ritonavir	moderate
Cimetidine	minor

Registered Products (12)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Vermin Tab	Tablet 100 mg	6 tab	Petra Drug Store	0.700
Vermin susp	Suspension 2 g/100 ml	30 ml	Petra Drug Store	0.800
Vermox tabs	Tablet 500 mg	1 tab	Telegraph Drug Store	0.850
Vermazol	Tablet 100 mg	6 tab pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	1.010
Bendazole	Tablet 100 mg	6 tab pack varies	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	1.280
Bendazole susp	Suspension 50 mg/5 ml	60 ml	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	1.650
Vermox tabs	Tablet 100 mg	6 tab	Telegraph Drug Store	1.710
Vermox Susp	Suspension 20 mg/ml	30 ml	Telegraph Drug Store	2.200
Bendazole susp.	Suspension 100 mg/5 ml	60 ml	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	2.220
Bendazole	Tablet 100 mg	500 tab pack varies	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	47.500
Vermazol	Tablet 100 mg	600 tab pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	76.760
Bendazole	Tablet 100 mg	1000 tab pack varies	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	95.000