Common name: NETOBIMIN

Other names: TOTABIN-SCH
Type: veterinary medecine
Chemical class: pro-benzimidazole

CHEMICAL STRUCTURE

Molecular structure of NETOBIMIN 

 


EFFICACY AGAINST PARASITES

Type of action: broad-spectrum nematicide, taenicide and flukicide anthelmintic, endoparasiticide
Main veterinary parasites controlled: gastrointestinal and respiratory roundworms (= nematodes), tapeworms and adult liver flukes

Efficacy against a specific parasite depends on the delivery form and on the dose administered. 

Click here for general information on features and characteristics of PARASITICIDES.


DOSING

Dosing recommendations for antiparasitics depend on national regulations. National regulatory authorities determine whether a product is approved for a given indication, i.e. use on a particular host at a specific dose and against a specific parasiteCheck the labels of the products available in your country for specific information on approved indications

The table below indicates some usual dosing recommendations for netobimin issued by manufacturers or documented in the scientific literature. They may not be approved in some countries.

Netobimin is a broad spectrum anthelmintic effective against roundworms and, depending on the dose also against some tapeworms (e.g. Moniezia spp) and a few trematodes (e.g. Fasciola hepatica adults). It is a so-called pro-benzimidazole, i.e. it is transformed into albendazole once in the host's gut, and has roughly the same spectrum of efficacy. It is completely ineffective against external parasites. Oral administration is the rule. It is used very scarcely in livestock (manily in drenches), but not in horses or pets.

In ruminants, a 50% reduction of the diet 36 prior and 8 hours after treatment slows down the passage through the stomach, which increases the bioavailability of albendazole and its metabolites and consequently its efficacy against gastrointestinal parasites.

All benzimidazoles have almost no residual effect, i.e. they kill the parasites during a few hours after treatment but offer no significant protection against re-infestation.

Dosing recommendations for NETOBIMIN
CATTLE
Delivery Parasites Dose (against albendazole-susceptible parasites)
Oral Gastrointestinal roundworms 5-10 mg/kg
Oral Ostertagia ostertagi inhibited larvae 10 mg/kg
Oral Dictyocaulus viviparus 3.8-10 mg/kg
Oral Fasciola hepatica, adults 20 mg/kg
Oral Tapeworms (e.g. Moniezia spp) 7.5 mg/kg 
Oral Dicrocoelium dendriticum 20 mg/kg or 2.8 mg/kg/day in drinking water
SHEEP & GOATS
Delivery Parasites  Dose (against albendazole-susceptible parasites)
Oral Gastrointestinal roundworms 7.5 mg/kg
Oral Gastr. roundworms inhib. larvae 20 mg/kg
Oral  Dictyocaulus filaria 7.5 mg/kg 
Oral  Muellerius capillaris 7.5 mg/kg x3 days, or 10 mg/kg x2 days
Oral Fasciola hepatica, adults 20 mg/kg
Oral Dicrocoelium dendriticum 15-20 mg/kg
Oral Moniezia spp 7.5 mg/kg
SOUTH AMERICAN CAMELIDS
Delivery Parasites  Dose (against albendazole-susceptible parasites)
Oral Roundworms 15 mg/kg

DISCLAIMER: Liability is denied for any possible damage or harm to persons, animals or any other goods that could follow the transmission or use of the information, data or recommendations in this site by any site visitor or third parties.


SAFETY

Oral LD50, rat, acute*: >6400 mg/kg
Dermal LD50, rat, acute*: not found
* These values refer to the active ingredient. Toxicity has to be determined for each formulation as well. Formulations are usually significantly less toxic than the active ingredients.

WARNING: netobimin, is quickly metabolized to albendazole and albendazole sulfoxide (= ricobendazole) which, as well as parbendazole and cambendazole can be teratogenic and should not be administered to pregnant females.

MRL (maximum residue limit) established for either beef, mutton pork or chicken meat*:

  • CODEX: Yes
  • EU: Yes
  • USA: Yes
  • AUS: Yes

* In the form of albandazole solfoxide and sulfone. This information is an indicator of the acceptance of an active ingredient by the most influential regulatory bodies for use on livestock.

Withholding periods for meat, milk, eggs, etc. depend on delivery form, dose and national regulations. Check the product label in your country.

General information on the safety of veterinary antiparasitics is available in specific articles in this site (click to visit):

WARNING

Never use products for livestock on dogs and cats unless they are explicitly approved for both livestock and pets. Pets may not tolerate livestock formulations

It is obvious that veterinary products are not intended for and should never be used on humans!!!


MARKETING & USAGE

Decade of introduction: 1980
Introduced by: SCHERING PLOUGH → INTERVET → MSD ANIMAL HEALTH
Some original brands: HAPADEX, HAPASIL
Patent: Expired (particular formulations may be still patent-protected)

Use in LIVESTOCK: Yes, scarce
Use in HORSES: No
Use in iDOGS and CATS: No

Main delivery forms: 

Use in human medicine: No
Use in public/domestic hygiene: No
Use in agriculture: No
Generics available:  Yes, few


PARASITE RESISTANCE

In livestock: Yes, as all benzimidazoles, very frequent worldwide in gastrointestinal roundworms in sheep, goats and cattle. Less frequent in liver flukes in ruminants in several countries.


SPECIFIC FEATURES

Albendazole is a veteran anthelmintic (wormer) compound belonging to the chemical class of the pro-benzimidazoles. It is transformed into albendazole in the stomach and the intestine of the host, shortly after ingestion. Once transformed its behavior is comparable to the one of albendazole.

Netobimin is scarcely used in livestock. It is available mainly in the form of drenches for cattle, sheep and goats.

Netobimin is not used in swine, poultry dogs and cats.

Efficacy of netobimin

Netobimin itself has no anthelmintic properties. Therefore its efficacy depends on its successful transformation to albendazole.

Albendazole is the benzimidazole with the broadest spectrum of efficacy. It is effective against gastrointestinal roundworms and lungworms of livestock, including adults and L4-larvae of the most important species (e.g. of the genus Bunostomum, Haemonchus, Ostertagia - Teladorsagia, Trichostrongylus, Cooperia, Nematodirus, Chabertia, Oesophagostomum, Trichuris, Dictyocaulus, etc.) as well as arrested larvae of several species. It is also effective against most livestock tapeworms (e.g. Moniezia, Taenia) and against adult liver flukes (Fasciola hepatica and Fascioloides magna), but not against immature stages.

Netobimin has only a limited residual effect. This means that a single administration will kill the parasites present in the host at the time of treatment and protect against re-infestations for a few days, but not for weeks.

Unfortunately, resistance of several gastrointestinal roundworms to all benzimidazoles, including albendazole (and its precursor netobimin) is already very high and very frequent worldwide in sheep and goats, slightly lower in cattle. Resistance of the liver fluke (Fasciola hepatica) is not that dramatic, but is spreading in several countries. For this reason, the risk that benzimidazoles fail to protect ruminants against gastrointestinal roundworms is considerable worldwide.

Pharmacokinetics of netobimin

Following oral administration netobimin is hardly detectable in plasma. It is very quickly transformed to albendazole in the gastrointestinal tract, which is progressively absorbed into the bloodstream.

Absorbed albendazole is very quickly metabolized in the liver to its sulfoxide derivative, which has also anthelmintic efficacy and is exactly ricobendazole, another commercial anthelmintic active ingredient. In fact, in most species the parent molecule remains almost undetectable in blood after administration. In a second much slower step the sulfoxide is further metabolized in the liver to the sulfone metabolite that has no anthelmintic efficacy. The high plasma levels of albendazole sulfoxide make it effective against adult worms and immature stages in various host tissues and organs outside the gastrointestinal tract.

Interestingly, part of the sulfoxide produced through metabolism is released back to the rumen, where the bacterial flora reduces it back to albendazole. This increases the bioavailability of albendazole in ruminants.

Excretion occurs through bile and feces, as well as through urine. In ruminants 60-70% of the administered dose is excreted through urine in the form of various metabolites, the major one being the sulfoxide. In sheep about 14% of the administered dose is excreted through the bile, partly in the form of various active metabolites, which enables reaching effective anthelmintic concentrations in the bile ducts.

Mechanism of action of netobimin

Netobimin acts on the worms only after transformation to albendazole. The molecular mode of action of albendazole and all benzimidazoles consists in binding to tubulin, a structural protein of microtubules. These microtubules are important organelles involved in the motility, the division and the secretion processes of cells in all living organisms. In the worms the blocking of microtubules perturbs the uptake of glucose, which eventually empties the glycogen reserves. This blocks the whole energy management mechanism of the worms that are paralyzed and die or are expelled.

Since cell division is also disturbed, worm egg production and development is also blocked by benzimidazoles, i.e. most of them also have an ovicidal effect.

Albendazole also inhibits a helminth-specific fumarate reductase, an enzyme involved in the energy management of the worm cells as well.

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