Brutal

Uses

Albendazoleis used as anthelmintic against most nematodes and cestodes. It is effective against these gastro-intestinal parasites Bunostomum, Chabertia, Cooperia, Haemonchus, Ostertagia, Nematodirus, Strongyloides, Dictyocaulusviviparus, Monieziaexpansa, Liver flukes and Paramphistomes. It is also effective against different types of worms, lung flukes and lung nematodes.

Levamisole is a fast acting drug which acts on nematode nerve ganglia paralysing the worm’s musculature within seconds of contact. Unable to maintain their position, the worms are then ejected by normal peristaltic movement, usually within 24 hours of levamisole administration. Although it is certain that levamisole primarily influences the neuromuscular system of nematodes, it is possible that in some helminthes the inhibition of the fumarate reductase system contributes to the anthelmintic efficacy of levamisole. Levamisole is used for the treatment of infections by the following gastrointestinal wormspecies:

• Ascaris lumbricoides: Roundworm
• Necator americanus: Hookworm
• Ancylostoma duodenal: Hookworm
• E nterobius vermicularis: Pinworm
• Trichuris trichuria: Whipworm
• Strongyloides stercoralis: Threadworm
• Trichostrongylus colubriformis

Brutal is also used to associated treatment for these conditions: Ascariasis, Hookworm Infection, Hydatid disease caused by Echinococcus granulosus, Neurocysticercosis caused by Taenia solium, Other specified protozoal diseasesAdenocarcinoma of Colon, Ancylostoma duodenale infection, Ascaris lumbricoides infection, Carcinoma, Colorectal, Enterobius vermicularis infection, Necatoriasis due to necator americanus, Strongyloides Stercoralis Infection, Trichuris Infection

How Brutal works

Albendazole causes degenerative alterations in the tegument and intestinal cells of the worm by diminishing its energy production, ultimately leading to immobilization and death of the parasite. It works by binding to the colchicine-sensitive site of tubulin, thus inhibiting its polymerization or assembly into microtubules. As cytoplasmic microtubules are critical in promoting glucose uptake in larval and adult stages of the susceptible parasites, the glycogen stores of the parasites are depleted. Degenerative changes in the endoplasmic reticulum, the mitochondria of the germinal layer, and the subsequent release of lysosomes result in decreased production of adenosine triphosphate (ATP), which is the energy required for the survival of the helminth.

The mechanism of action of levamisole as an antiparasitic agent appears to be tied to its agnositic activity towards the L-subtype nicotinic acetylcholine receptors in nematode muscles. This agonistic action reduces the capacity of the males to control their reproductive muscles and limits their ability to copulate. The mechanism of action of Levamisole as an anticancer drug in combination with fluorouracil is unknown. The effects of levamisole on the immune system are complex. The drug appears to restore depressed immune function rather than to stimulate response to above-normal levels. Levamisole can stimulate formation of antibodies to various antigens, enhance T-cell responses by stimulating T-cell activation and proliferation, potentiate monocyte and macrophage functions including phagocytosis and chemotaxis, and increase neutrophil mobility, adherence, and chemotaxis.

Dosage

Brutal dosage

To keep animal free from helminths animal should be treated at 3 months interval.

Cattle & Buffalo: 7.5-10 mg/kg body weight or 14 bolus for 30-40 kg body weight, 12 bolus for 60-80 kg body weight & 1 boli for 120-160 kg body weight.

Goat & Sheep: 5-7.5 mg/kg body weight or 112 bolus for 13-20 kg body weight & 1 6 bolus for 27-40 kg body weight.

Dog & Cat: 15 mg/kg body weight or 18 bolus for 8-10 kg body weight & 14 bolus for 16-20 kg body weight.

Or as directed by the registered Veterinarian.

The following doses of Levamisole are given as a single administration, preferably after a light meal.

• Age 1-4 year: 1 Tablets or5 mlSyrup
• Age 5-15 year: 2 Tablets or10 mlSyrup
• Age 16year and over: 3 Tablets or 15 mlSyrup

In cases of severe hookworm infection it is suggested that a second standard dose be given one or seven days after the first, whichever timing is feasible.

Side Effects

Albendazole is time tested and clinically proven well tolerated drug. Established wide safety margin than any other anthelmentic due to greater selective affinity for parasitic b-tubulin than for animal tissues. However, in some cases nausea and vomiting may occur.

Side-effects are infrequent. They are usually mild and transient and include nausea, vomiting, abdominal pain, giddiness(dizziness) and headache. An encephalopathylike syndrome has been reported to have occurred in a few patients two or three weeks after treatment.

Toxicity

Symptoms of overdose include elevated liver enzymes, headaches, hair loss, low levels of white blood cells (neutropenia), fever, and itching.

LD₅₀ = 40 mg/kg (Pigs, subcutaneous); LD₅₀ = 180 mg/kg (rat, oral)

Precaution

Before using Albendazole inform the registered Veterinarian that your animals are not allergic to it; or to other benzimidazole anthelmintic drugs (e.g. Mebendazole).

Effect on ability to drive or operate machinery: There is no evidence to suggest that Levamisole , used for anthelmintic purpose, will produce sedation. Mild and transient giddiness is an infrequent side-effect of treatment. No precautions are suggested concerning the ability to drive or operate machinery.

In case of concurrent microfilaraemia transient fever may occur.

Interaction

Albendazole has been shown to induce liver enzymes of the cytochrome P-450 system responsible for its own metabolism. There is, therefore, a theoretical risk of interaction with theophylline, anticonvulsants, anticoagulants, oral contraceptives and oral hypoglycaemics. Care should therefore be exercised during the introduction of Albendazole in patients receiving the above groups of compounds

May increase toxicity of phenytoin. Increases bioavailability of ivermectin; decreases bioavailability of albendazole. Alcohol causes disulfiram-like reaction.

Elimination Route

Poorly absorbed from the gastrointestinal tract due to its low aqueous solubility. Oral bioavailability appears to be enhanced when coadministered with a fatty meal (estimated fat content 40 g)

Levamisole is rapidly absorbed (2 hours) from the gastrointestinal tract.

Half Life

Terminal elimination half-life ranges from 8 to 12 hours (single dose, 400mg).

4.4-5.6 hours (biphasic)

Elimination Route

Albendazole is rapidly converted in the liver to the primary metabolite, albendazole sulfoxide, which is further metabolized to albendazole sulfone and other primary oxidative metabolites that have been identified in human urine. Urinary excretion of albendazole sulfoxide is a minor elimination pathway with less than 1% of the dose recovered in the urine. Biliary elimination presumably accounts for a portion of the elimination as evidenced by biliary concentrations of albendazole sulfoxide similar to those achieved in plasma.

Pregnancy & Breastfeeding use

Albendazole should not use first 45 days of pregnancy of cow. Do not administer to ewes or does during the first 30 days of pregnancy. Sufficient data on use during lactation is not available. Therefore breast feeding should be discontinued during and for a minimum of 5 days after treatment.

Although studies in animals have shown that Levamisole produces no teratogenic effects, current medical practice requires that the benefits of any drug used during pregnancy should be weighed against the possible dangers.

Contraindication

This is known to be teratogenic and embryo-toxic in some animals. Therefore it should not be administered during pregnancy or in women thought to be pregnant. It should only be used in the treatment of echinococcosis if there is constant medical supervision with regular monitoring of serumtransaminase concentrations and of leucocyte and platelet counts.

There is no absolute contra-indication to the use of Levamisole

Acute Overdose

If poisoning or excessive overdosageis suspected, it is recommended for vomiting be induction or gastric lavage and such symptomatic supportive therapy to be administered.

Counter possible anticholinesterase activity with e.g. atropine. Control blood pressure and respiration . Do not use sedatives.

Storage Condition

Do not store above 30 degree centigrade. Keep away from light and out of the reach of children.

Tablet: Store in room temperature and protect from moisture.

Syrup: Store in room temperature and protect from light.

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