Ascarilen

Uses

Ascarilen 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. Ascarilen 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

Ascarilen is also used to associated treatment for these conditions: Adenocarcinoma of Colon, Ancylostoma duodenale infection, Ascaris lumbricoides infection, Carcinoma, Colorectal, Enterobius vermicularis infection, Necatoriasis due to necator americanus, Strongyloides Stercoralis Infection, Trichuris Infection

How Ascarilen works

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 Ascarilen 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. Ascarilen 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

Ascarilen dosage

The following doses of Ascarilen 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

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

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

Precaution

Effect on ability to drive or operate machinery: There is no evidence to suggest that Ascarilen , 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

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

Food Interaction

• Take on an empty stomach.

Ascarilen Alcohol interaction

[Moderate] GENERALLY AVOID:

Case histories have suggested that levamisole is associated with some side effects (including headache, fever, shivers, and dizziness) that suggest an disulfiram-like interaction with alcohol.

These side effects could be alleviated by total abstinence from alcohol.

No mechanism has been established for this interaction.

Patients receiving levamisole should avoid alcohol.

Ascarilen Drug Interaction

Unknown: 5-hydroxytryptophan, charcoal, acetaminophen, aspirin, diphenhydramine, sucralfate, loratadine, dehydroepiandrosterone, diltiazem, doxycycline, multivitamin with iron, multivitamin, lysine, levothyroxine, atropine / diphenoxylate, metoprolol, acetaminophen, bioflavonoids, quetiapine, itraconazole

Elimination Route

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

Half Life

4.4-5.6 hours (biphasic)

Pregnancy & Breastfeeding use

Although studies in animals have shown that Ascarilen 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

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

Acute Overdose

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

Storage Condition

Tablet: Store in room temperature and protect from moisture.

Syrup: Store in room temperature and protect from light.

Innovators Monograph

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