Ascapil Mono

Uses

Ascapil Mono is used for the treatment of the following infections:

Strongyloidiasis of the intestinal tract. Ascapil Mono is used for the treatment of intestinal (i.e., nondisseminated) strongyloidiasis due to the nematode parasite Strongyloides stercoralis.

This indication is based on clinical studies of both comparative and open-label designs, in which 64-100% of infected patients were cured following a single 200-mcg/kg dose of ivermectin.

Onchocerciasis: Ascapil Mono is used for the treatment of onchocerciasis due to the nematode parasite Onchocerca volvulus.

This indication is based on randomized, double-blind, placebo-controlled and comparative studies conducted in 1427 patients in onchocerciasis-endemic areas of West Africa. The comparative studies used diethylcarbamazine citrate (DEC-C).

NOTE: Ascapil Mono has no activity against adult Onchocerca volvulus parasites. The adult parasites reside in subcutaneous nodules which are infrequently palpable. Surgical excision of these nodules (nodulectomy) may be considered in the management of patients with onchocerciasis, since this procedure will eliminate the microfilariae-producing adult parasites.

Ascapil Mono is also used to associated treatment for these conditions: Acne Rosacea, Ascaris lumbricoides infection, Cutaneous larva migrans, Demodicidosis, Gnathostomiasis, Mansonella ozzardi infection, Mansonella streptocerca infection, Oesophagostomiasis, Onchocerciasis, Pediculosis Capitis, Scabies, Trichuriasis, Wuchereria bancroftii infection

How Ascapil Mono works

Ascapil Mono binds selectively and with high affinity to glutamate-gated chloride ion channels in invertebrate muscle and nerve cells of the microfilaria. This binding causes an increase in the permeability of the cell membrane to chloride ions and results in hyperpolarization of the cell, leading to paralysis and death of the parasite. Ascapil Mono also is believed to act as an agonist of the neurotransmitter gamma-aminobutyric acid (GABA), thereby disrupting GABA-mediated central nervous system (CNS) neurosynaptic transmission. Ascapil Mono may also impair normal intrauterine development of O. volvulus microfilariae and may inhibit their release from the uteri of gravid female worms.

Dosage

Ascapil Mono dosage

Oral

Filariasis:

• Adult: Dosing regimen depends on the causative agent. Mansonella streptocerca 150 mcg/kg as a single dose; Mansonella ozzardi 200 mcg/kg as a single dose.
• Child: ≥15 kg: Dosing regimen depends on the causative agent. Mansonella streptocerca 150 mcg/kg as a single dose; Mansonella ozzardi 200 mcg/kg as a single dose.

Scabies:

• Adult: Sarcoptes scabiei 200 mcg/kg as a single dose, repeat dose in 2 wk.
• Child: ≥15 kg: Sarcoptes scabiei 200 mcg/kg as a single dose, repeat dose in 2 wk.

Onchocerciasis:

• Adult:150 mcg/kg as a single dose; retreatment may be given every 6-12 mth until adult worms die.
• Child: >5 yr and ≥15kg: 150 mcg/kg as a single dose every 6-12 mth until adult worms die.

Ascariasis:

• Adult: Ascaris lumbricoides 150-200 mcg/kg as a single dose.
• Child: ≥15 kg: Ascaris lumbricoides 150-200 mcg/kg as a single dose.

Strongyloidiasis:

• Adult: 200 mcg/kg as a single dose for 1-2 days.
• Child: >15 kg: 200 mcg/kg as a single dose for 1-2 days.

Gnathostomiasis:

• Adult: Gnathostoma spinigerum: 200 mcg/kg once daily for 2 days.
• Child: ≥15 kg: Gnathostoma spinigerum: 200 mcg/kg once daily for 2 days.

Should be taken on an empty stomach.

Side Effects

Diarrhoea, nausea, vomiting, dizziness, pruritus, urticaria, rash, arthralgia, fever, myalgia, asthenia, postural hypotension, tachycardia, oedema, lymphadenopathy, sore throat, cough, headache, somnolence, transient eosinophilia, raised liver enzyme values.

Toxicity

LD₅₀ = 29.5 mg/kg (Mouse, oral). LD₅₀ = 10 mg/kg (Rat, oral). Adverse effects include muscle or joint pain, dizziness, fever, headache, skin rash, fast heartbeat.

Precaution

Concurrent Loa loa infection, impaired blood-brain barrier function due to infection.

Interaction

Bioavailability may be increased by alcohol, levamisole.

Food Interaction

• Take on an empty stomach.

Ascapil Mono Alcohol interaction

[Moderate] GENERALLY AVOID:

Alcohol may increase the plasma concentrations of ivermectin.

The mechanism of interaction is unknown.

In 20 healthy, nonsmoking patients with onchocerciasis, mean plasma ivermectin concentrations at 1, 3 and 4 hours post-dose (150 mcg/kg) were approximately 34% to 40% higher in the group given the medication with 750 mL of beer (4.5% v/v alcohol) than in controls who ingested the medication with water.

There were no side effects in either study or control subjects.

However, there have been anecdotal reports of increased central nervous system adverse effects and postural hypotension in patients who combined ivermectin with alcohol.

Patients receiving ivermectin therapy should preferably avoid the consumption of alcohol to prevent any undue adverse effects of ivermectin.

Ascapil Mono Drug Interaction

Unknown: diphenhydramine, diphenhydramine, ubiquinone, ubiquinone, acetylcysteine, acetylcysteine, bioflavonoids, bioflavonoids, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, zinc sulfate, zinc sulfate, cetirizine, cetirizine

Volume of Distribution

The volume of distribution is 3 to 3.5 L/kg and it does not cross the blood-brain barrier.

Elimination Route

Moderately well absorbed. Improved absorption with high fat meal.

Half Life

16 hours (also reported at 22-28 hours)

Elimination Route

Ascapil Mono is metabolized in the liver, and ivermectin and/or its metabolites are excreted almost exclusively in the feces over an estimated 12 days, with less than 1% of the administered dose excreted in the urine.

Pregnancy & Breastfeeding use

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Contraindication

Hypersensitivity. Pregnancy and lactation. Children <15 kg body weight.

Storage Condition

Store below 30°C.

Innovators Monograph

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