Ivermectin

Common name: Ivermectin tablets

Trade name: Hisun Macdin

Full names: Ivermectin tablets, Hisun Macatin, Ivermectin

Indications:

Onchocerciasis and strongyloidiasis and hookworm, roundworm, whipworm, and pinworm infections.

Usage and dosage:

The recommended dose for strongyloidiasis is a single oral dose of 200 μg/kg, taken with water. Usually there is no need to increase the dosage, but follow-up is required to ensure cure. Common dosages are as follows:

For those 15-24 kg, the dose is half a tablet (about 3 mg);

For those 25-34 kg, the dose is 1 tablet (approximately 6 mg); For those weighing more than 80 kg, the dose is 2 and a half tablets (approximately 15 mg); for those weighing more than 80 kg, the dosage is 200 μg/kg.

The recommended dose for onchocerciasis is a single oral dose of 150 μg/kg with water. Commonly used dosages are as follows:

For those 15-24 g, the dose is half a tablet (about 3 mg);

For those 25-44 kg, the dose is 1 tablet (approximately 6 mg); kg, 150 μg/kg.

Hookworm infection: Children over 14 years old take a single oral dose of 12 mg (equivalent to 0.2 mg/kg); children under 14 years old take a single oral dose of 6 mg.

Ascaris infection: Children over 14 years old take a single oral dose of 6 mg (equivalent to 0.1 mg/kg), and those under 14 years old take a single oral dose of 3 mg.

Thripworm infection: Children over 14 years old take a single oral dose of 12 mg (equivalent to 0.2 mg/kg); those under 14 years old take a single oral dose of 6 mg.

Pinworm infection: Children over 14 years old take a single oral dose of 12 mg (equivalent to 0.2 mg/kg); those under 14 years old take a single oral dose of 6 mg.

Specifications:

12mg ;

Gastrointestinal reactions: including anorexia, constipation, diarrhea, nausea, and vomiting;

Nervous system reactions: including dizziness, drowsiness, vertigo, and tremor;

Skin: including itching, rash, papules, rubella, and small pustules;

Ophthalmology: The following ophthalmic adverse reactions are caused by the disease itself, but they have also been reported to appear after treatment with ivermectin. These adverse reactions include visual abnormalities, eyelid edema, anterior uveitis, conjunctivitis, Limbitis, keratitis, chorioretinitis, or choroiditis. The above symptoms are generally mild, do not cause blindness, and generally resolve spontaneously without corticosteroid treatment.

Others: including joint pain, synovitis, axillary lymph node enlargement and tenderness, cervical lymph node enlargement and tenderness, inguinal lymph node enlargement and tenderness, lymph node enlargement and tenderness in other parts of the body, facial edema, peripheral edema, orthostatic hypotension, tachycardia, drug-induced headache, myalgia;

Laboratory test abnormalities: including elevated ALT and/or AST, leukopenia, eosinophilia, and hemoglobin increase.

Domestic clinical research data of this product show that its adverse reactions are basically consistent with those abroad, with an incidence rate of 1.6%. The main manifestations are headache, dizziness, abdominal pain, diarrhea, nausea, vomiting, and rash.

Taboos:

Pregnant and lactating women should not take this product.

Notes:

Historical data indicate that antifilarial drugs [such as diethylcarbamazine citrate (DEC-C)] can cause severe allergic reactions (Mazzotti reaction) and ophthalmic reactions in the skin and/or body of patients with onchocercia microfilament larvae. These reactions may be due to allergic and inflammatory reactions caused by dead microfilament larvae. These reactions may occur clinically in patients treated with ivermectin, and may or may not be related to the drug itself.

After treatment with microfilaricidal drugs, patients with allergic onchocerciatic dermatitis are more likely to suffer from serious adverse reactions, especially edema and onchocerciatic dermatitis, which aggravate carcinogenesis, mutagenicity and reproductive toxicity.

Patients with strongyloidiasis using this product must have repeated stool tests to confirm that the infection has been cleared.

This product cannot kill adult onchocerciasis, so when using this product to treat onchocerciasis, continuous treatment is required.

Strongyloidiasis in immunocompromised hosts: Patients with immune deficiencies (including HIV infection) may require repeated treatment for intestinal strongyloidiasis. No clinical trials have been conducted to determine alternative dosing regimens in these patients, and suppressive therapy (eg, once monthly) may be useful.

A similar safety margin was observed in open trials in pediatric patients aged 6 to 13 years. The safety and effectiveness in children weighing less than 15 kg have not been established and should be used with caution in these pediatric patients.

Storage:

Shade, seal, and store in a dry place

Mechanism of action:

This product is a derivative of avermectin, an oral semi-synthetic broad-spectrum antiparasitic drug. This product is effective against most nematodes (but not all nematodes) of various life cycles; it is effective against microfilariae of onchocerciasis, but not against adult worms; it is also effective against Strongyloides faecalis which is only in the intestine.

This product has a selective inhibitory effect. It binds with high affinity to the chloride ion channel in the nerve cells and muscle cells of invertebrate animals, which has glutamate as the valve. This leads to an increase in the permeability of the cell membrane to chloride ions, causing hyperpolarization of nerve cells or muscle cells, paralyzing or killing the parasite. This product can also interact with chloride channels of other ligand valves such as the neurotransmitter g-aminobutyric acid (GABA).

The selectivity of this product is due to the fact that some mammals do not have glutamate-chloride channels, and abamectin has only low affinity for the mammalian ligand-chloride channel. This product cannot penetrate the human blood-brain barrier.

Safety and efficacy:

Ivermectin tablets are a broad-spectrum antiparasitic drug that is an agonist of the neurotransmitter gamma tyrosine, destroying the central nervous system mediated by it. It may also be caused by the increased permeability of chloride ions in the nerve cells and muscle cells of invertebrate animals using glutamate as a valve, causing hyperpolarization of nerve cells or muscle cells, causing paralysis or death of the parasite. Although it has no effect on adult onchocerciasis, it can affect the normal development of onchocerciasis microfilariae in the female uterus and inhibit their release from the uterus of pregnant worms. The effect of this product on microfilariae is slower and longer-lasting than that of diethylcarbamazine citrate. It can quickly reduce the number of microfilariae in the patient's skin, but has a slower effect on the microfilariae in the patient's cornea and anterior chamber. It is mainly used to treat onchocerciasis infections; it is also used to treat Strongyloides stercoralis, roundworms, whipworms, pinworms and other filarial worm infections. The oral administration is 1x for 4 hours. The drug concentration is very high in the liver and adipose tissue and cannot penetrate the blood-brain barrier. The plasma protein binding rate is 93%. After oral administration, only a small amount is excreted in the urine as unchanged form, and the rest is excreted in the feces with a t1/2 time of 10 hours.