Stromectol
Stromectol - General Information
Stromectol (22,23-dihydroavermectin B1a + 22,23-dihydroavermectin B1b) is a broad-spectrum anti-parasite medication, traditionally used against worms (except tapeworms), but more recently found to be effective against most mites and some lice too. It is mainly used in humans in the treatment of onchocerciasis, but is also effective against other worm infestations (such as strongyloidiasis, ascariasis, trichuriasis and enterobiasis).
Pharmacology of Stromectol
Stromectol is a semisynthetic, anthelminitic agent. It is an avermectin which a group of pentacyclic sixteen-membered lactone (i.e. a macrocyclic lactone disaccharide) derived from the soil bacterium Streptomyces avermitilis. Avermectins are potent anti-parasitic agents. Stromectol is the most common avermectin. It is a broad spectrum antiparasitic drug for oral administration. It is sometimes used to treat human onchocerciasis (river blindness). It is the mixture of 22,23-dihydro-avermectin B1a (at least 90%) and 22,23-dihydro-avermectin B1b (less than 10%).
Stromectol for patients
STROMECTOL should be taken on an empty stomach with water.
Strongyloidiasis: The patient should be reminded of the need for repeated stool examinations to document clearance of infection with Strongyloides stercoralis.
Onchocerciasis: The patient should be reminded that treatment with STROMECTOL does not kill the adult Onchocerca parasites, and therefore repeated follow-up and retreatment is usually required.
Stromectol Interactions
Stromectol Contraindications
STROMECTOL is contraindicated in patients who are hypersensitive to any component of this product.
Additional information about Stromectol
Stromectol Indication: For the treatment of intestinal (i.e., nondisseminated) strongyloidiasis due to the nematode parasite Strongyloides stercoralis. Also for the treatment of onchocerciasis (river blindness) due to the nematode parasite Onchocerca volvulus. Can be used to treat scabies caused by Sarcoptes scabiei.
Mechanism Of Action: Stromectol 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. Stromectol 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. Stromectol may also impair normal intrauterine development of O. volvulus microfilariae and may inhibit their release from the uteri of gravid female worms.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Ivermectin
Synonyms: 22,23-Dihydroxy-avermectin B; 22,23-Dihyroavermectin B1; 5-O-demethyl-22,23-dihydro-avermectin A1a
Drug Category: Anthelmintics; Antinematodal Agents; Antiprotozoal Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Ivermectin: Ivermectin B1; Ivermectin-luminol; Mectizan; Stromectol;
Absorption: Moderately well absorbed. Improved absorption with high fat meal.
Toxicity (Overdose): 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.
Protein Binding: 93%
Biotransformation: Primarily hepatic. 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.
Half Life: 16 hours (also reported at 22-28 hours)
Dosage Forms of Stromectol: Tablet Oral
Chemical IUPAC Name: Not Available
Chemical Formula: C95H146O28
Ivermectin on Wikipedia: https://en.wikipedia.org/wiki/Ivermectin
Organisms Affected: Parasitic nematodes and other roundworms
