Moxidectin

Moxidectin Uses, Dosage, Side Effects, Food Interaction and all others data.

Moxidectin is a potent, broad-spectrum endectocide (antiparasitic that is active against endo- and ecto-parasites) with activity against nematodes, insects, and acari. It was first used in cattle followed by an approved use in general animals. It is a semi-synthetic methoxine derivative of nemadectin which is a 16-member pentacyclic lactone of the milbemycin class. Moxidectin differs by the absence of a disaccharide moiety on carbon 13, a substituted olefinic side chain at carbon 25 and a unique methoxime moiety at carbon 23. Due to these modifications, moxidectin is classified as a second generation macrocyclic lactone. Moxidectin was developed by Medicines Development for Global Health and FDA approved in June 13, 2018.

Moxidectin has been reported to be highly effective against Onchocerca volvulus when compared to ivermectin. When moxidectin was administered in infected individuals, the microfilarial load in the skin was lower even when compared to the current therapy, ivermectin. The levels of microfilarial got reduced to an undetectable level while being safe to be used in mass drug administration.

Moxidectin
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Moxidectin
Generic	Moxidectin
Moxidectin Other Names	Moxidectin, Moxidectina, Moxidectinum
Type	Oral
Formula	C₃₇H₅₃NO₈
Weight	Average: 639.83 Monoisotopic: 639.377117671
Protein binding	This pharmacokinetic property in humans is unknown.
Groups	Approved, Investigational, Vet approved
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Moxidectin is indicated for the treatment of river blindness, also called onchocerciasis, in patients aged 12 years and older. River blindness is caused by a parasitic worm Onchocerca volvulus and it is manifested as severe itching, disfiguring skin conditions and visual impairment caused by the worm's larvae.

The transmission of Onchocerca volvulus is performed person to person by black flies that breed in fast-flowing rivers in sub-Saharan Africa, Yemen and South and Central America. The larvae released by the adult parasite invade skin and eyes where they can produce the severe disease manifestations.

Moxidectin is also used to associated treatment for these conditions: Onchocerciasis caused by Infection with Onchocerca volvulus

How Moxidectin works

Moxidectin selectively binds to the parasite's GABA-A and glutamate-gated chloride ion channels which are vital for the function of invertebrate nerve and muscle cells. It presents activity against the parasite but it does not kill him. Once moxidectin is bound, there is an increased permeability leading to an influx of chloride ions and flaccid paralysis of the parasite.

Toxicity

Moxidectin is reported to be safe as it is reported to be a poor substrate of P-glycoprotein. The reported LD50in mice are in the range of 70-131 micromol/kg. Carcinogenicity studies have not been performed. Moxidectin was shown to present no effects in genotoxicity, mutagenicity and fertility. The reports of overdose there are related to the presence of transient and self-limiting neurological signs including the presence of convulsions.

Food Interaction

Take with or without food. Co-administration with food slightly alters pharmacokinetics, but not to a clinically significant extent.

Volume of Distribution

Moxidectin presents a larger volume of distribution and mean residence time when compared to ivermectin. The reported volume of distribution is of 1.2 l/kg.

Elimination Route

The penetration of moxidectin in the parasite is not restricted as this compound is a very poor substrate of p-glycoprotein, which is vital for the reduction of the uptake of lipophilic compounds from the GI tract and for the increase in biliary, intestinal and renal secretion. After oral administration of moxidectin, the plasma maximal concentration of 70.4 mg/kg was reached after 0.37 day with a reported AUC of 363.6 mcg/day/ml. It is also important to mention that oral bioavailability is enhanced with the co-administration with lipids.