Peringatan Keamanan

Moxidectin is reported to be safe as it is reported to be a poor substrate of P-glycoprotein.A33385 The reported LD50in mice are in the range of 70-131 micromol/kg.A33397 Carcinogenicity studies have not been performed. Moxidectin was shown to present no effects in genotoxicity, mutagenicity and fertility.FDA label The reports of overdose there are related to the presence of transient and self-limiting neurological signs including the presence of convulsions.F139

Moxidectin

DB11431

small molecule approved investigational vet_approved

Deskripsi

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.A33385 Moxidectin was developed by Medicines Development for Global Health and FDA approved in June 13, 2018.L2970

Struktur Molekul 2D

Berat 639.83
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Moxidectin reporter terminal half-life is 20.2 days.[A33398]
Volume Distribusi 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.[A33398]
Klirens (Clearance) The apparent clearance of moxidectin is 3.5 L/hour.[A33428]

Absorpsi

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.A33385 It is also important to mention that oral bioavailability is enhanced with the co-administration with lipids.T237

Metabolisme

Reports have registered enzymatic modification in humans and in nematodes. In the case of moxidectin, there has been registered C29-30- and C14-mono-hydroxymethyl derivatives mainly by the cytochrome CYP3A and CYP2B. The metabolism of moxidectin is considered to contribute to a small extent to the elimination.A33398 Some other metabolites formed are O-demethyl-dihydroxy metabolites. The metabolism of the of moxidectin is not major as the major residue in fat, liver, kidney and muscle is the unchanged moxidectin.T236

Rute Eliminasi

When moxidectin is orally administered, 2% of the dose is eliminated unchanged in the feces within 72 hours. Renal elimination is negligible.FDA label

Interaksi Makanan

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

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Glutamate-gated chloride channel GluClX
GABA-A gated chloride channel
ABC transporters

Referensi & Sumber

Artikel (PubMed)
  • PMID: 19778466
    Cobb R, Boeckh A: Moxidectin: a review of chemistry, pharmacokinetics and use in horses. Parasit Vectors. 2009 Sep 25;2 Suppl 2:S5. doi: 10.1186/1756-3305-2-S2-S5.
  • PMID: 23133688
    Menez C, Sutra JF, Prichard R, Lespine A: Relative neurotoxicity of ivermectin and moxidectin in Mdr1ab (-/-) mice and effects on mammalian GABA(A) channel activity. PLoS Negl Trop Dis. 2012;6(11):e1883. doi: 10.1371/journal.pntd.0001883. Epub 2012 Nov 1.
  • PMID: 24533275
    Prichard R, Menez C, Lespine A: Moxidectin and the avermectins: Consanguinity but not identity. Int J Parasitol Drugs Drug Resist. 2012 Apr 14;2:134-53. doi: 10.1016/j.ijpddr.2012.04.001. eCollection 2012 Dec.
  • PMID: 21896908
    Korth-Bradley JM, Parks V, Chalon S, Gourley I, Matschke K, Gossart S, Bryson P, Fleckenstein L: Excretion of moxidectin into breast milk and pharmacokinetics in healthy lactating women. Antimicrob Agents Chemother. 2011 Nov;55(11):5200-4. doi: 10.1128/AAC.00311-11. Epub 2011 Sep 6.
Textbook
  • ISBN: 978-0-12-407691-4
    Brittain H. (2013). Profiles of drug substances and related methodology. Volume 38 (1st ed.). Elsevier.
  • Varga M. (2014). Textbook of rabbit medicine (2nd ed.). Butterworth Heinmann.
Attachment

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Moxidectin
    Tablet • 2 mg/1 • Oral • US • Approved
  • Moxidectin
    Tablet • 2 mg/1 • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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