The major final metabolites that are excreted by humans are:
methyl [5-(propylsulfonyl-1H-benzimidazol-2-yl)] carbamate,
methyl [6-hydroxy 5-(n-propylsulfonyl)-1H-benzimidazole-2-yl)] carbamate,
methyl [5-(n-propylsulfinyl)-1H-benzimidazole-2-yl)] carbamate,
5-(n-propylsulfonyl)-1H-benzimidazole-2-yl amine, and
5-(n-propysulfinyl)-1H-benzimidazole-2-yl amine.There are also some minor hydroxylated sulfated or glucuronidated derivatives. No unchanged albendazole is excreted, as it is metabolized too quickly.In humans, the metabolites are excreted mostly in bile, with only a small amount being excreted in the urine (less than 1%) and feces. In ruminants, 60–70% of the metabolites are excreted in the urine.Like all benzimidazoles, albendazole has no residual effect, and thus protects poorly against reinfestations. History
Albendazole, patented in 1975, was invented by Robert J. Gyurik and Vassilios J. Theodorides and assigned to SmithKline Corporation. It was introduced in 1977 as an antihelminthic for sheep in Australia, and was registered for human use in 1982. Society and culture
Brand names
Brand names include: Albenza, Alworm, Andazol, Eskazole, Noworm, Zentel, Alben-G, ABZ, Cidazole, Wormnil etc. Cost
In Raleigh, North Carolina, the brand-name prescription cost was around US$800, and US$540 for the generic. The pharmaceutical company Amedra increased the price after purchasing the rights to the drug, instead of lowering it as generics are predicted to do, drawing criticism from patients rights advocates.In 2013, GlaxoSmithKline donated 763 million albendazole tablets for the treatment and prevention of parasitic infections in developing countries, bringing the total to over 4 billion tablets donated since 1998. Veterinary use
Albendazole is mainly used in cattle and sheep, but has found some use in cats and dogs as well; it is also used in ratite birds for flagellate parasites and tapeworms.
Paromomycin may have dangerous reactions when used with the paralytic succinylcholine by increasing its neuromuscular effects.There are no known food or drink interactions with paromomycin. Mechanism
Paromomycin is a protein synthesis inhibitor in nonresistant cells by binding to 16S ribosomal RNA. This broad-spectrum antibiotic soluble in water, is very similar in action to neomycin. Antimicrobial activity of paromomycin against Escherichia coli and Staphylococcus aureus has been shown. Paromomycin works as an antibiotic by increasing the error rate in ribosomal translation. Paromomycin binds to a RNA loop, where residues A1492 and A1493 are usually stacked, and expels these two residues. These two residues are involved in detection of correct Watson-Crick pairing between the codon and anti codon. When correct interactions are achieved, the binding provides energy to expel the two residues. Paromomycin binding provides enough energy for residue expulsion and thus results in the ribosome incorporating the incorrect amino acid into the nascent peptide chain. Pharmacokinetics
Absorption
GI absorption is poor. Any obstructions or factors which impair GI motility may increase the absorption of the drug from the digestive tract. In addition, any structural damage, such as lesions or ulcerations, will tend to increase drug absorption.For intramuscular (IM) injection, the absorption is rapid. Paromomycin will reach peak plasma concentration within one hour following IM injection. The in-vitro and in-vivo activities parallel those of neomycin. Elimination
Almost 100% of the oral dose is eliminated unchanged via feces. Any absorbed drug will be excreted in urine.