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General Description:

Bioallethrin, identified by CAS number 584-79-2, is a notable compound with significant therapeutic applications. Bioallethrin refers to a mixture of two of the allethrin isomers (1R,trans;1R and 1R,trans;1S) in an approximate ratio of 1:1, where both isomers are active ingredients. A mixture of the two same stereoisomers, but in an approximate ratio of R:S in 1:3, is called esbiothrin. A mixture containing only S-forms of allethrin is referred to as esbioallethrin or S-bioallethrin. Bioallethrin is a synthetic pyrethroid used as a pesticide against household pest insects such as mosquitoes, houseflies and cockroaches. It is claimed to have low mammalian toxicity.

Indications:

This drug is primarily indicated for: Bioallethrin was used for lice and scabies infestation. Other pyrethroids are now used in place of bioallethrin. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Bioallethrin undergoes metabolic processing primarily in: Metabolism of bioallethrin in both rats and humans is considered to be virtually 100% oxidative . This is because bioallethrin is very resistant to hydrolysis of its ester group although a negligible amount of hydrolysis may occur. In humans bioallethrin is metabolized primarily by CYP2C19 with some metabolism by CYP2C8, CYP3A4, and CYP2C9*2 . The metabolites produced include primary alcohols via allylic oxidation near the cyclopropane group and subsequent oxidation to carboxylic acid, formation of a primary alcohol via oxidation of a methyl group to located on the cyclopropane portion of the molecule, formation of a primary alcohol via allylic oxidation near the 5-membered ring or formation of an epoxide at this location and subsequent hydrolysis to a diol. In rats bioallethrin has been found to be metabolized mainly by CYP2C6, CYP2C11, and CYP3A1 with some contribution from CYP1A1, CYP2A1 and CYP3A2 . Rats appear to metabolize bioallethrin at about 15 times the rate of humans. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Route of Elimination:

The elimination of Bioallethrin from the body primarily occurs through: Pyrethroids are excreted in both the feces and urine but values specific to bioallethrin are not available . Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Pharmacodynamics:

Bioallethrin exerts its therapeutic effects through: Bioallethrin causes respiratory paralysis in lice and scabies parasites resulting in death . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Bioallethrin functions by: Bioallethrin, like other pyrethroids, binds to voltage gated sodium channels in their closed state and modifies the gating kinetics . Channel opening appears to increase affinity of the channel for pyrethroids like bioallethrin. Once bound pyrethroids slow both the opening and closing of the sodium channel resulting in a need for stronger excitatory potentials to produce an action potential and a delay in repolarization. The these changes make the neuron more susceptible to large action potentials and repeated firing by both increasing the initial threshold and reducing the input needed for after-potentials. When repeated firing does occur, the nerve terminal will release more neurotransmitter which can produce muscle paralysis through tetanus. This paralysis stops the breathing of lice and scabies parasites resulting in death. Some pyrethroids act on calcium channels to increase intracelllular calcium . Bioallethrin produces a very small increase in intracellular calcium in mouse neocortical neurons by acting on N-type calcium channels but the effect returns to baseline within 2 min. In contrast bioallethrin has been found to block L T, and P/Q-types of voltage gated calcium channels in human embryonic kidney cell cultures . Bioallethrin has been found to inhibit both sodium-calcium dependent and magnesium-calcium ATP hydrolysis in insects although it, along with other type I pyrethroids, has a greater effect on sodium-calcium dependent hydrolysis . Bioallethrin may stimulate phosphoinositol breakdown in synaptoneuromes as other type I pyrethroids have been observed to do so . Other type I pyrethoids have also been found to bind to kainate receptors . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Categories:

Bioallethrin is categorized under the following therapeutic classes: Agents causing hyperkalemia, Agrochemicals, Antiarrhythmic agents, Antiparasitic Products, Insecticides and Repellents, Bradycardia-Causing Agents, Calcium Channel Blockers, Compounds used in a research, industrial, or household setting, Cyclopentane Monoterpenes, Cytochrome P-450 CYP2C19 Substrates, Cytochrome P-450 CYP2C8 Substrates, Cytochrome P-450 CYP2C9 Substrates, Cytochrome P-450 CYP3A Substrates, Cytochrome P-450 CYP3A4 Substrates, Cytochrome P-450 Substrates, Ectoparasiticides, Incl. Scabicides, Ectoparasiticides, Incl. Scabicides, Insecticides and Repellents, Insecticides, Monoterpenes, Pesticides, Pyrethrines, Incl. Synthetic Compounds, Pyrethrins, Stereoisomerism, Terpenes, Toxic Actions. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Bioallethrin include:

• Water Solubility: 4.6 mg/L
• Boiling Point: 165-170
• logP: 4.7