Depalléthrine

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

Depalléthrine 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. Depalléthrine 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.

Depalléthrine causes respiratory paralysis in lice and scabies parasites resulting in death .

Depalléthrine
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	Depalléthrine
Generic	Bioallethrin
Bioallethrin Other Names	Depalléthrine
Type
Groups	Approved, Experimental
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Depalléthrine was used for lice and scabies infestation. Other pyrethroids are now used in place of bioallethrin.

How Depalléthrine works

Depalléthrine, 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 . Depalléthrine 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 . Depalléthrine 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 . Depalléthrine 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 .

Toxicity

Depalléthrine can produce hypersensitivity reactions in patients sensitive to ragweed or chrysanthemum . Ingestion of bioallethrin can produce life-threatening convulsions or coma. Less serious toxic effects include sore throat, nausea, vomiting, abdominal pain, mouth ulceration, increased secretions and/or dysphagia. Systemic effects include dizziness, headache and fatigue are common, and palpitations, chest tightness and blurred vision and occur 4-48 h after exposure.

Depalléthrine is not carcinogenic or mutagenic . In rats doses over 58.7 mg/kg/day produce reproductive effects and doses over 125 mg/kg/day are embryotoxic.