PERMETHRIN

Description

Permethrin is a synthetic pyrethrin derivative acts as a neurotoxin by depolarizing the nerve cell membrane. Permethrin disrupts the sodium channel current by which membrane repolarization is regulated resulting in fatal paralysis of the nerves in the exoskeletal respiratory muscles of susceptible arthropods, including lice and mite. Permethrin is sold under brand names NIx and Elimite to treat pediculosis, scabies and demodicidosis.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Voltage-sensitive sodium channel 7	Activator 1,430
Voltage-sensitive sodium channel alpha-subunit 5	Activator 1,430
Voltage-sensitive sodium channel 7	Inhibitor 8,297

Conditions

Condition	Modality	Highest Phase	Product
Scabies 9	Curative	Approved 8,429	ELIMITE
Head lice infestation 5	Curative	Approved 8,429	NIX
Pediculosis 9	Curative	Approved 8,429	NIX
Scabies 9	Curative	Approved 8,429	NIX

C_max

Value	Dose	Analyte	Population
49.46 μg/mL	460 mg/kg single, oral	PERMETHRIN plasma	Rattus norvegicus
0.6 μg/mL	10 mg/kg bw single, oral	PERMETHRIN serum	Gallus gallus domesticus
253 ng/mL	143 g single, oral	PERMETHRIN serum	Homo sapiens
615 ng/mL	143 g single, oral	PERMETHRIN serum	Homo sapiens
868 ng/mL	143 g single, oral	PERMETHRIN serum	Homo sapiens

AUC

Value	Dose	Analyte	Population
159 mg × h/L	46 mg/kg single, intravenous	PERMETHRIN plasma	Rattus norvegicus
965 mg × h/L	460 mg/kg single, oral	PERMETHRIN plasma	Rattus norvegicus
1.95 mg × h/L	10 mg/kg bw single, oral	PERMETHRIN serum	Gallus gallus domesticus
16.45 mg × h/L	10 mg/kg bw single, intravenous	PERMETHRIN serum	Gallus gallus domesticus
2.73 μg × h/mL	143 g single, oral	PERMETHRIN serum	Homo sapiens
6.26 μg × h/mL	143 g single, oral	PERMETHRIN serum	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
8.67 h	46 mg/kg single, intravenous	PERMETHRIN plasma	Rattus norvegicus
12.37 h	460 mg/kg single, oral	PERMETHRIN plasma	Rattus norvegicus
5.54 h	10 mg/kg bw single, oral	PERMETHRIN serum	Gallus gallus domesticus
4.73 h	10 mg/kg bw single, intravenous	PERMETHRIN serum	Gallus gallus domesticus
5.08 h	143 g single, oral	PERMETHRIN serum	Homo sapiens
4.82 h	143 g single, oral	PERMETHRIN serum	Homo sapiens

F_unbound

Value	Dose	Co-administered	Analyte	Population
10%			PERMETHRIN plasma	Homo sapiens

Doses

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Dose	Population	Adverse events
1 % 1 times / day multiple, topical Recommended	unhealthy, adult	Other AEs: Skin and subcutaneous conditions NEC...
5 % 1 times / day multiple, topical Recommended	unhealthy, adult	Other AEs: Dystonia...
200 ug/kg 1 times / day multiple, oral Recommended	unhealthy, adult

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AEs

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AE	Significance	Dose	Population
Skin and subcutaneous conditions NEC		1 % 1 times / day multiple, topical Recommended	unhealthy, adult
Dystonia		5 % 1 times / day multiple, topical Recommended	unhealthy, adult

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Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1,737	substrate 1,037	substrate 1,217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2B6 810 P-gp 1,461	CYP2B6 664 CYP1A2 1,054 CYP2C8 693 CYP2C19 991 CYP3A5 395 CYP2A6 543 CYP2E1 667 CYP3A7 110 CYP4A11 119 CES1 22 CES2 28 P-gp 1,537

Drug as perpetrator

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Target	Modality	Activity	Metabolite	Clinical evidence
P-gp 1,650	inhibitor 3,277	no
CYP2B6 1,001	inhibitor 3,277	yes

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Drug as victim

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Target	Modality	Activity
CYP1A2 1,054	substrate 3,367	likely
CYP2C8 693	substrate 3,367	likely
CYP2C9 1,037	substrate 3,367	likely
CYP2D6 1,217	substrate 3,367	likely
CYP3A5 395	substrate 3,367	likely

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Sourcing

Sourcing

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Vendor/Aggregator	ID	URL
ChEBI	CHEBI:34911	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:34911
ChemicalBook	CB8312237	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB8312237
MolPort	MolPort-003-933-021	https://www.molport.com/shop/molecule-link/MolPort-003-933-021
eMolecules	508544	https://www.emolecules.com/cgi-bin/more?vid=508544

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PubMed

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Title	Date	PubMed
Toxic effect of synthetic pyrethroid permethrin on the enzyme system of the freshwater fish Channa striatus.	1999 Nov	10576906
Estrogenicity of organophosphorus and pyrethroid pesticides.	2002 Oct 11	12396874
Molecular diagnosis of pyrethroid resistance in Mexican strains of Boophilus microplus (Acari: Ixodidae).	2002 Sep	12349861
Determination of pyrethrin and pyrethroid pesticides in urine and water matrixes by liquid chromatography with diode array detection.	2003 Nov-Dec	14979708
Determination of enantiomers of synthetic pyrethroids in water by solid phase microextraction - enantioselective gas chromatography.	2004 Feb 25	14969524

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Sample Use Guides

In Vivo Use Guide

Scabies: Thoroughly massage permethrin 5% cream into the skin from the head to the soles of the feet. Usually 30 grams is sufficient for an average adult. The cream should be removed by washing after 8 to 14 hours. Infants should be treated on the scalp, temple, and forehead. 1 application is generally curative. Lice: completely saturate the hair and scalp with the drug. Begin to apply it behind the ears and at the back of the neck. Leave the shampoo on the hair for 10 minutes, but no longer, rinse with warm water, towel dry hair and comb out tangles. If live lice are seen seven days or more after the first treatment, a second treatment should be given.

Route of Administration: Topical

In Vitro Use Guide

Unknown