Kokotine - General Information
An organochlorine insecticide that has been used as a pediculicide and a scabicide. It has been shown to cause cancer. [PubChem]
Pharmacology of Kokotine
Scabies is a common, highly pruritic infestation of the skin caused by Sarcoptes scabiei (lice). It is a very contagious condition with specific lesions, such as burrows, and nonspecific lesions, such as papules, vesicles and excoriations. The typical areas of the body it affects are finger webs, scalp (hair), wrists, axillary folds, abdomen, buttocks, inframammary folds and genitalia (males). It is characterized by intense night-time itching. Scabies is spread through close personal contact (relatives, sexual partners, schoolchildren, chronically ill patients and crowded communities). Scabies infestations and the corresponding symptoms can be eliminated by killing the scabies with topical insecticides or scabicides. Kokotine is a scabicide that is essentially and organochloride insecticide.
Kokotine for patients
Oils may enhance absorption. Therefore, simultaneous use of creams, ointments or oils should be avoided.
Lindane Lotion is contraindicated for premature neonates because their skin may be more permeable than full term infants and their liver enzymes may not be sufficiently developed. It is also contraindicated for patients with Norwegian (crusted) scabies due to possible increased absorption. It is also contraindicated for patients with known seizure disorders and for individuals with a known sensitivity to the product or any of its components.
Additional information about Kokotine
Kokotine Indication: For the treatment of patients infested with Sarcoptes scabiei (scabies or lice) who have either failed to respond to adequate doses, or are intolerant of other approved therapies.
Mechanism Of Action: Kokotine is an organochloride insecticide that exerts its parasiticidal action by being directly absorbed into the parasites (primarily lice, or scabies) and their ova. The gamma-aminobutyric acid (GABA(1)) receptor/chloride ionophore complex is the primary site of action for lindane, and other insecticides such as endosulfan, and fipronil. Blockage of the GABA-gated chloride channel reduces neuronal inhibition, which leads to hyperexcitation of the central nervous system, convulsions, and death.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Lindane
Synonyms: Not Available
Drug Category: Antiscabies Agent; Scabicide
Drug Type: Small Molecule; Approved
Other Brand Names containing Lindane: Aalindan; Aficide; Agrocide; Agrocide III; Agrocide WP; Ameisenmittel merck; Ameisentod; Aparasin; Aphtiria; Aplidal; Arbitex; Atlas steward; BBH; Ben-Hex; Bentox 10; Benzene hexachloride; Bexol; Celanex; Chloresene; Codechine; DBH; Detmol-Extrakt; Devoran; Dol Granule; Drilltox-Spezial Aglukon; Entomoxan; Esoderm; Fumite lindane; Gamacid; Gamene; Gamma-BHC dust; Gamma-Col; Gamma-HCH dust; Gammalin; Gammalin 20; Gammasan; Gammaterr; Gammexane; Gexane; HCCH; HCH; HGI; Heclotox; Hexa; Hexachloran; Hexachlorane; Hexachlorocyclohexane; Hexatox; Hexaverm; Hexicide; Hexit; Hexyclan; Hortex; Indane; Isotox; Jacutin; Kokotine; Kwell; Lendine; Lentox; Lidenal; Lindafor; Lindatox; Lindex; Lindosep; Lintox; Linvur; Lorexane; Milbol 49; Mszycol; Murfume grain store smoke; Neo-Scabicidol; New kotol; Nexen FB; Nexit; Nexit-Stark; Nexol-E; Nicochloran; Omnitox; Ovadziak; Owadziak; PMS Lindane; Pedraczak; Pflanzol; Quellada; Sang-"gamma"; Scabene; Scabene lotion; Spritz-Rapidin; Spruehpflanzol; Streunex; TAP 85; Thionex; Tri-6; Viton; beta-BHC; beta-Hexachlorocyclohexane; beta-Lindane;
Absorption: Lindane is absorbed significantly through the skin. A mean peak blood concentration of 28 nanograms per mL occurred in infants and children 6 hours after total body application of lindane lotion for scabies.
Toxicity (Overdose): Lindane is a moderately toxic compound via oral exposure, with a reported oral LD50 of 88 to 190 mg/kg in rats. Gamma-HCH (which constitutes 99% of lindane) is generally considered to be the most acutely toxic of the isomers following single administration. It is moderately toxic via the dermal route as well, with reported dermal LD50 values of 500 to 1000 mg/kg in rats, 300 mg/kg in mice, 400 mg/kg in guinea pigs, and 300 mg/kg in rabbits. Acute exposure to lindane may lead to central nervous system stimulation (usually developing within 1 hour), mental/motor impairment, excitation, clonic (intermittent) and tonic (continuous) convulsion. Other adverse reactions include central nervous system toxicity, as well as skin and gastrointestinal changes.
Protein Binding: 91%
Biotransformation: Primarily hepatic through dechlorination leading to 2-chlorophenol, 0-chlorophenol, chlorocyclohexane, chlorocyclohexanol.
Half Life: 18 hours
Dosage Forms of Kokotine: Lotion Topical
Chemical IUPAC Name: 1,2,3,4,5,6-hexachlorocyclohexane
Chemical Formula: C6H6Cl6
Lindane on Wikipedia: https://en.wikipedia.org/wiki/Lindane
Organisms Affected: Scabies (Sarcoptes scabei) and other insects