LINDANE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LINDANE (LINDANE).
Lindane is an organochlorine insecticide that acts by binding to the GABA-A receptor, inhibiting chloride ion influx, leading to hyperexcitation and death of arthropods. It also blocks voltage-gated sodium channels in neurons.
| Metabolism | Hepatic metabolism via cytochrome P450 (CYP) enzymes, predominantly CYP3A4 and CYP2B6, to polar metabolites (e.g., hexachlorobenzene). |
| Excretion | Primarily renal; ~50% as metabolites (conjugated and oxidized), <20% unchanged. Fecal excretion accounts for ~10-15% via biliary elimination. Small amounts excreted in sweat. |
| Half-life | Terminal half-life: 18-21 hours in adults; prolonged in obesity (up to 30-40 hours) due to adipose storage. Accumulation occurs with repeated dermal applications. |
| Protein binding | ~90% bound to plasma proteins, primarily albumin and lipoproteins. |
| Volume of Distribution | 2-4 L/kg, indicating extensive tissue distribution and accumulation in adipose tissue, brain, and liver. |
| Bioavailability | No systemic bioavailability data for topical use (minimal absorption ~10%). Oral bioavailability is not applicable (not used systemically). |
| Onset of Action | Topical: scabicidal effect begins within 24 hours after a single 8-12 hour application; pediculicidal effect within 12 hours. |
| Duration of Action | A single topical application provides scabicidal effect for 7-10 days due to residual drug in stratum corneum; pediculicidal effect lasts until nits are removed. Systemic effects are not relevant for topical use. |
Scabies: Apply 1% lotion or cream thinly to entire body from neck to toes; leave on for 8-12 hours, then wash off. Lice: Apply 1% shampoo to dry hair, lather with water, leave for 4 minutes, then rinse; repeat in 7 days if needed.
| Dosage form | LOTION |
| Renal impairment | No dose adjustment required for topical use; systemic absorption minimal. For severe renal impairment (eGFR <30 mL/min), consider alternative therapy due to potential neurotoxicity. |
| Liver impairment | Contraindicated in Child-Pugh Class C due to risk of neurotoxicity. In Child-Pugh Class B, use with caution; no specific dose adjustment defined. |
| Pediatric use | Children ≥2 years: Same as adult dosing. Infants <2 years: Avoid due to immature blood-brain barrier; alternative therapy recommended. |
| Geriatric use | Use with caution due to increased risk of neurotoxicity; consider alternative therapy. Apply same regimen as adults, but monitor for adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LINDANE (LINDANE).
| Breastfeeding | LINDANE is excreted in human milk; M/P ratio not established. Due to potential neurotoxic effects in the infant, breastfeeding is not recommended during treatment. Discontinue breastfeeding for at least 4 days after last application if treatment is necessary. |
| Teratogenic Risk | LINDANE is contraindicated during pregnancy due to potential neurotoxicity; however, specific teratogenic risk in humans is not well-defined. Animal studies have shown embryotoxicity and fetotoxicity at doses below those causing maternal toxicity. First trimester: theoretical risk; avoid use. Second and third trimesters: avoid unless no alternative and benefit outweighs risk. |
■ FDA Black Box Warning
Lindane is contraindicated in premature infants and patients with uncontrolled seizure disorders. It should not be used in infants, children <10 kg, or elderly patients due to risk of neurotoxicity. Use with caution in patients with history of seizures, head trauma, or HIV infection.
| Serious Effects |
Hypersensitivity to lindane or any component; premature infants; uncontrolled seizure disorders; infants <10 kg; patients with known seizure history; children <2 years; breastfeeding women (avoid application to breast); pregnancy (risk vs benefit; avoid in first trimester if possible).
| Precautions | Neurotoxicity risk (seizures, dizziness), especially in low body weight or compromised blood-brain barrier. Avoid contact with eyes and mucous membranes. Do not apply to open wounds or inflamed skin. Do not use concurrently with oils or oil-based products. Limit to one application unless indicated by live mites. Accidental ingestion may cause toxicity. |
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| Fetal Monitoring | Monitor for neurological symptoms (e.g., seizures, dizziness) in the mother. For fetus, no specific monitoring established; consider fetal surveillance in cases of maternal toxicity. Avoid use in pregnancy unless clearly needed. |
| Fertility Effects | LINDANE has been shown to impair fertility in animal studies. In humans, limited data suggest possible adverse effects on spermatogenesis and ovarian function. Use with caution in patients planning conception. |