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Ectoparasiticides
Dr. D. K. Brahma
Associate Professor
Department of Pharmacology
NEIGRIHMS, Shillong
Introduction
ā€¢Drugs used to kill parasites that live on body
surface
ā€¢ Lice ā€“ Pediculosis sp. ā€“ wingless insects
ā€¢Mites ā€“ Sarcoptes/Acarus scabiei ā€“
Arachnids ā€“ minute arthropods infesting
human hair and skin
Scabies
ā€¢ Highly contagious mite
ā€¢Burrows through the epidermis, laying eggs ā€“
form papules ā€“ immenseitching
ā€¢ Secondary infection ā€“ antibiotics
ā€¢ Finger webs
ā€¢ Forearm, trunks, genitals and lower legs
ā€¢ Family members
ā€¢ Cross infection andre-infection
Source: Google Images
Pediculosis
ā€¢The lice thrive on head - P. capitis
ā€¢ Body ā€“ P. corporis
ā€¢ Pubic region ā€“ P. pubis
ā€¢Cause itching, suck blood and produce typhus and
relapsing fever
ā€¢The eggs are called nits ā€“ attached to hair and
clothes by chitin like content
Source: Google Images
Available drugs
ā€¢Permethrin
ā€¢ Lindane
ā€¢ Benzyl benzoate
ā€¢ Crotamiton
ā€¢ Sulfur
ā€¢ Dicophane (DDT)
ā€¢ Ivermectin
Sulfur ointment
ā€¢ Oldest scabicide ā€“ weak pediculocide, antiseptic, fungicide an
keratolytic
ā€¢ MOA: Slowly reduced to H2S and SO2on skin and pentathionic acid
ā€¢ pentathionic acid ā€“ dissolve the cuticle of mice and kill it
ā€¢ Reactions are carried out by epidermal cells and arthropod
themselves
ā€¢ Used as 10% ointment ā€“ After a warm scrubbing bath (to open up
burrows) ā€“ messaged over the entire body (below neck) ā€“ 3
consecutive nights ā€“ soap water bath on 4th day
ā€¢ Disadvantages:
ā€¢Messy treatment
ā€¢Socially unacceptable ā€“ interfere with person`s vocation
ā€¢Repeated applicationneeded
Permethrin
ā€¢ Broad spectrum
ā€¢ Most efficacious and most convenient for both scabies and lice
ā€¢ MOA: Neurological paralysis of insects ā€“ delayed
depolarization
ā€¢ Toxicity lower in human than lindane
ā€¢ Persists over skin for days but systemic absorption low
ā€¢ 100% cure rate and resistance rare
ā€¢ Effective in lindane non-responsivecases
ā€¢ ADRs: Transient burning, itching, tingling, erythema and rash
ā€¢ Preparations: For scabies ā€“ 5% cream, 1$ soap and 5% lotion
For head lice: 1% lotion and 5% cream
ā€¢ First choice drug now for scabies and lice
Source: Google Images
Lindane
ā€¢Gamma benzene hexachloride
ā€¢ broad spectrum ā€“ lice and mites
ā€¢MOA: Penetrates to insects through their chitinous cover and
affects nervous system
ā€¢ Head lice ā€“ 67% to 92%cure rate and scabies ā€“ 84 t0 92%
ā€¢ Lower efficacy than permethrin andresistance
ā€¢ Combines with Benzyl benzoate ā€“100%
ā€¢ Preparations: 1% lotion and cream
ā€¢Pediculosis: apply over scalp, 12 ā€“ 24 hours, shower cap ā€“ repeat
after one week if needed, avoideyes
ā€¢For Scabies: Rubbed over body below neck and scrub bath after
12 -24 hours ā€“ repeat after one week if needed
ā€¢Disadvantages: Lipid soluble, gets absorbed, systemic toxicity ā€“
CN stimulation, vertigo, convulsion (Children) and cardiac
arrhythmia
Lindane
ā€¢Widely distributed in the body ā€“ fats
ā€¢Metabolized and eliminated and half-life 24
hours
ā€¢ Microsomal enzyme inducer
ā€¢ Less favoured for treatment of scabies
ā€¢ Whole body application ā€“ systemic toxicity
ā€¢Avoid in infants, young children and
pregnancy
Source: Google Images
Benzyl benzoate
ā€¢ Oily liquid with faint aromatic smell
ā€¢ The emulsion is applied all over the body and 2nd
coat on next day ā€“ except face and neck
ā€¢ Wash off after 24 hours
ā€¢ Convenient and does not interfere normal works
ā€¢70 ā€“ 100% cure rate in scabies ā€“ no systemic
toxicity
ā€¢ Contraindicated in children - Neurological symptoms
ā€¢ Preparatin ā€“ 25% lotion
Other drugs
Crotamiton
ā€¢ Scabicidal, pediculocide and antipruritic
ā€¢ Low cure rate
ā€¢ Lesser systemictoxicity
ā€¢ Preferred in children
ā€¢10% cream andlotion
Dicophane (DDT)
ā€¢ Popular insecticide fpor mosquitoes, flies and pests
ā€¢ Scabies and pediculosis 1 ā€“ 2% lotion or cresam
ā€¢ Washed off after 24 hours
ā€¢Absorbed through skin and ā€“ enzyme induction, rashes, tremor
etc.
ā€¢ Acts as neurotoxin forarthropods
Ivermectin
ā€¢ Source: Streptomyces avermitilis
ā€¢Anthelmintic drug ā€“ also useful in scabies
and pediculosis
ā€¢ SARS Cov 2 ???
ā€¢Only orally effective drug ā€“ 12 mg single
dose ā€“ 100% cure rate
ā€¢ AIDS with scabies and head lice also
ā€¢ Replaced DEC ā€“ in River blindness
ā€¢ DOC in Strongyloidosis
ā€¢ Bancroftian and brugian filaria
Source: Google Images
Ivermectin ā€“ contd.
MOA:
ā€¢Nematodes develop tonic paralysis
ā€¢ Acts through special type of Cl- channel present
only in invertebrates
ā€¢No such channel in flukes and tapeworm ā€“
ineffective
ā€¢ Potentiation of GABAergic receptors
ā€¢ p-glycoprotein related efflux from brain in human ā€“
no action
Any question ?
Thank you

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Ectoparasiticides

  • 1. Ectoparasiticides Dr. D. K. Brahma Associate Professor Department of Pharmacology NEIGRIHMS, Shillong
  • 2. Introduction ā€¢Drugs used to kill parasites that live on body surface ā€¢ Lice ā€“ Pediculosis sp. ā€“ wingless insects ā€¢Mites ā€“ Sarcoptes/Acarus scabiei ā€“ Arachnids ā€“ minute arthropods infesting human hair and skin
  • 3. Scabies ā€¢ Highly contagious mite ā€¢Burrows through the epidermis, laying eggs ā€“ form papules ā€“ immenseitching ā€¢ Secondary infection ā€“ antibiotics ā€¢ Finger webs ā€¢ Forearm, trunks, genitals and lower legs ā€¢ Family members ā€¢ Cross infection andre-infection
  • 5. Pediculosis ā€¢The lice thrive on head - P. capitis ā€¢ Body ā€“ P. corporis ā€¢ Pubic region ā€“ P. pubis ā€¢Cause itching, suck blood and produce typhus and relapsing fever ā€¢The eggs are called nits ā€“ attached to hair and clothes by chitin like content
  • 7. Available drugs ā€¢Permethrin ā€¢ Lindane ā€¢ Benzyl benzoate ā€¢ Crotamiton ā€¢ Sulfur ā€¢ Dicophane (DDT) ā€¢ Ivermectin
  • 8. Sulfur ointment ā€¢ Oldest scabicide ā€“ weak pediculocide, antiseptic, fungicide an keratolytic ā€¢ MOA: Slowly reduced to H2S and SO2on skin and pentathionic acid ā€¢ pentathionic acid ā€“ dissolve the cuticle of mice and kill it ā€¢ Reactions are carried out by epidermal cells and arthropod themselves ā€¢ Used as 10% ointment ā€“ After a warm scrubbing bath (to open up burrows) ā€“ messaged over the entire body (below neck) ā€“ 3 consecutive nights ā€“ soap water bath on 4th day ā€¢ Disadvantages: ā€¢Messy treatment ā€¢Socially unacceptable ā€“ interfere with person`s vocation ā€¢Repeated applicationneeded
  • 9. Permethrin ā€¢ Broad spectrum ā€¢ Most efficacious and most convenient for both scabies and lice ā€¢ MOA: Neurological paralysis of insects ā€“ delayed depolarization ā€¢ Toxicity lower in human than lindane ā€¢ Persists over skin for days but systemic absorption low ā€¢ 100% cure rate and resistance rare ā€¢ Effective in lindane non-responsivecases ā€¢ ADRs: Transient burning, itching, tingling, erythema and rash ā€¢ Preparations: For scabies ā€“ 5% cream, 1$ soap and 5% lotion For head lice: 1% lotion and 5% cream ā€¢ First choice drug now for scabies and lice
  • 11. Lindane ā€¢Gamma benzene hexachloride ā€¢ broad spectrum ā€“ lice and mites ā€¢MOA: Penetrates to insects through their chitinous cover and affects nervous system ā€¢ Head lice ā€“ 67% to 92%cure rate and scabies ā€“ 84 t0 92% ā€¢ Lower efficacy than permethrin andresistance ā€¢ Combines with Benzyl benzoate ā€“100% ā€¢ Preparations: 1% lotion and cream ā€¢Pediculosis: apply over scalp, 12 ā€“ 24 hours, shower cap ā€“ repeat after one week if needed, avoideyes ā€¢For Scabies: Rubbed over body below neck and scrub bath after 12 -24 hours ā€“ repeat after one week if needed ā€¢Disadvantages: Lipid soluble, gets absorbed, systemic toxicity ā€“ CN stimulation, vertigo, convulsion (Children) and cardiac arrhythmia
  • 12. Lindane ā€¢Widely distributed in the body ā€“ fats ā€¢Metabolized and eliminated and half-life 24 hours ā€¢ Microsomal enzyme inducer ā€¢ Less favoured for treatment of scabies ā€¢ Whole body application ā€“ systemic toxicity ā€¢Avoid in infants, young children and pregnancy Source: Google Images
  • 13. Benzyl benzoate ā€¢ Oily liquid with faint aromatic smell ā€¢ The emulsion is applied all over the body and 2nd coat on next day ā€“ except face and neck ā€¢ Wash off after 24 hours ā€¢ Convenient and does not interfere normal works ā€¢70 ā€“ 100% cure rate in scabies ā€“ no systemic toxicity ā€¢ Contraindicated in children - Neurological symptoms ā€¢ Preparatin ā€“ 25% lotion
  • 14. Other drugs Crotamiton ā€¢ Scabicidal, pediculocide and antipruritic ā€¢ Low cure rate ā€¢ Lesser systemictoxicity ā€¢ Preferred in children ā€¢10% cream andlotion Dicophane (DDT) ā€¢ Popular insecticide fpor mosquitoes, flies and pests ā€¢ Scabies and pediculosis 1 ā€“ 2% lotion or cresam ā€¢ Washed off after 24 hours ā€¢Absorbed through skin and ā€“ enzyme induction, rashes, tremor etc. ā€¢ Acts as neurotoxin forarthropods
  • 15. Ivermectin ā€¢ Source: Streptomyces avermitilis ā€¢Anthelmintic drug ā€“ also useful in scabies and pediculosis ā€¢ SARS Cov 2 ??? ā€¢Only orally effective drug ā€“ 12 mg single dose ā€“ 100% cure rate ā€¢ AIDS with scabies and head lice also ā€¢ Replaced DEC ā€“ in River blindness ā€¢ DOC in Strongyloidosis ā€¢ Bancroftian and brugian filaria Source: Google Images
  • 16. Ivermectin ā€“ contd. MOA: ā€¢Nematodes develop tonic paralysis ā€¢ Acts through special type of Cl- channel present only in invertebrates ā€¢No such channel in flukes and tapeworm ā€“ ineffective ā€¢ Potentiation of GABAergic receptors ā€¢ p-glycoprotein related efflux from brain in human ā€“ no action