P H AR M AC O L O G Y OF ANTI-INFECTIVE AG E N T S

PH C 634 – YEAR 3 ( PART 5)

ANTHELMINTIC
DRUGS
AS S OC . PROF. DATO’ DR. S. VELLAYAN
Faculty of Pharmacy, UiTM Selangor, Puncak Alam

11th April 2023

LE ARN IN G OBJECTIVES:

You should be able to:

1. Identify the drugs of choice for treatment of
common infections caused by nematodes,
trematodes and cestodes.

2. Describe the mechanisms of action,

important pharmacokinetic features and the
major toxic effects of these drugs.

3. Describe the main features of important

back-up antihelmintics. 2
 Oveíview

 3 major groups of helminths:-

a) nematodes
b) trematodes
c) cestodes

 Anthelminthic drugs are aimed at metabolic

targets that are present in the parasite.

3
Nematode

Trematode

4
Incidence of Helminth
Infections in Malaysia
 1950 - High

 1960 - Average

 1970 - Improved

 2023– Lesser

Malaysian researchers in Medical and Veterinary

Parasitology work with helminths

5
Relative Incidents of Helminth
Infections Woíldwide

6
Life Cycle of Trichinella

7
Life Cycle of Strongyloidiasis

8
Life Cycle of Tapeworms

9
Life Cycle of Schistosomes

10
Life Cycle of Enterobius

11
Life Cycle of Trichuris

12
Life Cycle of Hookworm

13
Life Cycle of Ascaris

14
Life Cycle of Filaria

15
16
D R U G S FOR THE TREATMENT
OF NEMATODES
 Nematodes are elongated roundworms that possess a complete
digestive system.
 They cause infections of the intestine as well as the blood and
tissues.

A. MEBENDAZOLE (Vermox)
 A synthetic benzimidazole compound (methly-5-benzoyl-2-
benzimidazole carbamate) is effective against a wide spectrum of
nematodes.
 A drug of choice in the treatment of infections by whipworm
(Trichuris trichiura), pinworm (Enterobius vermicularis),
hookworm (Necator americanus ) and (Ancylostoma duodenale), &
roundworm (Ascariasis lumbricoides).
17
Cont.

 It acts by binding to and interfering with the synthesis of the parasite's

microtubules and also by decreasing glucose uptake.

 Depleting endogenous glycogen stored within the parasite which is

required for survival and reproduction of the helminth.

 Affected parasites are expelled with the feces.

 Does not affect blood glucose concentrations in the host.

 Mebendazole is insoluble in aqueous solution.

18
 Cont.

 2% of Mebendazole administered is excreted in urine and the

remainder in the feces as unchanged drug or primary
metabolite.

 It is also relatively free of toxic effects, although patients may

complain of abdominal pain and diarrhea.

 Contraindicated in pregnant women, because it has been shown

to be embryotoxic and teratogenic in experimental animals.

19
Adverse Effects
 Anorexia, nausea, distention, vomiting, diarrhea, and abdominal
discomfort.
 Occasionally, it may caused skin rashes, itching, drug, and fever.

Uses
 Highly effective against intestinal nematodes: roundworm,
hookworm, whipworm, pinworm and mixed worm infections.

Dose and Administration

 100 mg orally b.d. for 3 days.
 It doesn’t require fasting or purging, well tolerated.
 If deem should be repeated in 2 weeks for another 3 days.
20
 B. ALBENDAZOLE & THIABENDAZOLE

Albendazole
• Drug of choice for treatment cystic hydatid disease
(Echinococcus granulosus) .

• Treatment for neurocysticercosis caused by larva form of

Taenia solium.
• Dosage: 400mg
o Therapy for microsporidial intestinal infection in
patients with AIDS.
o Infection with Capillaria phillipinensis
o Albendazole combined with either D EC or ivermectin in
programs directed toward controlling LF (lymphatic

falariasis). 21
Thiabendazole

• Another synthetic benzimidazole, is effective against

strongyloidiasis caused by threadworm (Strongyloides
stercoralis) cutaneous larva migrans and early stages of
trichinosis (Trichinella spiralis).

• It also affects microtubular aggregation.

• Insoluble in water, the drug is readily absorbed on oral
administration.

• It is hydroxylated in the liver and excreted in the urine.

22
CONT.
Mode of Action Albendazole

• Poorly soluble in aqueous solution.

• Variable and erratically absorbed after oral administration.
• Absorbed enhance in presence of fatty foods & bile salts.
• Enhance absorption by 5-fold in humans.
• 400mg oral dose not detected in plasma :
o Rapidly metabolized in liver & intestine to albendazole sulfoxide.
o Albendzole sulfoxide has potent anthelmintic activity.

Mode of Action Thiabendazole

• Soluble in water
• Same as albendazole
23
 Adveíse Affects

Thiabendazole

• Anorexia, nausea, vomiting and dizziness & C N S symptomatology.

Albendazole

• Epigastric pain, diarrhea, nausea and vomiting.

• Dizziness and headache occur.

24
 C. DIETHYLCARBAMAZINE (DEC)

• First-line agent for control and treatment of lymphatic filariasis

caused by Wuchereria bancrofti & Brugia malayi.

• Therapy for tropical pulmonary eosinophilia (uncommon

manifestation of lymphatic filarial infection).

• Drug of choice for loiasis caused by infection with the filarial

parasite L. loa.

• Cautious
o Can caused life-threatening post-treatment complications.

25
 Annual single dose combination chemotherapy with both DEC
and albendazole show promise for the control of lymphatic
filariasis.

 It is safe to use during pregnancy.

 Available in citrate salts.

26
 Anthelmintic Action

• MoH of D EC against susceptible filarial species is not well understood.

• Exert a direct effect on W. bancrofti microfilariae by causing organelle

damage and apoptosis.

• The mechanism of filaricidal action is unknown.

• Suggest D EC compromises intracellular processing and transport of

certain macromolecules to plasma membrane.

• May affect specific immune and inflammatory response of the host by

undefined mechanism.
27
 Mode of Action

• Absorption – absorbed rapidly from the G I tract.

• Peak plasma occurs 1-2 hours after a single oral dose.

• Plasma t½ varies from 2- 10 hours ( depends on urinary pH).

• Excretion – Both urinary and extra-urinary routes

o >50% of oral dose appears in acidic urine as unchanged drug

28
o Values decreased in alkaline urine (Alkaline urine elevate
plasma levels).
o Prolong plasma t½ and increase both therapeutic effect and
toxicity of DEC.

• Metabolism rapidly and extensive:

o Major metabolite, DEC-N-oxide is active

29
 Uses
 Dosage of D EC citrate used to prevent or treat filarial infections
have evolved empirically and vary according to local experience.

 Filariasis
- Administered orally, 6 mg/kg/day in three divided doses for 3
weeks (Dietylcarbamazine citrate 100 mg three times daily taken
after food for 3 weeks).
- Addition of single dose of albendazole 400 mg to D EC produces
sustained microfilaricidal effect.
- Standard regimen for treatment has been 12-day, 72mg/kg ( 6mg/kg
per day) course of DEC.

30
 Tropical Eosinophilia
- It is treated with DEC , 100 mg t.d.s for 3 weeks.
- Antihistamine and glucocorticoids may be required to control
allergic reaction.

 It is also used for mass chemotherapy to reduce transmission of

filariasis.

31
 Adverse effects are primarily caused by host reactions to the
killed organisms.

 Severity of symptoms  parasite load (fever, malaise, rash,

myalgias and headache).

 Antihistamines or steroids may be given to reduce many of

the symptoms.

32
Adverse effects:

1)Drug-induced effects : anorexia, nausea, vomiting, headache,

tiredness, and dizziness.

2)Parasite-induced reactions: it is due to the release of proteins from

dying parasites.
- In onchocerciasis, it produce severe reaction (Mazzotti) that can be
characterized by fever, skin rashes, severe itching, nausea,
vomiting, headache, cough, chest pain, muscle and joint pain,
lymphadenitis, keratitis, uveitis, leukocytosis, eosinophilia and
proteinuria.

- In W. bancrofti, the reaction is usually mild, and can be minimized

by administering H1-blockers.
33
 D. PYRANTEL PAMOATE

 First introduced into veterinary practice as a broad-spectrum

anthelmintic directed against pinworm, roundworm and
hookworm.

 Its effectiveness and lack of toxicity led its trial against related
intestinal helminths in humans.

 Oxantelpamoate, an m-oxyphenol analog of pyrantel ( single-

dose treatment of trichuriasis)

34
 Pyrantel pamoate with mebendazole is effective in, the treatment
of infections caused by roundworms, pinworms and hookworms.

 It is derivative of tetrahydropyrimidine - thought to act by

depolarising the helminth neuromuscular junction, causing
paralysis and spasm.

 Has some anti cholinesterase activity.

 It is poorly absorbed orally and exerts its effects in the intestinal

tract.

35
 Antihelmintic Action

• Pyrantel and its analogs are depolarizing neuromuscular

blocking agents

• Open nonselective cation channels and induce persistent

activation of nicotinic acetylcholine receptors

• Spastic paralysis of the worm

• Inhibits cholinesterases
36
• Developing contracture of isolated preparations of Ascaris at 1%of
concentration of acetylcholine required.

• Pyrantel exposure leads to depolarization and increased spike-

discharged frequency accompanied by increase in tension.

37
 Mode of Action

 Poorly absorbed from the G I tract ( a property that confines its

action to intralumental G I nematodes).

 Less than 15%excreted in urine as parent drug and metabolites.

 Major proportion of an administered dose is recovered in the

feces.

 The paralyzed worm is then expelled from the host's intestinal

tract.

38
Adverse effects

 Mild, nausea, vomiting, diarrhea, dizziness, fever

 No serious effects on blood, kidney or liver

 It is contraindicated in infants

39
Precautions

 No studies done in pregnant women

 N OT recommended to be used in pregnant woman and

children <2 years of age.

 Pyrantel and Piperazine should N OT be used together

(mutually antagonistic with respect to their neuromuscular
effects on parasites).

40
41
E. IVERMECTIN

 Drug of choice for the treatment of onchocerciasis (river

blindness) caused by Onchocerca volvulus, cutaneous larva
migrans and strongyloides .

 It used both oral and topical in the treatment of scabies and

pediculosis.

 lvermectin targets the parasite's glutamate-gated Cl- channel

receptors.

 Chloride influx is enhanced and hyperpolarization occurs,

resulting in paralysis of the worm.
42
 M E C H A N I S M OF A C T IO N

 Ivermectin potentiates glutamate gated chloride channels and

also increase G A B A transmission in worms

 Cause hyperpolarization and paralysis of the worms

 Lead to death/phagocytosis

43
 Contd.

 It kills microfilariae and has little effect on adult worms. It relieves pruritus and skin
lesions.

 On the death of microfilaria it can caused a Mazzotti-like reaction  fever, headache,

dizziness, somnolence and hypotension.

 Drug of choice for onchocerciasis, lymphatic filariasis and tropical pulmonary

eosinophilia. (Wucheria bancrofti and Brugia malayi).

 Effective against microfilaria but not against adult worms of W. bancrofti, B. malayi, L.
loa, and M. ozzardi.

 Excellent efficacy in humans against Ascaris lumbricoides, Strongyloides stercoralis,

cutaneous larva migrans, Trichuris trichura, Enetrobius vermicularis, Necator
americanus and Ancyclostoma duodenale.
44
 PHARMACOKINEľICS

 Peak levels of ivermectin in plasma are achieved within 4– 5hours

after oral administration.

 93% bound to plasma protein.

 Extensively converted by hepatic CYP3A4 to at least 10metabolites,

mostly hydroxylated and demethylated derivatives.

 Metabolized in the liver, and excreted in the faeces.

 No ivermectin appears in urine in either unchanged or conjugated

form.
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Adverse Effects

 It does not cross the blood-brain barrier and thus, it has no

pharmacologic effects in the C N S .

 Itching, skin rashes, oedema, headache, fever, muscle and

joint pain.

 It is contraindicated in pregnancy and children, and patients

with meningitis, because their blood-brain barrier is more
permeable, and C N S effects might be expected.

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47
CHARACTERISTICS AND THERAPY FOR COMMONLY ENCOUNTERED
NEMATODE INFECTONS

48
49
 D R U G S FOR THE TREATMENT
OF TREMATODES

 Trematodes (flukes) are leaf-shaped flatworms.

 They may be categorized as liver, lung, intestinal, or blood flukes.

PRAZIQUANTEL
 Drug is an agent of choice for the treatment of all forms of
schistosomiasis and other trematode infections and for cestode
infections like cysticercosis (but not for nematodes).

 Permeability of the cell membrane to calcium is increased, causing

contracture and paralysis of the parasite.

50
 Anthelmintic Action

• Praziquantel is a pyrazinoisoquinoline derivative developed after

this class compounds was discovered to have anthelmintic activity
in 1972.

• After rapid and reversible uptake, praziquantel has two major

effects on adult schistosomes. (low concentrations)

• Causes increased muscular activity, followed by contraction and

spastic paralysis.

• Affected worms detach and migrate from the mesenteric veins to

the liver.

• Causes tegumental damage and exposes a number of tegumental

antigens at high concentrations.

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 Mechanism of actions

- Praziquantel increased the influx of Ca2+ into the tegument

- Thus, increased the muscular contraction and spastic paralysis

- Vacuolization and disintegration of the tegument

- Lead to dead of the parasite

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 Praziquantel is rapidly absorbed after oral administration
and distributes into the cerebrospinal fluid.

 High levels occur in the bile.

 The drug is extensively first –pass metabolism in liver,

highly bound to plasma proteins, crosses the BBB and
excreted mainly in urine.

 Extensively metabolized oxidatively  short half-life.

 The metabolites are inactive and excreted through the urine

and bile.
53
 Adverse effect  drowsiness, dizziness, malaise, skin rashes,
itching, muscle pain, joint pain as well as gastrointestinal
upsets(nausea, vomiting, abdominal discomfort).

 Anorexia, fatigue and low-grade fever are seen in heavily

infested patients.

 Contraindicated for pregnant women or nursing mothers.

 For the treatment of ocular cysticercosis, because destruction

of the organism in the eyes may damage the organ.

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 Uses
1) Schistosomiasis
-40 mg/kg, a single oral dose usually produces a high cure rate,
well tolerated

2) Tapeworm infestation
-A single oral dose gives very high cure rate in all tapeworm
infestations
- T. solium, a saline purge is given 2 hours after the administration
of praziquantel to wash off all mature segments before ova can be
released by disintegration to prevent cysticercosis

3) Neurocysticercosis
- It is contraindicated in pregnancy and ocular cysticercosis
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TREMATODE INFECTIONS

56
57
 D R U G S FOR THE TREATMENT
OF CESTODES

 Flat, segmented body and attach to the host's intestine.

 The tapeworms lack a mouth and a digestive tract throughout
their life cycle.

A. NICLOSAMIDE
 The drug of choice for most cestode (tapeworm) infections
(Taemia saginata, T. solium, Hymenolepis nana,
Diphyllobothrium latum).

 Its action is by inhibition of the parasite's mitochondrial

anaerobic phosphorylation of ADP, which produces usable
energy in the form of ATP.
58
 The drug is lethal for the cestode's scolex and segments of
cestodes but not for the ova.

 In case of T. solium, after purge helps to expel all dead

segments and so preclude digestion and liberation of the ova,
which may lead to cysticercosis.

 It is poorly absorbed from the G I tract.

 A laxative is administered prior to oral administration of

niclosamide.

 It is given orally in the form of chewable tablets

 Avoid alcohol. 59
Adverse effects
 Produces few minor side effects: nausea, vomiting, diarrhoea,
headache, skin rashes, itching, and abdominal discomfort.

Treatment schedule of niclosamide:

1 g of niclosamide on empty stomach

1 hour later

Another 1 g of niclosamide

2 hour later

A saline purge is given to wash off all the

worms
60
 B. ALBENDAZOLE (Zentel)
 It is a benzimidazole and has broad spectrum of anthelmintic activity

 It inhibits microtubule synthesis and glucose uptake in nematodes.

 In the treatment of cestodal infestations, such as cysticercosis (caused

by Taenia solium larvae) and hydatid disease (caused by Echinococcus
granulosis).

 Albendazole is erratically absorbed after oral administration, but

absorption is enhanced by a high-fat meal and metabolized in liver.

 It produces an active metabolite (albendazole sulphoxide) that widely

distributed into various tissues including hydatid cyst. Hence, it is
preferred to mebendazole in the treatment of hydatid disease.

 Albendazole and its metabolites are primarily excreted in

61
the urine.
 Adverse effects
 It is very well tolerated

 The sides effect are rare, but can cause nausea, vomiting, diarrhea
and epigastric distress.

 When used in short-course therapy (1 – 3 days) for nematode

infections, adverse effects are mild and transient

 During long-term therapy, it may cause headache, dizziness, fever,

weakness, and loss of hair .

 Treatment of hydatid disease (3 months) has risk of hepatotoxicity

and rarely agranulocytosis or pancytopenia.

 Contraindicated in pregnancy or to children under

62
2 years of age.
 Dose and Administration:
- A single oral dose of 400 mg at any time of day, does not require fasting
or purging and side effects are rare
Uses:
1) Nematodes: highly effective against intestinal nematodes-roundworm,
hookworm, whipworm, pinworm, threadworm, and also in mixed worm
infestations
2) Neurocysticercosis: it is preferred to praziquantel because of shorter of
duration of treatment, reachs high concentration in brain and CSF, less
toxic and better tolerated.

- High doses of glucocorticoids are usually given with albendazole/

praziquantel to minimize the inflammatory reactions to dying
parasites.

- Contraindicated in ocular cysticercosis, blindness can occu r due to

inflammatory reaction 63
3) H ydatid disease
- In Echinococcus hydatid cyst, surgical resection is the treatment
of choice, but albendazole is drug of choice in medical therapy
- It should be started at least 4 days before the surgery and
continued for at least 4 weeks afterward

4) Filariasis
- Albendazole is given with DEC or ivermectin in the treatment of
lymphatic filariasis. It has adjuvant value

- Albendazole is also very effective in cutaneous larva migrans

64
CHARACTERISTICS AND THERAPY FOR COMMON ENCOUNTERED CESTODE
INFECTIONS
ECHINOCOCCOSIS
•This disease (also called hydatid
disease) is caused by Echinococcus
granulosus (dog tapeworm). Infection
produces large, hydatic cysts in the
liver, lung, and brain. Anaphylactic
reaction to worm antigens can occur if
the cyst ruptures.
•The disease follows ingestion of
eggs in dogs faeces. Sheep often
serve as an intermediate host.
•Echinococcosis is diagnosed by CT
scan or biopsy of infected tissue and
is treated by surgical excision of
cysts.
• Therapy: Albenzaloze.
TAENIASIS
•This disease is caused by the adult
from Taenia solium (pork tapeworm).
Intestines are the primary site of
infection, where the organism can
cause diarrhea. Most of these
infections, however, are asymptomatic.
•The disease is transmitted by larvae in
undercooked pork or by ingestion of
tapeworm eggs.
•Teaniasis is diagnosed by detection of
proglottids in stools.
• Therapy: Praziquantel.
CYSTICERCOSIS
•This disease is caused by Taenia
solium larvae. Infection produces
cysticerci in the brain (causing seizures,
headache, and vomiting) and in the
eyes.
•The disease follows ingestion of eggs
from human faeces.
•Cysticercosis is diagnosed by CT scan
or biopsy.
•Therapy: Praziquantel, albendazole,
and/or surgery.
TAENIASIS
•This disease is caused by the larvae
from Taenia saginata (beef tapeworm).
The organism primarily infects the
intestines and does not produce
cysticerci. Most infected individuals are
asymptomatic.
•The disease is transmitted by larvae in
undercooked or raw beef.
•Teaniasis is diagnosed by detection of
proglottids in stools.
• Therapy: Praziquantel.
TDIPHYLLOBOTHRIASIS
• This disease is caused by the adult from Diphyllobothrium latum
(fish tapeworm). The adult worm in a host’s intestine can be as long
as 15 meters.
• The disease is transmitted by larvae in undercooked fish.
65
• Diphyllobothriasis is diagnosed by detection of characteristic eggs
in stools.
• Therapy: Praziquantel or niclosamide.
66
 SUMMARY OF ANTHELMINTHIC AGENTS

CHEMOTHERAPY OF HELMINTHIC INFECTIONS

CHEMOTHERAPY OF NEMATODES

Ivermectin
Mebendazole
Pyrantel pamoate
Thiabendazole

CHEMOTHERAPY OF TRAMATODES

Praziquantel

CHEMOTHERAPY OF CESTODES

Niclosamide

67
68
 ANTHELMINTIC D R U G S
AVAILABLE IN MALAY S IA

1 ) A lbendazole 200 mg Tablet

Zentel – Trade Name
Denzol – Trade Name
Thelban – Trade Name

2)Albendazole Suspension
Zentel - Trade Name (200 mg/5 ml)
Denzol – Trade Name (20mg/ml)
Thelban – Trade Name (100mg/5ml and 200mg/5ml)

69
 ANTHELMINTIC D R U G S
AVAILABLE IN MALAY S IA

3)Mebendazole 500mg chewable tab

Quemox – Trade Name
4)Pyrantel Pamoate 125 mg/250 mg Tablet
Combantrin – Trade Name

Pyrantel Pamoate

70
 Common question ask by
patients to a pharmacist

1) What is helminth infection?

- Soil-transmitted helminth infections are caused by different species of
parasitic worms. They are transmitted by eggs present in human faeces,
which contaminate the soil in areas where sanitation is poor.
2) What are anthelmintic drugs used for?
- These drugs are also used to treat infected animals. Pills containing
anthelmintics are used in mass deworming campaigns of school-aged
children in many developing countries. For example, the treatment of
choice for soil-transmitted helminths is mebendazole and albendazole
and praziquantel for schistosomiasis.

71
 Cont.

3) How do anthelmintic drugs work?

Most medicines used to treat worm infections kill worms by either
starving them or paralysing them; for example:
-Mebendazole, albendazole and tiabendazole work by preventing the
worms from absorbing the sugars they need for survival.
-Praziquantel and ivermectin work by paralysing the worms in the gut
(intestine)
4) Does mebendazole kill tapeworm?
- This kills the worm within a few days. Although mebendazole
kills adult worms, it does not kill the eggs. Because of this it is
important to break the cycle of re-infection.

72
 Cont.

5) How fast does mebendazole work?

- Mebendazole works by preventing the threadworms absorbing
sugar, which means they should die within a few days. This
medication is 90-100% effective at killing the threadworms, but it
doesn't kill the eggs. This is why the hygiene measures outlined
below should also be followed for 6 weeks.
6) How do I get rid of worms naturally?
- Coconut is the most effective home remedy
to treat intestinal worms. Consume a tbsp of crushed coconut in
your breakfast. After 3 hours, drink about one glass of lukewarm
milk mixed with 2 tbsps of castor oil. Drink this for a week to get
rid of all types of intestinal worms.

73
REFERENCES

1. Goodman & Gilman’s The Pharmacological Basis of Therapeutics.

McGraw Hill, 13th edition. Laurence Brunton, Randa Hilal-Dandan,
Bjorn Knollmann

2. Board Review Series. Pharmacy, 3rd Edition. Gary C. Rosenfeld, David

S. Loose-Mitchell and James B. Jones.

3. Lippincott’s Illustrated Review. Pharmacology. Richard D. Howland

and Mary J. Mycek.

4. Basic & Clincal Pharmacology. Bertram G. Katzung

74
ECTOPARASITIC
DRUGS
AS S OC . PROF. DATO’ DR. S. VELLAYAN
Faculty of Pharmacy, UiTM Selangor, Puncak Alam.

11th April 2023

OVERVIEW

• An ectoparasiticide is an antiparasitic drug

used in the treatment of ectoparasitic
infestations.
• These drugs are used to kill the parasites that
live on the body surface.
• Permethrin, sulfur, lindane, dicophane, benzyl
benzoate, ivermectin and crotamiton are well
known ectoparasiticides.
• The drugs available in Malaysia are A-Lices,
and A-Scabs

76
 Pediculosis

• Different species of lice prefer to feed on certain locations on

the body of the host.

• Louse species include:

• Pediculus capitis (head lice), Habitat: (head).
• Pediculus corporis or Pediculus humanus (body lice),
Habitat: (body) and
• Pthirus pubis (pubic louse), habitat: occurs on hair in the
pubic and perianal regions of the body, and occasionally in
the axillae, eyebrows and beard).

77
LO U SE

78
LIFE CYCLE OF LICE

79
(Sarcoptes scabiei) Scabies

80
Pediculus capitis (head lice)

81
Pediculus coípoíis oí
Pediculus humanus (body
lice)

82
Pthiíus pubis (pubic louse)

83
84
ECTOPARASITICIDES

85
 1. LINDANE
(gamma-hexachlorocyclohexane)

• H as been used both as an agricultural insecticide and as

a pharmaceutical treatment for lice and scabies
• Is a neurotoxin that interferes
with G A B A neurotransmitter function by interacting with
the G A B A A receptor-chloride channel complex at
the picrotoxin binding site
• It is effective pediculicide and scabicide
• Percutaneous absorption.
• After absorption, it is concentrated in fatty tissues, including
the brain.
• Available as a shampoo or lotion.
86
 Continued…

• Pediculosis capitis or pubis, one application of 30 ml of

shampoo is worked into a lather and left on the scalp or
genital area for 5 minutes and then rinsed off.

• No additional application is indicated unless living lice

are present one week after 1 week treatment.

• Patients should be retreated only if active mites seen.

• Controversy exists about the possible systemic toxicities

of topically applied Lindane.
87
 Continued…

• Neurotoxicity and hematotoxicity.

• Should be used with cautions in infants, children and

pregnant women.

• Local irritation occur, and contact with the eyes and mucous
membrane should be avoided.

88
 Adverse Reactions

• Skin irritation to seizures

• Burning sensations, itching, dryness and rash

89
 2. IVERMECTIN

• Actinomycete Streptomyces avermitilis.

• Treat infections by parasitic nematodes (roundworms) and

arthropods (insects, ticks, and mites) from livestock and domestic
animals.

• Used to treat head lice, scabies, river blindness, worm infestations

(except for cestodes) and lymphatic filariasis.

• Applied to the skin or orally.

• Discovered in 1975 and came into medical use in 1981.

• Can be used against mites, lice and bed bugs.

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 Antiparasitic Activity and Resistance

• Inducing a tonic paralysis of the musculature.

• Ivermectins induce paralysis by activating a family of ligand-

gated Cl − channels.

• Glutamate-gated Cl − channels that are only in inverterbrates.

91
 Mechanism of Action

• Binds to glutamate-gated chloride channels (Glu-Cls) in

the membranes of invertebrate nerve and muscle cells.

• Causes increased permeability to chloride ions, resulting

in cellular hyper-polarization, followed by paralysis and
death

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 Side Effects

• Neurotoxicity

• Cannot be used in certain species of dogs, tortoises and

turtles

93
 3. C ROTAMITON

• N-ethyl-o-crotonotoluidide, is a scabicide with some

antipruritic properties.

• Mechanism of action is unknown.

• Percutaneous absorption had not been published.

• It is available as a cream or lotion

• For two applications to the entire body from the chin down
at 24hr intervals, with a cleansing bath 48hr after the last
application. 94
 Continued…

• Can be used as an alternative to Lindane.

• Allergic contact hypersensitivity and primary irritation

occur, necessitating discontinuance of therapy.

• Application to acutely inflamed skin or to the eyes or

mucous membranes should be avoided.

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 4. SULFUR

• Has a long history of used as a scabicide.

• It is non-irritating, unpleasant odour, is staining and is

thus disagreeable to use.

• More aesthetic and effective scabicide on recent years.

• Alternative drug for use in infants and pregnant

women.

• 5% precipitated sulfur in petrolatum.

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97
 5. PERMETHRIN

• It is neurotoxic to Pediculus humanus, Pthirus pubis, and

Sarcoptes scabiei.
• Less than 2% of an applied dose is absorbed
percutaneously.
• Residual drugs persist up to ten days following
applications.
• It is recommended Permethrin 1% cream rinse (Nix) be
applied undiluted to affected areas of pediculosis for 10
mins and rinse off with warm water.
• Treatment of scabies, a single application of 5% cream is
applied to the body from the neck.

98
99
 6. MALATHION

• It is an organophosphate cholinesterase inhibitors that

is hydrolyzed by plasma carboxylesterases much faster
in humans than in insects.

• A therapeutic advantage in treating pediculosis.

• It is available as a 0.5% lotion that should be applied to

the hair when dry and the hair then combed to remove
nits and lice after 4-6 hrs.

100
REFERENCES

1.Board Review Series. Pharmacy, 3rd Edition. Gary C. Rosenfeld,

David S. Loose-Mitchell and James B. Jones.

2.Lippincott’s Illustrated Review. Pharmacology. Richard D.

Howland and Mary J. Mycek.

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Thank You For
Your Attention

102