ANTHELMENTIC AGENTS

 Anthelmintics are drugs that have the ability to

get rid of the parasitic worms or helmenths from
the human or other animal bodies.

 Prevention of human helminthic infection all

over the world represents the major WORLD
HEALTH ORGANIZATION (WHO) problem.
 The anthelmintic agents are drugs which could
get rid of the following kinds of worms:

 Nematodes (Pin worm, Filarial worm, Hook

worm, Round worm).
 Cestodes (Fish tapeworm, Beef tapeworm,
Pork tapeworm).
 Trematodes (Schistosoma Heamtobium,
Schistosoma mansonis, & Scistosoma japonicum).
 DRUGS ACTING ON NEMATODES:

a) Benzimidazoles

b) Imidazothiazole.

c) Piperazines.

d) Vinyl-pyrimidines (Pyrentel)
 Anti-NEMATODES:
A) BENZIMIDAZOLES
Benzimidazoles are broad- spectrum group of drugs with high activity
against GIT helminthes.

Their mode of action

• Inhibit the formation of microtubules through binding to beta-
tubulin monomers and preventing polymerization.
 Most of the benzimidazoles are weakly soluble in the intestinal
fluids to exert a useful local action in the GIT infections.
Examples of benzimidazoles;
i) Thiabendazole (Mintezole)
 • Levamizole (KETRAX)

The active form is the Levo isomer named:

(-),2,3,5,6-Tetrahydro-6-phenyimidazo-(2,1-
b)thiazole

this drug is the drug of choice to treat Ascariasis,

and ancylostomiasis.
 c) PIPERAZINES,

They are the drug of choice to get rid of pinworms and

roundworms and various nematodes.
The mode of action;
•piperazine blocks the response of ascaris muscle to
acetylcholine blocking of the neuromuscular
transmission in the worms causing a flaccid paralysis of
it ,which dislodges it from GIT and expelled in the face.
 ii) Diethyl Carbamazine Citrate (DEC)
(Hetrazan)

DEC is active against FILARIASIS and MICROFALA-

RIASIS.
 The mode of action of DEC is suggested to
have one of the following:
1) Complexation with the filarial antigyn which
inhibit blood platelets.
2) Binding to the helminthes proteins; tubuline
and preventing its polymerization to
microtubuline.
3) Interfere with arachidonic acid metabolism.
Hence this drug has antiinflammatory activity
by inhibiting COX-II enzyme.
 d) PYRANTEL PAMOATE:

 IT is a deplolarzing neuromuscular blocking agent

that causes spastic paralysis .
 It is used in the treatment of infestation caused by
pinworms and Ascariasis.
 Because its action opposes that of piperazine, the
two helmentics should not be used together.
 DRUGS ACTING ON
CESTODES

A. Benzimidazoles (as mentioned before)

B. Miscellaneous (the most important is
Niclosamide (Yomesan)
 Drugs acting on TREMATODES
(Antischistosomal or Antibilharsial agents)

A) Oxamniquine (VANSIL)
 1,2,3, 4 -Tetrahydro-2-(isopropyl- amino)methyl

-7 – nitro -6-quinolinemethanol (Vansil)

 It inhibit nucleic acid synthesis of Schistosomes

 The 6- hydroxymethyl group is critical for activity

 The metabolic activation of its precursor 6- methyl group is vital

 Metabolized in to 6 carboxylic derivative and is inactive

 Has good oral bioavailability

 d) PRAZEQUANTEL (Biltracide , PZQ)

The Levo-isomer of PZQ is the active enantiomers.

 Mode of PZQ
• Increases cell membrane permeability,
resulting in loss of extracellular calcium.
• Muscle contraction and ultimate paralysis and
hence their ease eradication.

• PZQ is the drug of choice for treating

Schisosomiasis and liver Flukes (Trematodes
and Cestode infections).
 Lice
 Two Species: (body, head, and crab lice(pubic hair)
 Pediculus humanus capitis (head louse)
 Pediculus humanus corporis (body louse).
 Female lice deposit eggs on the hair.
 The eggs (or nits) remain firmly attached to the hair, and in about
10 days, the lice hatch to form nymphs, which mature in 2 weeks.
 larva and adults feed on the blood of the host
 Piercing mouth parts and a pumping device
 Severe pruritus from papular lesions produced by the bite of the
louse.
 Macular swellings and secondary bacterial infections
 Hypersensitivity to foreign material injected by the lice can
produce.
 Treatment: Lice
 Permethrin (Nix®) 1% or Permethrin 1% (Nix-Creme
Rinse®)
 Pediculicidal and ovicidal activity against P. humanus var.
capitis. (85% to 95%).
 Side effects: Itching, burning, stinging, and tingling.
 The scalp should be saturated with permethrin liquid, and a
towel should be wrapped around the scalp to allow the
application to stay on for 10 minutes; followed by rinse
 may be necessary to repeat the application.
 0.5% malathion (Ovide) to be left on the scalp for about
90 minutes.
 Treatment: Lice
 Calamine liniment or lotion with 0.1% menthol
 Other members of the family or sexual partners
also should be treated.
 All bedding and clothes should be sterilized by
boiling or washing in the hot water cycle of the
washing machine to avoid reinfections.
• An ocular lubricant (e.g., Lacri-Lube S.O.P.)
applied twice daily may be used to remove crab
louse infection of the eyelids.
 Scabies
• Causative Organism: Sarcoptes scabiei
• Clinical Presentation
 Severe itching and an inability to sleep
 Diagnosis: looking for burrows formed
• Treatment: Permethrin 5% (Elimite) cream
 Scrub skin in a warm soapy bath using a soft brush
to remove all scabs.
 Apply lotion to the whole body, avoiding the face,
mucous membranes, and eyes.
 Bathing after 8 to 14 hours
 Scabies
 A single application: 97%
 Crotamiton 10% (Eurax®)
 Oral Ivermectin (Stromectol®) 200 mcg/kg as a
single dose; may be repeated in 2 weeks.
 Topical corticosteroids and antihistamines (to
treat pruritus).
 Children and infants:
 Permethrin (1% and 5%) for pediculosis and
scabies (90%)
THANK YOU!