AnthelminticsSory اهاعم يذه اتلكام رخاب  وص عط وم شب رس ةوتكد اعط

Mebendazole, thiabendazoleAlbendazoleIntestinal capillariasisMebendazole,diethylcarbamazineAlbendazoleVisceral larva migransThiabendazole (topical)Albendazole, ivermectinCutaneous larva migransThiabendazole, mebendazoleMetronidazole

Guinea worm

DiethylcarbamazineIvermectin

O. volvulus

IvermectinDiethylcarbamazine

W. bancrofti and Brugiamalayi (Filariasis);tropical eosinophilia; Loaloa

SomaticnematodesThiabendazole, albendazoleIvermectin

Strongyloidiasis

Oxantel, pyrantelMebendazole, albendazole

Trichuriasis (whipworm)

thiabendazoleMebendazole, albendazole-add corticosteroids for severeinfection

Trichinosis (Trichinellaspiralis)

levamisol, thiabendazoleAlbendazole, mebendazole, pyrantel

AncylostomiasisNecator americanusAncylostoma. duodenale

Albendazole, piperazineMebendazole, pyrantel

Enterobiasis

Piperazine, levamisolAlbendazole, pyrantel,mebendazole

AscariasisAlternative drugsDrug of choiceWorm infestation1.Intestinal nematodes

BithionolPraziquantel, triclabendazole

Paragonimuswestermani(lung fluke)

AlbendazolePraziquantel

Clonorchissinensis(liver fluke)

Praziquantel, niclosamide

Fasciolabuski(large intestinal fluke)

-Bithionol, triclabendazole

Fasciolahepatica (sheep liver fluke)

Praziquantel

S. japonicum

OxamniquinePraziquantel

S. mansoni

MetrifonatePraziquantel

Schistosomahematobium (bilharziasis)3.Trematodes:Flukes

MebendazoleAlbendazole

Echinococcus granulosus (hydatidtapeworm)

NiclosamidePraziquantelHymenolepis nana (dwarf tapeworm)-Praziquantel, niclosamideDiphyllobothrium latum (fish tapeworm)PraziquantelAlbendazoleCysticercosis cellulosae(pork tapewormlarval stage)-Praziquantel, niclosamide

Taeniasolium(pork tapeworm)

MebendazolePraziquantel, niclosamide

Taeniasaginata(beef tapeworm)2. Cestodes(tape worms)

Mechanism of action of anthelmintics

1.Against nematodesi.Depolarsing block

•

Pyrantel and levamisoleNN receptors agonists

and also i

ncrease ACh levelby

inhibiting ChE. They produce

depolarizing NM blockade

. Detached wormsare expelled in feces.

ii.Inhibitory action.

•

Piperazine:

is a

GABA agonist

, activates GABA gated Cl channel-

causehyperpolarization, flaccid paralysis, paralysed worms are expelled alive.

•

Ivermectin: activates glutamate-gated Cl channels which are inhibitory, cause hyperpolarization.

•

Diethylcarbamazine

: though a piperazine (causing hyperpolarization),mechanism of action is different:

it alters microfilarial membrane surfacecharacteristics so that they are phagocytosed by tissue fixed monocytes.2.Broad spectrum antheminticsBenzimidazole group:

•

Albendazol, mebendazole- broad spectrum anthelmintic (many nematodesand cestodes).

•

Thiabendazole and triclabendazole- restricted use.Benzimidazoles bind to β tubulins & prevent their assembly, i.e.depolymerisation resulting in breakdown of microtubules (cytoplasmic,tegumental and intestinal) with selective and irreversible inhibition of glucoseuptake. The end result is depletion of parasite’s glycogen stores, reducedformation of ATP, disruption of metabolic pathways and ultimately parasiticdeath.3.Against trematodes

•

Metrifonate

an organophosphate compound which gets converted todichlorovos which acts as an antiChE, produces depolarizing block of S.hematobium

.•

Oxamniquine

acts by intercalation in the parasitic DNA

leading to death of Schistosome by blocking its nucleic acid and protein synthesis. The fluke firstesterifies oxamniquine to produce a reactive metabolite that alkylates parasiteDNA.•

Bithionol

uncouples parasitic specific fumarate reductase mediated oxidativephosphorylation4.Against cestodes and against cestodes and trematodesAgainst cestodes:

•

Niclosamide

uncouples oxidative phosphorylation

in adult cestodes. It inhibitsanaerobic incorporation of energy rich inorganic phosphates into ATP which isharmful to the parasite.

5.Against trematodes and cestodes

.•

Praziquantel:

causes influx of calcium from endogenous stores of the cestodesresulting in intense contraction and subsequent expulsion of the worm fromthe GIT. In schistosomes praziquantel induced influx of calcium damages thetegument, causing holes which exposes hidden parasite antigens, theantibodies in the host bind to these antigen and destroy them byphagocytosis

Individual drugs.Albendazole

Mechanism of action:

•

Has larvicidal effects

in hydatid disease, cysticercosis.•

Has ovicidal effects

in ascariasis, ancylostomiasis and trichuriasis.

Uses

•

DOC for ascaris lumbricoides (AL), trichuris trichuria (TT), ancylostomaduodenale (AD) and Necator americanis (NA).

•

Preferred for cutaneous larva migrans, visceral larva migrans, intestinalcapillariasis.

.•

DOC for neurocysticercosis

: given with corticosteroid to decrease theinflammatory reaction due to dying worm. It is

superior to praziquantel becauseof short duration , low cost and improved penetration in subarachnoid spaceand increased blood levels of drug when administered with corticosteroid.

•For

hydatid disease

better results obtained when given with praziquantel.Treatment given for months 1-6 M•Alternative for strongyloides stercoralis (SS), enterobius vermicularis (EV) andclonorchis sinensis.•Albendazole + diethylcarbamazine or ivermectin is a synergistic combination for treating or controlling lymphatic filariasis.It is adm in empty stomach for intestinal worms and with fatty meal when usedagainst tissue parasites

Adverse effects

.Well tolerated with 3-5 days treatment, even with 1 month treatment for cysticercosis/hydatid disease not much adverse reactions. More than 3 months treatment may produce:•

Mild and transient epigastric distress, nausea, diarrhea, abdominal distress

• Headache, dizziness, lassitude, insomnia, fever, fatigue, alopecia, increased liver enzymes and pancytopenia.•

Monitor LFT and CBC during prolonged therapy.

•

It is teratogenic- avoid long term use in pregnancy

Mebendazole

Mechanism of action: similar to albendazole.•Like albendazole, it is also

wide spectrum anthelmintic

- effective against GInematodes (AL, EV, TT, AD, NA), intestinal capillariasis and hydatid disease.•It is given orally, poorly absorbed, abs. increases with fatty meal. Has first passmetabolism. Tablet chewed before swallowing.

Uses: