By Satarkulova A.M. Human is the primary host for most helminthic infections. Most worms produce eggs and larva. These pass out of human body and infect secondary host. Immature forms invade humans via skin or GIT. 1. Worms live in hosts alimentary canal. 2. Worms or larvae live in other tissues of host body like: muscles , viscera , menninges , lungs, subcutaneous tissues. 3 Ascaris lumbricoids ( common round worm) Filariasis Hookworm Tapeworm Whipworm Cysticercosis Elephantiasis The goal of anthelmintic therapy is to eradicate the parasite completely. Anthelmintics should be used only when clearly indicated (laboratory documentation of parasitic infestation). Monitoring of safety and efficacy is required. Ascariasis Fillariasis Ancylostomiasis Trichocephaliasis Enterobiasis Trichinosis Strongyliasis Toxocariasis Trichuriasis Pyrantel Mebendazole Thiabendazole Albendazole Flubendazole Ivermectine Diethylcarbamazine Opisthorchiasis Clonorchiasis Praziquantel Triclabendazole Paragonomiasis Bithionol Fascioliasis Oxamniquine Schistosomiasis Taeniasis Taeniarhynchiasis Praziquantel Diphillobotriasis Niclosamide Hymenolepiasis Echinococcosis Albendazole May act by causing : paralysis of the worm. damaging the worm leading to partial digestion or rejection by immune mechanisms. interfere with the metabolism of the worm. Broad spectrum. MOA: Inhibits microtubule synthesis that irreversibly impairs glucose uptake , intestinal parasites are immobilized and die slowly. Given orally , absorption ↑ with a fatty meal. Metabolized in the liver to the active metabolite albendazole sulfoxide. Plasma half life 8-12 hours. Albendazole sulfoxide is mostly protein bound distributes well to tissues and enters bile, CSF . Metabolites are excreted in urine. Used on empty stomach when used against intraluminal parasites, but with a fatty meal when used against tissue parasites. In ascariasis , trichuriasis , hookworm, pin worm infections. Hydatid diseases . Neurocysticercosis. Other infections: drug of choice in cutaneous and visceral larva migrans , intestinal capillariasis . In short term(1-3 days): No adverse effects. In long term use : abdominal pain, headache, fever, fatigue, alopecia, increased liver enzymes, pancytopenia. Contraindication: pregnancy, hypersensitive peoples, children under 2 y. (may cause convulsion) Synthetic benzimidazole. Wide spectrum and safer than albendazole. MOA, Clinical uses, Adverse effects, Contraindication as albendazole. Converted to inactive metabolites . Half- life 2-6 hrs. MOA as other benzimidazole. Half- life of 1-2 hrs. Metabolized in liver and 90% is excreted in urine. Can also absorbed through skin. Clinical uses: Strongyloidal infections. In cutaneous larva migrans . Adverse effects: Pruritus ,headache, drowsiness , irreversible liver failure. Contraindication: children , pregnancy, hepatic and renal diseases. Broad spectrum. Poorly absorbed orally. Excreted unchanged in the feces. MOA: Neuromuscular blocking drug leads to paralizes of worms. Clinical uses: Pin worm. Ascariasis . Hookworm. Adverse effects: mild GI disturbance, drowsiness , headache ,insomnia, rash , fever. Contraindications Pregnancy. Children under 2 y. of age. Only for the treatment of ascariasis cure rate 90% for 2 days treatment. Readily absorbed orally. Excreted mostly unchanged in urine. MOA: Causes paralysis of ascaris by blocking acetylcholine at myoneural junction , the live worms expelled by normal peristalsis. Adverse effects: GI disturbance, neurotoxicity , allergic reactions . Contraindications: Epilepsy Impaired liver or kidney functions Pregnancy Second-line drug for treatment of tape worm infections. Given in the morning on empty stomach. Poorly absorbed from gut & excreted in urine. MOA: adult worm is rapidly killed by inhibition of oxidative phosphorylation . Clinical uses: Treatment of most forms of tapeworms. Purgative is necessary to purge all dead segments& prevent liberation of ova. Adverse effects: Mild GI disturbance. Contraindication: Children under 2 y. Pregnancy. MOA: Immobilizes microfilariae and alters their surface structure ,displacing them from tissues & making them susceptible to destruction by host defense mechanism. Given orally after meals, rapidly absorbed from GIT. Half- life is 2-3 hrs. It is excreted in urine as unchanged or metabolite. Adverse effects: Fever , rash, headache, GIT problems, cough, pain, retinal hemorrhage, encephalopathy, lymphadenopathy. Contraindication: Hypertension, renal disease, patient with lymphangitis. MOA: Paralyze nematodes by intensifying GABAmediated transmission of signals in peripheral nerves. Given only orally, rapidly absorbed. Does not cross BBB. Half- life is 16 hrs. Excretion in urine & feces. Clinical uses: Cutaneous larva migrans. Strongyloidiasis. Onchocerciasis. Filariasis ( it is microfilaricidal ). Adverse effects: Fatigue , dizziness, GI disturbance. Killing of microfilaria result in a Mazotti reaction: fever, headache, hypotension , tachycardia, peripheral edema. Corneal opacities & other eye lesions. Contraindication: Concomitant use with other drugs that enhance GABA (Barbiturates, bnzodiazepines, valproic acid). Pregnancy. Meningitis. Children under 5 y. MOA: Bithionol interferes with the neuromuscular physiology of helminths, impairs egg formation and inhibit oxidative phosphorylation . Given orally & Excreted in urine Clinical uses: Drug of choice for the treatment of fascioliasis ( sheep liver fluke). Adverse effects: GI disturbance, dizziness, headache, skin rashes , urticaria, leucopenia. Contraindications and precautions: Hepatitis , leucopenia. Used with caution in children under 8 y. Worms (helminths) Drug of choice Tapeworms (cestodes) Niclosamide or Praziquantel or Albendazole Roundworms (nematodes) •Enterobius vermicularis (pinworm) •Ascaris lumbricoides •Trichuris trichiura (whipworm) •Trichinella spiralis (trichinellosis) •Strongyloides stercoralis •Necator americanus (hookworm) •Ancylostoma duodenale •Onchocerca volvulus (Onchocercosis) •Wuchereria bancrofti (Elephantiasis) Mebendazole or Pyrantel Mebendazole or Pyrantel Mebendazole or Albendazole Mebendazole and Thiabendazole Thiabendazole Mebendazole or Pyrantel Mebendazole, Pyrantel, or Albendazole Ivermectin Diethylcarbamazine Flukes (trematodes) •Schistzoma (Schistozomes) Praziquantel