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1.Intestinal nematodes Worm infestation Ascariasis Enterobiasis Ancylostomiasis Necator americanus Ancylostoma. duodenale Trichinosis spiralis) Drug of choice Albendazole, mebendazole Mebendazole, pyrantel Albendazole, pyrantel Alternative drugs pyrantel, Piperazine, levamisol Albendazole, piperazine
mebendazole, levamisol, thiabendazole
(Trichinella Mebendazole, albendazole- thiabendazole add corticosteroids for severe infection Mebendazole, albendazole Ivermectin Diethylcarbamazine Oxantel, pyrantel Thiabendazole, albendazole Ivermectin
Trichuriasis (whipworm) Strongyloidiasis Somatic nematodes W. bancrofti and Brugia malayi (Filariasis); tropical eosinophilia; Loa loa O. volvulus Guinea worm Cutaneous larva migrans Visceral larva migrans Intestinal capillariasis
Ivermectin Metronidazole Albendazole, ivermectin Albendazole Albendazole
Diethylcarbamazine Thiabendazole, mebendazole Thiabendazole (topical) Mebendazole, diethylcarbamazine Mebendazole, thiabendazole
2. Cestodes (tape worms)
Taenia saginata (beef tapeworm) Taenia solium (pork tapeworm)
Praziquantel, niclosamide Praziquantel, niclosamide
Mebendazole Praziquantel Niclosamide Mebendazole Metrifonate Oxamniquine -
Cysticercosis cellulosae(pork tapeworm Albendazole larval stage) Diphyllobothrium latum (fish tapeworm) Hymenolepis nana (dwarf tapeworm) Echinococcus tapeworm) granulosus Praziquantel, niclosamide Praziquantel
(hydatid Albendazole Praziquantel Praziquantel Praziquantel Bithionol, triclabendazole Praziquantel, niclosamide Praziquantel Praziquantel, triclabendazole
3.Trematodes: Schistosoma hematobium (bilharziasis) Flukes S. mansoni S. japonicum Fasciola hepatica (sheep liver fluke) Fasciola buski (large intestinal fluke) Clonorchis sinensis (liver fluke) Paragonimus westermani (lung fluke)
Mechanism of action of anthelmintics
1. Against nematodes i. Depolarsing block • Pyrantel and levamisole NN receptors agonists and also increase ACh level by inhibiting ChE. They produce depolarizing NM blockade. Detached worms are expelled in feces. ii. Inhibitory action. 1
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Piperazine: is a GABA agonist, activates GABA gated Cl channel- cause hyperpolarization, 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 surface characteristics so that they are phagocytosed by tissue fixed monocytes. Broad spectrum anthemintics Benzimidazole group: Albendazol, mebendazole- broad spectrum anthelmintic (many nematodes and 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 glucose uptake. The end result is depletion of parasite’s glycogen stores, reduced formation of ATP, disruption of metabolic pathways and ultimately parasitic death. Against trematodes Metrifonate: an organophosphate compound which gets converted to dichlorovos 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 first esterifies oxamniquine to produce a reactive metabolite that alkylates parasite DNA. Bithionol: uncouples parasitic specific fumarate reductase mediated oxidative phosphorylation Against cestodes and against cestodes and trematodes Against cestodes: Niclosamide: uncouples oxidative phosphorylation in adult cestodes. It inhibits anaerobic incorporation of energy rich inorganic phosphates into ATP which is harmful to the parasite. Against trematodes and cestodes. Praziquantel: causes influx of calcium from endogenous stores of the cestodes resulting in intense contraction and subsequent expulsion of the worm from the GIT. In schistosomes praziquantel induced influx of calcium damages the tegument, causing holes which exposes hidden parasite antigens, the antibodies in the host bind to these antigen and destroy them by phagocytosis.
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Individual drugs. Albendazole
Mechanism of action: • Has larvicidal effects in hydatid disease, cysticercosis. • Has ovicidal effects in ascariasis, ancylostomiasis and trichuriasis. Uses 2
DOC for ascaris lumbricoides (AL), trichuris trichuria (TT), ancylostoma duodenale (AD) and Necator americanis (NA). • Preferred for cutaneous larva migrans, visceral larva migrans, intestinal capillariasis.. • DOC for neurocysticercosis: given with corticosteroid to decrease the inflammatory reaction due to dying worm. It is superior to praziquantel because of short duration , low cost and improved penetration in subarachnoid space and 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) and clonorchis 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 used against 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
Mechanism of action: similar to albendazole. • Like albendazole, it is also wide spectrum anthelmintic- effective against GI nematodes (AL, EV, TT, AD, NA), intestinal capillariasis and hydatid disease. • It is given orally, poorly absorbed, abs. increases with fatty meal. Has first pass metabolism. Tablet chewed before swallowing. Uses: • DOC for AL, TT, NA, AD, EV . • Alternative for trichinosis. • Intestinal capillariasis. • Visceral larva migrans. Side effects: • Short term: Diarrhea, abdominal pain, nausea, vomiting • Long term: increase in transaminases and urticaria, rash. Contraindications: • Pregnancy • Children below 2 years. • Liver cirrhosis
• Narrow spectrum benzimidazole- used primarily in veterinary practice. • DOC for fasciola hepatica infection not responding to praziquantel. • Effective for lung fluke. Adverse reactions: • Not significant side effects 3
Rarely used now a days. • Mechanism of action: similar to albendazole. Chew the tablet, rapidly absorbed, metabolised and excreted. Uses • Broad spectrum, has largely been replaced by safer drugs such as albendazole and ivermectin. • Alternative agent to treat SS (oral), cutaneous larva migrans (creeping eruptions)- topical or oral. Trichinosis (oral). Side effects • Dizziness, headache, drowsiness, neuropsychiatric symptoms- hallucinations.. • Gastrointestinal symptoms- nausea, anorexia, vomiting. • Erythema multiforme, Steven-Johnson syndrome. • Liver failure. Cautions • Activity requiring alertness (driving, working with machines) should be avoided during therapy. • Patients with decreased hepatic and renal function. • Pregnancy
• • Depolarization results in a paralysis and loss of muscle activity, and hence expulsion of the worm by peristaltic movements. Safe drug, poorly abs after oral adm., high conc. remain in gut (effective for luminal helminthes), excreted in feces.
Uses: • As alternative drug for ascariasis, enterobiasis, and hookworm or mixed infections . • Not effective against trichuriasis. A combined formulation of oxantel and pyrantel has broader spectrum. Side effects: • GI symptoms, dizziness, headache, drowsiness. • Should not be combined with piperazine, they have antagonistic action. Contraindications: • During pregnancy • In children less than 2 years.
• • Analogue of pyrantel pamoate. Effective for trichuris infection. Since trichuris commonly occurs as multiple infections (with ascaris and ancylostoma) oxantel is given in combination with pyrantel.
Well absorbed • DOC for fascioliasis (liver fluke) and paragonimus westermanii (lung fluke). Adverse reactions: • Anorexia, nausea, vomiting, diarrhea.
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Dizziness, headache, Skin rashes (as reaction to antigen released from dying helminth). Avoid in children less than 8 years.
Tetramisole is racemic, and levamisole is its levo and more active isomer. Both isomers are effective against many nematodes but use is restricted to ascariasis and ancylostomiasis. It is a weak-base- rapidly absorbed, metabolized and excreted. Excretion is pH dependent. One metabolite is active. Crosses BBB. Uses • As an alternative drug for ascariasis, and ancylostomiasis. • Also used as an immunomodulatory agent; it restores depressed T cell function. –For this purpose, used in rheumatoid arthritis, as an adjunct in malignancies (along with 5 fluorouracil in colorectal carcinoma), aphthous ulcers, recurrent herpes infections, leishmaniasis, vitiligo. Adverse reactions • Nausea, abdominal pain, giddiness, fatigue, drowsiness, confusion or insomnia. • Prolonged use and high doses may produce skin rashes, febrile illness (flu like – fever, arthralgia), rarely agranulocytosis and thrombocytopenia.
It is readily absorbed after oral adm, excretion complete in 24 H. Uses • Ascariasis. • Enterobiasis. Side effects • GI distress: nausea, vomiting, abdominal pain • Urticaria: allergic reaction- rare • Neurological symptoms: headache, ataxia, hypotonia, visual disturbancesrare. • Epilepsy. Contraindications • Pregnancy because nitrosamine metabolite has carcinogenic and teratogenic potential. • Epilepsy • Impaired liver and renal functions. • Concomitant use of pyrantel- antagonistic effect.
It is a piperazine derivative. DOC for filariasis and tropical eosinophilia. It has been replaced by ivermectin for the treatment of onchocerciasis. It immobilizes microfilariae, alters their surface structures, displacing them from tissues and making them more susceptible to host defense mechanism. Taken after food, rapidly absorbed, widely distributed in tissues and fat. Excreted in urine as unchanged and as metabolite. Adjust dose in renal failure and in patients with renal alkalosis. Excretion delayed in alkaline urine Uses
DOC for treatment of lymphatic filariasis due to W. bancrofti, B. malayi and loa-loa. Active against microfilarial and adult worms. For Onchocerca volulus: ivermectin is preferred. Use antihistamines and corticosteroid in the beginning to limit allergic reaction to dying filariae. • For chemoprophylaxis of W. bancrofti- monthly treatment to reduce transmission. • DOC for tropical eosinophilia Side effects • Dose dependent : headache, weakness, malaise, anorexia, nausea, vomiting, dizziness and lethargy. • Allergic reaction: fever, rash, headache, cutaneous swelling, lymphadenopathy, leukocytosis, eosinophilia, proteinuria, edema and rarely retinal hemorrhage and encephalopathy. • In onchocerciasis- microfilariae dying in the eye- may produce optic neuritis and visual field loss.
Abs. from GIT, widely distributed, excreted mainly in feces. Uses • Drug of choice for onchocerciasis (river blindness) reduces microfilarial load without the toxicity seen with diethylcarbamazine. Repeat dose every 6- 12 M until the adult worms die- may take 10-12 years. Corticosteroides may be used to avoid inflammatory eye reactions. Annual mass treatment leads to major reduction in disease transmission. Effective for other filarial worms. • For disseminated stronglyloidiasis. • For cutaneous larva migrans. • Round worms • Single dose for scabies- not preferred- cure rate is slow. • Single dose for lice. Adverse effects: • Fatigue, dizziness, nausea, vomiting, abdominal pain, rashes. • Mazotti reaction due to killing of microfilariae in onchocerciasis- the reaction includes fever, headache, dizziness, somnolence, weakness, rash, increased pruritus, diarrhea, joint and muscle pains, hypotension, bronchospasm, tachycardia, lymphadenitis, lymphangitis, peripheral edema. In severe cases corticosteroids may be administered. • Corneal opacities. • Avoid concurrent administration of drugs which enhance GABA activity e.g. barbiturates, benzodiazepines, valproic acid. • Avoid use during pregnancy and children under 5 years.
• Not absorbed, high conc in lumen. Affects scolex and proximal segments of most cestodes- resulting in their detachment from intestinal wall and expulsion by peristaltic activity. Not ovicidal • Administered orally after fasting overnight. Uses: • For treatment tapeworms: T. saginata, D. latum,, T. solium and H. nana.- now superseded by praziquantel. For T solium, the drug is followed by saline purgative to remove damaged worm. • Alternative for intestinal fluke. 6
Side effects: • Abdominal discomfort, nausea, loose motion. • With alcohol- disulfiram like reaction
It is a broad-spectrum schistosomicidal agent. Well absorbed after oral adm, has significant 1st pass metabolism, crosses BBB, excretion is mainly by kidneys. Effective against male and female adults and immature stages Uses: • Trematodes. schistosomiasis(all forms); clonorchiasis and paragonimiasis • Cestodes: taeniasis, diphyllobothriasis, infection with H. nana and hydatid disease – for cestodes the dose schedule is simpler and efficacy is higher than niclosamide. • For neurocystocercosis- equivalent to albendazole- kills the larvae in brain and other tissues. Corticosteroids decrease plasma conc of praziquantel, concurrent use- controversial. It may be used as an adjunct to albendazole as it enhances plasma conc. of albendazole sulfoxide. Side effects: • GI intolerance- nausea, vomiting, abdominal pain. • Headache, drowsiness, dizziness. • Allergic response to release of proteins from dying worms: urticaria, arthralgia, myalgia, low grade fever, eosinophilia. • Increase in hepatic enzymes. Contraindications/ cautions: • Children below 4 years. • Pregnancy- may cause abortion. • Avoid driving as it causes dizziness and drowsiness. • Ocular cysticercosis- severe eye damage due to occlusion by dead parasites.
It is an organophosphate compound. In the body it is converted to active form, dichlorvos (DDVP) that inhibits AChE, paralyses the worm resulting in shift from bladder venous plexus to small arterioles of the lungs, where they are trapped, acted upon by immune system and killed. Not effective against eggs. Live eggs may pass in urine for months after all adult worms have been killed. Uses Treatment of S. hematobium. Adverse reactions: • Mild vertigo, nausea, vomiting, diarrhea, sweating, bronchospasm, abdominal colic. Contraindications: • Pregnancy. • Recent exposure to insecticides • Don’t give depolarizing neuromuscular blockers for 48 hours after treatment
It is readily absorbed after oral administration. Metabolised and excreted in urine. It is preferentially concentrated in male worm. Stimulates parasites' motility and induces shift of the flukes from the mesenteric veins to the liver where the males die and the surviving unpaired female returns to mesentery but lays no eggs.
Uses: • Effective against S. mansoni, used orally. • With metrifonate may be used for mixed infections. Side effects: • CNS: Neuropsychiatric disturbances- drowsiness, dizziness, dullness, headache, seizures. • Gastrointestinal symptoms: nausea, colic • Minor elevations of transaminases. • Pruritus, urticaria • Rare: low grade fever, orange to red discoloration or urine, proteinuria, hematuria, leukocytosis, seizure Contraindications/cautions • Epilepsy, person should avoid activities which require mental alertness • Pregnancy
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