ANTIHELMINTIC DRUGS Roundworms
A. LUMBRICOIDES VERMICULARIS ROUNDWORM
N. AMERICANUS HOOKWORM
E. PINWORM
T. TRICHURA WHIPWORM
S. STERCORALIS THREADWORM
DRUGS THAT ACT AGAINST NEMATODES A. ALBENDAZOLE MECH OF ACTION – blocks glucose uptake in both larval and adult parasite , which leads to decrease formation of atp - inhibition of microtubule assembly CLINICAL USE : broad anthelintic spectrum first drug of choice for larve migrans( ancylostoma spc) alternative drug for roundworms , whipworm, hookworms,pinworms and threadworm TOXICITY : reversible leukopenia , alopecia and changes in the liver anzymes LONG TERM USE : bone marrow suppresion and fetal toxicity B. DITHYLCARBAMAZINE MECHANISM OF ACTION : immobilizes microfilariae CLINICAL USE: drug of choice for filariasis alternative for onchocerciasis ( in combination with suramin) TOXICITY : headache, malaise, weakness, anorexia can cause the mazzotti reaction in onchocerciasis – hypotension, pyrexia respiratory distress and prostration fever, rashes and ocular damage
Tissue Nematodes
ONCHOCERCA bancrofti
ANCYCLOSTOMA
Wuchereria
C. IVERMECTIN MECHANISM OF ACTION : intesifies gaba mediated neurotransmission in nematodes resulting to paralysis CLINICAL USE : drug of choice for onchocerciasis : drug of first choice for strongloidiasis and alternative drug for filariasis TOXICITY : fever, headache ,dizziness ,rashes, pruritus, tachycardia ,hypotension , joint pains , muscle [ain and pain ion lymph nodes D. MEBENDAZOLE MECHANISM OF ACTION – selctively inhibit microtubule syntheisi and glucose uptake in nematodes CLINICAL USE : drug of first choice for pinworms , whipworms and round worms second drug of choice for cestodes nad trematode infection
TOXICITY : only limited to gastrointestinal irritation . embyrotoxic E. PIPERAZINE MECH. OF ACTION – acting as agonist at gaba recptors CLINICAL USE ; drug of choice for ascariasis TOXICITY : git irritation F. PYRANTEL PAMOATE MECH OF ACTION – pyrantel pamoate and its congener axantel pamoate, stimulate nicotinic receptor present at tne neuromuscular junctions of nematodes. contraction of muscle occurs ,followed by a depolarizarion induced paralysis CLINICAL USE : ( along with mebendazole) drug of choice for hookworm, pinworm and roundworm infestation . TOXICITY - git distress ,headache and weakness
CLINICAL USE : drug of choice for schistosomiasis, clornorchiasis and paragonimiasis it is also one of the drug of choice for cestodes TOXICITY – headache , dizziness, malaise and git irritation , skin rashes and fever CONTRAINDICATION : ocular cysticercosis B. BITHIONOL = drug of choice for the treatment of fascioliasis ( sheep liver fluke) TOXICITY : nausea , vomiting, diarrhea, abdominal cramps, dizziness, dizziness, headache , phototoxicity , pyrxia, tinnitus, proteinuria and leukopenia C. METRIFONATE – is an organophosphate prodrug that is converted in the body to cholinesterase inhibitor dichlorvos , this active metabolite acts solely against schistosoma haematobium ( the cause of bilharziasis )
TREMATODES D. OXAMNIQUINE – effective solely in schistosoma mansoni infections TOXICITY : dizziness ,git irritation , pruritus REACTION TO DYING PARASITES – eosinophilia ,urticaria and pulmonary infiltrates SCHISTOSOMA (BLOOD FLUKE )
LUNG FLUKE
DRUG THAT ACT AGAIST CESTODES (TAPEWORM)
CLONORCHIS SINENSIS(LIVER FLUKE)
DRUGS THAT ACT AGAINST TREMATODES A. PRAZIQUANTEL MECH. OF ACTION – increases membrane permeability to calcium, causing marked contraction initially and then paralysis of trematode muscles ; this is followed by vacuolization and parasite death
NICLOSAMIDE MECHANISM OF ACTION ; act by uncoupling oxidative phosphorylation or by activating atpase CLINICAL USE : effective in beef, pork and fish tapeworm but not in cysticercosis ( albendazole or prqaziquatel is more effective) TOXICITY ; git distress ,headache, rash and fever