ANTIHELMINTIC DRUGS
Roundworms
A. LUMBRICOIDES E.
VERMICULARIS ROUNDWORM PINWORM
N. AMERICANUS T. TRICHURAHOOKWORM WHIPWORM
S. STERCORALIS THREADWORM
Tissue Nematodes
ONCHOCERCA Wuchereria bancrofti
ANCYCLOSTOMA
DRUGS THAT ACT AGAINST NEMATODES
A. ALBENDAZOL EMECH OF ACTION – blocks glucose uptake in
both larval and adult parasite , which leads to decrease formation of atp
- inhibition of microtubule assemblyCLINICAL USE : broad anthelintic spectrumfirst 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 filariasisalternative 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
C. IVERMECTINMECHANISM 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
TREMATODES
SCHISTOSOMA (BLOOD FLUKE ) LUNG FLUKE
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
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 )
D. OXAMNIQUINE – effective solely in schistosoma mansoni infections
TOXICITY : dizziness ,git irritation , pruritusREACTION TO DYING PARASITES –
eosinophilia ,urticaria and pulmonary infiltrates
DRUG THAT ACT AGAIST CESTODES (TAPEWORM)
NICLOSAMIDEMECHANISM 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
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