Anti-Helminthics
DRUG Mechanism of Action Pharmacokinetics Clinical Uses Adverse Effects
Oral; taken w/ water during or after
1) inhibits microtubule synthesis in
meals; poorly absorbed in GIT; taken 1) Ascariasis, Trichuiasis, Hookworm, back pain, nausea,vomiting,
nematodes, impairing glucose
Albendazole in empty stomach (intraluminal Pinworm; 2) Hydatid disease - DOC; 3) dizziness, headache, lassitude,
uptake; 2) immobilizes parasites and
parasites); taken w/ fatty meal (tissue Neurocysticercosis insomnia
dies slowly
parasites)
Other: cutaneous larva migrans, visceral may increase serum
absorption enhanced by fatty meal;
larva migrans, intestinal capillariasis, aminotransferase - monitor liver for
70% plasma protein-bound; excreted
microsporidial infections, long-term therapy; saftey for
in urine; half-life: 8-12 hrs
gnathostomiasis, clonorchiasis pregnancy and <2yrs not established
skin rashes from dying worms; used
Bithionol peak blood levels in 4-8 hours 1) Paragonimiasis 2) Fascioliasis
in caution for children <8 yrs
Pulmonary Paragonimiasis- 90%;
given orally after meals Cerebral Paragonimiasis -repeated
doses
1) W. bancrofti, B malayi, B. timori, Loa
1) immobilizes microfilariae causing
synthetic piperazine derivative; loa - DOC; also for prophylaxis; 2) result from release of proteins from
displacement in tissues; 2) alters
Diethylcarbamazine readily absorbed in GIT, skin, Onchocerca volvulus - Suramin added dying microfilariae or adult worms;
their surface structure making it more
Citrate conjunctiva; drug rapidly equilibrates (kill adult worms); 3) Tropical reactions severe w/ onchocerciasis
susceptible to host defenses; 3) moa
except fat; half-life: 2-3 hours eosinophilia; 4) Mass therapy w/ W. (replaced w/ Ivermectin)
for adult worm unknown
bancrofti - many a/e
1) Mazotti Reaction (fever &
1) intensify GABA-mediated semisynthetic macrocylic lactone hypotension) - onchocerciasis; joint
1) Onchocerciasis- single oral dose w/
transmission of signals in peripheral derived from soil actinomycete; does & muscle pains, hypotension,
water on empt stomach; 2)
Ivermectin nerves (paralyze nematodes & not cross BBB; well-absorbed orally, tachycardia, lymphadenitis,
Strongyloidiasis; 3) Scabies, lice,
arthropods); 2) microfilaricidal - metabolized in liver, excreted in lymphangitis, peripheral edema; 2)
cutaneous larva migrans
onchocerciasis feces; half-life: 16 hours avoided w/ drugs that enhance
GABA activity; 3) CI in pregnancy
poorly absorbed in GIT (<10%) stay
Hypersensitivity reactions;
1) inhibits microtubule synthesis in in the lumen and will act on the
Ascariasis, Trichuriasis, Hookworms, agranulocytosis, alopecia, elevation
nematodes, impairing glucose parasite; rapid 1st pass in liver
Mebendazole Pinworms, Intestinal capillariasis, of liver enzymes; teratogenic in
uptake; 2) immobilizes parasites and (converted to inactive); half-life: 2-6
Trichinosis, Taeniasis, Strongyloides animals (CI in pregnancy); used in
dies slowly hrs; excreted in urine & bile;
caution for children <2yrs
absorption increased w/ fatty meal
wide spectrum of anti-helminthic
should be chewed
actvity; active drug
mild & transient cholinergic
organophosphate compound; rapidly
cholineserase inhibition (paralyzes symptoms (30 mins -12hrs); not be
absorbed orally; half-life: 1.5 hrs; 1) Schistosoma haematobium - drug not
Metrifonate adult worms; shift from bladder used after recent exposure to
clearace: nonenzymatic effective in eggs; live eggs continue to
(Trichlorfon) venous plexus to small arterioles of insecticides or drugs w/
transformation to dichlorvos (active pass in urine; 2) prophylactic agent
lungs where they are killed cholinesterase inhibition; CI in
metabolite)
pregnancy
inhibits oxidative phosphorylation or
minimally absorbed from GIT; given 1) beef, pork, fish tapeworm; 2) H.
stimulation of ATPase activity - consumption of alcohol avoided on
Niclosamide on an empty stomach w/ water and diminuta, D. caninum; 3) Intestial fluke
scoleces and segments rapidly killed; the day of tx
must be chewed infections
no effect on ova
CNS (dizziness, headache,
S. mansoni - effective for all stages
MOA unknown; active against mature semisynthetic tetrahydroquinolone; drowsiness); pruritus, uritcaria, low-
including advanced
Oxamniquine and immature stages of S. mansoni; readily absorbed orally; should be grade fever, orange to red urine;
hepatosplenomegaly; less effective in
not cercaricidal though taken w/ food; half-life: 2.5 hours proteinuria, microscopic hematuria,
children
transient decrease in leukocytes
paralysis of ascaris by blocking Ach
CI in pregnancy, px w/ renal or
at the myoneural junction; unable to not recomended for other helminth
Piperazine readily absorbed; oral hepatic function, hx of epilepsy or
maintain position in host, expelled by infections; ascariasis
chronic neurologic dse
normal peristalsis
1) all forms of Schistosomiasis; 2) mild and transient elevations of liver
increase permeability of cestode and synthetic isoquinolone-pyrazine Clonorchis, Opistorchis, Paragonimiasis; enzymes; low-grade fever, pruritus,
trematode cell membranes to derivative; rapidly absorbed; CSF 3) Taeniasis, Diphyllobothriasis - only kill skin rashes, worsened eosinophilia
Praziquantel
calcium, resulting in paralysis, concentrations; half-life: 0.8-1.5 larvae; 4) Neruocysticercosis; 5) H. (dying worms); Ci- ocular
dislodgment and death hours; excretion via kidneys and bile nana - DOC; 6) Hydatid disase - kills cysticercosis, lactating & pregnant
protoscoleces moms; children <4
a neuromuscular blocking agent
causes release of Ach and inhibition
tetrahydropyrimidine derivative;
of cholinesterase - spastic paralysis 1) Pinworm 2) ascariasis 3) Hookworm
Pyrantel Pamoate poorly absorbed; active mainly CI in liver dysfunction
and expulsion; active against all foms & Trichostrongylus orientalis
against luminal organisms
of helminths w/in intestinal tract
except migratory stages
much more toxic than other
benzimiazole compound; chelating
given after meals, should be chewed; 1) benzimidazole; irreversible liver
inhibit microtubule synthesis; has agent; rapidly absorbed; half-life: 1.2
Thiabendazole Strongyloides; 2) cutaneous larva failure and fatal Steven-Johnson's
ovicidal effects hrs; can also be absorbed from the
migrans - cream Syndrome; limited in children <15kg;
skin
CI in pregnancy, hepatic or renal dse
DRUG Mechanism of Action Pharmacokinetics Clinical Uses Adverse Effects
Oral; taken w/ water during or after
1) inhibits microtubule synthesis in
meals; poorly absorbed in GIT; taken 1) Ascariasis, Trichuiasis, Hookworm, back pain, nausea,vomiting,
nematodes, impairing glucose
Albendazole in empty stomach (intraluminal Pinworm; 2) Hydatid disease - DOC; 3) dizziness, headache, lassitude,
uptake; 2) immobilizes parasites and
parasites); taken w/ fatty meal (tissue Neurocysticercosis insomnia
dies slowly
parasites)
Other: cutaneous larva migrans, visceral may increase serum
absorption enhanced by fatty meal;
larva migrans, intestinal capillariasis, aminotransferase - monitor liver for
70% plasma protein-bound; excreted
microsporidial infections, long-term therapy; saftey for
in urine; half-life: 8-12 hrs
gnathostomiasis, clonorchiasis pregnancy and <2yrs not established
skin rashes from dying worms; used
Bithionol peak blood levels in 4-8 hours 1) Paragonimiasis 2) Fascioliasis
in caution for children <8 yrs
Pulmonary Paragonimiasis- 90%;
given orally after meals Cerebral Paragonimiasis -repeated
doses
1) W. bancrofti, B malayi, B. timori, Loa
1) immobilizes microfilariae causing
synthetic piperazine derivative; loa - DOC; also for prophylaxis; 2) result from release of proteins from
displacement in tissues; 2) alters
Diethylcarbamazine readily absorbed in GIT, skin, Onchocerca volvulus - Suramin added dying microfilariae or adult worms;
their surface structure making it more
Citrate conjunctiva; drug rapidly equilibrates (kill adult worms); 3) Tropical reactions severe w/ onchocerciasis
susceptible to host defenses; 3) moa
except fat; half-life: 2-3 hours eosinophilia; 4) Mass therapy w/ W. (replaced w/ Ivermectin)
for adult worm unknown
bancrofti - many a/e
1) Mazotti Reaction (fever &
1) intensify GABA-mediated semisynthetic macrocylic lactone hypotension) - onchocerciasis; joint
1) Onchocerciasis- single oral dose w/
transmission of signals in peripheral derived from soil actinomycete; does & muscle pains, hypotension,
water on empt stomach; 2)
Ivermectin nerves (paralyze nematodes & not cross BBB; well-absorbed orally, tachycardia, lymphadenitis,
Strongyloidiasis; 3) Scabies, lice,
arthropods); 2) microfilaricidal - metabolized in liver, excreted in lymphangitis, peripheral edema; 2)
cutaneous larva migrans
onchocerciasis feces; half-life: 16 hours avoided w/ drugs that enhance
GABA activity; 3) CI in pregnancy
poorly absorbed in GIT (<10%) stay
Hypersensitivity reactions;
1) inhibits microtubule synthesis in in the lumen and will act on the
Ascariasis, Trichuriasis, Hookworms, agranulocytosis, alopecia, elevation
nematodes, impairing glucose parasite; rapid 1st pass in liver
Mebendazole Pinworms, Intestinal capillariasis, of liver enzymes; teratogenic in
uptake; 2) immobilizes parasites and (converted to inactive); half-life: 2-6
Trichinosis, Taeniasis, Strongyloides animals (CI in pregnancy); used in
dies slowly hrs; excreted in urine & bile;
caution for children <2yrs
absorption increased w/ fatty meal
wide spectrum of anti-helminthic
should be chewed
actvity; active drug
mild & transient cholinergic
organophosphate compound; rapidly
cholineserase inhibition (paralyzes symptoms (30 mins -12hrs); not be
absorbed orally; half-life: 1.5 hrs; 1) Schistosoma haematobium - drug not
Metrifonate adult worms; shift from bladder used after recent exposure to
clearace: nonenzymatic effective in eggs; live eggs continue to
(Trichlorfon) venous plexus to small arterioles of insecticides or drugs w/
transformation to dichlorvos (active pass in urine; 2) prophylactic agent
lungs where they are killed cholinesterase inhibition; CI in
metabolite)
pregnancy
inhibits oxidative phosphorylation or
minimally absorbed from GIT; given 1) beef, pork, fish tapeworm; 2) H.
stimulation of ATPase activity - consumption of alcohol avoided on
Niclosamide on an empty stomach w/ water and diminuta, D. caninum; 3) Intestial fluke
scoleces and segments rapidly killed; the day of tx
must be chewed infections
no effect on ova
CNS (dizziness, headache,
S. mansoni - effective for all stages
MOA unknown; active against mature semisynthetic tetrahydroquinolone; drowsiness); pruritus, uritcaria, low-
including advanced
Oxamniquine and immature stages of S. mansoni; readily absorbed orally; should be grade fever, orange to red urine;
hepatosplenomegaly; less effective in
not cercaricidal though taken w/ food; half-life: 2.5 hours proteinuria, microscopic hematuria,
children
transient decrease in leukocytes
paralysis of ascaris by blocking Ach
CI in pregnancy, px w/ renal or
at the myoneural junction; unable to not recomended for other helminth
Piperazine readily absorbed; oral hepatic function, hx of epilepsy or
maintain position in host, expelled by infections; ascariasis
chronic neurologic dse
normal peristalsis
1) all forms of Schistosomiasis; 2) mild and transient elevations of liver
increase permeability of cestode and synthetic isoquinolone-pyrazine Clonorchis, Opistorchis, Paragonimiasis; enzymes; low-grade fever, pruritus,
trematode cell membranes to derivative; rapidly absorbed; CSF 3) Taeniasis, Diphyllobothriasis - only kill skin rashes, worsened eosinophilia
Praziquantel
calcium, resulting in paralysis, concentrations; half-life: 0.8-1.5 larvae; 4) Neruocysticercosis; 5) H. (dying worms); Ci- ocular
dislodgment and death hours; excretion via kidneys and bile nana - DOC; 6) Hydatid disase - kills cysticercosis, lactating & pregnant
protoscoleces moms; children <4
a neuromuscular blocking agent
causes release of Ach and inhibition
tetrahydropyrimidine derivative;
of cholinesterase - spastic paralysis 1) Pinworm 2) ascariasis 3) Hookworm
Pyrantel Pamoate poorly absorbed; active mainly CI in liver dysfunction
and expulsion; active against all foms & Trichostrongylus orientalis
against luminal organisms
of helminths w/in intestinal tract
except migratory stages
much more toxic than other
benzimiazole compound; chelating
given after meals, should be chewed; 1) benzimidazole; irreversible liver
inhibit microtubule synthesis; has agent; rapidly absorbed; half-life: 1.2
Thiabendazole Strongyloides; 2) cutaneous larva failure and fatal Steven-Johnson's
ovicidal effects hrs; can also be absorbed from the
migrans - cream Syndrome; limited in children <15kg;
skin
CI in pregnancy, hepatic or renal dse
