U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Praziquantel, marketed as Biltricide, is an anthelmintic used in humans and animals for the treatment of tapeworms and flukes. Specifically, it is effective against schistosoma, Clonorchis sinensis the fish tape worm Diphyllobothrium latum. Praziquantel works by causing severe spasms and paralysis of the worms' muscles. This paralysis is accompanied - and probably caused - by a rapid Ca 2+ influx inside the schistosome. Morphological alterations are another early effect of praziquantel. These morphological alterations are accompanied by an increased exposure of schistosome antigens at the parasite surface. The worms are then either completely destroyed in the intestine or passed in the stool. An interesting quirk of praziquantel is that it is relatively ineffective against juvenile schistosomes. While initially effective, effectiveness against schistosomes decreases until it reaches a minimum at 3-4 weeks. Effectiveness then increases again until it is once again fully effective at 6-7 weeks. Glutathione S-transferase (GST), an essential detoxification enzyme in parasitic helminths, is a major vaccine target and a drug target against schistosomiasis. Schistosome calcium ion channels are currently the only known target of praziquantel. The antibiotic rifampicin decreases plasma concentrations of praziquantel. Carbamazepine and phenytoin are reported to reduce the bioavailability of praziquantel. Chloroquine reduces the bioavailability of praziquantel. The drug cimetidine heightens praziquantel bioavailability.
Status:
US Approved OTC
Source:
21 CFR 357.110 anthelmintic pyrantel pamoate
Source URL:
First approved in 1971
Source:
Antiminth by Roerig (Pfizer)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pyrantel is an anthelmintic, which acts as an agonist of nicotinic receptors (AChRs) of nematodes and exerts its therapeutic effects by depolarizing their muscle membranes. It is used to treat a number of parasitic worm infections. This includes ascariasis, hookworm infections, enterobiasis (pinworm infection), trichostrongyliasis and trichinellosis. Common adverse reactions include diarrhea, nausea, vomiting, dizziness, headache and somnolence.
Status:
Investigational
Source:
USAN:Abamectin Component B1b
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Abamectin B1b (Avermectin B1b) is a macrocyclic lactone containing an isopropyl reside in the 25-position broad anthelmintic activity. The oral administration of this formulation of avermectin B1 appeared to be highly efficacious against intestinal strongyles and Onchocera microfilaria. Avermectin B1b is a component of marketed and provided commercially Abamectin, which is used to control livestock parasitic nematodes. It is a broad-spectrum acaricide with additional insecticidal action on a limited number of insects. Abamectin acts on insects by increasing the membrane permeability to chloride ions, and it mainly stimulates the release of Ȗ-aminobutyric acid (GABA). The affected arthropod becomes paralysed, stops feeding, and dies after a few days. It exerts contact and stomach action, with limited plant systemic activity, but exhibits translaminar movement into treated leaves. Abamectin is also used as an anthelmintic drug in veterinary medicine.
Status:
US Previously Marketed
First approved in 1950

Class (Stereo):
CHEMICAL (ACHIRAL)


Diethylcarbamazine is used in humans, dogs and cats for the treatment of parasitic infections, including pulmonary eosinophilia, loiasis, and lymphatic filariasis. The exact mechanism of its action is unknown, however some studies showed the involvment of inducible nitric-oxide synthase and the cyclooxygenase pathway. Although there is no information on whether the drug is marketed in the USA and Europe, it is currently used in India.
Imidacloprid is a systemic, chloro-nicotinyl insecticide used for the control of sucking insects such as fleas, aphids, whiteflies, termites, turf insects, soil insects, and some beetles. It is used on co on and vegetable crops as foliar and seed treatments, soil, structures, indoor and outdoor insect control, home gardening and pet products. It is indicated for the prevention of heartworm disease caused by Dirofilaria immitis. It kills adult fleas and is indicated for the treatment of flea infestations (Ctenocephalides felis). It is also indicated for the treatment and control of the following intestinal parasites Hookworm species, Roundworm species, Whipworms. Adverse events in animals included: malaise, vomiting, diarrhea, shaking, mydriasis, hypersalivation with abnormal neurologic signs, seizures, death, generalized hematoma of the body, and alopecia at the treatment site. Adverse reactions in humans included: burning, tingling, numbness, bad taste in the mouth, dizziness, and headache.
Status:
Possibly Marketed Outside US
Source:
STROMECTOL by Merck
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ivermectin B1B (dihydroavermectin B1b) is the minor component (<10%) of the commercial anthelmintic, ivermectin. Members of the avermectin/milbemycin anthelmintic class exert their anthelmintic effects by binding to glutamate-gated chloride channels expressed on nematode neurons and pharyngeal muscle cells. The avermectin/milbemycins are also potent insecticides. In vitro, the B1b (25-isopropyl) analog is slightly more potent than the 25-sec-butyl (B1a) analog as an inhibitor of nematode larval development and paralysis, and also a more sensitive probe for ivermectin resistance.
Ivermectin is a broad-spectrum anti-parasite medication. It was first marketed under the name Stromectol® and used against worms (except tapeworms), but, in 2012, it was approved for the topical treatment of head lice infestations in patients 6 months of age and older, and marketed under the name Sklice™ as well. Ivermectin is mainly used in humans in the treatment of onchocerciasis but is also effective against other worm infestations (such as strongyloidiasis, ascariasis, trichuriasis, and enterobiasis). Ivermectin binds selectively and with high affinity to glutamate-gated chloride ion channels in invertebrate muscle and nerve cells of the microfilaria. This binding causes an increase in the permeability of the cell membrane to chloride ions and results in hyperpolarization of the cell, leading to paralysis and death of the parasite. Ivermectin also is believed to act as an agonist of the neurotransmitter gamma-aminobutyric acid (GABA), thereby disrupting GABA-mediated central nervous system (CNS) neurosynaptic transmission. Ivermectin may also impair the normal intrauterine development of O. volvulus microfilariae and may inhibit their release from the uteri of gravid female worms. It is sold under brand names Heartgard, Sklice and Stromectol in the United States, Ivomec worldwide by Merial Animal Health, Mectizan in Canada by Merck, Iver-DT in Nepal by Alive Pharmaceutical and Ivexterm in Mexico by Valeant Pharmaceuticals International. In Southeast Asian countries, it is marketed by Delta Pharma Ltd. under the trade name Scabo 6.