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At least 595 records · Page 33Linked to original sources
PubMed1978

Clinical pharmacology in normal volunteers of praziquantel, a new drug against schistosomes and cestodes. An example of a complex study covering both tolerance and pharmacokinetics.

The tolerance of Praziquantel (2-cyclohexylcarbonyl-1, 3, 4, 6, 7, 11b-hexahydro-2H-pyrazino-[2, 1-a]isoquinoline-4-one) in oral doses of 1 X 20 mg/kg, 1 X 50 mg/kg, 3 X 10 mg/kg and 3 X 25 mg/kg body weight (tau = 4 h) was tested in a complex study involving 36 healthy volunteers. In addition to the usual assessment of clinical chemistry, haematology, coagulation physiology, urinalysis, clinico-physiological examination including EEG, and medical examination, clinico-psychological parameters were also recorded and special neurological investigations were performed. No clinically relevant changes were found in any of the laboratory parameters, nor in the medical-neurological or clinico-physiological examinations. Based on a few clinico-psychological parameters and subjective comments, the largest daily dose tested (3 X 25 mg/kg = 75 mg/kg) produced a slight, transient disturbance in general well-being, which was barely detectable on objective clinical examination. The pharmacokinetic behaviour was dominated by rapid metabolism and pronounced first-pass metabolism of praziquantel, which greatly limits the value of results obtained by GC analysis of unchanged drug in serum. The peak concentration in serum was reached after 1--2 h, and the elimination half-life for the period 2--8 h was 1--1.5 h.

Adult↗
PubMed1985

The effect of praziquantel on the pseudophyllidean cestode Bothriocephalus acheilognathi in vitro.

Adult Bothriocephalus acheilognathi were incubated in solutions containing 0 (control), 0.1, 1.0, 10.0 and 100 micrograms praziquantel per ml (0, 10(2), 10(3), 10(4) and 10(5) micrograms l-1) of 0.9% saline for 5, 15 and 60 min at a temperature of 18 degrees C. The worms contracted immediately upon being placed in the drug. Scanning and transmission electron microscopy revealed considerable tegumental damage particularly in the neck region. Vacuolization and 'bubbling' of the tegument occurred in all of the drug solutions tested. Exposure to drug concentrations of more than 1.0 micrograms ml-1 (10(3) micrograms l-1) praziquantel for 15 min or greater resulted in many of the 'bubbles' bursting and releasing their contents to the exterior. Mature proglottides were distorted and had occasional large swellings resulting in the mass expulsion of eggs. Praziquantel had no ovicidal activity. Exposure to drug concentrations of 100 micrograms (10(5) micrograms l-1) praziquantel per ml saline for 24 h was not lethal to the worms.

Animals↗
PubMed1981

Ultrastructural investigations on the effect of praziquantel on the tegument of five species of cestodes.

Adult Hymenolepis diminuta, H. microstoma, H. nana, Echinococcus multilocularis, and Taenia (Hydatigera) taeniaeformis have been exposed in vitro in media containing 0.1 to 100 micrograms praziquantel/ml. Already after 5 min characteristic tegumental lesions, that were restricted to the growth zone of the neck region, were recognized using both scanning and transmission electron microscopy. Within the tegument numerous vacuoles were formed that released their contents to the exterior and finally caused destruction of the tegument. Proglottides of the central or posterior strobilar portions were never damaged. Larvae of T. taeniaeformis (cysticerci) and E. multilocularis (alveolar cysts) were studied employing the same methods both after in vitro exposure to and after in vivo treatment of their hosts with praziquantel. Strobilocerci of T. taeniaeformis developed identical tegumental lesions after contact with praziquantel whether incubated in vitro or treated in vitro. The wall of the bladder containing the larva remained unaffected. Evaginated protoscolices of E. multilocularis were damaged by in vitro contact with praziquantel while invaginated protoscolices remained intact. After in vivo exposure there were some fully developed evaginated and damaged protoscolices whereas all invaginated protoscolices and the cyst wall with its germinative layer were unaffected.

Animals↗
PubMed1989

Kinetics of mast cells, eosinophils and phospholipase B activity in the spontaneous-cure response of two strains of mice (rapid and slow responder) to the cestode Hymenolepis nana.

Primary egg-derived infection of Hymenolepis nana (100 eggs) in BALB/c (rapid responder) and C3H (slow responder) mice resulted in increased levels of mucosal mast cells (MMCs), eosinophilia (bone marrow, peripheral, tissue) and phospholipase B activity. The response appeared to be similar in both strains used, with a slight difference in cellular accumulation but a significantly earlier response in BALB/c than in C3H mice. These findings suggest that the prolongation of H. nana infection in C3H mice may be related to the delayed appearance of MMCs and eosinophils, which triggers a slower generation of the intestinal inflammation response. The rapidity with which phospholipase B activity increased was strictly correlated with eosinophil tissue number; this further supports the hypothesis for a direct parallel between eosinophils and phospholipase B activity in infected tissue.

Animals↗
PubMed1995

Electrical field-stimulated release of L-[G-3H]-glutamate from tissue slices of the cestode Hymenolepis diminuta.

The release of preloaded [3H]-L-glutamate by tissue slices of Hymenolepis diminuta was examined by the technique of electrical field stimulation. For tissues slices in balanced saline, a high-field strength of 1.78 A resulted in a highly elevated increase in the rate of release of radiolabel, which was suppressed in calcium-free saline. This technique may prove useful for screening helminth tissues for potential neurotransmitters.

Animals↗
PubMed1995

Phylogenetic relationships within Taenia taeniaeformis variants and other taeniid cestodes inferred from the nucleotide sequence of the cytochrome c oxidase subunit I gene.

Nucleotide sequence variations in a region of the mitochondrial cytochrome c oxidase subunit I (COI) gene (391 bp) were examined within seven species of the genus Taenia and two species of the genus Echinococcus, including ten isolates of T. taeniaeformis and six isolates of E. multilocularis. More than a 12% rate of nucleotide differences between taeniid species was found, allowing the species to be distinguished. In E. multilocularis, no sequence variation was observed among isolates, regardless of the host (gray red-backed vole, tundra vole, pig, Norway rat) or area (Japan, Alaska) from which each metacestode had been isolated. In contrast, six distinct sequences were detected among the ten T. taeniaeformis isolates examined. The level of nucleotide variation in the COI gene within T. taeniaeformis isolates except for one isolate from the gray red-backed vole (TtACR), which has been proposed as a distinct strain or a different species, was about 0.3%-4.1%, whereas the COI gene sequence for TtACR differed from those of the other isolates, with levels being 9.0%-9.5%. Phylogenetic trees were then inferred from these sequence data using two different algorithms.

Amino Acid Sequence↗