The biochemical mode of action of some modern anthelmintics

Coles, G.C.

doi:10.1002/ps.2780080518

Cited by 52 publications

(18 citation statements)

References 58 publications

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“…It might be expected that, as flukes mature and move from more anaerobic conditions in liver parenchyma to more aerobic conditions in bile ducts, the increased efficacy of uncouplers of oxidative phosphorylation against mature flukes would be explained. However, whether this difference in efficacy is due to a different biochemical metabolism, a different position in the host, or a different uptake or metabolism of the drugs in the mature and immature flukes is still not resolved (Coles, 1977).…”

Section: Discussionmentioning

confidence: 99%

The pharmacodynamics of the flukicidal salicylanilides, rafoxanide, closantel and oxyclosanide

Mohammed-Ali

Bogan

1987

Vet Pharm & Therapeutics

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The pharmacokinetics of oxyclosanide, rafoxanide and closantel were investigated in sheep (n = 5). All three drugs were extensively (greater than 99%) bound to plasma proteins and the plasma concentration/time curve was best described by a tri-exponential equation. Closantel and rafoxanide had long terminal half-lives (mean 14.5 and 16.6 days, respectively) compared with oxyclosanide (mean 6.4 days). In a study of the efficacy of rafoxanide against Fasciola hepatica, a dose rate of 7.5 mg kg-1 against 6-week-old flukes appeared to be similarly effective to a dose rate of 2.5 mg kg-1 against 10-week-old flukes (86% and 88% efficacy, respectively), as assessed at autopsies carried out on all sheep when the flukes were 14 weeks old. Part of this putative efficacy against immature flukes may be due to rafoxanide persisting in the plasma and affecting the mature flukes when they reach the bile ducts.

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Section: Discussionmentioning

confidence: 99%

The pharmacodynamics of the flukicidal salicylanilides, rafoxanide, closantel and oxyclosanide

Mohammed-Ali

Bogan

1987

Vet Pharm & Therapeutics

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“…Given that the inactivation of FRD permits H. pylori to grow under artificial conditions [31], these anthelmintics, in addition to the inhibition of FRD activity, also appear to confer other lethal effects on H. pylori. This notion is supported by early studies showing that morantel also affects the nervous system of nematodes [60]; thiabendazole inhibits microtubule polymerisation in nematodes, cestodes and mammals [61][62][63].…”

Section: Inhibitory and Bactericidal Effect Of Helminthic Frd Inhibitmentioning

confidence: 86%

Potential of fumarate reductase as a novel therapeutic target in Helicobacter pylori infection

2002

Expert Opinion on Therapeutic Targets

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Approximately 50% of the world's population carries Helicobacter pylori, a gastric bacterial pathogen linked to diseases including gastritis, ulcers and gastric cancer. Chemotherapies are being routinely used to treat systemic H. pylori infection. The common regimens consist of proton pump inhibitors (PPIs) or ranitidine bismuth citrate (RBC) and two antibiotics. Although these regimens efficiently eradicate H. pylori, the emergence of antibiotic-resistant H. pylori strains, their severe side effects and high costs are major drawbacks of these treatments. More efficient, economic and friendly drugs need to be developed. Fumarate reductase (FRD) catalyses the reduction of fumarate to succinate in the Krebs cycle and is also a key enzyme in anaerobic respiration with fumarate as the terminal electron acceptor for many facultative bacteria. H. pylori FRD contains three subunits, FrdA, FrdB and FrdC. Genome analysis and experimental evidence indicate that this enzyme appears to play an important role in the energy metabolism of H. pylori. In addition, FRD is essential for the colonisation of H. pylori in the acidic stomach as demonstrated in the mouse model of infection. Furthermore, three FRD inhibitors used to cure helminthic infection in animals and humans have both inhibitory and bactericidal effects on H. pylori. These lines of evidence indicate that FRD may be a promising chemotherapeutic target. Given that FrdA is strongly immunogenic in the sera from H. pylori-positive patients, this protein may also be used as a candidate for the development of an anti-H. pylori vaccine.

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“…Μικρή πτωτική τάση των τιμών, μη στατιστικά σημαντική (<0,05), παρατηρήθηκε και στον πληθυσμό των λευκών αιμοσφαιρίων στην ομάδα των ζώων που χορηγήθηκε η κιτρική μοραντελη. Αυτό οφείλεται στο διαφορετικό μηχανισμό δράσης της 678 , αλλά και στη μικρή έως μηδαμινή απορροφητικότητα της από το γαστρεντερι-κό σωλήνα 18,19 . Αντίθετα, στην αλβενδαζόλη παρατηρήθηκε στατιστικά σημαντική διαφορά (>0,05) μείωσης του αριθ μού των λευκών αιμοσφαιρίων.…”

Section: αποτελεσματα -συζητησηunclassified

Effect of anthelmintics upon host organism

Theodoridis

Frydas

Rizos³

2018

J Hellenic Vet Med Soc

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To be estimated the effects of anthelmintics to the host, 21 female sheep of various age, breed and weight, which were naturally infected with gastrointestinal nematodes, were used. These animals were divided into three groups and given per os: in the 1st group, which was composed of 7 sheep, Morantel citrate (tetrahydropyrimidine group) approx. 465 mg/b.w., in the 2nd, which was composed of 8 sheep, Albendazole (benzimidazole group) approx. 300 mg/b.w. and in the 3rd, which was composed of 6 sheep, tap water only and this group was used as control. From these animals, blood samples intrajagularly were taken, at the same day, once a week for 9 continuous weeks. The first blood sample was taken 4 weeks before the anthelmintic therapy and the last one 5 weeks after therapy. There were no significance diferences (p> 0,005) in pre- and posttherapy measurements, regarding the PCV,s in all groups. In the control and morantel citrate groups, the leucocyte volume remained static, while contrarily, in the albendazole group a significance difference (p< 0,005) were observed. Because, the albendazole inhibits the construction of intestine cell microtubules of parasites, it can be concluded that, this activity, effects the host cells, and thus, this reduction of leucocytes was observed.

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The biochemical mode of action of some modern anthelmintics

Cited by 52 publications

References 58 publications

The pharmacodynamics of the flukicidal salicylanilides, rafoxanide, closantel and oxyclosanide

The pharmacodynamics of the flukicidal salicylanilides, rafoxanide, closantel and oxyclosanide

Potential of fumarate reductase as a novel therapeutic target in Helicobacter pylori infection

Effect of anthelmintics upon host organism

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