Therapy for neurocysticercosis

Takayanagui, Osvaldo Massaiti

doi:10.1586/14737175.4.1.129

Cited by 39 publications

(22 citation statements)

References 65 publications

(116 reference statements)

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“…Praziquantel (PQZ), a chiral drug available as a racemic mixture, and albendazole (ABZ), a drug metabolized into the chiral active metabolite albendazole sulfoxide (ASOX), have been used as antiparasitic drugs for the treatment of human neurocysticercosis (NCC) [1–5].…”

Section: Introductionmentioning

confidence: 99%

Albendazole‐praziquantel interaction in healthy volunteers: kinetic disposition, metabolism and enantioselectivity

Lima¹,

Ferreira

Carvalho

et al. 2011

Brit J Clinical Pharma

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WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT• Pharmacokinetic interactions between albendazole and praziquantel are based on plasma concentrations of the enantiomeric mixture of both drugs with contradictory data, although the antiparasitic activity arises from (-)-(R)-praziquantel and (+)-albendazole sulfoxide. WHAT THIS STUDY ADDS• The pharmacokinetic interaction between albendazole and praziquantel is enantioselective. Praziquantel increased the plasma concentrations of (+)-albendazole sulfoxide more than those of (-)-albendazole sulfoxide and the administration of albendazole did not change the kinetic disposition of (+)-(S)-praziquantel, but increased the plasma concentration of (-)-(R)-praziquantel. AIMThis study investigated the kinetic disposition, metabolism and enantioselectivity of albendazole (ABZ) and praziquantel (PZQ) administered alone and in combination to healthy volunteers. METHODSA randomized crossover study was carried out in three phases (n = 9), in which some volunteers started in phase 1 (400 mg ABZ), others in phase 2 (1500 mg PZQ), and the remaining volunteers in phase 3 (400 mg ABZ + 1500 mg PZQ). Serial blood samples were collected from 0-48 h after drug administration. Pharmacokinetic parameters were calculated using a monocompartmental model with lag time and were analyzed using the Wilcoxon test; P Յ 0.05. RESULTSThe administration of PZQ increased the plasma concentrations of (+)-ASOX (albendazole sulphoxide) by 264% (AUC 0.99 vs. 2.59 mg ml -1 h), (-)-ASOX by 358% (0.14 vs. 0.50 mg ml -1 h) and albendazole sulfone (ASON) by 187% (0.17 vs. 0.32 mg ml -1 h). The administration of ABZ did not change the kinetic disposition of (+)-(S)-PZQ (-)-(R)-4-OHPZQ or (+)-(S)-4-OHPZQ, but increased the plasma concentration of (-)-(R)-PZQ by 64.77% (AUC 0.52 vs. 0.86 mg ml -1 h). CONCLUSIONSThe pharmacokinetic interaction between ABZ and PZQ in healthy volunteers was demonstrated by the observation of increased plasma concentrations of ASON, both ASOX enantiomers and (-)-(R)-PZQ. Clinically, the combination of ABZ and PZQ may improve the therapeutic efficacy as a consequence of higher concentration of both active drugs. On the other hand, the magnitude of this elevation may represent an increased risk of side effects, requiring, certainly, reduction of the dosage. However, further studies are necessary to evaluate the efficacy and safety of this combination.

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Section: Introductionmentioning

confidence: 99%

Albendazole‐praziquantel interaction in healthy volunteers: kinetic disposition, metabolism and enantioselectivity

Lima¹,

Ferreira

Carvalho

et al. 2011

Brit J Clinical Pharma

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“…Although treatment should cause earlier degeneration of cysticerci and could therefore decrease the risk of persistent neurological symptoms,7 there are concerns that seizures and other neurological events can be triggered by the inflammatory reaction to treatment induced cysticercal degeneration 6. Frequently, spontaneous resolution of parenchymal cysticerci is observed on serial imaging studies 8.…”

mentioning

confidence: 99%

Effects of albendazole treatment on neurocysticercosis: a randomised controlled trial

Carpio

Kelvin²,

Bagiella³

et al. 2008

Journal of Neurology, Neurosurgery & Psychiatry

143

116

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Aim: The aim of this trial was to evaluate the effects of albendazole (ALB) on cyst disappearance, reduction of the number of cysts and seizure recurrence. Methods: 178 patients with new onset symptoms due to active or transitional neurocysticercosis were randomly assigned to receive either 800 mg of ALB daily or placebo for 8 days. All patients also received prednisone. Imaging studies were done at baseline and at months 1, 6 and 12 of follow-up. Results: Active cysts were identified in 59 of 88 people randomised to ALB and 57 of the 90 in the placebo arm.

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“…Neurocysticercosis is the most common helminthic disease of the nervous system, being considered a serious public health problem in developing countries of Latin America, Asia, and Africa [1][2][3]. Although restricted to palliative measures, the treatment of neurocysticercosis has advanced over the last 20 years with the use of praziquantel (PZQ) and albendazole (ABZ), drugs considered effective against the cystic larvae [2,4].…”

Section: Introductionmentioning

confidence: 99%

“…Although restricted to palliative measures, the treatment of neurocysticercosis has advanced over the last 20 years with the use of praziquantel (PZQ) and albendazole (ABZ), drugs considered effective against the cystic larvae [2,4]. ABZ has been found to be more effective than PZQ, but in some patients there is persistence of cysts even after repeated use of ABZ [2]. For these cases, alternative treatment schedules such as the simultaneous use of PZQ and ABZ has been evaluated [4,5].…”

Section: Introductionmentioning

confidence: 99%

Simultaneous determination of albendazole metabolites, praziquantel and its metabolite in plasma by high-performance liquid chromatography–electrospray mass spectrometry

Bonato

Oliveira

Santana

et al. 2007

Journal of Pharmaceutical and Biomedical Analysis

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Therapy for neurocysticercosis

Cited by 39 publications

References 65 publications

Albendazole‐praziquantel interaction in healthy volunteers: kinetic disposition, metabolism and enantioselectivity

Albendazole‐praziquantel interaction in healthy volunteers: kinetic disposition, metabolism and enantioselectivity

Effects of albendazole treatment on neurocysticercosis: a randomised controlled trial

Simultaneous determination of albendazole metabolites, praziquantel and its metabolite in plasma by high-performance liquid chromatography–electrospray mass spectrometry

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