Abstract
A brief therapeutic regimen of praziquantel, reduced to a single day, has been effective for treatment of neurocysticercosis. To study its pharmacokinetic characteristics, levels of praziquantel in plasma were determined for eight healthy volunteers after the administration of three oral doses of 25 mg/kg of body weight given at 2-h intervals, alone and with the simultaneous administration of cimetidine. Each volunteer received both regimens in a randomized crossover design. Blood samples were taken during a period of 12 h, and praziquantel concentration was measured by high-performance liquid chromatography. Levels of praziquantel in plasma remained above 300 ng/ml during a period of 12 h; they increased 100% when cimetidine was jointly administered. Compared with other regimens, the high levels obtained and the longer duration of action seem to be advantageous in prolonging the exposure of the parasites to the drug and support previous clinical experience showing that the treatment of neurocysticercosis with praziquantel can be reduced from 2 weeks to 1 day with the drug still retaining its cysticidal properties. Moreover, simultaneous administration of praziquantel and cimetidine could improve further the efficacy of the single-day therapy for cysticercosis and other parasitic diseases, such as schistosomiasis.
Full Text
The Full Text of this article is available as a PDF (99.5 KB).
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Bittencourt P. R., Gracia C. M., Gorz A. M., Mazer S., Oliveira T. V. High-dose praziquantel for neurocysticercosis: efficacy and tolerability. Eur Neurol. 1990;30(4):229–234. doi: 10.1159/000117352. [DOI] [PubMed] [Google Scholar]
- Bittencourt P. R., Gracia C. M., Gorz A. M., Oliveira T. V. High-dose praziquantel for neurocysticercosis: serum and CSF concentrations. Acta Neurol Scand. 1990 Jul;82(1):28–33. doi: 10.1111/j.1600-0404.1990.tb01583.x. [DOI] [PubMed] [Google Scholar]
- Corona T., Lugo R., Medina R., Sotelo J. Single-day praziquantel therapy for neurocysticercosis. N Engl J Med. 1996 Jan 11;334(2):125–125. doi: 10.1056/NEJM199601113340216. [DOI] [PubMed] [Google Scholar]
- Dachman W. D., Adubofour K. O., Bikin D. S., Johnson C. H., Mullin P. D., Winograd M. Cimetidine-induced rise in praziquantel levels in a patient with neurocysticercosis being treated with anticonvulsants. J Infect Dis. 1994 Mar;169(3):689–691. doi: 10.1093/infdis/169.3.689. [DOI] [PubMed] [Google Scholar]
- Ebeid F. A., Metwally A. A., Botros S. S., Bennet J. L. Treatment of experimental schistosomiasis mansoni with praziquantel alone and combined with cimetidine. Arzneimittelforschung. 1994 Nov;44(11):1268–1270. [PubMed] [Google Scholar]
- Estañol B., Juárez H., Irigoyen M. del C., González-Barranco D., Corona T. Humoral immune response in patients with cerebral parenchymal cysticercosis treated with praziquantel. J Neurol Neurosurg Psychiatry. 1989 Feb;52(2):254–257. doi: 10.1136/jnnp.52.2.254. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Flisser A., Madrazo I., Plancarte A., Schantz P., Allan J., Craig P., Sarti E. Neurological symptoms in occult neurocysticercosis after single taeniacidal dose of praziquantel. Lancet. 1993 Sep 18;342(8873):748–748. doi: 10.1016/0140-6736(93)91743-6. [DOI] [PubMed] [Google Scholar]
- González-Esquivel D. F., Okuno C. M., Sánchez Rodríguez M., Solelo Morales J., Cook H. J. Sensitive high-performance liquid chromatographic assay for praziquantel in plasma, urine and liver homogenates. J Chromatogr. 1993 Mar 5;613(1):174–178. doi: 10.1016/0378-4347(93)80213-n. [DOI] [PubMed] [Google Scholar]
- Jung H., Hurtado M., Medina M. T., Sanchez M., Sotelo J. Dexamethasone increases plasma levels of albendazole. J Neurol. 1990 Aug;237(5):279–280. doi: 10.1007/BF00314741. [DOI] [PubMed] [Google Scholar]
- Jung H., Hurtado M., Sanchez M., Medina M. T., Sotelo J. Plasma and CSF levels of albendazole and praziquantel in patients with neurocysticercosis. Clin Neuropharmacol. 1990 Dec;13(6):559–564. doi: 10.1097/00002826-199012000-00008. [DOI] [PubMed] [Google Scholar]
- Jung H., Vazquez M. L., Sanchez M., Penagos P., Sotelo J. Clinical pharmacokinetics of praziquantel. Proc West Pharmacol Soc. 1991;34:335–340. [PubMed] [Google Scholar]
- Leopold G., Ungethüm W., Groll E., Diekmann H. W., Nowak H., Wegner D. H. 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. Eur J Clin Pharmacol. 1978 Dec 1;14(4):281–291. doi: 10.1007/BF00560463. [DOI] [PubMed] [Google Scholar]
- Mandour M. E., el Turabi H., Homeida M. M., el Sadig T., Ali H. M., Bennett J. L., Leahey W. J., Harron D. W. Pharmacokinetics of praziquantel in healthy volunteers and patients with schistosomiasis. Trans R Soc Trop Med Hyg. 1990 May-Jun;84(3):389–393. doi: 10.1016/0035-9203(90)90333-a. [DOI] [PubMed] [Google Scholar]
- Metwally A., Bennett J. L., Botros S., Ebeid F. Effect of cimetidine, bicarbonate and glucose on the bioavailability of different formulations of praziquantel. Arzneimittelforschung. 1995 Apr;45(4):516–518. [PubMed] [Google Scholar]
- Overbosch D., van de Nes J. C., Groll E., Diekmann H. W., Polderman A. M., Mattie H. Penetration of praziquantel into cerebrospinal fluid and cysticerci in human cysticercosis. Eur J Clin Pharmacol. 1987;33(3):287–292. doi: 10.1007/BF00637564. [DOI] [PubMed] [Google Scholar]
- Sotelo J., Escobedo F., Rodriguez-Carbajal J., Torres B., Rubio-Donnadieu F. Therapy of parenchymal brain cysticercosis with praziquantel. N Engl J Med. 1984 Apr 19;310(16):1001–1007. doi: 10.1056/NEJM198404193101601. [DOI] [PubMed] [Google Scholar]
- Sotelo J., del Brutto O. H., Penagos P., Escobedo F., Torres B., Rodriguez-Carbajal J., Rubio-Donnadieu F. Comparison of therapeutic regimen of anticysticercal drugs for parenchymal brain cysticercosis. J Neurol. 1990 Apr;237(2):69–72. doi: 10.1007/BF00314663. [DOI] [PubMed] [Google Scholar]
- Vazquez M. L., Jung H., Sotelo J. Plasma levels of praziquantel decrease when dexamethasone is given simultaneously. Neurology. 1987 Sep;37(9):1561–1562. doi: 10.1212/wnl.37.9.1561. [DOI] [PubMed] [Google Scholar]
- Vazquez V., Sotelo J. The course of seizures after treatment for cerebral cysticercosis. N Engl J Med. 1992 Sep 3;327(10):696–701. doi: 10.1056/NEJM199209033271005. [DOI] [PubMed] [Google Scholar]
- Watt G., Adapon B., Long G. W., Fernando M. T., Ranoa C. P., Cross J. H. Praziquantel in treatment of cerebral schistosomiasis. Lancet. 1986 Sep 6;2(8506):529–532. doi: 10.1016/s0140-6736(86)90110-8. [DOI] [PubMed] [Google Scholar]