Iodoquinol and Quinacrine
M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson in Kucers’ The Use of Antibiotics, 2017
Quinacrine, also known as mepacrine hydrochloride, was synthesized by scientists at Bayer in Germany in 1931. It was one of the first synthetic antimalarial substitutes for quinine but was later superseded by chloroquine because of the latter’s more favorable toxicity profile. During World War II, it was marketed as Mepacrine or Atabrine, and it has been used for malaria chemoprophylaxis. More recently, it has been used as an antiprotozoal agent because it has activity against G. lamblia as well as Plasmodium species. However, quinacrine is now rarely used to treat giardiasis because of the drug’s toxicity and the superiority of metronidazole for this indication (see Chapter 99, Metronidazole) (Upcroft and Upcroft, 2001). Quinacrine has also been used for the treatment of tapeworm, but it has been replaced for this indication by newer, less toxic agents. It is an acridine derivative that is both water and alcohol soluble, with the chemical formula C23H30ClN3O and a molecular weight of 400.0 g/mol; the chemical structure is shown in Figure 191.2.
Cryptosporidium sp. findings in AIDS patients: A case report
Cut Adeya Adella in Stem Cell Oncology, 2018
Clinical manifestation similarities are found in giardiasis, isosporiasis and cyclosporiasis. After a 3-12 day incubation period, clinical manifestation will be present. Watery diarrhoea is the main symptom, which may be associated with other symptoms, such as: abdominal cramps (96% of patients); anorexia, malaise, flatulence, nausea, vomiting (65%); and mildly elevated temperature (59%) (Davies & Chalmers, 2009). Cryptosporidiosis is associated with a higher mortality rate and more severe symptoms when an immunocompromised host is infected. Moreover, the CD4 count can be a predictor for this infection. There is no effective therapy for this infection because of its resistance to many antiprotozoal drugs, particularly for immunocompromised patients. Vaccine is also unavailable, however, ongoing research is still trying to find a vaccine using microRNAs (Checkley et al., 2015).
Medicinal Plants: A Potent Antimicrobial Source and An Alternative to Combat Antibiotic Resistance
Jayanta Kumar Patra, Gitishree Das, Sanjeet Kumar, Hrudayanath Thatoi in Ethnopharmacology and Biodiversity of Medicinal Plants, 2019
Antibiotics also referred to as antibacterial or antimicrobial are biochemical compounds of microbial origin used for the treatment and prevention of microbial infection. They either kill the infection-causing bacteria or inhibit its growth. Some of the antibiotics also show antiprotozoal activity but are ineffective against the virus. During 20th century application/use of antibiotics emerged as a revolution in the field of medicine. Their usage in combination with vaccines eradiated disease like tuberculosis in many parts of the world. However, massive production, usage and rapid control of disease symptoms by antibiotics resulted in their over and misuse, this led to the development of antibiotic resistance by bacterial strains. According to the World Health Organization (WHO), antibiotic-resistant could be a great challenge for the future and thus classified as a serious threat to the medical field and practices. But in past years rather than a future prediction antibiotic resistance has emerged as a problem in almost every part of the globe and shown to adversely affect every individual irrespective of age and country. Thus, there is a need to identify new antibacterial agents so the problem associated with the development of resistant against existing antibacterial agents/antibiotics can be addressed. This has forced researchers to discover new drugs/antibacterial agents with less side effects at a comparable cost. Plants promise a source of natural antimicrobial agents. Antibacterial substances derived from plant sources have thus come up as an answer to the problem. These antimicrobial substances are natural and can provide an extensive range of application (Amenu, 2014).
Controlled delivery of the antiprotozoal agent (tinidazole) from intravaginal polymer matrices for treatment of the sexually transmitted infection, trichomoniasis
Published in Pharmaceutical Development and Technology, 2019
Hevanshi Vidhushika Fernando, Li Li Chan, Nhung Dang, Diviya Santhanes, Hasini Banneheke, Sivalingam Nalliah, Allan G. A. Coombes
Microporous PCL matrices incorporating tinidazole may be prepared by rapidly cooling co-solutions of PCL and the drug, resulting in a maximum tinidazole loading of 3.9% (w/w). Gradual release of around 50% of the drug load occurred over 7 days in SVF with retained antiprotozoal activity of almost 50% at day 7 compared with 35% for equivalent concentrations of ‘non-formulated’ drug solutions. Based on in vitro measurements, the predicted in vivo concentrations of tinidazole produced over 7 days by a PCL matrix in the form of an IVR would exceed the MIC against the protozoan parasite T. vaginalis. These findings recommend investigations of IVRs produced from the matrix material to evaluate their flexural properties, insertion and retention characteristics and in vivo behaviour.
Thio- and selenosemicarbazones as antiprotozoal agents against Trypanosoma cruzi and Trichomonas vaginalis
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Alexandra Ibáñez-Escribano, Cristina Fonseca-Berzal, Mónica Martínez-Montiel, Manuel Álvarez-Márquez, María Gómez-Núñez, Manuel Lacueva-Arnedo, Teresa Espinosa-Buitrago, Tania Martín-Pérez, José Antonio Escario, Penélope Merino-Montiel, Sara Montiel-Smith, Alicia Gómez-Barrio, Óscar López, José G. Fernández-Bolaños
Management of diseases caused by pathogenic protozoa is not a simple task4. On the one hand, development of successful vaccines is a hitherto unachieved goal5; on the other hand, the chemotherapeutic arsenal available so far suffers from important drawbacks: most of them are old drugs that are developing chemoresistance6, and are endowed with severe side-effects7 and low efficiency8. Moreover, their high prices, and complex administration protocols make them unaffordable for underdeveloped countries9. Accordingly, the development of new antiprotozoal agents is a hot topic in current Medicinal Chemistry research10,11.
Exploiting drug delivery systems for oral route in the peptic ulcer disease treatment
Published in Journal of Drug Targeting, 2021
Larissa Spósito, Giovanna Capaldi Fortunato, Bruna Almeida Furquim de Camargo, Matheus Aparecido dos Santos Ramos, Maurício Palmeira Chaves de Souza, Andréia Bagliotti Meneguin, Taís Maria Bauab, Marlus Chorilli
The nitroimidazoles are a class of antimicrobials that have antibacterial and antiprotozoal activity. Metronidazole and tinidazole are the main drugs that integrate this class, remaining as the drugs of choice in several infections of parasitic and bacterial origin [39]. In general, the mechanism of action occurs through the inhibition of nucleic acid synthesis, resulting in DNA degradation [40]. Another point that should be highlighted is that the reduction in metronidazole occurs only under low oxygen concentrations, justifying why metronidazole is only toxic to anaerobic and microaerophilic microorganisms, such as H. pylori [41,42].
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