Quinacrine: An Effective Addition to the Treatment of Refractory Cutaneous Lupus Erythematosus

Summary@#Treatment of refractory cutaneous lupus is challenging. When conventional therapy, including hydroxychloroquine (HCQ), corticosteroids and immunosuppressants, has failed, the addition of quinacrine may be a promising option. We describe a case of refractory chronic cutaneous lupus erythematosus (CCLE) who responded well to quinacrine.

Quinacrine causes apoptosis in human cancer cell lines through caspase-mediated pathway and regulation of small-GTPase

Quinacrine (QC), an FDA-approved anti-malarial drug, has shown to have anticancer activities. Due to its‘shotgun’ nature, QC has become an inevitable candidate for combination chemotherapy. There is lack of studyof the molecular interplay between colorectal cancer (CRC) microenvironment and its metastasis. In this study,we focused on the differential anti-cancerous effect of QC on two different human cancer cell lines, HCT 116and INT 407. Results suggest that cytotoxicity increased in both the cell lines with an increase in QCconcentration. The expression patterns of small-GTPases and caspases were altered significantly in QC-treatedcells compared to non-treated cells. HSP70 and p53 showed comparable differences in the expression pattern.The wound-healing assay showed an increase in the denuded zone, with an increase in the concentration ofQC. The formation of apoptotic nuclei increased with a rise in the concentration of QC in both the cell lines.The decrease and increase in caspase 9 and caspase 3 expression respectively were studied, confirmingapoptosis by the extrinsic pathway

Avaliação das concentrações de zinco no aparelho reprodutor feminino por ativação neutrônica instrumental / Assessment of zinc concentration in the female reproductive system by instrumental neutron activation

A esterilização feminina não cirúrgica por meio da aplicação intracervical de pastilhas de cloridrato de quinacrina foi considerada um método contraceptivo definitivo de baixo custo, seguro e eficaz. O zinco, presente no útero e nas tubas uterinas, inibe a ação da quinacrina. A adição de cobre aumenta a eficácia da quinacrina, reduzindo o risco de gravidez devido às falhas de obstrução das tubas uterinas. O cobre neutraliza o efeito deletério do zinco, aumentando a eficácia do método. Para obter o mapeamento da concentração de zinco no aparelho reprodutor feminino, amostras de útero e de tubas uterinas foram analisadas por ativação neutrônica instrumental. Os resultados obtidos são apresentados neste trabalho.

Nonsurgical female sterilization through the transcervical insertion of quinacrine pellets was considered a definitive, low-cost, safe and effective contraceptive method. The zinc, present in both uterus and Fallopian tubes, inhibit the action of quinacrine. The addition of copper increases the efficacy of quinacrine, thus reducing the risk of pregnancy due to the failure to obstruct the Fallopian tubes. The copper neutralized the deleterious effect of the zinc and so the treatment efficacy is increased. In order to obtain a mapping to study the zinc concentration in the female reproductive system, samples of both uterus and Fallopian tubes were analyzed by neutron activation. The results are here reported.

Desenvolvimento de metodologia para fabricação de pastilhas de cobre para utilização em esterilização feminina não cirúrgica com quinacrina / Development of methods for the manufacturing of copper pellets to use inquinacrine female non-surgical sterilization

Objetivo: A esterilização feminina não cirúrgica por meio da aplicação intracervical de pastilhas de quinacrina foi considerada um método contraceptivo definitivo, de baixo custo, seguro e eficaz, e é sabido que a adição do cobre aumenta a eficácia da quinacrina. Com o objetivo de produzir pastilhas de cobre a serem aplicadas juntamente com pastilhas de quinacrina, foi desenvolvido, no Centro de Desenvolvimento daTecnologia Nuclear da Comissão Nacional de Energia Nuclear (CDTN/CNEN), um processo para sua fabricação. Material e métodos: Utilizou-se póde cobre metálico esferoidal e amido de milho e empregaram-se as mesmas técnicas de metalurgia do pó empregada na fabricação de pastilhas combustíveis nucleares. Resultados: Foi possível definir o teor ideal de amido de milho para diminuir o intertravamento entre as partículas metálicas de cobre que propicia uma adequada desagregação das pastilhas quando umidificada, de modo a criar no útero um ambiente rico em cobre antes da dissolução das pastilhas de quinacrina. Conclusões: Foram, então, produzidas 200 pastilhas de cobre com 6% em peso de amido de milho, para viabilizar um projeto de pesquisa da Faculdade de Medicina da Universidade Federal de Minas Gerais sobre esterilização feminina não cirúrgica com quinacrina. São descritas as técnicas, os testes e os resultados do desenvolvimento desta metodologia.

Objectives: Non-surgical female sterilization through the transcervical insertion of quinacrine pellets was considered a definitive, low-cost, safe and effective contraceptive method. The addition of copper increases the efficacy of quinacrine, reducing the risk of pregnancy due to a failure in the obstruction’s procedure of the Fallopian tubes. In order to produce copper pellets to be applied together with the quinacrine pellets, a manufacturing procedure was developed at Centro de Desenvolvimento da Tecnologia Nuclear da Comissão Nacional de Energia Nuclear (CDTN/CNEN). Material and Methods: It was used spheroidal metallic copper and corn starch and the same technics of powder metallurgy employed to the fabrication of nuclear fuel pellets. Results: It was possible to defi ne the ideal corn starch content to decrease the interlock degree between the metallic copperparticles that provide an appropiate desintegration of the pellets when humidfied in order to create in the uterus an environment rich in copper before the quinacrine pellet dissolution. Conclusions: Two hundred copper pellets were produced with 6% by weight of corn starch to make possible a research project of Faculdade de Medicina of Universidade Federal de Minas Gerais about non-surgical female sterilization with quinacrina. The techniques, tests and results of the developed methodology are here presented.

Untoward effects of quinacrine hydrochloride as observed in 302,206 malaria cases

Observation study was made on 302,206 Filipino malaria patients who were given therapeutic doses of quinacrine hydrochloride (Atabrine). Of the 302,206 cases, 82.46% had vivax malaria and 17.54% had falciparum malaria. Two hundred twenty cases showed one or more untoward effect of the drug. Distribution of the 340 untoward effects observed in these subjects were presented. These untoward effects were temporary in nature and disappeared from one to eight days after the drug was discontinuedSelected untoward effects of drugs included the following: manic excitement, talkativeness, insomnia, depression, delusions, hallucinations, absent-mindedness and toxic psychoses.(Author)