RESUMO
The anti-inflammatory and antimalarial drug chloroquine is said to be one of the most frequently used drugs to commit suicide in the Orient and Far East. After the ingestion of large amounts of this 4-amino-chinoline derivate, signs of cardiac conduction disturbances are evidence of cardiotoxic action. For clinical treatment, hemoperfusion by activated charcoal has rather than hemodialysis proved to be partly effective for the removal of the toxic substance. Following a suicidal overdose of chloroquine tablets in a 13-year-old boy, we could confirm the efficiency of hemoperfusion by continued toxicologic examinations. The total elimination was nevertheless slow. Due to high postmortem concentrations in the blood and tissues, we believe that chloroquine is deposited and especially concentrated in the reticulohistiocytary system of the liver. Death after 5 days of clinical treatment in this case may be referred to as the first cardiac arrest with irreversible hypoxic damage of the brain.
Assuntos
Cloroquina/intoxicação , Medicina Legal , Adolescente , Autopsia , Cloroquina/análise , Cloroquina/sangue , Humanos , Masculino , Suicídio , Fatores de TempoRESUMO
In guinea pigs we studied the noradrenaline (NA) depletion in the sympathetic nerve terminals of the heart exerted by 24 derivatives of guanidine and amidine; the effects of these substances being considerably similar in their chemical structure were compared to those of reserpine, guanethidine, guanoxan and cyclazenin. Substitution of the free guanidine group to give an imidazoline or imidazolidine ring diminished the activity of the compounds. If the benzodioxane ring of guanoxan was "opened" to give a diether of catechol, the activity of the substances was not altered. We also observed a NA depletion after injection of some guanidine derivatives substituted with piperazine. The elongation of the aliphatic chain between guanidine and the aromatic substituent considerably decreased the activity of the compounds.
Assuntos
Amidinas/farmacologia , Guanidinas/farmacologia , Miocárdio/metabolismo , Norepinefrina/metabolismo , Animais , Relação Dose-Resposta a Droga , Guanetidina/farmacologia , Cobaias , Coração/efeitos dos fármacos , Coração/inervação , Masculino , Terminações Nervosas/metabolismo , Reserpina/farmacologia , Espectrometria de Fluorescência , Relação Estrutura-Atividade , Sistema Nervoso Simpático/metabolismo , Fatores de TempoRESUMO
Acridine dyes inhibit the incorporation of 3H-thymidine and 3H-uridine in intact cells to the same extent as Actinomycin D. In contrast to Actinomycin D, RNA synthesis by DNA - dependent RNA polymerase in a cell-free system is inhibited at lo2 higher concentrations of acridine dyes, only. Possible differential effects on the cell membrane resulting in decreased intracellular pools of uridine and thymidine are discussed.