RESUMO
The aim of this work was to analyze the prevalence of level function disorder in patients with atrial fibrillation taking constantly amiodarone. Two groups of patients were studied: in group 1 (n = 78) patients with persistent atrial fibrillation taking constantly amiodarone for rhythm control were included, group 2 (n = 67) consisted of patients with permanent atrial fibrillation taking propafenon, ethacizine and digoxin for rate control. In studied groups liver transaminase activity and data of liver echography after 90 +/- 8 days of treatment were estimated. In 51.58% patients of group 1 asymptomatic increase of liver transaminase activity was found. If liver transaminase activity had been raised before taking amiodarone, frequency and degree of liver transaminase increase extended. Consequently, patients taking constantly amiodarone, require dynamic control of GGTP, AIAT, AsAT once a quarter. If liver transaminase activity increases because of amiodarone taking the method of treatment is possible to be changed and rate control therapy may be chosen.
Assuntos
Amiodarona/efeitos adversos , Antiarrítmicos/efeitos adversos , Fibrilação Atrial/tratamento farmacológico , Doença Hepática Induzida por Substâncias e Drogas/sangue , Fígado/metabolismo , Transaminases/sangue , Idoso , Amiodarona/administração & dosagem , Antiarrítmicos/administração & dosagem , Fibrilação Atrial/sangue , Fibrilação Atrial/fisiopatologia , Doença Hepática Induzida por Substâncias e Drogas/fisiopatologia , Feminino , Humanos , Fígado/fisiopatologia , Masculino , Pessoa de Meia-IdadeRESUMO
Five different types of muscarine-sensitive receptors were identified until now. In routine practice, the nonselective antagonist of cholinoreceptors are replaced by ipratropium bromide that is selectively blocking M1, M2, and M3 subtypes with the same affinity to each of them. However, the blockage of M2 subtype leads to bronchoconstriction and is accompanied by inhibition of M3 receptors in bronchial smooth muscles. The new drug tiotropium bromide selectively inhibits only the M1 and M3 types of receptors and does not affect the M2 subtype. This drug is administered only once a day, which is very important in clinical practice. Thus tiotropium bromide is the drug of choice for basic therapy of COPD.
Assuntos
Broncodilatadores/uso terapêutico , Doença Pulmonar Obstrutiva Crônica/tratamento farmacológico , Doença Pulmonar Obstrutiva Crônica/metabolismo , Derivados da Escopolamina/uso terapêutico , Animais , Brônquios/metabolismo , Brônquios/fisiopatologia , Broncoconstrição/efeitos dos fármacos , Humanos , Antagonistas Muscarínicos/uso terapêutico , Músculo Liso/metabolismo , Músculo Liso/fisiopatologia , Doença Pulmonar Obstrutiva Crônica/fisiopatologia , Receptores Muscarínicos , Brometo de TiotrópioRESUMO
The original pseudopeptide drug ingamine (4-[N-[2-(imidazol-4-yl)ethyl]-carbamoyl] butyric acid) was studied on the traditional model of antigen-induced bronchospasm in actively sensitized guinea pigs. The drug was introduced using various methods (by inhalation, via intragastric tube, and by intraperitoneal injections) in a range of doses (20, 50, 150, or 500 mg/kg). The new drug exhibited a pronounced dose-dependent protector action for all ways of introduction, but the most significant effect was observed upon inhalation, whereby the degree of bronchospasm inhibition exceeded 80%. In comparison to the reference drug sodium cromoglycate, ingamine (in equimolar doses) showed a higher activity with respect to the antigen-dependent bronchospasmic reactions. It can be expected that ingamine will provide for the effective treatment of bronchial obstruction under clinical conditions.
Assuntos
Espasmo Brônquico/tratamento farmacológico , Broncoconstrição/efeitos dos fármacos , Histamina/análogos & derivados , Histamina/administração & dosagem , Animais , Hiper-Reatividade Brônquica/tratamento farmacológico , Hiper-Reatividade Brônquica/fisiopatologia , Espasmo Brônquico/fisiopatologia , Relação Dose-Resposta a Droga , Feminino , Cobaias , MasculinoRESUMO
Data available in literature on the biological activity of antisense oligonucleotides are reviewed with emphasis on the results of tests of the related antitumor and antiasthmatic preparations and the basic novelty of these drugs.
Assuntos
Terapia Genética/métodos , Oligonucleotídeos Antissenso/uso terapêutico , Humanos , Oligonucleotídeos Antissenso/administração & dosagem , Oligonucleotídeos Antissenso/farmacologiaRESUMO
Lycopine in a daily dose of 0.2 mg/kg produced a gastroprotector effect on the model of hydrocortisone-induced gastritis in rats. A change in the dosage (toward significant increase or decrease) significantly reduces the gastroprotector effect.
Assuntos
Adjuvantes Imunológicos/uso terapêutico , Antioxidantes/uso terapêutico , Carotenoides/uso terapêutico , Mucosa Gástrica/patologia , Gastrite/tratamento farmacológico , Hidrocortisona , Doença Aguda , Animais , Gastrite/induzido quimicamente , Gastrite/prevenção & controle , Contagem de Leucócitos , Licopeno , Masculino , Neutrófilos/patologia , RatosRESUMO
A-25 sephadex-induced granulomatous inflammation of the lungs in rats was treated with beta-carotene and intal in inhalations. Both drugs showed antiinflammatory activity reducing the area of alveolitis and emphysema in the lungs, number of neutrophils and lymphocytes in the bronchoalveolar fluid. The experimental data allow to recommend further trial of intal and beta-carotene in granulomatous pulmonary diseases.
Assuntos
Anti-Inflamatórios/uso terapêutico , Cromolina Sódica/uso terapêutico , Modelos Animais de Doenças , Granuloma de Células Plasmáticas Pulmonar/tratamento farmacológico , beta Caroteno/uso terapêutico , Animais , Líquido da Lavagem Broncoalveolar/citologia , Dextranos , Avaliação Pré-Clínica de Medicamentos , Pulmão/efeitos dos fármacos , Pulmão/patologia , Granuloma de Células Plasmáticas Pulmonar/induzido quimicamente , Granuloma de Células Plasmáticas Pulmonar/patologia , Ratos , Ratos Wistar , Fatores de TempoRESUMO
The authors studied the effect of some antiasthmatic drugs (theophylline, budesonide, sodium cromalyne) and beta-carotene in vitro on spontaneous and PHA-induced proliferation of human peripheral blood mononuclears (PBMN). It was found that the drugs had no effect on spontaneous cell proliferation. But budesonide caused a 4-fold and beta-carotene a 6-fold decrease of the index of PHA-stimulated PBMN proliferation. It is concluded that beta-carotene may be used in clinical practice as an anti-inflammatory agent for bronchial asthma treatment.
Assuntos
Antiasmáticos/farmacologia , Leucócitos Mononucleares/efeitos dos fármacos , Divisão Celular/efeitos dos fármacos , Células Cultivadas , Humanos , Leucócitos Mononucleares/citologia , Leucócitos Mononucleares/metabolismo , Fito-Hemaglutininas/farmacologia , Timidina/metabolismo , TrítioRESUMO
The article deals with the latest achievements in the interpretation of the mechanism of programmed cell death (apoptosis). The effect of drugs on the different stages of the apoptotic signal conduction is analysed. The earliest prospects of creating apoptosis regulating agents are planned. It is suggested that tests for apoptosis should be included in the list of obligatory ones in the preclinical studies of new biologically active compounds.
Assuntos
Apoptose/efeitos dos fármacos , Animais , Apoptose/genética , Apoptose/fisiologia , Humanos , Necrose , Receptores de Superfície Celular/efeitos dos fármacos , Receptores de Superfície Celular/fisiologiaRESUMO
The article discusses the principal structure of nuclear receptors. The structure and function of retinoid receptors, their main ligands and inhibitors are analysed. Data (experimental and clinical) concerning the immunotropic antineoplastic and cardiovascular activity of the main retinoids are given.
Assuntos
Receptores do Ácido Retinoico/fisiologia , Receptores do Ácido Retinoico/ultraestrutura , Animais , Humanos , Ligantes , Substâncias Macromoleculares , Receptores do Ácido Retinoico/antagonistas & inibidores , Receptores do Ácido Retinoico/classificação , Retinoides/metabolismo , Retinoides/farmacologiaRESUMO
The modern advancements in the study of the mechanisms of reperfusion damage in myocardial infarction are analysed. Emphasis is placed on the leukocyte-endothelial interactions and the role of various adhesive molecules and cytokines. The effect of various biotechnological agents and drugs, products of chemical synthesis, on some links of the reperfusion syndrome are discussed. A classification of substances possessing a protective effect in ischemia/reperfusion is proposed.