RESUMO
BACKGROUND: Obstructive sleep apnea (OSA) and hypertension are common conditions that may be linked through sympathetic activation and water retention. We hypothesized that diuretics, which reduce the body water content, may be more effective than amlodipine, a blood pressure (BP)-lowering agent implicated with edema, in controlling OSA in patients with hypertension. We also aimed to compare the effects of these treatments on ambulatory blood pressure monitoring (ABPM). METHODS: In a randomized, double-blind clinical trial, we compared the effects of chlorthalidone/amiloride 25/5 mg with amlodipine 10 mg on OSA measured by portable sleep monitor and BP measured by ABPM. The study included participants older than 40 who had moderate OSA (10-40 apneas/hour of sleep) and BP within the systolic range of 140-159 mmHg or diastolic range of 90-99 mmHg. RESULTS: The individuals in the experimental groups were comparable in age, gender, and other relevant characteristics. Neither the combination of diuretics nor amlodipine alone reduced the AHI after 8 weeks of treatment (AHI 26.3 with diuretics and 25.0 with amlodipine. P = 0.713). Both treatments significantly lowered office, 24-h, and nighttime ABP, but the two groups had no significant difference. CONCLUSION: Chlorthalidone associated with amiloride and amlodipine are ineffective in decreasing the frequency of sleep apnea episodes in patients with moderate OSA and hypertension. Both treatments have comparable effects in lowering both office and ambulatory blood pressure. The notion that treatments could offer benefits for both OSA and hypertension remains to be demonstrated. TRIAL REGISTRATION CLINICALTRIALS. GOV IDENTIFIER: NCT01896661.
Assuntos
Amilorida , Anlodipino , Anti-Hipertensivos , Monitorização Ambulatorial da Pressão Arterial , Clortalidona , Hipertensão , Apneia Obstrutiva do Sono , Humanos , Masculino , Feminino , Método Duplo-Cego , Hipertensão/tratamento farmacológico , Hipertensão/complicações , Pessoa de Meia-Idade , Anti-Hipertensivos/uso terapêutico , Clortalidona/uso terapêutico , Anlodipino/uso terapêutico , Apneia Obstrutiva do Sono/tratamento farmacológico , Apneia Obstrutiva do Sono/complicações , Amilorida/uso terapêutico , Diuréticos/uso terapêutico , Pressão Sanguínea/efeitos dos fármacos , Polissonografia/efeitos dos fármacos , IdosoRESUMO
Background: Sporotrichosis caused by Sporothrix brasiliensis is a globally emerging infectious disease with limited therapeutic options. Thus, we aimed to evaluate the in vitro activity of amlodipine (AML) and lufenuron (LUF) alone and their interaction with itraconazole (ITZ), the first-choice drug against S. brasiliensis. Methods: Twenty clinical isolates of S. brasiliensis from two hyperendemic regions were tested through a microdilution assay to evaluate the minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC) of AML and LUF. Checkerboard assay was performed with 10 isolates for both drug interactions with ITZ. Results: AML showed inhibitory and fungicidal activity against all isolates included, with MIC values ranging from 32 to 256 µg/mL, and MFC from 64 to 256 µg/mL. However, none of the S. brasiliensis isolates were inhibited by the highest soluble concentration of LUF (MIC >64 µg/mL for all strains). Synergic interaction of AML and LUF with ITZ occurred in 50% and 40% of the isolates tested, without any antagonistic effects. Conclusion: Both repurposing drugs evaluated in our study showed a promising in vitro activity, especially in synergy with ITZ against S. brasiliensis, warranting future in vivo investigations regarding its activity.
Assuntos
Antifúngicos , Leucemia Mieloide Aguda , Humanos , Antifúngicos/farmacologia , Anlodipino/farmacologia , Reposicionamento de Medicamentos , Itraconazol/farmacologia , Leucemia Mieloide Aguda/tratamento farmacológicoRESUMO
INTRODUÇÃO: A hipertensão arterial sistêmica (HAS), uma doença crônica, é um grave problema de saúde pública, caracterizada por níveis elevados e persistentes da pressão sanguínea, medidos em geral como uma razão da pressão arterial sistólica e diastólica (respectivamente maior ou igual a 140 mmHg; e/ou maior ou igual a 90 mmHg). Esta é uma doença altamente prevalente em todo o mundo. No Brasil, os números podem variar de acordo com a metodologia utilizada. Reportou-se na Pesquisa Nacional de Saúde de 2013, cujos dados são obtidos por autorrelato, a prevalência de hipertensão em 21% dos pacientes, mas ao considerar a aferição da pressão arterial e uso de medicamentos, o percentual de adultos com pressão arterial ≥140/90 mmHg foi de 32%. Sabe-se que a falta de controle da pressão arterial pode elevar o risco de ocorrência de eventos cardiovasculares, como infarto agudo do miocárdio, insuficiência cardíaca, acidente vascular cerebral, doenças renais, entre outros. Isso consequentemente pode causar problemas crônicos que reduzem a qualidade de vida do indivíduo, e até mesmo o
Assuntos
Humanos , Inibidores da Enzima Conversora de Angiotensina/administração & dosagem , Anlodipino/administração & dosagem , Hipertensão/tratamento farmacológico , Sistema Único de Saúde , Brasil , Eficácia , Análise Custo-Benefício/economia , Combinação de MedicamentosRESUMO
Advancing with our project about the development of new antiparasitic agents, we have enzymatically synthesized a series of amides derived from amlodipine, a calcium channel blocker used as an antihypertensive drug. Through lipase-catalyzed acylation with different carboxylic acids, nineteen amlodipine derivatives were obtained, eighteen of which were new compounds. To optimize the reaction conditions, the influence of several reaction parameters was analyzed, finding different requisites for aliphatic carboxylic acids and phenylacetic acids. All synthesized compounds were evaluated as antiproliferative agents against Trypanosoma cruzi, the etiological agent of American trypanosomiasis (Chagas' disease). Some of them showed significant activity against the amastigote form of T. cruzi, the clinically relevant form of the parasite. Among synthesized compounds, the derivatives of myristic and linolenic acids showed higher efficacy and lower cytotoxicity. These results added to the advantages shown by the enzymatic methodology, such as mild reaction conditions and low environmental impact, making this approach a valuable way to synthesize these amlodipine derivatives with an application as promising antiparasitic agents.
Assuntos
Doença de Chagas , Tripanossomicidas , Trypanosoma cruzi , Humanos , Anlodipino/farmacologia , Anlodipino/uso terapêutico , Antiparasitários/uso terapêutico , Acilação , Ácidos Carboxílicos , Tripanossomicidas/farmacologia , Tripanossomicidas/uso terapêutico , Doença de Chagas/tratamento farmacológicoRESUMO
Apresentação Clínica ⢠Paciente feminina, 39 anos; ⢠Diabetes Mellitus tipo 1 complicada com retinopatia e nefropatia ⢠TFG 13 mL/min/1.73m² ⢠HbA1c 11,5% ⢠HAS, DLP, Obesidade; ⢠Medicamentos em uso crônico: AAS, atenolol, anlodipino, monocordil, hidralazina, furosemida, Insulina NPH ⢠Apresenta-se com angina CCS III há 6 meses, motivo pelo qual foi submetida à cinecoronariografia em Dezembro/2021. ⢠Por manter angina limitante, à despeito do tratamento medicamentoso, foi encaminhada para intervenção coronária percutânea, em caráter eletivo.
Assuntos
Humanos , Feminino , Adulto , Intervenção Coronária Percutânea , Nefropatias , Atenolol , Anlodipino , Diabetes Mellitus Tipo 1 , Furosemida , Hidralazina , Hipertensão , ObesidadeRESUMO
BACKGROUND: Children and adolescents undergoing kidney transplantation may present oral conditions after the procedure, but a few studies have recently described them. AIM: To describe the oral conditions of post-renal transplant children and adolescents. DESIGN: Two calibrated dentists examined all the participants by assessing caries experience, enamel defects, periodontal condition and soft tissue lesions. RESULTS: A total of 120 participants were included in the study, in which 63 (52.5%) were male and 57 (47.5%) were female, with a mean age of 12.78 ± 3.9 years. Among the participants, 104 (86.7%) showed at least one oral change directly related to kidney disease. The most frequent oral findings were enamel defect (49/120; 40.8%) and drug-induced gingival overgrowth (DIGO) (20/120; 16.7%). Gingival bleeding was observed on probing in 115 (95.8%) participants, whereas 69 (57.5%) presented dental calculus and 51 (42.5%) had caries experience. CONCLUSION: Gingival bleeding, enamel defects and DIGO were the most frequent oral findings in kidney transplant children and adolescents. The use of amlodipine and anticonvulsants was associated with DIGO, and there was a positive correlation between oral ulcers and use of everolimus.
Assuntos
Cárie Dentária , Crescimento Excessivo da Gengiva , Transplante de Rim , Doenças Dentárias , Adolescente , Anlodipino/efeitos adversos , Anticonvulsivantes/efeitos adversos , Criança , Everolimo/efeitos adversos , Feminino , Crescimento Excessivo da Gengiva/induzido quimicamente , Crescimento Excessivo da Gengiva/patologia , Humanos , Transplante de Rim/efeitos adversos , Masculino , Saúde BucalAssuntos
Humanos , Masculino , Feminino , Pessoa de Meia-Idade , Pressão Sanguínea/efeitos dos fármacos , Bisoprolol/administração & dosagem , Anlodipino/administração & dosagem , Quimioterapia Combinada , Irbesartana/administração & dosagem , Hipertensão/tratamento farmacológico , Indapamida/administração & dosagem , Anti-Hipertensivos/administração & dosagem , Austrália , Ensaios Clínicos Controlados Aleatórios como Assunto , Resultado do TratamentoRESUMO
La intoxicación por bloqueantes de los canales de calcio es un cuadro poco frecuente en la población pediátrica. Los signos y síntomas pueden progresar de forma rápida y llevar al colapso cardiovascular y muerte. El sostén hemodinámico con inotrópicos y vasopresores no suele ser efectivo. La terapia con insulina y glucosa es un complemento eficaz del tratamiento inicial, que está ampliamente estudiado, y se utiliza en diferentes patologías con compromiso hemodinámico. Se presenta el caso de una paciente pediátrica con antecedente de ingestión de dosis altas de amlodipina con fines suicidas, con descompensación hemodinámica refractaria al tratamiento de soporte inotrópico habitual. A partir del tratamiento con insulina y glucosa, se logró la estabilidad hemodinámica, con evolución favorable de la paciente.
Calcium channel blocker poisoning is a rare condition in the pediatric population. Signs and symptoms can be rapidly progressive and lead to cardiovascular collapse and death. Hemodynamic support with inotropics and vasopressors is usually not effective. The insulin/glucose therapy is an effective complement to the initial treatment, which is widely studied and used in different pathologies with hemodynamic compromise. The case of a pediatric patient with a history of high-dose ingestion of amlodipine for suicidal purposes, with hemodynamic decompensation refractory to usual inotropic support treatment, is presented. From the insulin/glucose treatment, hemodynamic stability was achieved with a favorable evolution
Assuntos
Humanos , Feminino , Adolescente , Tentativa de Suicídio , Bloqueadores dos Canais de Cálcio/intoxicação , Anlodipino/intoxicação , Overdose de Drogas/terapia , Glucose/uso terapêutico , Insulina/uso terapêuticoRESUMO
Calcium channel blocker poisoning is a rare condition in the pediatric population. Signs and symptoms can be rapidly progressive and lead to cardiovascular collapse and death. Hemodynamic support with inotropics and vasopressors is usually not effective. The insulin/glucose therapy is an effective complement to the initial treatment, which is widely studied and used in different pathologies with hemodynamic compromise. The case of a pediatric patient with a history of highdose ingestion of amlodipine for suicidal purposes, with hemodynamic decompensation refractory to usual inotropic support treatment, is presented. From the insulin/glucose treatment, hemodynamic stability was achieved with a favorable evolution.
La intoxicación por bloqueantes de los canales de calcio es un cuadro poco frecuente en la población pediátrica. Los signos y síntomas pueden progresar de forma rápida y llevar al colapso cardiovascular y muerte. El sostén hemodinámico con inotrópicos y vasopresores no suele ser efectivo. La terapia con insulina y glucosa es un complemento eficaz del tratamiento inicial, que está ampliamente estudiado, y se utiliza en diferentes patologías con compromiso hemodinámico. Se presenta el caso de una paciente pediátrica con antecedente de ingestión de dosis altas de amlodipina con fines suicidas, con descompensación hemodinámica refractaria al tratamiento de soporte inotrópico habitual. A partir del tratamiento con insulina y glucosa, se logró la estabilidad hemodinámica, con evolución favorable de la paciente.
Assuntos
Anlodipino/intoxicação , Bloqueadores dos Canais de Cálcio/intoxicação , Overdose de Drogas , Glucose/uso terapêutico , Insulina/uso terapêutico , Suicídio , Criança , Overdose de Drogas/terapia , HumanosRESUMO
Background: Primary hyperlipidemia is a condition that affects some specific breeds. It has been previously describedin Miniature Shnauzer, Beagles, Shetland Shepdog and West Highland White Terrier. There are no reports of primaryhyperlipidemia in Maltese dogs. It is a hereditary disorder of lipoprotein metabolism. The etiology is unknown and maybe related to a genetic problem in lipoprotein lipase or to the absence of apaprotein CII. Clinical signs include spontaneousarterosclerosis, retinal lipemia, cutaneous xanthomas, abdominal pain, lethargy, vomiting and / or diarrhea. Neurologicalmanifestations such as seizures and behavioral changes may also occur. The aim of this report is to describe a case ofreactive seizures due to hyperlipidemia in a dog.Case: A 5-year-old male Maltese dog was admitted with a history of seizures. Hypertension and abdominal distensionwith large amounts of intestinal gases were found in general physical examination. Neurological examination revealedimpaired nasal septum sensory perception, which was slightly bilaterally reduced, and pain on cervical palpation and inthe brachial plexus region. Based on history and clinical examination, it was possible to locate the lesion in the thalamocortical region and to suspect idiopathic epilepsy, reactive seizures, and symptomatic epilepsy due to meningoencephalitisof unknown origin. The diagnosis of primary hyperlipidemia was made by exclusion with the aid of laboratory tests andultrasound. After the establishment of a fat restriction diet, bezafibrate, phenobarbital, and omega-3 supplementation, theanimal improved significantly with the reduction of epileptic seizures.Discussion: The initial clinical suspicion was hyperadrenocorticism as the primary cause of hyperlipidemia. This suspicion was based on the presence of polyphagia, polydipsia, polyuria and abdominal distension, together with laboratory...(AU)