RESUMEN
Aspergillus niger causes infections such as otitis and pulmonary aspergillosis in immunocompromised individuals. Treatment involves voriconazole or amphotericin B, and due to the increase in fungal resistance, the search for new compounds with antifungal activity has intensified. In the development of new drugs, cytotoxicity and genotoxicity assays are important, as they allow predicting possible damage that a molecule can cause, and in silico studies predict the pharmacokinetic properties. The aim of this study was to verify the antifungal activity and the mechanism of action of the synthetic amide 2-chloro-N-phenylacetamide against Aspergillus niger strains and toxicity. 2-Chloro-N-phenylacetamide showed antifungal activity against different strains of Aspergillus niger with minimum inhibitory concentrations between 32 and 256 µg/mL and minimum fungicides between 64 and 1024 µg/mL. The minimum inhibitory concentration of 2-chloro-N-phenylacetamide also inhibited conidia germination. When associated with amphotericin B or voriconazole, 2-chloro-N-phenylacetamide had antagonistic effects. Interaction with ergosterol in the plasma membrane is the probable mechanism of action.2-Chloro-N-phenylacetamide has favorable physicochemical parameters, good oral bioavailability and absorption in the gastrointestinal tract, crosses the blood-brain barrier and inhibits CYP1A2. At concentrations of 50 to 500 µg/mL, it has little hemolytic effect and a protective effect for type A and O red blood cells, and in the cells of the oral mucosa it promotes little genotoxic change. It is concluded that 2-chloro-N-phenylacetamide has promising antifungal potential, favorable pharmacokinetic profile for oral administration and low cytotoxic and genotoxic potential, being a promising candidate for in vivo toxicity studies.
Asunto(s)
Antifúngicos , Aspergilosis , Aspergillus , Humanos , Antifúngicos/toxicidad , Anfotericina B/toxicidad , Voriconazol/toxicidad , Voriconazol/uso terapéutico , Aspergilosis/tratamiento farmacológico , Aspergilosis/microbiología , Acetanilidas/uso terapéutico , Pruebas de Sensibilidad MicrobianaRESUMEN
OBJECTIVE: To compare the use of mirabegron with anticholinergics drugs for the treatment of overactive bladder (OB). DATA SOURCE: Systematic searches were conducted in EMBASE, PUBMED, Cochrane, and LILACS databases from inception to September 2021. We included RCTs, women with clinically proven OB symptoms, studies that compared mirabegron to antimuscarinic drugs, and that evaluated the efficacy, safety or adherence. DATA COLLECTION: RevMan 5.4 was used to combine results across studies. We derived risk ratios (RRs) and mean differences with 95% CIs using a random-effects meta-analytic model. Cochrane Collaboration Tool and GRADE was applied for risk of bias and quality of the evidence. DATA SYNTHESIS: We included 14 studies with a total of 10,774 patients. Fewer total adverse events was reported in mirabegron group than in antimuscarinics group [RR 0.93 (0.89-0.98)]. The risk of gastrointestinal tract disorders and dry mouth were lower with mirabegron [RR 0,58 (0.48-0.68); 9375 patients; RR 0.44 (0.35-0.56), 9375 patients, respectively]. No difference was reported between mirabegron and antimuscarinics drugs for efficacy. The adherence to treatment was 87.7% in both groups [RR 0.99 (0.98-1.00)]. CONCLUSION: Mirabegron and antimuscarinics have comparable efficacy and adherence rates; however, mirabegron showed fewer total and isolated adverse events.
OBJETIVO: Comparar o uso de mirabegrom com anticolinérgicos para o tratamento da bexiga hiperativa (BH). FONTE DE DADOS: Buscas sistemáticas foram realizadas nas bases de dados EMBASE, PUBMED, Cochrane e LILACS desde o início até setembro de 2021. Incluímos ECR, mulheres com sintomas de BH clinicamente comprovados, estudos que compararam mirabegrom a medicamentos antimuscarínicos e avaliaram a eficácia, segurança ou adesão. COLETA DE DADOS: RevMan 5.4 foi usado para combinar os resultados entre os estudos. Derivamos razões de risco (RRs) e diferenças médias com intervalo de confiança (IC) de 95% usando um modelo meta-analítico de efeitos aleatórios. Cochrane Collaboration Tool e GRADE foi aplicado para risco de viés e qualidade da evidência. SíNTESE DOS DADOS: Foram incluídos 14 estudos com um total de 10.774 pacientes. Menos eventos adversos totais foram relatados no grupo mirabegrom do que no grupo antimuscarínicos [RR: 0,93 (0,890,98)]. O risco de distúrbios do trato gastrointestinal e boca seca foram menores com mirabegrom [RR: 0,58 (0,480,68); 9.375 pacientes; RR: 0,44 (0,350,56), 9.375 pacientes, respectivamente]. Nenhuma diferença foi relatada entre mirabegrom e drogas antimuscarínicos para eficácia. A adesão ao tratamento foi de 87,7% em ambos os grupos [RR: 0,99 (0,981,00)]. CONCLUSãO: Mirabegrom e antimuscarínicos têm eficácia e taxas de adesão comparáveis, porém o mirabegrom apresentou menos eventos adversos totais e isolados.
Asunto(s)
Antagonistas Colinérgicos , Vejiga Urinaria Hiperactiva , Humanos , Femenino , Antagonistas Colinérgicos/uso terapéutico , Antagonistas Muscarínicos/uso terapéutico , Vejiga Urinaria Hiperactiva/tratamiento farmacológico , Vejiga Urinaria Hiperactiva/inducido químicamente , Acetanilidas/uso terapéutico , Resultado del TratamientoRESUMEN
OBJECTIVES: The Brazilian public health system does not cover pharmacotherapy for urge urinary incontinence (UUI). The aim of this study was to estimate the cost-effectiveness and budget impact of providing tolterodine, solifenacin, oxybutynin (OXY), darifenacin, and mirabegron for the treatment of UUI in Brazilian public health system. METHODS: A cost-effectiveness analysis with budget impact was performed. Six scenarios were assessed: in one scenario, all 5 therapeutic alternatives approved for coverage, and in the remaining 5 scenarios, only 1 alternative is approved for adoption for all patients. Clinical data were derived from a rapid systematic review conducted in several databases. One-way sensitivity analysis was also performed. The time horizon was 12 months. RESULTS: The cost-effectiveness analysis showed that patients treated with OXY had the lowest incremental cost-effectiveness ratio (ICER) per outcomes assessed (change in urinary incontinence episodes (UIE): R$1180.08; change in urge incontinence episodes: R$757.85 and change in micturition frequency: R$907.75), corresponding to a budget impact of R$17.9 billion over 5 years. The change in effectiveness measures was the parameter that most influenced the results of the ICER per patient-year. CONCLUSION: The results of the study have shown that OXY and solifenacin had the lowest ICER per patient-year and the lowest budget impact when compared with other drugs.
Asunto(s)
Acetanilidas/economía , Antagonistas Muscarínicos/economía , Salud Pública/tendencias , Tiazoles/economía , Incontinencia Urinaria de Urgencia/tratamiento farmacológico , Acetanilidas/uso terapéutico , Adulto , Brasil , Análisis Costo-Beneficio/métodos , Análisis Costo-Beneficio/estadística & datos numéricos , Femenino , Humanos , Masculino , Persona de Mediana Edad , Antagonistas Muscarínicos/uso terapéutico , Salud Pública/economía , Salud Pública/estadística & datos numéricos , Tiazoles/uso terapéutico , Incontinencia Urinaria de Urgencia/economía , Agentes Urológicos/economía , Agentes Urológicos/uso terapéuticoRESUMEN
Central neuropathic pain is a common untreated symptom in progressive multiple sclerosis (PMS) and is associated with poor quality of life and interference with patients' daily activities. The neuroinflammation process and mitochondrial dysfunction in the PMS lesions generate reactive species. The transient potential receptor ankyrin 1 (TRPA1) has been identified as one of the major mechanisms that contribute to neuropathic pain signaling and can be activated by reactive compounds. Thus, the goal of our study was to evaluate the role of spinal TRPA1 in the central neuropathic pain observed in a PMS model in mice. We used C57BL/6 female mice (20-30 g), and the PMS model was induced by the experimental autoimmune encephalomyelitis (EAE) using mouse myelin oligodendrocyte glycoprotein (MOG35-55) antigen and CFA (complete Freund's adjuvant). Mice developed progressive clinical score, with motor impairment observed after 15 days of induction. This model induced mechanical and cold allodynia and heat hyperalgesia which were measured up to 14 days after induction. The hypersensitivity observed was reduced by the administration of selective TRPA1 antagonists (HC-030031 and A-967079, via intrathecal and intragastric), antioxidants (α-lipoic acid and apocynin, via intrathecal and intragastric), and TRPA1 antisense oligonucleotide (via intrathecal). We also observed an increase in TRPA1 mRNA levels, NADPH oxidase activity, and 4-hydroxinonenal (a TRPA1 agonist) levels in spinal cord samples of PMS-EAE induced animals. In conclusion, these results support the hypothesis of the TRPA1 receptor involvement in nociception observed in a PMS-EAE model in mice.
Asunto(s)
Encefalomielitis Autoinmune Experimental/complicaciones , Hiperalgesia/fisiopatología , Proteínas del Tejido Nervioso/fisiología , Neuralgia/fisiopatología , Nocicepción/fisiología , Médula Espinal/fisiopatología , Canal Catiónico TRPA1/fisiología , Acetanilidas/farmacología , Acetanilidas/uso terapéutico , Acetofenonas/farmacología , Analgésicos/farmacología , Analgésicos/uso terapéutico , Animales , Antipirina/análogos & derivados , Antipirina/farmacología , Antipirina/uso terapéutico , Dipirona/farmacología , Dipirona/uso terapéutico , Encefalomielitis Autoinmune Experimental/fisiopatología , Femenino , Hiperalgesia/tratamiento farmacológico , Hiperalgesia/etiología , Ratones , Ratones Endogámicos C57BL , Glicoproteína Mielina-Oligodendrócito/inmunología , Glicoproteína Mielina-Oligodendrócito/toxicidad , NADPH Oxidasas/antagonistas & inhibidores , Proteínas del Tejido Nervioso/biosíntesis , Proteínas del Tejido Nervioso/genética , Neuralgia/tratamiento farmacológico , Neuralgia/etiología , Nocicepción/efectos de los fármacos , Oligonucleótidos Antisentido/farmacología , Estrés Oxidativo , Oximas/farmacología , Oximas/uso terapéutico , Fragmentos de Péptidos/inmunología , Fragmentos de Péptidos/toxicidad , Pregabalina/farmacología , Pregabalina/uso terapéutico , Purinas/farmacología , Purinas/uso terapéutico , Canal Catiónico TRPA1/antagonistas & inhibidores , Canal Catiónico TRPA1/biosíntesis , Canal Catiónico TRPA1/genética , Ácido Tióctico/farmacología , Regulación hacia Arriba/efectos de los fármacosRESUMEN
Breast carcinoma causes severe pain, which decreases the quality of life of patients. Current treatments produce adverse effects and have limited efficacy. Transient potential receptor ankyrin 1 (TRPA1) is related to the onset of cancer and neuropathic pain. The aim of this study was to evaluate the involvement of TRPA1 in a model of breast carcinoma. We injected 4T1 cells in the fourth caudal mammary fat pad of female BALB/c mice, and after 20 days we observed mechanical and cold allodynia and spontaneous nociception behavior (mouse grimace scale detection, MGS). TRPA1 selective antagonist (HC-030031 or A-967079) administration or intrathecal administration of TRPA1 antisense (AS) oligonucleotide was performed. The activity of NADPH oxidase, superoxide dismutase (SOD) and hydrogen peroxide (H2O2) levels were evaluated. The chemical hyperalgesia produced by a TRPA1 agonist (allyl isothiocyanate, AITC) was also detected. The administration of TRPA1 antagonists, TRPA1 AS, or antioxidant, transiently attenuated MGS, or mechanical and cold allodynia. Intraplantar injection of AITC also caused nociception. NADPH oxidase or SOD activity and H2O2 levels were increased in the sciatic nerve and hind paw skin samples. The 4T1 cells did not express TRPA1, and the use of HC-030031 or α-lipoic acid did not reduce the cytotoxic effect of a chemotherapeutic drug (paclitaxel). Thus, TRPA1 could be investigated as a target for breast carcinoma pain treatment.
Asunto(s)
Dolor en Cáncer , Neoplasias Mamarias Experimentales , Canal Catiónico TRPA1 , Acetanilidas/farmacología , Acetanilidas/uso terapéutico , Analgésicos/uso terapéutico , Animales , Antineoplásicos Fitogénicos/farmacología , Dolor en Cáncer/tratamiento farmacológico , Dolor en Cáncer/etiología , Dolor en Cáncer/genética , Dolor en Cáncer/metabolismo , Línea Celular Tumoral , Femenino , Peróxido de Hidrógeno/metabolismo , Hiperalgesia/tratamiento farmacológico , Neoplasias Mamarias Experimentales/complicaciones , Neoplasias Mamarias Experimentales/tratamiento farmacológico , Neoplasias Mamarias Experimentales/genética , Neoplasias Mamarias Experimentales/metabolismo , Ratones Endogámicos BALB C , NADPH Oxidasas/metabolismo , Nocicepción/efectos de los fármacos , Oximas/uso terapéutico , Paclitaxel/farmacología , Purinas/farmacología , Purinas/uso terapéutico , Nervio Ciático/efectos de los fármacos , Nervio Ciático/metabolismo , Piel/metabolismo , Superóxido Dismutasa/metabolismo , Canal Catiónico TRPA1/antagonistas & inhibidores , Canal Catiónico TRPA1/genética , Ácido Tióctico/uso terapéuticoRESUMEN
ABSTRACT Purpose To evaluate the efficacy and tolerability of mirabegron in females with overactive bladder (OAB) symptoms after surgical treatment for stress urinary incontinence (SUI). Materials and Methods The study was conducted with a prospective, randomized and double-blinded design. 62 patients over the age of 40 who met the inclusion-exclusion criterias of the study were enrolled and randomly divided into two groups as Group A (mirabegron 50mg) and B (solifenacin 5mg). Patients were compared based on efficacy of treatment [Patient Perception of Bladder Condition (PPBC) scale and micturition diaries], safety of treatment (heart rate, systolic and diastolic blood pressure, adverse events), number of micturitions per day, patient's satisfaction status after treatment [Visual Analog Scale(VAS)] and quality of life. Results The mean age of the population was 48.2±3.8 years and the duration of OAB symptoms was 5.9±2.9 months. Baseline values for the mean number of micturitions, volume voided in each micturition, nocturia episodes, urgency and urgency incontinence episodes were 15.3±0.34, 128±3.88mL, 3.96±1.67, 5.72±1.35 and 4.22±0.69, respectively. After treatment, values for these parameters were 11.7±0.29, 164.7±2.9mL, 2.25±0.6, 3.38±0.71, 2.31±0.49 respectively. Quality of life score, symptom bother score, VAS for treatment satisfaction score, PPBC score after treatment were 66.1±0.85, 43.7±0.77, 4.78±0.14, 4.78±0.14, respectively. There were no significant differences between two groups on any parameter. However, mirabegron showed better tolerability than solifenacin, particularly after 6 months. Conclusion Mirabegron is safe, effective and tolerable in the long-term treatment of females with OAB symptoms after surgery for stress urinary incontinence.
Asunto(s)
Humanos , Femenino , Adulto , Tiazoles/uso terapéutico , Incontinencia Urinaria de Esfuerzo/cirugía , Vejiga Urinaria Hiperactiva/tratamiento farmacológico , Agonistas de Receptores Adrenérgicos beta 3/uso terapéutico , Acetanilidas/uso terapéutico , Calidad de Vida , Valores de Referencia , Incontinencia Urinaria de Esfuerzo/fisiopatología , Método Doble Ciego , Estudios Prospectivos , Reproducibilidad de los Resultados , Resultado del Tratamiento , Antagonistas Muscarínicos/uso terapéutico , Vejiga Urinaria Hiperactiva/fisiopatología , Escala Visual Analógica , Succinato de Solifenacina/uso terapéutico , Persona de Mediana EdadRESUMEN
PURPOSE: To evaluate the efficacy and tolerability of mirabegron in females with overactive bladder (OAB) symptoms after surgical treatment for stress urinary incontinence (SUI). MATERIALS AND METHODS: The study was conducted with a prospective, randomized and double-blinded design. 62 patients over the age of 40 who met the inclusion-exclusion criterias of the study were enrolled and randomly divided into two groups as Group A (mirabegron 50mg) and B (solifenacin 5mg). Patients were compared based on efficacy of treatment [Patient Perception of Bladder Condition (PPBC) scale and micturition diaries], safety of treatment (heart rate, systolic and diastolic blood pressure, adverse events), number of micturitions per day, patient's satisfaction status after treatment [Visual Analog Scale(VAS)] and quality of life. RESULTS: The mean age of the population was 48.2±3.8 years and the duration of OAB symptoms was 5.9±2.9 months. Baseline values for the mean number of micturitions, volume voided in each micturition, nocturia episodes, urgency and urgency incontinence episodes were 15.3±0.34, 128±3.88mL, 3.96±1.67, 5.72±1.35 and 4.22±0.69, respectively. After treatment, values for these parameters were 11.7±0.29, 164.7±2.9mL, 2.25±0.6, 3.38±0.71, 2.31±0.49 respectively. Quality of life score, symptom bother score, VAS for treatment satisfaction score, PPBC score after treatment were 66.1±0.85, 43.7±0.77, 4.78±0.14, 4.78±0.14, respectively. There were no significant differences between two groups on any parameter. However, mirabegron showed better tolerability than solifenacin, particularly after 6 months. CONCLUSION: Mirabegron is safe, effective and tolerable in the long-term treatment of females with OAB symptoms after surgery for stress urinary incontinence.
Asunto(s)
Acetanilidas/uso terapéutico , Agonistas de Receptores Adrenérgicos beta 3/uso terapéutico , Tiazoles/uso terapéutico , Vejiga Urinaria Hiperactiva/tratamiento farmacológico , Incontinencia Urinaria de Esfuerzo/cirugía , Adulto , Método Doble Ciego , Femenino , Humanos , Persona de Mediana Edad , Antagonistas Muscarínicos/uso terapéutico , Estudios Prospectivos , Calidad de Vida , Valores de Referencia , Reproducibilidad de los Resultados , Succinato de Solifenacina/uso terapéutico , Resultado del Tratamiento , Vejiga Urinaria Hiperactiva/fisiopatología , Incontinencia Urinaria de Esfuerzo/fisiopatología , Escala Visual AnalógicaRESUMEN
AIMS: To evaluate the effects of the beta-3 adrenoceptor agonist, mirabegron in a mouse model of detrusor overactivity induced by obesity. METHODS: C57BL/6 male mice were fed with standard chow or high-fat diet for 12 weeks. Lean and obese mice were treated orally with mirabegron (10 mg/kg/day) from the last 2 weeks of diet. Cystometric evaluations, functional assays, protein expression for phosphodiesterase type 4 (PDE4), and cyclic adenosine monophosphate (cAMP) measurement were carried out. RESULTS: In obese mice the body weight, epididymal fat mass, fasting glucose, and low-density lipoprotein (LDL) levels were higher (P < 0.001) than in the lean mice. A reduction of 34% and 54% and an increase of 35% in the epididimal fat, LDL, and HDL levels (P < 0.05), respectively, were observed in the obese group treated with mirabegron, whereas no changes were seen in the lipid profile from lean mice. Obese group showed irregular micturition pattern, characterized by significant increases in frequency and non-void contractions. Carbachol, potassium chloride, and electrical-field stimulation induced detrusor smooth muscle (DSM) contractions, which were greater in bladders from obese mice than from lean mice. Two-week treatment with mirabegron restored all the contractile response alterations in the DSM. Basal intracellular levels of cAMP were reduced (68%), whereas PDE4 protein expression was increased (54%) in bladder from obese mice. Mirabegron restored the cAMP levels in obese bladder, without changing the PDE4 expression. CONCLUSION: Mirabegron was able to completely restore the urinary alterations seen in the bladder from obese mice.
Asunto(s)
Acetanilidas/uso terapéutico , Agonistas de Receptores Adrenérgicos beta 3/uso terapéutico , AMP Cíclico/metabolismo , Músculo Liso/efectos de los fármacos , Obesidad/fisiopatología , Tiazoles/uso terapéutico , Vejiga Urinaria Hiperactiva/tratamiento farmacológico , Acetanilidas/farmacología , Agonistas de Receptores Adrenérgicos beta 3/farmacología , Animales , Peso Corporal/efectos de los fármacos , Carbacol/farmacología , Fosfodiesterasas de Nucleótidos Cíclicos Tipo 4/metabolismo , Masculino , Ratones , Ratones Endogámicos C57BL , Ratones Obesos , Contracción Muscular/efectos de los fármacos , Músculo Liso/metabolismo , Músculo Liso/fisiopatología , Obesidad/metabolismo , Tiazoles/farmacología , Vejiga Urinaria/efectos de los fármacos , Vejiga Urinaria/metabolismo , Vejiga Urinaria/fisiopatología , Vejiga Urinaria Hiperactiva/metabolismo , Vejiga Urinaria Hiperactiva/fisiopatología , Micción/efectos de los fármacosRESUMEN
The aim of this study was to investigate the involvement of the transient receptor potential ankyrin 1 (TRPA1) in haemorrhagic cystitis, the main side effect of cyclophosphamide-based chemotherapy. Hannover female rats received intraperitoneal (i.p.) injection of cyclophosphamide (three doses of 100 mg/kg, every other day, in a total of five days). This treatment was followed by the treatment with TRPA1 antagonist HC 030031 (50 mg/kg, p.o.). The threshold for hindpaw withdrawal or abdominal retraction to von Frey Hair and the locomotor activity were measured. The treatment with the TRPA1 antagonist HC 030031 significantly decreased mechanical hyperalgesia induced by cyclophosphamide without interfere with locomotor activity. Urodynamic parameters were performed by cystometry 24 h after a single treatment with cyclophosphamide (200 mg/kg, i.p.) in control and HC 030031 treated rats. Analyses of the urodynamic parameters showed that a single dose of cyclophosphamide was enough to significantly increase the number and amplitude of non-voiding contractions and to decrease the voided volume and voiding efficiency, without significantly altering basal, threshold or maximum pressure. The treatment with HC 030031 either before (100 mg/kg, p.o.) or after (30 mg/kg, i.v.) cyclophosphamide inhibited the non-voiding contractions but failed to counteract the loss in voiding efficiency. Our data demonstrates that nociceptive symptoms and urinary bladder overactivity caused by cyclophosphamide, in part, are dependent upon the activation of TRPA1. In this context, the antagonism of the receptor may be an alternative to minimise the urotoxic symptoms caused by this chemotherapeutic agent.
Asunto(s)
Ciclofosfamida/efectos adversos , Cistitis/inducido químicamente , Cistitis/complicaciones , Hemorragia/complicaciones , Hiperalgesia/tratamiento farmacológico , Canales Catiónicos TRPC/antagonistas & inhibidores , Vejiga Urinaria Hiperactiva/tratamiento farmacológico , Acetanilidas/farmacología , Acetanilidas/uso terapéutico , Animales , Antineoplásicos Alquilantes/efectos adversos , Cistitis/metabolismo , Cistitis/fisiopatología , Femenino , Hiperalgesia/complicaciones , Purinas/farmacología , Purinas/uso terapéutico , Ratas , Canal Catiónico TRPA1 , Vejiga Urinaria Hiperactiva/complicaciones , Urodinámica/efectos de los fármacosRESUMEN
The effectiveness of drug therapy in controlling angina and the resulting improvement in exercise capacity were reviewed. We performed a Medline search of published reports on ranolazine, trimetazidine, and other medicines that act metabolically. Quality of life with regards to work capacity alone was analyzed. Most reports were about trimetazidine, with strong evidence of its efficacy and tolerability. Its effect on episodes of angina, total exercise time, and time to the onset of ischemia on ECG is impressive with no negative effects found on double product (workload) and improvement in quality of life. The second most evaluated drug was ranolazine, particularly regarding quality of life. Results are similar to those with trimetazidine but are not as significant for quality of life issues. For the other drugs, L-carnitine, ribose, and dichloroacetate, accumulated experimental data provide a physiological background in which clinical trials have been started, but as yet very few patients have been enrolled. Also, studies that intended to evaluate, by echocardiography, ischemic dysfunction induced by dobutamine-atropine stress were examined; these also showed a reduction in ischemia and fewer anginal episodes, but only with trimetazidine in this regard. Taken together, these drug effects are important to ameliorate quality of life. The issue of quality of life was evaluated in specific reports, and the results of the application of validated questionnaires (SF36, 5-dimensional EuroQol Instrument, and Seattle Angina Questionnaire) attest to the positive drug effects on patients' perception of wellness, particularly with the use of trimetazidine, and less with ranolazine.
Asunto(s)
Angina de Pecho/tratamiento farmacológico , Enfermedad de la Arteria Coronaria/tratamiento farmacológico , Vasodilatadores/uso terapéutico , Acetanilidas/farmacología , Acetanilidas/uso terapéutico , Angina de Pecho/metabolismo , Animales , Carnitina/farmacología , Carnitina/uso terapéutico , Ensayos Clínicos como Asunto , Enfermedad de la Arteria Coronaria/metabolismo , Ácido Dicloroacético/farmacología , Ácido Dicloroacético/uso terapéutico , Humanos , Piperazinas/farmacología , Piperazinas/uso terapéutico , Calidad de Vida , Ranolazina , Ribosa/farmacología , Ribosa/uso terapéutico , Encuestas y Cuestionarios , Trimetazidina/farmacología , Trimetazidina/uso terapéutico , Vasodilatadores/farmacologíaRESUMEN
Agina pectoris is a discomfort in the chest or adjacent areas caused by myocardial ischemia. It is most commonly caused by the inability of narrowed atherosclerotic coronary arteries to supply adequate oxygen to the heart under conditions of increase demand. This review article will focus in the medical treatment of chronic stable angina, with a focus in new strategies or medications. Treatment by revascularization techniques will not be discussed in this article. The goal of treatment is to improve quality of life, decrease cardiovascular events and mortality. All patients should be evaluated for reversible causes of their angina, such as anemia, hyperthyroidism, sympathomimetic drugs and hypertension. Sublingual nitroglycerin should be used for immediate relief of symptoms. In general, all patients should be on aspirin (ASA) unless they are allergic or other contraindications, if so; clopidogrel should be added to the therapy. In addition to the antiplatelet therapy, which decreases mortality, patients should be started on beta blockers and nitrates. If there is no improvement in symptoms then a calcium channel blockers of the dihydropyridine family should be added. Patients with Diabetes Mellitus and/or left ventricular systolic dysfunction should be also started on angiotensin converting enzyme inhibitors. If the patient continues with limiting angina, ranolazine should be started and finally enhanced external counterpulsation should be considered in those patients who have not responded to maximal drug therapy.