Colesevelam
Fuentes regulatorias consultadas
Indicaciones aprobadas
- Complemento de la dieta en adultos con hipercolesterolemia primaria: con estatina para una reducción adicional de C-LDL, en monoterapia cuando la estatina no es apropiada o no se tolera, o con ezetimiba con o sin estatina.
Contraindicaciones
Absolutas
- Hipersensibilidad al colesevelam o a los excipientes.
- Antecedente de obstrucción intestinal (FDA); obstrucción intestinal o biliar (CIMA).
- Triglicéridos séricos superiores a 500 mg/dl (contraindicación FDA).
- Antecedente de pancreatitis inducida por hipertrigliceridemia (contraindicación FDA).
Advertencias clínicas
- Advertencia mayor · Puede aumentar los triglicéridos; usar con precaución si superan 3,4 mmol/l y vigilarlos regularmente. — https://cima.aemps.es/cima/dochtml/ft/03268004/FT_03268004.html
- Advertencia mayor · Puede causar o empeorar estreñimiento; valorar especialmente el riesgo en cardiopatía coronaria o angina. Usar con precaución en disfagia, trastornos de motilidad gastrointestinal, enfermedad inflamatoria intestinal, insuficiencia hepática o cirugía digestiva mayor. — https://cima.aemps.es/cima/dochtml/ft/03268004/FT_03268004.html
- Advertencia mayor · Vigilar estrechamente ciclosporina y anticoagulación con warfarina; los cambios al iniciar o suspender colesevelam pueden alterar sus efectos. — https://cima.aemps.es/cima/dochtml/ft/03268004/FT_03268004.html
- Advertencia mayor · Puede reducir la absorción de las vitaminas liposolubles A, D, E y K; los suplementos orales de estas vitaminas deben administrarse al menos 4 horas antes del colesevelam. Extremar la precaución en pacientes con malabsorción y vigilar el INR con warfarina, especialmente al iniciar o suspender colesevelam. — https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5d1b8dfd-cfe7-4c86-9d7b-a709b593acf7
Interacciones medicamentosas
- ModeradaCiclosporina, fenitoína, hormonas tiroideas, anticonceptivos con etinilestradiol y noretindrona, olmesartán y sulfonilureas
Mecanismo: Colesevelam puede reducir la exposición a ciclosporina, fenitoína, levotiroxina u otras hormonas tiroideas, etinilestradiol y noretindrona, olmesartán y las sulfonilureas glimepirida, glipizida y glibenclamida.
Recomendación: Administrar estos medicamentos al menos 4 horas antes del colesevelam; monitorizar niveles o respuesta clínica cuando corresponda.
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5d1b8dfd-cfe7-4c86-9d7b-a709b593acf7
- ModeradaWarfarinaB01AA03
Mecanismo: Colesevelam puede disminuir la exposición a warfarina; se han notificado reducciones del INR durante el tratamiento concomitante.
Recomendación: Administrar warfarina al menos 4 horas antes del colesevelam y monitorizar el INR con frecuencia al iniciar colesevelam y después periódicamente.
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5d1b8dfd-cfe7-4c86-9d7b-a709b593acf7
- ModeradaMedicamentos orales no estudiados o con margen terapéutico estrecho
Mecanismo: La unión gastrointestinal por colesevelam puede reducir la biodisponibilidad de un medicamento oral cuando la interacción no se ha estudiado o no puede excluirse.
Recomendación: FDA: considerar administrarlo al menos 4 horas antes del colesevelam. CIMA: si no puede excluirse una interacción, administrarlo al menos 4 horas antes o 4 horas después. Esta separación no se aplica a metformina de liberación prolongada, que requiere monitorización glucémica según su entrada específica.
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5d1b8dfd-cfe7-4c86-9d7b-a709b593acf7https://cima.aemps.es/cima/dochtml/ft/03268004/FT_03268004.html
- ModeradaMetformina de liberación prolongada
Mecanismo: La administración conjunta aumenta la exposición a metformina.
Recomendación: Vigilar la respuesta glucémica habitual al tratamiento antidiabético y ajustar según valoración clínica.
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5d1b8dfd-cfe7-4c86-9d7b-a709b593acf7
Eventos adversos
Comunes (≥1%)
Flatulencia · Estreñimiento · Cefalea · Vómitos · Diarrea · Dispepsia · Dolor o distensión abdominal · Náuseas · Aumento de triglicéridos
Raros pero graves
Pancreatitis · Obstrucción intestinal
Embarazo y lactancia
Usar con precaución durante el embarazo y la lactancia; no se ha establecido la seguridad en estas poblaciones.
Bibliografía reciente (PubMed)
Bile acid diarrhea is a common cause of bowel symptoms and often goes unrecognized or misdiagnosed. Many aspects of management remain contentious. The primary, idiopathic condition should be suspected in people with functional diarrhea or diarrhea-predominant irritable bowel syndrome. Secondary causes include ileal resection, inflammation, and post-cholecystectomy. Diagnostic tests vary globally, being unavailable in many countries, and further refinement of testing strategy is needed. Management is usually long-term symptom control, rather than reversal of the causative factors, which are still being defined. Bile acid sequestrants remain the main drugs used. They are relatively inexpensive, and better-quality data is now available for colesevelam. However, optimal use, including timing and formulation, needs clarification. The GLP-1 receptor agonist, liraglutide, is also effective, although mechanisms of action and whether this effect is common to other class members is unclear. They are more expensive, and availability varies. FXR agonists can also be effective but require further validation. The role of dietary factors in symptom development is a major patient concern, needing more formal studies. To build on recent findings, bile acid diarrhea needs further investment into causes, diagnosis and therapy to guide present and future patient care. The condition known as bile acid diarrhea (BAD) causes frequent loose stools, which need to be passed urgently, sometimes causing incontinence. It can be a complication of surgery or other intestinal disorders, and gives similar symptoms to IBS. It is not widely known and clinicians often fail to diagnose it. In this article, we review recent publications about how to make the diagnosis of BAD. Some of these are contentious and there may be limited availability of the tests or poor accuracy. We then review current treatments and how to best manage BAD. There are some new treatments, which are not yet fully proven or accep
Low anterior resection syndrome (LARS) is a series of bowel dysfunction symptoms, including altered bowel frequency, irregular bowel rhythms, fecal incontinence, and constipation. LARS occurs in 80% of patients undergoing sphincter-preserving surgery, affecting patients' quality of life along with social avoidance. Different measurements and treatments have been raised to deal with LARS, but no systematic standard has been developed. To promote the standardization of clinical trials and clinical management of LARS, this review summarizes the latest findings up until 2023 regarding the diagnostic criteria, assessment protocols, and treatment modalities for postoperative LARS in rectal cancer. The diagnostic criteria for LARS need to be updated to the definition proposed by the LARS International Collaborative Group, replacing the current application of the LARS score. In both clinical trials and clinical treatment, the severity of LARS should be assessed using at least one symptom assessment questionnaire, the LARS score or MSKCC BFI, and at least one scale related to quality of life. Anorectal manometry, fecoflowmetry, endoscopic ultrasonography, and pelvic floor muscle strength testing are recommended to be adopted only in clinical trials. After analysis of the latest literature on LARS treatment, a stepwise classification model is established for the standardized clinical management of LARS. Patients with minor LARS can start with first-line treatment, including management of self-behavior with an emphasis on diet modification and medication. Lamosetron, colesevelam hydrochloride, and loperamide are common antidiarrheal agents. Second-line management indicates multi-mode pelvic floor rehabilitation and transanal irrigation. Patients with major LARS should select single or several treatments in second-line management. Refractory LARS can choose antegrade enema, neuromodulation, or colostomy. In clinical trials of LARS treatment between 2020 and 2022, the eligibilit
The aim of this paper is to raise awareness of MC as a clinically significant condition and to highlight its under-recognition, risk factors, diagnosis, management, and complications. This paper underlines the diagnostic and therapeutic challenges associated with the often nonspecific symptoms of MC. In order to create this article, we reviewed available articles found in the PubMed database and searched for articles using the Google Scholar platform. Microscopic colitis (MC) is a chronic inflammatory bowel disease, classified into three types: lymphocytic, collagenous, and unspecified. The average age of onset of MC is around 62-65 years and the disease is more common in women than men (nine times more common). The main symptom of MC is watery diarrhoea without blood, other symptoms include defecatory urgency, faecal incontinence, abdominal pain, nocturnal bowel movements, and weight loss. Once considered a rare disease, MC is now being diagnosed with increasing frequency, but diagnosis remains difficult. To date, a number of causative factors for MC have been identified, including smoking, alcohol consumption, medications (including NSAIDs, PPIs, SSRIs, and ICPIs), genetic factors, autoimmune diseases, bile acid malabsorption, obesity, appendicitis, and intestinal dysbiosis. It may be difficult to recognize and should be differentiated from inflammatory bowel diseases (Crohn's disease and ulcerative colitis), irritable bowel syndrome (IBS), coeliac disease, infectious bowel disease, and others. Diagnosis involves biopsy at colonoscopy and histopathological evaluation of the samples. Treatment consists of budesonide oral (the gold standard) or enema. Alternatives include bile acid sequestrants (cholestyramine, colesevelam, and colestipol), biologics (infliximab, adalimumab, and vedolizumab), thiopurines, methotrexate, and rarely, surgery.