Colesevelam
Sources réglementaires consultées
Indications approuvées
- Complément au régime chez l'adulte atteint d'hypercholestérolémie primaire : avec une statine pour une réduction supplémentaire du LDL-C, en monothérapie lorsqu'une statine est inappropriée ou mal tolérée, ou avec l'ézétimibe avec ou sans statine.
Contre-indications
Absolues
- Hypersensibilité au colésévélam ou aux excipients.
- Antécédent d’obstruction intestinale (FDA) ; obstruction intestinale ou biliaire (CIMA).
- Triglycérides sériques supérieurs à 500 mg/dl (contre-indication FDA).
- Antécédent de pancréatite induite par une hypertriglycéridémie (contre-indication FDA).
Mises en garde cliniques
- Mise en garde majeure · Les triglycérides peuvent augmenter ; utiliser avec prudence s'ils dépassent 3,4 mmol/l et les surveiller régulièrement. — https://cima.aemps.es/cima/dochtml/ft/03268004/FT_03268004.html
- Mise en garde majeure · Il peut provoquer ou aggraver la constipation ; évaluer particulièrement le risque en cas de cardiopathie coronaire ou d'angor. Utiliser avec prudence en cas de dysphagie, troubles de la motilité digestive, maladie inflammatoire intestinale, insuffisance hépatique ou chirurgie digestive majeure. — https://cima.aemps.es/cima/dochtml/ft/03268004/FT_03268004.html
- Mise en garde majeure · Surveiller étroitement la ciclosporine et l'anticoagulation par warfarine ; les changements lors de l'instauration ou de l'arrêt du colésévélam peuvent modifier leurs effets. — https://cima.aemps.es/cima/dochtml/ft/03268004/FT_03268004.html
- Mise en garde majeure · Il peut réduire l’absorption des vitamines liposolubles A, D, E et K ; les suppléments oraux de ces vitamines doivent être administrés au moins 4 heures avant le colésévélam. Une prudence particulière s’impose chez les patients présentant une malabsorption et l’INR doit être surveillé avec la warfarine, notamment lors de l’instauration ou de l’arrêt du colésévélam. — https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5d1b8dfd-cfe7-4c86-9d7b-a709b593acf7
Interactions médicamenteuses
- ModéréeCiclosporine, phénytoïne, hormones thyroïdiennes, contraceptifs contenant de l’éthinylestradiol et de la noréthindrone, olmésartan et sulfamides hypoglycémiants
Mécanisme: Le colésévélam peut réduire l’exposition à la ciclosporine, à la phénytoïne, à la lévothyroxine ou à d’autres hormones thyroïdiennes, à l’éthinylestradiol et à la noréthindrone, à l’olmésartan ainsi qu’aux sulfamides hypoglycémiants glimépiride, glipizide et glibenclamide.
Recommandation: Administrer ces médicaments au moins 4 heures avant le colésévélam ; surveiller les concentrations ou la réponse clinique, le cas échéant.
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5d1b8dfd-cfe7-4c86-9d7b-a709b593acf7
- ModéréeWarfarineB01AA03
Mécanisme: Le colésévélam peut diminuer l’exposition à la warfarine ; des diminutions de l’INR ont été rapportées pendant le traitement concomitant.
Recommandation: Administrer la warfarine au moins 4 heures avant le colésévélam et surveiller fréquemment l’INR lors de l’instauration du colésévélam, puis périodiquement.
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5d1b8dfd-cfe7-4c86-9d7b-a709b593acf7
- ModéréeMédicaments oraux non étudiés ou à marge thérapeutique étroite
Mécanisme: La fixation gastro-intestinale par le colésévélam peut réduire la biodisponibilité d’un médicament oral lorsque l’interaction n’a pas été étudiée ou ne peut être exclue.
Recommandation: FDA : envisager de l’administrer au moins 4 heures avant le colésévélam. CIMA : si une interaction ne peut être exclue, l’administrer au moins 4 heures avant ou 4 heures après. Cet espacement ne s’applique pas à la metformine à libération prolongée, qui nécessite une surveillance glycémique selon son entrée spécifique.
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5d1b8dfd-cfe7-4c86-9d7b-a709b593acf7https://cima.aemps.es/cima/dochtml/ft/03268004/FT_03268004.html
- ModéréeMetformine à libération prolongée
Mécanisme: L'administration concomitante augmente l'exposition à la metformine.
Recommandation: Surveiller la réponse glycémique habituelle au traitement antidiabétique et adapter selon l'évaluation clinique.
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5d1b8dfd-cfe7-4c86-9d7b-a709b593acf7
Effets indésirables
Communs (≥1%)
Flatulences · Constipation · Céphalées · Vomissements · Diarrhée · Dyspepsie · Douleur ou distension abdominale · Nausées · Augmentation des triglycérides
Rares mais graves
Pancréatite · Obstruction intestinale
Grossesse et allaitement
Utiliser avec prudence pendant la grossesse et l'allaitement ; la sécurité n'est pas établie dans ces populations.
Bibliographie récente (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.