Cholestagel

For patients who require cholesterol lowering but cannot tolerate a statin, or who need additional LDL reduction alongside existing treatment, a non-statin approach to lipid management can be a clinically appropriate option. Cholestagel tablets are a prescription-only bile acid sequestrant used in adults for LDL reduction as an adjunct to a statin or as monotherapy when a statin is not appropriate. Colesevelam, the active ingredient, works entirely within the digestive system without being absorbed into the body, making it a useful option in specific patient groups. A prescription can only be issued following a clinical consultation.

Cholestagel is a branded oral prescription medicine. The active ingredient is colesevelam hydrochloride. Colesevelam belongs to the bile acid sequestrant class of lipid-lowering medicines, also known as anion exchange resins or bile acid binding resins. It is the most recently developed medicine in this class and has a different formulation to older bile acid sequestrants such as colestyramine and colestipol, which were available as powders requiring mixing with water. Cholestagel is available as film coated tablets, which many patients find more convenient.

Cholestagel is licensed in the UK for two indications. The first is as primary adjunctive therapy with diet and exercise for reduction of elevated LDL cholesterol in adults with primary hypercholesterolaemia, either as monotherapy or in combination with an HMG-CoA reductase inhibitor (statin). The second is as adjunctive therapy to diet and exercise in combination with a statin for the treatment of mixed hyperlipidaemia in adults. Cholestagel may be particularly useful when statins alone have not achieved adequate LDL reduction, or as a statin alternative in patients who cannot tolerate statin medicines.

Cholestagel is available in a single tablet strength of 625 mg. The daily dose is typically three to six tablets per day divided across meals. Because Cholestagel can affect the absorption of other medicines taken at the same time, careful attention to the timing of other medicines in relation to Cholestagel is an important part of using it safely.

Cholestagel lowers LDL cholesterol through a mechanism that is entirely local within the digestive system. It is not absorbed into the bloodstream.

Bile Acid Sequestration. The liver produces bile acids from cholesterol and secretes them into the small intestine to help with the digestion and absorption of dietary fats. Under normal circumstances, the majority of bile acids are reabsorbed from the small intestine and returned to the liver for re use (enterohepatic circulation). Colesevelam works by binding to bile acids in the small intestine, preventing their reabsorption. The bound bile acids are excreted in the faeces instead of being returned to the liver.

Upregulation of LDL Receptors. When less bile acid returns to the liver, the liver increases its conversion of cholesterol into new bile acids to replace the excreted supply. This increased demand for cholesterol within the liver leads to upregulation of LDL receptors on liver cell surfaces. More LDL receptors mean the liver captures more LDL cholesterol from the bloodstream, reducing circulating LDL levels. The net result is a fall in plasma LDL cholesterol.

Because colesevelam acts entirely within the gut and is not absorbed, it does not cause the systemic side effects associated with statins such as muscle problems or liver enzyme changes. It does not raise triglyceride levels to the same extent as older bile acid sequestrants. However, it has a significant potential to reduce the absorption of many other medicines taken concurrently, which is the most important practical consideration when using Cholestagel alongside other treatments.

Always take Cholestagel exactly as your prescriber instructs. Read the Patient Information Leaflet supplied with your medicine before starting treatment.

• Cholestagel must be taken with meals. Do not take it on an empty stomach.
• The usual dose is three tablets taken twice daily with meals (six tablets per day total), or six tablets taken once daily with a meal.
• Swallow the tablets whole with a glass of water. Do not crush or chew the tablets.
• Other medicines should be taken at least four hours before Cholestagel, as it can bind to many other medicines in the gut and reduce their absorption.

If you miss a dose, take it as soon as you remember with your next meal. If you only remember after finishing that meal, skip the missed dose and take your next scheduled dose as normal with the following meal. Do not take two doses at once. Do not stop taking Cholestagel without speaking to your prescriber first.

Your prescriber will arrange blood tests to check your lipid levels before and after starting treatment.

Cholestagel 625 mg film-coated tablets are the only strength available. The standard daily dose is six tablets per day, which may be divided across two meals as three tablets twice daily, or taken all together as six tablets once daily with the main meal of the day. The once daily schedule requires taking six tablets at one time, which some patients find less convenient than the divided twice daily approach.

The maximum recommended daily dose is six tablets (3,750 mg colesevelam hydrochloride per day). All dose decisions and schedules are determined by your prescriber. Do not change your dose without medical advice.

The side effects of Cholestagel are mostly gastrointestinal and reflect its mechanism of action within the gut. Because it is not absorbed, it does not cause the systemic side effects associated with statins.

Common Side Effects (may affect up to 1 in 10 people):

• Constipation — the most commonly reported side effect. Maintaining adequate fluid intake and dietary fibre helps. Contact your prescriber if constipation is severe or persistent.
• Nausea and dyspepsia (indigestion or stomach discomfort).
• Abdominal pain or bloating.
• Diarrhoea.

Uncommon Side Effects (may affect up to 1 in 100 people):

• Raised triglyceride levels, monitored during treatment. Cholestagel is not suitable for patients with severely raised triglyceride levels.
• Dysphagia (difficulty swallowing) or oesophageal discomfort — take the tablets with adequate water.
• Fatigue.

Serious Side Effects — Seek Urgent Medical Attention: Go to your nearest accident and emergency department or call 999 immediately if you experience signs of bowel obstruction such as severe abdominal pain, vomiting, and inability to pass stools, or signs of a severe allergic reaction such as sudden widespread rash, difficulty breathing, or swelling of the face, lips, tongue, or throat.

Cholestagel tablets may be suitable if you:

• Are an adult with primary hypercholesterolaemia or mixed hyperlipidaemia and require LDL reduction.
• Are taking a statin and have not achieved adequate LDL control, and your prescriber has determined that adding Cholestagel is appropriate.
• Cannot tolerate a statin and require a statin alternative for cholesterol lowering as monotherapy.
• Are already prescribed Cholestagel and require a repeat prescription through an online prescribing service.

Cholestagel tablets are not suitable if you:

• Have severe triglyceride elevation (above 4.5 mmol/L).
• Have a history of bowel obstruction or severe gastrointestinal motility problems.
• Have phenylketonuria — some formulations contain phenylalanine.
• Have dysphagia or oesophageal disorders that would make swallowing the tablets problematic.
• Are pregnant. Cholestagel may impair absorption of fat soluble vitamins (A, D, E, K) and folic acid, important in pregnancy.
• Are breastfeeding.
• Are under 18 years of age.
• Have a known allergy or hypersensitivity to colesevelam hydrochloride or any excipient.

Important Drug Interactions — Timing of Other Medicines: All other oral medicines should be taken at least four hours before Cholestagel. This applies to statins, thyroid medicines such as levothyroxine, ciclosporin, oral contraceptives and other hormonal medicines, fat-soluble vitamins (A, D, E, K), folic acid, and warfarin and other anticoagulants. Discuss the correct timing with your prescriber and pharmacist before starting Cholestagel.

Cholestagel is a Prescription Only Medicine. The clinical consultation is the essential first step. A prescription will only be issued if a registered prescriber concludes, based on their individual assessment of your circumstances, that Cholestagel is clinically appropriate for you.

During your online consultation with Pharmacy Planet, a registered prescriber will review your lipid levels, triglyceride levels, current medicines, medical history, and reason for seeking Cholestagel. The prescriber will confirm whether Cholestagel is appropriate, whether it should be used alongside a statin or as a statin alternative, and whether online prescribing is suitable for your situation.

The interactions between Cholestagel and other oral medicines require particularly careful assessment of your full medicines list. The prescriber will advise on how to time your other medicines in relation to Cholestagel to minimise the risk of reduced absorption.

Not all consultations will result in a prescription. The prescriber may request blood test results, recommend a different approach to lipid management, or advise that a more detailed review by your GP is needed before prescribing proceeds.