Kolestyramin Alternova
Bile Acid Sequestrant for High Cholesterol, Pruritus and Bile Acid Diarrhoea
Quick Facts About Kolestyramin Alternova
Key Takeaways About Kolestyramin Alternova
- Non-absorbed cholesterol-lowering agent: Cholestyramine works entirely within the gut by binding bile acids, forcing the liver to convert more cholesterol into bile acids, thereby reducing blood cholesterol by 15–30%
- Always mix with liquid before drinking: The powder must be dissolved in at least 150 ml of water, juice, or another beverage and consumed immediately – never swallow the dry powder
- Drug interaction alert: Take all other medications at least 1 hour before or 4–6 hours after cholestyramine to prevent reduced absorption
- Gradual dose increase recommended: Start with half a dose sachet daily for the first week and increase gradually to minimise constipation and gastrointestinal side effects
- Long-term vitamin monitoring required: Prolonged use may reduce absorption of fat-soluble vitamins (A, D, E, K) – your doctor may prescribe supplements
What Is Kolestyramin Alternova and What Is It Used For?
Kolestyramin Alternova is a bile acid sequestrant containing cholestyramine. It is used to lower elevated blood cholesterol levels when dietary measures alone have not been sufficient, to relieve itching (pruritus) caused by partial bile duct obstruction, and to treat diarrhoea caused by excess bile acids in the intestine.
Cholestyramine belongs to a group of medicines known as bile acid sequestrants or bile acid binding resins. It is a large, non-absorbable anion exchange resin that works entirely within the gastrointestinal tract. When taken orally, cholestyramine binds to bile acids in the small intestine, forming an insoluble complex that cannot be reabsorbed and is instead excreted in the faeces. This interruption of the normal enterohepatic circulation of bile acids has several important therapeutic consequences.
In high cholesterol (hypercholesterolaemia), the binding of bile acids by cholestyramine forces the liver to divert more cholesterol towards the synthesis of new bile acids to replace those lost. This increased conversion of cholesterol to bile acids upregulates the expression of low-density lipoprotein (LDL) receptors on liver cells, which in turn increases the clearance of LDL cholesterol from the bloodstream. Clinical studies have demonstrated that cholestyramine can reduce LDL cholesterol by approximately 15–30% when used at therapeutic doses, depending on the dose and individual patient factors. The Lipid Research Clinics Coronary Primary Prevention Trial (LRC-CPPT), a landmark randomised controlled trial, demonstrated that cholestyramine therapy reduced the incidence of coronary heart disease by 19% over an average follow-up of 7.4 years.
In patients with pruritus (itching) caused by partial bile duct obstruction, bile acids accumulate in the bloodstream and are deposited in the skin, causing intense itching. By binding these bile acids in the intestine and promoting their faecal excretion, cholestyramine reduces the circulating levels of bile acids and provides significant relief from pruritus. This indication is particularly relevant in conditions such as primary biliary cholangitis (formerly primary biliary cirrhosis) and intrahepatic cholestasis of pregnancy.
Cholestyramine is also effective for bile acid diarrhoea, a condition in which excessive bile acids reach the colon and stimulate water and electrolyte secretion, leading to chronic watery diarrhoea. This can occur after ileal resection, in Crohn's disease affecting the ileum, after cholecystectomy (gallbladder removal), or as idiopathic bile acid malabsorption. By capturing bile acids in the small intestine before they reach the colon, cholestyramine reduces the secretory stimulus and alleviates the diarrhoea.
Cholestyramine has been used in clinical practice since the 1960s and has one of the longest safety records of any cholesterol-lowering medication. While newer drugs such as statins have largely replaced bile acid sequestrants as first-line therapy for hypercholesterolaemia, cholestyramine remains an important option for patients who cannot tolerate statins, as an add-on therapy for patients who require additional LDL reduction, and for its non-lipid indications such as pruritus and bile acid diarrhoea.
What Should You Know Before Taking Kolestyramin Alternova?
Before starting Kolestyramin Alternova, inform your doctor about all your medical conditions, especially inflammatory bowel disease, chronic constipation, and any other medications you are taking. This product contains aspartame and is contraindicated in phenylketonuria (PKU).
Contraindications
You should not take Kolestyramin Alternova if any of the following apply to you:
- Allergy to cholestyramine or any other ingredient in this product – if you have previously experienced an allergic reaction to cholestyramine or any bile acid sequestrant, do not use this medicine
- Complete biliary obstruction – if your bile ducts are completely blocked, cholestyramine will not be effective as there are no bile acids reaching the intestine to bind
- Phenylketonuria (PKU) – Kolestyramin Alternova contains aspartame (E951), which is a source of phenylalanine. Patients with PKU, a rare inherited metabolic disorder, must avoid phenylalanine as it accumulates to harmful levels in their bodies
Warnings and Precautions
Talk to your doctor, pharmacist, or nurse before using Kolestyramin Alternova if you have or have had any of the following:
- Inflammatory bowel disease (Crohn's disease or ulcerative colitis) – cholestyramine may worsen symptoms in some patients, and careful monitoring is required
- Chronic constipation or haemorrhoids – constipation is the most common side effect of cholestyramine and can aggravate these conditions. Your doctor may recommend a lower starting dose, increased fluid and fibre intake, or a stool softener
- Swallowing difficulties (dysphagia) – the powder must always be mixed with liquid before swallowing. Taking dry powder could cause choking or oesophageal obstruction
- Fat-soluble vitamin deficiency – long-term use of cholestyramine can reduce the absorption of vitamins A, D, E, and K. Your doctor may monitor your vitamin levels and prescribe supplements if necessary. Vitamin K deficiency can lead to increased bleeding tendency
- Kidney disease – chronic use of cholestyramine in patients with renal impairment may cause hyperchloraemic acidosis, particularly in children
Pregnancy and Breastfeeding
If you are pregnant, think you may be pregnant, planning to become pregnant, or breastfeeding, talk to your doctor or pharmacist before using this medicine.
Pregnancy: Experience with cholestyramine use during pregnancy is limited. Because cholestyramine is not absorbed from the gastrointestinal tract, direct exposure of the foetus to the drug is not expected. However, cholestyramine can reduce the absorption of fat-soluble vitamins and certain nutrients, which are critically important during pregnancy. Your doctor will carefully weigh the benefits against the potential risks and may prescribe vitamin supplements if treatment is deemed necessary.
Breastfeeding: Cholestyramine is not absorbed into the bloodstream and therefore does not pass into breast milk. However, the potential reduction in fat-soluble vitamin absorption in the mother could theoretically affect the nutritional quality of breast milk. If you are breastfeeding, discuss the benefits and risks with your doctor.
Driving and Operating Machinery
You are responsible for assessing whether you are fit to drive or operate machinery while taking this medicine. Cholestyramine is not known to directly impair cognitive function or motor skills, as it is not absorbed systemically. However, some side effects such as dizziness or fatigue have been reported. If you experience any symptoms that could affect your ability to drive safely, refrain from driving and consult your doctor.
Important Information About Ingredients
Aspartame (E951): Each dose sachet of Kolestyramin Alternova contains 30 mg of aspartame, which is a source of phenylalanine. This product must not be used by patients with phenylketonuria (PKU). For patients without PKU, the amount of phenylalanine per dose is very low and not considered harmful.
Propylene glycol (E1520): Each dose sachet contains 32.49 mg of propylene glycol. If your child is younger than 4 weeks old, consult your doctor or pharmacist before giving this medicine, especially if the child is also taking other medicines containing propylene glycol or alcohol.
How Does Kolestyramin Alternova Interact with Other Drugs?
Cholestyramine can significantly reduce the absorption of many other medications because it binds substances in the intestine. Always take other medicines at least 1 hour before or 4–6 hours after your cholestyramine dose. Never take cholestyramine at the same time as other oral medications without first consulting your doctor.
Because cholestyramine is a powerful adsorbent that binds many different substances in the gastrointestinal tract, it has one of the broadest drug interaction profiles of any medicine. The primary mechanism is reduced absorption of co-administered oral drugs, as cholestyramine can bind them in the intestine and prevent them from entering the bloodstream. This is why it is critically important to maintain a time gap between taking cholestyramine and any other oral medication.
The general rule is to take all other oral medicines at least 1 hour before or 4–6 hours after your cholestyramine dose. However, for certain drugs with narrow therapeutic windows (such as warfarin, digoxin, and levothyroxine), even greater vigilance may be required, including more frequent blood monitoring.
Major Interactions
| Drug | Category | Effect | Recommendation |
|---|---|---|---|
| Warfarin / Phenprocoumone | Anticoagulant (blood thinner) | Cholestyramine significantly reduces warfarin absorption, potentially leading to inadequate anticoagulation and increased thrombotic risk | Take warfarin 1 hour before or 4–6 hours after cholestyramine. Monitor INR closely |
| Levothyroxine | Thyroid hormone | Markedly reduced absorption of levothyroxine, leading to potential hypothyroidism | Take levothyroxine at least 4 hours before cholestyramine. Monitor TSH regularly |
| Digoxin / Digitoxin | Cardiac glycoside | Reduced absorption and enterohepatic recycling of digoxin, potentially reducing its therapeutic effect | Take digoxin 1–2 hours before cholestyramine. Monitor digoxin levels |
| Mycophenolic acid / Leflunomide | Immunosuppressant | Cholestyramine significantly reduces mycophenolate levels by interrupting enterohepatic circulation | Avoid combination if possible. If unavoidable, monitor drug levels closely |
| Ursodeoxycholic acid (UDCA) | Bile acid therapy | Cholestyramine binds UDCA in the intestine, completely negating its therapeutic effect | Avoid combination – these drugs have opposing mechanisms of action |
Moderate Interactions
| Drug | Category | Effect | Recommendation |
|---|---|---|---|
| Amiodarone | Antiarrhythmic | Reduced absorption of amiodarone, potentially reducing antiarrhythmic efficacy | Take amiodarone at least 1 hour before cholestyramine |
| Methotrexate | Immunosuppressant / Anti-inflammatory | Reduced absorption and interrupted enterohepatic circulation of methotrexate | Separate administration by at least 4 hours. Monitor drug response |
| Diclofenac / Meloxicam / Piroxicam | NSAIDs (pain relief) | Reduced absorption and efficacy of NSAIDs | Take NSAIDs 1 hour before or 4–6 hours after cholestyramine |
| Furosemide | Loop diuretic | Reduced absorption of furosemide, potentially diminishing its diuretic effect | Take furosemide at least 1 hour before cholestyramine |
| Raloxifene | Selective oestrogen receptor modulator | Approximately 60% reduction in raloxifene absorption | Avoid concurrent administration. Separate doses by at least 6 hours |
| Pravastatin / Fluvastatin / Ezetimibe | Lipid-lowering agents | Reduced absorption of these drugs when given simultaneously | Take statins/ezetimibe 1 hour before or 4–6 hours after cholestyramine |
| Valproate | Anticonvulsant / Mood stabiliser | Reduced valproate absorption potentially leading to seizure breakthrough | Separate doses by at least 3 hours. Monitor valproate levels |
| Ethinylestradiol | Hormonal contraceptive | Reduced absorption of oral contraceptive, potentially reducing efficacy | Take oral contraceptives 1 hour before or 4–6 hours after cholestyramine. Consider additional contraceptive measures |
| Tetracycline / Penicillin | Antibiotics | Reduced antibiotic absorption and potentially inadequate antimicrobial levels | Take antibiotics at least 1 hour before cholestyramine |
The single most important thing to remember when taking cholestyramine alongside other medicines is to never take them at the same time. Always maintain a gap of at least 1 hour before or 4–6 hours after your cholestyramine dose. If in doubt about the timing of a specific medication, always ask your doctor or pharmacist.
What Is the Correct Dosage of Kolestyramin Alternova?
The recommended adult dose is 1–2 sachets (4–8 g) taken 2–3 times daily. It is important to start with a low dose and increase gradually over several weeks to reduce the risk of gastrointestinal side effects, particularly constipation.
Always take this medicine exactly as your doctor or pharmacist has told you. Do not change your dose without consulting your doctor first. The powder must always be mixed with liquid before swallowing – never attempt to swallow the dry powder.
Adults
High Cholesterol (Hypercholesterolaemia)
Usual dose: 1–2 dose sachets (4–8 g cholestyramine) taken 2–3 times daily
Maximum dose: 6 sachets (24 g) per day
The cholesterol-lowering effect typically becomes apparent within 1–2 weeks and reaches its maximum after 4–6 weeks of continued use. The dose-response relationship is not linear; most of the cholesterol reduction occurs at lower doses, with diminishing additional benefit at higher doses.
Pruritus (Itching from Bile Duct Obstruction)
Usual dose: 1–2 dose sachets (4–8 g) taken 2–3 times daily
The antipruritic effect is usually noticeable within 1–2 weeks of starting treatment. The dose should be adjusted according to the severity of the itching and the patient's tolerance of side effects.
Bile Acid Diarrhoea
Usual dose: 1 dose sachet (4 g) taken 1–3 times daily
For bile acid diarrhoea, lower doses are often sufficient. Many patients achieve good symptom control with 1–2 sachets per day. The dose should be titrated to the minimum effective dose that controls symptoms.
Gradual Dose Increase (Important)
To minimise gastrointestinal side effects, particularly constipation and bloating, it is strongly recommended to start with a low dose and increase gradually:
- Week 1: Half a dose sachet (2 g) once daily
- Week 2: One dose sachet (4 g) once daily
- Week 3: One dose sachet (4 g) twice daily
- Week 4 and onwards: Increase to the full prescribed dose as tolerated
Children
The dose for children is determined by the prescribing doctor and is individually adjusted based on the child's weight, age, and the condition being treated. Cholestyramine can be used in children for certain conditions, but the dose is typically lower than in adults and requires careful medical supervision. Special attention should be paid to the risk of hyperchloraemic acidosis and fat-soluble vitamin deficiency in paediatric patients.
Elderly Patients
No specific dose adjustment is required in elderly patients based on age alone. However, elderly patients may be more susceptible to constipation and should start with a low dose. Adequate fluid intake and dietary fibre should be ensured. If constipation becomes problematic, a stool softener may be recommended by your doctor.
How to Prepare and Take the Powder
Proper preparation of cholestyramine powder is essential for safe and effective use:
- Empty the contents of the dose sachet into a glass
- Add at least 150 ml (half a glass) of water, fruit juice, or another non-carbonated beverage
- Stir well until the powder is completely suspended – it will not dissolve but should form a smooth suspension
- Drink the suspension immediately
- Rinse the glass with a small amount of liquid and drink this as well to ensure the full dose is taken
- Discard any remaining undissolved powder
It is helpful to vary the type of beverage used to prevent taste fatigue. The powder can also be mixed into thin soups or pureed fruit such as applesauce or crushed pineapple. Do not mix with carbonated beverages as excessive foaming may occur.
Missed Dose
If you forget to take a dose, simply skip it and take your next dose at the usual time. Do not take a double dose to make up for the missed one. If you forget doses frequently, consider setting a daily alarm or taking your cholestyramine at the same times each day in relation to meals.
Overdose
Because cholestyramine is not absorbed from the gastrointestinal tract, overdose is unlikely to cause systemic toxicity. However, taking an excessive amount may cause severe constipation, abdominal pain, bloating, and in extreme cases intestinal obstruction. If you or someone else has taken a very large amount of cholestyramine, or if a child has accidentally ingested this medicine, contact your doctor, hospital, or poison control centre for advice.
What Are the Side Effects of Kolestyramin Alternova?
The most common side effects of cholestyramine are gastrointestinal, particularly constipation, bloating, flatulence, nausea, and abdominal discomfort. Most side effects are dose-dependent and can be minimised by starting with a low dose and increasing gradually.
Like all medicines, cholestyramine can cause side effects, although not everybody gets them. Because cholestyramine is not absorbed from the gastrointestinal tract, most side effects are confined to the digestive system. The following side effects have been reported (frequency not always known from available data):
- Signs of intestinal obstruction: severe abdominal pain, inability to pass gas or stool, vomiting
- Unusual bleeding or bruising (may indicate vitamin K deficiency)
- Night blindness or visual changes (may indicate vitamin A deficiency)
- Signs of severe allergic reaction: skin rash, itching, swelling of face or throat, difficulty breathing
Very Common (Gastrointestinal)
The most frequently reported side effects
- Constipation (most common, especially at higher doses)
- Abdominal discomfort and bloating
- Flatulence (gas)
- Nausea
Common (Gastrointestinal and Nutritional)
Reported in a notable number of patients
- Heartburn and acid reflux
- Diarrhoea (paradoxically, in some patients)
- Vomiting
- Loss of appetite
- Steatorrhoea (fatty stools)
- Decreased absorption of fat-soluble vitamins (A, D, E, K)
- Decreased folate levels (particularly in children)
Uncommon (Various Body Systems)
Reported less frequently
- Headache, dizziness
- Inflammation of the tongue (glossitis)
- Difficulty swallowing (dysphagia)
- Pancreatitis (inflammation of the pancreas)
- Gallstones and gallbladder pain
- Skin rash, irritation, and urticaria (hives)
- Dental erosion and dental caries
- Increased bleeding tendency (vitamin K deficiency)
Rare (Serious or Unusual)
Reported in isolated cases
- Night blindness (vitamin A deficiency)
- Osteoporosis (vitamin D deficiency with prolonged use)
- Hyperchloraemic acidosis (elevated chloride in blood, especially in children and patients with renal impairment)
- Anaemia (reduced protein or folate levels)
- Intestinal obstruction
- Rectal bleeding and haemorrhoidal bleeding
- Increased or decreased libido
- Fatigue, oedema (swelling)
- Weight gain or weight loss
- Tinnitus (ringing in the ears)
- Asthma or wheezing
- Uveitis (eye inflammation)
- Joint pain (arthralgia) and back pain
- Blood in urine, difficulty urinating
Managing Common Side Effects
Constipation: This is the most common complaint. To minimise constipation, start with a low dose and increase gradually, drink plenty of water (at least 2 litres per day), eat a high-fibre diet, and exercise regularly. Your doctor may recommend a stool softener if constipation persists despite these measures.
Bloating and flatulence: These are usually worst during the first few weeks of treatment and tend to improve as your body adjusts. Starting with a low dose and increasing gradually helps reduce these effects.
Vitamin deficiency: Long-term use of cholestyramine can reduce the absorption of fat-soluble vitamins A, D, E, and K. Your doctor should monitor your vitamin levels periodically, especially if you are taking cholestyramine for more than a few months. Supplementation may be prescribed as a preventive measure.
How Should You Store Kolestyramin Alternova?
Store Kolestyramin Alternova at room temperature with no special storage conditions required. Keep the medicine out of sight and reach of children. Do not use after the expiry date printed on the carton and dose sachets.
There are no special storage requirements for Kolestyramin Alternova. Store the dose sachets at room temperature in their original packaging. Protect from excessive moisture. Do not use this medicine after the expiry date which is stated on the carton and on the dose sachets after "EXP." The expiry date refers to the last day of that month.
Once a dose sachet is opened, the powder should be used immediately. Do not save opened sachets for later use. If any powder remains after preparation of your dose, discard it.
Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. These measures will help protect the environment.
What Does Kolestyramin Alternova Contain?
Each dose sachet contains 4 g of cholestyramine as the active ingredient, along with orange flavouring, aspartame (E951), propylene glycol alginate, and other excipients. The product is a white to off-white powder with an orange flavour.
Active Ingredient
The active substance is cholestyramine 4 g per dose sachet. Cholestyramine is a quaternary ammonium anion exchange resin – a large polymer that is not absorbed from the gastrointestinal tract. Its large molecular weight and ionic structure mean that it remains entirely within the gut lumen, where it binds bile acids through ionic exchange.
Other Ingredients (Excipients)
- Orange flavouring: maltodextrin, acacia gum (E414), natural flavouring agents, butylated hydroxyanisole (E320)
- Propylene glycol alginate (E1520)
- Xanthan gum (E415)
- Aspartame (E951) – contains a source of phenylalanine; 30 mg per dose sachet
- Anhydrous citric acid (E330)
- Colloidal anhydrous silica
Appearance and Packaging
Kolestyramin Alternova is a white to off-white powder with an orange scent and flavour. It is supplied in dose sachets consisting of paper, polyethylene, aluminium, and polyethylene layers. Each carton contains 50 or 56 dose sachets.
Frequently Asked Questions About Kolestyramin Alternova
Kolestyramin Alternova (cholestyramine) is used for three main conditions: (1) lowering elevated blood cholesterol levels when dietary measures alone are not sufficient, (2) relieving itching (pruritus) caused by partial bile duct obstruction, and (3) treating diarrhoea caused by excess bile acids in the intestine. It works by binding bile acids in the small intestine and preventing their reabsorption, which forces the liver to convert more cholesterol into bile acids.
Empty the dose sachet into a glass and add at least 150 ml (half a glass) of water, fruit juice, or another non-carbonated beverage. Stir well until a smooth suspension forms. Drink it immediately. You can also mix the powder into thin soups or pureed fruit such as applesauce. Never swallow the dry powder, as this could cause choking or oesophageal blockage. It helps to vary the beverages you use to prevent taste fatigue.
Cholestyramine is a powerful adsorbent that binds many substances in the intestine, not just bile acids. If you take other medicines at the same time, cholestyramine may bind them and significantly reduce their absorption, making them less effective or even ineffective. To avoid this, take all other oral medicines at least 1 hour before or 4–6 hours after your cholestyramine dose. This is especially critical for blood thinners (warfarin), thyroid hormones (levothyroxine), heart medicines (digoxin), and oral contraceptives.
Constipation is the most common side effect of cholestyramine. To manage it, start with a low dose (half a sachet daily) and increase gradually over several weeks. Drink at least 2 litres of water daily, eat a high-fibre diet rich in fruits, vegetables, and whole grains, and stay physically active. If constipation persists despite these measures, talk to your doctor – they may recommend a stool softener such as lactulose or macrogol, or adjust your cholestyramine dose.
Yes, Kolestyramin Alternova contains 30 mg of aspartame (E951) per dose sachet. Aspartame is a sweetener that is a source of phenylalanine. This means the product must not be used by patients with phenylketonuria (PKU), a rare inherited metabolic disorder where phenylalanine cannot be properly processed by the body. If you have PKU, inform your doctor so they can prescribe an alternative treatment.
Yes, cholestyramine is commonly used to treat bile acid diarrhoea that may develop after cholecystectomy (gallbladder removal). After the gallbladder is removed, bile is continuously secreted into the small intestine rather than being stored and released in response to meals. In some patients, excess bile acids reach the colon and cause chronic watery diarrhoea. Cholestyramine binds these bile acids and can provide effective relief. Typically a lower dose (1–2 sachets per day) is sufficient for this indication.
References
- Lipid Research Clinics Program. The Lipid Research Clinics Coronary Primary Prevention Trial Results: I. Reduction in Incidence of Coronary Heart Disease. JAMA. 1984;251(3):351–364. doi:10.1001/jama.1984.03340270029025
- Mach F, Baigent C, Catapano AL, et al. 2019 ESC/EAS Guidelines for the Management of Dyslipidaemias. European Heart Journal. 2020;41(1):111–188. doi:10.1093/eurheartj/ehz455
- Grundy SM, Stone NJ, Bailey AL, et al. 2018 AHA/ACC/AACVPR/AAPA/ABC/ACPM/ADA/AGS/APhA/ASPC/NLA/PCNA Guideline on the Management of Blood Cholesterol. Journal of the American College of Cardiology. 2019;73(24):e285–e350.
- National Institute for Health and Care Excellence (NICE). Cardiovascular disease: risk assessment and reduction, including lipid modification (CG181). Updated 2023.
- Wedlake L, A’Hern R, Russell D, Thomas K, Walters JR, Andreyev HJ. Systematic review: the prevalence of idiopathic bile acid malabsorption as diagnosed by SeHCAT scanning in patients with diarrhoea-predominant irritable bowel syndrome. Alimentary Pharmacology & Therapeutics. 2009;30(7):707–717.
- European Medicines Agency (EMA). Cholestyramine – Summary of Product Characteristics. Accessed December 2025.
- World Health Organization (WHO). Model List of Essential Medicines – 23rd List, 2023.
- British National Formulary (BNF). Colestyramine. National Institute for Health and Care Excellence. Accessed December 2025.
About the Medical Editorial Team
This article was written by the iMedic Medical Editorial Team and reviewed by qualified specialists in gastroenterology, clinical pharmacology, and internal medicine. All medical content follows the GRADE evidence framework and is based on international guidelines from the WHO, ESC/EAS, AHA/ACC, and NICE.
iMedic Editorial Team – specialists in clinical pharmacology, gastroenterology, and hepatology with experience in evidence-based medicine and patient education.
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