Cholestyramine is a medication primarily used to manage high cholesterol levels and alleviate itching caused by certain liver conditions. While some studies suggest a potential link between cholestyramine and weight loss due to its effect on gastric emptying and appetite, it's crucial to understand its approved uses, potential side effects, and necessary precautions.
What is Cholestyramine?
Cholestyramine is a bile acid sequestrant. It functions by binding to bile acids in the intestine, preventing their reabsorption into the body. This process prompts the liver to convert more cholesterol into bile acids, which ultimately lowers cholesterol levels in the blood. Cholestyramine is available as a generic drug and as brand-name drugs like Prevalite and Questran. It comes in the form of a powder that must be mixed with a non-carbonated liquid or food before consumption.
How Cholestyramine Works
Cholesterol, whether ingested or produced by the body, is primarily eliminated through its conversion into bile acids in the liver. These bile acids are then excreted into the intestine with bile, where most are reabsorbed. This reabsorbed bile is then removed from the blood by the liver and re-excreted into bile, creating a cycle of re-circulation.
Cholestyramine disrupts this cycle by binding to bile acids in the intestine, preventing their absorption and leading to their elimination in the stool. This loss of bile acids forces the liver to increase the conversion of cholesterol into bile acids, reducing cholesterol levels in the body.
Approved Uses of Cholestyramine
- High Cholesterol (Hyperlipidemia): Cholestyramine is prescribed to reduce high cholesterol levels in individuals who have not achieved sufficient cholesterol reduction through diet changes alone. Lowering blood levels of cholesterol and fats may help to prevent heart disease, angina (chest pain), strokes, and heart attacks.
- Itching (Pruritus) due to Partial Bile Obstruction: In cases of liver and biliary disease, itching can occur due to the accumulation of bile acids in the skin. Cholestyramine helps alleviate this itching by binding to bile acids in the intestines and promoting their elimination from the body.
- Other Uses: Cholestyramine can also be used to treat overdoses of digoxin or thyroid hormone and for the rapid elimination of leflunomide.
Dosage and Administration
Cholestyramine is typically taken two to four times a day. It's crucial to follow the directions on your prescription label carefully and consult your doctor or pharmacist if you have any questions.
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- Powder Form: Do not take the powder alone. Stir the powder into a glass of water, milk, heavy or pulpy fruit juices such as orange juice, or other beverage. If you use a carbonated beverage, mix the powder slowly in a large glass to avoid excessive foaming. Drink the mixture slowly. Rinse the drinking glass with more of the beverage and drink it to be sure that you get all of the powder. The powder also may be mixed with applesauce, crushed pineapple, pureed fruit, and soup. Although the powder may be mixed in hot foods, do not heat the powder. To improve the taste and for convenience, you can prepare doses for an entire day on the previous evening and refrigerate them.
- Chewable Bars: Chew each bite thoroughly before swallowing.
- General Advice: Drink plenty of liquids while taking this medication. Take this medication before a meal and/or at bedtime, and try to take any other medications at least 1 hour before or 4 hours after you take cholestyramine because cholestyramine can interfere with their absorption. Continue to take cholestyramine even if you feel well. Do not stop taking cholestyramine without talking to your doctor. This precaution is especially important if you also take other drugs; changing your cholestyramine dose may change their effects.
Dosage for High Cholesterol (Hyperlipidemia):
- Adults (18 years and older):
- Cholestyramine/Cholestyramine light: The starting dose is 1 pouch (4 grams) or 1 level scoopful (4 grams) taken by mouth once or twice per day. After one month, your doctor may increase your dosage based on your cholesterol levels. You may take up to 2 to 4 pouches or level scoopfuls per day, divided into 2 doses. You can take individual doses 1 to 6 times per day. You shouldn’t take more than 6 pouches or level scoopfuls per day.
- Children (0-17 years):
- Cholestyramine/Cholestyramine light: The usual dosage in children is 240 mg/kg of body weight per day of anhydrous cholestyramine resin taken in 2 to 3 divided doses. Most children won’t need more than 8 grams per day.
- Special considerations:
- Constipation: If you have constipation, you should start taking cholestyramine once per day for 5 to 7 days. Then, increase your dosage to twice per day if you’re able to. Your doctor may increase your dosage slowly (over several months) to make sure that your constipation doesn’t get worse.
Dosage for Itching due to Partial Bile Obstruction:
- Adult dosage (ages 18 years and older)
- Cholestyramine/Cholestyramine light: The starting dose is 1 pouch (4 grams) or 1 level scoopful (4 grams) taken by mouth once or twice per day. After one month, your doctor may increase your dosage based on your cholesterol levels. You may take up to 2 to 4 pouches or level scoopfuls per day, divided into 2 doses. You can take individual doses 1 to 6 times per day. You shouldn’t take more than 6 pouches or level scoopfuls per day.
- Child dosage (ages 0-17 years)
- Cholestyramine/Cholestyramine light: The usual dosage in children is 240 mg/kg of body weight per day of anhydrous cholestyramine resin, taken in 2 to 3 divided doses. Most children won’t need more than 8 grams per day.
- Special considerations
- Constipation: If your child has constipation, they should start taking cholestyramine once per day for 5 to 7 days. Then, increase their dose to twice per day if they’re able to take that. Your doctor may increase their dose slowly (over several months) to make sure that their constipation doesn’t get worse.
Potential Side Effects
The most common side effects of cholestyramine are:
- Constipation
- Abdominal pain
- Bloating
- Vomiting
- Diarrhea
- Belching
- Excessive gas (flatulence)
- Discolored teeth
Other less frequent side effects include:
- Gallstones
- Weight loss
- Gastric ulcer
- Gastrointestinal bleeding
Long-term use of cholestyramine may lead to a deficiency in vitamins A, D, E, and K.
Drug Interactions
Cholestyramine can interact with several medications, potentially reducing their absorption and effectiveness. It is crucial to inform your doctor about all prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take while on cholestyramine.
Examples of drugs that can interact with cholestyramine include:
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- Warfarin
- Thyroid hormones
- Digoxin
- Thiazide diuretics
- Phenylbutazone
- Propranolol
- Tetracycline
- Penicillin G
- Phenobarbital
- Estrogens and progestins
- Phosphate supplements
To minimize potential interactions, other oral medications should be taken at least 1 hour before or 4 to 6 hours after taking cholestyramine.
Warnings and Precautions
Before taking cholestyramine, inform your doctor if you:
- Are allergic to cholestyramine or any other drugs.
- Have heart disease, especially angina (heart pain).
- Have stomach, intestinal, or gallbladder disease.
- Have phenylketonuria (PKU).
- Are pregnant, plan to become pregnant, or are breastfeeding.
Cholestyramine may cause or worsen constipation. If you have constipation, your doctor may adjust your dosage or dosing schedule.
Cholestyramine and Weight Loss: Is There a Connection?
While cholestyramine is not FDA-approved as a weight-loss medication, some studies suggest a potential link between its use and weight loss. This connection is primarily attributed to cholestyramine's ability to slow gastric emptying and potentially reduce appetite.
One study involving healthy volunteers demonstrated that cholestyramine dose-dependently slowed liquid gastric emptying compared to a control group. This delayed gastric emptying can create a feeling of fullness, potentially leading to reduced food consumption.
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However, it's essential to note that the evidence supporting cholestyramine's effectiveness as a weight-loss agent is limited. Furthermore, the potential side effects and risks associated with its use should be carefully considered.
Important Considerations
- Vitamin Deficiencies: Cholestyramine can interfere with the absorption of fat-soluble vitamins (A, D, E, and K) and folate (a form of vitamin B). Long-term use may lead to deficiencies in these vitamins, potentially causing health problems. Your doctor may recommend taking vitamin supplements to address these deficiencies.
- Pregnancy and Breastfeeding: Use of cholestyramine in pregnant women has not been adequately evaluated. While the risk of adverse effects on the fetus is likely low due to minimal absorption into the bloodstream, cholestyramine may decrease the intestinal absorption of vitamins A, D, E, and K in the mother. This could lead to vitamin deficiencies in both the mother and the breastfed infant. Consult your doctor before breastfeeding while taking cholestyramine.
- Self-Medication: Cholestyramine should never be taken as an over-the-counter medication or for self-medication. It is essential to consult with a healthcare professional to determine if cholestyramine is appropriate for your individual needs and to monitor for potential side effects.
- Lifestyle Changes: Cholesterol management may include lifestyle interventions (diet and exercise) as well as medications to get your total cholesterol, LDL, HDL, and triglycerides in an optimal range. High cholesterol and triglyceride levels increase the risk of heart disease, stroke, and other cardiovascular conditions.
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