Cholestyramine brand name. Cholestyramine: Uses, Side Effects, Dosage, and Interactions Explained

04.11.202208.06.2023 by alexxlab

How does cholestyramine work to lower cholesterol levels. What are the common side effects of cholestyramine. When should cholestyramine be taken in relation to other medications. Can cholestyramine cause vitamin deficiencies. Who should avoid taking cholestyramine.

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Understanding Cholestyramine: A Comprehensive Overview

Cholestyramine is a medication that plays a crucial role in managing high cholesterol levels and alleviating itching caused by partial bile obstruction. Available as both a generic drug and under the brand name Prevalite, this medication comes in powder form, which is mixed with non-carbonated drinks or applesauce for oral consumption. As a member of the bile acid sequestrant class of drugs, cholestyramine operates through a unique mechanism to achieve its therapeutic effects.

What is Cholestyramine Used For?

Cholestyramine serves two primary purposes in medical treatment:

Treating high cholesterol (hyperlipidemia)
Relieving itching caused by partial bile obstruction

For patients with high cholesterol who have not achieved sufficient reduction through dietary changes alone, cholestyramine offers an additional intervention. Its ability to bind with bile acids in the intestine makes it an effective tool in cholesterol management.

The Mechanism of Action: How Cholestyramine Works

Cholestyramine’s effectiveness lies in its unique mode of action. But how exactly does it work to lower cholesterol and relieve itching?

Cholesterol Reduction

In the context of high cholesterol treatment, cholestyramine functions by:

Combining with bile acids in the intestine
Preventing the reabsorption of these bile acids into the body
Forcing the body to break down cholesterol into bile acids to replace those lost
Resulting in an overall reduction of cholesterol levels in the body

Itching Relief

For patients experiencing itching due to partial bile obstruction, cholestyramine provides relief by:

Reducing the amount of bile acids absorbed into the body
Decreasing the levels of bile acids in the skin, which are responsible for causing itching

Dosage and Administration: Getting the Most from Cholestyramine

Proper administration of cholestyramine is crucial for its effectiveness. How should patients take this medication?

Cholestyramine is available as a powder for oral suspension. The typical administration process involves:

Mixing the prescribed amount of powder with a non-carbonated drink or applesauce
Consuming the mixture orally
Taking the medication as directed by a healthcare provider

It’s important to note that cholestyramine may be used as part of a combination therapy, meaning it might be prescribed alongside other medications for optimal results.

Side Effects: What to Watch Out For

While cholestyramine can be highly effective, it’s not without potential side effects. What are the most common adverse reactions patients might experience?

Common Side Effects

The more frequently reported side effects of cholestyramine include:

Constipation
Upset stomach or stomach pain
Diarrhea or loose stools
Nausea
Vomiting
Belching
Loss of appetite
Skin irritation

These effects are often mild and may resolve on their own within a few days or weeks. However, if they persist or worsen, it’s advisable to consult a healthcare provider.

Serious Side Effects

While less common, some patients may experience more severe side effects that require immediate medical attention. These can include:

Low vitamin K levels, leading to easy bleeding or bruising
Low vitamin B levels, potentially causing anemia
High acid levels in the body

Symptoms of these serious side effects may include shortness of breath, weakness, tiredness, nausea, vomiting, confusion, headache, and abnormally rapid breathing. If any of these symptoms occur, it’s crucial to seek medical help promptly.

Drug Interactions: Navigating Potential Conflicts

Cholestyramine can interact with various medications, vitamins, and herbs. How can patients avoid potentially harmful interactions?

One of the primary concerns with cholestyramine is its ability to delay or slow the absorption of other oral medications. This can significantly reduce the effectiveness of these drugs. To mitigate this risk:

Take other oral medications at least 1 hour before cholestyramine
Alternatively, take other medications 4 to 6 hours after cholestyramine

Some medications that may interact with cholestyramine include:

Phenylbutazone
Warfarin
Thiazide diuretics

It’s crucial for patients to inform their healthcare provider about all medications, vitamins, and supplements they’re taking to avoid potential interactions.

Special Considerations: When Caution is Needed

While cholestyramine can be highly beneficial for many patients, there are certain situations where its use requires special consideration or may be contraindicated. What are these situations?

Complete Biliary Obstruction

Patients with a full blockage of their bile ducts should not take cholestyramine. This condition prevents bile from being released into the intestine, which is necessary for the medication to work effectively.

Vitamin Deficiencies

Cholestyramine can interfere with the absorption of certain vitamins, particularly vitamin K and folate (a form of vitamin B). This can lead to deficiencies that may increase the risk of bleeding or bruising. Healthcare providers may recommend vitamin supplementation for patients taking cholestyramine.

Acid-Base Balance

In some cases, cholestyramine can increase acid levels in the body. Patients experiencing symptoms such as low energy, headaches, nausea, or vomiting while taking this medication should inform their healthcare provider promptly.

Maximizing the Benefits: Tips for Taking Cholestyramine

To ensure the best possible outcomes when taking cholestyramine, patients should keep the following tips in mind:

Follow the prescribed dosage and administration instructions carefully
Be consistent with the timing of doses
Maintain proper hydration, as cholestyramine can cause constipation
Inform healthcare providers about all other medications and supplements being taken
Report any persistent or severe side effects promptly
Attend regular check-ups to monitor cholesterol levels and overall health
Continue following a heart-healthy diet and lifestyle while taking cholestyramine

By adhering to these guidelines, patients can maximize the cholesterol-lowering benefits of cholestyramine while minimizing potential side effects and complications.

Beyond Cholestyramine: Complementary Approaches to Cholesterol Management

While cholestyramine can be an effective medication for managing high cholesterol, it’s often most successful when combined with other lifestyle modifications. What additional strategies can support cholesterol reduction?

Dietary Changes

A heart-healthy diet can significantly impact cholesterol levels. Key dietary recommendations include:

Reducing saturated and trans fat intake
Increasing consumption of fruits, vegetables, and whole grains
Incorporating omega-3 fatty acids through fish or supplements
Limiting dietary cholesterol

Regular Exercise

Physical activity plays a crucial role in cholesterol management. Aim for at least 150 minutes of moderate-intensity aerobic exercise or 75 minutes of vigorous-intensity aerobic exercise per week.

Weight Management

Maintaining a healthy weight can help improve cholesterol levels. Even modest weight loss can have significant benefits for overall cardiovascular health.

Stress Reduction

Chronic stress can negatively impact cholesterol levels. Incorporating stress-reduction techniques such as meditation, yoga, or deep breathing exercises can be beneficial.

Smoking Cessation

Quitting smoking can help improve HDL (good) cholesterol levels and overall cardiovascular health.

By combining these lifestyle modifications with cholestyramine treatment, patients can often achieve more significant and sustainable reductions in cholesterol levels.

The Future of Cholesterol Management: Emerging Trends and Research

As medical science continues to advance, new approaches to cholesterol management are emerging. What developments might we see in the future of hyperlipidemia treatment?

Gene Therapy

Researchers are exploring gene therapy approaches that could potentially “turn off” genes responsible for excessive cholesterol production.

PCSK9 Inhibitors

These newer medications work by blocking a protein that reduces the liver’s ability to remove LDL cholesterol from the blood. They’re showing promise in treating patients with particularly high cholesterol levels or those who can’t tolerate statins.

Nanotechnology

Scientists are investigating the use of nanoparticles to deliver cholesterol-lowering drugs more effectively and with fewer side effects.

Personalized Medicine

Advances in genetic testing and biomarker identification may lead to more tailored cholesterol management strategies based on individual patient characteristics.

While these developments are exciting, it’s important to note that cholestyramine and other current treatments remain valuable tools in managing high cholesterol. Patients should work closely with their healthcare providers to determine the most appropriate treatment approach for their individual needs.

As we continue to learn more about cholesterol metabolism and develop new therapeutic strategies, the goal remains the same: to reduce the risk of cardiovascular disease and improve overall health outcomes for patients with hyperlipidemia. Cholestyramine, with its proven efficacy and well-understood safety profile, will likely continue to play an important role in this ongoing effort.

Side Effects, Dosage, Uses and More

Highlights for cholestyramine

Cholestyramine is available as a generic drug and a brand-name drug. Brand name: Prevalite.
This medication comes as a powder that you mix with a non-carbonated drink or applesauce and take by mouth.
Cholestyramine is used to treat high cholesterol (hyperlipidemia) and itching caused by partial bile obstruction.

Complete biliary obstruction: You shouldn’t take this drug if you have a full blockage of your bile ducts that doesn’t allow bile to be released into your intestine.
Low vitamin levels: This drug may stop your body from absorbing vitamin K and folate (a form of vitamin B). Low levels of these vitamins can be harmful and make you more likely to bleed or bruise if you get hurt. Your doctor will let you know if you need to take extra vitamins.
High acid levels: This drug can increase the acid levels in your body. Tell your doctor if you have low energy, headaches, nausea, or vomiting when you take this medication.

Cholestyramine is a prescription drug. It’s available as a powder for oral suspension.

Cholestyramine is available as the brand-name drug Prevalite. It’s also available as a generic drug. Generic drugs usually cost less. In some cases, they may not be available in every strength or form as the brand-name version.

This drug may be used as part of a combination therapy. This means you may need to take it with other medications.

Why it’s used

Cholestyramine is used to reduce high cholesterol levels. It’s given to people with high cholesterol who haven’t been able to lower their cholesterol enough with diet changes.

This drug is also used to treat itching due to partial bile obstruction.

How it works

Cholestyramine belongs to a class of drugs called bile acid sequestrants. A class of drugs is a group of medications that work in a similar way. These drugs are often used to treat similar conditions.

For high cholesterol: This drug combines with bile acids in your intestine, which stops them from being taken up into your body. When less bile acids are taken up into your body, cholesterol is broken down into acids. Breaking down cholesterol helps to lower your body’s cholesterol levels.

For itching due to partial bile obstruction: High levels of bile acids in your skin can cause itching. This drug can decrease this itching by stopping bile acids from being taken up into your body.

Cholestyramine oral suspension doesn’t cause drowsiness, but it can cause other side effects.

More common side effects

The more common side effects of cholestyramine can include:

constipation
upset stomach or stomach pain
diarrhea or loose stools
nausea
vomiting
belching
loss of appetite
skin irritation

If these effects are mild, they may go away within a few days or a couple of weeks. If they’re more severe or don’t go away, talk to your doctor or pharmacist.

Serious side effects

Call your doctor right away if you have serious side effects. Call 911 if your symptoms feel life-threatening or if you think you’re having a medical emergency. Serious side effects and their symptoms can include the following:

Low vitamin K levels. Symptoms can include:

bleeding or bruising more easily

Low vitamin B. This can cause changes to the red blood cells in your body and cause anemia. Symptoms can include:

shortness of breath
weakness
tiredness

High acid levels. Symptoms can include:

nausea
vomiting
confusion
headache
breathing faster than normal

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this information includes all possible side effects. This information is not a substitute for medical advice. Always discuss possible side effects with a healthcare provider who knows your medical history.

Cholestyramine oral suspension can interact with other medications, vitamins, or herbs you may be taking. An interaction is when a substance changes the way a drug works. This can be harmful or prevent the drug from working well.

To help avoid interactions, your doctor should manage all of your medications carefully. Be sure to tell your doctor about all medications, vitamins, or herbs you’re taking. To find out how this drug might interact with something else you’re taking, talk to your doctor or pharmacist.

Examples of drugs that can cause interactions with cholestyramine are listed below.

Other medications taken by mouth

Cholestyramine can delay or slow other oral medications from being absorbed by your body. This can lower the amount of the medication in your body. This means that it won’t work as well to treat your condition.

You should take other oral drugs at least 1 hour before you take cholestyramine, or 4 to 6 hours after you take it. Examples of these drugs include:

phenylbutazone
warfarin
thiazide diuretics, such as:

hydrochlorothiazide
indapamide
metolazone

propranolol
tetracycline
penicillin G
phenobarbital
thyroid drugs
estrogens/progestins, such as oral birth control pills
digoxin
phosphate supplements, such as:

K-Phos
Phospho-soda
Visicol

Certain vitamins

Cholestyramine interferes with fat digestion and may stop certain vitamins from getting into your body. Examples of these drugs include:

vitamin A
vitamin D
vitamin E
vitamin K

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs interact differently in each person, we cannot guarantee that this information includes all possible interactions. This information is not a substitute for medical advice. Always speak with your healthcare provider about possible interactions with all prescription drugs, vitamins, herbs and supplements, and over-the-counter drugs that you are taking.

This drug comes with several warnings.

Allergy warning

This drug can cause a severe allergic reaction. Symptoms can include:

itching
trouble breathing
wheezing

If you have an allergic reaction, call your doctor or local poison control center right away. If your symptoms are severe, call 911 or go to the nearest emergency room.

Don’t take this drug again if you’ve ever had an allergic reaction to it. Taking it again could be fatal (cause death).

Warnings for people with certain health conditions

For people with constipation: This drug can cause or worsen constipation. If you have constipation, your doctor may change your dosage or dosing schedule. If your constipation gets worse, your doctor may take you off of this drug and give you a different drug, especially if you have heart disease or hemorrhoids.

For people with phenylketonuria (PKU): The light form of cholestyramine contains 22.4 mg of phenylalanine per 5.7-gram dose. It may be better if you take regular cholestyramine, which doesn’t contain phenylalanine.

Warnings for other groups

For pregnant women: This drug is a category C pregnancy drug. That means two things:

Research in animals has shown adverse effects to the fetus when the mother takes the drug.
There haven’t been enough studies done in humans to be certain how the drug might affect the fetus.

Cholestyramine stays in your digestive tract and does not reach the bloodstream. However, this drug may reduce your body’s absorption of vitamins it needs during pregnancy.

Talk to your doctor if you’re pregnant or planning to become pregnant. This drug should be used only if the potential benefit justifies the potential risk to the fetus.

For women who are breastfeeding: This drug doesn’t pass into breast milk. However, this drug may reduce the amount of vitamins absorbed by the mother’s body. As a result, babies who are breastfed may not get the vitamins they need.

Talk to your doctor if you breastfeed your baby. You may need to decide whether to stop breastfeeding or stop taking this medication.

All possible dosages and drug forms may not be included here. Your dosage, drug form, and how often you take the drug will depend on:

your age
the condition being treated
how severe your condition is
other medical conditions you have
how you react to the first dose

Forms and strengths

Generic: Cholestyramine

Form: powder for oral suspension
Strengths: cartons of 60 pouches (4 grams each) or cans (168 grams or 42 doses)

Generic: Cholestyramine (light)

Form: powder for oral suspension (light)
Strengths: cartons of 60 pouches (4 grams each) or cans (239. 4 grams each)

Brand: Prevalite

Form: powder for oral suspension
Strengths: cartons of 42 or 60 pouches (4 grams each) or cans (231 grams or 42 doses)

Dosage for high cholesterol (hyperlipidemia)

Adult dosage (ages 18 years and older)

Cholestyramine: 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.
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: 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.
Cholestyramine light: The usual dose 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: 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.
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: 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.
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.

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this list includes all possible dosages. This information is not a substitute for medical advice. Always speak with your doctor or pharmacist about dosages that are right for you.

Cholestyramine is used for long-term treatment. It comes with risks if you don’t take it as prescribed.

If you stop taking the drug or don’t take it at all: If you don’t take this drug, your cholesterol may not improve. This could increase your risk of heart attack or stroke. If you take this drug for itching due to partial bile obstruction, your itching may not get better.

If you miss doses or don’t take the drug on schedule: Your medication may not work as well or may stop working completely. If this drug doesn’t work as well, your cholesterol or itching may not improve.

If you take too much: This drug doesn’t get taken up into your body, so taking too much likely won’t cause major problems. Taking too much may cause worse constipation or your digestive tract may become blocked. Call your doctor right away if you think you’ve taken too much of this drug.

What to do if you miss a dose: Take your dose as soon as you remember. But if you remember just a few hours before your next scheduled dose, take only one dose. Never try to catch up by taking two doses at once. This could result in increased constipation.

How to tell if the drug is working: You’ll be able to tell this drug is working if your cholesterol level decreases or your itching improves.

Keep these considerations in mind if your doctor prescribes cholestyramine for you.

General

Take this drug with food.
You should take this drug with meals unless a different time of day would be better to help you avoid interactions with other medications.
Always mix this drug with water, juice, other non-carbonated drinks, applesauce, pulpy fruits (such as crushed pineapple), or thin soups.

Storage

Store the dry powder at room temperature between 68°F and 77°F (20°C and 25°C).
Keep it away from high temperatures.
You can mix your dose with the liquid a day before taking it and store it in the refrigerator overnight.
Don’t store this medication in moist or damp areas, such as bathrooms.

Refills

A prescription for this medication is refillable. You should not need a new prescription for this medication to be refilled. Your doctor will write the number of refills authorized on your prescription.

Travel

When traveling with your medication:

Always carry your medication with you. When flying, never put it into a checked bag. Keep it in your carry-on bag.
Don’t worry about airport X-ray machines. They can’t hurt your medication.
You may need to show airport staff the pharmacy label for your medication. Always carry the original prescription-labeled box with you.
Don’t put this medication in your car’s glove compartment or leave it in the car. Be sure to avoid doing this when the weather is very hot or very cold.

Self-management

You should drink plenty of fluids with this drug. Mix each dose in at least 2 ounces of non-carbonated fluid. (If you mix the drug with a carbonated drink, it will foam up and may be hard to drink). Before taking it, stir the mixture until the powder is dissolved. This drug can also be mixed with liquid soups or pulpy fruits that contain lots of water, such as applesauce or crushed pineapple.
You can mix your dose with the liquid a day before taking it and store it in the refrigerator overnight. This may make it easier to drink.
Drink the mixture like you would drink a glass of water. Don’t sip it slowly or keep it in your mouth too long. If you do, it can discolor your teeth or cause tooth decay.

Clinical monitoring

You may need to have your cholesterol monitored while you take this drug. This will tell if your medication is working.

This monitoring may be done using this test:

Cholesterol levels, including triglycerides. Your doctor will do this blood test often during your first few months of treatment. You’ll have your cholesterol checked less often after you’ve been taking this drug for a while.

Your diet

This drug may stop vitamin K and folate (a form of vitamin B) from being absorbed by your body. Low levels of these vitamins can be harmful. Your doctor will let you know if you need to take extra vitamins.

Availability

Not every pharmacy stocks this drug. When filling your prescription, be sure to call ahead to make sure they carry it.

There are other drugs available to treat your condition. Some may be better suited for you than others. Talk to your doctor about other drug options that may work for you.

Disclaimer: Healthline has made every effort to make certain that all information is factually correct, comprehensive, and up-to-date. However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or other healthcare professional before taking any medication. The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.

Cholestyramine – LiverTox – NCBI Bookshelf

NCBI Bookshelf. A service of the National Library of Medicine, National Institutes of Health.

LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-.

LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet].

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Last Update: September 28, 2017.

OVERVIEW

Introduction

Cholestyramine is a nonabsorbed bile acid sequestrant that is used a therapy of hyperlipidemia and for the pruritus of chronic liver disease and biliary obstruction. Cholestyramine has been associated with mild and transient serum enzyme elevations during therapy, but has not been linked to cases of clinically apparent liver injury with jaundice.

Background

Cholestyramine (koe” le stye’ ra meen) is a large, highly positively charged anion exchange resin that binds to negatively charged anions such as bile acids (as well as other organic compounds and some medications). The binding of bile acids to cholestyramine creates an insoluble compound that cannot be reabsorbed and is thus excreted in the feces. Bile acids ordinarily undergo extensive (>95%) enterohepatic recirculation, being secreted in bile, acting as fat solubilizing compounds in the upper intestine, and then being reabsorbed in the distal small bowel. Chronic loss of bile acids from cholestyramine use results in a contraction of the total bile acid pool. The liver compensates for this decrease by increasing bile acid synthesis, which directly competes with cholesterol synthesis resulting in a decrease in serum levels. In addition, cholestyramine may also decrease in serum cholesterol by direct inhibition of fat absorption caused by its binding to bile acids in the intestine. Cholestyramine was approved for use in the United States in 1973 and is one of the oldest and safest cholesterol lowering agents, but it is currently used largely as an adjunctive therapy when statins or other lipid lowering agents result in an inadequate decrease in cholesterol levels. Cholestyramine is also effective in reducing the pruritus of chronic liver disease, probably as a function of binding the “pruritogen” in the intestine (which is either a bile acid or an organic anion like a bile acid that undergoes enterohepatic circulation). Because cholestyramine binds to negatively charged molecules, it can also be used to reduce absorption of medications taken in toxic overdoses and has multiple drug-drug interactions. Cholestyramine is available in multiple generic forms and under the brand name of Questran as a powder or in single dose packet form, generally in 4 gram amounts. The usual dose of cholestyramine is 4 grams, given one to six times per day usually before meals and at bedtime. Other drugs should be given 1 hour before or 4 to 6 hours after cholestyramine. Cholestyramine is unpalatable and can be difficult to swallow. Side effects include abdominal discomfort, indigestion, nausea, flatulence and constipation.

Hepatotoxicity

There is little evidence that cholestyramine causes significant liver injury. However, mild elevations in serum aminotransferase levels occur in a proportion of patients on cholestyramine. The elevations have been mild, transient and without accompanying symptoms or jaundice. In one prospective study, cholestyramine therapy was associated with serum ALT elevations above 3 times the upper limit of normal in 11% of subjects. In all cases, the abnormalities were asymptomatic and resolved rapidly upon stopping cholestyramine. Serum alkaline phosphatase levels are usually normal. A single case report of marked serum aminotransferase elevations on bile acid sequestrant therapy with rapid resolution on stopping has been published. However, there have been no reports of clinically apparent liver injury with jaundice attributed to cholestyramine or the other bile acid sequestrants. Cholestyramine is used in patients with liver disease to treat pruritus, and has little or no effect on serum enzyme or bilirubin levels.

Likelihood score: E (unlikely cause of clinically apparent liver injury with jaundice).

Mechanism of Injury

The mechanism by which cholestyramine causes serum aminotransferase elevations is not known. Because cholestyramine is not absorbed, it is surprising that it might cause liver injury, even mild and asymptomatic serum enzyme elevations. There is also little evidence that the contraction of the bile acid pool caused by its use harms the liver. Because cholestyramine can interfere with the absorption of other medications or vitamins, it may affect the levels of medications used for liver disease. These effects are particularly important for vitamins A, D, E, K, hormones such as estrogens, corticosteroids, and thyroid hormone, and medications such as thiazide diuretics, acetaminophen and digoxin.

References on the safety and hepatotoxicity of cholestyramine are given with those for colesevelam and colestipol in the Overview section on Bile Acid Resins/Sequestrants.

Drug Class: Antilipemic Agents, Bile Acid Resins/Sequestrants

CHEMICAL FORMULA AND STRUCTURE

DRUG	CAS REGISTRY NUMBER	MOLECULAR FORMULA	STRUCTURE
Cholestyramine	11041-12-6	Unspecified	T1_1_1_1_4″ rowspan=”1″ colspan=”1″>

Bookshelf ID: NBK548431PMID: 31643750

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Provided by Lexicomp ^® , this document contains all the information you need to know about this medicine, including indications, directions for use, side effects, and when your healthcare provider should be contacted.

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Warning

All Forms:

The use of this drug was accompanied by violations of the liver. In some cases, these violations have led to death. In most cases, liver problems occurred within the first 6 months after starting this drug. Sometimes problems do not improve after stopping treatment with this drug. Call your doctor right away if you develop signs of liver problems such as dark urine, fatigue, lack of appetite, nausea or abdominal pain, light-colored stools, vomiting, yellowing of the skin or eyes. In patients suffering from seizures, there may be a loss of control over seizures.
Perform blood tests as directed by your doctor. Consult with your doctor.
The risk of life-threatening liver problems is increased in children under 2 years of age. The risk is highest in patients taking more than 1 anti-seizure drug or who have a metabolic disorder, severe epilepsy with mental retardation, or congenital brain disease. Consult your doctor.
Patients with a genetic liver disorder are at an increased risk of developing liver failure due to a mitochondrial disorder such as Alpers-Huttenlocher syndrome. You may need genetic testing to detect this condition. If you have or may have mitochondrial disorders, do not take this drug without talking to your doctor.
This drug can cause serious birth defects if taken during pregnancy. It can also lower your child’s IQ and may increase the risk of autism or ADHD. If you are pregnant or may become pregnant, check with your doctor to make sure this drug is right for you. Use birth control to prevent pregnancy while you are taking this drug. If you become pregnant while taking this drug, contact your doctor immediately.
Do not take this migraine prevention drug if you are pregnant or not using birth control to prevent pregnancy.
This drug can cause very serious and sometimes deadly problems with the pancreas (pancreatitis). Such a danger exists both at the very beginning of taking the drug, and many years after its use. Symptoms of pancreatitis include abdominal pain, nausea, vomiting, or decreased appetite. If any of these symptoms occur, contact your doctor immediately.

All oral preparations:

This drug comes with a separate patient information leaflet called Patient Drug Information. Read it carefully each time you take this drug. If you have any questions about this drug, ask your doctor, pharmacist, or other health care professional.

What is this drug used for?

Used to treat seizures.
It is used to prevent migraine.
Used to treat bipolar disorder.
This drug may also be used for other indications. Consult your doctor.

What should I tell my doctor BEFORE taking this drug?

If you have an allergy to this drug, any of its ingredients, other drugs, foods or substances. Tell your doctor about your allergies and how they have manifested.
If you have any of the following health problems: liver disease or a urea cycle disorder.

This list of drugs and conditions that may interact with this drug is not exhaustive.

Tell your doctor and pharmacist about all medicines you take (prescription and over-the-counter, natural products and vitamins) and any health problems you have. You need to make sure that this drug is safe for your conditions and in combination with other drugs you are already taking. Do not start or stop taking any drug or change the dosage without your doctor’s advice.

What do I need to know or do while taking this drug?

For all uses of this drug:

Tell all your health care workers that you are taking this drug. These are doctors, nurses, pharmacists and dentists.
Avoid driving or doing other tasks or jobs that require alertness or keen eyesight until you know how this drug affects you.
Perform blood tests as directed by your doctor. Consult with your doctor.
Check with your doctor before using alcohol, marijuana or other forms of cannabis, or prescription or over-the-counter drugs that can slow you down.
This drug may affect the results of some lab tests. Tell all your health care workers and laboratory staff that you are taking this drug.
If you are unable to eat or drink as usual, please consult your physician. This includes illness, fasting, certain procedures, or surgery.
Some brands of this drug contain peanut butter. If you are allergic to peanuts, ask your pharmacist to test this brand of product for peanut oil content.
There is an increased chance of bleeding. Be careful and avoid injury. Use a soft toothbrush and an electric razor.
This drug has been associated with increased levels of ammonia in the blood. This can lead to certain brain disorders. Some fatalities. Consult your doctor.
In some individuals, certain brain disorders were not accompanied by an increase in the level of ammonia in the blood. In some cases, these brain disorders resolved after discontinuation of treatment with this drug. However, in some cases they did not go completely. Consult your doctor.
There was a serious reaction that could be deadly. In most cases, this reaction was accompanied by symptoms such as fever, rash, inflammation of the lymph nodes, and dysfunction of various organs such as the liver, kidneys, blood, heart, muscles, joints and lungs. If you have any questions, please consult your doctor.
If you are 65 years of age or older, use this drug with caution. You may experience more side effects.
This drug may affect a man’s ability to have a child. Consult your doctor.
Tell your doctor if you are breastfeeding. It is necessary to consult whether the drug poses any risk to the child.

Anti-seizure:

Talk to your doctor if your seizures change or get worse after you start taking this drug.

What side effects should I report to my doctor immediately?

WARNING. In rare cases, this drug can cause serious and sometimes deadly side effects in some patients. Contact your doctor or seek medical attention right away if you have any of the following signs or symptoms that may be associated with serious side effects:

Signs of an allergic reaction, such as rash, hives, itching, red and swollen skin with blisters or peeling, possibly accompanied by fever, wheezing or wheezing, tightness in the chest or throat, difficulty breathing, swallowing or speaking, unusual hoarseness, swelling in the mouth, face, lips, tongue or throat.
Signs of infection, such as fever, chills, very bad pain in the throat, ear, or sinuses, cough, more sputum or change in color, pain when urinating, mouth sores, or a sore that doesn’t heal.
Signs of high ammonia levels such as irregular heartbeat, trouble breathing, confusion, pale skin, bradycardia, seizures, sweating, vomiting, or muscle twitches.
Chest pain.
Swelling of the hands or feet.
Vision change.
Impairment or loss of memory.
Balance change.
Difficulties with walking.
Any unexplained bruising or bleeding.
The appearance of purple spots on the skin or redness of the skin.
Difficulty urinating or a change in the amount of urine produced.
Muscle pain or weakness.
Pain or inflammation in the joints.
Shiver.
Loss of control over eye movements.
Tinnitus.
Chills.
Like other seizure medicines, this medicine can rarely increase the risk of suicidal ideation or behavior. This risk may be higher in people who have tried or had suicidal thoughts in the past. Call your doctor right away if you develop or worsen symptoms such as depression, nervousness, anxiety, irritability, panic attacks, or other mood or behavioral disturbances. If you have suicidal thoughts or attempted suicide, contact your doctor immediately.

What are some other side effects of this drug?

Any medicine can have side effects. However, for many people, side effects are either minor or non-existent. Contact your doctor or seek medical attention if these or any other side effects bother you or do not go away:

Headache.
Constipation, diarrhea, abdominal pain, nausea, vomiting, or decreased appetite.
Increased appetite.
Feeling dizzy, drowsy, tired or weak.
Sleep disorders.
Weight gain or loss.
Hair loss.
Nervous tension and agitation.
Flu-like symptoms.

This list of possible side effects is not exhaustive. If you have any questions about side effects, please contact your doctor. Talk to your doctor about side effects.

You can report side effects to the National Health Board.

You can report side effects to the FDA at 1-800-332-1088. You can also report side effects at https://www.fda.gov/medwatch.

What is the best way to take this drug?

Use this drug as directed by your doctor. Read all the information provided to you. Strictly follow all instructions.

All oral preparations:

Take with or without food. Take with food if medicine causes nausea.
Keep taking this drug as instructed by your doctor or other health care professional, even if you feel well.
Do not stop taking this drug abruptly without consulting your doctor. This can increase the risk of seizures. If necessary, taking this drug should be stopped gradually, in accordance with the doctor’s instructions.
If you are taking cholestyramine, you may need to take it at a different time from when you take this drug. Consult with a pharmacist.

Tablets and capsules:

Swallow whole. Do not chew, break or crush.
Take this drug with a full glass of water.
If you have difficulty swallowing, check with your doctor.

Long acting tablets:

If you see particles of this drug in your stool, contact your doctor.

Split capsule:

You can swallow the capsule whole or mix the contents of the capsule with certain foods such as applesauce. Take the mixture immediately. Do not store for future use.
The mixture should not be chewed.
If you see particles of this drug in your stool, contact your doctor.

Liquid:

Liquid doses should be measured with caution. Use the dispenser that comes with the medicine. If the dispenser is not provided in the package, ask the pharmacist for a dosing agent for this drug.

Injection:

This drug is administered by infusion intravenously continuously for a certain time.

What if I miss a dose of a drug?

All oral preparations:

Take the missed dose as soon as you can.
If it’s time for your next dose, don’t take the missed dose and then go back to your regular dosing schedule.
Do not take 2 doses or an additional dose at the same time.

Injection:

See your doctor for further instructions.

How do I store and/or discard this drug?

All oral preparations:

Store at room temperature in a dry place. Do not store in the bathroom.

Injection:

If you need to store this drug at home, check with your doctor, nurse, or pharmacist for storage conditions.

All forms:

Keep all medicines in a safe place. Keep all medicines out of the reach of children and pets.
Dispose of unused or expired drugs. Do not empty into a toilet or sewer unless instructed to do so. If you have any questions about disposing of medicines, ask your pharmacist. Drug disposal programs may be in place in your area.

General information about medicines

If your health does not improve or even worsens, see your doctor.
Do not give your medicine to anyone and do not take other people’s medicines.
Some medicines may come with other patient information leaflets. If you have questions about this drug, talk with your doctor, nurse, pharmacist, or other health care professional.
Some medicines may come with other patient information leaflets. Check with your pharmacist. If you have questions about this drug, talk with your doctor, nurse, pharmacist, or other health care professional.
If you think you have overdosed, call a poison control center or get medical help right away. Be prepared to tell or show what drug you took, how much, and when it happened.

Consumer Use of Information and Limitation of Liability

This summary information includes a summary of the diagnosis, treatment, and/or drug product. It is not intended to be a comprehensive source of data and should be used as a tool to help the user understand and/or evaluate potential diagnostic and treatment options. It does NOT include all information about conditions, treatments, medications, side effects, or risks that may apply to a particular patient. It should not be considered medical advice or a substitute for medical advice, diagnosis or treatment provided by a physician based on a medical examination and assessment of the patient’s specific and unique circumstances. Patients should consult with their physician for full information about their health, medical issues, and treatment options, including any risks or benefits regarding the use of medications. This information is not a guarantee that a treatment or drug is safe, effective, or approved for a particular patient. UpToDate, Inc. and its subsidiaries disclaim any warranties or liabilities related to this information or its use. The use of this information is subject to the Terms of Use found at https://www. wolterskluwer.com/en/know/clinical-effectiveness-terms.

Last revision date

2023-03-22

Copyright

Date last updated

Monday, December 12, 2022

Fenofibrate and Derivatives | Memorial Sloan Kettering Cancer Center

Adult Medication

This document provided by Lexicomp ^® contains all the information you need to know about the drug, including indications, directions for use, side effects, and when you should contact your healthcare provider.