What is cholestyramine used for. Cholestyramine: Uses, Side Effects, and Precautions for Managing Cholesterol
How is cholestyramine used to lower cholesterol levels. What are the potential side effects of taking cholestyramine. Who should exercise caution when using cholestyramine. How does cholestyramine work to reduce bile acids in the body.
Understanding Cholestyramine: A Powerful Cholesterol-Lowering Medication
Cholestyramine is a medication primarily used to lower cholesterol levels in the blood. This powerful drug belongs to a class of medications known as bile acid-binding resins. By effectively removing bile acids from the body, cholestyramine prompts the liver to use more cholesterol to produce new bile acids, thereby reducing overall cholesterol levels.
But how exactly does this process work? When cholestyramine binds to bile acids in the intestines, it prevents their reabsorption into the bloodstream. As a result, the liver must use more cholesterol from the blood to create new bile acids, leading to a decrease in blood cholesterol levels. This mechanism makes cholestyramine an effective tool in managing hypercholesterolemia and reducing the risk of cardiovascular diseases.
Primary Uses of Cholestyramine
- Lowering high cholesterol levels
- Reducing the risk of heart attacks and strokes
- Treating itching associated with certain liver and bile duct disorders
Can cholestyramine be used for purposes other than cholesterol management? Indeed, while its primary use is in lowering cholesterol, cholestyramine has also shown efficacy in treating pruritus (itching) in patients with partial biliary obstruction. This condition causes an excess of bile acids in the body, and cholestyramine helps alleviate symptoms by binding to these excess acids.
Proper Administration and Dosage of Cholestyramine
Administering cholestyramine correctly is crucial for its effectiveness and to minimize potential side effects. The medication comes in powder form and should never be taken dry. Instead, it must be mixed with liquids or soft foods before consumption.
How to Take Cholestyramine
- Mix the prescribed dose with 2-6 ounces (60-180 ml) of liquid
- Stir the mixture thoroughly
- Consume immediately after mixing
- Rinse the glass with additional liquid and drink to ensure complete dosage
Is it possible to mix cholestyramine with foods other than liquids? Yes, cholestyramine can also be mixed with watery soups, applesauce, or pulpy fruits with high juice content, such as crushed pineapple or peaches. This flexibility in administration can help patients who struggle with the taste or texture of the medication when mixed with liquids alone.
It’s important to note that the dosage is tailored to each patient’s specific medical condition and response to treatment. Typically, doctors may start with a lower dose and gradually increase it to minimize side effects. Patients should follow their healthcare provider’s instructions carefully and not adjust the dosage without consultation.
Potential Side Effects and Mitigation Strategies
Like all medications, cholestyramine can cause side effects. While many people tolerate the drug well, being aware of potential adverse effects is crucial for proper management and early intervention if necessary.
Common Side Effects
- Constipation
- Stomach or abdominal pain
- Gas
- Nausea
- Vomiting
How can patients manage constipation caused by cholestyramine? To prevent or alleviate constipation, patients are advised to:
- Increase dietary fiber intake
- Drink plenty of water
- Engage in regular exercise
- Consider using a laxative (after consulting with a healthcare provider)
While these side effects are generally mild, patients should report persistent or worsening symptoms to their healthcare provider. In rare cases, more serious side effects may occur, necessitating immediate medical attention.
Serious Side Effects Requiring Immediate Attention
- Severe stomach or abdominal pain
- Unusual bleeding or bruising
- Rapid breathing
- Confusion
- Signs of allergic reaction (rash, itching, swelling, severe dizziness, trouble breathing)
Are there long-term risks associated with cholestyramine use? While cholestyramine is generally considered safe for long-term use, it can interfere with the absorption of certain nutrients and medications. Patients on long-term therapy should be monitored for potential vitamin deficiencies, particularly fat-soluble vitamins (A, D, E, K) and folic acid.
Drug Interactions and Precautions
Cholestyramine can interact with various medications, potentially affecting their absorption and efficacy. Understanding these interactions is crucial for patients and healthcare providers to ensure optimal treatment outcomes and minimize risks.
Timing of Medication Administration
To mitigate the risk of drug interactions, other medications should generally be taken:
- At least 1 hour before cholestyramine, or
- 4 to 6 hours after cholestyramine
Why is the timing of medication administration so critical with cholestyramine? Cholestyramine can bind to other medications in the digestive tract, preventing their absorption. By spacing out the administration of cholestyramine and other drugs, patients can ensure that their medications are properly absorbed and effective.
Medical Conditions Requiring Caution
Certain medical conditions may require special consideration when using cholestyramine. Patients should inform their healthcare provider if they have:
- A history of constipation
- Hemorrhoids
- Kidney disease
- Diabetes
- Phenylketonuria (PKU)
How does cholestyramine affect patients with diabetes or PKU? Some cholestyramine products contain sugar or aspartame, which can impact blood sugar levels in diabetic patients or pose risks for those with PKU. Healthcare providers may need to adjust treatment plans or recommend alternative formulations for these patients.
Lifestyle Modifications to Enhance Cholestyramine’s Effectiveness
While cholestyramine is a potent medication for managing cholesterol levels, its effectiveness can be significantly enhanced when combined with appropriate lifestyle changes. These modifications not only support the medication’s action but also contribute to overall cardiovascular health.
Key Lifestyle Changes
- Adopting a low-cholesterol, low-fat diet
- Engaging in regular physical exercise
- Maintaining a healthy body weight
- Quitting smoking
How do these lifestyle changes complement cholestyramine therapy? A healthy diet low in saturated fats and cholesterol helps reduce the overall cholesterol burden on the body. Regular exercise improves cardiovascular health and can help raise HDL (good) cholesterol levels. Weight management and smoking cessation further reduce cardiovascular risk factors, enhancing the cholesterol-lowering effects of cholestyramine.
Patients should work closely with their healthcare providers to develop a comprehensive treatment plan that includes both medication and lifestyle modifications. This holistic approach can lead to more significant improvements in cholesterol levels and overall health outcomes.
Long-Term Management and Monitoring
Successful cholesterol management with cholestyramine requires ongoing monitoring and adjustment. Patients should maintain regular follow-ups with their healthcare providers to assess the medication’s effectiveness and address any emerging concerns.
Regular Monitoring
- Lipid profile tests to track cholesterol levels
- Assessment of potential nutrient deficiencies
- Evaluation of side effects and medication tolerance
- Adjustment of dosage as needed
How often should patients have their cholesterol levels checked while on cholestyramine? Initially, healthcare providers may recommend more frequent lipid profile tests, possibly every 4-6 weeks, to assess the medication’s effectiveness. Once cholesterol levels stabilize, testing may be reduced to every 3-6 months or as determined by the healthcare provider.
It’s important to note that the full benefit of cholestyramine may take several weeks to become apparent. Patients should continue taking the medication as prescribed, even if they don’t immediately notice changes in their cholesterol levels or overall health.
Special Considerations for Specific Patient Groups
While cholestyramine is generally safe and effective for many patients, certain groups may require special considerations or alternative treatments. Understanding these specific needs is crucial for healthcare providers in tailoring treatment plans.
Pediatric Patients
Cholestyramine can be used in pediatric patients with familial hypercholesterolemia, but dosage and administration may differ from adult protocols. Close monitoring is essential to ensure proper growth and development, as the medication can interfere with the absorption of essential nutrients.
Pregnant and Breastfeeding Women
The use of cholestyramine during pregnancy and breastfeeding requires careful consideration. While the medication is not absorbed systemically, it can potentially affect the absorption of vital nutrients for fetal development and infant nutrition.
Elderly Patients
Older adults may be more sensitive to the side effects of cholestyramine, particularly constipation. Dosage adjustments and closer monitoring may be necessary for this population.
How should treatment approaches differ for these special patient groups? Healthcare providers must weigh the benefits and risks of cholestyramine therapy for each individual patient. In some cases, alternative cholesterol-lowering strategies or modified dosing regimens may be more appropriate. Regular consultations and personalized care plans are essential for ensuring optimal outcomes in these special populations.
In conclusion, cholestyramine remains a valuable tool in the management of high cholesterol and certain bile acid disorders. Its unique mechanism of action, combined with lifestyle modifications, can significantly improve lipid profiles and reduce cardiovascular risk. However, proper administration, awareness of potential side effects, and regular monitoring are crucial for maximizing its benefits while minimizing risks. As with any medication, patients should work closely with their healthcare providers to determine if cholestyramine is the right choice for their individual health needs and to develop a comprehensive treatment strategy that ensures the best possible outcomes.
Cholestyramine Light Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing
Uses
Cholestyramine is used along with a proper diet to lower cholesterol in the blood. Lowering cholesterol helps decrease the risk for strokes and heart attacks.In addition to a proper diet (such as a low-cholesterol/low-fat diet), other lifestyle changes that may help this medication work better include exercising, losing weight if overweight, and stopping smoking. Consult your doctor for more details.Cholestyramine may also be used to treat itching in people with too much bile acid caused by a certain type of liver/bile duct disease (partial biliary obstruction).This medication is known as a bile acid-binding resin. It works by removing bile acid from the body. In people with high cholesterol, this causes the liver to make more bile acid by using cholesterol in the blood. This helps to lower the cholesterol levels.
How to use Cholestyramine Light 4 Gram Oral Powder
Take this medication by mouth as directed by your doctor, usually 1 to 2 times a day. This medication comes as a powder with doses measured by the scoopful (using the provided scoop) or in individual dose packets. Do not take your dose in the dry powder form. Mix the medication in at least 2 to 6 ounces (60 to 180 milliliters) of liquid (such as water, milk, fruit juice), stir completely, and drink right away. Rinse your glass with more liquid and drink the rinse liquid to be sure that you have taken the entire dose. You may also mix this medication with watery soups, applesauce, or a pulpy fruit which has a lot of juice (such as crushed pineapple, peaches).
Do not hold the mixture in your mouth for long since doing so can damage your teeth. Practice good dental habits (such as brushing and flossing your teeth regularly).
The dosage is based on your medical condition and response to treatment. To reduce your risk of side effects, your doctor may direct you to start this medication at a low dose and gradually increase your dose. Follow your doctor’s instructions carefully. It may take several weeks before you get the full benefit of this drug.
Cholestyramine may decrease your absorption of other medications. Take your other medications as directed by your doctor, usually at least 1 hour before or 4 to 6 hours after cholestyramine. Ask your doctor or pharmacist for more information or if you have any questions.
Take this medication regularly in order to get the most benefit from it. To help you remember, take it at the same time(s) each day. Keep taking this medication even if you feel well. Most people with high cholesterol do not feel sick.
Side Effects
Constipation, stomach/abdominal pain, gas, nausea, and vomiting may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.
To prevent constipation, eat dietary fiber, drink enough water, and exercise. You may also need to take a laxative. Ask your pharmacist which type of laxative is right for you.
Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.
Tell your doctor right away if you have any serious side effects, including: severe stomach/abdominal pain, unusual bleeding/bruising, rapid breathing, confusion.
A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.
In the US – Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.
In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
Precautions
Before taking cholestyramine, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.
Before using this medication, tell your doctor or pharmacist your medical history, especially of: constipation, hemorrhoids, kidney disease.
Some products may contain sugar or aspartame. Caution is advised if you have diabetes, phenylketonuria (PKU), or any other condition that requires you to limit/avoid these substances in your diet. Ask your doctor or pharmacist about using this product safely.
Because this drug can interfere with the absorption of certain nutrients (such as folic acid, fat-soluble vitamins including A, D, E, K), your doctor may direct you to take a multivitamin supplement. Consult your doctor for more information.
Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).
Older adults may be more sensitive to the side effects of this drug, especially constipation.
During pregnancy, this medication should be used only when clearly needed. It may affect the absorption of certain nutrients. Discuss the risks and benefits with your doctor.
This medication is unlikely to pass into breast milk. However, it may affect the absorption of certain nutrients. Consult your doctor before breast-feeding.
Interactions
See also How to Use section.
Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.
Some products that may interact with this drug include: “blood thinners” (such as warfarin), mycophenolate, raloxifene.
Does Cholestyramine Light 4 Gram Oral Powder interact with other drugs you are taking?
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Overdose
If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe stomach/abdominal pain.
Do not share this medication with others.
Lab and/or medical tests (such as blood cholesterol/triglyceride levels, vitamin levels) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.
If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
Store at room temperature away from light and moisture. The color of the medication may sometimes vary. This is normal and will not affect how the drug works. If you have any questions about storage, ask your pharmacist. Do not store the medication in the bathroom. Keep all medications away from children and pets.
Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Images
Cholestyramine Light 4 gram oral powder
Color: yellowShape: Imprint:
This medicine is a yellow, orange-vanilla, powder
Cholestyramine Light 4 gram oral powder
Color: creamShape: Imprint:
This medicine is a yellow, orange-vanilla, powder
Cholestyramine Light 4 gram powder for susp in a packet
Color: off-whiteShape: Imprint:
This medicine is a yellow, orange-vanilla, powder
Cholestyramine Light 4 gram powder for susp in a packet
Color: yellowShape: Imprint:
This medicine is a yellow, orange-vanilla, powder
Cholestyramine Light 4 gram oral powder
Color: off-whiteShape: Imprint:
This medicine is a yellow, orange-vanilla, powder
Cholestyramine Light 4 gram powder for susp in a packet
Color: creamShape: Imprint:
This medicine is a yellow, orange-vanilla, powder
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CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.
Cholestyramine: Uses, Interactions, Mechanism of Action
- Summary
Cholestyramine is a bile acid sequestrant used as an adjunct in the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia, and for the relief of pruritus associated with partial biliary obstruction.
- Brand Names
Prevalite, Questran
- Generic Name
- Cholestyramine
- DrugBank Accession Number
- DB01432
- Background
Cholestyramine or colestyramine is a bile acid sequestrant. Bile acid sequestrants are polymeric compounds which serve as ion exchange resins. Cholestyramine resin is quite hydrophilic, but insoluble in water.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Synonyms
- Cholestyramine resin
- Colestiramina
- Colestyramine
- Indication
Indicated as adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia (elevated low density lipoprotein [LDL] cholesterol) who do not respond adequately to diet. Also for the relief of pruritus associated with partial biliary obstruction.
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- Associated Conditions
- Atherosclerosis
- Primary Hypercholesterolemia
- Pruritus
- Contraindications & Blackbox Warnings
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- Pharmacodynamics
Cholesterol is probably the sole precursor of bile acids. During normal digestion, bile acids are secreted into the intestines. A major portion of the bile acids is absorbed from the intestinal tract and returned to the liver via the enterohepatic circulation. Only very small amounts of bile acids are found in normal serum. Cholestyramine resin adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces. This results in a partial removal of bile acids from the enterohepatic circulation by preventing their absorption.
- Mechanism of action
Cholestyramine forms a resin that acts as a bile acid sequestrant to limit the reabsorption of bile acids in the gastrointestinal tract. Cholestyramine resin is a strong anion exchange resin, allowing it to exchange its chloride anions with anionic bile acids present in the gastrointestinal tract and form a strong resin matrix. Cholestyramine consists of a functional group, which is a quaternary ammonium group attached to an inert styrene-divinylbenzene copolymer, in the anion exchange resin.
Target Actions Organism ABile acids binder
Humans - Absorption
Not absorbed from the gastrointestinal tract following oral administration.
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
Bile acids
- Route of elimination
Cholestyramine resin adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces.
- Half-life
6 minutes
- Clearance
Not Available
- Adverse Effects
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- Toxicity
Overdose may result in blockage of intestine or stomach.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
- Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
- Approved
- Vet approved
- Nutraceutical
- Illicit
- Withdrawn
- Investigational
- Experimental
- All Drugs
Drug Interaction Acarbose The therapeutic efficacy of Acarbose can be increased when used in combination with Cholestyramine. Aceclofenac Cholestyramine can cause a decrease in the absorption of Aceclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy. Acemetacin Cholestyramine can cause a decrease in the absorption of Acemetacin resulting in a reduced serum concentration and potentially a decrease in efficacy. Acenocoumarol Cholestyramine can cause a decrease in the absorption of Acenocoumarol resulting in a reduced serum concentration and potentially a decrease in efficacy. Acetaminophen Cholestyramine can cause a decrease in the absorption of Acetaminophen resulting in a reduced serum concentration and potentially a decrease in efficacy. Acetazolamide Cholestyramine can cause a decrease in the absorption of Acetazolamide resulting in a reduced serum concentration and potentially a decrease in efficacy. Acetyl sulfisoxazole Cholestyramine can cause a decrease in the absorption of Acetyl sulfisoxazole resulting in a reduced serum concentration and potentially a decrease in efficacy. Acetyldigitoxin Cholestyramine can cause a decrease in the absorption of Acetyldigitoxin resulting in a reduced serum concentration and potentially a decrease in efficacy. Acetylsalicylic acid Cholestyramine can cause a decrease in the absorption of Acetylsalicylic acid resulting in a reduced serum concentration and potentially a decrease in efficacy. Alclofenac Cholestyramine can cause a decrease in the absorption of Alclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy. Learn more
- Food Interactions
- Take with fluids. Do not take with carbonated fluids.
- Take with food. Take with a meal unless this interferes with other medications.
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- International/Other Brands
- Cholybar / Locholest / Locholest light / Questran Light
- Brand Name Prescription Products
json?group=approved” data-total=”11″>
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Cholestyramine Powder, for suspension 4 g / 9 g Oral Sorres Pharma Inc 1998-02-17 2010-10-06 Canada Cholestyramine Powder, for suspension 4 g / 5 g Oral Sorres Pharma Inc 1998-02-17 2010-10-19 Canada Cholestyramine-odan Powder, for suspension 4 g / sachet Oral Odan Laboratories Ltd 2016-12-23 Not applicable Canada Olestyr Powder, for suspension 4 g / sachet Oral Pharmascience Inc 1996-03-15 Not applicable Canada Olestyr Powder, for suspension 4 g / sachet Oral Pharmascience Inc 1993-12-31 Not applicable Canada Questran Powder, for suspension 4 g/9g Oral Par Pharmaceutical 2009-06-01 2011-09-09 US Questran Powder, for suspension 4 g/6. 4g Oral Par Pharmaceutical 2009-06-01 2011-09-09 US Questran Light Pws 4gm/pck Powder, for solution 4 g / pck Oral Bristol Labs Division Of Bristol Myers Squibb 1991-12-31 2005-08-01 Canada Questran Pwr 378gm/can Powder, for solution 4 g / pck Oral Bristol Labs Division Of Bristol Myers Squibb 1985-12-31 2005-08-01 Canada Questran Pwr 4gm/9gm Powder, for solution 4 g / 9 g Oral Bristol Labs Division Of Bristol Myers Squibb 1979-12-31 2005-08-01 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Alti-cholestyramine Light Kit; Powder 4 g / pck Oral Altimed Pharma Inc. 1994-12-31 1999-09-17 Canada Cholestyramine Powder, for suspension 4 g/5g Oral Par Pharmaceutical, Inc. 2005-09-15 Not applicable US Cholestyramine Powder, for suspension 4 g/5g Oral bryant ranch prepack 2005-09-15 Not applicable US Cholestyramine Powder, for suspension 4 g/9g Oral Physicians Total Care, Inc. 2010-03-22 Not applicable US Cholestyramine Powder, for suspension 4 g/9g Oral Zydus Lifesciences Limited 2018-08-01 Not applicable US Cholestyramine Powder, for suspension 4 g/5g Oral bryant ranch prepack 2005-09-15 Not applicable US Cholestyramine Powder, for suspension 4 g/9g Oral Upsher-Smith Laboratories, Inc. 1996-08-15 2023-09-30 US Cholestyramine Powder, for suspension 4 g/9g Oral Epic Pharma, LLC 2021-12-15 Not applicable US Cholestyramine Powder, for suspension 4 g/9g Oral Ajanta Pharma USA Inc. 2020-04-06 Not applicable US Cholestyramine Powder, for suspension 4 g/9g Oral Par Pharmaceutical, Inc. 2005-09-15 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image KOLESTRAN 9 GR 30 POSET Cholestyramine (4 g) Powder Oral SANDOZ İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey
- ATC Codes
- C10AC01 — Colestyramine
- C10AC — Bile acid sequestrants
- C10A — LIPID MODIFYING AGENTS, PLAIN
- C10 — LIPID MODIFYING AGENTS
- C — CARDIOVASCULAR SYSTEM
- Drug Categories
- Anion Exchange Resins
- Anticholesteremic Agents
- Bile Acid Sequestrants
- Bile-acid Binding Activity
- Compounds used in a research, industrial, or household setting
- Hypolipidemic Agents
- Hypolipidemic Agents Indicated for Hyperlipidemia
- Ion Exchange Resins
- Laboratory Chemicals
- Lipid Modifying Agents
- Lipid Modifying Agents, Plain
- Lipid Regulating Agents
- Macromolecular Substances
- Non-statin Hypolipidemic Agents Indicated for Hyperlipidemia
- Plastics
- Polymers
- Polystyrenes
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
- UNII
- 4B33BGI082
- CAS number
- 11041-12-6
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
- Synthesis Reference
Moh. S. Amer, Jack C. Gray, “Cholestyramine compositions and method for preparation thereof.” U.S. Patent US4895723, issued March, 1967.
US4895723
- General References
- Not Available
- External Links
- PubChem Substance
- 46506251
- RxNav
- 2447
- ChEMBL
- CHEMBL1201625
- PharmGKB
- PA448974
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Cholestyramine
- MSDS
Download (74.1 KB)
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Prevention Diabetes / Diabetic Neuropathies / Diabetic Retinopathy (DR) 1 4 Completed Treatment Healthy Subjects (HS) 2 4 Enrolling by Invitation Treatment Chronic Kidney Disease (CKD) / Complication of Hemodialysis / Hyperphosphataemia 1 3 Completed Prevention Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Myocardial Infarction / Myocardial Ischemia / Primary Hypercholesterolemia 1 3 Completed Prevention Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Myocardial Ischemia 2 3 Completed Treatment High Cholesterol 2 3 Completed Treatment Multiple Sclerosis 1 3 Unknown Status Treatment Graves’ Disease / Hyperthyroidism 1 2 Completed Treatment Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Myocardial Ischemia 1 2 Completed Treatment High Cholesterol 1
- Manufacturers
Not Available
- Packagers
- A-S Medication Solutions LLC
- Bristol-Myers Squibb Co.
- Catalent Pharma Solutions
- Eon Labs
- Major Pharmaceuticals
- Mead Johnson and Co.
- Medisca Inc.
- Novopharm Ltd.
- Par Pharmaceuticals
- Physicians Total Care Inc.
- Upsher Smith Laboratories
- Dosage Forms
Form Route Strength Kit; powder Oral 4 g / pck Granule Oral 4 g Powder, for suspension Oral 4 g/5g Powder, for suspension Oral 4 g/8.3g Powder, for suspension Oral 4 g / 9 g Powder, for suspension Oral 4 g / 5 g Powder, for suspension Oral 4 g/9g Powder, for suspension Oral 4 g/5.5g Powder Not applicable 1 kg/1kg Powder Oral 4 g/9g Powder Oral 4 g/5. 7g Powder, for suspension Oral 4 g/4.8g Powder, for suspension Oral 4 g/5.7g Powder, for suspension Oral 4 g/8.780g Powder, for suspension Oral 4 g / sachet Powder, for suspension Oral 4 g/5.718g Powder, for suspension Oral 4 g Tablet Oral Powder Parenteral 4 G Powder Parenteral 4 g/9.5g Powder Oral Powder Oral 4 g Powder; suspension Oral 4 g / dose Powder, for suspension Oral 400 g / can Powder Oral 4.00 g Powder, for solution Oral 4 g / 5 g Powder, for solution Oral 400 g / pck Powder Oral 4 g / 9 g Powder, for suspension Oral 4 g/6. 4g Powder, for suspension Oral 9 g Powder, for solution Oral 4 g / pck Powder, for solution Oral 4 g / 9 g Tablet Oral 1 g / tab Powder Granule Oral 0.7382 g/g Granule Oral 4 g/5.4g - Prices
Unit description Cost Unit Questran Light 4 gm/dose Powder 210 gm Can 116.3USD can Questran 4 gm/dose Powder 378 gm Can 115.62USD can Questran Light 4 gm/dose Powder 268 gm Can 102.35USD can Cholestyramine 4 gm/dose Powder 378 gm Can 57.99USD can Cholestyramine Light 4 gm/dose Powder 210 gm Can 57.99USD can Cholestyramine resin powder 16. 83USD g Questran 4 gm Packets 4.4USD packet Questran light packet 4.25USD each Questran packet 4.23USD each Cholestyramine 4 gm Packets 3.5USD packet Cholestyramine Light 4 gm Packets 3.49USD packet Cholestyramine light packet 3.35USD each Prevalite packet 2.58USD each Pms-Cholestyramine Light 4 g Powder Packet 1.41USD packet Pms-Cholestyramine Regular 4 g Powder Packet 1.41USD packet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
- Patents
- Not Available
- State
- Solid
- Experimental Properties
Property Value Source water solubility Insoluble Not Available - Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Targets
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Yes
Binder
References
- Nichifor M, Cristea D, Mocanu G, Carpov A: Aminated polysaccharides as bile acid sorbents: in vitro study. J Biomater Sci Polym Ed. 1998;9(6):519-34. [Article]
- Benson GM, Alston DR, Hickey DM, Jaxa-Chamiec AA, Whittaker CM, Haynes C, Glen A, Blanchard S, Cresswell SR, Suckling KE: SK&F 97426-A: a novel bile acid sequestrant with higher affinities and slower dissociation rates for bile acids in vitro than cholestyramine. J Pharm Sci. 1997 Jan;86(1):76-81. [Article]
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Drug created at July 24, 2007 18:41 / Updated at June 24, 2023 20:44
Description COLESTYRAMINE indications, dosages, contraindications of the active substance COLESTYRAMINE
When used simultaneously with tricyclic antidepressants (including imipramine, amitriptyline, desipramine, nortriptyline), their concentration in blood plasma may decrease.
Co-administration with acarbose may enhance the effects of acarbose.
With simultaneous use with amiodarone, the concentration of amiodarone in the blood plasma decreases.
With simultaneous use with sodium valproate, a slight decrease in the absorption of sodium valproate is possible.
Concomitant use with vancomycin reduces the effectiveness of vancomycin.
When used simultaneously with warfarin, phenprocoumon, dicoumarol, ethyl biscum acetate, the effectiveness of anticoagulants may decrease.
When used simultaneously with hydrocortisone, the absorption of hydrocortisone from the gastrointestinal tract decreases.
When used simultaneously with hydrochlorothiazide, the absorption and diuretic effect of hydrochlorothiazide is reduced.
Co-administration with glipizide may reduce the absorption of glipizide.
When administered 1.5 hours apart, cholestyramine does not significantly affect plasma concentrations of digoxin and digitoxin. A decrease in the concentration of digoxin and digitoxin in the blood plasma is possible with prolonged joint use with cholestyramine.
When used simultaneously with diclofenac, ibuprofen, the absorption of diclofenac and ibuprofen from the gastrointestinal tract decreases.
With simultaneous use with iron sulfate, phenylbutazone, it is possible to reduce the absorption of iron sulfate and phenylbutazone.
When used simultaneously with levothyroxine, thyroid hormones, the absorption of levothyroxine and thyroid hormones from the gastrointestinal tract decreases.
Co-administration with loperamide may reduce the effectiveness of loperamide.
With simultaneous use with methotrexate, a decrease in the concentration of methotrexate in blood plasma is possible.
When used simultaneously with metronidazole, a slight decrease in the absorption of metronidazole from the gastrointestinal tract is possible.
Co-administration with paracetamol may reduce the absorption of paracetamol.
When used simultaneously with cholestyramine, it is possible to increase the excretion of piroxicam, meloxicam, tenoxicam from the body and reduce their effectiveness.
With simultaneous use with pravastatin, fluvastatin, the concentration of pravastatin in blood plasma decreases, C max and fluvastatin AUC. At the same time, the overall lipid-lowering effect is enhanced.
When used simultaneously with raloxifene, the absorption of raloxifene is reduced.
When used simultaneously with sulindac, the absorption of sulindac decreases (even if the interval between doses is 3 hours).
When used simultaneously with spironolactone, cases of hypochloremic alkalosis have been described.
When used simultaneously with furosemide, the absorption and diuretic effect of furosemide are reduced.
pms-Cholestyramine Regular
Application of cholestyramine
Cholestyramine – composition and form of release of the drug
Cholestyramine: how to take the drug
Cholestyramine – contraindications, side effects
Cholestyramine analogs
Cholestyramine reduces the concentration of low density lipoproteins and cholesterol in the blood.
Application of Cholestyramine
Indications.
Cholestyramine is indicated as an adjuvant therapy (as an adjunct to diet and exercise) to lower elevated serum cholesterol in patients with primary hypercholesterolemia to reduce the risk of atherosclerotic coronary artery disease and myocardial infarction.
Cholestyramine can be used to lower high cholesterol in patients with combined hypercholesterolemia and hypertriglyceridemia, but is not indicated when hypertriglyceridemia is the dominant pathology.
Cholestyramine can be used for the symptomatic treatment of diarrhea caused by bile acids in patients with short bowel syndrome, as well as for the relief of itching in cholestasis due to partial obstruction of the biliary tract.
Cholestyramine – composition and form of release of the drug
Composition
active ingredient : cholestyramine resin (cholestyramine resin), a copolymer of styrene and divinylbenzene with quaternary ammonium functional groups;
1 powder sachet contains cholestyramine rubber 4 g
Excipients : sucrose, citric acid, colloidal silicon dioxide, sunset yellow FCF (E 110), D & C yellow No. 10 (quinoline yellow E 104), dye D & C yellow No. 10 aluminum lacquer 15% (quinoline yellow E 104), propylene glycol alginate, orange flavor, which contains orange flavor, maltodextrin, acacia (gum arabic E 414), butylhydroxytoluene (E 321).
Dosage form. Powder for oral suspension.
Basic physical and chemical properties: fine whitish or yellowish powder with a slight orange odor. Slices of foreign material are absent.
Cholestyramine: how to take the drug
Dosage and administration.
Use cholestyramine orally.
It is advisable to start therapy with a single dose of the drug once a day. Then after 1-2 days the dosage can be increased.
The recommended adult dose is 4 g cholestyramine 1 to 6 times a day. The dosage can be changed according to the individual needs of the patient.
The drug should not be taken dry, it is intended only for use as an aqueous suspension.
Preparation of the drug for administration: to prepare the suspension, place the contents of 1 sachet in a glass with 120-180 ml of water or a drink that does not contain carbon dioxide (milk or fruit juice). After 1 minute, mix the powder intensively in the liquid. The powder can be mixed in soup or juice with pulp, squeezed out of fruits (apples or pineapples).
Children.
The safety and efficacy of cholestyramine in children have not been established.
Cholestyramine – contraindications, side effects
Contraindications.
Cholestyramine is contraindicated in complete obstruction of the biliary tract, when bile does not enter the intestine at all.
The drug is contraindicated in case of hypersensitivity to the active substance or other components that make up the drug.
Please note that cholestyramine may bind other drugs. Therefore, other medicines should be taken no later than 1:00 before taking cholestyramine and not earlier than 4-6 hours (and preferably even later) after taking cholestyramine.
Application features.
The drug should not be used dry. The drug is intended only for use in the form of an aqueous suspension.
Other cholesterol-lowering therapies (diet therapy, weight loss) should be tried before starting cholestyramine treatment. It is also necessary to deal with the treatment of underlying diseases such as hypothyroidism, diabetes mellitus, nephrotic syndrome, dysproteinemia, obstructive liver disease, which can cause hypercholesterolemia. It is also necessary to check whether the use of drugs leads to an increase in low-density lipoprotein cholesterol. With the use of cholestyramine, a positive trend towards a decrease in cholesterol levels is observed already during the first month of treatment. Taking the drug can be extended to consolidate the effect.
Effects on vitamin absorption: Since cholestyramine binds bile acids, it may interfere with intestinal absorption of fat-soluble vitamins A, D and K. For long-term use of cholestyramine, parenteral forms of a mixture of vitamins A and D should be used.
Use in patients over 60 years of age . In the elderly, side effects from the gastrointestinal tract are more likely.
Excipients.
The preparation contains sucrose. If you have an intolerance to some sugars, consult your doctor before taking this medicine.
The product contains sunset yellow FCF (E 110), which may cause allergic reactions.
Use during pregnancy or lactation.
The use of the drug in pregnant women and women who are breastfeeding is possible only in cases where the potential benefit from the use of the drug outweighs the potential risk to the fetus or child.
The ability to influence the reaction rate when driving vehicles or operating other mechanisms.
There are no data, but the possibility of developing adverse reactions from the nervous system, such as dizziness, drowsiness, loss of consciousness, should be taken into account.
Overdose.
The main consequence of overdose may be a violation of the patency of the gastrointestinal tract.
Adverse reactions.
Constipation occurs most frequently with cholestyramine, especially at high doses and in elderly patients (over 60 years of age).
Less commonly, side effects such as a feeling of distension of the stomach, flatulence, bloating, nausea, vomiting, diarrhea, steatorrhea, anorexia, heartburn, skin rashes, irritation of the skin, tongue, perianal zone, bleeding tendency due to hypoprothrombinemia (lack of vitamin K ), deterioration of vision in the dark due to lack of vitamin A, hyperchloremic acidosis in children, osteoporosis, manifestations of vitamin D deficiency.
Biliary tract indurations, including indurations in the gallbladder, have occasionally been observed, may be a manifestation of liver disease, and are not related to the use of the drug.
Other adverse reactions have been observed, not all of which may be due directly to cholestyramine. These are gastrointestinal and rectal bleeding, black stools, hemorrhoidal bleeding, duodenal ulcer bleeding, dysphagia, hiccups, belching, rectal pain, exacerbation of peptic ulcer, sour taste, exacerbation of pancreatitis, diverticulitis.
Changes in laboratory parameters: impaired liver function.
Hematological changes: changes in the value of PV (decrease or increase), ecchymosis, anemia, bleeding gums.
From the musculoskeletal system: pain in the back, muscles, joints, arthritis.
Neurological changes: headache, dizziness, anxiety, fatigue, tinnitus, loss of consciousness, drowsiness, ischioneuralgia, paresthesia.
From the side of the kidneys: hematuria, dysuria, burning smell of urine, diuresis (increased urine output).
On the part of the organ of vision: uveitis.
Hypersensitivity reactions: urticaria, bronchial asthma, shortness of breath, wheezing.
Other changes: decrease or increase in body weight, increased libido, swelling of the glands, edema, caries.
Cholestyramine analogues
- Questran
- Kolestir
Source: State Register of Medicines of Ukraine. The instruction is published with abbreviations for reference only. Before use, consult your doctor and carefully read the instructions.