Cholestyramine resin is a medication primarily used to lower cholesterol levels in the blood. It belongs to a class of drugs known as bile acid sequestrants. Cholestyramine works by binding to bile acids in the intestines, preventing them from being reabsorbed into the bloodstream. This leads to increased excretion of bile acids in the feces, which prompts the liver to use more cholesterol to produce bile acids, thereby reducing cholesterol levels in the blood.
By preventing the bile acid-bound low-density lipoprotein complex from being absorbed, cholestyramine, an insoluble bile acid binding resin, causes its excretion. These conditions are treated with it:
- be used in conjunction with statins to treat primary hypercholesterolemia and slow the progression of arteriolosclerosis.
- for the treatment of cholestasis-related pruritus brought on by a partial biliary blockage.
Off-Label Uses of cholestyramine in Adults include:
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- Chronic diarrhoea resulting from the malabsorption of bile acids.
- To enhance the elimination of digoxin (in non-life threatening toxicity)
- As adjunctive therapy in Graves disease.
Cholestyramine resin Dose in Adults
Cholestyramine resin in dyslipidemia (in patients not achieving the target lipids with the maximally tolerated dose of statins and ezetimibe):
- The usual starting dose of cholestyramine resin is 4 grams, taken 1 to 2 times a day.
- Your doctor may gradually increase this dose every month if needed.
- The typical maintenance dose is between 8 to 16 grams per day, split into two doses.
- The highest dose you should take in a day is 24 grams.
Note: This medication might be suggested for people with moderately high triglyceride levels (up to 300 mg/dL) who haven't reached their cholesterol goals even after trying changes in diet and other cholesterol-lowering medications like statins and ezetimibe.
Cholestyramine resin off-label use in the treatment of chronic diarrhoea due to bile acid malabsorption:
- The usual starting dose of cholestyramine resin is 4 grams taken once a day.
- Then, your doctor may increase the dose by 4 grams each week, splitting it into 1 to 4 doses per day if needed.
- The highest dose you should take in a day is 36 grams.
It's worth noting that more research might be needed to fully understand how effective cholestyramine resin is for treating this condition.
Cholestyramine resin off-label use in the adjunctive therapy of Hyperthyroidism due to Graves disease:
- The usual dose is 4 grams taken twice a day according to one study (Tsai, 2005), or 4 grams taken three times a day according to another study (Mercado, 1996).
It's important to note that cholestyramine resin is used alongside other medications like antithyroid drugs (such as methimazole or propylthiouracil) and propranolol. These medications work together to manage the symptoms of hyperthyroidism.
Cholestyramine resin dose in Pruritus associated with cholestasis:
- The typical starting dose of cholestyramine resin is 4 grams taken once or twice a day.
- Your doctor may gradually increase this dose up to 16 grams per day, split into two doses, if needed.
This medication helps by binding to bile acids, which can reduce itching associated with cholestasis.
Cholestyramine resin Dose in Children
Cholestyramine resin does in Diaper dermatitis:
Infants and Children: Topical:
- Cholestyramine resin isn't available as a commercial product for this purpose, so it needs to be specially made by a pharmacist.
- It's usually mixed into ointments or pastes, commonly using bases like Aquaphor® or polyethylene glycol.
- The typical concentration is between 5% to 10%, but it can be compounded at higher concentrations, up to 20%.
- Some pharmacies might use petrolatum as the base for compounding.
Cholestyramine resin Dose in Dyslipidemia:
For children aged 6 years and older with dyslipidemia (high cholesterol), the dose of cholestyramine resin can vary based on age or weight:
- Age-Directed Dosage:
- Start with 2 to 4 grams per day for the first week, then increase gradually up to 8 grams per day, as tolerated.
- Children under 10 years old may only tolerate a daily dose of 4 grams.
- It's better to take the dose once daily with the evening meal for better lipid-lowering effects. If once-daily dosing isn't tolerated, the total daily dose can be split into two doses and taken with morning and evening meals. It can also be taken in three divided doses daily.
- Doses higher than 8 grams per day may not significantly lower cholesterol further but could increase side effects.
- Weight-Directed Dosage:
- For children and adolescents, the starting dose is 240 milligrams per kilogram per day, divided into three doses.
- The dose should be adjusted based on the individual's response, but the maximum daily dose should not exceed 8 grams.
Cholestyramine resin dose in Pruritus secondary to cholestasis:
Children ≤10 years old:
- Start with 240 milligrams per kilogram per day, divided into 2 or 3 doses.
- Give the doses in the morning around breakfast and, if needed, a third dose at lunch.
- The dose can be adjusted based on how effective it is. Some experts suggest a maximum daily dose of 4 grams, but higher doses up to 6.6 grams have been used in children under 10. Higher doses may cause increased fat in the stool (steatorrhea), which might require reducing the dose.
Children >10 years old and Adolescents:
- Start with 240 milligrams per kilogram per day, given in the morning before breakfast.
- The dose can be adjusted based on how effective it is. Some experts suggest a maximum daily dose of 8 grams. However, adult guidelines recommend starting with 4 grams per day and increasing up to 16 grams per day if needed. Higher doses may also lead to increased fat in the stool, requiring a dose reduction.
Cholestyramine resin Diarrhoea secondary to intestinal failure and short-bowel syndrome:
Children and Adolescents:
- Oral: Start with 240 milligrams per kilogram per day, divided into three doses.
- The maximum daily dose suggested is 8 grams per day, but it's important to note that there haven't been completed trials in pediatric patients for this specific use.
- Some experts recommend avoiding the use of cholestyramine resin for this purpose at this time due to limited data.
Pregnancy Risk Factor C
- During pregnancy, it's normal for lipid levels to rise to support the baby's growth, but if they rise too much, doctors usually start with dietary changes.
- If more help is needed, they might suggest bile acid sequestrants like cholestyramine.
- Even though cholestyramine doesn't get absorbed into the body, it might affect how the body absorbs vitamins, so regular prenatal vitamins might not be enough.
Cholestyramine resin use during breastfeeding:
- Since cholestyramine isn't absorbed into the body, it's not likely to pass into breast milk.
- If a breastfeeding woman needs treatment for high cholesterol, bile acid sequestrants like cholestyramine can be an option, according to some sources.
- However, because it might affect how the body absorbs vitamins, it's essential to be cautious if considering it while breastfeeding, as per the manufacturer's recommendation.
Cholestyramine resin Dose in Renal disease:
- The manufacturer's instructions don't specify dosage adjustments for people with kidney problems, but it's important to be cautious if you have renal impairment.
- Cholestyramine could potentially lead to hyperchloremic acidosis, a condition where there's too much chloride in the blood.
Cholestyramine resin Dose in liver Disease:
- Dosage adjustments aren't typically needed for people with liver problems since cholestyramine isn't absorbed from the digestive system.
Cholestyramine resin Side effects:
- Cardiovascular:
- Edema
- Syncope
- Dermatologic:
- Skin rash
- Urticaria
- Perianal skin irritation
- Skin irritation
- Central nervous system:
- Fatigue
- Neuralgia
- Paresthesia
- Vertigo
- Headache
- Anxiety
- Dizziness
- Drowsiness
- Gastrointestinal:
- Biliary colic
- Constipation
- Anorexia
- Dental caries
- Dental discolouration
- Dental bleeding
- Abdominal pain
- Diarrhoea
- Diverticulitis
- Duodenal ulcer with haemorrhage
- Dysgeusia
- Flatulence
- Gallbladder calcification
- Dysphagia
- Eructation
- Gastric ulcer
- Hiccups
- Nausea
- Pancreatitis
- Rectal pain
- Melena
- Tongue irritation
- Dental erosion
- Vomiting
- Gastrointestinal haemorrhage
- Hemorrhoidal bleeding
- Steatorrhea
- Intestinal obstruction
- Endocrine & metabolic:
- Weight gain
- Weight loss
- Hyperchloremic metabolic acidosis
- Increased libido
- Respiratory:
- Asthma
- Dyspnea
- Wheezing
- Genitourinary:
- Diuresis
- Dysuria
- Hematuria
- Hepatic:
- Abnormal hepatic function tests
- Neuromuscular & skeletal:
- Back pain
- Myalgia
- Arthralgia
- Arthritis
- Osteoporosis
- Hematologic & oncologic:
- Hemorrhage
- Hypoprothrombinemia
- Prolonged prothrombin time
- Adenopathy
- Anemia
- Bruise
- Rectal hemorrhage
- Ophthalmic:
- Nocturnal amblyopia
- Uveitis
- Otic:
- Tinnitus
Contraindications to cholestyramine resin include:
- Cholestyramine shouldn't be used if someone has a hypersensitivity (allergic reaction) to bile acid sequestering resins or any part of the medication's formula.
Warnings & Precautions
Bleeding:
- Long-term use of cholestyramine, especially in high doses, might lead to bleeding issues.
- To help prevent this, doctors may recommend oral vitamin K therapy alongside cholestyramine treatment.
- Vitamin K plays a crucial role in blood clotting, so supplementing it can counteract the potential bleeding problems associated with cholestyramine use.
Constipation:
- Cholestyramine can cause constipation or make existing constipation worse.
- If a person has a history of constipation, doctors might start them on a lower dose to minimize this side effect.
- It's important to be aware that cholestyramine could worsen hemorrhoids, which are swollen veins in the rectum or anus.
Hypertriglyceridemia:
- Bile acid sequestrants like cholestyramine shouldn't be used in patients with high baseline fasting triglyceride levels of 300 mg/dL or higher or in those with type III hyperlipoproteinemia, as they can lead to severe elevations in triglyceride levels.
- If a patient's triglyceride levels are between 250 to 299 mg/dL, caution is advised when using bile acid sequestrants, and a follow-up lipid panel should be done within 4 to 6 weeks after starting treatment.
- If triglyceride levels exceed 400 mg/dL, the use of bile acid sequestrants should be discontinued.
Renal impairment:
- It's important to be cautious when using cholestyramine in patients with renal impairment, which means their kidneys aren't functioning as well as they should.
Cholestyramine resin: Drug Interaction
Note: Drug Interaction Categories:
- Risk Factor C: Monitor When Using Combination
- Risk Factor D: Consider Treatment Modification
- Risk Factor X: Avoid Concomitant Use
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Risk Factor C (Monitor therapy) |
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Cardiac Glycosides |
Cardiac Glycosides may not be as readily absorbed while using bile acid sequestrants. |
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Corticosteroids (Oral) |
The absorption of corticosteroids may be decreased by bile acid sequestrants (Oral). |
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The absorption of methotrexate may be reduced by bile acid sequestrants. |
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Methylfolate serum levels may be decreased by cholestyramine resin. |
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Propranolol |
Bile Acid Sequestrants may lower the level of propranolol in the serum. |
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The harmful or toxic effects of spironolactone may be amplified by cholestyramine resin. In particular, this combination may increase the risk of developing metabolic acidosis and hyperkalemia. |
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Vitamin K Antagonists (eg, warfarin) |
Bile Acid Sequestrants may decrease the absorption of Vitamin K Antagonists. |
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Risk Factor D (Consider therapy modification) |
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The bioavailability of amiodarone may be decreased by bile acid sequestrants. |
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Chenodiol's serum levels may drop if bile acid sequestrants are used. Treatment: Chenadol administration five or more hours following bile acid sequestrants may decrease chenodiol absorption in the digestive system. In patients taking bile acid sequestrants, keep an eye out for any diminished therapeutic benefits of chenodiol. |
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Cholic Acid |
Bile Acid Sequestrants could make it harder for choline to be absorbed. To reduce the likelihood of a substantial interaction, provide cholic acid at least 1 to 4 hours before or 4 to 6 hours after administering any bile acid-binding products. |
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The serum concentration of Deferasirox may be lowered by bile acid sequestrants. Management: If a combination must be used, consider increasing the first deferasirox dose by 50% and using clinical responses and monitoring of serum ferritin concentrations to direct future dosing. |
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Estrogen Derivatives (Contraceptive) |
Bile Acid Sequestrants could lower the level of Estrogen Derivatives in the serum (Contraceptive). Treatment: Give bile acid sequestrants at least 1 to 4 hours before or 6 to 8 hours after giving estrogen-based oral contraceptives. |
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Bile Acid Sequestrants could make it harder for ezetimibe to be absorbed. Ezetimibe should be used at least two hours before or four hours after using any bile acid sequestrant. |
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Fibric Acid Derivatives |
Fibric Acid Derivatives' ability to be absorbed may be reduced by bile acid sequestrants. Treatment: To reduce this interaction, separate doses by at least 2 hours; the labelling for fenofibric acid advises administration one hour before or 4-6 hours after a bile acid sequestrant. |
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Fluvastatin serum levels may be reduced by cholestyramine resin. To reduce the possibility of any significant interactions, fluvastatin should be taken at least 1 hour or more (especially when taken in extended-release form) before or at least 4 hours after cholestyramine. |
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Leflunomide |
The active metabolite(s) of leflunomide may be present in lower serum concentrations when using bile acid sequestrants. Management: When feasible, look for alternatives to the bile acid sequestrants unless you're utilising this combination to specifically increase leflunomide elimination. It is unlikely that segregating drug administration will be successful in preventing this interaction. |
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Lomitapide |
The absorption of lomitapide may be decreased by bile acid sequestrants. Treatment: Give lomitapide at least 4 hours before or following bile acid sequestrant administration. |
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Loop Diuretics |
Loop Diuretics' ability to be absorbed may be decreased by bile acid sequestrants. |
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Multivitamins/Fluoride (with ADE) |
Fluoride and multivitamin serum concentrations may be reduced by bile acid sequestrants (with ADE). Avoid administering bile acid sequestrants and multivitamins at the same time for management (eg, cholestyramine). Separate these medications' delivery by several hours to reduce the possibility of an interaction. |
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Multivitamins/Minerals (with ADEK, Folate, Iron) |
Minerals and multivitamin serum concentrations may be lowered by bile acid sequestrants (with ADEK, Folate, Iron). Bile acid sequestrants in particular may hinder the absorption of fat-soluble vitamins. Avoid administering bile acid sequestrants and multivitamins at the same time for management (eg, cholestyramine). Separate these medications' delivery by several hours to reduce the possibility of an interaction. |
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Multivitamins/Minerals (with AE, No Iron) |
Minerals and multivitamin serum concentrations may be lowered by bile acid sequestrants (with AE, No Iron). Avoid administering bile acid sequestrants and multivitamins at the same time for management (e.g., cholestyramine). Separate these medications' delivery by several hours to reduce the possibility of an interaction. |
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Niacin |
Niacin absorption may be decreased by bile acid sequestrants. |
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Nonsteroidal Anti-Inflammatory Agents |
Nonsteroidal Anti-Inflammatory Drugs' absorption may be reduced by bile acid sequestrants. |
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The serum concentration of obeticholic acid may drop in response to bile acid sequestrants. Treatment: Give obeticholic acid at least four hours before or four hours after giving bile acid sequestrants. |
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PHENobarbital |
Cholestyramine Resin may lower the level of PHENobarbital in the blood. To reduce the chance of any major interactions, provide phenobarbital at least one hour before or four to six hours after giving cholestyramine. |
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Pravastatin |
Pravastatin's serum levels may drop if bile acid sequestrants are used. To reduce the chance of any significant interactions, provide pravastatin at least 1 hour before or 4 hours after administering bile-acid resins (such as cholestyramine, colestipol, and colesevelam). |
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Progestins (Contraceptive) |
The serum concentration of progesterone may be lowered by bile acid sequestrants (Contraceptive). Treatment: Give oral contraceptives containing progestin at least one to four hours before or six to eight hours after taking a bile acid sequestrant. |
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Raloxifene absorption may be decreased by bile acid sequestrants. |
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The serum concentration of Rosiglitazone may drop if you take cholestyramine resin. To lessen the possibility of an interaction, rosiglitazone should be given at least two hours before cholestyramine. Patients should also be closely watched for signs of diminished rosiglitazone efficacy. |
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The therapeutic benefit of Sincalide may be reduced by medications that affect gallbladder function. Prior to using sincalide to induce gallbladder contraction, you should think about stopping any medications that can impair gallbladder motility. |
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Teriflunomide |
Teriflunomide's serum levels may drop if bile acid sequestrants are used. Management: When feasible, look for alternatives to the bile acid sequestrants, unless you're using this combination to deliberately increase teriflunomide elimination. The interaction is unlikely to be prevented by separating medication administration. |
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Tetracyclines |
Tetracyclines' ability to be absorbed may be reduced by bile acid sequestrants. Eravacycline is an exception. |
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Thiazide and Thiazide-Like Diuretics |
Thiazide and Thiazide-Like Diuretics may be less readily absorbed when bile acid sequestrants are used. Also reduced is the diuretic reaction. |
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Thyroid Products |
Bile Acid Sequestrants may lower the level of thyroid products in the blood. Treatment: Give oral thyroid medications at least 1 hour before or 4-6 hours after cholestyramine and at least 4 hours before colestipol. There are no recommendations for colestipol in particular. Keep an eye out for any changes in the thyroid product's effects or concentrations. |
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Ursodiol's serum levels may drop if bile acid sequestrants are used. To reduce the possibility of any major interactions, provide ursodiol 2 to 4 hours before or at least 2 to 5 hours after bile acid sequestrants. Keep an eye out for any diminished ursodiol therapeutic benefits in patients receiving bile acid sequestrants. |
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Valproic Acid and Derivatives |
Cholestyramine The serum content of valproic acid and its derivatives may drop as a result of resin. Management: To reduce the possibility of a significant interaction, provide valproic acid and cholestyramine at least 3 hours apart whenever feasible. |
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Vancomycin |
Bile Acid Sequestrants may reduce the effectiveness of vancomycin as a treatment. Management: Whenever feasible, avoid giving oral vancomycin and bile acid sequestrants at the same time. If both medications must be used, think about giving the dosages at least two hours apart to lessen the impact of the interaction. |
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Vitamin D Analogs |
Bile Acid Sequestrants may lower the level of Vitamin D Analogs in the blood. Bile acid sequestrants specifically may hinder the absorption of vitamin D analogues. Avoid administering bile acid sequestrants and vitamin D analogues at the same time for management (eg, cholestyramine). To reduce the chance of interaction, provide these drugs many hours apart. track the levels of calcium in the plasma. Calcipotriene, calcitriol (Topical), and tacalcitol are exceptions. |
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Risk Factor X (Avoid combination) |
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Mycophenolate |
Cholestyramine Resin may lower the level of mycophenolate in the blood. |
Monitoring Parameters:
Before Treatment:
- Get a lipid profile test, whether fasting or nonfasting, before starting treatment for high cholesterol.
During Treatment:
- Check a fasting lipid profile 4 to 12 weeks after starting therapy.
- After that, continue to monitor with lipid profile tests every 3 to 12 months.
How to administer cholestyramine resin?
Prepared Suspension:
- Administer the prepared suspension orally.
- Do not take cholestyramine in its dry form.
- Avoid sipping or holding the suspension in the mouth for too long, as it may cause tooth discoloration or enamel decay.
Timing of Administration:
- It's recommended to take cholestyramine at mealtime.
- While twice-daily dosing is suggested, it can be taken in 1 to 6 doses throughout the day.
Mechanism of action of cholestyramine resin:
- Cholestyramine works by creating a nonabsorbable mix with bile acids in the gut, releasing chloride ions in the process.
- This action stops the reabsorption of bile salts in the intestine, which leads to more bile salt-bound low-density lipoprotein cholesterol being excreted in the feces.
Onset and Peak Effect:
- Onset of Action: Cholestyramine's effects typically start to show over time.
- Peak Effect: The maximum impact is usually reached around 21 days after starting treatment.
Absorption and Excretion:
- Absorption: Cholestyramine isn't absorbed by the body.
- Excretion: It's eliminated primarily through the feces, forming insoluble complexes with bile acids.
Cholestyramine International Brand Names:
- Cholestyramine-ODAN
- Questran
- Questran Light
- Questran Lite
- DOM-Cholestyramine
- NOVO-Cholamine
- Novo-Cholestyramine Light
- Olestyr
- Olestyr Light
- Choles
- Cholestran
- Colestiramina
- Olipo
- Lipramina
- Zuckerfrei
- Quantanash
- Quantalan
- Quantalan
- Colestrol
- Efensol
- Kolestran
- Questran Loc
- Resincolestiramina
- Semide
- Sequest
- Vasosan P-Granulat
- Vasosan S-Granulat
Cholestyramine brands in Pakistan:
Questran sachet (4.0 gms per sachet) - Bristol-Myers Squibb
