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:
-
- 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 Dose in Adults
Cholestyramine Dosage:
Cholestyramine does in dyslipidemia (in patients not achieving the target lipids with the maximally tolerated dose of statins and ezetimibe):
- Orally, take 4 gm once or twice per day.
- The dosage can be gradually increased to the maximum dose of 24 g/day and the typical maintenance dose of 8 to 16 g/day.
Off-label use in the treatment of chronic diarrhoea due to bile acid malabsorption:
- Once a day, 4 gms.
- To reach the maximum dose of 36 gms/day in one to four split doses, the dose may be raised by 4 gms monthly.
Off-label use in the adjunctive therapy of Hyperthyroidism due to Graves disease:
- 4 gms twice or thrice daily in combination with beta-blockers and anti-thyroid drugs.
Pruritus associated with cholestasis:
- 4 gms once or twice a day.
- The dose may be increased to 16 gms per day in two divided doses.
Cholestyramine Dose in Children
Cholestyramine does in Diaper dermatitis:
-
Infants and Children:
- Apply 5% to 10% of an Aquaphor, polyethene glycol, or petrolatum topical paste or ointment to the afflicted region after each diaper change.
Dose in Dyslipidemia:
- Children older than 6 years and Adolescents:
- 2 - 4 gms/day for one week to a maximum dose of 8 gms per day.
- Children and Adolescents:
- 240 mg/kg/day orally in three divided doses to the maximum daily dose of 8 gms/day.
Pruritus secondary to cholestasis:
- Children less than 10 years:
- 240 mg/kg/day in two or three divided doses administered after meals to a maximum daily dose of 4 g/day.
- Children older than 10 years and Adolescents:
- 240 mg/kg/day orally to a maximum daily dose of 8 g/day.
Diarrhoea secondary to intestinal failure and short-bowel syndrome:
- Children and Adolescents:
- 240 mg/kg/day split into three doses, with a daily dosage cap of 8 gm.
Pregnancy Risk Factor C
- It may be used in pregnant patients when required.
- Lipid profile should be monitored during therapy.
- Pregnant patients should also be given supplemental vitamin K.
Cholestyramine resin use during breastfeeding:
- Since it is not systemically absorbed, it does not affect the breastfeeding infant.
- However, it may result in vitamins deficiency in the mother that may require supplementation.
Cholestyramine Dose in Renal disease:
- The manufacturer has not recommended any dose adjustment, however, it should be used with caution in patients with renal impairment.
- It may also cause hyperchloremic metabolic acidosis, especially in children.
Cholestyramine Dose in liver Disease:
- Dose adjustment is not necessary as it is not absorbed from the gastrointestinal tract.
Cholestyramine 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:
- Allergic reactions to the drug or any component of the formulation
- Biliary obstruction
Warnings & Precautions
- Bleeding:
- Prolonged therapy may result in vitamin K deficiency. This can cause bleeding problems.
- Vitamin K supplementation may be necessary.
- Constipation:
- It should be initiated in a low dose as it may cause constipation and worsen hemorrhoids.
- Hypertriglyceridemia:
- Cholestyramine should be avoided in patients with baseline fasting triglyceride levels of more than 300 mg/dL or type III hyperlipoproteinemia as severe triglyceride elevations may occur.
- Patients with triglyceride levels of 250 - 299 mg/dL should use it with caution and get the levels rechecked after 4 - 6 weeks of therapy.
- Treatment should be discontinued if the triglyceride levels are more than 400 mg/dl.
- Renal impairment:
- Patients with renal impairment should use the drug with caution.
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
Risk Factor C (Monitor therapy) |
|
| Cardiac Glycosides | Cardiac Glycosides may not be as readily absorbed while using bile acid sequestrants. |
| Corticosteroids (Oral) | The absorption of corticosteroids may be decreased by bile acid sequestrants (Oral). |
| Methotrexate | The absorption of methotrexate may be reduced by bile acid sequestrants. |
| Methylfolate | Methylfolate serum levels may be decreased by cholestyramine resin. |
| Propranolol | Bile Acid Sequestrants may lower the level of propranolol in the serum. |
| Spironolactone | 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. |
| Vitamin K Antagonists (eg, warfarin) | Bile Acid Sequestrants may decrease the absorption of Vitamin K Antagonists. |
Risk Factor D (Consider therapy modification) |
|
| Amiodarone | The bioavailability of amiodarone may be decreased by bile acid sequestrants. |
| Chenodiol | 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. |
| 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. |
| Deferasirox | 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. |
| 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. |
| Ezetimibe | 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. |
| 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. |
| Fluvastatin | 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. |
| 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. |
| 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. |
| Loop Diuretics | Loop Diuretics' ability to be absorbed may be decreased by bile acid sequestrants. |
| 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. |
| 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. |
| 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. |
| Niacin | Niacin absorption may be decreased by bile acid sequestrants. |
| Nonsteroidal Anti-Inflammatory Agents | Nonsteroidal Anti-Inflammatory Drugs' absorption may be reduced by bile acid sequestrants. |
| Obeticholic Acid | 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. |
| 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. |
| 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). |
| 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. |
| Raloxifene | Raloxifene absorption may be decreased by bile acid sequestrants. |
| Rosiglitazone | 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. |
| Sincalide | 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. |
| 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. |
| Tetracyclines | Tetracyclines' ability to be absorbed may be reduced by bile acid sequestrants. Eravacycline is an exception. |
| 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. |
| 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. |
| Ursodiol | 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. |
| 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. |
| 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. |
| 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. |
Risk Factor X (Avoid combination) |
|
| Mycophenolate | Cholestyramine Resin may lower the level of mycophenolate in the blood. |
Monitoring Parameters:
- Before beginning therapy, 4–12 weeks into it, and then every 3–12 months after that, a lipid profile checkup is recommended.
How to administer cholestyramine resin?
- It is administered as an oral suspension when prepared.
- The powder should not be ingested directly, snipped, or held in the mouth for a prolonged period of time (as it may result in tooth decay and discolouration).
- It should be administered with meals twice daily.
Mechanism of action of cholestyramine resin:
- It increases the excretion of bile salts via faeces by inhibiting its reuptake.
- By forming a nonabsorbable combination with bile acids in the colon, it increases the excretion of low-density lipoprotein cholesterol that is bound to bile salts.
The peak effect of cholestyramine is seen in about three weeks. It is not absorbed when ingested orally and is excreted via faeces as an insoluble complex 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
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