Cholestyramine

Drug Overview

Cholestyramine is a medication used to regulate blood lipids, primarily classified as an anion exchange resin. It works by binding to bile acids in the intestine, promoting the metabolism and excretion of cholesterol, and is used to treat primary hyperlipidemia and familial hypercholesterolemia.

This drug effectively reduces low-density lipoprotein cholesterol (LDL-C, known as "bad cholesterol") in the blood, usually as an adjunct to dietary control and lifestyle modifications. Its mechanism of action differs from that of statins and is often combined with other lipid-lowering agents to enhance efficacy.

Brand Names and Generic Name

Common brand names include:

  • Questran
  • Prevalite
The generic name is simply "Cholestyramine".

Drug Classification

It belongs to the categories of "Cholesterol Absorption Inhibitors" and "Anion Exchange Resins." Its action occurs within the gastrointestinal tract and does not directly affect hepatic metabolic pathways, distinguishing it from statins.

Indications

Primarily used to treat primary hypercholesterolemia, especially in patients with elevated LDL-C levels. Suitable for patients who do not meet lipid targets after dietary and lifestyle modifications or who are on combination therapy with other lipid-lowering drugs.

In specific cases, it can also be used to treat pruritus caused by liver disease or as an emergency treatment for excessive mineral absorption (e.g., lead poisoning).

Common Side Effects

Mild side effects include:

  • Bloating, diarrhea, nausea
  • Constipation or gastrointestinal discomfort
These symptoms usually resolve after adaptation; if persistent, consult a physician.

Severe side effects requiring immediate medical attention include:

  • Abnormal liver function (e.g., jaundice, dark urine)
  • Signs of intestinal obstruction (severe abdominal pain, vomiting)
If these symptoms occur, stop medication immediately and seek medical assistance.

Warnings and Precautions

Contraindications: Not to be used in individuals allergic to the drug components, or with intestinal obstruction. Patients with severe liver dysfunction or gastrointestinal diseases should use with caution.

Pregnancy category C; use during pregnancy or lactation should be evaluated by a healthcare provider. Regular monitoring of liver function and lipid levels is recommended during therapy to ensure safety and efficacy.

Drug Interactions

This medication may affect the absorption of other drugs, such as:

  • Statins (e.g., Atorvastatin), taken at different times
  • Oral contraceptives, thyroid hormones
  • Fat-soluble vitamins (A, D, E, K)
It is recommended to separate the administration of other drugs by 4-6 hours from Cholestyramine.

When used with digoxin (e.g., Digoxin), it may reduce absorption efficiency, requiring dose adjustments. Always inform your healthcare provider of all medications and supplements you are taking.

Dosage and Administration

Usually supplied as a powder that must be mixed with water or other liquids to form a suspension. The starting dose is often 4-12 grams daily, divided into 2-3 doses, with specific doses adjusted by the physician based on lipid targets.

It is recommended to take with meals or after eating, possibly with juice or milk to reduce gastrointestinal discomfort. Do not swallow the powder directly; it must be fully dissolved before ingestion. Continuous monitoring of blood lipid levels is necessary during treatment.

Missed Dose Management

If a dose is missed, take it as soon as remembered; if close to the next dose, skip the missed dose and resume the regular schedule. Do not double doses to make up for missed ones.

If long-term missed doses lead to poor lipid control, discuss with your doctor to adjust the treatment plan and avoid self-modification of doses.

Overdose Management

Overdose may cause severe gastrointestinal discomfort, weakness, and other symptoms. If overdose is suspected, seek immediate medical attention and bring the medication packaging for reference.

Medical interventions may include gastric lavage or administration of activated charcoal to adsorb unabsorbed drug components. Severe cases may require hospitalization for monitoring liver and kidney functions.

Frequently Asked Questions

Q: How can I avoid drug interactions when taking Cholestyramine?

A: Cholestyramine may adsorb other oral medications, reducing their absorption. It is recommended to separate the administration times of Cholestyramine and other drugs by at least 4 to 6 hours and follow your healthcare provider’s instructions regarding the order of taking medications. Special attention should be paid when using thyroid hormones or warfarin, with monitoring of blood concentrations.

Q: What should I do if I experience bloating or constipation while taking Cholestyramine?

A: These side effects may be due to increased water absorption in the intestines. Increasing dietary fiber intake (such as whole grains and vegetables) and drinking more than 2000 ml of water daily can help. If symptoms persist, your doctor may adjust the dose or prescribe laxatives. Seek medical attention if symptoms worsen.

Q: Does Cholestyramine affect the absorption of oral contraceptives?

A: Yes, Cholestyramine may reduce the absorption of oral contraceptives. If used concurrently, take the two at least 4 hours apart and consult your healthcare provider about additional contraceptive measures. Using other methods such as condoms is recommended to ensure effectiveness.

Q: What dietary precautions should I take while on Cholestyramine?

A: Avoid taking mineral supplements (such as iron or calcium tablets) or plant sterol preparations simultaneously; it is best to separate these by at least 2 hours. You can consume high-fiber foods normally but should drink sufficient water in multiple doses to reduce gastrointestinal discomfort. If you are using fish oil or vitamin supplements, inform your doctor to adjust the timing of medication.

Q: Is regular liver function testing necessary during long-term use of Cholestyramine?

A: Although this medication primarily affects intestinal absorption, it is recommended to check liver function every 6 to 12 months during long-term use. If jaundice, dark urine, or right upper quadrant pain occurs, stop the medication immediately and seek medical attention. Your healthcare provider will adjust your treatment plan based on lipid control and liver function results.

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