Cholestyramine is a drug that is mainly prescribed to lower cholesterol levels. However, due to its effects on bile acids, it is sometimes used as an off-label treatment for chronic diarrhea .
It belongs to a class of drugs known as bile acid binders, or sequestrants, and works by binding with bile acids in the digestive tract to leave the body. Cholestyramine is available as a generic drug and is usually available as a powder that can be added to drinks.
Trademarks of cholestyramine
- Weaker light
- Questran Light
If you have high cholesterol, this reduction in bile acids from cholestyramine causes your body to convert cholesterol to bile acids, which lowers blood cholesterol.
Cholestyramine is used in conjunction with dietary changes to lower low-density lipoprotein (LDL) cholesterol . It is also called "bad" cholesterol because it increases the risk of heart disease.
Cholestyramine is also prescribed to relieve itching (itching) associated with partial biliary obstruction and high levels of bile acids in the skin.
Use not indicated on the label
If you have a condition known as bile acid diarrhea (BAD), also known as bile acid malabsorption (BAM), in which excess bile acids pass into the colon and cause loose, watery stools, the drug may reduce the diarrhea. symptoms .
Bile acids are produced in the liver and stored in the gallbladder. They are released to aid in the absorption of fat and fat-soluble vitamins. After this digestion process, most of the unbound bile acids are reabsorbed and sent to the liver for reuse; only a small portion passes through the intestines and colon.
In people with BAD, more bile acids travel to the colon, where they increase motor skills and stimulate water secretion, leading to diarrhea .
Cholestyramine may also be prescribed for Graves' disease , an autoimmune disease that leads to the overproduction of thyroid hormones. Cholestyramine has been used to treat people with Graves' disease with severe thyrotoxicosis, which is a high level of thyroid hormones in the blood.
The drug helps bind thyroid hormones in the intestines, increasing their excretion, which reduces the level of thyroid hormones in the blood.
Your healthcare provider may perform blood tests or stool samples for bile acids, or simply prescribe cholestyramine if BAM is suspected to see if it reduces or eliminates your diarrhea. There are four different BAM categories:
- Diseases of the ileum, including Crohn 's disease, which interferes with reabsorption of bile acids from the terminal ileum (the end of the small intestine that crosses the colon)
- Major malabsorptive diseases such as celiac disease or pancreatic diseases such as chronic pancreatitis
- Diarrhea-predominant irritable bowel syndrome (IBS-D) with no clear underlying cause
- Excessive bile acid synthesis, which can occur in people with hypertriglyceridaemia or high levels of fatty acids in the blood, or in those taking metformin , a diabetes medicine.
Although more research is needed, some research suggests that idiopathic BAM (I-BAM) may be common in a third of people with irritable bowel syndrome (IBS) who have recurrent diarrhea .
Precautions and contraindications.
Your healthcare provider will consider whether cholestyramine is right for you if you have the following conditions:
- Complete blockage of the bile ducts: Do not take this drug if you have a complete blockage of the bile ducts that prevents bile from flowing into the intestines.
- Phenylketonuria (PKU) : This drug contains the amino acid phenylalanine, which can be dangerous for people with inherited metabolic disorders of PKU, in which the body cannot fully break down phenylalanine.
- Low levels of vitamin K or folic acid : Chronic use of cholestyramine can interfere with your body's absorption of vitamin K, putting you at risk for increased bleeding from injury, and folate, vitamin B. Your healthcare provider may recommend that you take a supplement of these. vitamins if you are taking cholestyramine.
- Hyperchloremic acidosis : This medicine can cause high acid levels in the body or pH below 7.35, especially in children or young patients, who may receive a higher relative dose. Acidosis can also occur in people with poor kidney function or those who take diuretics.
- Pregnancy or breastfeeding : There are no adequate studies on the effects of cholestyramine in pregnant and lactating people. But because it interferes with the supply of fat-soluble vitamins, it can affect nutrition or milk production. The dose of prenatal vitamins may need to be adjusted.
- Intestinal obstruction : There are rare reports of intestinal obstruction in children, which can be life-threatening.
Cholestyramine comes in the form of a powder or gummies when taken to control cholesterol. A 4-7 gram (g) dose of the drug (often equivalent to 5-9 grams of powder) can be taken one to six times a day, as directed by your healthcare provider. The powder is supplied in cardboard boxes in individual bags or in cans with a portioned measuring spoon.
When taken for itching associated with partial biliary tract obstruction, a 4 g dose can be administered up to three times a day. Cholestyramine for diarrhea is usually given in a starting dose of 4 g per day, which can be increased to 4 g if necessary, taken two to four times a day.
For Graves' disease, 4 g can be given up to four times a day. Alternatively, a small dose of 1 to 2 g may be prescribed as adjunctive therapy in combination with other medications.
The dose for children will vary depending on body weight and symptoms, but usually does not exceed 8 g per day, divided into two or three doses, the amount of which depends on body weight.
How to take and store
Observe the following precautions:
- Always mix the powdered form with 2-6 ounces of non-carbonated liquids such as water, juice, or milk before using. You can also add it to foods rich in liquids like fruit purees or soups.
- Take this medicine before meals or at bedtime.
- Try to take other medications or vitamins at least 1 hour before or 4 hours after taking cholestyramine, as this can interfere with absorption.
- Store at room temperature, ideally 66 to 77 degrees Fahrenheit.
- If you are using a bar form, be sure to drink plenty of water.
- Do not forcibly pack the powder into a scoop to ensure you do not take more than the prescribed dose.
- Drink your medicine quickly instead of drinking slowly and brushing your teeth frequently. If the medicine is left in the mouth for a long time, it can cause discoloration, enamel erosion, or cavities.
- If you miss a dose, take it as soon as you remember; but if it is close to the next dose, skip it to avoid double doses.
Side effects are more common in people over the age of 60. Check with your healthcare professional if any of the side effects listed below are persistent or bothersome, or if you have any questions about them. Your healthcare provider can tell you about ways to prevent or reduce some of these side effects.
The most common side effects of cholestyramine are related to digestion and may go away as your body gets used to the medicine. They include:
- Abdominal discomfort or pain
The following side effects can also occur :
- Additional bleeding due to vitamin K deficiency.
- Lack of vitamin A or D
- Hyperchloremic acidosis, especially in children.
- Rash or irritation of the skin or tongue.
Seek medical attention if you have signs of an allergic reaction, such as hives, and call your doctor immediately if you experience:
- Rectal bleeding
- Severe abdominal pain
- Sudden weight loss
- Threw up
- Rectal bleeding or black stools
Warnings and interactions
Tell your doctor if you are pregnant, breastfeeding, or have any chronic health problems such as diabetes, kidney disease, heart disease, or blood vessel disease.
Cholestyramine can delay or reduce the absorption of other oral medications. Be sure to tell your doctor what other medications you are currently taking, for example:
- Oral contraceptive pills or hormone therapy
- Penicillin G
- Thyroid medications
- Oral phosphate supplements
- Thiazide diuretics
Frequently asked questions
Cholestyramine is a drug that helps lower cholesterol levels by binding to bile acids and excreting them in the stool. Cholesterol is necessary for the production of bile acids, and by removing them from the intestines, the body has to use more cholesterol to bring bile acid levels back to normal. This, in turn, lowers blood cholesterol levels.
Cholestyramine is used off-label to treat bile acid diarrhea (BAD). This is a form of diarrhea caused by the fact that bile acids are not reabsorbed after they have stopped breaking down fats. With dietary supplements, poor absorption of these acids causes watery diarrhea . By removing excess bile acids from the intestines, symptoms of diarrhea can be eliminated.
Cholestyramine is usually given in an initial dose of 4 grams per day and is increased to 4 grams, two to four times a day if necessary. In general, 4 grams twice a day is effective in eliminating dietary supplements.
When used at the recommended dosage, common side effects of cholestyramine include:
- Abdominal pain