Colesevelam Hydrochloride - Dosage, Uses, and Side Effects

What Is Colesevelam Hydrochloride?

Colesevelam hydrochloride belongs to a medicine class that is the same as the resins of our bile acids. It was approved by both the United States Food and Drug Administration (US FDA) in 2000 and by the European Medicines Agency (EMA) in 2004 for medical use.

This medicine can lower our low-density lipoprotein cholesterol (LDL-C) level. It is often used in combination with other medicines to lower cholesterol and triglyceride levels. Also, it is effective in sugar control. That is why both the US FDA and the EMA have approved this medicine for various uses.

How Does Colesevelam Hydrochloride Work?

Colesevelam hydrochloride is a bile acid sequestrant. These are nothing but bile acid resins. They attach to bile acids in our gastrointestinal tract. Upon its attachment, it prevents the reabsorption of bile acid into the system. Bile acids are not absorbed into the bloodstream, forcing the liver to produce more. This increases the secretion of liver enzyme 7-alpha-hydroxylase. As a result, LDL receptors are activated, leading to increased cholesterol uptake for bile acid production. This lowers blood cholesterol levels and reduces the risk of heart disease.

What Are the Approved Uses of Colesevelam Hydrochloride?

• Adult patients suffer from a high level of lipid in their blood, often due to primary hyperlipidemia. Colesevelam hydrochloride decreases LDL-C and lowers the lipid level.

• It can also be used in heterozygous familial hypercholesterolemia (high cholesterol level in the blood) in boys and postmenarchal girls of 10 to 17 years of age as a monotherapy or in combination with a statin.

• It is indicated in patients with coronary heart disease (CHD) (cholesterol deposits in the walls of the major blood vessels of the heart) or the presence of CHD risk factors.

• In type 2 diabetes, it helps control blood glucose levels via glycemic control.

• Irritable bowel syndrome often leads to diarrhea or constipation. Colesevelam hydrochloride can improve stool consistency in such cases.

What Are the Contraindications of Colesevelam Hydrochloride?

• If you have type 1 diabetes or suffer from diabetic ketoacidosis, you should not take Colesevelam hydrochloride.

• It is not recommended for children below ten or premenarchal girls. Children or premenarcheal girls should not take these.

• Colesevelam hydrochloride has not been studied in individuals with type 2 diabetes as monotherapy or in combination with a dipeptidyl peptidase IV inhibitor or thiazolidinediones, or in patients with Fredrickson type (Type I, III, IV, and V) dyslipidemias (increased triglycerides).

• If you have gut issues like bowel obstructions or pancreatitis, you should not take this medication. Also, this medicine is not indicated in cases where triglycerides are too high, 500 mg/dL (milligrams per deciliter).

What Are the Doses and Dose Forms?

Colesevelam hydrochloride is available as 625 mg (milligrams) tablets and as a powder for oral suspension in single-dose packets of 3.75 grams or 1.875 grams.

The recommended dose of Colesevelam hydrochloride is:

• As monotherapy or in combination with a statin, six tablets of Colesevelam hydrochloride must be taken once or three tablets twice daily with food.

• Oral suspension must be prepared by emptying the entire contents of one packet into a cup or glass. About half to one cup of water (4 to 8 ounces), fruit juice, or any diet soft drinks are added and stirred well; this mixture must be taken with meals. Colesevelam hydrochloride can be taken at the same time as a statin, or both drugs can be dosed apart. Oral suspension powder must not be consumed in its dry form, as it can cause esophageal distress. Oral suspension can also be recommended for patients having difficulty swallowing the tablet due to its size.

• Colesevelam hydrochloride must be taken regularly and exactly as prescribed by the doctor. However, if a dose is missed, it must be taken as soon as it is remembered; if it is almost time for the next dose, the missed dose can be skipped, and the regular dosing schedule must be followed. A double dose must not be taken to make up for a missed dose.

For Patients

How Should Colesevelam Hydrochloride Be Taken?

• You can take Colesevelam hydrochloride tablets orally once or twice daily as prescribed with food.

• The chewable bars or oral suspension are also available, which must be taken daily with a meal.

• You can also take it in powder form. You can mix the powder with 8 ounces of water or fruit juice, then stir well. The mixture must be consumed immediately.

What Are the Side Effects of Colesevelam Hydrochloride?

Some of the side effects of Colesevelam hydrochloride include:

• Nausea and vomiting.

• Acidity, which can lead to heartburn and chest pain.

• Diarrhea.

• Abdominal pain.

• Constipation.

• Muscle pain.

• Headache.

• Weakness.

What Must the Patient Inform the Doctor Before Taking Colesevelam Hydrochloride?

• Before starting the treatment, patients must tell the doctor if they are allergic to Colesevelam hydrochloride, its components, or other medications.

• Situations like pregnancy, breastfeeding, or pregnancy planning must be discussed with your doctor before taking Colesevelam hydrochloride.

• Patients must inform the healthcare provider if they take Cyclosporine, oral contraceptives, vitamins or herbal supplements, over-the-counter (OTC) drugs, or any other medications before taking Colesevelam hydrochloride.

What Are the Precautions for Colesevelam Hydrochloride?

• If you have, or have had, a blockage in the stomach or intestine, swelling of the pancreas, any digestive problems, or high triglyceride levels, you must tell your doctor before starting treatment with Colesevelam hydrochloride.

• Before starting the treatment, you must inform the doctor if you have had any gastrointestinal surgery, problems with swallowing, or other stomach problems.

• Patients with phenylketonuria (increased levels of phenylalanine in the blood) must be aware that the oral suspension powder contains Aspartame, which forms phenylalanine.

• During the treatment with Colesevelam hydrochloride, you must exercise daily. Also, your diet must be healthy with low fat and cholesterol.

What Are the Dietary Considerations?

During treatment with Colesevelam hydrochloride, a low-fat, low-cholesterol diet and other doctor-recommended diets must be followed, along with regular exercise.

For Doctors

What Are the Pharmacological Aspects of Colesevelam Hydrochloride?

Pharmacodynamics

The maximum therapeutic response to lipid-lowering therapy with Colesevelam hydrochloride was achieved within 2 weeks of treatment and was maintained during long-term therapy. In diabetes clinical studies, a reduction in hemoglobin A1C was observed as a therapeutic response. It was observed that after 4 to 6 weeks of treatment, it reached a maximum at 12 to 18 weeks.

Pharmacokinetics

• Absorption:

Colesevelam hydrochloride is a hydrophilic, water-insoluble polymer that is not hydrolyzed by digestive enzymes; hence, it is not absorbed.

• Distribution:

As Colesevelam hydrochloride is not absorbed, its distribution to the gastrointestinal tract (GIT) is limited.

• Metabolism:

Colesevelam hydrochloride is not metabolized in the body and does not interfere with systemic enzymes such as cytochrome P-450.

• Excretion:

In healthy volunteers, approximately 0.05 percent of Colesevelam hydrochloride (a single C-labelled radioactive) administered was excreted in the urine.

Drug Interactions

Colesevelam hydrochloride can interact with certain drugs; therefore, close monitoring is required.

These include:

• Cyclosporine.

• Levothyroxine.

• Metformin.

• Glimepiride.

• Norethindrone.

• Levonorgestrel.

• Olmesartan.

• Phenytoin.

• Vitamin D.

• Warfarin.

What Are the Considerations for Colesevelam Hydrochloride Treatment?

• Pregnancy:

Some reports say Colesevelam hydrochloride can harm the unborn baby in the womb. As a result, it should be used cautiously during pregnancy and only when needed.

• Lactation:

Colesevelam hydrochloride is not excreted in breast milk, as it is not absorbed from the gastrointestinal tract. So it can be used by breastfeeding mothers.

• Pediatric Use:

Do not use this medicine for children below ten years of age and pre-menarchal girls.

• High Triglyceride:

Colesevelam hydrochloride can increase serum triglyceride levels; therefore, care must be taken when treating patients with triglyceride levels above 300 mg/dL. Triglyceride and non-HDL-C levels must be obtained before treatment begins and periodically thereafter. Colesevelam hydrochloride must be discontinued if patients develop hypertriglyceridemia-induced pancreatitis if triglyceride levels increase more than 500 mg/dL.

• Gastric Issues:

Colesevelam hydrochloride is not recommended in patients with gastrointestinal motility disorders or gastroparesis, as it can delay gastric emptying. Also, patients with abdominal surgery should not take it. Also, it should not be taken if you have swallowing issues or problems with food intake.

• Vitamins:

This medicine impairs the absorption of fat-soluble vitamins, such as A, D, E, and K. Therefore, patients taking oral supplements must take them at least 4 hours before Colesevelam hydrochloride. Care must be taken in patients prone to vitamin K deficiencies and malabsorption syndromes, as well as patients on Warfarin.

• Cardiovascular Issues:

The effect of Colesevelam hydrochloride on cardiovascular conditions has not been adequately studied.

Drug Absorption:

Colesevelam hydrochloride has the potential to reduce the gastrointestinal absorption of certain drugs. Therefore, drugs that interact with Colesevelam hydrochloride or those with a narrow therapeutic index must be administered 4 hours before, or the doctor must monitor the levels of the co-administered drug.

Phenylketonuria:

Care must be taken when recommending Colesevelam hydrochloride in people with phenylketonuria (PKU), as the oral suspension contains 24 mg of phenylalanine per 1.875 g and 48 mg per 3.75 g packets.

Conclusion

Colesevelam hydrochloride is a bile acid resin that belongs to the bile acid sequestrant. It binds to bile acids and activates our liver enzymes. This lowers blood cholesterol levels. It is used in conditions like primary hyperlipidemia and heterozygous familial hypercholesterolemia. Apart from this, it helps in glycemic control in type 2 diabetes. However, if you have gut issues, you should not take this. If you have any queries, you can consult a heart health physician for further guidance.

Key Takeaways

1. Colesevelam hydrochloride is a bile acid sequestrant.

2. It helps to lower the cholesterol and low-density lipoprotein cholesterol levels in the blood.

3. It is used in primary hyperlipidemia, type 2 diabetes, and heterozygous familial hypercholesterolemia.