Indications
Colesevelam Hydrochloride is used, together with diet and exercise, to lower high LDL cholesterol (the “bad” cholesterol) in adults with primary hyperlipidaemia. It can be used alone or with a statin. It is also used, with diet and exercise, to help control blood sugar in adults with type 2 diabetes.
How It Works
Colesevelam is a bile acid sequestrant. It stays inside the gut and binds bile acids, which are made from cholesterol in the liver. The bound bile acids leave the body in the stool, so the liver uses more cholesterol from the blood to make new bile acids, and LDL cholesterol falls. How it lowers blood sugar is not fully understood. It is not absorbed into the bloodstream.
Dosage and Administration
The usual adult dose for both cholesterol and type 2 diabetes is 3.75 g a day: six 625 mg tablets once a day, or three 625 mg tablets twice a day. Take with a meal and plenty of water. Swallow the tablets whole; they are large, so take them one at a time if needed. Follow your doctor’s instructions.
Interactions
Colesevelam can bind other medicines in the gut and reduce how much is absorbed. Take these at least 4 hours before colesevelam: Levothyroxine, Glibenclamide (Glyburide), Olmesartan, oral contraceptives containing Ethinylestradiol and Norethindrone, Phenytoin and Ciclosporin. If you take Warfarin, your INR should be checked more often. It may lower absorption of fat-soluble vitamins (A, D, E, K); take vitamin supplements at least 4 hours before. Metformin extended-release levels may rise slightly.
Contraindications
- History of bowel blockage (intestinal obstruction).
- Very high blood triglycerides (above 500 mg/dL).
- History of pancreatitis caused by high triglycerides.
- Allergy to colesevelam.
Side Effects
Common effects are constipation, indigestion, nausea, bloating and stomach discomfort. It may also raise triglyceride levels and, in people with diabetes, cause low blood sugar when used with other diabetes medicines.
Get urgent medical help if you have severe stomach pain, severe constipation with vomiting or inability to pass wind, trouble swallowing or a tablet stuck in the throat, or severe upper abdominal pain spreading to the back (possible pancreatitis).
Pregnancy and Lactation
Colesevelam is not absorbed into the blood, so it is not expected to reach the baby directly, but it may reduce absorption of vitamins needed in pregnancy. Use only if your doctor advises, and discuss vitamin supplements. It is not expected to pass into breast milk; ask your doctor before use while breastfeeding.
Precautions and Warnings
- Use with care if you have swallowing problems, severe constipation, stomach or bowel disorders, or have had major bowel surgery.
- Triglycerides should be checked before and during treatment.
- It is not a treatment for type 1 diabetes or diabetic ketoacidosis.
- Long-term use may lower vitamin K and other vitamins; report unusual bleeding or bruising.
Overdose
Because it is not absorbed, serious poisoning is unlikely, but too much may cause severe constipation or bowel blockage. Contact a doctor if a large amount has been taken.
Therapeutic Class
Bile acid sequestrant; lipid-lowering agent with blood sugar lowering effect.
Storage
Store below 30°C in a dry place, protected from moisture and light, out of the reach of children.
Prepared by the Oshud Alo team from standard drug references. For information only; always follow your doctor's advice.