CholestaGel
CholestaGel - General Information
CholestaGel is a bile acid sequestrant. CholestaGel is used with exercise and diet changes (restriction of cholesterol and fat intake) to reduce the amount of cholesterol and certain fatty substances in the blood. It works by binding bile acids in the intestine. Bile acids are made when cholesterol is broken down in the body. Removing these bile acids helps to lower blood cholesterol.
Pharmacology of CholestaGel
CholestaGel is a high capacity bile-acid binding molecule. CholestaGel binds to bile acids in the intestine which reduces the amount of bile acids that are returned to the liver via enterohepatic circulation. Clinical studies have demonstrated that elevated levels of total cholesterol (total-C), LDL-C, and apolipoprotein B (Apo B, a protein associated with LDL-C) are associated with an increased risk of atherosclerosis in humans. Similarly, decreased levels of high-density lipoprotein cholesterol (HDL-C) are associated with the development of atherosclerosis. Epidemiological investigations have established that cardiovascular morbidity and mortality vary directly with the levels of total-C and LDL-C, and inversely with the level of HDL-C. The combination of colesevelam and an HMG-CoA reductase inhibitor is effective in further lowering serum total-C and LDL-C levels beyond that achieved by either agent alone.
CholestaGel for patients
WelChol® may be taken once per day with a meal, or taken twice per day in divided doses with meals. Patients should be directed to take WelChol® with a liquid and a meal, and adhere to their NCEP-recommended diet. Patients should tell their physicians if they are pregnant, are intending to become pregnant, or are breastfeeding.
What is Welchol used for?
Welchol is used alone or with another drug to lower high levels of low-density lipoprotein (LDL) in the blood when response to diet and non-drug therapy is inadequate. Diet and exercise are very important factors to help control cholesterol.
Who should not take Welchol?
Do not take Welchol if you have a blockage of your intestinal tract
What does my doctor or health care provider need to know?
Tell your doctor or health care provider if you have:
- difficulty in swallowing, severe intestinal problems, or have had major abdominal surgery
- fat soluble vitamin deficiencies
- high triglyceride levels (> 300mg/dL)
- Indigestion
- Constipation
- Gas
CholestaGel Interactions
WelChol® has been studied in several human drug interaction studies in which it was administered with a meal and the test drug. WelChol® was found to have no significant effect on the bioavailability of digoxin, lovastatin, metoprolol, quinidine, valproic acid, and warfarin. WelChol® decreased the Cmax and AUC of sustained-release verapamil (Calan SR®) by approximately 31% and 11%, respectively. Since there is a high degree of variability in the bioavailability of verapamil, the clinical significance of this finding is unclear. In clinical studies, coadministration of WelChol® with atorvastatin, lovastatin, or simvastatin did not interfere with the lipid-lowering activity of the HMG-CoA reductase inhibitor. Other drugs have not been studied. When administering other drugs for which alterations in blood levels could have a clinically significant effect on safety or efficacy, physicians should consider monitoring drug levels or effects.
CholestaGel Contraindications
WelChol® is contraindicated in individuals with bowel obstruction and in individuals who have shown hypersensitivity to any of the components of WelChol®.
Additional information about CholestaGel
CholestaGel Indication: For use, alone or in combination with an HMG-CoA reductase inhibitor, as adjunctive therapy to diet and exercise for the reduction of elevated LDL cholesterol in patients with primary hypercholesterolemia (Fredrickson Type IIa).
Mechanism Of Action: CholestaGel is a non-absorbed, lipid-lowering polymer that binds bile acids in the intestine, impeding their reabsorption. As the bile acid pool becomes depleted, the hepatic enzyme, cholesterol 7-(alpha)-hydroxylase, is upregulated, which increases the conversion of cholesterol to bile acids. This causes an increased demand for cholesterol in the liver cells, resulting in the dual effect of increasing transcription and activity of the cholesterol biosynthetic enzyme, hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase, and increasing the number of hepatic low-density lipoprotein (LDL) receptors. These compensatory effects result in increased clearance of LDL cholesterol (LDL-C) from the blood, resulting in decreased serum LDL-C levels. Serum triglyceride levels may increase or remain unchanged. The end result is increased clearance of LDL-cholesterol from the blood with decreased serum LDL-cholesterol.
Drug Interactions: Not Available
Food Interactions: Take with a meal.
Drink liberally.
Generic Name: Colesevelam
Synonyms: Colesevelam hydrochloride
Drug Category: Bile acid sequestrants
Drug Type: Small Molecule; Approved
Other Brand Names containing Colesevelam: CholestaGel; Welchol;
Absorption: Not hydrolyzed by digestive enzymes and is not absorbed.
Toxicity (Overdose): Symptoms of overdose may include eye irritation, constipation, abdominal cramps, nausea, vomiting, diarrhea, and hypersensitivity. However, as colesevelam is not absorbed, the risk of systemic toxicity is low. Doses in excess of 4.5 g per day have not been tested.
Protein Binding: Not applicable (not hydrolyzed by digestive enzymes and not absorbed).
Biotransformation: Not applicable (not hydrolyzed by digestive enzymes and not absorbed).
Half Life: Not Available
Dosage Forms of CholestaGel: Tablet, film coated Oral
Chemical IUPAC Name: 2-(chloromethyl)oxirane; prop-2-en-1-amine; N-prop-2-enyldecan-1-amine; trimethyl-[6-(prop-2-enylamino)hexyl]azanium; chloride; hydrochloride
Chemical Formula: C31H67Cl3N4O
Colesevelam on Wikipedia: https://en.wikipedia.org/wiki/Colesevelam
Organisms Affected: Humans and other mammals