Welchol (colesevelam HCl)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Colesevelam hydrochloride is a bile acid sequestrant antilipemic agent. Colesevelam hydrochloride also is used as an antidiabetic agent.
Colesevelam hydrochloride is a bile acid sequestrant antilipemic agent that is pharmacologically related to other agents in this class (e.g., cholestyramine, colestipol). Like other bile acid sequestrants, colesevelam is not absorbed from the GI tract. Following oral administration, the drug binds to bile acids in the intestine and forms a nonabsorbable complex that is excreted in feces.
Partial removal of bile acids from the enterohepatic circulation via this mechanism results in increased conversion of cholesterol to bile acids in the liver. This causes an increased demand for cholesterol in liver cells, resulting in a compensatory increase in hepatic uptake (and thus systemic clearance) of circulating low-density lipoprotein (LDL)-cholesterol.
Colesevelam reduces serum total cholesterol, LDL-cholesterol, and apolipoprotein B (apo B), and increases high-density lipoprotein (HDL)-cholesterol concentrations. In patients with primary hypercholesterolemia, serum triglyceride concentrations may remain unchanged or increase slightly (5-10%) following colesevelam therapy; serum triglyceride concentrations increased a median of 18 or 22% in patients with type 2 diabetes mellitus receiving concurrent sulfonylurea or insulin therapy, respectively. The maximum therapeutic response to the lipid-lowering effects of colesevelam are achieved within 2 weeks and is maintained during long-term therapy.
The cholesterol-lowering effects of colesevelam and statins are additive. Unlike cholestyramine and colestipol, colesevelam does not appear to reduce the antilipemic activity of concomitantly administered statin therapy.
The mechanism by which colesevelam improves glycemic control is unknown. Proposed mechanisms that may lower blood glucose concentrations include increased insulin secretion and glucose sensitivity, improved glucose disposal, downregulation of enzymes related to hepatic insulin resistance, and suppression of hepatic gluconeogenesis. In patients with type 2 diabetes mellitus, a reduction in glycosylated hemoglobin (hemoglobin A1c) is noted following 4--6 weeks of treatment and reaches maximal or near-maximal effect after 12--18 weeks of treatment.
As colesevelam is not absorbed, distribution is limited to the GI tract. Colesevelam is not metabolized systemically and does not interfere with drug-metabolizing enzymes such as cytochrome P-450. Colesevelam is excreted in the feces; in healthy volunteers, 0.05% of a single radiolabeled dose of colesevelam was excreted in the urine.
USES: This medication is used along with a proper diet and exercise to lower cholesterol in people with high levels of cholesterol in the blood. Lowering cholesterol decreases the risk of heart disease and helps prevent strokes and heart attacks. Colesevelam is also used along with a proper diet and exercise to lower high blood sugar in people with type 2 diabetes.
Controlling high blood sugar helps prevent kidney damage, blindness, nerve problems, loss of limbs, and sexual function problems. Proper control of diabetes may also lessen your risk of a heart attack or stroke. Colesevelam belongs to a class of drugs called bile acid-binding resins.
Bile acid is a natural substance the liver makes by using cholesterol. This medication works by removing bile acid from the body. This causes the liver to make more bile acid by using cholesterol, which reduces cholesterol levels in the blood.
It is not known how colesevelam works in lowering blood sugar.
Generic name: colesevelam HCl
Pronunciation: (KOE-le-SEV-e-lam)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Welchol
Indications
The following indications are listed for Welchol:
- Heterozygous Familial Hypercholesterolemia
- Hyperlipidemia
- Type 2 Diabetes Mellitus Treatment Adjunct
Also known as: Familial Heterozygous Hypercholesterolemia, Heterozygous Familial Elevated Blood Cholesterol, Hyperlipoidemia, Lipemia, Lipidemia, Lipoidemia.
Dosing
Available as colesevelam hydrochloride; dosage expressed in terms of the salt.
Colesevelam hydrochloride tablets are administered orally once or twice daily with a liquid at mealtime. For patients that have difficulty swallowing the tablets, colesevelam oral suspension should be used. Due to tablet size, the oral solution is recommended in pediatric patients.
Colesevelam oral suspension is administered orally once daily at mealtime. To prepare the oral suspension, empty the contents of one packet into a glass or cup and add 1 cup (8 ounces) of water, fruit juice, or diet soft drink. Stir the suspension well and then administer. Do not administer the oral suspension in its dry form.
Unlike other bile acid sequestrants (e.g., cholestyramine, colestipol), colesevelam may be administered simultaneously with statin therapy. Drugs known to interact with colesevelam, as well as drugs that have not been evaluated in formal drug interaction studies with colesevelam, especially those with a narrow therapeutic index, should be administered at least 4 hours prior to colesevelam.
Store colesevelam tablets and oral suspension at 25degreesC protected from moisture; excursions are permitted to 15--30degreesC. Brief exposure to temperatures up to 40degreesC does not adversely affect colesevelam tablets.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Colesevelam reduces the GI absorption of some drugs. Drugs with a known interaction should be administered at least 4 hours prior to colesevelam.
Due to the potential for decreased absorption of other drugs that have not been tested for interaction, especially those with a narrow therapeutic index, consider administering these drugs at least 4 hours prior to colesevelam.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Serum triglyceride concentrations >500 mg/dL.
*History of hypertriglyceridemia-induced pancreatitis.
*History of bowel obstruction.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse effects occurring in at least 2% of patients receiving colesevelam hydrochloride in clinical trials and more frequently than with placebo include constipation, dyspepsia, and nausea.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Safety and efficacy of colesevelam for the treatment of heterozygous familial hypercholesterolemia have been established in males and postmenarchal females 10--17 years of age. Use for this indication is supported by a study conducted in 129 pediatric patients 10--17 years of age. Adverse effects commonly observed in pediatric patients compared to placebo, but not in adults, included headache (3.9%), increased creatine phosphokinase (2.3%), and vomiting (2.3%). There were no substantial effects on fat-soluble vitamin levels or clotting factors in pediatric patients relative to placebo. Due to the size of the tablet, colesevelam oral suspension is recommended for use in pediatric patients. Safety and effectiveness in pediatric patients <10 years of age or in premenarchal females with heterozygous familial hypercholesterolemia have not been established.
Safety and effectiveness of colesevelam for the treatment of type 2 diabetes mellitus have not been established in pediatric patients.
There is insufficient evidence on colesevelam use in pregnant women to evaluate a drug-associated risk of major congenital malformations or miscarriage. There have been infrequent reports of use of colesevelam in pregnancy, and a causal association with congenital anomalies has not been established. Colesevelam is not absorbed systemically following oral administration, and use during pregnancy is not expected to result in fetal exposure to the drug. In reproduction studies in rats and rabbits, no evidence of maternal or fetal toxicity was found when colesevelam was administered during the period of fetal organogenesis at 8 and 5 times, respectively, the maximum recommended human dosage of 3.75 g/day based on body surface area. No adverse effects on offspring survival and development were observed in rats administered 5 times the maximum recommended human dosage.
Colesevelam may decrease the absorption of fat-soluble vitamins. There are no data available on the effect of colesevelam on the absorption of fat-soluble vitamins in pregnant women. If the patient becomes pregnant while taking colesevelam, the patient should be advised of the lack of known clinical benefit with continued use during pregnancy.
The manufacturer states that since colesevelam is not absorbed systemically, the drug is not expected to distribute into human milk.
The manufacturer makes no specific dosage recommendations for geriatric patients.
Of the 1350 patients enrolled in clinical trials of colesevelam for treatment of primary hyperlipidemia, 349 (26%) patients were >=65 years of age and 58 (4%) were >=75 years of age. Of the 2048 patients enrolled in clinical trials of colesevelam for the treatment of type 2 diabetes mellitus, 397 (19%) were >=65 years of age and 36 (2%) were >=75 years of age. No overall differences in safety and efficacy were observed relative to younger adults, but increased sensitivity cannot be ruled out.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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