Synopsis Colesevelam (WelChol) is...

Synopsis

Colesevelam (WelChol) is a nonabsorbed binder of bile acids in the intestine, and thereby impedes the reabsorption of this source of endogenously produc cholesterol It can be used alone or in combination with a statin for the reduction of elevated low-density lipoprotein (LDL) cholesterol on a levels in patients with primary hypercholesterolemia. (1)

Safety

The risk of systemic toxicity is subdued because colesevelam is not absorbed. Doses in exces of 45 g for day have not been proofed Colesevelam is pregnancy category B based forward animal studies; there are no studies upon the absorption of vitamins and other nutrients in pregnant women taking colesevelam. Colesevelam is contraindicated in bodily substances with bowel obstruction and in those who have shown hypersensitivity to any of the drug's ingredients (1) In studies (2,3) of the pharmacokinetics of colesevelam, there were no significant drifts on absorption of the following concurrently administered drugs: digoxin, warfarin (Coumadin), sustained-release verapamil (Calan), metoprolol (Toprol XL) quinidine, valproic acid (Depakene), and lovastatin (Mevacor).

Tolerability

Side weights are infrequent and rarely ensue in discontinuation. In one trial, (4) researchers randomized patients to receive placebo or colesevelam (23 g 30 g 38 g or 45 g) daily for 24 weeks; no significant differences were ground in adverse events or discontinuation rates among clusters and compliance rates were between 88 and 92 percent for all disposes In three separate trials, (5-7) researchers examined the administration of colesevelam alone or in combination with a statin medication. The oftenness of side effects did not differ among assemblages in any of these trials.

Effectiveness

Colesevelam has been studied in several short-term trials, alone and in combination with statins. In sum of two units double-blind, placebo- controlled trials (48) with 650 patients with hypercholesterolemia, colesevelam alone lowered LDL cholesterol horizontals in a dose-dependent manner athwart six to 24 weeks, with a median LDL cholesterol reduction of 20 percent at a daily dose of 45 g The mean total cholesterol flats also decreased compared with placebo in a dose- hanging manner by 10 percent from baseline with 45 g of colesevelam daily. High-density lipoprotein (HDL) cholesterol evens increased by 3 percent across baseline. Triglyceride levels increased through approximately 9 percent over baseline in the colesevelam cluster but this was statistically similar to the 5 percent rise in triglyceride horizontals in the placebo group.

In three double-blind studies (5-7) lasting from four to six weeks, researchers gave patients with hypercholesterolemia colesevelam (23 to 38 g daily) alone or in combination with a statin (atorvastatin [Lipitor], (5) lovastatin [Altocor], (6) or simvastatin [Zocor] (7)) at varied doses. Reductions in LDL cholesterol on a levels with combination therapy (32 to 48 percent) were significantly superior to colesevelam or statins alone (7 to 16 percent and 22 to 34 percent respectively). Combination therapy also decreased total cholesterol on a levels 6 to 10 percent more than statins alone, however did not impact HDL or triglyceride flats whereas atorvastatin alone decreased triglyceride flats (5) High-dose atorvastatin (80 mg daily) lowered LDL cholesterol flats by 53 percent; a similar deduction was found with 10 mg of atorvastatin daily plus colesevelam.

Colesevelam has not been compared with ezetimibe (Zetia), another nonabsorbed cholesterol-lowering unsalable article Most important, there have been no studies examining the consequence of colesevelam on patient-oriented issues such as mortality, myocardial infarction, or hardship risk.

Price

A one-month fill up of colesevelam at a dosage of six tablets daily will expense patients approximately $161. The monthly costliness of ezetimibe is $78, atorvastatin 20 mg is $108 lovastatin 20 mg is $37-71 and ezetimibe 10 mg/simvastatin 20 mg (Vytorin) is $86

Simplicity

Each solid tablet contains 625 mg of colesevelam. The commended starting dose is four to six tablets daily with a statin or six to seven tablets daily alone. Colesevelam should be taken with a meal and a liquid. The dose may be divided and taken twice by day, though this would be earnestly less convenient than many other lipid-lowering medications that are dosed daily.

Bottom Line

Colesevelam lowers LDL cholesterol of the same heights a small amount (7 to 16 percent) when used alone and provides additional cholesterol lowering when added to statin therapy. It has a slightly beneficial force on HDL cholesterol levels, has no result on triglyceride levels, and is well tolerated. However, given the high price, more convenient treatment alternatives, and the lack of long-term studies or information regarding patient-oriented results colesevelam should be considered single in those who cannot take statins or in those who have not reached lipid profile goals despite lifestyle modification and maximum statin dosages.

REFERENCES

(1) WelChol tablets (colesevelam hydrochloride) Sankyo. Physicians' desk regard (electronic version). Thomson MICROMEDEX, Greenwood Village, Colo (Edition expires March, 2005)