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LESCOL

(generic name: Fluvastatin)

Pharmacological category: antihyperlipidemic, HMG-CoA reductase inhibitor

Reviews

Fluvastatin

World J Gastroenterol. 2005 Feb 21;11(7):1040-3.
Inhibitory effect of fluvastatin on ileal ulcer formation in rats induced by nonsteroidal antiinflammatory drug.
Hagiwara M, Kataoka K, Arimochi H, Kuwahara T, Nakayama H, Ohnishi Y.
Department of Molecular Bacteriology, Graduate School of Medicine, The University of Tokushima, Tokushima 770-8503, Japan.

AIM: Nonsteroidal anti-inflammatory drugs (NSAIDs) cause gastrointestinal damage as one of their side effects in humans and experimental animals. Lipid peroxidation plays an important role in NSAID-induced ulceration. The aim of this study was to investigate the inhibitory effect of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors on the ulceration in small intestines of rats. METHODS: The effects of three HMG-CoA reductase inhibitors, fluvastatin, pravastatin and atorvastatin on ileal ulcer formation in 5-bromo-2-(4-fluorophenyl)-3-(4- methylsulfonylphenyl) thiophene (BFMeT)-treated rats were examined. Antioxidative activity of the inhibitors was measured by a redox-linked colorimetric method. RESULTS: Fluvastatin, which was reported to have antioxidative activity, repressed the ileal ulcer formation in rats treated with BFMeT an NSAIDs. However, the other HMG-CoA reductase inhibitors (pravastatin and atorvastatin) did not repress the ileal ulcer formation. Among these HMG-CoA reductase inhibitors, fluvastatin showed a significantly stronger reducing power than the others (pravastatin, atorvastatin). CONCLUSION: Fluvastatin having the antioxidaitive activity suppresses ulcer formation in rats induced by NSAIDs.
Expert Opin Drug Saf. 2003 May;2(3):269-86.
Combination lipid-lowering therapy with statins: safety issues in the postcerivastatin era.
Jacobson TA.
Office of Health Promotion and Disease Prevention, Department of Medicine, Emory University School of Medicine, Atlanta, GA 30303, USA.

Combination lipid-altering regimens represent an emerging clinical paradigm to meet increasingly stringent consensus lipoprotein targets for coronary prevention. This practice, together with escalating prevalences of coronary artery disease in certain ageing (western industrial) populations, polypharmacy in the elderly and the recent voluntary market withdrawal of cerivastatin, warrants a re-examination of the safety profiles of 3-hydroxy-3-methylglutaryl co-enzyme A (HMG-CoA) reductase inhibitors (i.e., statins). These agents are exceedingly well-tolerated in the vast majority of patients, very infrequently precipitating musculoskeletal symptoms and/or signs. Statins vary in their pharmacological profiles, leading to distinct levels of systemic exposure and capacities to penetrate skeletal myocytes. Pharmacokinetic interactions with certain agents increase the likelihood of statin-induced myopathy and, in exceedingly rare instances, potentially fatal rhabdomyolysis with myoglobinuria and renal failure. As with other medical decisions, the anticipated benefits of long-term statin therapy, with or without other lipid-altering agents, need to be weighed against the prospects of clinically significant drug interactions. In clinical trials and postmarketing surveillance, the two statins that are not metabolised by the cytochrome P450 3A4 system (fluvastatin and pravastatin) have exhibited very low propensities to elicit myopathy when combined with other agents. These agents should be considered initially when contemplating combination lipid-lowering regimens for coronary prevention.
Cleve Clin J Med. 2003 Jun;70(6):561-6
The Lescol Intervention Prevention Study (LIPS): start all patients on statins early after PCI
Messerli AW, Aronow HD, Sprecher DL
Department of Cardiovascular Medicine, The Cleveland Clinic Foundation, OH 44195, USA.

The Lescol Intervention Prevention Study (LIPS) was the first randomized trial to show a significant reduction in the risk of cardiac events in patients started on fluvastatin immediately after a successful percutaneous coronary intervention. The benefit was independent of baseline cholesterol levels. The results suggest that all patients should be discharged on lipid-lowering therapy after a percutaneous coronary intervention. Currently, this is seldom done.

Clinical results:

Twelve placebo-controlled studies were conducted involving subjects with Type IIa or IIb hyperlipoproteinemia. Lescol was administered daily to 1621 subjects for at least 6 weeks. After 24 weeks, treatment resulted in average LDL-C reductions of 22% for the 20mg dose, 25% for the 40mg dose and 36% for the 80mg dose. Treatment with Lescol reduced Apo B and triglycerides while increasing HDL-C.

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Drug information

GENERIC NAME: fluvastatin
BRAND NAME: Lescol


DRUG CLASS AND MECHANISM: Fluvastatin is a cholesterol- lowering medicine. It inhibits the production of cholesterol by the liver. It lowers overall blood cholesterol as well as blood LDL cholesterol levels. LDL cholesterol is believed to be the "bad" cholesterol that is primarily responsible for the development of coronary artery disease. Lowering LDL cholesterol levels retards progression and may even reverse coronary artery disease, thus reducing the chance of heart attacks.

PREPARATIONS: tablets:20 mg, 40 mg

STORAGE: Tablets should be stored at room temperature in a tightly closed container.

PRESCRIBED FOR: High blood LDL cholesterol is first treated with exercise, weight loss, and a diet low in cholesterol and saturated fats. When these measures fail, cholesterol-lowering medications such as fluvastatin can be added. The National Cholesterol Education Program (NCEP) has published treatment guidelines for use of these medications. These treatment guidelines take into account the level of LDL cholesterol as well as the presence of other risk factors such as diabetes, hypertension, cigarette smoking, low HDL cholesterol level, and family history of early coronary heart disease. Blood cholesterol determinations are performed in regular intervals during treatment so that dosage adjustments can be made.

DOSING: May be taken on an empty or full stomach.

DRUG INTERACTIONS: Fluvastatin is generally well- tolerated by most patients. The medication should be used with caution in patients with alcohol or liver diseases. Persistently abnormal liver blood tests are rare, but may lead the doctor to discontinue the medication. Rare cases of muscle inflammation (myositis) and breakdown have been reported with other medications in the same class. Muscle breakdown causes the release of muscle protein (myoglobin) into the blood and kidney tubules, and may result in kidney failure. To date, significant muscle inflammation or breakdown has not been reported with fluvastatin. This medication may interact with other medications like digoxin (Lanoxin), cimetidine (Tagamet), and ranitidine (Zantac). The clinical significance of these interactions are not clear. Fluvastatin is not recommended for use in children. Fluvastatin is not habit forming.

PREGNANCY: Fluvastatin may cause fetal harm and should not be taken by pregnant women.

NURSING MOTHERS: Fluvastatin should not be used by nursing mothers because of potential adverse side effects to the nursing infant.

SIDE EFFECTS: Side effects are rare. Minor side effects include constipation, diarrhea, fatigue, gas, heartburn, headache, insomnia, and joint pains. Major side effects include abdominal pain or cramps, blurred vision, dizziness, easy bruising or bleeding, itching, muscle pain or cramps, rash, and yellowing of the skin or eyes.

Caution! Before starting to take this medicine, it is vital that you should consult your doctor! Do not use it on your own initiative, without medical advice.

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LESCOL
Generic name: Fluvastatin
Manufacturer: Novartis

 
Dosage
Packing
Price
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20 mg
28 tab
USD 43.00
40 mg
28 tab
USD 65.00
 

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