J Immunol. 2005 Feb 15;174(4):2327-35.
Suppression of autoimmune retinal disease by lovastatin does not require th2 cytokine induction.
Gegg ME, Harry R, Hankey D, Zambarakji H, Pryce G, Baker D, Adamson P, Calder V, Greenwood J.
Division of Cellular Therapy.

Intraocular inflammatory diseases are a common cause of severe visual impairment and blindness. In an acute mouse model of autoimmune retinal disease, we demonstrate that treatment with the 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, lovastatin, suppresses clinical ocular pathology, retinal vascular leakage, and leukocytic infiltration into the retina. Efficacy was reversed by coadministration of mevalonolactone, the downstream product of 3-hydroxy-3-methylglutaryl coenzyme A reductase, but not by squalene, which is distal to isoprenoid pyrophosphate metabolites within the cholesterol biosynthetic pathway. Lovastatin treatment (20 mg/kg/day i.p.) over 7 days, which resulted in plasma lovastatin hydroxyacid concentrations of 0.098 +/- 0.03 muM, did not induce splenocyte Th2 cytokine production but did cause a small reduction in Ag-induced T cell proliferation and a decrease in the production of IFN-gamma and IL-10. Thus, it is possible to dissociate the therapeutic effect of statins in experimental autoimmune uveitic mice from their activity on the Th1/Th2 balance. Statins inhibit isoprenoid pyrophosphate synthesis, precursors required for the prenylation and posttranslational activation of Rho GTPase, a key molecule in the endothelial ICAM-1-mediated pathway that facilitates lymphocyte migration. Consistent with inhibition of leukocyte infiltration in vivo, lovastatin treatment of retinal endothelial cell monolayers in vitro leads to inhibition of lymphocyte transmigration, which may, in part, account for drug efficacy. Unlike lovastatin, atorvastatin treatment showed little efficacy in retinal inflammatory disease despite showing significant clinical benefit in experimental autoimmune encephalomyelitis. These data highlight the potential differential activity of statins in different inflammatory conditions and their possible therapeutic use for the treatment of human posterior uveitis.

Arzneimittelforschung. 2003;53(9):605-11.
Pharmacological comparison of the statins.
Klotz U.
Margarete Fischer-Bosch Institute of Clinical Pharmacology, Stuttgart, Germany.

The statins (3-hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitors) represent drugs of first choice for treatment of hypercholesterolemia. The safety and efficacy of atorvastatin (CAS 134523-00-5), simvastatin (CAS 79902-63-9), lovastatin (CAS 75330-75-7), pravastatin (CAS 81093-37-0) and fluvastatin (CAS 93957-54-1) has been well documented. Statins decrease dose-dependently low-density lipoprotein (LDL) cholesterol as well as coronary events and total mortality. Clinical outcome data indicate that for simvastatin the lowest number of treated patients is needed to prevent one major coronary event (NNT 15). Based on an approximately 30% reduction of LDL (valid surrogate parameter) atorvastatin (5 mg/day) and simvastatin (10 mg/day) are the most potent agents whereas 40 mg of lovastatin or pravastatin and 60 mg of fluvastatin are needed to reach this "therapeutic target". While all statins share the same mode of action their pharmacokinetic properties and their susceptibility to drug interactions differ slightly. Agents inhibiting CYP3A4 (e.g. grapefruit juice, itraconazole, cyclosporine) should be discouraged if a patient is on atorvastatin, lovastatin or simvastatin. Likewise, fluconazole interferes with the CYP2C9-mediated hepatic elimination of fluvastatin. Moreover, coadministration of gemfibrozil should be avoided because it seems to increase the very low risk for statin-induced rhabdomyolysis. Several statins are available and their equieffective doses have been defined. Selection of a particular drug should be primarily based on clinical outcome data. However, costs and in certain situations the pharmacokinetic profile including the interaction potential of the statins should be taken into account.

Am J Cardiol 2001 Aug 16;88(4 Suppl):10F-5F
Are we aggressive enough in lowering cholesterol?
Waters DD
Cardiology Division, Department of Medicine, San Francisco General Hospital, San Francisco, California 94110, USA.

To date, 5 major randomized, placebo-controlled statin trials--the Scandinavian Simvastatin Survival Study, West of Scotland Coronary Prevention Study, Cholesterol and Recurrent Events trial, Long-term Intervention with Pravastatin in Ischaemic Disease, and Air Force/Texas Coronary Atherosclerosis Prevention Study--have convincingly shown that total mortality and major coronary events can be significantly reduced by lowering levels of low-density lipoprotein cholesterol (LDL-C) with statin therapy. These results were achieved in a broad range of patients including those with and without a history of coronary artery disease and with elevated or average LDL-C levels. The results also support the large body of epidemiologic evidence demonstrating that the lower the cholesterol level, the lower the cardiovascular risk. Evidence now substantially supports the urgency of physicians to aggressively target the lowering of LDL-C levels for the primary and secondary prevention of coronary disease.

Drug information

GENERIC NAME: lovastatin
BRAND NAME: Mevacor, Altocor

DRUG CLASS AND MECHANISM: Lovastatin 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.

PREPARATIONS: Tablets: 10, 20, and 40 mg. Extended release tablets: 10, 20, 40, and 60 mg.

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

PRESCRIBED FOR: High LDL cholesterol is usually first treated with exercise, weight loss in obese individuals, and a diet low in cholesterol and saturated fats. When these measures fail, cholesterol-lowering medications such as lovastatin 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. The effectiveness of the medication in lowering cholesterol is dose- related. Blood cholesterol determinations are performed in regular intervals during treatment so that dosage adjustments can be made. A reduction in LDL cholesterol level can be seen two weeks after starting therapy.

DOSING: May be taken on an empty or full stomach. The medication seems to be most effective when given with the evening meal.

DRUG INTERACTIONS: Lovastatin is generally well- tolerated by most patients. The medication should be used with caution in patients with alcohol or other liver diseases. Persistent abnormal liver tests during treatment are rare, but may lead to the discontinuation of the medication. Rare cases of muscle inflammation (myositis) and breakdown have been reported with lovastatin. Muscle breakdown causes release of muscle protein (myoglobin) into the blood and kidney tubules, resulting in kidney failure. Severe muscle breakdown and kidney failure have been reported when lovastatin is used together with gemfibrozil (Lopid). Therefore their concomitant use is discouraged. The risk of muscle breakdown is also increased when lovastatin is given together with other medications, such as cyclosporine (Sandimmune), erythromycin and nicotinic acid. Therefore, lovastatin should be used with caution and in lower doses when medications, such as cyclosporine are also needed. Lovastatin should not be used by children. It is not habit forming.

PREGNANCY: Lovastatin may cause fetal harm, and should not be given to pregnant women.

NURSING MOTHERS: Lovastatin 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, gas, heartburn, headache, insomnia. Major side effects include abdominal pain or cramps, blurred vision, dizziness, itching, muscle pain or cramps, rash, 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.
Also, you should read carefully important health information about this drug given here:

www.nlm.nih.gov

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MEVACOR
Generic name: Lovastatin
Manufacturer: Merck & Co., INC. (Germany)

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Dosage	Packing	Price	Pay now
20 mg	28 tab	USD 48.00
40 mg	28 tab	USD 73.00