Lovastatin Drug Info

Lovastatin Generic
Lovastatin Brand Name / Trade Name
Lovastatin is a generic drug to Lestric, Mevacor, Altoprev, Altocor which are Lovastatin brand name / trade name

Lovastatin Classification
Lovastatin is classified under statins drugs which are of HMG-CoA reductase inhibitors. Lovastatin help reduce the levels of 'bad' cholesterol or LDL (low-density lipoprotein) and triglycerides in our blood level while at the same time increasing 'good' cholesterol or HDL (high-density lipoprotein). It works by preventing certain enzymes in our body from synthetizing cholesterol.

Lovastatin Uses / Indications
Normally, lovastatin is indicated to lower the risk of cardiovascular disease, including stroke, heart attack, coronary heart disease and other heart complications. It is used in adults and not recommended for children who below 10 years old. Thus, the primary use would be for the treatment of dyslipidemia and prevention of heart disease. However, it is advised that patient should adopt healthy lifestyle (diet, exercise regularly) to enhance and improve lovastatin treatment.

Lovastatin Mechanism of Action / How lovastatin works
Lovastatin works by catalyzing the conversion of HMG-CoA to mevalonate by inhibiting competitively HMG-CoA reductase enzyme (or known as 3-hydroxy-3methylglutaryl-coenzyme A reductase). Mevalonate is a precursor and building block for cholesterol biosynthesis and thus would be interfered by lovastatin. Lovastatin is hydrolysed to the beta hydroxy acid form in the body before it becomes active.

Lovastatin Dose / Dosage Form
The usual recommended lovastatin dosage would be 20 mg once daily given with the evening meal. The dose range would be 10-80 mg a day in single or 2 divided doses. The maximum dose for lovastatin is 80 mg per day. Lovastatin is available in tablet dosage forms with lovastastin strength as below
Lovastatin 10 mg
Lovastatin 20 mg.
Currently, lovastatin extended-release formulation is also available in the market. The initial dose would be 20-60 mg at bedtime with maintenance 10-60 mg daily.



Lovastatin History / Origin
Lovastatin was discovered together with compactin in the 1970s since it was found with powerful inhibitory effect on enzyme HMG-CoA reductase which lead to clinical development as potential drugs for lowering LDL cholesterol.
Also, in 1982, There was significant reductions in LDL level observed during small-scale investigations done on lovastatin where it were taken by high-risk patients with concomitantly minimal side effects being observed. Followingly, large-scale clinical trials were done further confirmed the effectiveness of lovastatin in decreaseing LDL cholesterol level where it was approved by US FDA in 1987 due to its good tolerability. Lovastatin was the first statin approved by FDA.
Certain fungi such as Pleurotus species including Pleurotus ostreatus (oyster muschroom) was found to produce lovastatin naturally which was then being researched for its effect of extract animal cholesterol levels.

Lovastatin structure / biochemistry
Lovastatin is isolated from a strain of Aspergillus terreus in which would be hydrolyzed to active beta hydroxyacid form from inactive lactone after oral ingestion. The hydrolyzed metabolite acts as inhibitors to 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase which is the enzyme responsible for the conversion of HMG-CoA to mevalonate. The latter is an early and rate limiting step in biosynthesis of cholesterol.
Lovastatin is [1S-[1α(R*),3α,7β,8β(2S*,4S*), 8aβ]]-1,2,3,7, 8,8a-hexahydro-3,7-dimethyl-8-[2- (tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1-naphthalenyl 2-methylbutanoate. The empirical formula of lovastatin is C24H36O5 and its molecular weight is 404.55. Its structural formula is:


Lovastatin Side Effects
Lovastatin is usually well tolerated, however, it may cause myopathy or rhabdomyolysis which is the common side effects found among statin drugs though rarely happen. The risk of myopathy/rhamdomyolysis is dose related and patients should carefully monitored when taking other medicines known to affect lovastatin metabolism. Any risk of myopathy or unexplained muscle pain, tenderness or weakness should be reported as soon as possible. Lovastatin therapy should be withhold and discontinued if myopathy is suspected diagnosed due to lovastatin.
Other side effects may include GI discomfort, muscle cramps, myalgia, asthenia
Gastrointestinal: Abdominal pain, constipation, diarrhea, dyspepsia, flatulence, nausea
Skin: Rash
Nervous system: Dizziness, headache

Lovastatin pregnancy category: X

Lovastatin Contraindications
Lovastatin is contraindicated during pregnancy as it would cause skeletal deformities or learning disabilities. Also, lovastatin is contraindicated in patients with liver failure, acute liver disease or unexplained persistent elevations of serum transaminases.

Lovastatin Drug Interactions
Since statin drugs (including lovastatin) are metabolized via CYP3A4, grapefruit juice with its components flavanoid naringin (or furanoccoumarin bergamottin) would inhibit CYP3A4 resulting in decrease in metabolic clearance of lovastatin and thus increasing its plasma concentrations. There are drug interactions of lovastatin with fibrates including gemfibrozil, niacin, or ciclosporin and hence, lovastatin at doses higher than 20mg per day should not be used together with these drugs as risk of rhabdomyolysis is significantly increased.
Other drugs found to reduce the lovastatin elimination include erythromycin, ketoconazole, itraconazole, clarithromycin, telithromycin, cyclosporine, nefazodone and protease inhibitors such as indinavir and ritonavir.