Altoprev

Altoprev is the first clinically used statin; is lipophilic and given orally in the precursor lactone form. Its absorption is incomplete and first pass metabolism is extensive. 

Its metabolites are excreted mainly in bile. The half-life of lovastatin is relatively short (1-4 hours). Generally, 10 mg and 20 mg tablets are available in the market. The usual therapeutic dose of lovastatin is regarded as 10-40 mg/day that must not exceed 80 mg. 

Lovastatin is mostly an effective drug in reducing LDL. Its action is mediated in the following ways:

• It works by inhibiting an enzyme in the liver that is responsible for manufacturing cholesterol.
• It primarily lowers LDL-cholesterol levels but also increases HDL-cholesterol levels and sometimes, lowers triglyceride levels as well.
• Additionally, lovastatin has the effect that prevents heart disease. This drug also possesses a mild blood thinning effect and an anti-inflammatory effect on the walls of the blood vessels.

Lipid travels in blood packaged with proteins as lipoproteins.

There are 4 classes of lipids in the human body:

• Chylomicrons
• VLDL (mainly triglyceride)
• LDL (mainly cholesterol)
• HDL (mainly phospholipid)

The evidence that Cholesterol is a major risk factor for cardiovascular diseases (CVD) is now incontrovertible and indeed it may even be the “green light” that allows other risk factors to act. 

Positive family history of Hyperlipidemia, presence of corneal arcus in those below 50 years, and presence of Xanthomata or Xanthelasmata paves the way to cause Dyslipidemia i.e. Hyperlipidemia. 

Xanthomata refers to yellow lipid deposits which may be eruptive (itchy nodules in hypertriglyceridemia), tuberous (plaques on elbows and knees) or planar-also called palmar (orange streaks in palmar creases). When they are found in eyelids, they are named as Xanthelasma and in case of cornea called as arcus.

There are several types of hyperlipidemia which may demand drug therapy. They are:

• Common primary hyperlipidemia: accounts for 70% of hyperlipidemia which is characterized by increased LDL only.
• Familial primary hyperlipidemia: risk of CVD, although evidence suggests protection from CVD is achieved with lower doses of statins (e.g. lovastatin) than for common primary hyperlipidemia
• Secondary hyperlipidemia: may be caused by Cushing’s syndrome, hypothyroidism, nephrotic syndrome, or cholestasis. Increased LDL is the diagnostic feature. Treatment of the cause should be confirmed first. 
• Mixed hyperlipidemia: results in increased both LDL and triglycerides. It is caused by type 2 diabetes mellitus, metabolic syndrome, alcohol abuse and chronic renal failure.

Hyperlipidemia may predispose to cardiovascular diseases (CVD). Those below 65 years with positive family history of CVD are at higher risk of developing CVD. 

Diabetes mellitus, hypertension, impaired glucose tolerance, smoking, increased BMI and low socio-economic background also pave the way to CVD.

Management of hyperlipidemia does not demand drug therapy all the time. Lifestyle advices may become sufficient in many cases. BMI of 20-25, fibre-rich diet with <10% of calories from saturated fats, fresh fruits and vegetables, omega-3 fatty acids and regular exercise help to prevent the disease process.

In order to treat hyperlipidemia, HMG CoA reductase inhibitors; statins (e.g. lovastatin) are used as the first-line drug, whereas  fibric acid derivatives; fibrates, cholesterol absorption inhibitors, bile acid binding resins and niacin are considered as second-line therapy.

Lovastatin and other drugs used in the treatment of elevated serum lipids (hyperlipidemia) generally target to: 

• decrease production of lipoprotein by the tissues,
• increase catabolism of a lipoprotein in the plasma, or
• increase removal of cholesterol from the body.

Altoprev is the first choice of drugs for primary hyperlipidemias with raised LDL and total CH levels, with or without raised TG levels, as well as for secondary hypercholesterolemia; which may occur as a result of diabetes and nephrotic syndrome. 

Efficacy of lovastatin in reducing raised LDL-CH associated mortality and morbidity is now well established. 

Beneficial effects in subjects who have raised CH levels but no evidence of CAD may relate to improved coronary artery compliance and atheromatous plaque stabilization due to suppression of macrophage mediated inflammation, reducing chances of plaque rupture and thrombus formation. Recently, a reduction in venous thromboembolism has also been observed with Lovastatin. 

On the basis of these beneficial effects as well as the excellent patient acceptability, lovastatin and other statins are being increasingly used for primary and secondary hypercholesterolemia with or without raised TG levels. 

As the liver makes cholesterol mostly at night, therefore, such medications should be taken in the evening.

Before using Altoprev, there are some precautions you must take. Full screening for hyperlipidemia requires a fasting lipid profile. Further, frequent measures of creatinine kinase activity are recommended when starting and even after completing this drug therapy. 

You should be careful to avoid the unwanted drug interactions and other toxicity that may arise because of such medications. Monitoring of liver function is recommended as there is strong evidence of some increase in creatinine kinase. 

Myopathy is more likely to take place when lovastatin is used with some other drugs such as:

• Cyclosporine
• Fibric acid derivatives
• Azoles
• Macrolide antibiotics (e.g. erythromycin)
• Danazol
• Niacin (vitamin B₃)

The use of lovastatin is contraindicated in porphyria, cholestasis, pregnancy and lactation. Even in case of suspected pregnancy, it is better to avoid this drug. Moreover, children should not be given such medications.

Lovastatin is remarkably well tolerated. Although overall incidence of side-effects may not be differing from placebo, but some side effects are notable:

• Gastrointestinal complaints and headache are usually mild.
• Rashes and sleep disturbances are uncommon.
• Rise in serum transaminase can occur, but liver damage is rare.
• Muscle aches are the commonest (10%) side effects.
• Rise in CPK level occurs infrequently.
• Myopathy is the only serious reaction, but is rare (<1 per 1000).