Medical, Drugs, Pharmaceuticals And Diseases Information

 Lovastatin belongs to statin class of drugs and is used for lowering cholesterol (hypolipidemic agent). Lovastatin is absorbed from GIT.   It under goes extensive first pass metabolism in liver which is it’s primary site of action.    It is highly bound to plasma protein.    Absorption is reduced by approxi 30% in empty stomach than with food. Lovastatin  is available under brand names like Mevacor, Advicor, Altocor , Altoprev and Statosan.

Lovastatin inhibits 3-hydroxy-3methylglutaryl-coenzyme A reductase (HMG-CoA reductase). It is the enzyme which catalyzes the conversion of HMG-CoA to mevalonate which is a required building block for cholesterol biosynthesis. Lovastatin effectively interferes with its production by acting as a competitive inhibitor for HMG-CoA which binds to the HMG-CoA reductase. Lovastatin, is inactive in the native form, the form in which it is administered. It  is hydrolysed to the β-hydroxy acid form in the body and it becomes active only in this form.

Lovastatin is eliminted primarily through fecal route which is the 83% of orally administered dose, 10% of drug is eliminated by renal route. Indication : As an adjunct to diet for the reduction of elevated total & LDL cholesterol in patients of primary hypercholesterolemia, for reduction of elevated  LDL cholesterol levels in patients with combined  hypercholesterolemia  and hypertriglyceridemia.

 Dosage : 10-80 mg/day in single or divided doses. Contraindications of Lovastatin include Hypersensitivity, Active liver disease or unexplained persistent elevations of serum, transaminases, pregnancy & nursing. Special Precaution has to be taken during : Pregnancy & Lactation.

Side effects of Lovastatin are  : Flatulence, diarrhoea, constipation, nausea, abdominal pain, cramps, dyspepsia, heart burn,  dysgeusia,  myopathy,        myalgia, rhabdbmyolysis, blurred vision, headache, dizziness, rashes, impotence, insomnia.

Lovastatin  has Drug interactions  with Anticoagulants, coumarin-or indandione derivative, HMG-COA reductase inhibitors,   cyclosporine   erythromycin,   Gemfibrozil, immunosuppresants or niacin.

Fenofibrate is a lipid lowering drug possessing a prominent lowering action on serum triglycerides. It also reduces serum uric acid levels in hyperuicemic and normal individuals by increasing the urinary excretion of uric acid. Fenofibrate was discovered by France based Groupe Fournier SA which is presently owned by Solvay Pharmaceutical. It is available under brand name Lipanthyl.

Fenofibrate is used in the treatment of in the treatment of type lla, Mb, III, IV and V hyperlipidemia resistant to diet therapy. Fenofibrate is helpful in reducing serum triglyceride levels.  Dosage: One capsule of 200mg per day should be administered with food.

Contraindications:     Hepatic dysfunction, Preexisting gall bladder disease and Hypersensitivity.

Side effects of Fenofibrate include Digestive problems, hepatitis, cholelithiasis, cholecystitis,   hepatomegaly;   Musculoskeletal myalgia, myasthenia, rhabdomylosis; Skin and appendages : photosensitivity, eczema; Respiratory: allergic pulmonary alveolitis.

Bezafibrate  suppresses endogenous cholesterol synthesis, causing the expression of an increased number of specific LDL (low density lipoproteins) receptors and thus an increased catabolism of LDL which  leads to lower plasma cholesterol.  It also suppresses the endogenous synthesis of triglycerides while simultaneously stimulating their catabolism through systemic lipoprotein lipase and hepatic lipase. Bezafibrate effectively brings about lower triglyceride levels. Bezafibrate  is commercially available under brand name Bezalip. 

Bezafibrate is used in the treatment of    Type    Ma,    lib,    III,    IV   &   V hyperlipidemias resistant to diet alone.  Dosage : Bezafibrate 200 mg is given three times daily with food.

Contraindications of Bezafibrate include: Gall bladder disease, Pregnancy, lactation, kidney or liver dysfunction, Nephrotic syndrome. Side effects of Bezafibrate are  Myalgia, diarrhoea, skin rashes, Reversible alopecia, decreased libido, G.I. upset.  Drug  Interaction:    Action  of sulphonylureas potentiated .

GEMFIBROZIL - brand name Lopid  is a hypolipidemic drug & has action resembling nicotinic acid; decreases very low density lipoprotein and blood lipids (VLDL). It is very effective in lowering triglycerides levels primarily. Though the decrease in total cholesterol may be modest, a more favorable distribution is indicated. Primary action of GEMFIBROZIL appears to be reduction of VLDL secretion by liver. Additional decrease in adipose tissue lipolysis and   uptake of fatty acids by liver has been demonstrated.

GEMFIBROZIL is used to treat Hyperlipidemia and lipoprotein abnormalities resistant to diet alone.

Dosage: 900-1500 mg daily (usual dose : 1200 mg) in 2 divided doses 1/2 hr before meals. Contra-indications  : Children,  severe impairment of renal & hepatic functions, Alcoholism, gall bladder disease and hypersensitivity.

Special Precautions: Conduct   blood count, liver function BEFORE TREATMENT & lipid profile tests before initiating therapy and repeat   them periodically. Discontinue if abnormal liver function persists. Regular Ophthalamic checkup required.

Paediatrics: Should not be used in children as well as in pregnant women and those lactating.

GEMFIBROZIL (lopid) Side effects include Epigastric distress, loose motions. Skin rashes, eosinophilia, bodyache, Raised blood sugar, blurred vision and impotence. GEMFIBROZIL (lpoid) has drug interactions with anticoagulants – aggravating effects.