HMG-COA reductase inhibitors include- Fluvastatin, Lovastatin, Pravastatin, Simvastatin

Refer - Lovastatin

Bile salts with Pravastatin decrease a 40% decrease in pravastatin bioavailability may occur. Take Pravastatin 1 hour before and 4 hour after bile acid sequestrant

Concomittant administration with cholestyramine or colestipol may result in approximately 40 to 50 % decrease in the mean AUC of parvastatin

Pravastatin when administered along with gemifibrol decreases the urinary excretion and protein binding of pravastatin

Primary Hypercholesterolaemia

HMG-COA reductase inhibitors include- Fluvastatin, Lovastatin, Pravastatin, Simvastatin

Refer - Lovastatin 

        Patent Expiry Date of drugs (Ref - IDMA Publication)   

Myopathy, headache, Non-cardiac chest pain, Nausea, vomiting, Diarrhea, fatigue, Biochemical abnormalities of liver function, and transcient elevation of creatinine phosphokinase, values

Active liver disease,. Patients with history of serious adverse reaction to prior administration of HMG-CoA reductase inhibitors Pregnancy and breast feeding. Women of child bearing potential unless protected by adequate contraception. hypersensitivity to the drug.

Special prercautions:

Not recommended for administration to nursing mothers. To be administered to women of child bearing age only if the patients are receving contraceptive therapy. Past history of liver disease.

Heavy alcohol ingestion Sporadic elevation of creatinine phosphokinase (CPK ) have been observed.

Approved by FDA in October 1991

 Primary Hypercholesterolaemia

Dosage:

Individualise dose Initial- 10 to 20mg once daily at bed time Elderly- 10mg once daily at bed time Dosage range- 10 to 40mg once daily at bed time

1. May cause photosentivity (sensitivity to sunlight) . Avoid prolonged exposure to the sun and other ultraviolet light.

2. Use sunscreens and wear protective clothing until tolerance is determined

3. Promptly report unexplained muscle pain, tenderness or weakness, especially if accompanied by fever or malaise

4. Follow dietary recommendations.

5. Take lovastatin with meals, fluvastatin and simvastatin may be taken without regrads to meals.

Pharmacology:

Pravastatin inhibits 3-hydroxyl-3-methlglutaryl-coenzyme. A HMG-CoA reductase , the enzyme which catalyses the rate limiting step within the cholestreol biosynthetic pathway. By inhibiting (de novo ) chloesterol production and reducing intracellular cholesterol stores, pravastatin stimulates the synthesis and activity of low density lipoprotein(LDL) receptors, thereby enhancing the clearance of arthogenic LDL- chlolesterol

Pharmacokinetics:

Pravastatin is administered as the sodium salt. It is rapidly absorbed with the mean peak plasma concentration occuring occuring between 0.9 and 1.6hours after single or multiple dose administration in hypercholesterolamic patients. The drug has an oral bioavailability of 17%. Approximately 50% of the drug is bound to plasma proteins. It is rapidly excreted and has a terminal plasma elimination of half-life of 1.3 to 2.6 hours. Approximately 70% and 20% of the oral dose is eliminated in feces and urine, over 96 hours.

May be taken without regards to meals.

Not recommended for nursing mothers. Women of child bearing potential should receive effective contraceptive therapy