Cyclosporin Warfarin Gemifibrozil

Erythromycin

Antacids

Oral contraceptives

Hormone replacement therapy

Hypercholesterolaemia

NEWS UPDATE-

ROSUVASATIN - RISKY IN INDIANS

As per data submitted to the USFDA,  the pharmacokinetic behaviour of rosuvastatin is
ethinic- sensitive wih blood levels reaching higher levels in Asian populations compared
to Caucasians. This can lead to more severe side effects such as life-threatening
rhabdomylosis.

Western drug regulators have made  it obligatory that prescribers inform all patients that

- rosuvastatin can cause muscle injury which in severe cases " can cause kidney damage and
  other organ failure that are potentially life threatening.

Hence patients must promptly report signs and symptoms of muscle pain and weakness,
malaise, fever, dark urine, nausea or vomiting to their doctors" (MIMS)
 

Headache, dizziness Constipation, nausea Abdominal pain Myalgia Asthena

Severe renal impairment Active liver disease

Hypersentivity to Rosuvastatin

Myopathy Cyclosporin

Pregnancy and lactation

Date of Approval       2008

Indication-

Hypercholesterolaemia

Dosage-

Recommended starting dose-

10mg orally once daily. A dose adjustment of 20mg can be made after 4 weeks if necessary

Rosuvastatin can be given at any time of day with or without food.

Pharmacology

Rosuvastatin is a selective and competitive inhibitor of HMG CoA reductase , the rate-limiting enzyme tat converts 3-hydroxy 3-methylglutaryl coenzyme A to mevalonate, a precursor for cholesterol. The primary site of action of rosuvastain is inthe liver, the target organ for cholesterol lowering. Rosuvastatin increases the number of hepatic LDL receptors on the cell-surface enhancing uptake and catabolism of LDL anf it inhibits the hepatic synthesis of of VKDL., therby reducing the total number of VLDL and LDl particles. Rosuvastatin produces larger reductions in LDL cholesterol and improved other lipid parameters to a greater extent tan either pravastatin or simavastatin. This incresed efficacy allows more patients to achieve lDL cholesterol goals at lower daily doses.

Pharmacokinetics-

Rosuvastatin has a moderately rapid absorption and an oral bioavailability of approx 20%.. Food decreases its rate of absorption by 20%. Eighty percent of rosuvastatin is bound to plasma proteins. It is not extensively absorbed by the liver and has a long elimination half life of approximately 20 hours. Rosuvastatin was found to be mainly excreted in the feces (90%) and 10% via urine.

Rosuvastatin can be given with or without food. Food decreases its rate of absorption by 20%.

Contraindicated for use during pregnancy and lactation.