Fluvastatin
Mechanism :
Fluvastatin selectively and competitively inhibits the hepatic enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase is responsible for converting HMG-CoA to mevalonate, the rate-limiting step in cholesterol biosynthesis. Inhibition results in a decrease in hepatic cholesterol levels which stimulates the synthesis of LDL receptors and increases hepatic uptake of LDL cholesterol. The end result is decreased levels of plasma total and LDL cholesterol.
Indication :
- Heterozygous Familial Hypercholesterolemia
- Hypercholesterolemia & Mixed Dyslipidemia
Contraindications :
Hypersensitivity to fluvastatin.
Active liver disease, or unexplained elevated transaminases.
Withhold or discontinue treatment if myopathy develops, renal failure, or transaminase levels >3 times the upper limit of normal.
Dosing :
Under 10 years:
Safety and efficacy not established.
10-16 years:
20 mg once orally at bedtime initially; may increase dose at 6 week intervals up to 40 mg orally twice daily immediate release or 80 mg once orally for extended release.
Adverse Effect :
Constipation, fatigue, diarrhea, gas, headache, insomnia, heartburn, joint pains, dizziness, abdominal pain or cramps, blurred vision, easy bruising or bleeding, muscle pain or cramps, itching, rash, jaundice, rhabdomyolysis, increases in HbA1c, increase fasting serum glucose levels, confusion, memory loss, amnesia, forgetfulness, and memory impairment.
Interaction :
Cyclosporine and Fluconazole: Increase blood levels of fluvastatin. Therefore, the dose of fluvastatin should be limited to 20 mg twice daily when patients are also taking cyclosporine or fluconazole.
Gemfibrozil: Should not be combined with fluvastatin due to increased risk of muscle-related side effects when the two drugs are combined.
Colchicine & Niacin: Combining fluvastatin with colchicine or one gram or larger doses of niacin also increases the risk of muscle-related side effects.
Warfarin: Fluvastatin increases the effect of warfarin. Patients taking warfarin should be monitored carefully for toxic effects of warfarin.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
20-50 | Dose as in normal renal function |
10-20 | Dose as in normal renal function |
<10 | Dose as in normal renal function |
Dose in Patients undergoing Renal Replacement Therapies
CAPD | Removal unlikely. Dose as in normal renal function |
HD | Removal unlikely. Dose as in normal renal function |
HDF/High flux | Removal unlikely. Dose as in normal renal function |
CAV/VVHD | Removal unlikely. Dose as in normal renal function |
Hepatic Dose :
Contraindicated in patients with hepatic Impairment, active hepatic disease, with unexplained persistent hepatic transaminase elevations.