fluvastatin
Brand: Lescol, Lescol XL
Prototype: atorvastatin
Drug Class: HMG-CoA reductase inhibitor (statin)
Drug Family: antilipemic
Subclass: synthetic statin
Organ Systems: cardiovascular
Mechanism of Action
Fully synthetic statin that competitively inhibits HMG-CoA reductase; metabolized primarily by CYP2C9 rather than CYP3A4, providing a distinct interaction profile from most other statins.
HMG-CoA reductase
Indications
- hypercholesterolemia
- mixed dyslipidemia
- secondary prevention of cardiac events post-PCI
Contraindications
- active liver disease
- pregnancy
- breastfeeding
- hypersensitivity
Adverse Effects
Common
- myalgia
- headache
- dyspepsia
- nausea
- elevated transaminases
Serious
- rhabdomyolysis
- myopathy
- hepatotoxicity
Pharmacokinetics (ADME)
| Absorption | approximately 24-29% oral bioavailability due to first-pass effect; XL form provides extended release |
| Distribution | highly protein bound; Vd approximately 330 L |
| Metabolism | hepatic CYP2C9 (primary), CYP2C8 (minor); active hydroxylated metabolites |
| Excretion | fecal (~90%) via bile; minimal renal excretion (<6%) |
| Half-life | approximately 3 hours (immediate-release); approximately 9 hours (extended-release) |
| Onset | days to weeks |
| Peak | 1 hour (IR); 3 hours (XL) |
| Duration | 24 hours |
| Protein Binding | >98% |
| Vd | approximately 330 L |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| fluconazole | CYP2C9 inhibition increases fluvastatin exposure significantly | major |
| gemfibrozil | CYP2C9 and OATP1B1 inhibition increases fluvastatin levels | moderate |
| cyclosporine | OATP1B1 inhibition increases fluvastatin exposure | moderate |
| warfarin | CYP2C9 competition may increase warfarin anticoagulant effect | moderate |
Nursing Considerations
- Immediate-release capsules may be taken at any time; extended-release tablets should be taken at bedtime and must not be crushed or chewed.
- Monitor liver enzymes at baseline and symptomatically; fluvastatin has a lower overall myopathy risk than higher-potency statins.
- Advise patients taking warfarin that fluvastatin may potentiate anticoagulation; monitor INR more frequently when initiating or adjusting dose.
- Instruct patients to report unexplained muscle pain, dark urine, or signs of liver dysfunction; these warrant prompt evaluation and possible discontinuation.
Clinical Pearls
- Fluvastatin is the weakest LDL-lowering statin; at maximum dose (80 mg XL) it reduces LDL by approximately 35%, compared with 50-60% for high-intensity statins.
- CYP2C9 metabolism means fluvastatin interacts with azole antifungals and warfarin more prominently than CYP3A4-metabolized statins — an important nursing medication reconciliation point.
Safety Profile
Pregnancy contraindicated
Lactation contraindicated
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.