FLUVASTATIN SODIUM
Clinical safety rating: avoid
Contraindicated (not allowed)
Competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis, leading to decreased intracellular cholesterol levels and upregulation of LDL receptors.
| Metabolism | Hepatic via CYP2C9; minor contributions from CYP3A4 and CYP2D6. |
| Excretion | Fluvastatin sodium is primarily eliminated via biliary/fecal excretion (approximately 90%), with renal excretion accounting for less than 6% of the administered dose. |
| Half-life | The terminal elimination half-life is 2.3 hours (range 1.4–3.1 hours). Due to its short half-life, it is dosed once daily for sustained HMG-CoA reductase inhibition; however, pharmacodynamic effects (LDL reduction) persist beyond plasma clearance. |
| Protein binding | Fluvastatin is highly protein-bound (>99%), primarily to albumin. |
| Volume of Distribution | Volume of distribution (Vd) is approximately 0.35 L/kg, indicating distribution mainly into extracellular fluid and minimal tissue binding. |
| Bioavailability | Oral bioavailability is 24% (range 19–29%) due to extensive first-pass metabolism; absorption is rapid (Tmax 0.5–1 hour). |
| Onset of Action | Oral administration: Onset of lipid-lowering effect is observed within 1–2 weeks, with maximal effect at 4 weeks. |
| Duration of Action | Duration of lipid-lowering effect: After discontinuation, the effect persists for several days; LDL-C levels return to baseline within about 6 weeks. The duration of clinical benefit requires continuous dosing. |
| Molecular Weight | 433.45 |
20 to 80 mg orally once daily in the evening; immediate-release: 20-40 mg once daily; extended-release: 80 mg once daily.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (eGFR ≥30 mL/min/1.73 m²). Not recommended in severe renal impairment (eGFR <30 mL/min/1.73 m²) due to lack of data. |
| Liver impairment | Contraindicated in active liver disease or unexplained persistent transaminase elevations. Child-Pugh Class A: use with caution; Class B or C: not recommended. |
| Pediatric use | For heterozygous familial hypercholesterolemia: 20 mg orally once daily initially, may increase up to 80 mg once daily (immediate-release) based on response. Limited data for children <10 years. |
| Geriatric use | No specific dose adjustment; consider increased risk of myopathy and rhabdomyolysis, especially with higher doses or concurrent interacting medications. Use lowest effective dose. |
| 1st trimester | Avoid. Animal studies show teratogenic effects; no adequate human studies. |
| 2nd trimester | Avoid. Potential fetal harm; use only if benefit outweighs risk. |
| 3rd trimester | Avoid. Risk of fetal skeletal abnormalities and impaired growth. |
Clinical note
Can increase the effects of warfarin and other drugs metabolized by CYP2C9 Can cause myopathy and rhabdomyolysis.
| Placental transfer | Crosses placenta; detectable in fetal plasma (animal studies). |
| Breastfeeding | Excreted into breast milk; potential for serious adverse effects in nursing infant. Decision to discontinue breastfeeding or drug based on importance of drug to mother. |
| Lactation Rating |
■ FDA Black Box Warning
Not applicable.
| Common Effects | Headache |
| Serious Effects |
Active liver diseaseUnexplained persistent elevations of serum transaminasesHypersensitivity to fluvastatin or any componentPregnancy
| Precautions | Myopathy/rhabdomyolysis risk increased with concomitant use of gemfibrozil, cyclosporine, or high-dose niacin, Hepatic enzyme elevations, Increased risk of diabetes mellitus, Use caution in patients with risk factors for myopathy, Avoid in pregnancy |
| Food/Dietary | Grapefruit juice may increase fluvastatin exposure and risk of adverse effects; patients should avoid grapefruit products. High-fat meals may reduce absorption; however, it can be taken with or without food. Alcohol should be limited due to potential hepatotoxicity. |
Loading safety data…
| L4 (Possibly Hazardous) |
| Teratogenic Risk | Fluvastatin is contraindicated in pregnancy. First trimester: Case reports suggest teratogenic potential, including skeletal and CNS defects; risk not quantified. Second and third trimesters: Theoretical risk of fetal toxicity from cholesterol synthesis inhibition; no human data. Absolute contraindication due to risk of embryotoxicity. |
| Fetal Monitoring | Monitor liver function tests (AST, ALT, bilirubin) at baseline and per routine; monitor for muscle symptoms (CPK if myopathy suspected). No specific fetal monitoring beyond standard obstetric care. |
| Fertility Effects | No published human data on effects on fertility. Animal studies show no adverse effects on male or female fertility at clinically relevant doses. |
| Clinical Pearls | Fluvastatin is a hydrophilic statin with lower potency than atorvastatin or rosuvastatin; it is less dependent on CYP3A4 metabolism (primarily CYP2C9), reducing some drug interactions. Its short half-life (2-3 hours) supports evening dosing for maximal LDL reduction. Monitor for myopathy, especially with gemfibrozil or cyclosporine; fluvastatin may have less drug interaction potential with warfarin than other statins. |
| Patient Advice | Take this medication once daily in the evening, with or without food. · Avoid grapefruit juice as it may increase the risk of side effects. · Report unexplained muscle pain, tenderness, or weakness, especially with fever or dark urine. · Avoid alcohol consumption as it may increase liver damage risk. · Notify your doctor if you have liver disease or if you use other medications like warfarin, gemfibrozil, or cyclosporine. |