Dosing & Uses
Dosage Forms & Strengths
tablets, extended release
Hypercholesterolemia & Mixed Dyslipidemia
Start 20-40 mg PO qHS
Dose range 20-80 mg PO qDay
If 80 mg/day needed, divide into 40 mg PO q12hr
Sustained-release (Lescol XL): 80 mg PO qDay
Patients Requiring <25% Decrease in LDL-C
20 mg PO qDay; may adjust dose based on response and tolerability not to exceed 40 mg PO q12hr (immediate release capsule) or 80 mg PO q24hr extended release tablet
CrCl <30 mL/min: Adjust dose amount; not to exceed 40 mg/day
Contraindicated in active liver disease or unexplained transaminase elevations
Adverse drug reactions from overdose may include peripheral neuropathy, diarrhea, increased K+, myopathy, rhabdomyolysis, acute renal failure, elevated LFT's, eye lens opacities
Treatment is supportive
Dosage Forms & Strengths
tablets, extended release
Heterozygous Familial Hypercholesterolemia
Indicated for adolescents unresponsive to dietary restriction and LDL-C remains >190 mg/dL, OR LDL-C >160 mg/dL AND positive family history exists or 2 or more cardivascular risk factors; girls must be at least 1 year postmenarche
<10 years: Safety and efficacy not established
10-16 years: 20 mg PO qHS initially; may increase dose at 6 week intervals up to 40 mg PO q12hr immediate release or 80 mg (Lescol XL) PO qDay
Serious - Use Alternative
Significant - Monitor Closely
Abdominal pain (5%)
Transaminases increased (1.1%)
Rupture of tendon
Musculoskeletal: Muscle cramps, myalgia, myopathy, rhabdomyolysis, arthralgias, muscle spasms, muscle weakness, myositis
Neurological: Dysfunction of certain cranial nerves (including alteration of taste, impairment of extra-ocular movement, facial paresis), tremor, dizziness, vertigo, paresthesia, hypoesthesia, dysesthesia, peripheral neuropathy, peripheral nerve palsy; also rare reports of cognitive impairment (eg, memory loss, forgetfulness, amnesia, memory impairment, confusion) associated with statin use
Psychiatric: Anxiety, insomnia, depression, psychic disturbances
Hypersensitivity reactions: Hypersensitivity syndrome including anaphylaxis, angioedema, lupus erythematosus-like syndrome, polymyalgia rheumatica, vasculitis, purpura, thrombocytopenia, leukopenia, hemolytic anemia, positive ANA, increased ESR, eosinophilia, arthritis, arthralgia, urticaria, asthenia, photosensitivity reaction, fever, chills, flushing, malaise, dyspnea, toxic epidermal necrolysis, and erythema multiforme including Stevens-Johnson syndrome
Gastrointestinal: Pancreatitis, hepatitis, including chronic active hepatitis, cholestatic jaundice, fatty change in liver, cirrhosis, fulminant hepatic necrosis, hepatoma, anorexia, vomiting, fatal and nonfatal hepatic failure
Skin: Rash, dermatitis, including bullous dermatitis, eczema, alopecia, pruritus, a variety of skin changes (eg, nodules, discoloration, dryness of skin/mucous membranes, changes to hair/nails)
Reproductive: Gynecomastia, loss of libido, erectile dysfunction
Eye: Progression of cataracts (lens opacities), ophthalmoplegia
Laboratory abnormalities: Elevated transaminases, alkaline phosphatase, gamma-glutamyl transpeptidase and bilirubin; thyroid function abnormalities
Hypersensitivity to fluvastatin
Active liver disease, or unexplained elevated transminases
Non-serious and reversible cognitive side effects may occur
Increased blood sugar and glycosylated hemoglobin (HbA1c) levels reported with statin intake
Heavy alcohol use, history of liver disease, renal failure
Myopathy, risk of myopathy - incr by co-administration w/ fibrates, niacin, cyclosporine, macrolides, azole antifungals.
Withhold or discontinue treatment if myopathy develops, renal failure, or transaminase levels >3 times the upper limit of normal
Rare reports of immune-mediated necrotizing myopathy (IMNM), characterized by increased serum creatine kinase that persist despite discontinuing statin
Lipid-lowering effects additive with bile-acid binding resin or niacin
Take 2 hr after bile acid sequestrant
Pregnancy & Lactation
Pregnancy Category: X
Lactation: enters breast milk; contraindicated
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
HMG-CoA reductase inhibitor, inhibits the rate-limiting step in cholesterol biosynthesis by competitively inhibiting HMG-CoA reductase
Bioavailability: 24% (capsule); 29% (extended release tablet)
Onset: 3-4 wk (Lescol)
Peak Plasma Time: 0.5-1 hr (capsule); 3hr (extended release tablet)
Protein Bound: 98% (Lescol)
Vd: 0.35 L/kg (Lescol)
Metabolite: No active metabolite
Metabolism: hepatic P450 enzyme CYP2C9 (75%); CYP2C8 (5%); CYP3A4 (20%)
Half-Life: <3 hr (capsule); 9hr (extended release tablet)
Total Body Clearance: 0.97 L/hr/kg (Lescol)
Excretion: feces (95%), urine (5%) (Lescol)
SLCO1B1 (OATP1B1) CC genotype significantly increases AUCs of parent drug and metabolites compared with the CT or TT genotypes
This polymorphism is proposed to reduced transport into the liver, the main site of statin metabolism and elimination, resulting in elevated plasma concentrations
SLCO1B1 polymorphism is thought to have a lesser effect on the more hydrophilic statins (eg, rosuvastatin, fluvastatin) compared with more those that are more lipophilic (eg, atorvastatin, pravastatin, simvastatin)
Other genetic polymorphisms of elimination (eg, CYP450, P-glycoprotein) for each individual drug must also be considered to explain variability for statin clearance among patients that exhibit SCLO1B1 polymorphism
SLCO1B1 CC genotype is most common in Caucasians and Asians (15%)
Risk of myopathy is 2.6- to 4.3-fold higher if the C allele is present and 16.9-fold higher in CC homozygotes compared with TT homozygotes
Genetic testing laboratories
- Optivia Biotechnology, Inc (http://optiviabio.com/index.html)
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