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| __NOTOC__
| | #REDIRECT [[Fluvastatin#Pharmacology]] |
| {{drugbox
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| | IUPAC_name = 7-[3-(4-fluorophenyl) -1-(1-methylethyl) -1H-indol-2-yl]-3, 5-dihydroxy-hept-6-enoic acid
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| | image = Fluvastatin.png
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| | width = 157
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| | CAS_number = 93957-54-1
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| | ATC_prefix = C10
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| | ATC_suffix = AA04
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| | ATC_supplemental =
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| | PubChem = 1548972
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| | DrugBank = APRD00346
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| | C=24 | H=26 | F=1 | N=1 | Oxygen|O=4
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| | molecular_weight = 411.466 g/mol
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| | bioavailability =
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| | protein_bound = 98%
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| | metabolism =
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| | elimination_half-life = 2.5 hours
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| | pregnancy_category =
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| | legal_status =
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| | routes_of_administration =
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| }}
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| {{SI}}
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| {{CMG}}
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| ==[[Fluvastatin (patient information)|For patient information, click here]]==
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| ==Overview==
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| Class: Antihyperlipidemic, HMG-CoA reductase inhibitor
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| ==Trade Names==
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| Lescol
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| - Capsules 20 mg
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| - Capsules 40 mg
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| Lescol XL
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| - Tablets, extended-release 80 mg
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| ==Pharmacology==
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| Increases rate at which body removes cholesterol from blood and reduces production of cholesterol in body by inhibiting enzyme that catalyzes early rate-limiting step in cholesterol synthesis; increases HDL; reduces LDL, VLDL, and triglycerides.
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| ==Pharmacokinetics==
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| ===Absorption===
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| Absolute bioavailability is 9% to 50%. The relative bioavailability for the extended-release (ER) form is 9% to 66%. T max is less than 1 h. C max is 48.9 to 990 ng/mL.
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| ===Immediate-release===
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| Administration with food at steady state increases T max and decreases C max .
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| ===ER===
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| Administration with a high-fat meal increases bioavailability by about 50%.
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| ===Distribution===
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| Fluvastatin is 98% protein bound. The mean Vd at steady state is about 0.35 L/kg.
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| ===Metabolism===
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| No active metabolites are present systemically. The drug is metabolized in the liver primarily via hydroxylation; oxidation occurs via CYP2C9 isozyme systems (75%), 3A4 (about 20%), and 2C8 (about 5%).
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| ===Elimination===
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| About 90% is excreted in feces as metabolites, and less than 2% is unchanged. The t ½ is less than 3 h.
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| ==Special Populations==
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| Hepatic Function Impairment
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| AUC and C max increase 2.5-fold.
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| ==Indications and Usage==
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| ===Atherosclerosis===
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| To slow the progression of coronary atherosclerosis
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| ===Heterozygous familial hypercholesterolemia in children===
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| Adjunct to diet to reduce total-cholesterol (C), LDL-C, and apolipoprotein (apo) B levels in adolescent boys and girls at least 1 yr post-menarche whose response to dietary restriction has not been adequate and who have the following: 1) LDL-C remains at a value of at least 190 mg/dL, or 2) LDL-C remains at a level of 160 mg/dL or more and there is a positive family history of premature CV disease, or 2 or more other CV disease risk factors are present.
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| ===Hypercholesterolemia===
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| Reduction of elevated total-C, LDL, apo B, and triglyceride cholesterol levels, and to increase HDL levels.
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| ===Secondary prevention of coronary events===
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| To reduce the risk of undergoing coronary revascularization procedures in patients with coronary heart disease.
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| ==Contraindications==
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| Active liver disease or unexplained persistent elevations of LFTs; pregnancy; lactation.
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| ==Dosage and Administration==
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| ===Adults===
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| PO 20 to 80 mg daily.
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| General Advice
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| * Administer without regard to meals, but administer with food if GI upset occurs.
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| * Have patient swallow ER tablets whole. Tablets should not be crushed, chewed, or cut.
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| ==Storage/Stability==
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| Store capsules and tablets at controlled room temperature (59° to 86°F). Protect from light.
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| ==Drug Interactions==
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| ===Azole antifungal agents (eg, fluconazole), cyclosporine, gemfibrozil, macrolide antibiotics (eg, erythromycin), niacin===
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| Severe myopathy or rhabdomyolysis may occur with coadministration.
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| ===Cholestyramine===
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| Reduced absorption of fluvastatin if taken with or up to 4 h after cholestyramine.
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| ===Cimetidine, cyclosporine, fluconazole, omeprazole, ranitidine===
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| Fluvastatin serum levels may be increased.
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| ===Diclofenac, digoxin, glyburide, hydantoins===
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| Serum levels of these agents may be increased.
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| ===Rifampin===
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| Fluvastatin serum levels may be reduced.
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| ===Warfarin===
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| Anticoagulant effect of warfarin may be increased.
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| ==Laboratory Test Interactions==
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| None well documented.
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| ==Adverse Reactions==
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| ===CNS===
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| Headache (9%); fatigue, insomnia (3%).
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| ===ENT===
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| Sinusitis (4%).
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| ===GI===
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| Dyspepsia (8%); abdominal pain, diarrhea (5%); flatulence, nausea (3%).
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| ===Genitourinary===
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| UTI (3%).
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| ===Musculoskeletal===
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| Myalgia (5%).
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| ===Respiratory===
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| Bronchitis (3%).
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| ===Miscellaneous===
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| Flu-like symptoms (7%); accidental trauma (5%).
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| ==Precautions==
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| ===Monitor===
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| Ensure that serum cholesterol and triglycerides are measured before therapy is started and not less than 4 wk of starting therapy or changing the fluvastatin dose, and then periodically thereafter.
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| ===Pregnancy===
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| Category X .
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| ===Lactation===
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| Excreted in breast milk; patients should not breast-feed while taking.
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| Children
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| Heterozygous familial hypercholesterolemia
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| Safety and efficacy not established in children younger than 9 years of age.
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| ===Endocrine effects===
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| Use caution when administering HMG-CoA reductase inhibitors with drugs that affect steroid levels or activity.
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| ==LFTs==
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| Perform LFTs before initiating therapy, at 12 wk (or after elevation in dose), and periodically thereafter.
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| ===Hepatic function impairment===
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| Use with caution in patients who consume substantial quantities of alcohol or who have a history of liver disease. If elevated serum transaminase levels develop during treatment, repeat levels more frequently. Be prepared to reduce dose or discontinue therapy.
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| ===Secondary causes of hypercholesterolemia===
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| Ensure that secondary causes of hypercholesterolemia (eg, poorly controlled diabetes, hypothyroidism) are excluded before starting therapy.
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| ===Skeletal muscle effects===
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| Rhabdomyolysis with renal function impairment secondary to myoglobinuria has been reported with other drugs in this class. Temporarily withhold therapy in any patient experiencing an acute or serious condition suggestive of myopathy or predisposing to the development of renal failure secondary to rhabdomyolysis (eg, sepsis, hypotension). The risk of myopathy with other drugs in this class was found to be increased if therapy with either cyclosporine, gemfibrozil, erythromycin, or niacin is coadministered. Consider myopathy in any patient with diffuse myalgias, muscle tenderness or weakness, or marked elevations of CPK.
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| ==Patient Information==
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| * Advise patient to take prescribed dose without regard to meals but to take with food if stomach upset occurs.
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| * Instruct patient to swallow ER tablet whole and not to cut, chew, or crush the tablet.
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| * Advise patient who is also taking a bile acid resin (eg, cholestyramine) to take the resin at least 2 h before fluvastatin.
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| * Advise patient to try to take each dose(s) at about the same time each day.
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| * Inform patient that drug helps control, but does not cure, cholesterol abnormality and instruct patient to continue taking drug as prescribed if cholesterol levels are lowered.
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| * Advise patient that if a dose is missed, to take it as soon as remembered but never to take more than 1 dose of medicine a day.
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| * Instruct patient to continue taking other cholesterol-lowering medications as prescribed by health care provider.
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| * Emphasize to patient importance of following other modalities on cholesterol control: dietary changes (eg, reduced saturated fat intake, increased soluble fiber intake), weight control, regular exercise, and smoking cessation.
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| * Advise women of childbearing potential to use effective contraception during treatment with fluvastatin, and that the drug should be discontinued immediately if pregnancy occurs.
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| * Instruct patient to notify health care provider if experiencing any unexplained muscle pain, tenderness, and/or weakness, or any other unusual feelings.
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| {{Statins}}
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| [[Category:Statins]]
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| [[Category:Cardiology]]
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| [[Category:Drugs]]
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| [[es:Fluvastatina]]
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| [[nl:Fluvastatine]]
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| [[th:ฟลูวาสแตติน]]
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