降血脂 (statin) Hypercholesterolemia; hypertriglyceridemia
#仿單變更2021#仿單變更2022

Antilipemic Agent, HMG-CoA Reductase Inhibitor
Inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol synthesis (reduces the production of mevalonic acid from HMG-CoA); this then results in a compensatory increase in the expression of LDL receptors on hepatocyte membranes and a stimulation of LDL catabolism.

Absorption
1. Rapidly absorbed; extensive first-pass metabolism in GI mucosa and liver
2. Onset of action: (Initial changes) 3 to 5 days; (Maximal reduction in plasma cholesterol and triglycerides) 2 to 4 weeks
3. Bioavailability: ~14% (parent drug); ~30% (parent drug and equipotent metabolites)
4. Time to peak, serum: 1 to 2 hours
Distribution:
1. Vd: ~381 L
2. Protein binding: 98%
Metabolism:
1. Hepatic via CYP3A4; forms active ortho- and parahydroxylated derivatives and an inactive beta-oxidation product; plasma concentrations are elevated in patients with chronic alcoholic liver disease and Child-Pugh class A and B liver disease
2. Half-life elimination: (Parent drug) ~14 hours; (Equipotent metabolites) 20 to 30 hours
Excretion:
Bile (following hepatic and/or extra-hepatic metabolism; does not appear to undergo enterohepatic recirculation); urine (<2% as unchanged drug)

1. Active liver disease
2. Unexplained, persistent elevation of serum transaminases
3. Pregnancy and lactation
4. Hypersensitivity to atorvastatin

Use is contraindicated in breastfeeding women.

Atorvastatin should be discontinued immediately if an unplanned pregnancy occurs during treatment.

Significant:
1. Hepatic effects
2. Muscle-related effects: Myalgia, Myopathy, Rhabdomyolysis, Immune-mediated necrotizing myopathy <20220407>
Common:
Headache, diarrhea, flatulence, mild elevations in liver enzymes, arthralgia, nasopharyngitis

10-80 mg PO QD

1. Mild to severe impairment: No dosage adjustment necessary
2. Hemodialysis: Poorly dialyzed; No supplemental dose or dosage adjustment necessary
3. Peritoneal dialysis, CRRT, PIRRT: No dosage adjustment necessary

1. Contraindicated in active liver disease or in patients with unexplained persistent elevations of serum transaminases.
2.It is recommended to monitor liver function when clinical symptoms of liver injury appear before medication, when the dose is increased, when drug items are changed, or when the clinician considers it necessary.<20230721>