Mechanism of Action
HMG-CoA reductase inhibitor, inhibits rate-limiting step in cholesterol biosynthesis by competitively inhibiting HMG-CoA reductase
Pharmacokinetics
Bioavailability: 14% (parent drug)
Onset: 3-5 days
Duration: 48-72 hr
Peak serum time: 1-2 hr
Maximum effect: 2 weeks
Excretion: Mainly via bile, urine (2%)
Contraindications
• Hypersensitivity to atorvastatin
• Acute liver failure or decompensated cirrhosis
Adverse Reactions
Diarrhea, Nasopharyngitis, Arthralgia, Insomnia, Urinary tract infection, Nausea, Dyspepsia, Increased transaminases, Muscle spasms, Musculoskeletal pain, Myalgia, Limb pain, Pharyngolaryngeal pain
Major Drug Interactions
Cyclosporine - Gemfibrozil - Lonafarnib - Pazopanib - Red Yeast Rice - Tipranavir
Warnings
• Therapy may cause myopathy (muscle pain, tenderness, or weakness with creatine kinase (CK) above ten times upper limit of normal) and rhabdomyolysis (with or without acute renal failure secondary to myoglobinuria)
• Risk factors for myopathy include age 65 years or greater, uncontrolled hypothyroidism, renal impairment, concomitant use with certain other drugs, and higher dosage
• Discontinue therapy if markedly elevated CK levels occur or myopathy is diagnosed or suspected
Recommendations for Patient
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Pregnancy Considerations
Most patients should stop statins once they learn they are pregnant.
Breastfeeding Considerations
Patients should not breastfeed when taking a statin because it may pass into breast milk and pose a risk to the baby. Many can stop statins temporarily until breastfeeding ends.
Pregnancy Categories
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.
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