Dosing & Uses
Dosage Forms & Strengths
Hypertension/Angina & Hyperlipidemia
Dosage must be individualized for each individual component for treatment of hypertension, angina, and/or hyperlipidemia; amlodipine dose may be titrated after 1-2 weeks and the atorvastatin dose after 2-4 weeks; not to exceed 10 mg amlodipine or 80 mg atorvastatin
2.5-10 mg amlodipine; 10-80 mg atorvastatin PO qDay
Dose adjustment not necessary
Contraindicated in active liver disease
Dosage Forms & Strengths
Hypertension & Hyperlipidemia
Dosage must be individualized for each individual component for treatment of hypertension/hyperlipidemia; amlodipine dose may be titrated after 1-2 weeks and the atorvastatin dose after 2-4 weeks; not to exceed 5 mg amlodipine or 20 mg atorvastatin
<6 years: Safety and efficacy not established
>6 years: 2.5-5 mg amlodipine; 10-20 mg atorvastatin PO qDay
Consider initiating amlodipine dose at lower end of the spectrum due to possible decrease in renal or hepatic clearance
Serious - Use Alternative
Significant - Monitor Closely
- Peripheral edema (2-15%)
- Arthralgia (4-12%)
- Diarrhea (5-14%)
- Nasopharingitis (4-13%)
- Palpitation (1-5%)
- Dizziness (1-3%)
- Flushing (1-5%)
- Somnolence (1-2%)
- Rash (1-2%)
- Fatigue (5%)
- Pruritus (1-2%)
- Male sexual dysfunction (1-2%)
- Nausea (3%)
- Dyspepsia (1-2%)
- Dyspnea (1-2%)
- Weakness (1-2%)
- Nausea (4-7%)
- Dyspepsia (3-6%)
- Increased transaminases (2-3% with 80 mg/day)
- Urinary tract infection (4-8%)
- Insomnia (1-5%)
- Myalgia (3-8%)
- Musculoskeletal pain (2-5%)
- Respiratory pharyngeal pain (1-4%)
- Abnormal vision
- Chest pain
- Abnormal dreams
- Increased apetite
- Acute interstitial nephritis
- Bullous rash
- Biliary pain
- Cholestatic jaundice
- Duodenal ulcer
Hypersensitivity to amlodipine or atorvastatin
Active liver disease, or unexplained elevated transminases
Hypotension with or without syncope is possible (particularly with severe aortic stenosis)
Persistent progressive dermatologic reactions
Exacerbation of angina and/or MI (during initiation of treatment, after dose increase, or withdrawal of beta blocker)
Caution in liver impairment
Heavy alcohol use, history of liver disease, renal failure
Rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported with the atorvastatin
Myopathy, risk of myopathy increased by coadministration with CYP3A4 inhibiors (eg, fibrates, niacin, cyclosporine, macrolides, azole antifungals); therapy should be discontinued if myopathy diagnosed or suspected
Co-administration with CYP3A inhibitors (moderate and strong) results in increased systemic exposure to amlodipine and may require dose reduction; monitor for symptoms of hypotension and edema when amlodipine is co-administered with CYP3A inhibitors to determine the need for dose adjustment
Rare reports of immune-mediated necrotizing myopathy (IMNM), characterized by increased serum creatine kinase that persist despite discontinuing statin
Withhold or discontinue if myopathy, renal failure, or transaminase levels >3x ULN develops
Use in patients with recent stroke or TIA: SPARCL study observed higher incidence of hemorrhagic stroke with atorvastatin 80 mg (compared with placebo)
Increased HbA1c and fasting serum glucose levels reported with HMG-CoA reductase inhibitors
Clarithromycin, itraconazole, HIV protease inhibitors (saquinavir plus ritonavir, darunavir plus ritonavir, fosamprenavir, fosamprenavir plus ritonavir) may increase risk of myopathy/rhabdomyolysis; do not exceed 20 mg atorvastatin
Amlodipine may increase systemic exposure of cyclosporine or tacrolimus when co-administered; frequent monitoring of trough blood levels of cyclosporine and tacrolimus recommended; adjust dose when appropriate
Pregnancy & Lactation
Pregnancy Category: X
Lactation: It is not known whether atorvastatin is excreted into human milk. Because statins have the potential for serious adverse reactions in nursing infants, women taking this drug should not breastfeed their infants
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
Amlodipine: Ca channel blocker: inhibits extracellular Ca ions across the membranes of myocardial cells and vascular smooth muscle cells, without changing serum calcium concentrations, resulting in inhibition of cardiac & vascular smooth muscle contraction, thereby dilating the main coronary and systemic arteries
Atorvastatin: HMG-CoA reductase inhibitor, inhibits rate-limiting step in cholesterol biosynthesis by competitively inhibiting HMG-CoA reductase
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)
- Duration: 24 hr (antihypertensive effects)
- Vd: 21 L/kg
- Bioavailability: 64-90%
- Half-life: 30-50 hr
- Metabolism: Liver (>90%)
- Protein binding: 93-98%
- Peak plasma time: 6-12 hr
- Excretion: Urine (70%)
- Bioavailability: 30 %
- Vd: 381 L
- Protein binding: >98%
- Half-life: 14 hr (parent drug); 20-30 hr (active metabolites)
- Peak plasma time: 1-2 hr
- Onset of action: 3-5 days
- Excretion: Bile; urine (< 2% as unchanged drug)
Adding plans allows you to compare formulary status to other drugs in the same class.
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Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.
|1||This drug is available at the lowest co-pay. Most commonly, these are generic drugs.|
|2||This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.|
|3||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.|
|NC||NOT COVERED – Drugs that are not covered by the plan.|
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.