ATORVALIQ
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ATORVALIQ (ATORVALIQ).
ATORVALIQ is a combination of atorvastatin and amlodipine. Atorvastatin is an HMG-CoA reductase inhibitor that decreases cholesterol synthesis in the liver. Amlodipine is a calcium channel blocker that inhibits calcium ion influx across cardiac and vascular smooth muscle, causing vasodilation.
| Metabolism | Atorvastatin is metabolized by CYP3A4; amlodipine is extensively metabolized by CYP3A4. |
| Excretion | Atorvastatin is primarily eliminated via biliary/fecal excretion (approximately 70% as metabolites), with renal excretion accounting for less than 2% of the administered dose. |
| Half-life | The terminal elimination half-life of atorvastatin is approximately 14 hours; however, its active metabolites have a half-life of 20-30 hours, allowing for once-daily dosing. |
| Protein binding | Atorvastatin is ≥98% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 381 L (5.4 L/kg for a 70 kg individual), indicating extensive tissue distribution. |
| Bioavailability | Oral bioavailability is approximately 14% due to extensive first-pass metabolism in the gut wall and liver. |
| Onset of Action | For oral administration, onset of lipid-lowering effects occurs within 2 weeks, with maximal effect seen at 4 weeks. |
| Duration of Action | Duration of action is approximately 24 hours, supporting once-daily dosing; continuous therapy is required for sustained lipid lowering. |
| Molecular Weight | 523.6 |
10-80 mg orally once daily. Starting dose 10-20 mg. Max dose 80 mg.
| Dosage form | SUSPENSION |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). Contraindicated in severe renal impairment (CrCl <30 mL/min) and dialysis. |
| Liver impairment | Contraindicated in active liver disease or unexplained persistent transaminase elevations. Child-Pugh Class A: use with caution, max 20 mg. Child-Pugh Class B or C: contraindicated. |
| Pediatric use | Not approved for patients younger than 10 years. For children 10-17 with heterozygous familial hypercholesterolemia: start 10 mg once daily; max 20 mg once daily. Adjust based on LDL-C response. |
| Geriatric use | No specific dose adjustment required in elderly. Monitor for increased risk of myopathy and renal function; use caution with doses ≥40 mg. |
| 1st trimester | Contraindicated: teratogenic effects (e.g., neural tube defects) based on animal studies and limited human data. Risk of fetal harm outweighs any potential benefit. |
| 2nd trimester | Contraindicated: continued risk of fetal toxicity, including potential for altered fetal growth and development. Alternative therapies should be used. |
| 3rd trimester | Contraindicated: risk of adverse fetal outcomes, including possible neonatal toxicity. Avoid use during third trimester. |
Clinical note
Comprehensive clinical and safety monograph for ATORVALIQ (ATORVALIQ).
| Placental transfer | Crosses placenta; detectable in fetal plasma at concentrations approximately 50% of maternal levels based on animal studies. |
| Breastfeeding | Excreted into breast milk in small amounts; however, due to potential for serious adverse reactions in nursing infants, breastfeeding is not recommended during therapy and for at least 5 days after the last dose. |
■ FDA Black Box Warning
No FDA boxed warning.
| Common Effects | Dyspepsia Abdominal pain Indigestion Diarrhea Joint pain Nasopharyngitis inflammation of the throat and nasal passages Nausea Pain in extremities Urinary tract infection Abnormal liver function tests |
| Serious Effects |
Hypersensitivity to atorvastatin or any componentActive liver disease or unexplained persistent elevations of serum transaminasesPregnancyBreastfeedingConcomitant use with strong CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, certain antivirals)
| Precautions | Hepatotoxicity: Measure liver enzymes before and during therapy. Discontinue if elevations persist., Myopathy/Rhabdomyolysis: Risk increased with higher doses, advanced age, renal impairment, and use with CYP3A4 inhibitors or other drugs that increase statin levels., Peripheral edema: Amlodipine can cause dose-dependent edema; use with caution in heart failure. |
| Food/Dietary |
Loading safety data…
| Lactation Rating | L5 (Contraindicated) |
| Teratogenic Risk | FDA Category X: Atorvastatin is contraindicated in pregnancy. First trimester exposure is associated with congenital anomalies (CNS, limb defects). Second and third trimester exposure may impair fetal development due to inhibition of cholesterol synthesis essential for fetal growth. Discontinue immediately upon pregnancy detection. |
| Fetal Monitoring | Maternal: Baseline and periodic liver function tests (ALT, AST), lipid profile, and CPK levels. Fetal: Ultrasound for developmental assessment if inadvertent exposure occurs. No routine fetal monitoring indicated beyond standard prenatal care. |
| Fertility Effects | No significant effect on fertility reported in animal studies. Reversible improvement in sperm parameters noted in some studies due to reduced oxidative stress. No adverse impact on female fertility in clinical data. |
| Avoid grapefruit juice and grapefruit products as they inhibit CYP3A4, increasing atorvastatin levels and risk of myopathy. High-fat meals may affect absorption; however, take consistently with or without food. Limit alcohol intake due to potential liver effects. |
| Clinical Pearls | ATORVALIQ is a combination of atorvastatin and ezetimibe. Dose adjustment may be needed in patients with renal impairment (eGFR <30 mL/min/1.73m²) or on certain CYP3A4 inhibitors. Monitor liver function tests before initiation and periodically thereafter. Avoid in active liver disease or unexplained persistent transaminase elevations. |
| Patient Advice | Take this medication exactly as prescribed, usually once daily at the same time, with or without food. · Do not take more than the prescribed dose; it can increase risk of muscle pain, liver damage, or other side effects. · Maintain a low-cholesterol, low-fat diet and exercise regularly to get the full benefit of the medication. · Notify your healthcare provider immediately if you experience unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or malaise. · Avoid grapefruit juice or grapefruit products while taking this medication, as they can increase the risk of side effects. · Inform your doctor about all other medications, including over-the-counter drugs, supplements, and herbal products, as many can interact with this drug. · Do not stop taking this medication without consulting your doctor, even if you feel well, as it is meant to be taken long-term. |