Drug reference

Alirocumab

Statin · Lipid-lowering agent

StatinLipid-lowering agent

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

—

not curated

Top interactionssee all 12 →

AmiodaroneSevereTextbookG&G 14e · p736
Azole AntifungalsSevereTextbookG&G 14e · p736
CyclosporineSevereTextbookG&G 14e · p736
ErythromycinSevereTextbookKDT 7e · p637

Mechanism

Alirocumab is a humanized antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9). PCSK9 normally binds to the LDL receptor on the hepatic cell surface, leading to its degradation in lysosomes. By blocking this interaction, alirocumab allows the LDL receptor to recycle to the cell surface, increasing the uptake and clearance of LDL cholesterol from the blood.

Indications

Familial hypercholesterolemiaClinical atherosclerotic cardiovascular disease requiring additional LDL reductionHigh-risk patients with uncontrolled cholesterol despite other lipid-lowering therapyfamilial hypercholesterolemia (FH)other lipid disordersLower risk of myocardial infarction, stroke, and unstable angina requiring hospitalization in patients with established cardiovascular diseaseLower LDL-C as adjunctive therapy alone or in combination with other LDL-C–lowering medication in adult patients with HeFHLower LDL-C as adjunctive therapy in combination with other LDL-C–lowering medications in adult patients with HoFHFurther reduction of LDL-C and prevention of future cardiovascular events in ACS patients not adequately responding to maximally tolerated statin therapy

Dosing

Adult: 75 or 150 mg subcutaneously every 14 days, or 300 mg subcutaneously monthly

Pharmacokinetics

Half-life

11–20 days (availability for 2-3 weeks after administration)

Excretion

As with other monoclonal antibodies, degraded into small peptides and amino acids via catabolic pathways

Contraindications

Pregnancy (transplacental transmission expected)

Side effects

Common

NasopharyngitisUrinary tract infectionsUpper respiratory infectionsInjection site reactions (<10%)

Serious

Neurocognitive effects (small risk <1%)

Pregnancy & lactation

Lactation

Not recommended for use during lactation as it is not known to what degree the medication will be present in breast milk.

Drug interactions

Amiodarone

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.

Source: G&G 14e · p736

Azole Antifungals

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.

Source: G&G 14e · p736

Cyclosporine

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy. For simvastatin, coadministration is contraindicated.

Source: G&G 14e · p736

Erythromycin

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

Concomitant use should be avoided or used with extreme caution, especially for statins metabolized by CYP3A4. Dose reduction of the statin and vigilant monitoring for muscle symptoms are necessary.

Source: KDT 7e · p637

Gemfibrozil

Severe

Textbook

Increased plasma concentration of statin hydroxy acids, leading to an increased risk of myopathy (including rhabdomyolysis).

Avoid coadministration. The FDA withdrew approval for statin drug combinations containing fibrates in 2016.

Source: G&G 14e · p736

Hiv Protease Inhibitor

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

Concomitant use should be avoided or used with extreme caution, especially for statins metabolized by CYP3A4. Dose reduction of the statin and vigilant monitoring for muscle symptoms are necessary.

Source: KDT 7e · p637

Hiv Protease Inhibitors

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Source: G&G 14e · p736

Ketoconazole

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

Concomitant use should be avoided or used with extreme caution, especially for statins metabolized by CYP3A4. Dose reduction of the statin and vigilant monitoring for muscle symptoms are necessary.

Source: KDT 7e · p637

Macrolide Antibiotics

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Source: G&G 14e · p736

Nefazodone

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.

Source: G&G 14e · p736

Niacin

Severe

Textbook

Increased risk of myopathy.

Avoid coadministration. The FDA withdrew approval for statin drug combinations containing niacin in 2016.

Source: G&G 14e · p736

Nicotinic Acid

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

A lower dose of statin is advisable when nicotinic acid is given concurrently. Close monitoring for muscle symptoms is essential.