alirocumab, Praluent

 Indications

Lowering of low density lipoprotein cholesterol (LDLC)

as an adjunct to diet and maximally tolerated statin

(HMG CoA reductase inhibitor) therapy in patients with

heterozygous familial hypercholesterolemia (HeFH) or

cardiovascular disease who require supplemental

agents.

Action

A human monoclonal immunoglobulin (IgG1) produced

in genetically engineered Chinese hamster ovary

cells that binds to PCSK9 inhibiting its binding to the

low density lipoprotein receptor (LDLR) resulting inq

number of LDLRs available to clear LDL from blood.

Therapeutic Effects:pLDL-C.

Pharmacokinetics

Absorption: Well absorbed (85%) following subcut

administration.

Distribution: Mostly distributed in the circulatory

system; crosses the placenta.

Metabolism and Excretion: Eliminated by binding

to PCSK9 and by proteolytic degradation.

Half-life: 17–20 days.

TIME/ACTION PROFILE (effect circulating

unbound PCSK9)

ROUTE ONSET PEAK DURATION

subcut rapid 4–8 hr 2 wk

Contraindications/Precautions

Contraindicated in: History of serious hypersensitivity

to alirocumab.

Use Cautiously in: Severe renal/hepatic impairment;

Geri: Elderly patients may be more sensitive to drug effects; OB: Crosses the placenta, consider fetal

risks; Lactation: Consider benefits of breast feeding

against possible risk to infant; Pedi: Safe and effective

use in children has not been established.

Adverse Reactions/Side Effects

CNS: confusion. Local: injection site reactions.

Misc: serious allergic reactions including VASCULITIS.

Interactions

Drug-Drug: None noted.

Route/Dosage

Subcut (Adults): 75 mg every 2 wk; if desired LDL-C

has not been achieved, dose may beqto 150 mg every

2 wk. If less frequent dosing desired, may initiate therapy

with 300 mg every 4 wk; if desired LDL-C has not

been achieved, may adjust dose to 150 mg every 2 wk.

Availability

Solution for subcutaneous injection: 75 mg/mL (in

prefilled pen or prefilled syringe), 150 mg/mL (in

prefilled pen or prefilled syringe).