inclisiran

Contraindicated in:

Hypersensitivity;
OB: Pregnancy.

Use Cautiously in:

End-stage renal disease;
Severe hepatic impairment;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

GI: diarrhea

GU: urinary tract infection

Local: injection site reactions

MS: arthralgia, pain

Resp: bronchitis, dyspnea

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

None reported.

Availability ⬆ ⬇

Solution for SUBQ injection: 284 mg/1.5 mL

Route/Dosage ⬆ ⬇

SC (Adults ): 284 mg as a single dose initially, then in 3 mo, then every 6 mo thereafter.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as a small interfering ribonucleic acid that is taken up by hepatocytes. In hepatocytes, it causes breakdown of mRNA for proprotein convertase subtilisin kexin type 9 (PCSK9), which ultimately increases low-density lipoprotein cholesterol (LDL-C) uptake and lowers LDL-C levels.

Therapeutic effects:

Reduction in LDL-C levels.

Classifications ⬆ ⬇

Therapeutic Classification: lipid-lowering agents

Pharmacologic Classification: small interfering ribonucleic acid agents

Pharmacokinetics ⬆ ⬇

Absorption: Extent of absorption unknown following SUBQ administration.

Distribution: Widely distributed to tissues.

Metabolism/Excretion: Primarily metabolized by nucleases to shorter nucleotides. 16% excreted in the urine.

Half-Life: 9 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
SUBQ	unknown	4 hr	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Explain need for continued medical follow-up to assess effectiveness and possible side effects of medication. Periodic lab tests will be needed.
Advise patient that this medication should be used in conjunction with diet restrictions (fat, cholesterol, carbohydrates, alcohol), exercise, and cessation of smoking.
Educate patient that injection site reaction symptoms are usually mild (redness, swelling, itching, pain, tenderness, warmth, bruising, burning, or a small amount of bleeding) and last for 1–3 days.
Advise patient to notify health care professional of medication regimen before treatment or surgery.
Rep: May cause fetal harm. Advise females or reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Discontinue inclisiran when pregnancy is recognized.

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Indications ⬇

Contraind./Precautions ⬆ ⬇