Alirocumab


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : SC Heterozygous familial hypercholesterolaemia; Nonfamilial hypercholesterolaemia; Mixed dyslipidaemia Monotherapy or adjunct to diet modification and statin therapy and other lipid-regulating agents: Initial: 75 mg once every 2 weeks, may increase to Max 150 mg once every 2 weeks. Alternatively, 300 mg once every 4 weeks. Patients requiring >60% LDL-C reduction or undergoing LDL apheresis: Initial: 150 mg once every 2 weeks. Dose is individualised according to response.
Dosage Details
Subcutaneous
Heterozygous familial hypercholesterolaemia, Mixed dyslipidaemia, Nonfamilial hypercholesterolaemia
Adult: As monotherapy or adjunct to diet modification and statin therapy and other lipid-regulating agents: Initially, 75 mg once every 2 weeks, may increase to Max 150 mg once every 2 weeks. Alternatively, 300 mg once every 4 weeks. Patients requiring >60% LDL-C reduction or undergoing LDL apheresis: Initially, 150 mg once every 2 weeks. Dose is individualised according to response.
Contraindications
Hypersensitivity.
Special Precautions
Severe renal and hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Hypersensitivity reactions (e.g. pruritus, nummular eczema, urticaria, hypersensitivity vasculitis, rash).
Gastrointestinal disorders: Diarrhoea.
Infections and infestations: Influenza.
Injury, poisoning and procedural complications: Local injection site reactions (e.g. erythema, itching, swelling, pain/tenderness).
Musculoskeletal and connective tissue disorders: Myalgia, muscle spasm.
Respiratory, thoracic and mediastinal disorders: Rhinorrhoea, oropharyngeal pain, nasopharyngitis, sneezing.
MonitoringParameters
Asses and exclude secondary causes of hyperlipidaemia or mixed dyslipidaemia (e.g. nephrotic syndrome, hypothyroidism) prior to initiation of therapy. Monitor lipid levels at baseline then 4-8 weeks after treatment initiation or titration and every 3-12 months thereafter. Assess lipid level prior to next schedule dose in patients receiving 300 mg monthly.
Drug Interactions
Increased target-mediated clearance and reduced systemic plasma concentration with statins and other lipid-lowering agents (e.g. ezetimibe, fenofibrate).
Action
Description: Alirocumab is a human monoclonal antibody (IgG1) which binds to proprotein convertase subtilisin kexin type 9 (PCSK9), a protein responsible for the recycling of LDL receptors (LDLR) on the hepatocyte surfaces. It acts by inhibiting PCSK9 from binding to LDLR thereby, increasing numbers of receptors available to clear out circulating LDL in the blood and lowering plasma LDL-cholesterol (LDL-C) levels.
Pharmacokinetics:
Absorption: Bioavailability: Approx 85% (SC). Time to peak plasma concentration: 3-7 days (SC).
Distribution: Crosses the placenta. Volume of distribution: Approx 0.04-0.05 L/kg (IV).
Metabolism: Undergoes proteolysis to small peptides and amino acids.
Excretion: Elimination half-life: 17-20 days (SC); 12 days with statins.
Storage
Store between 2-8°C. Do not freeze. Protect from light. Do not shake.
ATC Classification
C10AX14 - alirocumab ; Belongs to the class of other lipid modifying agents.
Disclaimer: This information is independently developed by MIMS based on Alirocumab from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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