Alirocumab


Generic Medicine Info
Indications and Dosage
Subcutaneous
Heterozygous familial hypercholesterolaemia, Mixed dyslipidaemia, Nonfamilial hypercholesterolaemia
Adult: Adjunct to diet, alone or in combination with statin therapy and/or other lipid-lowering treatments: Initially, 75 mg once every 2 weeks. Alternatively, an initial dose of 150 mg once every 2 weeks or 300 mg once every 4 weeks may be given in patients requiring >60% LDL-C reduction. If LDL-C response is inadequate for the 75 mg once every 2 weeks or 300 mg once every 4 weeks initial dosing, the dose may be adjusted to a Max of 150 mg once every 2 weeks. Assess LDL-C levels within 4-8 weeks after treatment initiation or titration and adjust the dose if needed. Individualise dosing according to the patient's baseline LDL-C level, goals of therapy, and response. Dosage and treatment recommendations may vary between countries (refer to detailed local guidelines).

Subcutaneous
Cardiovascular risk reduction
Adult: To reduce the risk of CV events (e.g. MI, stroke, unstable angina requiring hospitalisation) by decreasing LDL-C levels in patients with established atherosclerotic CV disease: Alone or in combination with the maximally tolerated statin dose and/or other lipid-lowering therapies: Initially, 75 mg once every 2 weeks. Alternatively, an initial dose of 150 mg once every 2 weeks or 300 mg once every 4 weeks may be given in patients requiring >60% LDL-C reduction. If LDL-C response is inadequate for the 75 mg once every 2 weeks or 300 mg once every 4 weeks initial dosing, the dose may be adjusted to a Max of 150 mg once every 2 weeks. Assess LDL-C levels within 4-8 weeks after treatment initiation or titration and adjust the dose if needed. Individualise dosing according to the patient's baseline LDL-C level, goals of therapy, and response. Dosage and treatment recommendations may vary between countries (refer to detailed local guidelines).
Contraindications
Hypersensitivity.
Special Precautions
Severe renal and hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Hypersensitivity reactions (e.g. hypersensitivity vasculitis, angioedema, nummular eczema).
Gastrointestinal disorders: Diarrhoea.
General disorders and administration site conditions: Local inj site reactions (e.g. pruritus, erythema, pain/tenderness, swelling).
Immune system disorders: Antibody development.
Investigations: Increased serum transaminases.
Musculoskeletal and connective tissue disorders: Muscle spasms. myalgia.
Respiratory, thoracic and mediastinal disorders: Cough, nasopharyngitis, influenza, upper respiratory tract symptoms (e.g. oropharyngeal pain, rhinorrhoea, sneezing).
Skin and subcutaneous tissue disorders: Pruritus, urticaria, rash.
Monitoring Parameters
Evaluate and exclude secondary causes of hyperlipidaemia or mixed dyslipidaemia (e.g. nephrotic syndrome, hypothyroidism) prior to treatment initiation. Monitor lipid levels at baseline, then 4-8 weeks after treatment initiation or titration, and then every 3-12 months thereafter. For patients receiving 300 mg once every 4 weeks, obtain LDL-C levels just prior to the next scheduled dose (LDL-C may vary between doses in some patients). Assess for signs and symptoms of hypersensitivity reactions.
Drug Interactions
Increased target-mediated clearance and reduced systemic exposure with statins and other lipid-lowering agents (e.g. ezetimibe, fenofibrate).
Action
Description:
Mechanism of Action: Alirocumab is a human IgG1 monoclonal antibody that binds to proprotein convertase subtilisin kexin type 9 (PCSK9), a protein which binds to LDL receptors (LDLR) on hepatocyte surfaces to promote the degradation of LDLR in the liver. Since LDLRs are responsible for the clearance of circulating LDL, the decrease in LDLR levels by PCSK9 leads to higher LDL-C blood levels. As alirocumab inhibits the binding of PCSK9 to LDLR, the available number of LDLRs is increased to clear LDL thus lowering plasma LDL-C levels.
Pharmacokinetics:
Absorption: Bioavailability: Approx 85% (SC). Time to peak plasma concentration: 3-7 days (SC).
Distribution: Crosses the placenta.
Metabolism: Undergoes proteolysis to form small peptides and amino acids.
Excretion: Elimination half-life: SC: 17-20 days, decreased to 12 days when given with statins.
Storage
Pre-filled pen or syringe: Store between 2-8°C. Do not freeze. If necessary, may be stored at room temperature (<25°C) for a single period of up to 30 days. After removal from the refrigerator, it should be used within 30 days or discarded. Keep in the original carton to protect from light. Do not expose to extreme heat or shake.
MIMS Class
Dyslipidaemic Agents
ATC Classification
C10AX14 - alirocumab ; Belongs to the class of other lipid modifying agents.
References
Anon. Alirocumab. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 02/08/2023.

Anon. Alirocumab. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 02/08/2023.

Buckingham R (ed). Alirocumab. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/08/2023.

Joint Formulary Committee. Alirocumab. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/08/2023.

Pharmacy Retailing (NZ) Ltd t/a Healthcare Logistics. Praluent 75 mg and 150 mg Solution for Injection in Pre-filled Pen or Syringe data sheet 20 June 2022. Medsafe. http://www.medsafe.govt.nz. Accessed 02/08/2023.

Praluent 75 mg and 150 mg Solution for Injection in Pre-filled Pen or Syringe (Sanofi-Aventis [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia.  https://www.npra.gov.my. Accessed 02/08/2023.

Praluent 75 mg Solution for Injection in Pre-filled Pen (Aventis Pharma Limited, Trading as Sanofi). MHRA. https://products.mhra.gov.uk. Accessed 02/08/2023.

Praluent Injection, Solution (Sanofi US Corporation). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/08/2023.

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 © 2024 MIMS. All rights reserved. Powered by MIMS.com
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