Liraglutide


Thông tin thuốc gốc
Chỉ định và Liều dùng
Subcutaneous
Type 2 diabetes mellitus
Adult: As an adjunct to diet and exercise: Monotherapy or in combination with other antidiabetic agents: Victoza Initially, 0.6 mg once daily for 1 week, then increase to 1.2 mg once daily; may further increase to 1.8 mg once daily after at least 1 week of treatment with 1.2 mg daily dose if additional glycaemic control is required.
Child: ≥10 years Victoza Same as adult dose.

Subcutaneous
Weight management
Adult: As an adjunct to a reduced-calorie diet and increased physical activity in patients with BMI ≥30 kg/m2 (obese) or ≥27 kg/m2 to <30 kg/m2 (overweight) with at least 1 weight-related comorbidity: Saxenda Initially, 0.6 mg once daily; may increase in increments of 0.6 mg at weekly intervals up to a maintenance dose of 3 mg once daily. Discontinue treatment if patients have not lost at least 5% of their initial body weight after 12 weeks on a 3 mg/day dosing.
Child: ≥12 years As an adjunct to a reduced-calorie diet and increased physical activity in patients weighing >60 kg or with BMI corresponding to ≥30 kg/m2 for adults (obese) by international cut-off points: Saxenda Same as adult dose. If the 3 mg maintenance dose is not tolerated, reduce to 2.4 mg daily; discontinue if the 2.4 mg dose is not tolerated. If the patient cannot tolerate an increased dose during dose escalation, consider lowering the dose to the previous level. Discontinue treatment if patients have not lost at least 4% of their initial body weight after 12 weeks on a 3 mg/day or Max tolerated dose.
Chống chỉ định
Hypersensitivity. Personal or family history of medullary thyroid carcinoma (MTC); multiple endocrine neoplasia syndrome type 2 (MEN 2), history of suicidal attempts or ideation; type 1 diabetes mellitus, diabetic ketoacidosis. Pregnancy.
Thận trọng
Patient with thyroid disease, history of anaphylaxis or angioedema with another GLP-1 agonist; obesity secondary to endocrinological or eating disorders or treatment (Saxenda). Not recommended for use in patients with CHF New York Heart Association (NYHA) class IV, inflammatory bowel disease, and diabetic gastroparesis. Victoza is not a substitute for insulin; Saxenda is not indicated for the treatment of type 2 diabetes mellitus. Do not switch between brands. Renal and hepatic impairment. Children; elderly (when used for weight management). Lactation.
Tác dụng không mong muốn
Significant: Antibody formation, increased resting heart rate, psychiatric effects (e.g. suicidal thoughts or behaviour), acute pancreatitis, goitre, dehydration, acute renal failure, worsening of chronic renal failure, cholelithiasis, cholecystitis, medullary thyroid carcinoma.
Gastrointestinal disorders: Nausea, vomiting, dyspepsia, upper abdominal pain, diarrhoea, constipation, dry mouth, gastritis, flatulence, abdominal distension, GERD, eructation, dysgeusia, abdominal discomfort, toothache, delayed gastric emptying.
General disorders and administration site conditions: Fatigue, inj site reactions, malaise, asthenia.
Investigations: Increased lipase, amylase, serum creatinine.
Metabolism and nutrition disorders: Hypoglycaemia, anorexia, decreased appetite.
Nervous system disorders: Headache, dizziness.
Psychiatric disorders: Insomnia.
Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, bronchitis.
Skin and subcutaneous tissue disorders: Rash, urticaria, pruritus.
Potentially Fatal: Serious hypersensitivity reactions (e.g. anaphylaxis, angioedema); haemorrhagic or necrotising pancreatitis.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor heart rate, plasma glucose, triglycerides, renal function; HBA1c at least twice yearly in patients with stable glycaemic control or quarterly in patients not meeting treatment goals or with changes in treatment; signs and symptoms of pancreatitis, gall bladder disease; worsening depression, suicidal thoughts and behaviour; body weight (for weight management).
Quá liều
Symptoms: Severe nausea, vomiting, and hypoglycaemia. Management: Symptomatic and supportive treatment. Monitor blood glucose level and signs of dehydration.
Tương tác
Increased risk of hypoglycaemia with insulin, sulfonylurea. May affect the absorption of concomitantly administered oral drugs due to slow gastric emptying. May enhance the adverse effect of other GLP-1 agonists.
Tác dụng
Description: Liraglutide is an acylated analogue of glucagon-like peptide 1 (GLP-1), an endogenous incretin hormone and acts as a GLP-1 receptor agonist. Activation of GLP-1 receptor stimulates insulin secretion and suppression of glucagon secretion in a glucose-dependent manner. It also delays gastric emptying thus reducing the rate of postprandial glucose present in the circulation. The exact mechanism of action in regulating the appetite and food intake is still unclear, however, it is believed to be via the specific activation of the GLP-1 receptor, which increases key satiety and decreases key hunger signals leading to a decrease in body weight.
Pharmacokinetics:
Absorption: Slowly absorbed after SC inj. Time to peak plasma concentration: 8-12 hours (SC). Bioavailability: Approx 55% (SC).
Distribution: Volume of distribution: Approx 13-25 L (SC); 0.07 L/kg (IV). Plasma protein binding: >98%.
Metabolism: Metabolised endogenously by dipeptidyl peptidase-4 (DPP-4) and endogenous endopeptidase enzymes.
Excretion: Via urine (6% as metabolites); faeces (5% as metabolites). Elimination half-life: Approx 13 hours.
Đặc tính

Chemical Structure Image
Liraglutide

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 16134956, Liraglutide. https://pubchem.ncbi.nlm.nih.gov/compound/Liraglutide. Accessed June 28, 2022.

Bảo quản
Prior to initial use, store between 2-8°C. After initial use, it can be stored between 15-30°C or 2-8°C for 30 days. Do not freeze or store directly adjacent to the refrigerator cooling element. Protect from heat and light.
Phân loại MIMS
Thuốc trị đái tháo đường / Thuốc chống béo phì
Phân loại ATC
A10BJ02 - liraglutide ; Belongs to the class of glucagon-like peptide-1 (GLP-1) analogues. Used in the treatment of diabetes.
Tài liệu tham khảo
Anon. Liraglutide. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 14/06/2022.

Anon. Liraglutide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 02/05/2022.

Buckingham R (ed). Liraglutide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/05/2022.

Joint Formulary Committee. Liraglutide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/05/2022.

Liraglutide. Drugs and Lactation Database (LactMed) [Internet]. Bethesda, MD. U.S. National Library of Medicine. https://www.ncbi.nlm.nih.gov/books/NBK501922. Accessed 14/06/2022.

Novo Nordisk Pharmaceuticals Ltd. Saxenda data sheet 27 April 2021. Medsafe. http://www.medsafe.govt.nz. Accessed 02/05/2022.

Saxenda 6 mg/mL Solution for Injection in Pre-filled Pen (Novo Nordisk A/S). MHRA. https://products.mhra.gov.uk. Accessed 02/05/2022.

Saxenda 6 mg/mL Solution for Injection in Pre-filled Pen (Novo Nordisk Pharma [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. tps://www.npra.gov.my. Accessed 02/05/2022.

Saxenda Injection, Solution (Novo Nordisk A/S). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/05/2022.

Victoza 6 mg/mL Solution for Injection in Pre-filled Pen (Novo Nordisk A/S). MHRA. https://products.mhra.gov.uk. Accessed 02/05/2022.

Victoza 6 mg/mL Solution for Injection in Pre-filled Pen (Novo Nordisk Pharma [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 02/05/2022.

Victoza Injection (Novo Nordisk A/S). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/05/2022.

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