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Liraglutide

Specification: 10mg/vial; 15mg/vial; 20mg/vial

 

Pharmacological category: GLP-1 receptor agonist, Antidiabetic agent, Anti-obesity drug, Cardiovascular protective agent

Product Description

Mechanism of action: 97% homology with endogenous human GLP-1, exerts glucose-dependent hypoglycemic & weight-loss effects by stimulating insulin secretion, inhibiting glucagon release, slowing gastric emptying and enhancing central satiety (no hypoglycemia risk as monotherapy). Improves insulin sensitivity, protects pancreatic β-cells, reduces visceral fat, lowers blood lipid/blood pressure, and significantly reduces major adverse cardiovascular events (MACE). Long half-life (≈13h), once-daily subcutaneous injection after reconstitution, ultra-high stability in lyophilized form, easy storage and transportation.

 

Indications:

1. Adult type 2 diabetes mellitus (T2DM): Monotherapy or combined with metformin/sulfonylurea/insulin for glycemic control, suitable for oral medication intolerant patients.

2. Chronic weight management: Adults with obesity (BMI≥30kg/m²) or overweight (BMI≥27kg/m²) complicated with hypertension, dyslipidemia, T2DM, fatty liver.

3. Cardiovascular risk reduction: Secondary prevention of myocardial infarction, stroke and cardiovascular death in T2DM patients with cardiovascular disease or high-risk factors.

4. Adjuvant treatment for polycystic ovary syndrome (PCOS) with insulin resistance & obesity.

 

Usage and dosage: Subcutaneous injection only (abdomen/thigh/upper arm) after reconstitution with sterile water for injection, once daily at any time, no food restriction.

1. Antidiabetic dosage: Initial 0.6mg qd for 1 week (titration to reduce GI reactions) → maintenance 1.2mg qd; max 1.8mg qd if needed.

2. Anti-obesity dosage: 0.6mg→1.2mg→1.8mg→2.4mg qd (increase every 7 days) → maintenance 2.4mg qd (max effective dose).

3. Special population: Elderly/renal insufficiency patients start with 0.6mg qd, titrate slowly; avoid use in severe hepatic/end-stage renal disease.

4. Key note: Rotate injection sites, prohibit IV/IM injection, use immediately after reconstitution, no residual storage.

 

Contraindications:

1. Hypersensitivity to liraglutide, any excipients or GLP-1 analogs.

2. History of medullary thyroid carcinoma (MTC) or multiple endocrine neoplasia syndrome type 2 (MEN 2).

3. Type 1 diabetes mellitus, diabetic ketoacidosis (DKA).

4. Severe acute pancreatitis, severe gastrointestinal obstruction.

 

Cautious population:

1. Mild-moderate gastrointestinal diseases (may aggravate nausea/vomiting/diarrhea).

2. Renal insufficiency (adjust dose in stage 3-4 CKD, avoid ESRD); mild-moderate hepatic insufficiency (use cautiously, avoid severe liver disease).

3. Pregnant/lactating women (discontinue use, insufficient safety data); women of childbearing age (adopt contraception during treatment).

4. History of pancreatitis/gallbladder disease (monitor abdominal pain and gallstone formation).

5. Elderly (≥65y) and frail patients (closely monitor blood glucose, weight and adverse reactions).

6. Avoid combined use with other GLP-1 agonists; reduce sulfonylurea/insulin dose to prevent hypoglycemia.

 

Adverse reactions: Mild-moderate, transient, relieved with continuous use/dosage titration, excellent tolerance

1. Common (≥5%): Gastrointestinal reactions (nausea, vomiting, diarrhea, abdominal pain, anorexia), injection site reactions (erythema, swelling, pain, pruritus), headache, fatigue, mild hypoglycemia (only combined with hypoglycemic drugs), weight loss.

2. Rare (1%-5%): Constipation, flatulence, dizziness, insomnia, mild transaminase elevation, gallbladder polyps/cholelithiasis, TSH elevation, rash/urticaria.

3. Severe (<1%): Acute pancreatitis, severe hypoglycemic coma, anaphylactic shock, medullary thyroid nodules, acute kidney injury (secondary to severe vomiting/diarrhea); no severe hepatotoxicity/nephrotoxicity with conventional dosage.

 

Notes:

1. Reconstitution: Dissolve strictly with sterile water for injection, shake gently to clear solution, use immediately (invalid if placed for >30mins).

2. Safety warning: Stop medication and seek emergency care for persistent severe abdominal pain (with/without vomiting) (suspected acute pancreatitis).

3. Regular monitoring: Blood glucose, HbA1c, body weight, blood lipid, thyroid function (TSH/ultrasound) during long-term use.

4. Storage: 2-8℃ refrigerated, sealed, protected from light for whole shelf life; avoid freezing, high temperature, direct sunlight; no need for cold chain transportation after sealed packaging; validity period: 36 months (unopened vial).

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