VICTOZA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VICTOZA (VICTOZA).
Glucagon-like peptide-1 (GLP-1) receptor agonist; increases insulin secretion, decreases glucagon secretion, slows gastric emptying, and promotes satiety.
| Metabolism | Metabolized via endogenous proteolysis and dipeptidyl peptidase-4 (DPP-4) mediated degradation; no specific CYP enzyme involvement. |
| Excretion | Liraglutide is eliminated via degradation by general proteolysis and not by specific enzymes; the intact drug is not excreted in urine or feces. Degraded metabolites are excreted via urine and feces. |
| Half-life | After subcutaneous administration, the terminal elimination half-life is approximately 13 hours, supporting once-daily dosing. |
| Protein binding | Liraglutide is highly protein bound (>98%), primarily to albumin. |
| Volume of Distribution | The volume of distribution after subcutaneous administration is approximately 11-17 L (or 0.15-0.25 L/kg), indicating limited tissue distribution consistent with a large peptide. |
| Bioavailability | Subcutaneous: The absolute bioavailability is approximately 55% for the approved injection sites (abdomen, thigh, upper arm). |
| Onset of Action | Subcutaneous: The onset of action is observed within 1-2 hours of the first dose, with maximum glucose-lowering effect seen after 3-4 days of once-daily dosing. |
| Duration of Action | Subcutaneous: The glucose-lowering effect persists for approximately 24 hours, allowing once-daily administration. The effect is dose-dependent and steady-state is achieved after 1-2 weeks. |
| Molecular Weight | 3751.2 |
| Action Class | GLP-1 Receptor Agonist |
Subcutaneous injection: 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 if needed for glycemic control.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). Limited data in severe renal impairment (CrCl <30 mL/min); use with caution; not recommended in end-stage renal disease. |
| Liver impairment | No dose adjustment required for mild hepatic impairment (Child-Pugh A). Limited data in moderate (Child-Pugh B) or severe (Child-Pugh C) impairment; use with caution. |
| Pediatric use | Not indicated for pediatric patients <18 years of age. Safety and efficacy not established. |
| Geriatric use | No dose adjustment required. Limited experience in patients ≥75 years; consider renal function and potential for increased risk of adverse effects due to age-related decline in renal function. |
| 1st trimester | Insufficient human data; animal studies show reproductive toxicity. Avoid use unless no safe alternative. |
| 2nd trimester | Insufficient human data; avoid use due to potential fetal risk. |
| 3rd trimester | Avoid use; potential for fetal harm and neonatal hypoglycemia. |
Clinical note
Comprehensive clinical and safety monograph for VICTOZA (VICTOZA).
| Placental transfer | Liraglutide crosses the placenta in animal studies; human data are limited but suggest transfer. |
| Breastfeeding | Liraglutide is excreted in breast milk in animal studies; no human data. Potential adverse effects on infant gastrointestinal motility and risk of hypoglycemia. Not recommended during breastfeeding. |
| Lactation Rating |
■ FDA Black Box Warning
Risk of thyroid C-cell tumors. Liraglutide causes dose-dependent and treatment-duration-dependent thyroid C-cell tumors at clinically relevant exposures in rats. It is contraindicated in patients with a personal or family history of medullary thyroid carcinoma or in patients with Multiple Endocrine Neoplasia syndrome type 2.
| Common Effects | Constipation Decreased appetite Diarrhea Nausea Vomiting Abdominal pain Dyspepsia Flatulence Nasopharyngitis inflammation of the throat and nasal passages |
| Serious Effects | Pancreatitis, Acute kidney injury, Gallbladder disease (cholelithiasis, cholecystitis), Thyroid C-cell tumors (medullary thyroid carcinoma), Hypoglycemia (when used with insulin or sulfonylureas), Increased heart rate, Suicidal behavior or ideation |
Personal or family history of medullary thyroid carcinoma (MTC)Multiple endocrine neoplasia syndrome type 2 (MEN 2)Severe gastrointestinal disease (e.g., gastroparesis)Hypersensitivity to liraglutide or any excipientsPregnancy (category X)
| Precautions | Risk of acute pancreatitis, including fatal and non-fatal hemorrhagic or necrotizing pancreatitis, Hypoglycemia risk when used with insulin or sulfonylureas, Renal impairment including acute renal failure and worsening of chronic renal failure, Severe gastrointestinal adverse reactions, Diabetic retinopathy complications, Pregnancy and lactation considerations |
Loading safety data…
| L5 (Contraindicated) |
| Teratogenic Risk | Pregnancy Category X. Based on animal studies and human postmarketing data, liraglutide is associated with fetal harm. First trimester exposure carries risk of major congenital malformations; second and third trimester exposure may cause fetal growth abnormalities and neonatal complications including hypoglycemia. |
| Fetal Monitoring | Monitor maternal blood glucose and HbA1c. Fetal monitoring includes ultrasound for growth and anatomy (structural evaluation if exposed), and neonatal surveillance for hypoglycemia after delivery. |
| Fertility Effects | In animal studies, liraglutide caused prolonged estrous cycles and reduced fertility at high doses. Human data limited; potential for menstrual irregularities due to weight loss or direct gonadal effects. Use with caution in women planning pregnancy. |
| Food/Dietary | Take VICTOZA with or without food. No significant food interactions. However, liraglutide slows gastric emptying, which may affect absorption of oral medications, especially those requiring rapid onset. Monitor oral medications with narrow therapeutic index. Alcohol may increase risk of hypoglycemia or pancreatitis; advise moderation. |
| Clinical Pearls | VICTOZA (liraglutide) is a GLP-1 receptor agonist for type 2 diabetes. It reduces HbA1c and weight. Start at 0.6 mg daily for 1 week to minimize GI side effects, then increase to 1.2 mg; may titrate to 1.8 mg if needed. It has a boxed warning for thyroid C-cell tumors; contraindicated in patients with personal or family history of medullary thyroid carcinoma or MEN-2. Monitor for acute pancreatitis (discontinue if suspected). Renal impairment may occur with dehydration. Use with caution in combination with insulin or sulfonylureas due to hypoglycemia risk. |
| Patient Advice | Inject once daily at any time of day, with or without meals, at the same time each day. · Use the pen for up to 30 days after first use, then discard even if some medicine remains. · Store unused pens in refrigerator (36°F to 46°F); after first use, can be stored at room temperature (59°F to 86°F) for up to 30 days. · Missed dose: take within 12 hours of scheduled time; if >12 hours, skip that dose and take next day's dose as usual. · Common side effects include nausea, vomiting, diarrhea, and constipation; these often improve over time. · Seek medical attention for symptoms of pancreatitis: severe abdominal pain with or without vomiting. · Do not stop or change dose without consulting your doctor. · Report symptoms of thyroid tumors: lump in neck, hoarseness, trouble swallowing. · Have glucagon available if taking insulin or sulfonylureas for severe hypoglycemia. · Do not share pen even if needle is changed. |