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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for VICTOZA (VICTOZA).
| Breastfeeding | No human data on excretion into breast milk. Animal studies show presence in milk; M/P ratio not established. Risk to infant cannot be excluded; manufacturer advises against breastfeeding while using VICTOZA. |
| 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. |
■ 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 |
["Personal or family history of medullary thyroid carcinoma","Multiple Endocrine Neoplasia syndrome type 2","Hypersensitivity to liraglutide or any product component"]
| 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"] |
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| 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. |