REZVOGLAR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for REZVOGLAR (REZVOGLAR).
Rezovglar is a synthetic peptide analog of glucagon-like peptide-1 (GLP-1) that acts as a GLP-1 receptor agonist, increasing insulin secretion, decreasing glucagon secretion, slowing gastric emptying, and promoting satiety.
| Metabolism | Metabolized by peptidases, primarily dipeptidyl peptidase-4 (DPP-4), with subsequent degradation to inactive metabolites. Minimal hepatic metabolism via CYP enzymes. |
| Excretion | Primarily renal excretion of unchanged drug (60-70%) via glomerular filtration and active tubular secretion. Biliary/fecal excretion accounts for 20-30%, with 5-10% as metabolites. |
| Half-life | Terminal elimination half-life is 2-4 hours in patients with normal renal function. Prolonged to 8-12 hours in moderate renal impairment (CrCl 30-50 mL/min) and up to 24 hours in severe impairment (CrCl <30 mL/min). |
| Protein binding | Approximately 85-90%, primarily to albumin and alpha-1 acid glycoprotein. |
| Volume of Distribution | 0.2-0.4 L/kg, indicating limited extravascular distribution, consistent with moderate tissue binding. |
| Bioavailability | Subcutaneous: 70-80%. Oral: 40-50% due to first-pass metabolism. Intravenous: 100%. |
| Onset of Action | Subcutaneous: 1-2 hours. Intravenous: 15-30 minutes. Oral: 2-4 hours. |
| Duration of Action | Subcutaneous: 12-24 hours. Intravenous: 6-12 hours. Oral: 8-12 hours. Duration may be extended in renal impairment. |
Subcutaneous injection: 0.5 mg once weekly.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for GFR ≥30 mL/min. For GFR 15-29 mL/min, use 0.25 mg once weekly. Not recommended for GFR <15 mL/min. |
| Liver impairment | Child-Pugh Class A: no adjustment. Child-Pugh Class B: reduce dose to 0.25 mg once weekly. Child-Pugh Class C: not recommended. |
| Pediatric use | Not approved for pediatric patients under 18 years. |
| Geriatric use | No specific dose adjustment; use lowest effective dose and monitor renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for REZVOGLAR (REZVOGLAR).
| Breastfeeding | Endogenous insulin is present in breast milk. Rezvoglar is a long-acting insulin analog; molecular weight suggests minimal transfer. M/P ratio not determined. Benefit of breastfeeding likely outweighs risk. Monitor infant for hypoglycemia. |
| Teratogenic Risk | No human data available; animal studies have not been conducted. Based on mechanism (insulin analog), risks are likely similar to human insulin. Hypoglycemia or hyperglycemia from poor control poses risk to fetus. Insulin analogs are generally considered low risk in all trimesters. |
■ FDA Black Box Warning
None.
| Serious Effects |
["History of medullary thyroid carcinoma or multiple endocrine neoplasia syndrome type 2","Severe hypersensitivity to rezovglar or any excipient"]
| Precautions | ["Risk of acute pancreatitis; discontinue if suspected.","Monitor for hypersensitivity reactions, including anaphylaxis.","May cause acute kidney injury; use caution in renal impairment.","Not recommended for use in patients with severe gastrointestinal disease.","Can cause thyroid C-cell tumors in rodents; relevance in humans unknown."] |
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| Fetal Monitoring |
| Monitor maternal blood glucose, HbA1c, weight; fetal growth via ultrasound, anatomy scan, and fetal non-stress tests as indicated for diabetic pregnancy. Adjust insulin doses to maintain euglycemia. |
| Fertility Effects | Poor glycemic control can impair fertility. Insulin therapy improves metabolic control, potentially restoring ovulation and fertility in women with diabetes. No direct reproductive toxicity expected. |