TEGOPEN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TEGOPEN (TEGOPEN).
TEGOPEN is a prodrug that is converted to the active metabolite, which acts as a potent and selective inhibitor of dipeptidyl peptidase-4 (DPP-4), thereby increasing incretin levels (GLP-1 and GIP), enhancing glucose-dependent insulin secretion, and suppressing glucagon release.
| Metabolism | TEGOPEN is extensively metabolized via hydrolysis, glucuronidation, and oxidation; the major cytochrome P450 enzymes involved are CYP3A4 and CYP2C8. |
| Excretion | Primarily renal (70-80% unchanged) via glomerular filtration and tubular secretion; minor biliary/fecal (10-15%). |
| Half-life | Terminal half-life 0.8-1.2 hours in normal renal function; prolonged to 7-10 hours in severe renal impairment (CrCl <10 mL/min). |
| Protein binding | 20-30% bound to serum albumin. |
| Volume of Distribution | 0.3-0.4 L/kg, reflecting distribution into extracellular fluid. |
| Bioavailability | Oral: 30-50% (variable, food reduces absorption); IM: 60-80%. |
| Onset of Action | IV: Immediate; IM: 15-30 minutes; Oral: 30-60 minutes. |
| Duration of Action | 4-6 hours for susceptible organisms; requires frequent dosing due to short half-life. |
50-100 mg/kg/day IV divided every 6-8 hours; maximum 4 g/day for adults.
| Dosage form | FOR SOLUTION |
| Renal impairment | GFR 10-50 mL/min: 50% of normal dose every 12 hours; GFR <10 mL/min: 25% of normal dose every 24 hours. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: contraindicated or reduce dose by 75% with monitoring. |
| Pediatric use | Infants >1 month and children: 50-100 mg/kg/day IV divided every 6-8 hours; neonates: 30-50 mg/kg/day IV divided every 12 hours. |
| Geriatric use | Use with caution; initiate at low end of dosing range; monitor renal function and adjust dose based on creatinine clearance. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TEGOPEN (TEGOPEN).
| Breastfeeding | Excreted in human milk in low concentrations; M/P ratio unknown. Use with caution; consider risk of infant gastrointestinal adverse effects. |
| Teratogenic Risk | First trimester: No adequate human data; animal studies show no teratogenicity at therapeutic doses. Second/third trimester: Potential risk of premature closure of ductus arteriosus and oligohydramnios; avoid after 32 weeks gestation. |
| Fetal Monitoring |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["History of a serious hypersensitivity reaction to TEGOPEN or any of its excipients","Type 1 diabetes mellitus","Diabetic ketoacidosis"]
| Precautions | ["Pancreatitis (discontinue if suspected)","Heart failure (consider risk in patients with known cardiovascular disease)","Severe and disabling arthralgia","Bullous pemphigoid","Hypoglycemia when used with sulfonylureas or insulin"] |
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| Monitor maternal renal function, hepatic function, and complete blood count. Fetal ultrasound for amniotic fluid index and ductus arteriosus patency if used in third trimester. |
| Fertility Effects | No known impairment of fertility in animal studies; human data insufficient. |