TECZEM
Clinical safety rating
cautionComprehensive clinical and safety monograph for TECZEM (TECZEM).
Enalapril inhibits angiotensin-converting enzyme (ACE), reducing angiotensin II formation, leading to vasodilation and decreased aldosterone secretion. Diltiazem inhibits calcium ion influx across cardiac and smooth muscle cells, causing coronary vasodilation and decreased myocardial contractility.
| Metabolism | Enalapril is hydrolyzed to active enalaprilat, mainly hepatically. Diltiazem is extensively metabolized in the liver via CYP3A4. |
| Excretion | Renal: 40-50% unchanged; hepatic/biliary/fecal: 50-60% as metabolites. |
| Half-life | Terminal elimination half-life: 3-4 hours for diltiazem; clinical context: requires twice-daily dosing due to short half-life. |
| Protein binding | 70-80% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 5-7 L/kg; indicates extensive tissue distribution. |
| Bioavailability | Oral: 35-60% due to first-pass metabolism; IV: 100%. |
| Onset of Action | Oral: 30-60 minutes; IV: 2-5 minutes. |
| Duration of Action | Oral: 6-8 hours; IV: 1-3 hours; clinical notes: extended-release formulations provide 12-24 hour coverage. |
| Molecular Weight | Diltiazem: 414.5 Da; Enalapril: 376.45 Da |
1 to 2 tablets (enalapril 5 mg/diltiazem 180 mg) orally once daily. Maximum: 2 tablets daily.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | GFR >30 mL/min: No adjustment. GFR 10-30 mL/min: Use with caution, monitor potassium and creatinine. GFR <10 mL/min: Avoid use. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Use with caution, consider starting at lowest dose. Child-Pugh C: Contraindicated. |
| Pediatric use | Safety and efficacy not established for patients <18 years. |
| Geriatric use | Start at lowest dose, monitor renal function and electrolytes due to age-related decreased renal function and increased sensitivity. |
| 1st trimester | Avoid due to potential teratogenicity; diltiazem and enalapril associated with fetal harm in animal studies and limited human data. |
| 2nd trimester | Use only if benefit outweighs risk; enalapril can cause fetal renal dysfunction and oligohydramnios in second trimester. |
| 3rd trimester | Contraindicated; enalapril exposure in third trimester is associated with neonatal hypotension, renal failure, and skull hypoplasia. |
Clinical note
Comprehensive clinical and safety monograph for TECZEM (TECZEM).
| Placental transfer | Both diltiazem and enalapril/enalaprilat cross the placenta; enalaprilat demonstrates significant fetal exposure with evidence of adverse fetal effects. |
| Breastfeeding | Diltiazem and enalapril are excreted into breast milk in low amounts; diltiazem may accumulate in breastfed infants due to immature metabolism; monitor infant for hypotension and bradycardia. Enalapril's active metabolite enalaprilat is excreted in negligible amounts. Use with caution, especially in preterm or jaundiced infants. |
| Lactation Rating | L4 (Possibly Hazardous) - limited data suggest potential risk to infant |
| Teratogenic Risk | TECZEM (enalapril maleate and felodipine) is contraindicated in pregnancy. ACE inhibitors can cause fetal and neonatal morbidity and death when administered to pregnant women. First trimester exposure may be associated with a small increased risk of congenital anomalies; second and third trimester exposure is associated with oligohydramnios, fetal renal dysfunction, skull ossification defects, and neonatal hypotension, anuria, and renal failure. Felodipine: No teratogenic effects in animal studies at clinically relevant doses; however, limited human data. Combined use should be avoided in pregnancy. |
| Fetal Monitoring | Monitor maternal blood pressure, renal function (serum creatinine, BUN), and serum electrolytes regularly. Assess fetal well-being with ultrasound if pregnancy is suspected. In case of inadvertent exposure, perform fetal ultrasound to assess amniotic fluid volume and renal function. |
| Fertility Effects | Enalapril: No significant effects on fertility in animal studies. Felodipine: No impairment of fertility in rats at clinically relevant doses. No human data on fertility effects; however, calcium channel blockers may affect sperm function theoretically. |
■ FDA Black Box Warning
Use in pregnancy: ACE inhibitors can cause injury and death to the developing fetus. Discontinue as soon as possible when pregnancy is detected.
| Serious Effects |
Pregnancy (especially second and third trimesters)History of angioedema related to ACE inhibitorsConcurrent use with neprilysin inhibitors (e.g., sacubitril) within 36 hoursSevere hypotension (systolic BP <90 mmHg)Advanced atrioventricular block (2nd or 3rd degree) without pacemakerSick sinus syndrome without pacemakerSevere left ventricular dysfunction (LVEF <40%)Hypersensitivity to diltiazem, enalapril, or any component of the formulation
| Precautions | Hypotension, Angioedema, Hepatic injury, Heart block, Bradycardia, Renal impairment, Hyperkalemia |
| Food/Dietary | Avoid high-potassium foods (e.g., bananas, oranges, spinach) due to potential for hyperkalemia from enalapril. Grapefruit juice may increase diltiazem levels and should be limited or avoided. Alcohol can exacerbate hypotension. |
| Clinical Pearls | TECZEM (enalapril/diltiazem ER) combines an ACE inhibitor and a non-dihydropyridine calcium channel blocker. Monitor renal function and serum potassium; avoid in patients with pre-existing high-grade AV block or severe left ventricular dysfunction. Use with caution in patients with hepatic impairment due to diltiazem metabolism. May cause reflex tachycardia less frequently than dihydropyridines. |
| Patient Advice | Take this medication exactly as prescribed; do not crush or chew the extended-release tablet. · Monitor blood pressure regularly and report symptoms such as dizziness, fainting, or irregular heartbeat. · Avoid salt substitutes containing potassium unless directed by your doctor. · Report any signs of angioedema (swelling of face, lips, tongue, or difficulty breathing) immediately. |
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