DEAPRIL-ST
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DEAPRIL-ST (DEAPRIL-ST).
Angiotensin-converting enzyme (ACE) inhibitor. Inhibits ACE, preventing conversion of angiotensin I to angiotensin II, reducing vasoconstriction and aldosterone secretion, leading to decreased blood pressure.
| Metabolism | Hepatic via glucuronidation; active metabolite perindoprilat formed by ester hydrolysis. |
| Excretion | Renal (90% as unchanged drug), biliary/fecal (10%) |
| Half-life | 8-10 hours; prolonged in renal impairment (up to 24 hours in severe cases) |
| Protein binding | 25-30% (primarily to albumin) |
| Volume of Distribution | 0.8-1.2 L/kg; indicates extensive tissue distribution |
| Bioavailability | Oral: 60-70% (with food reducing absorption rate but not extent) |
| Onset of Action | Oral: 1-2 hours; IV: 15-30 minutes |
| Duration of Action | Oral: 12-24 hours; IV: 12-24 hours; duration may extend in renal impairment |
| Molecular Weight | 369.5 |
Oral: 2.5 mg twice daily, titrated up to 5 mg twice daily as tolerated. Maximum dose: 10 mg daily.
| Dosage form | TABLET |
| Renal impairment | GFR 30-60 mL/min: 2.5 mg once daily; GFR <30 mL/min: 2.5 mg every other day; GFR <15 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 2.5 mg once daily; Child-Pugh C: not recommended. |
| Pediatric use | Weight <30 kg: 0.05 mg/kg/dose twice daily; ≥30 kg: adult dosing. Maximum: 0.1 mg/kg/day. |
| Geriatric use | Initiate at 2.5 mg once daily; titrate cautiously. Monitor renal function and electrolytes. |
| 1st trimester | Contraindicated: risk of fetal renal impairment and oligohydramnios, increased risk of congenital malformations (neural tube, cardiac, renal defects). |
| 2nd trimester | Contraindicated: fetal oligohydramnios, skull ossification defects, pulmonary hypoplasia, and neonatal anuria. |
| 3rd trimester | Contraindicated: severe neonatal hypotension, renal failure, hyperkalemia, and anuria. |
Clinical note
Comprehensive clinical and safety monograph for DEAPRIL-ST (DEAPRIL-ST).
| Placental transfer | Crosses placenta: extensively transferred to fetal circulation (approximately 50-60% of maternal concentration). |
| Breastfeeding | Minimal excretion into breast milk; however, potential for adverse effects on infant renal function and blood pressure. Use only if clearly necessary, and monitor infant for hypotension, oliguria, and hyperkalemia. |
■ FDA Black Box Warning
Fetal toxicity: Drugs acting directly on the renin-angiotensin system can cause injury and death to the developing fetus. Discontinue as soon as possible when pregnancy is detected.
| Serious Effects |
History of angioedema with ACE inhibitorsPregnancy (especially 2nd and 3rd trimesters)Bilateral renal artery stenosisSevere renal impairment (GFR < 30 mL/min)Hyperkalemia refractory to treatmentConcomitant use with aliskiren in diabetic patients
| Precautions | Angioedema, hypotension, hyperkalemia, renal impairment, cough, hepatotoxicity, neutropenia/agranulocytosis, anaphylactoid reactions during desensitization or LDL apheresis. |
| Food/Dietary | Avoid high-potassium foods (bananas, oranges, tomatoes, potatoes with skin, spinach, avocados) unless potassium levels are monitored. Avoid salt substitutes containing potassium chloride. Reduce alcohol intake to minimize hypotension risk. Maintain adequate fluid intake to prevent dehydration. |
Loading safety data…
| Lactation Rating | L3 (Moderately Safe) - limited data, caution advised. |
| Teratogenic Risk | First trimester: Risk of congenital malformations, particularly cardiovascular and central nervous system defects, based on ACE inhibitor class effects. Second and third trimesters: Fetal renal dysfunction, oligohydramnios, pulmonary hypoplasia, skeletal deformities, and neonatal hypotension, hyperkalemia, and acute renal failure. |
| Fetal Monitoring | Monitor maternal blood pressure, renal function (serum creatinine, BUN), and serum potassium regularly. Fetal ultrasound for amniotic fluid volume and fetal growth. Neonatal monitoring for hypotension, hyperkalemia, and renal function after delivery. |
| Fertility Effects | No significant effect on fertility reported in animal studies; however, ACE inhibitors may be associated with decreased sperm motility in some studies. Human data limited. |
| Clinical Pearls | DEAPRIL-ST is a fixed-dose combination of perindopril (ACE inhibitor) and indapamide (thiazide-like diuretic). Monitor serum creatinine and potassium within 2 weeks of initiation due to risk of hyperkalemia and renal impairment. Avoid in pregnancy (category D). Use with caution in renal artery stenosis. First-dose hypotension may occur; start at bedtime if tolerated. |
| Patient Advice | Take once daily in the morning, preferably before breakfast, to avoid nocturia. · Report signs of angioedema (swelling of face, lips, tongue, or difficulty breathing) immediately. · Do not use potassium supplements or salt substitutes containing potassium without consulting your doctor. · May cause dizziness or lightheadedness, especially after the first dose; avoid driving if affected. · Stay well hydrated to prevent dehydration from the diuretic effect. |