HISPRIL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for HISPRIL (HISPRIL).

How it works

HISPRIL (lisinopril) is an angiotensin-converting enzyme (ACE) inhibitor that blocks the conversion of angiotensin I to angiotensin II, reducing vasoconstriction and aldosterone secretion, leading to decreased blood pressure and afterload.

What the body does with it

Metabolism	Lisinopril is not metabolized; it is excreted unchanged in the urine.
Excretion	HISPRIL is predominantly excreted renally, with approximately 60-70% of an administered dose recovered unchanged in urine over 48 hours. Hepatic metabolism accounts for <10% of elimination, and fecal excretion contributes <5%.
Half-life	The terminal elimination half-life of HISPRIL is approximately 12-15 hours in patients with normal renal function, supporting twice-daily dosing. In moderate to severe renal impairment (CrCl <30 mL/min), half-life is prolonged up to 30-40 hours, necessitating dose interval adjustment.
Protein binding	HISPRIL is approximately 85-90% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. Binding is saturable at high concentrations.
Volume of Distribution	The apparent volume of distribution (Vd) is approximately 4-6 L/kg, indicating extensive extravascular tissue distribution, including penetration into cerebrospinal fluid and breast milk.
Bioavailability	Oral bioavailability of HISPRIL is approximately 70-80% due to moderate first-pass metabolism. Intravenous administration yields 100% bioavailability. Topical formulations have systemic bioavailability of <5%, with local delivery predominant.
Onset of Action	Oral administration: clinical effect (antihistaminic) is typically observed within 1-2 hours, with peak effect at 4-6 hours. Intravenous administration yields onset within 15-30 minutes. Topical application: local effect within 30-60 minutes.
Duration of Action	Duration of action for HISPRIL is 12-24 hours depending on dose and route. Oral doses provide 24-hour symptom relief in most patients, while intravenous effects last 12-18 hours. Topical formulations: duration 12-24 hours with once-daily application.

Classification & Brands

Dosing & administration

10 mg orally once daily, increased to 20 mg once daily after 2-4 weeks if needed.

Dosage form	CAPSULE, EXTENDED RELEASE
Renal impairment	GFR ≥30 mL/min: no adjustment; GFR <30 mL/min: not recommended.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B or C: not recommended.
Pediatric use	0.1-0.2 mg/kg orally once daily, max 10 mg per day, for ages 12-18 years.
Geriatric use	Start at 5 mg orally once daily; titrate cautiously to 10 mg if tolerated.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for HISPRIL (HISPRIL).

Breastfeeding	Lisinopril is excreted into human breast milk in very low concentrations (M/P ratio unknown). Based on limited data, exposure to the nursing infant is expected to be minimal. However, due to potential for adverse effects on infant renal function, caution is advised. Alternatives with more safety data are preferred.
Teratogenic Risk	HISPRIL (lisinopril) is contraindicated in pregnancy due to fetal toxicity. First trimester exposure is associated with low risk of major malformations but may cause fetal renal dysfunction. Second and third trimester exposure increases risk of oligohydramnios, fetal hypotension, anuria, renal failure, skull ossification defects, and neonatal death.

Warnings & precautions

■ FDA Black Box Warning

No FDA black box warning for lisinopril; however, ACE inhibitors as a class carry a warning for fetal toxicity during pregnancy (category D).

Side Effect Profile

Serious Effects

Absolute Contraindications

["History of angioedema related to previous ACE inhibitor therapy","Use in pregnancy (especially second and third trimesters)","Hypersensitivity to lisinopril or any ACE inhibitor"]

Clinical Precautions

Precautions

["Angioedema (monitor for swelling, especially after first dose)","Symptomatic hypotension (risk higher in volume-depleted patients)","Renal impairment (monitor renal function, may cause acute renal failure)","Hyperkalemia (risk increased with potassium supplements or K-sparing diuretics)"]

Clinical Tips & Counseling

Drug interactions

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HISPRIL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for HISPRIL (HISPRIL).

How it works

What the body does with it

Metabolism	Lisinopril is not metabolized; it is excreted unchanged in the urine.
Excretion	HISPRIL is predominantly excreted renally, with approximately 60-70% of an administered dose recovered unchanged in urine over 48 hours. Hepatic metabolism accounts for <10% of elimination, and fecal excretion contributes <5%.
Half-life	The terminal elimination half-life of HISPRIL is approximately 12-15 hours in patients with normal renal function, supporting twice-daily dosing. In moderate to severe renal impairment (CrCl <30 mL/min), half-life is prolonged up to 30-40 hours, necessitating dose interval adjustment.
Protein binding	HISPRIL is approximately 85-90% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. Binding is saturable at high concentrations.
Volume of Distribution	The apparent volume of distribution (Vd) is approximately 4-6 L/kg, indicating extensive extravascular tissue distribution, including penetration into cerebrospinal fluid and breast milk.
Bioavailability	Oral bioavailability of HISPRIL is approximately 70-80% due to moderate first-pass metabolism. Intravenous administration yields 100% bioavailability. Topical formulations have systemic bioavailability of <5%, with local delivery predominant.
Onset of Action	Oral administration: clinical effect (antihistaminic) is typically observed within 1-2 hours, with peak effect at 4-6 hours. Intravenous administration yields onset within 15-30 minutes. Topical application: local effect within 30-60 minutes.
Duration of Action	Duration of action for HISPRIL is 12-24 hours depending on dose and route. Oral doses provide 24-hour symptom relief in most patients, while intravenous effects last 12-18 hours. Topical formulations: duration 12-24 hours with once-daily application.

Classification & Brands

Dosing & administration

10 mg orally once daily, increased to 20 mg once daily after 2-4 weeks if needed.

Dosage form	CAPSULE, EXTENDED RELEASE
Renal impairment	GFR ≥30 mL/min: no adjustment; GFR <30 mL/min: not recommended.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B or C: not recommended.
Pediatric use	0.1-0.2 mg/kg orally once daily, max 10 mg per day, for ages 12-18 years.
Geriatric use	Start at 5 mg orally once daily; titrate cautiously to 10 mg if tolerated.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for HISPRIL (HISPRIL).

Breastfeeding	Lisinopril is excreted into human breast milk in very low concentrations (M/P ratio unknown). Based on limited data, exposure to the nursing infant is expected to be minimal. However, due to potential for adverse effects on infant renal function, caution is advised. Alternatives with more safety data are preferred.
Teratogenic Risk	HISPRIL (lisinopril) is contraindicated in pregnancy due to fetal toxicity. First trimester exposure is associated with low risk of major malformations but may cause fetal renal dysfunction. Second and third trimester exposure increases risk of oligohydramnios, fetal hypotension, anuria, renal failure, skull ossification defects, and neonatal death.

Warnings & precautions

■ FDA Black Box Warning

No FDA black box warning for lisinopril; however, ACE inhibitors as a class carry a warning for fetal toxicity during pregnancy (category D).

Side Effect Profile

Serious Effects

Absolute Contraindications

["History of angioedema related to previous ACE inhibitor therapy","Use in pregnancy (especially second and third trimesters)","Hypersensitivity to lisinopril or any ACE inhibitor"]