Lisinopril

Pronunciation

Pronunciation: lye-SIN-oh-pril
Class: ACE inhibitor

Trade Names

Prinivil
- Tablets 10 mg
- Tablets 20 mg

Zestril
- Tablets 2.5 mg
- Tablets 5 mg
- Tablets 10 mg
- Tablets 20 mg
- Tablets 30 mg
- Tablets 40 mg

Apo-Lisinopril (Canada)

Pharmacology

Competitively inhibits angiotensin-converting enzyme; prevents angiotensin I conversion to angiotensin II, a potent vasoconstrictor that also stimulates aldosterone secretion. Results in decrease in sodium and fluid retention, decrease in BP, and increase in diuresis.

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Pharmacokinetics

Absorption

T max is about 7 h.

Distribution

Does not appear to be bound to other serum proteins.

Metabolism

Does not undergo metabolism.

Elimination

The t ½ is 12 h. Excreted via the kidney; excreted unchanged entirely in the urine. Lisinopril can be removed by hemodialysis.

Onset

1 h.

Peak

6 h.

Duration

24 h.

Special Populations

Renal Function Impairment

Decreased elimination when glomerular filtration rate is 30 mL/min or less.

Race

Black patients with hypertension had a smaller response to monotherapy of ACE inhibitor.

CHF (New York Heart Association class II through IV)

Bioavailability decreases about 16% and Vd is slightly smaller.

Indications and Usage

Treatment of hypertension; treatment of heart failure not responding to diuretics and digitalis; treatment of acute MI within 24 h in hemodynamically stable patients.

Unlabeled Uses

Migraine prophylaxis.

Contraindications

Hypersensitivity to ACE inhibitors; hereditary or idiopathic angioedema.

Dosage and Administration

CHF
Adults Initial dose

PO 5 mg every day with diuretics and digitalis; reduce concomitant diuretic dose, if possible, to minimize hypovolemia.

Dose adjustment for hyponatremia (serum sodium less than 130 mEq/L) or moderate to severe renal function impairment (CrCl 30 mL/min or less or serum creatinine greater than 3 mg/dL)

PO Start with 2.5 mg once daily.

Usual dose

PO 5 to 40 mg once daily.

Hypertension
Adults

PO

Initial dose

10 mg once daily. If a diuretic is coadministered, start with lisinopril 5 mg (under medical supervision) for at least 2 h and until BP has stabilized for at least 1 additional h.

Maintenance

20 to 40 mg/day; may add diuretic if needed and decrease lisinopril dose.

Renal function impairment Moderate to severe function impairment (CrCl 10 mL/min or more to 30 mL/min or less)

5 mg/day as initial dose.

Dialysis (CrCl less than 10 mL/min)

2.5 mg/day as initial dose.

Children (6 yr of age and older)

PO Start with 0.07 mg/kg every day (up to 5 mg). Adjust dose according to BP response. Doses above 0.61 mg/kg (or in excess of 40 mg) have not been studied. Not recommended in children with glomerular filtration rate less than 30 mL/min per 1.73 m 2 .

MI
Adults Initial dose

PO 5 mg, then 5 mg after 24 h, then 10 mg after 48 h.

Dose adjustment

PO In patients with low systolic BP (120 mm Hg or less) or when treatment is started during the first 3 days after infarct, administer 2.5 mg. If hypotension occurs (systolic BP 100 mm Hg or less) a daily maintenance dose of 5 mg may be given with temporary reductions to 2.5 mg if needed. If prolonged hypotension occurs (systolic BP less than 90 mm Hg for more than 1 h), discontinue treatment.

Maintenance

PO 10 mg/day for 6 wk. Patients should receive, as appropriate, the standard recommended treatments, such as thrombolytics, aspirin, and beta-blockers.

Renal function impairment (CrCl exceeding 2 mg/dL)

Use with caution.

General Advice

  • Give prescribed dose without regard to meals. Administer with food if GI upset occurs.
  • Preparation of suspension: Add 10 mL of purified water to a polyethylene terephthalate bottle containing ten 20 mg tablets of lisinopril and shake for at least 1 minute. Add 30 mL of Bacitra diluent and 160 mL of OraSweet SF and shake gently for several seconds.

Storage/Stability

Tablets

Store tablets at 68° to 77°F. Protect from moisture, freezing, and excessive heat.

Suspension

Store suspension at controlled room temperature (below 77°F). Discard any unused suspension after 28 days.

Drug Interactions

Antacids

Lisinopril bioavailability may be decreased. Separate administration times by 1 to 2 h.

Antidiabetic agents

Risk of hypoglycemia may be increased.

Capsaicin

Cough may be exacerbated.

Digoxin

May increase or decrease plasma digoxin levels.

Diuretics

Excessive decrease in blood pressure may occur.

Gold therapy (eg, aurothiomalate)

Nitritoid reactions, including facial flushing, nausea, vomiting, and hypotension, may occur.

Indomethacin, salicylates (eg, aspirin)

Reduced hypotensive effects, especially in low-renin or volume-dependent hypertensive patients.

Lithium

Increased lithium levels and symptoms of lithium toxicity.

NSAIDs

Increased risk of renal function impairment.

Phenothiazines

May increase pharmacological effect of lisinopril.

Potassium-sparing diuretics, potassium preparations

May increase serum potassium levels.

Laboratory Test Interactions

False elevation of liver enzymes or serum bilirubin may occur.

Adverse Reactions

Cardiovascular

Hypotension (10%); orthostatic effects (1%); cardiac arrest, cerebral vascular accident, MI.

CNS

Dizziness (12%); headache (6%); fatigue (3%); stroke.

Dermatologic

Rash (2%); Stevens-Johnson syndrome, toxic epidermal necrolysis.

EENT

Visual loss.

GI

Diarrhea (4%); nausea (2%); vomiting (1%).

Genitourinary

Renal function impairment (2%); impotence (1%); acute renal failure, anuria, oliguria, progressive azotemia, uremia.

Hematologic

Bone marrow depression; hemolytic anemia; leukopenia/neutropenia; thrombocytopenia.

Hepatic

Hepatocellular or cholestatic jaundice.

Metabolic

Hyperkalemia.

Respiratory

Cough (4%); upper respiratory tract infections (2%); common cold (1%); malignant lung neoplasm.

Miscellaneous

Chest pain (3%); abdominal pain (2%); asthenia (1%); anaphylactoid reactions; angioedema; symptom complex that includes a positive antinuclear antibody, elevated erythrocyte sedimentation rate, arthralgia/arthritis, myalgia, fever, vasculitis, eosinophilia, and leukocytosis.

Precautions

Warnings

Pregnancy

When used in pregnancy during the second and third trimesters, ACE inhibitors can cause injury and even death to the developing fetus. When pregnancy is detected, discontinue therapy as soon as possible.


Monitor

Frequently monitor serum potassium in patients with risk factors for hyperkalemia (eg, renal insufficiency, diabetes mellitus, concomitant use of potassium supplements).


Pregnancy

Category D (second and third trimester); Category C (first trimester). Can cause injury or death to fetus if used during the second or third trimester.

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 6 yr of age.

Elderly

Use with caution, usually starting at the low end of the dosage range because of the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant diseases or other drug therapy.

Renal Function

Reduce dose and give less frequently. In renal function impairment, stable elevations in BUN and serum creatinine may occur because of inadequate renal perfusion; monitor renal function during first few weeks of therapy and adjust dosage carefully, especially if glomerular filtration rate is less than 30 mL/min.

Angioedema

Use with extreme caution in patients with hereditary angioedema. Angioedema of the face, extremities, lips, tongue, glottis, larynx, and intestine has been reported in patients treated with ACE inhibitors.

Aortic stenosis/hypertrophic cardiomyopathy

As with other vasodilators, use lisinopril with caution in patients with obstruction in the outflow tract of the left ventricle.

Hepatic failure

Rarely, ACE inhibitors have been associated with a syndrome that starts with cholestatic jaundice and progresses to fulminant hepatic necrosis and sometimes death.

Hypotension/First-dose effect

Significant decreases in BP may occur after first dose, especially in severely salt- or volume-depleted patients or those with heart failure. Minimize risk by discontinuing diuretics, decreasing dose, or increasing salt intake approximately 1 wk prior to initiating drug.

Neutropenia and agranulocytosis

May occur; risk appears greater in patients with renal function impairment, heart failure, or immunosuppression.

Surgery/Anesthesia

Risk of hypotension may be increased.

Overdosage

Symptoms

Hypotension.

Patient Information

  • Advise patient to take prescribed dose without regard to meals but to take with food if stomach upset occurs.
  • Advise patient or caregiver to shake suspension well before measuring dose and administer prescribed dose using dosing cup, spoon, or syringe.
  • Advise patient to try to take each dose at about the same time each day.
  • Inform hypertensive patient that drug controls, but does not cure, hypertension and to continue taking drug as prescribed even when BP is not elevated.
  • Instruct patient to continue taking other medications for the condition as prescribed by health care provider.
  • Instruct patient in BP and pulse measurement skills.
  • Advise patient to monitor and record BP and pulse at home and to inform health care provider should abnormal measurements be noted. Also advise patient to take record of BP and pulse to each follow-up visit.
  • Caution patient to avoid sudden position changes to prevent orthostatic hypotension.
  • Instruct patient to lie or sit down if experiencing dizziness or light-headedness when standing.
  • Emphasize to hypertensive patient the importance of other modalities on BP control: weight control, regular exercise, smoking cessation, and moderate intake of alcohol and salt.
  • Emphasize to heart failure patient the importance of other modalities that can help control heart failure symptoms: weight control, progressive exercise program, smoking cessation, and moderate intake of alcohol and salt.
  • Advise heart failure patient to weigh daily, keep a record of daily weights, and notify health care provider if rapid weight gain (eg, 5 pounds in 1 wk) is noted or if edema or shortness of breath is getting worse.
  • Caution patient that inadequate fluid intake, excessive perspiration, diarrhea, or vomiting can lead to excessive fall in BP, resulting in light-headedness or fainting.
  • Advise patient that medication may cause dizziness or light-headedness and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
  • Caution patient to avoid unnecessary exposure to ultraviolet (UV) light (eg, sunlight, tanning booths) and to use sunscreen and wear protective clothing when exposed to UV light to avoid photosensitivity reaction.
  • Instruct patient to stop taking drug and immediately report any of these symptoms to health care provider: chest pains; difficulty breathing; fainting; fever; irregular heartbeat; sore throat; swelling of the face, lips, eyelids, or tongue; or swelling of the hands or feet.
  • Instruct patient to inform health care provider if a persistent cough develops while taking this medication.
  • Caution patient not to take any prescription or OTC medications, potassium-containing salt substitutes, potassium supplements, or dietary supplements unless advised by health care provider.

Copyright © 2009 Wolters Kluwer Health.

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