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lisinopril (Rx)Brand and Other Names:Prinivil, Zestril

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 2.5mg
  • 5mg
  • 10mg
  • 20mg
  • 30mg
  • 40mg
more...

Acute Myocardial Infarction

5 mg PO within 24 hours of onset of symptoms of acute MI, THEN 5 mg after 24 hours, 10 mg after 48 hours, and 10 mg qDay for 6 weeks

If patient has low systolic blood pressure (ie, ≤120 mm Hg) when treatment initiated or during the first 3 days, administer a lower dose of 2.5 mg

If hypotension occurs (systolic BP ≤100 mm Hg), a daily maintenance dose of 5 mg may be given, with temporary reductions to 2.5 mg if needed

Dosing considerations

  • Discontinue with prolonged hypotension (ie, systolic BP <90 mm Hg for >1 hr)

Hypertension

Uncomplicated essential hypertension

Not taking diuretic: 10 mg PO qDay initially; usual range is 20-40 mg/day as single daily dose

Dosing considerations

  • Taking diuretic: Discontinue diuretic for 2-3 days before initiating lisinopril to reduce chance of hypotension; may resume diuretic if blood pressure is not controlled; if diuretic cannot be discontinued, initial dose of lisinopril 5 mg should be used under supervision for at least 2 hours and until blood pressure has stabilized for at least 1 hour

Heart Failure

Adjunctive therapy with diuretics and (usually) digitalis

5 mg PO qDay initially; increase by ≤10 mg no more frequent than 2 week intervals to 20-40 mg PO qDay

Patients with hypnatremia (<130 mEq/L serum sodium): 2.5 mg PO qDay initially; increase by ≤10 mg no more frequent than 2 week intervals to 20-40 mg PO qDay

Usual effective dosage range: 5-40 mg PO qDay (Zestril); 5-20 mg PO qDay (Prinivil)

Dosage Modifications

Renal impairment

  • Acute myocardial infarction: Use caution in renal dysfunction (serum creatinine >2 mg/dL)
  • Hypertension and CrCl >30 mL/min: 10 mg PO qDay initially; not to exceed 40 mg/day
  • Hypertension and CrCl 10-30 mL/min: 5 mg PO qDay initially; not to exceed 40 mg/day
  • Hypertension and CrCl <10 mL/min or hemodialysis: 2.5 mg PO qDay initially; not to exceed 40 mg/day
  • Heart failure and CrCl <30 mL/min: 2.5 mg PO qDay initially; not to exceed 40 mg/day
  • Children with GFR <30 mL/min/1.73 m²: Not recommended

Diabetic Nephropathy (Off-label)

Initial: 5 mg PO qDay (with diuretic)

May gradually increase dose according to blood pressure response; dosage range is 20-40 mg/day

Dosing considerations

  • Long-term treatment with ACE inhibitors, usually combined with diuretics, reduces blood pressure and albuminuria and protects kidney function in patients with hypertension, diabetes mellitus, and nephropathy

Dosage Forms & Strengths

tablet

  • 2.5mg
  • 5mg
  • 10mg
  • 20mg
  • 30mg
  • 40mg
more...

Hypertension (Off-label)

<6 years old: Safety and efficacy not established

≥6 years: 0.07 mg/kg PO qDay initially, not to exceed 5 mg/day; may titrate upward to 0.61 mg/kg/day, not to exceed 40 mg/day 

See Administration for extemporaneous suspension

Primary Hypertension (Orphan)

Oral solution: Orphan designation for treatment of primary hypertension with complications and secondary hypertension in pediatric patients (ages 0 through 16 years of age)

Sponsors

  • codaDose, Inc; 5659 Southfield Drive; Flowery Branch, GA 30542
  • Silvergate Pharmaceuticals, Inc; 6251 Greenwood Plaza Blvd, Suite 101; Greenwood Village, CO 80111

Hypertension

Uncomplicated essential hypertension

Consider lower initial dose of 2.5-5 mg and titrate to response in the elderly

Usual range is 20-40 mg/day as single daily dose

Adjust dose to blood pressure response; doses up to 80 mg have been used but do not appear to have a greater effect

Dosing considerations

Taking diuretic: Discontinue diuretic for 2-3 days before initiating lisinopril to reduce chance of hypotension; may resume diuretic if blood pressure is not controlled; if diuretic cannot be discontinued, initial dose of lisinopril 2.5 mg should be used under supervision for at least 2 hours and until blood pressure has stabilized for at least 1 hour

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Interactions

Interaction Checker

lisinopril and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Dizziness (5-12%)

            1-10%

            Cough (4-9%)

            Headache (4-6%)

            Hyperkalemia (2-5%)

            Diarrhea (3-4%)

            Hypotension (1-4%)

            Chest pain (3%)

            Fatigue (3%)

            Nausea/vomiting (2%)

            Kidney disease, of AMI patients (2%)

            Rash (1-2%)

            <1%

            Immune hypersensitivity reaction

            Psoriasis

            Angioedema of the face, lips, throat; intestinal angioedema

            Anuria

            Atrial tachycardia

            Acute renal failure

            Arthralgia

            Alopecia

            Atrial fibrillation

            Bone marrow suppression

            Cutaneous pseudolymphoma

            Hypersomnia

            Leukopenia

            Mood changes

            Pancreatitis

            Skin infections

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            Warnings

            Black Box Warnings

            Discontinue as soon as possible when pregnancy is detected; affects renin-angiotensin system, causing oligohydramnios, which may result in fetal injury and/or death

            Contraindications

            Hypersensitivity to lisinopril/other ACE inhibitors

            History of ACE inhibitor-induced angioedema, hereditary or idiopathic angioedema

            Coadministration with aliskiren in patients with diabetes mellitus or with renal impairment (ie, GFR <60 mL/min/1.73 m2)

            Cautions

            Anaphylactoid reactions reported in some patients dialyzed with high-flux membranes

            Hematologic effects including agranulocytosis and neutropenia/agranulocytosis reported especially in patients with renal impairment and collagen vascular disease; monitor CBC periodically with differential

            Less effective in African Americans

            Excessive hypotension with concomitant diuretics, hypovolemia, hyponatremia may occur

            Risk of hyperkalemia, especially in patients with renal impairment or DM or in patients taking concomitant K+-elevating drugs

            ACE inhibition also causes an increase in bradykinin levels, which putatively mediates angioedema; in comparison with other patients, a higher incidence of angioedema caused by ACE inhibitors has been observed in black patients

            A dry hacking cough may occur within a few months of initiating drug therapy with ACE inhibitors; exclude other causes of cough before discontinuing therapy

            Cholestatic jaundice associated with ACE inhibitors; discontinue if marked elevation of hepatic transaminases or jaundice occurs

            Coadministration with mTOR inhibitors (eg, temsirolimus, everolimus) may increased risk for angioedema

            Discontinue STAT if patient becomes pregnant

            Use caution in patients with renal impairment; renal deterioration reported in patients with low renal blood flow

            Use caution in patients with severe aortic stenosis, cardiovascular disease, collagen vascular disease, hypertrophic cardiomyopathy

            Dual blockade of the renin-angiotensin-aldosterone system (ie, ARB plus an ACE inhibitor) in patients with established atherosclerotic disease or heart failure or with diabetes with end organ damage is associated with a higher frequency of hypotension, syncope, hyperkalemia, and changes in renal function (including acute renal failure), as compared with use of a single renin-angiotensin-aldosterone system agent; limit dual blockade to individually defined cases, with close monitoring of renal function

            Neonates with history of in utero exposure: If oliguria or hypotension occurs, support of blood pressure and renal perfusion; exchange transfusions or dialysis may be required

            Angioedema of the face, extremities, lips, tongue, glottis and/or larynx, including some fatal reactions, at any time during treatment; patients with involvement of the tongue, glottis or larynx are likely to experience airway obstruction, especially patients with history of airway surgery; promptly discontinue and provide appropriate therapy and monitoring until complete and sustained resolution of signs and symptoms of angioedema has occurred

            Intestinal angioedema reported; patients presented with abdominal pain (with or without nausea or vomiting); in some cases there was no prior history of facial angioedema and C-1 esterase levels were normal; symptoms resolved after stopping the ACE inhibitor

            Hypotension may occur sometimes complicated by oliguria, progressive azotemia, acute renal failure or death; patients at risk of excessive hypotension include heart failure with systolic blood pressure below 100 mmHg, ischemic heart disease, cerebrovascular disease, hyponatremia, high dose diuretic therapy, renal dialysis, or severe volume and/or salt depletion of any etiology; in such patients initiate therapy under medical supervision and follow such patients for the first two weeks of treatment and whenever dose of lisinopril and/or diuretic is increased; avoid use in patients who are hemodynamically unstable after acute MI; symptomatic hypotension also possible in patients with severe aortic stenosis or hypertrophic cardiomyopathy

            Patients undergoing major surgery or during anesthesia with agents that produce hypotension, lisinopril may block angiotensin II formation secondary to compensatory renin release; if hypotension occurs and considered to be due to this mechanism, it can be corrected by volume expansion

            Monitor renal function periodically; changes in renal function including acute renal failure can be caused by drugs that inhibit renin-angiotensin system; patients whose renal function may depend in part on activity of the renin-angiotensin system (e.g., patients with renal artery stenosis, chronic kidney disease, severe congestive heart failure, post-myocardial infarction or volume depletion) may be at particular risk of developing acute renal failure; consider withholding or discontinuing therapy in patients who develop a clinically significant decrease in renal function

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            Pregnancy & Lactation

            Pregnancy category: D

            Discontinue as soon as pregnancy detected; during the second and third trimesters of pregnancy, drugs that act directly on the renin-angiotensin system have been associated with fetal injury, including hypotension, neonatal skull hypoplasia, anuria, reversible and irreversible renal failure, and death

            Lactation: Not known if excreted into breast milk; not recommended

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Prevents the conversion of angiotensin I to angiotensin II (a potent vasoconstrictor) through competitive inhibition of angiotensin-converting enzyme resulting in decreased plasma angiotensin II concentrations; blood pressure may be reduced in part through decreased vasoconstriction, increased renin activity, and decreased aldosterone secretion

            Absorption

            Bioavailability: 25%

            Onset: 1 hr (initial); 6 hr (peak)

            Duration: 24 hr

            Peak plasma time: 6-8 hr

            Therapeutic plasma concentration: 1-5 ng/mL

            Distribution

            Protein bound: 25%

            Vd: 124 L

            Metabolism

            Does not undergo metabolism

            Elimination

            Half-life: 12 hr

            Renal clearance: 106 mL/min

            Total body clearance: 250 mL/min

            Excretion: Excreted unchanged entirely in the urine

            Dialysis: Removed by hemodialysis

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            Administration

            Extemporaneous suspension

            Crush ten 10 mg tabs in a mortar to a fine powder; add small portions of 1:1 mixture of Ora-Plus and Ora-Sweet and mix to a uniform paste; mix while adding incremental amounts of the vehicle to almost 100 mL; transfer to a graduated cylinder; rinse mortar with vehicle and add enough quantitiy to make 100 mL; store in amber plastic prescription bottles; label "shake well"

            Stable for 13 weeks at room temperature or refrigerated

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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