Lisinopril (Zestril) - Uses, Dose, Side effects, MOA, Brands

Lisinopril (Zestril) is an ACE-inhibitor (angiotensin-converting enzyme inhibitor) that is used for treating hypertension and heart failure.

Indications of Lisinopril (Zestril):

  • Heart failure with reduced ejection fraction:
    • To lessen the signs and symptoms of systolic heart failure, it is used as an adjuvant therapy.
  • Hypertension:
    • It is approved for the treatment of hypertension in adults and children older than 6 years old.
  • ST-elevation myocardial infarction:
    • In hemodynamically stable patients, it is successful in treating acute MI within 24 hours to increase survival.
  • Off Label Use of Lisinopril in Adults:
    • Non-ST-elevation acute coronary syndrome
    • Posttransplant erythrocytosis (renal transplant recipients)
    • Proteinuric chronic kidney disease (diabetic or nondiabetic)
    • Stable coronary artery disease

Lisinopril (Zestril) dose in adults:

Lisinopril (Zestril) dose in the treatment of acute coronary syndromes:

For Non-ST-Elevation Acute Coronary Syndrome:

  • Patients must be stable before starting treatment.
  • It's used along with other medicines like antiplatelet agents, beta-blockers, and statins.
  • If patients have diabetes, a weak heart (left ventricular ejection fraction ≤40%), high blood pressure, or stable kidney disease, they should keep taking lisinopril indefinitely.
  • The initial dose is usually 2.5 to 10 milligrams once a day, depending on their initial blood pressure.
  • The doctor may slowly increase the dose up to a maximum of 40 milligrams per day based on how well they tolerate it and how well it works.

For ST-Elevation Myocardial Infarction:

  • Patients must be stable before starting treatment.
  • It's used along with other medicines like antiplatelet agents, beta-blockers, and statins.
  • Continue taking lisinopril indefinitely.
  • The initial dose is typically 2.5 to 5 milligrams once a day, and it should be started within 24 hours of the heart event.
  • The doctor may slowly increase the dose, up to 10 milligrams per day or more if it's well tolerated, while closely monitoring to prevent low blood pressure.
  • The maximum dose is usually 40 milligrams per day.

For Heart Failure with Reduced Ejection Fraction:

  • The initial dose is 2.5 to 5 milligrams once a day.
  • Depending on how well it's tolerated, the dose can be increased every 1 to 2 weeks, but not by more than 10 milligrams at a time.
  • The goal is to reach a target dose of 40 milligrams once a day, following guidelines from the ACCF/AHA.

These dosing guidelines can vary depending on the patient's specific condition and response to treatment. It's crucial for individuals to follow their doctor's instructions carefully and to have regular check-ups to monitor their progress and any potential side effects.

Lisinopril (Zestril) Treatment dose of Hypertension: Note:

  • If your blood pressure is significantly higher than the target level (≥20/10 mm Hg above the goal), your doctor may prescribe lisinopril in combination with another appropriate medication, such as a long-acting dihydropyridine calcium channel blocker or a thiazide diuretic.
  • For patients whose blood pressure is only slightly above the target level (<20/10 mm Hg above the goal), some experts suggest starting with lisinopril alone (monotherapy). However, as time goes on, many patients may require a combination of medications to effectively control their blood pressure.
  • The initial dose of lisinopril is typically 5 to 10 milligrams taken once a day.
  • Your doctor will monitor your blood pressure response every 4 to 6 weeks and adjust the dose as needed. The dose can be increased in one-step increments, such as doubling the daily dose.
  • The maximum recommended dose for hypertension is 40 milligrams taken once daily.

Lisinopril (Zestril) dose in the treatment of Post transplant erythrocytosis (renal transplant recipients) (off-label):

Lisinopril can be used off-label to treat a condition called Posttransplant Erythrocytosis in renal transplant recipients, especially when their hemoglobin concentration is greater than 17 g/dL (grams per deciliter).

  • The initial dose of lisinopril is typically 2.5 or 5 milligrams taken once a day.
  • If there isn't a sufficient improvement within 4 weeks, the doctor may increase the dose up to a maximum of 40 milligrams per day based on how the patient's hemoglobin and blood pressure respond.
  • If the hemoglobin level remains above 17 g/dL after an additional 4 weeks of treatment, the doctor may consider additional therapies like phlebotomy (removing blood from the body) to lower the hemoglobin level.

Lisinopril (Zestril) Treatment dose of proteinuric chronic kidney disease (diabetic or non-diabetic) (off-label):

Dosing recommendations based on expert opinion and general dosing range in manufacturer's labeling:

  • Initial Dose: The initial dose of lisinopril typically ranges from 2.5 to 10 milligrams taken once daily. The specific initial dose depends on the patient's blood pressure.
  • Titration: The dose can be slowly increased based on how well the patient tolerates the medication and their response to it. The maximum daily dose is usually 40 milligrams.
  • Goals: The treatment aims to achieve both an appropriate blood pressure goal and a proteinuria goal of less than 1 gram per day.
  • For IgA Nephropathy: In addition to achieving an appropriate blood pressure goal, there is a recommended proteinuria goal of less than 1 gram per day. Some experts even aim for a lower proteinuria goal of less than 500 milligrams per day.
  • If Goals Are Not Met: If the proteinuria goal is not reached with the maximum dose of lisinopril alone, the doctor may consider adding other treatment modalities or medications to achieve the desired proteinuria reduction.

Lisinopril (Zestril) dose in children:

Note:

  • When using lisinopril, especially in liquid form, it's important to be careful because there are different concentrations available.
  • To prevent confusion, always make sure the dose is clearly stated in milligrams (mg) so that you know exactly how much you're taking.
  • This helps avoid mistakes when dealing with different lisinopril concentrations, whether you're using a commercially available liquid or one that's specially made for you (compounded).
  • So, remember to double-check the dose in milligrams to stay safe.

Lisinopril (Zestril) Treatment dose of Hypertension:

For Children Under 6 Years Old:

  • There is limited data available for this age group.
  • The initial dose is typically 0.07 milligrams per kilogram of the child's weight, taken once daily.
  • The maximum initial daily dose is 5 milligrams per day.
  • The maximum daily dose should not exceed 0.6 milligrams per kilogram of the child's weight or 40 milligrams per day.

For Children 6 Years and Older, Including Adolescents:

  • The initial dose is the same as for younger children: 0.07 milligrams per kilogram of their weight, taken once daily.
  • The maximum initial daily dose is 5 milligrams per day.
  • The maximum daily dose should not exceed 0.6 milligrams per kilogram of their weight or 40 milligrams per day.

It's important to note that in some cases, especially when children have certain health conditions like low sodium levels (hyponatremia), low blood volume (hypovolemia), severe congestive heart failure (CHF), reduced kidney function, or are taking diuretic medications, doctors may start with a lower initial dose. The dose can be adjusted based on the child's response to treatment.

Lisinopril (Zestril) Treatment dose of proteinuria (eg, mild IgA nephropathy, focal segmental glomerulosclerosis): Limited data available:

For Children 2 Years and Older, Including Adolescents:

  • The initial dose is typically between 0.1 to 0.2 milligrams per kilogram of the child's weight, taken once daily.
  • The goal is to increase the dose at 1- to 2-week intervals until reaching a target dose of 0.4 milligrams per kilogram of the child's weight, taken once daily.
  • The maximum daily dose should not exceed 40 milligrams per day.

These dosing recommendations are based on limited data from studies involving children and adolescents with conditions like FSGS and mild IgA nephropathy. In these studies, lisinopril was used to help reduce proteinuria.


Lisinopril (Zestril) Pregnancy Risk Category: X

  • Lisinopril is a medication that can cross the placenta and can potentially harm the developing fetus if used during pregnancy.
  • There is an increased risk of fetal malformations, but this risk may also be influenced by the mother's underlying health condition.
  • It's essential to discontinue lisinopril as soon as pregnancy is detected because it can lead to problems in the developing baby, including kidney and lung issues, as well as skeletal malformations.
  • Babies exposed to lisinopril in the womb need monitoring for certain complications.
  • Chronic maternal hypertension itself can also have negative effects on both the baby and the mother.
  • If a pregnant woman needs treatment for high blood pressure, lisinopril is generally avoided, and other options are considered.
  • It's crucial for sexually active women to use effective contraception when taking lisinopril, and women planning to become pregnant should generally avoid this medication unless there are no other treatment options for their high blood pressure.

Lisinopril use during breastfeeding:

  • The presence of lisinopril in breast milk is not well-established.
  • Because there is a potential for serious adverse reactions in a breastfed infant, the manufacturer suggests that a decision should be made by the mother and her healthcare provider regarding whether to stop breastfeeding or to discontinue lisinopril use.
  • This decision should consider the potential risks and benefits to both the mother and the baby, and it's important to consult with a healthcare provider for guidance on the best course of action in this situation.
  • The safety of lisinopril during breastfeeding has not been definitively determined, so individual circumstances and medical advice should be taken into account.

Lisinopril (Zestril) Dose adjustment in renal disease:

These dosage adjustments for lisinopril are based on the patient's kidney function, as measured by the estimated creatinine clearance (CrCl) or glomerular filtration rate (GFR):

For Heart Failure with Reduced Ejection Fraction:

  • If the CrCl is greater than 30 mL/minute, no dosage adjustment is usually necessary.
  • If the CrCl is between 10 and 30 mL/minute or less than 10 mL/minute, the initial dose is typically 2.5 mg taken once daily, with a maximum daily dose of 40 mg.
  • For patients on hemodialysis, the initial dose is 2.5 mg once daily, as lisinopril is dialyzable. The maximum daily dose is 40 mg.

For Hypertension:

  • If the CrCl is greater than 30 mL/minute, no dosage adjustment is generally needed.
  • If the CrCl is between 10 and 30 mL/minute, the initial dose is typically 5 mg taken once daily, with a maximum daily dose of 40 mg.
  • For patients with a CrCl less than 10 mL/minute or those on hemodialysis, the initial dose is usually 2.5 mg taken once daily, with a maximum daily dose of 40 mg.

For ST-Elevation Myocardial Infarction:

  • Similar to heart failure and hypertension, if the CrCl is greater than 30 mL/minute, no dosage adjustment is usually required.
  • If the CrCl is between 10 and 30 mL/minute or less than 10 mL/minute, the initial dose is typically 2.5 mg taken once daily, with a maximum daily dose of 40 mg.
  • For patients on hemodialysis, the initial dose is 2.5 mg once daily, with a maximum daily dose of 40 mg.

Additionally, the following dosage adjustments have been recommended:

  • For GFR (glomerular filtration rate) greater than 50 mL/minute, typically no dosage adjustment is necessary.
  • For GFR between 10 and 50 mL/minute, the usual dose may need to be reduced to 50-75% of the regular dose.
  • For GFR less than 10 mL/minute, the dose may need to be reduced to 25-50% of the usual dose.
  • For patients on intermittent hemodialysis, the dose should be administered after dialysis.
  • For patients on continuous renal replacement therapy (CRRT), the dose may need to be reduced to 50-75% of the usual dose.

These adjustments are important to ensure that the medication is effectively cleared from the body, especially in patients with impaired kidney function, to prevent potential side effects.

Lisinopril (Zestril) Dose adjustment in liver disease:

The manufacturer's labeling for lisinopril does not provide specific dosage adjustments for individuals with liver impairment. However, it is recommended to use lisinopril with caution in such cases. Liver impairment can affect the way drugs are metabolized and eliminated from the body, potentially altering their effects.


Common Side Effects of Lisinopril (Zestril):

  • Cardiovascular:
    • Hypotension
  • Central nervous system:
    • Dizziness
  • Renal:
    • Increased blood urea nitrogen
    • Increased serum creatinine

Rare Side Effects of Lisinopril (Zestril):

  • Cardiovascular:
    • Chest Pain
    • Orthostatic Effect
    • Flushing
    • Vasculitis
    • Syncope
  • Central Nervous System:
    • Altered Sense Of Smell
    • Paresthesia
    • Fatigue
    • Vertigo
    • Headache
  • Dermatologic:
    • Toxic Epidermal Necrolysis
    • Skin Photosensitivity
    • Alopecia
    • Erythema
    • Diaphoresis
    • Pruritus
    • Stevens-Johnson Syndrome
    • Urticaria
    • Skin Rash
  • Endocrine & Metabolic:
    • SIADH
    • Diabetes Mellitus
    • Hyperkalemia
    • Gout
  • Gastrointestinal:
    • Flatulence
    • Constipation
    • Pancreatitis
    • Dysgeusia
    • Xerostomia
    • Diarrhea
  • Genitourinary:
    • Impotence
  • Hematologic & Oncologic:
    • Positive ANA Titer
    • Eosinophilia
    • Increased Erythrocyte Sedimentation Rate
    • Leukopenia
    • Hemolytic Anemia
    • Neutropenia
    • Thrombocytopenia
    • Leukocytosis
    • Bone Marrow Depression
  • Neuromuscular & Skeletal:
    • Arthritis
    • Weakness
    • Myalgia
    • Arthralgia
  • Ophthalmic:
    • Diplopia
    • Vision Loss
    • Photophobia
    • Blurred Vision
  • Otic:
    • Tinnitus
  • Renal:
    • Renal insufficiency
  • Respiratory:
    • Cough

Side effects of Lisinopril (Zestril) (Frequency not defined):

  • Hematologic & oncologic:
    • Decreased hemoglobin
    • Decreased hematocrit
  • Hepatic:
    • Increased serum bilirubin
    • Increased liver enzymes

Contraindications to Lisinopril (Zestril):

  • Hypersensitivity: If you are allergic to lisinopril, other ACE inhibitors, or any components of the medication, it should not be used.
  • Angioedema: If you have experienced angioedema (swelling of deeper layers of the skin) related to previous treatment with an ACE inhibitor, lisinopril should be avoided.
  • Idiopathic or Hereditary Angioedema: Lisinopril is contraindicated in individuals with idiopathic (of unknown cause) or hereditary angioedema, as it can potentially worsen these conditions.
  • Concomitant Use with Aliskiren: Do not take lisinopril if you are already using aliskiren and have diabetes mellitus. Combining these medications can be harmful.
  • Coadministration with Neprilysin Inhibitors: Lisinopril should not be taken together with or within 36 hours of switching to or from a neprilysin inhibitor, such as sacubitril. Combining these medications can increase the risk of side effects.

Additional Canadian Labeling Contradictions (not in US labeling):

  • Women who are pregnant, intend to become pregnant, or are of childbearing potential and not using adequate contraception should avoid lisinopril.
  • Breastfeeding is contraindicated.
  • Avoid concomitant use with aliskiren, angiotensin receptor blockers (ARBs), or other ACE inhibitors in patients with moderate to severe renal impairment, hyperkalemia, or heart failure who are hypotensive.
  • Also, avoid concomitant use with ARBs or other ACE inhibitors in diabetic patients with end organ damage.
  • Lisinopril is not recommended for use in pediatric patients under 6 years of age or in pediatric patients aged 6 to 16 years with severe renal impairment.

Warnings and precautions

Angioedema

  • Angioedema is a rare but potentially serious side effect that can occur with ACE inhibitors like lisinopril, even after the first dose.
  • It can cause swelling, especially in the head and neck areas, which could compromise the airway and make it difficult to breathe.
  • In some cases, it may affect the intestines and cause abdominal pain.
  • Black patients may have a higher risk of developing angioedema, and the risk may also increase if lisinopril is used alongside certain medications like mTOR inhibitors (e.g., everolimus) or neprilysin inhibitors (e.g., sacubitril).
  • If angioedema occurs, especially if it involves the tongue, glottis (part of the larynx), or larynx (voice box), it can be life-threatening due to the risk of airway blockage.
  • People with a history of airway surgery are at higher risk.
  • Immediate and appropriate medical attention is crucial in these situations.
  • Lisinopril is contraindicated in patients with a history of idiopathic or hereditary angioedema or previous angioedema associated with ACE inhibitor therapy, meaning it should not be used in these cases.

Cholestatic jaundice

  • While rare, ACE inhibitors like lisinopril can potentially lead to a condition called cholestatic jaundice or hepatitis, which affects the liver.
  • This condition may progress to severe liver damage, including fulminant hepatic necrosis, which can be life-threatening, and in some cases, fatal.
  • If you experience a significant increase in hepatic transaminases (liver enzymes) or develop jaundice (yellowing of the skin or eyes), it's crucial to discontinue lisinopril and seek immediate medical attention.
  • Regular monitoring of liver function may also be recommended during lisinopril treatment to detect any early signs of liver problems.

Cough:

  • Sometimes, when people take ACE inhibitors like lisinopril, they might develop a dry, persistent cough that usually starts within the first few months of taking the medication.
  • However, this cough should go away within 1 to 4 weeks after you stop taking the ACE inhibitor.
  • Before you stop, your doctor will check to make sure the cough is really caused by the medication and not something else, like lung congestion in people with heart problems, and they'll rule out other possible reasons for the cough.
  • So, if you have a cough while taking an ACE inhibitor, talk to your doctor before making any changes to your medication.

Hematologic effects

  • While this information specifically mentions another ACE inhibitor called captopril, it's important to be aware that ACE inhibitors in general, including lisinopril, can have potential effects on the blood.
  • These effects may include a condition called neutropenia, which involves a decrease in a type of white blood cell called neutrophils, leading to myeloid hypoplasia (reduced production of blood cells) and, in severe cases, agranulocytosis (a significant reduction in white blood cells).
  • Additionally, ACE inhibitors may also lead to anemia (low red blood cell count) and thrombocytopenia (low platelet count).
  • Patients with kidney problems are at a higher risk of developing neutropenia, and those with both kidney issues and collagen vascular diseases like systemic lupus erythematosus are at even greater risk.
  • Therefore, regular monitoring of complete blood counts (CBC) with a differential is recommended for patients with these risk factors to detect and manage any potential blood-related issues promptly.

Hyperkalemia:

  • Taking ACE inhibitors like lisinopril can sometimes lead to a condition called hyperkalemia, which means having too much potassium in the blood.
  • Certain factors can increase the risk of hyperkalemia when using ACE inhibitors, including kidney problems, diabetes, and the simultaneous use of potassium-sparing diuretics, potassium supplements, or potassium-containing salts.
  • If you have any of these risk factors, your healthcare provider may recommend using ACE inhibitors cautiously or may choose alternative medications.
  • It's essential to monitor your potassium levels regularly while taking ACE inhibitors to prevent and manage hyperkalemia.

Hypersensitivity reactions

  • When using ACE inhibitors like lisinopril, it's important to be aware of the potential for hypersensitivity reactions, including anaphylactic or anaphylactoid reactions.
  • These reactions can be severe and life-threatening.
  • In some cases, particularly during certain medical procedures like hemodialysis using specific dialysis membranes (e.g., AN69) or low-density lipoprotein apheresis with dextran sulfate cellulose, severe anaphylactoid reactions have been reported.
  • Rare instances of anaphylactoid reactions have also occurred in patients receiving ACE inhibitors while undergoing sensitization treatment for hymenoptera (bee or wasp) venom allergies.
  • If you experience symptoms of a severe allergic reaction, such as difficulty breathing, swelling, or a sudden drop in blood pressure, seek immediate medical attention.

Hypotension/syncope

  • Hypotension (low blood pressure) and syncope (fainting) can sometimes happen, particularly with the first few doses of ACE inhibitors like lisinopril.
  • These effects are more likely to occur in patients who have a lack of fluid in their bodies (volume depletion).
  • To prevent this, healthcare providers should correct any volume depletion in patients before they start taking ACE inhibitors.
  • Monitoring is crucial, especially during the first few weeks of treatment or when the dose is increased.
  • The goal is to lower blood pressure at a rate that is safe for the patient's health.
  • Sometimes, reducing the dose may be necessary, but experiencing hypotension is not a reason to stop taking ACE inhibitors, especially for patients with heart failure, where lowering systolic blood pressure can be beneficial.
  • However, it's important to avoid using ACE inhibitors in patients who are hemodynamically unstable after a heart attack.

Renal function deterioration:

  • The use of ACE inhibitors like lisinopril can sometimes lead to a decline in kidney function and an increase in blood urea nitrogen (BUN) and serum creatinine levels.
  • This is more likely to occur in patients with conditions that affect renal blood flow, such as renal artery stenosis or heart failure, where the glomerular filtration rate (GFR) relies on the constriction of certain blood vessels by angiotensin II.
  • The deterioration in kidney function may manifest as reduced urine output (oliguria), acute renal failure, and increasing levels of waste products in the blood (azotemia).
  • In some cases, there may be a slight and non-harmful increase in serum creatinine levels when starting ACE inhibitors.
  • It's generally recommended to discontinue ACE inhibitors only if there is a significant and progressive deterioration in renal function.

Aortic stenosis

  • In patients with severe aortic stenosis, the use of ACE inhibitors like lisinopril should be approached with caution.
  • ACE inhibitors may reduce the ability of the heart to adequately pump blood through a narrowed aortic valve, potentially leading to reduced coronary perfusion (blood flow to the heart muscle) and ischemia (inadequate oxygen supply to the heart).
  • This caution is important because ACE inhibitors can affect the balance of blood flow in the heart.
  • If you have severe aortic stenosis, your healthcare provider will carefully consider the potential risks and benefits of using lisinopril, and they may monitor your heart function closely while you are on the medication.

Ascites:

  • The use of ACE inhibitors like lisinopril should generally be avoided in patients with ascites caused by cirrhosis or refractory ascites.
  • However, if it is deemed necessary to use ACE inhibitors in such patients, close monitoring of blood pressure and kidney function is essential.
  • This monitoring helps prevent the rapid development of renal failure, which can occur in this specific population.
  • The decision to use ACE inhibitors in patients with ascites due to cirrhosis should be made carefully, and healthcare providers will assess the potential risks and benefits on a case-by-case basis.

Cardiovascular disease

  • In patients with cardiovascular disease, particularly those with ischemic heart disease or cerebrovascular disease, starting therapy with medications like lisinopril should be done with careful observation.
  • This is because a sudden drop in blood pressure, which can occur with these medications, may have serious consequences such as heart attacks (MI) or strokes.
  • If low blood pressure occurs, it can often be managed by providing fluid replacement, which can help restore blood pressure to safer levels.
  • Once the blood pressure stabilizes, therapy with the medication can be resumed.
  • However, if hypotension (low blood pressure) recurs or becomes problematic, discontinuing the medication may be necessary.

Collagen vascular disease:

  • Patients with collagen vascular diseases should use ACE inhibitors like lisinopril with caution, especially if they also have kidney impairment.
  • These patients may be at an increased risk for hematologic toxicity, which means there may be a higher chance of experiencing adverse effects related to blood cells.
  • It's essential for healthcare providers to carefully assess the risks and benefits of using ACE inhibitors in these patients and to monitor them closely, paying particular attention to their blood cell counts and overall health.

Hepatic impairment

  • Patients with hepatic (liver) impairment should exercise caution when using ACE inhibitors like lisinopril.
  • Before starting this medication, it is advisable to have baseline liver function tests (LFTs) done to assess the initial condition of the liver.
  • The liver plays a crucial role in metabolizing medications, and hepatic impairment can affect how drugs are processed in the body.
  • By monitoring liver function and being cautious, healthcare providers can ensure that lisinopril is administered safely in patients with liver issues.

Hypertrophic cardiomyopathy and outflow tract obstruction

  • Patients with hypertrophic cardiomyopathy (HCM) and outflow tract obstruction should use ACE inhibitors like lisinopril with caution.
  • These medications can reduce the heart's afterload, which is the force the heart has to overcome to pump blood out of the heart.
  • In some cases, this reduction in afterload may worsen symptoms associated with HCM, potentially making the condition more challenging to manage.
  • It's important for healthcare providers to carefully assess the risks and benefits of using lisinopril in these patients and to monitor their condition closely.

Renal artery stenosis

  • Patients with unstented unilateral or bilateral renal artery stenosis should use ACE inhibitors like lisinopril with caution.
  • Unilateral renal artery stenosis means that one of the arteries leading to the kidney is narrowed, while bilateral renal artery stenosis means both arteries are narrowed.
  • In cases of bilateral renal artery stenosis, the use of ACE inhibitors is generally avoided unless the potential benefits significantly outweigh the risks.
  • This caution is necessary because ACE inhibitors can affect kidney function, and in patients with renal artery stenosis, there is an elevated risk of deterioration in renal function.

Renal impairment

  • In individuals with preexisting renal insufficiency (kidney problems), ACE inhibitors like lisinopril should be used with caution.
  • In some cases, a dosage adjustment may be necessary to ensure safe and effective treatment.
  • It's crucial to avoid rapidly increasing the dosage of the medication, as this can potentially worsen renal impairment.
  • However, it's worth noting that in a retrospective cohort study involving elderly patients aged 65 and older who had experienced a heart attack and had impaired left ventricular function, the use of an ACE inhibitor was associated with a survival benefit.
  • This benefit was observed even in patients with elevated serum creatinine levels above 3 mg/dL (265 micromoles/L).
  • This suggests that, in some cases, the potential benefits of ACE inhibitors may outweigh the risks, even in individuals with impaired kidney function.

Lisinopril: Drug Interaction

Risk Factor C (Monitor therapy)

Alfuzosin

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Alteplase

Angiotensin-Converting Enzyme Inhibitors may intensify Alteplase's harmful or hazardous effects. In particular, there may be an elevated risk for angioedema.

Amphetamines

May lessen the effectiveness of antihypertensive agents.

Angiotensin II

May lessen the effectiveness of antihypertensive agents.

Antipsychotic Agents (Second Generation [Atypical])

Antipsychotic drugs' hypotensive effects may be enhanced by blood pressure-lowering medications (Second Generation [Atypical]).

Aprotinin

May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension.

AzaTHIOprine

AzaTHIOprine's myelosuppressive effects may be enhanced by angiotensin-converting enzyme inhibitors.

Barbiturates

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Benperidol

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Brigatinib

May lessen the effectiveness of antihypertensive agents.

Brimonidine (Topical)

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Dapoxetine

Antihypertensive Agents' bradycardic action may be strengthened by brutinib.

Dexmethylphenidate

May increase the angiotensin-converting enzyme inhibitors' orthostatic hypotensive effects.

Diazoxide

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Dipeptidyl Peptidase-IV Inhibitors

Can lessen an antihypertensive drug's therapeutic impact.

Drospirenone

May worsen angiotensin-converting enzyme inhibitors' toxic or severe effects. Particularly, there may be a higher incidence of angioedema.

DULoxetine

Drospirenone's hyperkalemic impact may be enhanced by angiotensin-converting enzyme inhibitors.

Eplerenone

Angiotensin-Converting Enzyme Inhibitors might make their effect on hyperkalemia stronger.

Everolimus

May intensify angiotensin-converting enzyme inhibitors' harmful or hazardous effects. Particularly, there may be a higher incidence of angioedema.

Ferric Gluconate

Angiotensin-Converting Enzyme Inhibitors might make ferric gluconate more harmful or poisonous.

Ferric Hydroxide Polymaltose Complex

Ferric Hydroxide Polymaltose Complex may have a more negative or toxic effect when taken with angiotensin-converting enzyme inhibitors. In particular, there may be an elevated risk for angioedema or allergic responses.

Gelatin (Succinylated)

Ferric Hydroxide Polymaltose Complex may have a more negative or toxic effect when taken with angiotensin-converting enzyme inhibitors. In particular, there may be an elevated risk for angioedema or allergic responses.

Gold Sodium Thiomalate

Ferric Hydroxide Polymaltose Complex may have a more negative or toxic effect when taken with angiotensin-converting enzyme inhibitors. In particular, there may be an elevated risk for angioedema or allergic responses.

Heparin

Angiotensin-Converting Enzyme Inhibitors might make their effect on hyperkalemia stronger.

Heparins (Low Molecular Weight)

Angiotensin-Converting Enzyme Inhibitors might make their effect on hyperkalemia stronger.

Herbs (Hypertensive Properties)

May lessen the effectiveness of antihypertensive agents.

Herbs (Hypotensive Properties)

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Hypotension-Associated Agents

The hypotensive action of hypotension-associated agents may be strengthened by blood pressure lowering medications.

Icatibant

May lessen the effectiveness of angiotensin-converting enzyme inhibitors in treating hypertension.

Levodopa-Containing Products

Levodopa-Containing Products' hypotensive effects may be strengthened by blood pressure-lowering medications.

Loop Diuretics

ay strengthen angiotensin-converting enzyme inhibitors' hypotensive effects. Angiotensin-Converting Enzyme Inhibitors' nephrotoxic effects may be increased by loop diuretics.

Lormetazepam

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Methylphenidate

May lessen the effectiveness of antihypertensive agents.

Molsidomine

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Naftopidil

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Nicergoline

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Nicorandil

Angiotensin-Converting Enzyme Inhibitors might make their effect on hyperkalemia stronger.

Nicorandil

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Nitroprusside

Nitroprusside's hypotensive impact may be strengthened by blood pressure-lowering medications.

Nonsteroidal Anti-Inflammatory Agents

Nonsteroidal Anti-Inflammatory Agents' negative/toxic effects may be increased by angiotensin-converting enzyme inhibitors. In particular, the combination may cause a marked decline in renal function. Angiotensin-Converting Enzyme Inhibitors' antihypertensive effects may be lessened by nonsteroidal anti-inflammatory drugs.

Pentoxifylline

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Pholcodine

Pholcodine's hypotensive impact may be strengthened by blood pressure lowering medications.

Phosphodiesterase 5 Inhibitors

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Potassium Salts

Angiotensin-Converting Enzyme Inhibitors might make their effect on hyperkalemia stronger.

Potassium-Sparing Diuretics

Angiotensin-Converting Enzyme Inhibitors might make their effect on hyperkalemia stronger.

Pregabalin

Angiotensin-Converting Enzyme Inhibitors may intensify Pregabalin's negative/toxic effects. Particularly, there may be a higher incidence of angioedema.

Prostacyclin Analogues

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Quinagolide

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Racecadotril

May intensify angiotensin-converting enzyme inhibitors' harmful or hazardous effects. In particular, this combination may make angioedema more likely.

Ranolazine

Angiotensin-Converting Enzyme Inhibitors might make their effect on hyperkalemia stronger.

Salicylates

May intensify angiotensin-converting enzyme inhibitors' nephrotoxic effects. The therapeutic benefit of angiotensin-converting enzyme inhibitors may be reduced by salicylates.

Sirolimus

Angiotensin-Converting Enzyme Inhibitors might make their effect on hyperkalemia stronger.

Tacrolimus (Systemic)

Tacrolimus's effect of making you more hyperkalemic may be enhanced by angiotensin-converting enzyme inhibitors (Systemic).

Temsirolimus

Angiotensin-Converting Enzyme Inhibitors might make their effect on hyperkalemia stronger.

Thiazide and Thiazide-Like Diuretics

May increase the angiotensin-converting enzyme inhibitors' hypotensive effects. Angiotensin-Converting Enzyme Inhibitors' nephrotoxic effects may be increased by thiazide and thiazide-like diuretics.

TiZANidine

May intensify Lisinopril's hypotensive effects.

Tolvaptan

Angiotensin-Converting Enzyme Inhibitors might make their effect on hyperkalemia stronger.

Trimethoprim

Angiotensin-Converting Enzyme Inhibitors might make their effect on hyperkalemia stronger.

Yohimbine

May lessen the effectiveness of antihypertensive agents.

Risk Factor D (Consider therapy modification)

Aliskiren

Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects. Angiotensin-Converting Enzyme Inhibitors' hypotensive effects may be strengthened by aliskiren. Angiotensin-Converting Enzyme Inhibitors' nephrotoxic effects may be made worse by aliskiren. Treatment: It is not advised for diabetic patients to take aliskiren along with ACEIs or ARBs. Combination therapy should be avoided in other patients, especially when CrCl is less than 60 mL/min. If combined, keep a close eye on your blood pressure, potassium, and creatinine levels.

Allopurinol

Angiotensin-Converting Enzyme Inhibitors might make Allopurinol more likely to cause allergic or hypersensitive reactions.

Amifostine

Amifostine's hypotensive impact may be strengthened by blood pressure lowering medications. Treatment: Blood pressure-lowering drugs need to be avoided for 24 hours before amifostine is administered when used at chemotherapeutic doses. Amifostine should not be given if blood pressure lowering treatment cannot be stopped.

Angiotensin II Receptor Blockers

May worsen angiotensin-converting enzyme inhibitors' toxic or severe effects. Angiotensin-Converting Enzyme Inhibitors' serum levels may rise in response to angiotensin II receptor blockers. Management: According to US labelling, it is not advisable to take telmisartan and ramipril. It is unclear whether another ACE inhibitor and ARB combo would be any safer. When possible, take into account alternatives to the mix.

Grass Pollen Allergen Extract (5 Grass Extract)

Grass pollen allergen extract may have a more negative or toxic effect if angiotensin-converting enzyme inhibitors are used (5 Grass Extract). With regard to grass pollen allergen extract, ACE inhibitors may specifically enhance the likelihood of a severe allergic reaction (5 Grass Extract).

Iron Dextran Complex

Angiotensin-Converting Enzyme Inhibitors might make Iron Dextran Complex more harmful or poisonous. Patients taking an ACE inhibitor may be more susceptible to events of the anaphylactic variety. Management: Adhere strictly to the instructions for iron dextran administration, including the use of a test dose before the initial therapeutic dose and the availability of resuscitation tools and qualified people.

Lanthanum

May lower angiotensin-converting enzyme inhibitors' serum concentration. Angiotensin-converting enzyme inhibitors should be given at least two hours before or after lanthanum.

Lithium

The serum concentration of lithium may rise in response to angiotensin-converting enzyme inhibitors. Management: After adding an ACE inhibitor, lithium dosage decreases will probably be required. Following the addition or discontinuation of concurrent ACE inhibitor therapy, carefully monitor the patient's response to lithium.

Obinutuzumab

The hypotensive effects of blood pressure-lowering medications may be strengthened. Management: Take into account temporarily stopping blood pressure-lowering drugs 12 hours before the start of the obinutuzumab infusion and keeping them off until 1 hour after the infusion is finished.

Sodium Phosphates

The nephrotoxic impact of sodium phosphates may be enhanced by angiotensin-converting enzyme inhibitors. In particular, there may be an increased risk of acute phosphate nephropathy. Treatment: You might want to temporarily stop taking ACEIs or look into alternatives to the oral sodium phosphate bowel preparation in order to prevent this combo. Maintaining appropriate hydration and properly monitoring renal function should be done if the combination cannot be avoided.

Urapidil

Angiotensin-Converting Enzyme Inhibitors may interact with them through an unidentified method. Avoid taking urapidil and ACE inhibitors simultaneously as a management strategy.

Risk Factor X (Avoid combination)

Bromperidol

The hypotensive impact of bromperidol may be enhanced by blood pressure lowering medications. Blood Pressure Lowering Agents' hypotensive effects may be lessened by bromperidol.

Sacubitril

The negative or hazardous effects of sacubitril may be increased by angiotensin-converting enzyme inhibitors. In particular, this combination may raise the risk of angioedema.

Monitoring parameters:

  • Blood Pressure and Heart Rate: Regularly monitor blood pressure and heart rate to ensure they are within target ranges.
  • Kidney Function: Monitor blood urea nitrogen (BUN), serum creatinine, and potassium levels to assess kidney function.
  • Liver Function: Consider baseline liver function tests (LFTs) if the patient has preexisting hepatic (liver) impairment. Watch for signs of jaundice or hepatic failure.
  • Collagen Vascular Disease and Renal Impairment: For patients with collagen vascular disease and/or renal impairment, periodically check complete blood counts (CBC) with a differential to assess blood cell levels.

Heart Failure Management

  • Renal Function and Serum Potassium: Within 1 to 2 weeks after starting treatment for heart failure, and periodically thereafter, reevaluate renal function and serum potassium levels. This is especially important for patients with preexisting hypotension, hyponatremia, diabetes, azotemia, or those taking potassium supplements.

Hypertension Management

  • 2017 ACC/AHA Guidelines:
    • Confirmed hypertension with known cardiovascular disease (CVD) or a 10-year risk of atherosclerotic cardiovascular disease (ASCVD) ≥10%: Target blood pressure should be below 130/80 mm Hg.
    • Confirmed hypertension without markers of increased ASCVD risk: A target blood pressure below 130/80 mm Hg may be reasonable.
  • Diabetes and Hypertension (ADA Guidelines 2019):
    • Patients aged 18 to 65 without ASCVD and a 10-year ASCVD risk below 15% should aim for a target blood pressure below 140/90 mm Hg.
    • Patients aged 18 to 65 with known ASCVD or a 10-year ASCVD risk exceeding 15% may consider a target blood pressure below 130/80 mm Hg if it's safe to achieve.
    • Patients aged over 65:
      • For those in good health or with complex/intermediate health, a target blood pressure below 140/90 mm Hg is recommended.
      • For those in very complex/poor health, a target blood pressure below 150/90 mm Hg is recommended.

How to administer Lisinopril (Zestril)?

Lisinopril should be taken by mouth as a single daily dose, and you can take it with or without food. You don't need to worry about timing it with your meals.


Mechanism of action of Lisinopril (Zestril):

Lisinopril is a medication that works as a competitive inhibitor of angiotensin-converting enzyme (ACE).

  • ACE normally converts angiotensin I into angiotensin II, which is a powerful vasoconstrictor (it narrows blood vessels).
  • Lisinopril inhibits this conversion, leading to lower levels of angiotensin II in the body.
  • When angiotensin II levels drop, it triggers an increase in plasma renin activity (a substance related to blood pressure regulation) and reduces the secretion of aldosterone (a hormone that affects blood pressure and electrolyte balance).
  • Lisinopril may also have an effect in the central nervous system (CNS), where it can decrease adrenergic (adrenaline-related) activity, helping to lower blood pressure.
  • Additionally, lisinopril may reduce the conversion of vasoactive kallikreins into active hormones by ACE inhibitors. This can further contribute to lowering blood pressure.

Overall, lisinopril's primary action is to relax blood vessels and reduce blood pressure, making it useful in managing conditions like hypertension and heart failure.

Onset of Action:

  • It typically starts working within about 1 hour after taking it.

Peak Effect (Hypotensive):

  • The peak effect for lowering blood pressure when taken orally occurs around 6 hours after taking the medication.

Duration:

  • Lisinopril's effects last for about 24 hours.

Metabolism:

  • Lisinopril is not metabolized in the body; it is eliminated primarily in its unchanged form.

Bioavailability:

  • In pediatric patients (2 to 15 years), it ranges from 20% to 36%.
  • In pediatric patients aged 6 to 16 years, it's approximately 28%.
  • In adults, it's around 25%, but this can vary (range: 6% to 60%). For patients with NYHA Class II-IV heart failure, the bioavailability is decreased to around 16%.

Half-Life Elimination:

  • The half-life of lisinopril is approximately 12 hours, meaning that it takes about 12 hours for half of the drug to be eliminated from the body.

Time to Peak Effect:

  • In pediatric patients aged 6 months to 15 years, the median time to peak effect is typically 5 to 6 hours.
  • In adults, it's around 7 hours.

Excretion:

  • Lisinopril is primarily excreted through the urine in its unchanged form.

International Brand Names of Lisinopril:

  • Prinivil
  • Qbrelis
  • Zestril
  • ACT Lisinopril
  • APO-Lisinopril
  • Auro-Lisinopril
  • DOM-Lisinopril
  • JAMP-Lisinopril
  • MYLANLisinopril
  • PMS-Lisinopril
  • Prinivil
  • PRO-Lisinopril-10
  • PRO-Lisinopril-20
  • PRO-Lisinopril-5
  • RAN-Lisinopril
  • RIVA-Lisinopril
  • SANDOZ Lisinopril
  • TEVA-Lisinopril
  • TEVA-Lisinopril
  • Acemin
  • Acepril
  • Acerbon
  • Acerdil
  • Aklis
  • Alapril
  • Albigone
  • Alfaken
  • Auroliza
  • Cipril
  • Coric
  • Dapril
  • Diroton
  • Dosteril
  • Doxapril
  • ES
  • Eucor
  • Fersivag
  • Fibsol
  • Genopril
  • Hypersil
  • Inhitril
  • Inopril
  • Irumed
  • Lestace
  • Linipril
  • Linopril
  • Linotor
  • Linvas
  • Lipril
  • Lisdene
  • Lisibeta
  • Lisidigal
  • Lisigamma
  • Lisihexal
  • Lisino
  • Lisipril
  • Lisir
  • Lisitens
  • Lisnoxl
  • Lisocard
  • Lisopress
  • Lisopril
  • Lisoril
  • Lispril
  • Listril
  • Longes
  • Nisirol
  • Nop
  • Noperten
  • Novatec
  • Odace
  • Omace
  • Pesatril
  • Presiten
  • Press
  • Prinil
  • Prinivil
  • Ranolip
  • Safepril
  • Sinopren
  • Sinopril
  • Skopryl
  • Stril
  • Tensikey
  • Tensiphar
  • Tensopril
  • Tensyn
  • Vitopril
  • Vivatec
  • Zenoril
  • Zestan
  • Zestril
  • Zinopril

Lisinopril Brand Names in Pakistan:

Lisinopril Tablets 5 mg in Pakistan

Bpmed

Medicraft Pharmaceuticals (Pvt) Ltd.

Corace

Bosch Pharmaceuticals (Pvt) Ltd.

Lace

Brookes Pharmaceutical Laboratories (Pak.) Ltd.

Lame

Atco Laboratories Limited

Liface

Hygeia Pharmaceuticals

Lisna

Zafa Pharmaceutical Laboratories (Pvt) Ltd.

Lisopril

Glaxosmithkline

Lispril

Werrick Pharmaceuticals

Lopress

Davis Pharmaceutical Laboratories

Lotide

Pharmatec Pakistan (Pvt) Ltd.

Nazipril

Nenza Pharmaceuticals (Pvt) Limited

Novatec

Obs

Renopril

Harmann Pharmaceutical Laboratories (Pvt) Ltd.

Sinopril

Obsons Pharmaceuticals

Trupril

Getz Pharma Pakistan (Pvt) Ltd.

Veskor

Raazee Theraputics (Pvt) Ltd.

Zenopril

Alliance Pharmaceuticals (Pvt) Ltd.

Zestril

Ici Pakistan Ltd.

Ziscar

Tabros Pharma

Lisinopril Tablets 10 Mg in Pakistan

Bepril

Unison Chemical Works

Bpmed

Medicraft Pharmaceuticals (Pvt) Ltd.

Corace

Bosch Pharmaceuticals (Pvt) Ltd.

Lace

Brookes Pharmaceutical Laboratories (Pak.) Ltd.

Lame

Atco Laboratories Limited

Liface

Hygeia Pharmaceuticals

Lisopril

Glaxosmithkline

Lispril

Werrick Pharmaceuticals

Lopress

Davis Pharmaceutical Laboratories

Lotide

Pharmatec Pakistan (Pvt) Ltd.

Nazipril

Nenza Pharmaceuticals (Pvt) Limited

Novatec

Obs

Renopril

Harmann Pharmaceutical Laboratories (Pvt) Ltd.

Sinopril

Obsons Pharmaceuticals

Trupril

Getz Pharma Pakistan (Pvt) Ltd.

Veskor

Raazee Theraputics (Pvt) Ltd.

Zenopril

Alliance Pharmaceuticals (Pvt) Ltd.

Zestril

Ici Pakistan Ltd.

Ziscar

Tabros Pharma

Lisinopril Tablets 20 Mg in Pakistan

Bpmed

Medicraft Pharmaceuticals (Pvt) Ltd.

Corace

Bosch Pharmaceuticals (Pvt) Ltd.

Gustorole

Pulse Pharmaceuticals

Lisna

Zafa Pharmaceutical Laboratories (Pvt) Ltd.

Lispril

Werrick Pharmaceuticals

Lopress

Davis Pharmaceutical Laboratories

Nazipril

Nenza Pharmaceuticals (Pvt) Limited

Zestril

Ici Pakistan Ltd.

Ziscar

Tabros Pharma

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