Zestril 20mg Tablets

Manufacturer UPSHER-SMITH Active Ingredient Lisinopril Tablets(lyse IN oh pril) Pronunciation lyse IN oh pril
WARNING: Do not take if you are pregnant. Use during pregnancy may cause birth defects or loss of the unborn baby. If you get pregnant or plan on getting pregnant while taking this drug, call your doctor right away. @ COMMON USES: It is used to treat high blood pressure.It is used to treat heart failure (weak heart).It is used to help heart function after a heart attack.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Antihypertensive
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Pharmacologic Class
Angiotensin-Converting Enzyme (ACE) Inhibitor
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Pregnancy Category
Not applicable (FDA has moved away from letter categories; contraindicated in 2nd/3rd trimesters)
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FDA Approved
Dec 1987
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Lisinopril is a medication used to treat high blood pressure, heart failure, and to improve survival after a heart attack. It works by relaxing blood vessels, which helps blood flow more easily and lowers blood pressure. This reduces the workload on your heart.
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How to Use This Medicine

Taking Your Medication Correctly

To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food, and it's best to take it at the same time every day.

Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better. It's also important to drink plenty of non-caffeinated liquids, unless your doctor advises you to limit your fluid intake.

Special Instructions for Liquid Formulation

If you have trouble swallowing pills, your doctor or pharmacist can help you prepare a liquid suspension. If a liquid formulation is prepared, make sure to shake it well before use. To ensure accurate dosing, measure the liquid carefully using the measuring device provided with the medication. If no device is included, ask your pharmacist for a suitable measuring tool.

Storing and Disposing of Your Medication

To maintain the quality and effectiveness of your medication, store it at room temperature in a dry place, away from the bathroom. Keep the lid tightly closed and avoid freezing the medication.

What to Do If You Miss a Dose

If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed dose.
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Lifestyle & Tips

  • Take medication exactly as prescribed, usually once daily.
  • Do not stop taking the medication without consulting your doctor, even if you feel well.
  • Avoid potassium supplements or salt substitutes containing potassium unless advised by your doctor.
  • Limit alcohol intake as it can further lower blood pressure.
  • Maintain a healthy diet (low sodium), regular exercise, and manage stress.
  • Inform your doctor or dentist that you are taking lisinopril before any surgery or dental procedures.

Dosing & Administration

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Adult Dosing

Standard Dose: Hypertension: 10 mg orally once daily. Heart Failure: 2.5-5 mg orally once daily. Acute MI: 5 mg orally (initial dose), then 5 mg after 24 hours, 10 mg after 48 hours, then 10 mg once daily for 6 weeks.
Dose Range: 2.5 - 40 mg

Condition-Specific Dosing:

hypertension: Initial: 10 mg once daily; Maintenance: 20-40 mg once daily. Max: 80 mg/day.
heartFailure: Initial: 2.5-5 mg once daily; Maintenance: 5-40 mg once daily.
acuteMyocardialInfarction: Initial: 5 mg within 24 hours of symptom onset, then 5 mg after 24 hours, 10 mg after 48 hours, then 10 mg once daily for 6 weeks.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Hypertension (6-16 years): Initial 0.07 mg/kg (max 5 mg) orally once daily; adjust dose based on response, max 0.6 mg/kg or 40 mg/day.
Adolescent: Hypertension (6-16 years): Initial 0.07 mg/kg (max 5 mg) orally once daily; adjust dose based on response, max 0.6 mg/kg or 40 mg/day.
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Dose Adjustments

Renal Impairment:

Mild: CrCl > 30 mL/min: No initial dose adjustment needed for hypertension. For heart failure, consider lower initial dose.
Moderate: CrCl 10-30 mL/min: Hypertension: Initial 5 mg once daily. Heart Failure: Initial 2.5 mg once daily.
Severe: CrCl < 10 mL/min (including dialysis patients): Hypertension: Initial 2.5 mg once daily. Heart Failure: Initial 2.5 mg once daily. Adjust dose based on blood pressure response.
Dialysis: Lisinopril is dialyzable. Administer dose after dialysis. Initial 2.5 mg once daily, adjust based on blood pressure response.

Hepatic Impairment:

Mild: No specific dose adjustment recommended.
Moderate: No specific dose adjustment recommended, but monitor closely as ACE inhibitors are primarily renally eliminated.
Severe: No specific dose adjustment recommended, but monitor closely as ACE inhibitors are primarily renally eliminated.

Pharmacology

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Mechanism of Action

Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor. It inhibits the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor. This inhibition leads to decreased angiotensin II levels, resulting in vasodilation (reduced peripheral vascular resistance), decreased aldosterone secretion (leading to increased sodium and water excretion and potassium retention), and reduced sympathetic nervous system activity. It also inhibits the degradation of bradykinin, a potent vasodilator, which may contribute to its antihypertensive effect and some side effects (e.g., cough, angioedema).
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 25-30% (variable, 6-60%)
Tmax: 6-8 hours
FoodEffect: Food does not affect the extent of absorption.

Distribution:

Vd: 0.64 L/kg
ProteinBinding: Not significantly protein bound (approximately 0%)
CnssPenetration: Limited

Elimination:

HalfLife: Functional half-life: 12.6 hours (due to prolonged binding to ACE)
Clearance: Renal clearance is approximately 50 mL/min
ExcretionRoute: Renal (unchanged)
Unchanged: 100%
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Pharmacodynamics

OnsetOfAction: Approximately 1 hour
PeakEffect: 6-8 hours
DurationOfAction: At least 24 hours

Safety & Warnings

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BLACK BOX WARNING

FETAL TOXICITY: When pregnancy is detected, discontinue ZESTRIL as soon as possible. Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus.
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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of kidney problems, including:
+ Inability to pass urine
+ Changes in urine output
+ Blood in the urine
+ Sudden significant weight gain
Signs of high potassium levels, such as:
+ Abnormal heartbeat
+ Confusion
+ Weakness, lightheadedness, or dizziness
+ Feeling like passing out
+ Numbness or tingling
+ Shortness of breath
Severe dizziness or fainting
Persistent cough
Severe stomach pain
Severe nausea or vomiting
Chest pain or pressure
Liver problems, which can be life-threatening. Monitor for signs such as:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes

Other Possible Side Effects

Most people experience few or no side effects. However, if you notice any of the following symptoms or any other unusual effects, contact your doctor for advice:

Dizziness or headache
* Cough

This is not an exhaustive list of potential side effects. If you have concerns or questions, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Sudden swelling of the face, lips, tongue, or throat (angioedema) - seek emergency medical attention immediately.
  • Difficulty breathing or swallowing.
  • Severe dizziness or fainting.
  • Persistent dry cough that does not go away.
  • Yellowing of skin or eyes (jaundice).
  • Signs of high potassium (e.g., muscle weakness, slow or irregular heartbeat).
  • Signs of infection (e.g., fever, sore throat) - rare, but report immediately.
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is crucial that you inform your doctor about the following conditions before starting this medication:

Any allergies you have, including allergies to this drug, its components, or other substances. Be sure to describe the symptoms you experienced, such as rash, itching, swelling, or difficulty breathing.
A history of angioedema, a severe and potentially life-threatening reaction characterized by swelling of the hands, face, lips, eyes, tongue, or throat, difficulty breathing, swallowing, or unusual hoarseness.
Kidney problems, as this medication may affect kidney function.
If you are taking a medication containing aliskiren, especially if you have diabetes or kidney problems, as this combination may increase the risk of adverse effects.
If you have taken a medication containing sacubitril within the last 36 hours, as this may interact with the current medication.
If you are breastfeeding, as it is recommended to avoid breastfeeding while taking this medication.

For Parents and Guardians:

If your child is under 6 years of age, do not administer this medication, as it is not recommended for children younger than 6 years old.

Additional Considerations:

This list is not exhaustive, and it is essential to inform your doctor and pharmacist about all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you may have.
* To ensure safe treatment, consult your doctor before starting, stopping, or changing the dose of any medication.
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Precautions & Cautions

Important Warnings and Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.

Caution with Daily Activities
Until you know how this medication affects you, avoid driving and other activities that require you to be alert. To minimize the risk of dizziness or fainting, rise slowly from a sitting or lying down position, and be cautious when climbing stairs.

Special Considerations

If you have diabetes (high blood sugar), closely monitor your blood sugar levels.
Follow your doctor's instructions for regular blood tests, blood pressure checks, and other laboratory tests.
If you are taking a salt substitute containing potassium, a potassium-sparing diuretic, or a potassium product, consult your doctor.
If you are on a low-salt or salt-free diet, discuss this with your doctor.
If you have high blood pressure and are taking this medication, talk to your doctor before using over-the-counter (OTC) products that may increase blood pressure, such as:
+ Cough or cold medications
+ Diet pills
+ Stimulants
+ Non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen or naproxen
+ Certain natural products or aids
Consult your doctor before consuming alcohol.
In hot weather or during physical activity, be cautious and drink plenty of fluids to avoid dehydration. Inform your doctor if you experience excessive sweating, fluid loss, vomiting, or diarrhea, as these may lead to low blood pressure.

Medication Effectiveness and Risks

This medication may be less effective in lowering blood pressure in Black patients. In some cases, additional medication may be necessary. If you have questions, discuss them with your doctor.
A severe and potentially life-threatening reaction called angioedema has been reported, with a higher risk in Black patients.
Low white blood cell counts have been associated with captopril, a similar medication. This may increase the risk of infection, particularly in individuals with kidney problems and other underlying health conditions. Seek medical attention immediately if you experience signs of infection, such as fever, chills, or sore throat.

Special Precautions for Older Adults
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects.
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Overdose Information

Overdose Symptoms:

  • Severe hypotension (very low blood pressure)
  • Dizziness
  • Lightheadedness
  • Fainting
  • Tachycardia (rapid heart rate)
  • Palpitations
  • Renal failure

What to Do:

If you suspect an overdose, seek emergency medical attention immediately or call a Poison Control Center at 1-800-222-1222. Management typically involves supportive care, including intravenous fluid administration to restore blood pressure.

Drug Interactions

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Contraindicated Interactions

  • Aliskiren (in patients with diabetes or renal impairment)
  • Sacubitril/valsartan (Entresto) - concurrent use or within 36 hours of last dose of sacubitril/valsartan due to increased risk of angioedema.
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Major Interactions

  • Potassium-sparing diuretics (e.g., spironolactone, triamterene, amiloride) - increased risk of hyperkalemia.
  • Potassium supplements - increased risk of hyperkalemia.
  • NSAIDs (e.g., ibuprofen, naproxen) - may reduce antihypertensive effect and increase risk of renal impairment, especially in elderly or volume-depleted patients.
  • Lithium - increased serum lithium levels and toxicity.
  • mTOR inhibitors (e.g., sirolimus, everolimus, temsirolimus) - increased risk of angioedema.
  • Racecadotril - increased risk of angioedema.
  • Gold (sodium aurothiomalate) - nitritoid reactions (facial flushing, nausea, vomiting, hypotension) reported rarely with concomitant injectable gold.
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Moderate Interactions

  • Diuretics (thiazide, loop) - enhanced hypotensive effect, especially with initial doses; may require lower initial lisinopril dose.
  • Other antihypertensives - additive hypotensive effect.
  • Insulin and oral hypoglycemics - enhanced glucose-lowering effect, increased risk of hypoglycemia.
  • Tricyclic antidepressants, antipsychotics, anesthetics - enhanced hypotensive effect.
  • Sympathomimetics - may reduce antihypertensive effects of ACE inhibitors.
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Minor Interactions

  • Not available

Monitoring

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Baseline Monitoring

Blood Pressure (BP)

Rationale: To establish baseline and guide initial dosing.

Timing: Prior to initiation

Serum Creatinine (SCr) and Blood Urea Nitrogen (BUN)

Rationale: To assess baseline renal function, as lisinopril is renally eliminated and can affect renal function.

Timing: Prior to initiation

Serum Potassium (K+)

Rationale: To assess baseline potassium levels, as lisinopril can cause hyperkalemia.

Timing: Prior to initiation

Urine Protein (if indicated)

Rationale: To assess for pre-existing renal disease, especially in diabetic or hypertensive patients.

Timing: Prior to initiation

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Routine Monitoring

Blood Pressure (BP)

Frequency: Regularly, especially after dose changes and during maintenance therapy (e.g., weekly for first few weeks, then monthly/quarterly)

Target: <130/80 mmHg (or individualized target)

Action Threshold: Persistent hypotension (<90/60 mmHg) or uncontrolled hypertension (>140/90 mmHg)

Serum Creatinine (SCr) and BUN

Frequency: Within 1-2 weeks of initiation or dose increase, then periodically (e.g., every 3-6 months) or as clinically indicated.

Target: Stable or within acceptable limits (e.g., <30% increase from baseline)

Action Threshold: Significant increase (>30% from baseline or >2.5 mg/dL), especially if accompanied by hyperkalemia.

Serum Potassium (K+)

Frequency: Within 1-2 weeks of initiation or dose increase, then periodically (e.g., every 3-6 months) or as clinically indicated, especially in patients with renal impairment, diabetes, or on potassium-sparing diuretics.

Target: 3.5-5.0 mEq/L

Action Threshold: >5.5 mEq/L

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Symptom Monitoring

  • Persistent dry cough
  • Swelling of face, lips, tongue, or throat (angioedema)
  • Dizziness or lightheadedness (especially upon standing)
  • Fatigue
  • Muscle weakness or irregular heartbeat (signs of hyperkalemia)
  • Signs of infection (fever, sore throat) - rare, but can indicate neutropenia

Special Patient Groups

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Pregnancy

Lisinopril is contraindicated in the second and third trimesters of pregnancy due to significant risk of fetal injury and death (e.g., fetal hypotension, anuria, renal failure, skull hypoplasia, death). Use in the first trimester is generally avoided due to potential, though less defined, risks. If pregnancy is detected, discontinue as soon as possible.

Trimester-Specific Risks:

First Trimester: Limited human data, but potential for major congenital malformations cannot be excluded. Generally avoided.
Second Trimester: High risk of fetal renal dysfunction, oligohydramnios, fetal lung hypoplasia, skeletal deformations, and death.
Third Trimester: High risk of fetal renal dysfunction, oligohydramnios, fetal lung hypoplasia, skeletal deformations, and death.
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Lactation

Lisinopril is excreted in human milk in very small amounts. The risk to a breastfed infant appears to be low, especially if the infant is older than 2 months. However, caution is advised, and monitoring the infant for hypotension is recommended. Consider alternatives, especially for preterm or neonates.

Infant Risk: L3 (Moderately Safe - limited data, potential for minor, non-serious adverse effects or no effects)
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Pediatric Use

Approved for hypertension in children 6 years and older. Dosing is weight-based. Safety and efficacy in children younger than 6 years or for indications other than hypertension have not been established. Close monitoring for blood pressure and renal function is crucial.

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Geriatric Use

No overall differences in effectiveness or safety have been observed between elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Start with lower doses (e.g., 2.5-5 mg) and titrate slowly, especially if renal function is impaired, due to increased risk of hypotension and renal adverse effects.

Clinical Information

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Clinical Pearls

  • First-dose hypotension can occur, especially in volume-depleted patients (e.g., those on diuretics, heart failure patients). Consider discontinuing diuretics 2-3 days prior to initiation or starting with a very low dose.
  • Dry, persistent cough is a common side effect (up to 20%) and is a class effect of ACE inhibitors. It typically resolves within 1-4 weeks after discontinuation.
  • Angioedema is a rare but life-threatening side effect. Patients should be educated on symptoms and advised to seek immediate medical attention if it occurs. Higher risk in Black patients.
  • Monitor potassium levels, especially in patients with renal impairment, diabetes, or those taking potassium-sparing diuretics or supplements.
  • Lisinopril is not a prodrug; it is active as administered, unlike enalapril or ramipril which are prodrugs.
  • Renal function should be monitored, especially in patients with pre-existing renal disease, heart failure, or bilateral renal artery stenosis, as ACE inhibitors can cause acute renal failure in these populations.
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Alternative Therapies

  • Angiotensin Receptor Blockers (ARBs) e.g., Valsartan, Losartan (often used if ACE inhibitor cough occurs)
  • Calcium Channel Blockers (CCBs) e.g., Amlodipine, Nifedipine
  • Thiazide Diuretics e.g., Hydrochlorothiazide, Chlorthalidone
  • Beta-blockers e.g., Metoprolol, Carvedilol
  • Direct Renin Inhibitors e.g., Aliskiren (limited use)
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Cost & Coverage

Average Cost: $10 - $50 per 30 tablets (20mg)
Generic Available: Yes
Insurance Coverage: Tier 1 (Generic)
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General Drug Facts

If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.