Zestril 5mg 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 available
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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 medicine used to treat high blood pressure and heart failure. It works by relaxing your blood vessels, which helps lower your blood pressure and makes it easier for your heart to pump blood. It can also be used after a heart attack to improve heart function.
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How to Use This Medicine

Taking Your Medication

To get the most benefit from your medication, follow these guidelines:

Take your medication exactly as directed by your doctor. Read all the information provided with your prescription and follow the instructions carefully.
You can take this medication with or without food.
Take your medication at the same time every day to establish a routine.
Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Drink plenty of non-caffeinated fluids, unless your doctor advises you to limit your fluid intake.

Special Instructions for Liquid Suspension

If you have trouble swallowing pills, your doctor or pharmacist can help you prepare a liquid suspension. If a liquid suspension is prepared:

Shake the suspension well before each use.
Measure your dose carefully using the measuring device provided with the medication. If no device is included, ask your pharmacist for a suitable measuring device.

Storing and Disposing of Your Medication

To maintain the effectiveness and safety of your medication:

Store it at room temperature in a dry place, away from the bathroom.
Keep the lid tightly closed.
Do not freeze your 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 continue with 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 increase the blood pressure-lowering effect.
  • Maintain a healthy diet (low sodium, low fat), regular exercise, and manage stress to support blood pressure control.
  • Report any swelling of the face, lips, tongue, or throat immediately to your doctor.

Dosing & Administration

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Adult Dosing

Standard Dose: Hypertension: 10 mg once daily; Heart Failure: 2.5-5 mg once daily; Acute MI: 5 mg initial dose, then 5 mg after 12 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.
Heart Failure: Initial: 2.5-5 mg once daily. Titrate up to 20-40 mg once daily.
Acute Myocardial Infarction: Initial: 5 mg (within 24 hours of symptom onset), then 5 mg after 12 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 (up to 5 mg) once daily. Max: 0.6 mg/kg or 40 mg/day.
Adolescent: Hypertension: Initial 0.07 mg/kg (up to 5 mg) once daily. 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.
Moderate: CrCl 10-30 mL/min: Hypertension/Heart Failure: Initial 2.5 mg once daily. Acute MI: Initial 2.5 mg.
Severe: CrCl < 10 mL/min (including dialysis patients): Hypertension/Heart Failure: Initial 2.5 mg once daily. Acute MI: Initial 2.5 mg.
Dialysis: Lisinopril is dialyzable. Administer dose after dialysis. Initial 2.5 mg once daily for patients on dialysis.

Hepatic Impairment:

Mild: No specific adjustment recommended, but use with caution.
Moderate: No specific adjustment recommended, but use with caution.
Severe: No specific adjustment recommended, but use with caution. Lisinopril is not metabolized by the liver.

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 leads to decreased angiotensin II levels, resulting in vasodilation, reduced aldosterone secretion (leading to decreased sodium and water reabsorption), and increased bradykinin levels (a vasodilator). These actions collectively reduce peripheral vascular resistance, blood pressure, and cardiac preload and afterload.
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Pharmacokinetics

Absorption:

Bioavailability: 25-30% (variable, dose-dependent)
Tmax: 6-8 hours
FoodEffect: Food does not affect the absorption of lisinopril.

Distribution:

Vd: Not extensively distributed into tissues (approximately 120 L)
ProteinBinding: Approximately 25%
CnssPenetration: Limited

Elimination:

HalfLife: Approximately 12 hours (effective accumulation half-life)
Clearance: Renal clearance is approximately 50 mL/min
ExcretionRoute: Urine
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

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 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 indicated by:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Stomach pain or upset
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes (jaundice)

Other Possible Side Effects

Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor for guidance:

Dizziness or headache
* Cough

Reporting Side Effects

This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, 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:

  • Swelling of the face, lips, tongue, or throat (angioedema) - seek emergency medical attention.
  • Severe dizziness or fainting (especially with the first dose or dose increases).
  • Persistent dry cough.
  • Signs of high potassium (muscle weakness, slow or irregular heartbeat).
  • Signs of kidney problems (decreased urination, swelling in ankles/feet, unusual tiredness).
  • Signs of liver problems (yellowing of skin/eyes, dark urine, persistent nausea/vomiting).
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Before Using This Medicine

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

It is essential to inform your doctor about the following conditions to ensure safe treatment:

Any allergies you have, including allergies to this medication, its components, or other substances. Describe the allergic reactions you have experienced, including any symptoms.
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 problems, or unusual hoarseness.
Kidney problems, as they may affect how your body processes this medication.
If you are taking a medication containing aliskiren, particularly if you have diabetes or kidney problems.
If you have taken a medication containing sacubitril within the last 36 hours.
If you are breastfeeding, as you should not breastfeed while taking this medication.

Special Considerations for Children:
* This medication is not recommended for children under 6 years of age. Do not administer this medication to a child younger than 6 years old.

Additional Important Information:
This list is not exhaustive, and it is crucial 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 have. This will help ensure that it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without consulting your doctor.
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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 understand how this medication affects you, avoid driving and other tasks that require alertness. To minimize the risk of dizziness or fainting, rise slowly from a sitting or lying position, and exercise caution 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 work, 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 prevent dehydration.
Inform your doctor if you experience excessive sweating, fluid loss, vomiting, or diarrhea, as these may lead to low blood pressure.

Racial Considerations
This medication may be less effective in lowering blood pressure in Black patients. In some cases, an additional medication may be necessary. If you have questions or concerns, discuss them with your doctor. Additionally, the risk of angioedema, a severe and potentially life-threatening reaction, may be higher in Black patients.

Infection Risk
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. If you experience symptoms of infection, such as fever, chills, or sore throat, contact your doctor immediately.

Age-Related Precautions
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 (low blood pressure)
  • Dizziness
  • Lightheadedness
  • Fainting
  • Tachycardia (rapid heart rate)
  • Palpitations
  • Renal failure

What to Do:

Call 1-800-222-1222 (Poison Control Center) or seek emergency medical attention immediately. Treatment is supportive, including intravenous fluid administration to restore blood pressure. Lisinopril can be removed by hemodialysis.

Drug Interactions

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Contraindicated Interactions

  • Aliskiren (in patients with diabetes or renal impairment)
  • Sacubitril/Valsartan (Entresto) - concomitant use or within 36 hours of switching
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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 (Nonsteroidal Anti-inflammatory Drugs) - may reduce antihypertensive effect and increase risk of renal impairment
  • Lithium - increased serum lithium levels and toxicity
  • mTOR inhibitors (e.g., sirolimus, everolimus, temsirolimus) - increased risk of angioedema
  • Gold (parenteral) - nitritoid reactions (facial flushing, nausea, vomiting, hypotension) reported rarely
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Moderate Interactions

  • Diuretics (thiazide or loop) - increased risk of symptomatic hypotension (especially first-dose)
  • Other antihypertensives - additive hypotensive effects
  • Antidiabetic agents (insulin, oral hypoglycemics) - increased risk of hypoglycemia
  • Corticosteroids - may reduce antihypertensive effect
  • Tricyclic antidepressants, antipsychotics - may enhance hypotensive effect
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Minor Interactions

  • Alcohol - may enhance hypotensive effect

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 ACE inhibitors can cause hyperkalemia.

Timing: Prior to initiation

Liver Function Tests (LFTs)

Rationale: Although not hepatically metabolized, rare cases of hepatic failure have been reported.

Timing: Prior to initiation (if clinically indicated)

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Routine Monitoring

Blood Pressure (BP)

Frequency: Regularly, especially after dose changes, then periodically (e.g., monthly, then every 3-6 months)

Target: <130/80 mmHg (individualized based on guidelines and patient comorbidities)

Action Threshold: Persistent hypotension (e.g., systolic <90 mmHg) or inadequate BP control

Serum Creatinine (SCr) and Blood Urea Nitrogen (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 in SCr (>30% from baseline or >2.5 mg/dL), especially if associated with 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)

Target: 3.5-5.0 mEq/L

Action Threshold: Hyperkalemia (>5.5 mEq/L) or hypokalemia (<3.5 mEq/L)

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Symptom Monitoring

  • Signs of angioedema (swelling of face, lips, tongue, glottis, larynx)
  • Persistent dry cough
  • Dizziness or lightheadedness (especially with first dose or dose increases)
  • Fatigue or weakness
  • Signs of infection (fever, sore throat) due to rare neutropenia
  • Signs of jaundice or unexplained elevations of liver enzymes

Special Patient Groups

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Pregnancy

Contraindicated in the second and third trimesters of pregnancy due to risk of fetal injury and death. Discontinue as soon as pregnancy is detected. First-trimester exposure risk is less clear but generally avoided.

Trimester-Specific Risks:

First Trimester: Potential risk, but less established than later trimesters. Generally avoided if possible.
Second Trimester: High risk of fetal injury (e.g., renal dysfunction, oligohydramnios, skull hypoplasia, lung hypoplasia, skeletal deformations) and death.
Third Trimester: High risk of fetal injury (e.g., renal dysfunction, oligohydramnios, skull hypoplasia, lung hypoplasia, skeletal deformations) and death.
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Lactation

Lisinopril is excreted in human milk in very low concentrations. Generally considered compatible with breastfeeding, especially for full-term, healthy infants. Monitor infant for hypotension.

Infant Risk: Low risk
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Pediatric Use

Approved for hypertension in children 6 years and older. Dosing is weight-based. Safety and efficacy not established in children younger than 6 years or for indications other than hypertension.

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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 mg) and titrate slowly, especially if renal function is impaired.

Clinical Information

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Clinical Pearls

  • Lisinopril is a non-prodrug ACE inhibitor, meaning it is active as administered and does not require hepatic metabolism for activation.
  • The most common side effect is a persistent, dry cough, which occurs in 5-20% of patients and often leads to discontinuation. It is a class effect of ACE inhibitors.
  • First-dose hypotension can occur, especially in patients who are volume-depleted (e.g., on diuretics, heart failure patients). Consider discontinuing diuretics 2-3 days prior to initiation if possible, or starting with a very low dose.
  • Angioedema is a rare but potentially life-threatening side effect. Patients should be educated on symptoms and to seek immediate medical attention if it occurs. It can occur at any time during therapy, even after prolonged use.
  • Monitor renal function and potassium levels regularly, especially in patients with pre-existing renal impairment, diabetes, or those on potassium-sparing diuretics or supplements.
  • Lisinopril is dialyzable, which is important for dosing in patients on hemodialysis.
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Alternative Therapies

  • Other ACE Inhibitors (e.g., enalapril, ramipril, captopril)
  • Angiotensin Receptor Blockers (ARBs) (e.g., valsartan, losartan, candesartan)
  • Calcium Channel Blockers (CCBs) (e.g., amlodipine, nifedipine, diltiazem)
  • 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 - $30 per 30 tablets (5mg generic)
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 for further guidance. 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 for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.