Lisinopril - Uses, Dosage, Side Effects, and Drug Warnings

Overview:

Lisinopril belongs to the group of drugs called ACE inhibitors, which is used to treat high blood pressure. Sometimes, it is also used in the treatment of heart failure. It is available as an oral tablet and solution. Lisinopril reduces blood pressure by relaxing the blood vessels. Avoid taking this medicine before or after 36 hours of using Sacubitril and do not use this with any medicine containing Aliskiren. If the patient experiences any persistent adverse effects after initiating the therapy, seek immediate medical help.

For Patients:

What Is Lisinopril Used For?

Lisinopril is used alone or in combination with medicines to treat hypertension. High blood pressure can affect the heart and arteries, which in the long run, impairs their function. This damage to the blood vessels of the brain, heart, and kidneys, can result in stroke, heart failure, or kidney failure. Thus, using this medicine will reduce the risk of cardiovascular diseases.

It can also be used to treat heart failure, and in some patients after a heart attack. Some of the heart muscles are damaged and weakened after a heart attack, which makes it difficult for the heart to pump blood. Lisinopril is given for individuals with low heart function in order to preserve, improve or slow the progression of the disease.

How Does Lisinopril Work?

In the renin-angiotensin-aldosterone system (RAAS), Lisinopril blocks the actions of angiotensin-converting enzyme (ACE), which prevents the conversion of angiotensin I to angiotensin II. This affects the adrenal cortex, which prevents the release of aldosterone. This action makes the kidney excrete sodium and retain potassium ions. This inhibition of the RAAS system lowers blood pressure and increases the supply of blood and oxygen to the heart.

What Is the Dosage of Lisinopril?

Lisinopril is available in 2.5, 5, 10, 20, 30, and 40 mg strengths.

• The dosage for high blood pressure is 20 to 40 mg taken once per day, up to 80 mg taken once per day.

• The dosage for heart failure is 5 mg orally once per day, up to 40 mg taken once per day.

• The dosage after a heart attack is 5 mg orally within the first 24 hours. Then if needed, another 5 mg after 24 hours. After this, 10 mg once per day for a minimum of 6 weeks.

How Is Lisinopril Taken?

It should be taken as prescribed by the doctor, and follow the instructions on the prescription label. Depending on how the patient reacts to the drug, the doctor might alter the doses. It can be taken with or without food. The solution form should be measured properly with a dose-measuring spoon or medicine cup. The patient's blood pressure, kidney function, and electrolytes need to be monitored regularly. Do not stop taking this medicine even after the blood pressure is under control, as it usually needs to be taken life long.

What Are the Precautions to Be Taken Before Using Lisinopril?

This drug should be avoided or taken under strict medical supervision if you have any of the following health conditions.

• History of angioedema.

• Prone to allergic reactions.

• Alcoholism.

• Kidney disease.

• Diabetes.

• Pregnant women.

• Trying to conceive.

• Breastfeeding.

• Children below 6 years of age.

What Are the Side Effects of Lisinopril?

The common side effects include:

• Lightheadedness.

• Headaches.

• Blurred vision.

• Sweating.

• Persistent cough.

• Hypotension.

• Chest pain

These side effects are usually mild and go away in some days. But if the symptoms are getting worse, get immediate medical help.

Some of the serious side effects include:

• Allergic reaction -

  • Face, lips, tongue, and throat swelling.

  • Breathing problems.

  • Inability to swallow.

  • Abdominal pain.

  • Nausea or vomiting.

• Kidney disease -

  • Fatigue.

  • Feet and ankles swelling.

  • Dyspnea.

• Liver disease -

  • Jaundice.

  • Abnormal liver enzymes.

  • Upper abdominal pain.

  • Nausea and vomiting.

  • Pale stools.

• Hyperkalemia (high potassium).

If the patient is profusely sweating or have vomiting or diarrhea while taking this medicine, the patient might get dehydrated, which increases the risk of hypotension and kidney failure.

What Are the Drugs That Lisinopril Can Interact With?

Lisinopril can interact with other medications the patient might be taking, which might change the way the drug works. This can make the drug not work properly or cause unwanted side effects. To prevent this, always inform the doctor about all the medicines, herbs, and supplements that the patient is currently taking. The drugs with which Lisinopril can interact are:

• Antihypertensive drugs -

  • Angiotensin receptor blockers (ARB) - Candesartan, Eprosartan, and Olmesartan.

  • Angiotensin-converting enzyme (ACE) inhibitors - Benazepril, Ramipril, and Captopril.

  • Renin-inhibitors - Aliskiren

• Anti-diabetic drugs - Insulin and oral anti-diabetic drugs.

• Diuretics - Hydrochlorothiazide and Furosemide.

• Potassium supplements.

• Potassium-sparing diuretics - Spironolactone and Amiloride.

• Lithium.

• Nonsteroidal anti-inflammatory drugs (NSAIDs) - Ibuprofen and Naproxen.

• Neprilysin inhibitors - Sacubitril.

Lisinopril is used for long-term treatment of hypertension. This drug if not taken as prescribed can cause serious side effects. If the patient stops taking it abruptly, the blood pressure might rise, which can increase the heart rate, cause sweating and anxiety. Taking it irregularly will not help control blood pressure, which puts the patient at higher risk for heart attack and stroke.

The doctor will monitor the blood pressure regularly and look out for any side effects. To know other ways to treat hypertension, consult a doctor online.

How to Store Lisinopril?

• Keep the formulations of the medication away from the reach of pets and children.

• After the expiration date listed on the tube and carton, do not use this medication. The last day of that month is referred to as the expiry date.

• Store no longer than 25 degrees Celsius.

• Avoid freezing the medication.

• Never dispose of medications in wastewater or household garbage. Find out from the pharmacist how to dispose of expired medications. These actions will aid in environmental protection.

Avoid Self-Medication:

Avoid taking this drug without the proper directions from a pharmacist or doctor. Avoid recommending the medication to others, and do not take it on someone else's advice. Different people react to medications differently, and some may even react worse. Hence, follow the directions provided by the healthcare professional for drug use.

For Doctors:

Indication

• Hypertension.

• Acute myocardial infarction.

• Adjunct therapy in heart failure.

Non- FDA Labelled Indications:

• Prophylaxis of migraine.
• Nondiabetic kidney disease.
• Diabetic nephropathy.

Dosing:

The general dosing information is as follows:

Dosing Considerations:

Renal Impairment:

• Creatinine clearance (CrCl) greater than 30 mL/min: No dosing adjustment required.

• CrCl 10 mL/min to 30 mL/min for hypertension: Therapy is preferable to be initiated at 5 mg orally once daily.

• CrCl less than 10 mL/min: The dosage should be reduced to 2.5 mg orally once daily.

Hepatic Impairment:

• No specific dosing recommendations are indicated for patients with hepatic impairment.

Hepatic Failure:

• If jaundice or noticeably elevated liver enzymes occur, discontinue the medication.

Pregnancy:

• Avoid use during pregnancy.

Monitoring Parameters:

Hypertension: Blood pressure response should be monitored carefully in patients with stage 2 hypertension and a BP of 160/100 mm Hg or higher. BP response should be monitored at monthly intervals until control is achieved in patients starting or adjusting antihypertensive medication and every three to six months in patients who have met BP goals. Especially in patients who are at risk, for orthostatic hypotension, like those older or with postural symptoms.

Serum Potassium: Periodic monitoring is recommended, especially in patients at risk for hyperkalemia, such as those with renal insufficiency, diabetes mellitus, concurrent use of potassium-sparing diuretics, potassium supplements, potassium-containing salt substitutes, or other medications that could raise serum potassium levels.

Pharmacology

Mechanism of Action:

Lisinopril acts by inhibiting angiotensin-converting enzyme inhibitors (ACEI). This stops the growth of vascular smooth muscle cells and myocyte hypertrophy, both of which are symptoms of untreated patients. For individuals using ACEIs, elevated bradykinin levels also have vasodilating effects. Additionally, Lisinopril prevents renin from converting angiotensin to angiotensin I.

Under normal circumstances, angiotensin II would increase vascular resistance and oxygen consumption because it constricts coronary blood arteries and is positively inotropic. Myocyte enlargement and the proliferation of vascular smooth muscle cells may eventually result from this action.

Pharmacodynamics:

Angiotensin-converting enzyme inhibitors like Lisinopril are used to treat heart disease, hypertension, and myocardial infarction. Since it is not a prodrug, Lisinopril works by inhibiting the renin-angiotensin-aldosterone system as well as the angiotensin-converting enzyme. Given to patients at a dosage of typically 10 to 80 mg per day, it has a broad therapeutic index and a longer duration of action.

Pharmacokinetics:

Absorption:

Lisinopril has 6 to 60 percent bioavailability based on intersubject variability. The time to attain maximum drug concentration (Tmax) is achieved within seven hours for adults and six hours for children and adolescents. The absorption is unaffected by food.

Distribution:

Lisinopril has considerable protein binding. The volume of distribution is 124 L.

Metabolism:

Lisinopril does not undergo any metabolism and is excreted in its unchanged form in the urine.

Excretion:

Lisinopril is completely excreted via the renal route. The total body clearance of the drug is 15L/hr and 10 L/hr in children less than or equal to 30 kilograms.

Toxicity

Non-clinical Toxicity:

Lisinopril has not been associated with carcinogenicity, tumorigenicity, or impairment in fertility, as documented in animal studies.

Clinical Toxicity:

Mild to Moderate Toxicity:

Patients may experience hypotension.

Management: Most patients will have no symptoms, but patients with mild orthostatic hypotension can be treated by remaining prone. Those who remain hypotensive can be treated with IV fluids.

Severe Toxicity:

Symptoms of severe toxicity, severe hypotension, syncope, hyperkalemia, renal failure, and bradycardia.

Management: If a patient exhibits circulatory collapse, adequate circulatory support should be ensured using IV fluids and vasopressors (if required). Correct severe hyperkalemia utilizing common therapies such as hemodialysis, calcium, sodium bicarbonate, sodium polystyrene sulfate, glucose, Insulin, and calcium.

Warnings and Precautions:

Angioedema:

• Angioedema of the face, glottis, tongue, lips, or larynx, including fatalities, have been reported.

• Patients are at increased risk of angioedema if there is a prior experience of angioedema and with concurrent use of ACE inhibitors and mammalian target of rapamycin (mTOR) inhibitors or neprilysin inhibitors; discontinuation and monitoring are recommended.

Cardiovascular:

• Hemodynamically unstable following an acute myocardial infarction; use with caution due to the possibility of critically low blood pressure. Monitoring is advised because acute myocardial infarction raises the risk of renal failure or enduring hypotension.

• Patients with heart failure are more likely to experience extreme hypotension, which is occasionally linked to oliguria, progressive azotemia, acute renal failure, and death; monitoring is advised in these patients, especially if their systolic blood pressure is below 100 mmHg. Ischemia of the heart; elevated risk of severe hypotension; monitoring advised.

• Symptomatic hypotension may occur in people with aortic stenosis or hypertrophic cardiomyopathy.

• The risk of extreme hypotension is increased by high-dose diuretic therapy, an increase in diuretic dose, or substantial volume or salt loss caused by intensive diuresis or renal dialysis; monitoring is advised.

Concomitant Use:

• Aliskiren should not be used concurrently in patients with a glomerular filtration rate (GFR) of less than 60 mL/min.

Endocrine and Metabolic:

• Monitoring is advised as hyponatremia raises the risk of extreme hypotension.

• There have been reports of hyperkalemia; it is advised to monitor individuals with renal impairment, diabetes mellitus or who are concurrently using potassium-sparing diuretics, potassium supplements, potassium-containing salt substitutes, or other medications that may raise serum potassium.

Gastrointestinal:

• Patients using ACE inhibitors without a history of facial angioedema and with normal C-1 esterase levels have been reported with the development of intestinal angioedema.

Hepatic:

• Hepatic syndrome starts as cholestatic jaundice or hepatitis and progresses to fulminant hepatitis, and sometimes death has been associated with ACE inhibitors; discontinue if jaundice or markedly elevated hepatic enzymes occur.

Neurologic:

• Monitoring is advised since cerebral vascular dysfunction raises the risk of extreme hypotension.

Renal:

• Patients who have renal artery stenosis, severe congestive heart failure, chronic kidney disease, volume depletion, or post-myocardial infarction are at an increased risk of developing acute renal failure; medication may need to be stopped or adjusted.

• Anaphylactoid reactions have been documented in individuals receiving hemodialysis with high-flux membranes; if reactions happen, consider alternative therapies.

Reproductive:

• When pregnancy is confirmed, discontinue the drug as soon as possible to avoid fetal toxicity, especially during the second and third trimesters.

Contraindications:

Lisinopril should be strictly avoided in the following conditions:

• Known allergy to the drug or its components.

• If on therapy with Aliskiren in diabetic patients.

• Hereditary angioedema (swelling under the skin).

• If on active therapy with the drug Sacubitril.

Adverse Effects:

The common adverse effects include

• Hypotension.

• Syncope.

• Dizziness.

• Headache.

• Cough.

Dose-related adverse effects include

• Gastrointestinal: Pancreatitis, constipation, gas, dry mouth, and diarrhea are digestive symptoms.

• Hematologic: Infrequent episodes of leukopenia or neutropenia, thrombocytopenia, hemolytic anemia, and bone marrow depression.

• Endocrine: Excessive antidiuretic hormone secretion and diabetes mellitus.

• Dermatological: Photosensitivity, flushing, erythema, diaphoresis, alopecia, toxic epidermal necrolysis, and urticaria.

• Immunological: Stevens-Johnson syndrome, pruritus, and necrosis.

• Ophthalmic: Visual loss, diplopia, hazy vision, tinnitus, photophobia, taste disturbances, and smell disturbance are examples of special senses.

• Other: A symptom complex that may include an ANA (antinuclear antibody) positive result, an elevated erythrocyte sedimentation rate (ESR), arthralgia, fever, eosinophilia, vasculitis, leukocytosis, paresthesia, and vertigo has been observed. Rash, photosensitivity, or other dermatological manifestations could appear by themselves or in conjunction with these signs.

Clinical Studies:

The following observations were made from different clinical studies of Lisinopril

• Patients with hypertension who were treated with lisinopril had a significant reduction in systolic and diastolic blood pressure compared to those who received a placebo.
• Lisinopril has also shown to reduce the risk of cardiovascular events, such as heart attack and stroke, in patients with hypertension.
• In a clinical trial, Lisinopril showed superior reductions of systolic and diastolic blood pressure compared to Hydrochlorothiazide in a population that was 75 percent Caucasian. It had similar blood pressure reductions and adverse effects in younger and older patients. It was less effective in reducing blood pressure in Blacks than in Caucasians.

Drug Interactions:

Medications tend to interact with other drugs, food, supplements, or beverages, resulting in unwanted side effects.

The common interactions of Lisinopril are listed below:

1. With Other Drugs:

• Alteplase.

• Amiloride.

• Azathioprine.

• Azilsartan.

• Azilsartan Medoxomil.

• Candesartan.

• Canrenoate.

• Eprosartan.

• Everolimus.

• Irbesartan.

• Lithium.

• Losartan.

• Mercaptopurine.

• Olmesartan.

• Potassium.

• Potassium Citrate.

• Potassium Phosphate.

• Sirolimus.

• Telmisartan.

• Triamterene.

• Trimethoprim.

• Valsartan.

This list does not include all the drug interactions. Check with the pharmacist or doctor before taking the medication.

2. With Alcohol: Alcohol can increase the effect of Lisinopril and can result in side effects like dizziness, lightheadedness, etc. Hence, the consumption of alcohol is not recommended.

3. With Food: Avoid using food rich in potassium, sodium, calcium, and magnesium, as it can cause irregular heartbeats.

Other Specifications:

Lisinopril in Pregnant Women:

Lisinopril is a pregnancy Category D drug. Avoid use in pregnancy due to the potential risk of fetal toxicity.

Lisinopril in Lactating Women:

No data is available on the passage of Lisinopril into breast milk. The administration should comply with benefits vs. risks for the mother.

Lisinopril in Pediatrics:

Lisinopril is indicated for the use of pediatric hypertension from six years of age. The safety and efficacy of the drug in children less than six years are not yet known.

Lisinopril in Geriatrics:

No specific dosage adjustments are required for Lisinopril in geriatric patients. There were no significant differences in the safety and efficacy of the drug compared to adults.