Lisinopril

Lisinopril is a medicine that belongs to the class of angiotensin-converting enzyme inhibitors (ACEIs). It is used to treat hypertension (high blood pressure), heart failure and to prevent complications after myocardial infarction.

Lisinopril works by dilating blood vessels, which helps lower blood pressure and improve heart function. It is usually taken in tablet form, usually once a day. Like any medicine, lisinopril has side effects and should be taken under a doctor's supervision.

Before you start using lisinopril or any other medication, it is important to discuss this with your doctor to get the best advice and dosage given your individual health conditions.

Indications Lisinopril

1. Hypertension (high blood pressure): Lisinopril helps lower blood pressure by preventing vasoconstriction and improving blood flow.
2. Heart Failure: Lisinopril may help improve heart function in patients with heart failure by reducing the workload on the heart and improving its contractility.
3. Preventing Complications After myocardial infarction: Lisinopril may be prescribed after myocardial infarction to prevent further cardiovascular complications.

Release form

Lisinopril is available in the following dosage forms:

• Tablets: The most common form of release. Lisinopril tablets may contain different amounts of active substance - usually from 2.5 mg to 40 mg. Tablets may be coated or uncoated and are intended for oral administration. Sometimes the tablets may be designed to be chewed or have a release for easy dosing.

Lisinopril does not have a wide range of release forms, such as syrups or injections, due to its specificity of action and mechanism of absorption in the body. Tablet form provides convenience of administration, accuracy of dosage and is an appropriate way to deliver the active substance for the treatment of diseases on which lisinopril has therapeutic effect.

Pharmacodynamics

1. ACE inhibition: Lisinopril inhibits angiotensin-converting enzyme, which converts angiotensin I into active angiotensin II. Angiotensin II is a potent vasoconstrictor and stimulates the secretion of aldosterone, which leads to an increase in blood pressure. ACE inhibition reduces the level of angiotensin II, which leads to vasodilation and lower blood pressure.
2. Reduction of cardiac preload and afterload: Lisinopril reduces vascular resistance, which leads to a reduction in cardiac afterload. It also reduces reabsorption of sodium and water in the kidneys, which together with the reduction of vascular resistance reduces cardiac preload.
3. Antiremodeling action: Lisinopril helps to reduce remodeling of heart and vessels, which means preservation of their structure and function in various pathological conditions, such as heart failure and after myocardial infarction.
4. Protective effects on the kidneys: By lowering blood pressure and remodeling blood vessels, lisinopril may also protect the kidneys from damage associated with arterial hypertension.
5. Antimicrobial action: In some cases lisinopril may have antimicrobial properties due to modulation of the immune system.
6. Anti-atherosclerotic effect: There is evidence that lisinopril may have a protective effect on the vascular wall, which helps slow the development of atherosclerosis.

Pharmacokinetics

1. Absorption: Lisinopril is usually well absorbed from the gastrointestinal tract after oral administration. Most dosage forms of lisinopril have high bioavailability, which means that most of the dose taken enters the bloodstream.
2. Maximum concentration(Cmax): The maximum plasma concentration of lisinopril is usually reached about 6-8 hours after taking the drug.
3. Bioavailability: Bioavailability of lisinopril when taken orally is about 25%, because a significant part of the drug is metabolized during the first passage through the liver.
4. Metabolism: Lisinopril is metabolized in the liver to form the active metabolite, lisinoprilate.
5. Half-life (T1/2): Lisinopril has a relatively long half-life of about 12 hours. This means that the drug is usually taken once a day.
6. Excretion: Lisinopril and its metabolites are eliminated from the body mainly through the kidneys.
7. Protein binding: Approximately 25% of lisinopril binds to plasma proteins.
8. Effect of food: Food does not significantly affect the pharmacokinetics of lisinopril, so it can be taken regardless of food intake.

Dosing and administration

The following are general guidelines for the use of Lisinopril, but you should always follow your doctor's instructions.

Hypertension (High Blood Pressure)

• Thestarting dose is usually 10 mg once daily.
• Themaintenance dose may vary from 20 to 40 mg per day, depending on the patient's response to treatment. In some cases, the doctor may recommend a slow increase in dose.

Heart failure

• Thestarting dose for patients with heart failure is usually 2.5-5 mg once daily.
• Themaintenance dose may be gradually increased by the physician to the maximum recommended dose of 35-40 mg per day, depending on the patient's tolerance to the drug.

After a myocardial infarction

• Early initiation of treatment (within 24 hours of infarction) usually starts with 5 mg, followed by 5 mg after 24 hours, 10 mg after 48 hours and then 10 mg once daily.
• Patients with low blood pressure may have a lower starting dose.

General recommendations

• Lisinopril is taken once a day, preferably at the same time each day.
• Can be taken with or without food.
• It is important to drink enough fluids throughout the day during treatment with Lisinopril.
• Blood pressure should be monitored regularly to monitor the effectiveness of treatment.

It's important to remember

• Do not stop taking Lisinopril without consulting your doctor, even if you feel an improvement.
• When changing the dose, the body's reaction should be carefully monitored.
• Inform your doctor of all medications you are taking, including over-the-counter medications and dietary supplements, as there is a risk of interaction with Lisinopril.
• Alcohol should be avoided and caution should be taken when driving or operating heavy machinery until your reaction to Lisinopril is known.

Use Lisinopril during pregnancy

The use of lisinopril during pregnancy is strongly discouraged. Drugs in the class of ACE inhibitors, such as lisinopril, may cause serious birth defects in the fetus, especially when used in the second and third trimesters of pregnancy. These defects may include hypoplastia (underdevelopment) of the lungs, underdevelopment of the skull, delayed fetal growth and development, and other problems.

Contraindications

1. Hypersensitivity: Patients with known hypersensitivity to lisinopril or any other angiotensin-converting enzyme inhibitors (ACEIs) should not use this drug because of the risk of allergic reactions.
2. True arterial hypotension: Lisinopril may cause a decrease in blood pressure, so it should be used with caution in patients with true arterial hypotension (excessively low blood pressure) to avoid the development of hypotensive reactions.
3. Renal artery stenosis: Lisinopril should be used with caution in patients with renal artery stenosis as it may worsen renal function.
4. Pregnancy: The use of lisinopril during pregnancy may cause serious fetal damage, including malformations, delayed lung development, hypoplastic bladder and even fetal death. Therefore, lisinopril is contraindicated during pregnancy.
5. Breastfeeding: Lisinopril is excreted into breast milk and may have an adverse effect on the infant, therefore, discontinuation of breastfeeding may be necessary while taking the drug.
6. Angioedema: Lisinopril may cause angioedema, especially in patients with a previous history of such reactions.
7. Hyperkalemia: The use of lisinopril may lead to an increase in blood potassium levels, therefore it should be used with caution in patients with hyperkalemia.
8. Children: The safety and efficacy of lisinopril in young children have not been established; therefore, its use in this age group may be limited.

Side effects Lisinopril

1. Hypotension (decreased blood pressure), which may manifest as dizziness or feelings of weakness.
2. A cough that can be dry and irritating. This cough is often called a medicinal cough.
3. Headache.
4. Fatigue or weakness.
5. Drowsiness.
6. Hyperkalemia (elevated blood potassium levels), especially in people with impaired kidney function.
7. Elevation of urea and creatinine levels in the blood.
8. Swelling, especially in the face, lips, tongue, or larynx, which may be a sign of angioedema.
9. Changes in taste sensation.
10. Rarely, more serious side effects such as angioedema, agranulocytosis (decreased white blood cell count), and skin reactions such as hives or rashes may occur.

Overdose

1. Severe decrease in blood pressure: An overdose of lisinopril may cause a sharp drop in blood pressure, which may lead to fainting, dizziness, weakness and even loss of consciousness.
2. Electrolyte disturbances: Excessive effect of lisinopril on the kidneys may lead to electrolyte imbalance in the body, which may result in heart rhythm disturbances, muscle cramps and other serious complications.
3. Renal insufficiency: Lisinopril overdose may cause acute renal failure due to its effect on renal function and blood pressure regulation.
4. Hyperkalemia: Hyperkalemia (increased potassium in the blood) may develop, which can be dangerous for the heart.
5. Other symptoms: Other symptoms of lisinopril overdose may include nausea, vomiting, insomnia, headache, and slow heartbeat.

Treatment of lisinopril overdose usually involves urgent measures to maintain vital functions, such as maintaining adequate circulation and respiratory function. This may include administration of intravenous fluids, administration of vasopressors and other measures. In addition, further treatment may be required to restore electrolyte balance and treat other complications.

Interactions with other drugs

Lisinopril may interact with various medications, which may affect their efficacy, safety, and/or pharmacokinetics. Here are some common interactions to be aware of:

1. Diuretics (diuretics): Combined use of lisinopril with diuretics may result in a severe drop in blood pressure. However, it may be useful in the treatment of hypertension and heart failure. It is important to monitor blood potassium levels.
2. Drugs that increase the level of potassium in the blood (potassium-saving diuretics, spironolactone, potassium-containing supplements): Combination of lisinopril with such drugs may lead to hyperkalemia (increased blood potassium level), especially in patients with kidney damage.
3. Drugs that reduce the level of potassium in the blood (non-steroidal anti-inflammatory drugs, glucocorticoids): Lisinopril may increase the effect of such drugs, which may lead to the development of hypokalemia (decrease in the level of potassium in the blood).
4. Drugs that increase blood pressure (e.g. Sympathomimetics): Lisinopril may weaken the effects of these drugs, which may result in poorer blood pressure control.
5. Drugs causing hypotension (anesthetics, narcotic analgesics): Combination with lisinopril may increase hypotensive effect and lead to excessive decrease in blood pressure.
6. Drugs that increase the risk of hyperkalemia (non-steroidal anti-inflammatory drugs, potassium supplements): Lisinopril may increase the risk of hyperkalemia when used concomitantly with such drugs.
7. Drugs that increase the risk of angioedema (e.g. Calcineurin inhibitors): Combination with lisinopril may increase the risk of developing angioedema.
8. Drugs affecting renal function: Lisinopril may increase the risk of renal damage when used concomitantly with other drugs affecting renal function.

Storage conditions

1. Temperature: Lisinopril should usually be stored at room temperature, which is usually 15°C to 30°C (59°F to 86°F). Avoid storing the drug in places with extreme temperatures.
2. Humidity: The drug should be stored in a dry place to prevent lumping or sticking of tablets.
3. Light: It is recommended to store lisinopril in a dark place protected from direct sunlight to prevent decomposition of the active ingredients by light.
4. Packaging: Store the drug in its original packaging or container to prevent unintentional access to it and to protect it from external factors.
5. Availability to children: Ensure that lisinopril is stored out of the reach of children to prevent accidental use.