Imidapril

Imidapril is an antihypertensive agent belonging to angiotensin-converting enzyme (ACE) inhibitors.

Imidapril is approved for the treatment of Hypertension (high blood pressure), the prevention of heart attack and, stroke, and Heart failure.

Imidapril is rapidly but incompletely absorbed from the gastrointestinal tract. Reduced absorption with high-fat meals. The bioavailability of imidapril is approx 70%; approx 42%. The Plasma protein binding: 85%. It is metabolized in the liver via hydrolysis to imidaprilat (active metabolite).It is excreted Via faeces (approx 50%); urine (approx 40%).

The more common side effect that can occur with Imidapril includes Mild and transient cough, tachycardia, bronchitis, headache, nausea, dizziness, diarrhea., etc.

Imidapril is available in the form of dosage forms as tablets

Imidapril is available in India, Europe, China, and Japan.

Imidapril, a prodrug of imidaprilat, is a competitive ACE inhibitor that prevents the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor responsible for arterial vasoconstriction, increased blood pressure, and stimulation of aldosterone secretion. This action leads to lower angiotensin II levels, thereby increasing plasma renin activity and reducing aldosterone secretion.

Imidapril works by blocking (inhibiting) a chemical called an angiotensin-converting enzyme. This widens the blood vessels and helps to reduce the amount of water put back into the blood by your kidneys. These actions help to decrease blood pressure.

The Duration of action of Imidapril in the body is 24 hours.

The Tmax was found within 2.0 h for imidapril and 9.3 h for imidaprilat following the administration of Imidapril, and Cmax was reached within 5.8-54.9 ng/mL.

Imidapril is available in the form of tablets.

Imidapril tablets are to be swallowed whole with water.

Imidapril is approved for the treatment of Hypertension (high blood pressure) prevention of heart attack and stroke and Heart failure.

Imidapril, a prodrug, is an angiotensin-converting enzyme (ACE) inhibitor. It undergoes rapid hydrolysis in the liver to imidaprilat, the active metabolite. Imidapril may decrease blood pressure by inhibiting ACE in the heart and kidney, particularly during chronic heart failure.

Imidapril is approved for use in the following clinical indication.

Mild to moderate Hypertension.

Imidapril is available in the form of tablets with potencies of 5 mg, 10 mg, and 20 mg.

Essential Hypertension

Adult: Initially, 5 mg once daily may be increased to 10 mg daily if optimum blood pressure control has not been achieved after at least three weeks of therapy. Max: 20 mg daily.

Elderly: Initially, 2.5 mg once daily may be titrated according to blood pressure response. Max: 10 mg daily.

Imidapril can be administered orally after meals. The dosage and the Duration of treatment should be as per the clinical judgment of the treating physician.

Imidapril is available in various dosage strengths as 5 mg, 10 mg, and 20 mg.

Imidapril is available in the form of tablets.

Imidapril is approved for the treatment of Hypertension (high blood pressure), prevention of heart attack and, stroke and Heart failure.

Hypertension: It has been observed that the low-salt Dietary Approach to Stop Hypertension (DASH) diet lowers blood pressure. Sometimes after a few weeks, its effects on blood pressure become noticeable.

The dietary restriction should be individualized as per patient requirements.

Imidapril may be contraindicated in the following.

Hypersensitivity to imidapril and other ACE-Inhibitors. Angioedema. Severe renal impairment (creatinine clearance below 10ml/min) and patient on hemodialysis. Paediatric: Contraindicated. Pregnancy: Contraindicated. Lactation: Contraindicated. Elderly: Reduced the dose.

The treating physician must closely monitor the patient and keep pharmacovigilance as follows.

• Caution should be exercised in patients with a history of obstruction in large arteries, blood clots in blood vessels, idiopathic or hereditary angioedema, heart failure, dehydration, elderly, during pregnancy, and breastfeeding.
• Assess renal function before and during therapy; monitor for proteinuria.
• Regular WBC counts checking is recommended in SLE and scleroderma patients.
• Discontinue diuretics 2-3 days before starting therapy and resume later if required.

Drinking alcohol while taking Imidapril can increase drowsiness and dizziness, which in turn increases the risk of accidental injury.

Imidapril use in breastfeeding patients is not recommended.

Potassium-Rich Foods: Bananas, sweet potatoes, nuts, and other foods rich in potassium, when taken along with Imidapril, can be led to an increase in blood potassium levels.

Pleurisy Root: Pleurisy roots are not recommended with most heart medications due to the cardiac glycoside content of the root.

The adverse reactions related to the molecule Imidapril can be categorized as

• Common Adverse effects:

Body aches or pain, Chills, Cough, Difficulty breathing, Ear congestion, Fever, Headache, Loss of voice, Nasal congestion, Runny nose, Sneezing, Sore throat, Unusual tiredness or weakness, etc.,

• Less Common adverse effects:

Bladder pain, bloody or cloudy urine, change in hearing, chest pain, cold, congestion, diarrhea, difficulty, burning, or painful urination, dryness of the throat, earache or pain in the ear, ear drainage, etc.

• Rare adverse effects:

Agranulocytosis, bone marrow suppression, epistaxis, Raynaud's phenomenon, etc.

The clinically relevant drug interactions of Imidapril is briefly summarized here

• Increased risk of hyperkalemia with K-sparing diuretics (e.g. spironolactone, triamterene, amiloride), K supplements, or K-containing salt substitutes. Increased serum concentration and toxicity of lithium.
• NSAIDs (e.g. indometacin, aspirin), rifampicin, and sympathomimetics may decrease the antihypertensive effect of imidapril.
• May increase the risk of leucopenia with allopurinol, procainamide, and immunosuppressants. Enhanced hypotensive effect with other antihypertensive agents, diuretics (e.g., hydrochlorothiazide), nitrates, TCAs, and neuroleptics.
• May cause nutrition reactions (e.g., facial flushing, nausea, vomiting, hypotension) with Na aurothiomalate. May enhance the hypoglycaemic effect of antidiabetic agents (e.g., insulin).
• Potentially Fatal: Increased risk of hypotension, hyperkalemia, and reduced renal function (including acute renal failure) with aliskiren. This may result in severe anaphylactoid reactions when administered in patients undergoing LDL apheresis with dextran sulfate cellulose adsorption and hemodialysis with high-flux acrylonitrile methallyl sulfonate Na membranes.

The common side of Imidapril includes the following

Body aches or pain, Chills, Cough, Difficulty breathing, Ear congestion, Fever, Headache, Loss of voice, Nasal congestion, Runny nose, Sneezing, Sore throat, Unusual tiredness or weakness, etc,

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

Geriatric Use

There is no FDA guidance on the use of Imidapril in geriatric settings.

Symptoms: Severe hypotension, bradycardia, electrolyte disturbances, stupor, shock, and renal failure.

Management: If ingestion is recent, perform gastric lavage or administer adsorbents and Na sulfate within 30 minutes following intake. Closely observe the patient, preferably in an intensive care unit. Frequently monitor serum electrolytes and creatinine. In case of hypotension, place the patient in a shock position and immediately give salt and volume supplementation; consider treatment with angiotensin II. Administer atropine for the treatment of bradycardia and extensive vagal reactions; may consider the use of a pacemaker. Haemodialysis may be performed to remove imidapril and imidaprilat from the circulation

Pharmacodynamics:

Imidapril, a prodrug of imidaprilat, is a competitive ACE inhibitor that prevents the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor responsible for arterial vasoconstriction, increased blood pressure, and stimulation of aldosterone secretion. This action leads to lower angiotensin II levels, thereby increasing plasma renin activity and reducing aldosterone secretion.

Pharmacokinetics:

• Absorption: Rapidly but incompletely absorbed from the gastrointestinal tract. Reduced absorption with high-fat meals. Bioavailability: Approx 70% (imidapril); approx 42% (imidaprilat). Time to peak plasma concentration: Approx 2 hours (imidapril); 6-8 hours (imidaprilat).

• Distribution: Plasma protein binding: 85% (imidapril); 53% (imidaprilat).
• Metabolism: Metabolised in the liver via hydrolysis to imidaprilat (active metabolite).
• Excretion: Via faeces (approx 50%); urine (approx 40%). Elimination half-life: Imidapril: Approx 2 hours. Imidaprilat: 7-9 hours (initial); >24 hours (terminal).

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4. https://www.acc.org/latest-in-cardiology/clinical-trials/2010/02/23/19/05/fest

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2.https://www.drugtodayonline.com/drug-directory/drug_info/imidapril

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