Kelapril
Kelapril Uses, Dosage, Side Effects, Food Interaction and all others data.
Kelapril, brand name Lotensin, is a medication used to treat high blood pressure (hypertension), congestive heart failure, and chronic renal failure. Upon cleavage of its ester group by the liver, benazepril is converted into its active form benazeprilat, a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor.
Kelapril, an angiotensin-converting enzyme (ACE) inhibitor, is a prodrug which, when hydrolyzed by esterases to its active Kelaprilat, is used to treat hypertension and heart failure, to reduce proteinuria and renal disease in patients with nephropathies, and to prevent stroke, myocardial infarction, and cardiac death in high-risk patients. Kelapril and Kelaprilat inhibit angiotensin-converting enzyme (ACE) in human subjects and animals. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. Angiotensin II also stimulates aldosterone secretion by the adrenal cortex.
| Trade Name | Kelapril |
| Availability | Prescription only |
| Generic | Benazepril |
| Benazepril Other Names | Bénazépril, Benazepril, Benazeprilum |
| Related Drugs | amlodipine, lisinopril, metoprolol, losartan, furosemide, carvedilol, hydrochlorothiazide, spironolactone, valsartan, ramipril |
| Type | |
| Formula | C24H28N2O5 |
| Weight | Average: 424.4895 Monoisotopic: 424.199822016 |
| Protein binding | Benazepril is 96.7% protein bound while benazeprilat is 95.3% protein bound. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Belgium, France, Germany, Netherlands, United Kingdom |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Kelapril is an ACE inhibitor prodrug used to treat hypertension.
Kelapril is indicated for the treatment of hypertension. It may be used alone or in combination with thiazide diuretics.
Kelapril is also used to associated treatment for these conditions: Diabetic Nephropathy, Heart Failure, High Blood Pressure (Hypertension), Uncontrolled Hypertension, Nondiabetic nephropathy
How Kelapril works
Kelaprilat, the active metabolite of Kelapril, competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. Inhibition of ACE results in decreased plasma angiotensin II. As angiotensin II is a vasoconstrictor and a negative-feedback mediator for renin activity, lower concentrations result in a decrease in blood pressure and stimulation of baroreceptor reflex mechanisms, which leads to decreased vasopressor activity and to decreased aldosterone secretion.
Toxicity
The most common adverse effects include headache, dizziness, fatigue, somnolence, postural dizziness, nausea, and cough.
The most likely symptom of overdosage is severe hypotension.
Food Interaction
- Avoid potassium-containing products. Potassium products increase the risk of hyperkalemia.
- Take with or without food. Food slows the rate of absorption but not the extent.
[Moderate] GENERALLY AVOID: Moderate-to-high dietary intake of potassium can cause hyperkalemia in some patients who are using angiotensin converting enzyme (ACE) inhibitors.
In some cases, affected patients were using a potassium-rich salt substitute.
ACE inhibitors can promote hyperkalemia through inhibition of the renin-aldosterone-angiotensin (RAA) system.
MANAGEMENT: It is recommended that patients who are taking ACE inhibitors be advised to avoid moderately high or high potassium dietary intake.
Particular attention should be paid to the potassium content of salt substitutes.
Kelapril Alcohol interaction
[Moderate]
Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.
Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.
Caution and close monitoring for development of hypotension is advised during coadministration of these agents.
Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.
Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.
Kelapril Drug Interaction
Moderate: aspirin, aspirin, furosemide, furosemideUnknown: rosuvastatin, rosuvastatin, duloxetine, duloxetine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, atorvastatin, atorvastatin, metoprolol, metoprolol, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
Kelapril Disease Interaction
Major: angioedema, bone marrow suppression, CHF, hemodialysis, hyperkalemia, hypotensionModerate: liver disease, renal dysfunction
Volume of Distribution
The final population pharmacokinetic model in one study estimated the volume of distribution to be 203±69.9L.
Elimination Route
Bioavailability of oral dosing is 3% to 4% in horses. In humans at least 37% of oral benazepril is absorbed and reaches peak plasma concentration in 0.5 hours to 1 hour. Other studies have shown a peak plasma concentration at a median of 1.5 hours.
Half Life
The half life of the prodrug benazepril is 2.7±8.5h. The half life of the active metabolite benazeprilat is 22.3±9.2h The accumulation half life of benazepril is 10 to 11 hours.
Clearance
The final population pharmacokinetic model of one study estimates the clearance to be 129±30.0L.
Elimination Route
Kelapril and benazeprilat are cleared predominantly by renal excretion in healthy subjects with normal renal function. Nonrenal (i.e., biliary) excretion accounts for approximately 11%-12% of benazeprilat excretion in healthy subjects.
Innovators Monograph
You find simplified version here Kelapril
