Quinaprilum
Quinaprilum Uses, Dosage, Side Effects, Food Interaction and all others data.
Quinaprilum is the ethyl ester prodrug of the non-sulfhydryl angiotensin converting enzyme inhibitor quinaprilat. It is used to treat hypertension and heart failure. ACE inhibitors are commonly used as a first line therapy in the treatment of hypertension, along with thiazide diuretics or beta blockers.
Quinaprilum was granted FDA approval on 19 November 1991. A combination tablet with hydrochlorothiazide was also approved on 28 December 1999.
Quinaprilum is a prodrug of an angiotensin converting enzyme (ACE) inhibitor used in the treatment of hypertension or adjunct in the treatment of heart failure. Quinaprilum has a wide therapeutic window and a long duration of action as it is given in doses of 10-80mg once daily.
| Trade Name | Quinaprilum |
| Availability | Prescription only |
| Generic | Quinapril |
| Quinapril Other Names | Quinapril, Quinaprilum |
| Related Drugs | amlodipine, lisinopril, metoprolol, losartan, furosemide, carvedilol, hydrochlorothiazide, spironolactone, valsartan, ramipril |
| Type | |
| Formula | C25H30N2O5 |
| Weight | Average: 438.5161 Monoisotopic: 438.21547208 |
| Protein binding | Quinapril and the active metabolite quinaprilat are 97% protein bound in plasma. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Quinaprilum is an ACE inhibitor prodrug used to treat hypertension, congestive heart failure, and slow rate of progression of renal disease.
Quinaprilum is indicated for the treatment of hypertension and as an adjunct therapy in the treatment of heart failure. Quinaprilum in combination with hydrochlorothiazide is indicated for the treatment of hypertension.
Quinaprilum is also used to associated treatment for these conditions: Congestive Heart Failure (CHF), Diabetic Nephropathy, High Blood Pressure (Hypertension), Left Ventricular Dysfunction
How Quinaprilum works
Angiotensin II constricts coronary blood vessels and is positively inotropic, which under normal circumstances, would increase vascular resistance and oxygen consumption. This action can eventually lead to myocyte hypertrophy and vascular smooth muscle cell proliferation. Angiotensin II also stimulates production of plasminogen activator inhibitor-1 (PAI-1), increasing the risk of thrombosis.
Quinaprilumat prevents the conversion of angiotensin I to angiotensin II by inhibition of angiotensin converting enzyme, and also reduces the breakdown of bradykinin. Reduced levels of angiotensin II lead to lower levels of PAI-1, reducing the risk of thrombosis, especially after a myocardial infarction.
Toxicity
The oral LD50 in rats is 3541mg/kg and in mice is 1739mg/kg.
Patients experiencing an overdose may present with symptoms of severe hypotension. Due to the extensive protein binding of quinapril and the active metabolite quinaprilat, hemodialysis is not expected to remove the drug from circulation. Treat patients with symptomatic and supportive measures, including normal saline infusions to restore normal blood pressure.
Food Interaction
- Avoid fatty foods.
- Avoid hypertensive herbs (e.g. bayberry, blue cohosh, cayenne, ephedra, and licorice).
- Avoid potassium-containing products. Potassium products increase the risk of hyperkalemia.
- Limit salt intake. Salt may attenuate the antihypertensive effect.
[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.
Quinaprilum Drug Interaction
Moderate: aspirin, rosuvastatin, insulin glargine, furosemide, levothyroxine, alprazolamMinor: amlodipineUnknown: duloxetine, apixaban, omega-3 polyunsaturated fatty acids, sitagliptin, atorvastatin, metoprolol, metoprolol, esomeprazole, clopidogrel, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol
Quinaprilum Disease Interaction
Major: angioedema, bone marrow suppression, CHF, hemodialysis, hyperkalemia, hypotensionModerate: liver disease, renal dysfunction
Volume of Distribution
The mean volume of distribution of quinaprilat is 13.9L.
Elimination Route
Quinaprilum if 50-80% bioavailable. Quinaprilum has a Tmax of 6 while quinaprilat has a Tmax of 2.5h. The Cmax of quinaprilat is highly variable but reaches 1526ng/mL with an AUC of 2443ng*h/mL in healthy males given a 10mg dose. A high fat meal reduces the absorption of quinapril by 25-30%.
Half Life
The active metabolite quinaprilat has an elimination half life of 2.3 hours.
Clearance
The clearance of quinaprilat is 68mL/min.
Elimination Route
Quinaprilumat is up to 96% eliminated in the urine. The eliminated metabolites PD109488 and PD113413 account for approximately 6% of a dose of quinapril each. A small fraction of the dose recovered in the urine is accounted for by unmetabolized quinapril.
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