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Quinapril | CAS No: 85441-61-8 | GMP-certified suppliers
A medication that treats hypertension and heart failure, available alone or combined with diuretics, supporting cardiovascular management through blood pressure reduction.
Therapeutic categories
Primary indications
- Quinapril is indicated for the treatment of hypertension and as an adjunct therapy in the treatment of heart failure
- Quinapril in combination with hydrochlorothiazide is indicated for the treatment of hypertension
Product Snapshot
- Quinapril is available as oral coated and film-coated tablets as well as an intravenous injection solution
- It is primarily indicated for the treatment of hypertension and adjunct therapy for heart failure, including combination use with hydrochlorothiazide for hypertension
- Quinapril is approved for use in the US and Canada, with some investigational statuses
Clinical Overview
Pharmacologically, quinapril is an ethyl ester prodrug that is rapidly converted in vivo to its active metabolite, quinaprilat, a non-sulfhydryl ACE inhibitor. Quinaprilat exerts its clinical effects by inhibiting ACE, the enzyme responsible for converting angiotensin I to angiotensin II. This leads to decreased levels of angiotensin II, a potent vasoconstrictor and contributor to myocardial hypertrophy, vascular smooth muscle proliferation, and thrombosis via plasminogen activator inhibitor-1 (PAI-1) stimulation. Inhibition of ACE also reduces the degradation of bradykinin, which may contribute to vasodilatory effects. The net result is vasodilation, reduced vascular resistance, and lowered blood pressure.
Regarding absorption, distribution, metabolism, and excretion (ADME), quinapril is orally administered and exhibits a long duration of action, allowing once-daily dosing in the range of 10 to 80 mg. It has a wide therapeutic window, which facilitates dose adjustment according to clinical response and tolerance.
Safety considerations for quinapril include the risk of angioedema and hyperkalemia, consistent with the ACE inhibitor class. Monitoring of renal function and electrolytes is advised during therapy, particularly in susceptible populations. Quinapril should be used cautiously in patients with renal impairment or those concurrently taking potassium-sparing agents.
Quinapril is available under various generic and brand names worldwide, frequently formulated alone or in fixed-dose combinations with diuretics such as hydrochlorothiazide. For API procurement, attention to stringent quality standards is critical to ensure purity, consistent bioavailability, and compliance with relevant pharmacopeial specifications. Reliable sourcing should involve suppliers with validated manufacturing processes and appropriate regulatory certifications to support global pharmaceutical production.
Identification & chemistry
| Generic name | Quinapril |
|---|---|
| Molecule type | Small molecule |
| CAS | 85441-61-8 |
| UNII | RJ84Y44811 |
| DrugBank ID | DB00881 |
Pharmacology
| Summary | Quinapril is an angiotensin-converting enzyme (ACE) inhibitor that reduces the conversion of angiotensin I to angiotensin II, leading to decreased vasoconstriction, myocardial hypertrophy, and vascular smooth muscle proliferation. By lowering angiotensin II levels, it also reduces plasminogen activator inhibitor-1 (PAI-1) production, thereby mitigating thrombosis risk. Quinapril is employed primarily for hypertension management and as adjunctive therapy in heart failure. |
|---|---|
| Mechanism of action | 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. Quinaprilat 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. |
| Pharmacodynamics | Quinapril is a prodrug of an angiotensin converting enzyme (ACE) inhibitor used in the treatment of hypertension or adjunct in the treatment of heart failure. Quinapril has a wide therapeutic window and a long duration of action as it is given in doses of 10-80mg once daily. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Angiotensin-converting enzyme | Humans | inhibitor |
ADME / PK
| Absorption | Quinapril if 50-80% bioavailable. Quinapril has a T<sub>max</sub> of <1 hour, while quinaprilat has a T<sub>max</sub> of 2.5h. The C<sub>max</sub> 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. |
| Protein binding | Quinapril and the active metabolite quinaprilat are 97% protein bound in plasma. |
| Metabolism | Quinapril is de-esterified to the active quinaprilat or dehydrated to form the inactive PD109488. PD109488 can undergo O-deethylation to form another inactive metabolite, PD113413. |
| Route of elimination | Quinaprilat 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. |
| Volume of distribution | The mean volume of distribution of quinaprilat is 13.9L. |
| Clearance | The clearance of quinaprilat is 68mL/min. |
Formulation & handling
- Quinapril is available for oral administration primarily as coated tablets and also as an intravenous injectable solution.
- Its low water solubility and moderate lipophilicity (LogP ~2) suggest formulation strategies to enhance bioavailability may be required.
- Patients should avoid co-administration with fatty foods and potassium-containing products due to interaction risks affecting efficacy and safety.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is marketed in the United States and Canada, with key patents having expired between 2010 and 2015, indicating a mature market with generic availability. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Quinapril is manufactured by multiple originator and generic pharmaceutical companies with a diverse global footprint, including significant production presence in the US and Canada. The branded product, primarily known as Accupril, is established in North American markets. Given the patent expirations reported in the US (2015) and Canada (2010-2011), the market has likely experienced existing generic competition. |
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Safety
| Toxicity | The oral LD<sub>50</sub> 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. |
|---|
- Oral LD50 values indicate moderate acute toxicity (rats: 3541 mg/kg
- Mice: 1739 mg/kg)
- Exposure may result in severe hypotension
Quinapril is a type of ACE inhibitors
ACE inhibitors, or angiotensin-converting enzyme inhibitors, are a subcategory of pharmaceutical APIs (active pharmaceutical ingredients) commonly used in the treatment of various cardiovascular conditions. These medications work by inhibiting the activity of the angiotensin-converting enzyme, which plays a crucial role in the regulation of blood pressure and fluid balance.
By blocking the action of this enzyme, ACE inhibitors help relax and widen the blood vessels, reducing peripheral resistance and ultimately lowering blood pressure. This mechanism of action makes ACE inhibitors highly effective in treating hypertension (high blood pressure) and congestive heart failure.
Additionally, ACE inhibitors have been found to be beneficial for patients with certain kidney disorders and diabetic nephropathy. By dilating the renal blood vessels, they can help improve renal function and reduce proteinuria.
Some commonly prescribed ACE inhibitors include lisinopril, enalapril, and ramipril. These medications are typically administered orally and are available in various dosage forms, including tablets and capsules.
It's worth noting that ACE inhibitors may have certain side effects, such as dry cough, dizziness, and hyperkalemia (high potassium levels). However, these side effects are generally mild and well-tolerated by most patients.
In summary, ACE inhibitors are a vital subcategory of pharmaceutical APIs used in the management of hypertension, heart failure, and certain renal disorders. Their ability to lower blood pressure and improve renal function makes them an essential tool in the treatment of cardiovascular diseases.
Quinapril (ACE inhibitors), classified under Antihypertensive agents
Antihypertensive agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat high blood pressure, also known as hypertension. These medications are designed to lower blood pressure and reduce the risk of associated cardiovascular complications.
Antihypertensive agents function by targeting various mechanisms involved in blood pressure regulation. Some common classes of antihypertensive agents include angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor blockers (ARBs), beta-blockers, calcium channel blockers (CCBs), and diuretics.
ACE inhibitors work by inhibiting the enzyme responsible for converting angiotensin I to angiotensin II, a hormone that constricts blood vessels. ARBs, on the other hand, block the receptors to which angiotensin II binds, thereby preventing its vasoconstrictive effects.
Beta-blockers reduce blood pressure by blocking the effects of adrenaline and noradrenaline, which are responsible for increasing heart rate and constricting blood vessels. CCBs inhibit calcium from entering the smooth muscles of blood vessels, resulting in relaxation and vasodilation. Diuretics promote the elimination of excess fluid and sodium from the body, reducing blood volume and thereby lowering blood pressure.
Antihypertensive agents are typically prescribed based on the individual patient's condition and specific needs. They can be used alone or in combination to achieve optimal blood pressure control. It is important to note that antihypertensive agents should be taken regularly as prescribed by a healthcare professional and may require periodic monitoring to ensure their effectiveness and manage any potential side effects.
In summary, antihypertensive agents play a vital role in the management of hypertension by targeting various mechanisms involved in blood pressure regulation. These medications offer significant benefits in reducing the risk of cardiovascular complications associated with high blood pressure.
Quinapril API manufacturers & distributors
Compare qualified Quinapril API suppliers worldwide. We currently have 3 companies offering Quinapril API, with manufacturing taking place in 2 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Lupin | Producer | India | India | CoA, GMP, USDMF, WC | 155 products |
| Mylan | Producer | India | India | CEP, CoA, USDMF, WC | 201 products |
| Signa | Producer | Mexico | Mexico | CoA, USDMF | 42 products |
When sending a request, specify which Quinapril API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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