Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C19H32N2O5 |
| Molecular Weight | 368.4678 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 5 / 5 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@]12C[C@H](N(C(=O)[C@@H](C)N[C@@H](CCC)C(=O)OCC)[C@@]1([H])CCCC2)C(O)=O
InChI
InChIKey=IPVQLZZIHOAWMC-YXMSTPNBSA-N
InChI=1S/C19H32N2O5/c1-4-8-14(19(25)26-5-2)20-12(3)17(22)21-15-10-7-6-9-13(15)11-16(21)18(23)24/h12-16,20H,4-11H2,1-3H3,(H,23,24)/t12-,13+,14+,15+,16+/m1/s1
| Molecular Formula | C19H32N2O5 |
| Molecular Weight | 368.4678 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 5 / 5 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020184s022lbl.pdfhttp://pubs.rsc.org/-/content/getauthorversionpdf/C3AY42056Fhttps://www.ncbi.nlm.nih.gov/pubmed/1457697http://www.hmdb.ca/metabolites/HMDB60574Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/1718688
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020184s022lbl.pdfhttp://pubs.rsc.org/-/content/getauthorversionpdf/C3AY42056Fhttps://www.ncbi.nlm.nih.gov/pubmed/1457697http://www.hmdb.ca/metabolites/HMDB60574
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/1718688
Perindoprilat is a metabolite of perindopril. Perindopril is a long-acting angiotensin converting enzyme (ACE) inhibitor and it is used to treat high blood pressure, heart failure or stable coronary artery disease. Perindopril is designed to allow oral administration as perindoprilat is poorly absorbed from the gastrointestinal tract.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL1808 |
1.05 nM [IC50] | ||
Target ID: CHEMBL1808 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | ACEON Approved UsePerindopril erbumine tablets are indicated for treatment of patients with stable coronary artery disease to reduce the risk of cardiovascular mortality or nonfatal myocardial infarction. Perindopril erbumine tablets can be used with conventional treatment for management of coronary artery disease, such as antiplatelet, antihypertensive or lipid-lowering therapy. Launch Date7.5720963E11 |
|||
| Primary | ACEON Approved UsePerindopril erbumine tablets are indicated for the treatment of patients with essential hypertension. Perindopril erbumine tablets may be used alone or given with other classes of antihypertensives, especially thiazide diuretics. Launch Date7.5720963E11 |
|||
| Palliative | Unknown Approved UseUnknown |
|||
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
83.83 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21650082 |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
PERINDOPRIL plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3.54 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21650082 |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
PERINDOPRILAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
130 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21650082 |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
PERINDOPRIL plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
170.61 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21650082 |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
PERINDOPRILAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1.05 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21650082 |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
PERINDOPRIL plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
38.01 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21650082 |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
PERINDOPRILAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
40% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21650082 |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
PERINDOPRIL plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
80% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21650082 |
4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: |
PERINDOPRILAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
| Dose | Population | Adverse events |
|---|---|---|
4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: |
unhealthy, adult n = 320 Health Status: unhealthy Condition: hypertension Age Group: adult Sex: unknown Population Size: 320 Sources: |
Disc. AE: Cough... AEs leading to discontinuation/dose reduction: Cough (2.8%) Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Cough | 2.8% Disc. AE |
4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: |
unhealthy, adult n = 320 Health Status: unhealthy Condition: hypertension Age Group: adult Sex: unknown Population Size: 320 Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Challenges for the prevention of primary and secondary stroke: the importance of lowering blood pressure and total cardiovascular risk. | 2001 |
|
| [Effects of angiotensin-converting enzyme inhibitors and cosaar on quality of life of patients with pulmonary tuberculosis and chronic heart failure]. | 2001 |
|
| Interventions for deliberately altering blood pressure in acute stroke. | 2001 |
|
| [Hypotension followed the first dose of angiotensin-converting enzyme inhibitor in patients with heart failure (a multicenter clinical trial)]. | 2001 |
|
| [Effects of perindopril and its combination with indapamide on risk stratification in patients with hypertension]. | 2001 |
|
| [The comparison of clinical effectiveness of perindopril and acebutolol in the primary hypertension treatment]. | 2001 |
|
| Vasoactive peptides and procollagen propeptides in patients with hypertension in relation to cardiac hypertrophy and diastolic heart failure: design of the study and patient characteristics. | 2001 Aug |
|
| Anglo-Scandinavian Cardiac Outcomes Trial: a brief history, rationale and outline protocol. | 2001 Aug |
|
| Academic support for combination therapy in hypertension. | 2001 Aug-Sep |
|
| Comparison of endothelial pleiotropic actions of angiotensin converting enzyme inhibitors and statins. | 2001 Dec |
|
| ACE inhibitors in vascular disease: some PROGRESS, more HOPE. | 2001 Dec |
|
| Chronic ACE inhibition enhances the endothelial control of arterial mechanics and flow-dependent vasodilatation in heart failure. | 2001 Dec 1 |
|
| The lowering of blood pressure after stroke. | 2001 Dec 8 |
|
| The lowering of blood pressure after stroke. | 2001 Dec 8 |
|
| The lowering of blood pressure after stroke. | 2001 Dec 8 |
|
| The lowering of blood pressure after stroke. | 2001 Dec 8 |
|
| The lowering of blood pressure after stroke. | 2001 Dec 8 |
|
| Assessment of perindopril's efficacy on arterial distensibility in mild to moderate hypertension. | 2001 Jul |
|
| Coversyl plus--when monotherapy is not enough. | 2001 Jun-Jul |
|
| New benefits of blood pressure lowering treatments for millions of stroke sufferers. | 2001 Jun-Jul |
|
| The EUROPA trial: design, baseline demography and status of the substudies. | 2001 Mar |
|
| Clinical benefit of very-low-dose perindopril-indapamide combination in hypertension. | 2001 Nov |
|
| Amelioration of arterial properties with a perindopril-indapamide very-low-dose combination. | 2001 Nov |
|
| [Clinical study of the month. Secondary prevention of cerebrovascular accident with perindopril: the PROGRESS study]. | 2001 Nov |
|
| [Early prevention of experimental left ventricular hypertrophy in experimental hypertension and angiotensin II levels]. | 2001 Nov |
|
| Effect of angiotensin-converting enzyme inhibition on renal filtration surface area in hypertensive rats. | 2001 Nov |
|
| Does ACE inhibition slow progression of glomerulopathy in patients with Type 2 diabetes mellitus? | 2001 Nov |
|
| Angiotensin-converting enzyme gene insertion/deletion, not bradykinin B2 receptor -58T/C gene polymorphism, associated with angiotensin-converting enzyme inhibitor-related cough in Chinese female patients with non-insulin-dependent diabetes mellitus. | 2001 Nov |
|
| Angiotensin-converting enzyme inhibition improves defective angiogenesis in the ischemic limb of spontaneously hypertensive rats. | 2001 Nov |
|
| Effects of combined administration of ACE inhibitor and angiotensin II receptor antagonist are prevented by a high NaCl intake. | 2001 Nov |
|
| [Efficacy of a converting enzyme inhibitor in the prevention of recurrence of stroke]. | 2001 Nov 24 |
|
| A double-blind trial of perindopril and nitrendipine in incipient diabetic nephropathy. | 2001 Oct |
|
| Increased absorption of zinc from alimentary tract in primary arterial hypertension. | 2001 Oct |
|
| Improvement in blood pressure, arterial stiffness and wave reflections with a very-low-dose perindopril/indapamide combination in hypertensive patient: a comparison with atenolol. | 2001 Oct |
|
| Proangiogenic effect of angiotensin-converting enzyme inhibition is mediated by the bradykinin B(2) receptor pathway. | 2001 Oct 12 |
|
| Safety profile of perindopril. | 2001 Oct 4 |
|
| Effects of perindopril on cardiovascular remodeling. | 2001 Oct 4 |
|
| Dietary n-3 polyunsaturated fatty acids affect the development of renovascular hypertension in rats. | 2001 Sep |
|
| Very-low-dose combination of perindopril and indapamide as a novel strategy in first-line management of hypertension. | 2001 Sep |
|
| Study rationale and design of ADVANCE: action in diabetes and vascular disease--preterax and diamicron MR controlled evaluation. | 2001 Sep |
|
| Identification and determination of selected medicines reducing hypertension by densitometric and gas chromatographic methods. | 2001 Sep-Oct |
|
| [Antihypertensive agents after cerebral stroke are more effective than expected]. | 2001 Sep-Oct |
|
| Detection of coronary microvascular disease by means of cardiac scintigraphy. | 2002 Feb |
|
| Progress in secondary prevention of stroke with PROGRESS. The perindopril protection against recurrent stroke study. | 2002 Feb |
|
| Long-term treatment with perindopril ameliorates dobutamine-induced myocardial ischemia in patients with coronary artery disease. | 2002 Jan |
|
| Attenuation of tubular apoptosis by blockade of the renin-angiotensin system in diabetic Ren-2 rats. | 2002 Jan |
|
| The PROGRESS Trial: preventing strokes by lowering blood pressure in patients with cerebral ischemia. Emerging therapies: critique of an important advance. | 2002 Jan |
|
| Comparison of perindopril versus captopril for treatment of acute myocardial infarction. | 2002 Jan 15 |
|
| Effects of low-dose and early versus late perindopril treatment on the progression of severe diabetic nephropathy in (mREN-2)27 rats. | 2002 Mar |
|
| Combined therapy with indapamide and perindopril but not perindopril alone reduced the risk for recurrent stroke. | 2002 Mar-Apr |
Patents
Sample Use Guides
In patients with essential hypertension, the recommended initial dose is 4 mg once a day. The dose may be titrated, as needed to a maximum of 16 mg per day. The usual maintenance dose range is 4 mg to 8 mg administered as a single daily dose or in two divided doses. In patients with stable coronary artery disease, Perindopril erbumine tablets should be given at an initial dose of 4 mg once daily for 2 weeks, and then increased as tolerated, to a maintenance dose of 8 mg once daily. In elderly patients (greater than 70 years), Perindopril erbumine tablets should be given as a 2 mg dose once daily in the first week, followed by 4 mg once daily in the second week and 8 mg once daily for maintenance dose if tolerated.
Route of Administration:
Oral
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 08:05:12 UTC 2023
by
admin
on
Sat Dec 16 08:05:12 UTC 2023
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| Record UNII |
LUF968K225
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| Record Status |
Validated (UNII)
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| Record Version |
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LUF968K225
Created by
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60184
Created by
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