Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C19H32N2O5.C4H11N.H2O |
| Molecular Weight | 459.6199 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 5 / 5 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O.CC(C)(C)N.[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=AAQKIIDLRYLALW-MXLIJYGISA-N
InChI=1S/C19H32N2O5.C4H11N.H2O/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;1-4(2,3)5;/h12-16,20H,4-11H2,1-3H3,(H,23,24);5H2,1-3H3;1H2/t12-,13-,14-,15-,16-;;/m0../s1
| Molecular Formula | H2O |
| Molecular Weight | 18.0153 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C4H11N |
| Molecular Weight | 73.1368 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| 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 Date1993 |
|||
| 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 Date1993 |
|||
| 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 |
|---|---|---|
| Inhibition of angiotensin I-converting enzyme with S 9490: biochemical effects, interspecies differences, and role of sodium diet in hemodynamic effects. | 1984 Nov-Dec |
|
| Renal effects of perindoprilat, an angiotensin-converting enzyme inhibitor, in the anesthetized dog. | 1989 Feb |
|
| The initial hemodynamic response to newer antihypertensive agents at rest and during exercise: review of visacor, doxazosin, nisoldipine, tiapamil, perindoprilat, pinacidil, dilevalol, and carvedilol. | 1990 Aug |
|
| Specific and high affinity binding of perindoprilat, but not of perindopril to blood ACE. | 1992 Sep |
|
| [The effect of amlodipine, nifedipine and perindopril on insulin sensitivity and blood lipid of patients with essential hypertension]. | 1998 Mar |
|
| Challenges for the prevention of primary and secondary stroke: the importance of lowering blood pressure and total cardiovascular risk. | 2001 |
|
| [Hypotension followed the first dose of angiotensin-converting enzyme inhibitor in patients with heart failure (a multicenter clinical trial)]. | 2001 |
|
| Perindopril: an updated review of its use in hypertension. | 2001 |
|
| Hypertension in the Very Elderly Trial (HYVET): protocol for the main trial. | 2001 |
|
| Microthrombosis in sepsis. | 2001 Apr |
|
| Pulse wave velocity as endpoint in large-scale intervention trial. The Complior study. Scientific, Quality Control, Coordination and Investigation Committees of the Complior Study. | 2001 Apr |
|
| Effect of angiotensin-converting enzyme inhibition on myocardial vascularization in the adolescent and adult spontaneously hypertensive rat. | 2001 Apr |
|
| The angiotensin-I-converting enzyme inhibitor perindopril suppresses tumor growth and angiogenesis: possible role of the vascular endothelial growth factor. | 2001 Apr |
|
| Ongoing trials of angiotensin-converting enzyme inhibition: what they can tell us. | 2001 Aug |
|
| Comparison of endothelial pleiotropic actions of angiotensin converting enzyme inhibitors and statins. | 2001 Dec |
|
| The lowering of blood pressure after stroke. | 2001 Dec 8 |
|
| Significance of endothelial prostacyclin and nitric oxide in peripheral and pulmonary circulation. | 2001 Jan-Feb |
|
| Pharmacokinetic-pharmacodynamic model for perindoprilat regional haemodynamic effects in healthy volunteers and in congestive heart failure patients. | 2001 Jul |
|
| The quantitative determination of several inhibitors of the angiotensin-converting enzyme by CE. | 2001 Jul |
|
| Effects of an angiotensin-converting enzyme inhibitor and a beta-blocker on cerebral arteriolar dilatation in hypertensive rats. | 2001 Jun |
|
| Angiotensin-converting enzyme inhibitor therapy improves respiratory muscle strength in patients with heart failure. | 2001 Jun |
|
| 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 |
|
| Pulmonary vascular remodelling in hypoxic rats: effects of amlodipine, alone and with perindopril. | 2001 Mar 23 |
|
| Antihypertensive efficacy and tolerability of low-dose perindopril/indapamide combination compared with losartan in the treatment of essential hypertension. | 2001 May |
|
| Salt sensitivity in genetically hypertensive rats of the Lyon strain. | 2001 May |
|
| 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 |
|
| 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 |
|
| Increased absorption of zinc from alimentary tract in primary arterial hypertension. | 2001 Oct |
|
| Perindopril treatment for congestive heart failure. | 2001 Oct 4 |
|
| Dosage considerations with perindopril for systemic hypertension. | 2001 Oct 4 |
|
| Dietary n-3 polyunsaturated fatty acids affect the development of renovascular hypertension in rats. | 2001 Sep |
|
| Randomised trial of a perindopril-based blood-pressure-lowering regimen among 6,105 individuals with previous stroke or transient ischaemic attack. | 2001 Sep 29 |
|
| 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 |
|
| 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 |
|
| 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 |
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
Fri Dec 15 17:08:44 GMT 2023
by
admin
on
Fri Dec 15 17:08:44 GMT 2023
|
| Record UNII |
DV54578K4P
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
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100000130680
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9847044
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690267-97-1
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DV54578K4P
Created by
admin on Fri Dec 15 17:08:44 GMT 2023 , Edited by admin on Fri Dec 15 17:08:44 GMT 2023
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| Related Record | Type | Details | ||
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PARENT -> SALT/SOLVATE | |||
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ANHYDROUS->SOLVATE | |||
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PARENT -> SALT/SOLVATE |
