82834-16-0 Usage
Description
Perindopril is a potent, orally-active angiotensin-converting enzyme (ACE) inhibitor
useful in the management of hypertension. Against rat ACE, perindopril appears to be
more potent than enalapril and enalaprilat, and is approximately equipotent to rarnipril
(HOE 498). Its long duration of action suggests the possibility of once-daily dosing.
Chemical Properties
Light Pink Solid
Uses
Different sources of media describe the Uses of 82834-16-0 differently. You can refer to the following data:
1. Labeled Perindopril, intended for use as an internal standard for the quantification of Perindopril by GC- or LC-mass spectrometry.
2. An angiotensin-converting enzyme (ACE) inhibitor. Antihypertensive. Neuroprotective & Neuroresearch Product.
Brand name
Coversyl
Therapeutic Function
Antihypertensive
Clinical Use
Angiotensin-converting enzyme inhibitor:
Hypertension
Heart failure
Following myocardial infarction or revascularisation
Drug interactions
Potentially hazardous interactions with other drugs
Anaesthetics: enhanced hypotensive effect.
Analgesics: antagonism of hypotensive effect and
increased risk of renal impairment with NSAIDs;
hyperkalaemia with ketorolac and other NSAIDs.
Antihypertensives: increased risk of hyperkalaemia,
hypotension and renal failure with ARBs and
aliskiren.
Bee venom extract: possible severe anaphylactoid
reactions when used together.
Ciclosporin: increased risk of hyperkalaemia and
nephrotoxicity.
Cytotoxics: increased risk of angioedema with
everolimus.
Diuretics: enhanced hypotensive effect;
hyperkalaemia with potassium-sparing diuretics.
ESAs: increased risk of hyperkalaemia; antagonism
of hypotensive effect.
Gold: flushing and hypotension with sodium
aurothiomalate.
Lithium: reduced excretion (possibility of enhanced
lithium toxicity).
Potassium salts: increased risk of hyperkalaemia.
Tacrolimus: increased risk of hyperkalaemia and
nephrotoxicity.
Metabolism
Perindopril is a pro-drug. It is extensively metabolised,
mainly in the liver, to the active perindoprilat and
inactive metabolites including glucuronides. Perindopril
is excreted mainly in the urine, as unchanged drug, as
perindoprilat, and as other metabolites.
references
[1] ryuji yasumatsu, torahiko nakashima, muneyuki masuda, aya ito, yuichiro kuratomi, yuichiro kuratomi and shizuo komune. effects of the angiotensin-i converting enzyme inhibitor perindopril on tumor growth and angiogenesis in head and neck squamous cell carcinoma cells. j cancer res clin oncol. 2004, 130: 567–573.[2] a.a.ajayi, k.r.lees and j.l.reid. effects of angiotensin converting enzyme inhibitor, perindopril, on autonomic reflexes. eur j clin pharmacol. 1986, 30:177-182.
Check Digit Verification of cas no
The CAS Registry Mumber 82834-16-0 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 8,2,8,3 and 4 respectively; the second part has 2 digits, 1 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 82834-16:
(7*8)+(6*2)+(5*8)+(4*3)+(3*4)+(2*1)+(1*6)=140
140 % 10 = 0
So 82834-16-0 is a valid CAS Registry Number.
InChI: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)
82834-16-0Relevant articles and documents
Of enantiomerically enriched indoline - 2 - formic acid
-
Paragraph 0145; 0146; 0147; 0148, (2017/09/01)
The invention discloses a synthesis method of enantiomer-enriched indoline-2-formic acid shown in a formula (I). The synthesis method of the enantiomer-enriched indoline-2-formic acid comprises the following steps: by adopting low-cost and available ortho-position halogen substituted benzaldehyde and N-benzoyl substituted glycine as starting materials, carrying out Erlenmeyer-Plochl cyclization, alkaline hydrolysis and asymmetric catalytic hydrogen for constructing a chiral center, and then carrying out acid catalysis, deprotection and cyclization sequentially or cyclization, acid catalysis and deprotection sequentially, so that the enantiomer-enriched indoline-2-formic acid is obtained. The synthesis method of the enantiomer-enriched indoline-2-formic acid has the advantages that raw materials used in the whole process route are low-cost and easily available, harmful substances or multiple danger special processes are not used, reaction conditions are mild, technological operation is simple, production is safe and stable, the product yield is high, the purity is high, less three wastes are produced, and the energy consumption is low, so that the synthesis method of the enantiomer-enriched indoline-2-formic acid is a process route especially applicable to industrial production. The formula (1) is described in the specification.
PERINDOPRIL TOSYLATE
-
Page/Page column 15, (2010/12/31)
The present invention relates to a novel salt of perindopril, namely the paratoluene sulfonic acid salt. The present invention also relates to an amorphous form of the perindopril paratoluene sulfonic acid salt. The invention further relates to processes for the preparation of the novel salt and the amorphous form thereof. The invention also relates to pharmaceutical compositions comprising the perindopril tosylate for the treatment of hypertension and heart failure.
PROCESS FOR THE PREPARATION OF PERINDOPRIL ERBUMINE SALT AND NOVEL POLYMORPH (S) THEREOF
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Page/Page column 12, (2008/12/07)
A single pot process for the preparation of perindopril erbumine salt according to which condensation of (2S, 3aS, 7aS)-octahydroindole-2-carboxylic acid benzyl ester para toluene sulfonate with N-((S-)-ethoxy carbonyl -1-ethyl-(S)-alanine, catalytic hydrogenation of benzyl ester of (2S, 3aS, 7aS)-1-{2-[1-(ethoxycarbonyl)-(S)-butylamino]-(S)propionyl}- octahydro-indole-2-carboxylate and conversion of (2S,3aS, 7aS)-1-{2-[1-ethoxycarbonyl)_(S)-butylamino]-(S)-propionyl}octahydroindole-2-carboxylic acid to its perindopril erbumine salt are carried out in a single pot using a single solvent such as isopropyl acetate to obtain perindopril erbumine salt of very high purity. Also a novel polymorph S of perindopril erbumine having X-ray diffraction peaks of 9.10, 14.64, 15.37, 16.58, 17.39, 19.99, 20.62, 21.50, 22.15, 22.60, 24.20, 27.55 ± 0.2 at 2Θ values. Also processes for preparing the novel polymorph S.
