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QuickView for perindopril (compound)

Name: Perindopril
PubChem Compound ID: 107807
Description: An angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure.
Molecular formula: C19H32N2O5
Molecular weight: 368.468 g/mol
Aceon; SED-9490; 1H-Indole-2-carboxylic acid, 1-((2S)-2-(((1S)-1-(ethoxycarbonyl)butyl)amino)-1-oxopropyl)octahydro-, (2S,3aS,7aS)-; DW-7950; Spectrum2_001108; Spectrum4_000775; Coverex; McN-A-2833; Coverene Cor; Spectrum_001948.
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Name: Perindopril
Name (isomeric): DB00790
Drug Type: small molecule
Description: An angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure.
Perindopril Erbumine
Brand: Aceon, Coversyl
Brand name mixture: Preterax(perindopril erbumine + indapamide), Coversyl Plus(perindopril erbumine + indapamide)
Category: Angiotensin-converting Enzyme Inhibitors, Antihypertensive Agents
CAS number: 107133-36-8
Indication: For the treatment of mild to moderate essential hypertension, mild to moderate congestive heart failure, and to reduce the cardiovascular risk of individuals with hypertension or post-myocardial infarction and stable coronary disease.
Perindopril is a nonsulfhydryl prodrug that is metabolized via first pass effect (62%) and systemic hydrolysis (38%) to perindoprilat, its active metabolite, following oral administration. Perindoprilat lowers blood pressure by antagonizing the effect of the RAAS. The RAAS is a homeostatic mechanism for regulating hemodynamics, water and electrolyt...
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Mechanism of Action:
There are two isoforms of ACE: the somatic isoform, which exists as a glycoprotein comprised of a single polypeptide chain of 1277; and the testicular isoform, which has a lower molecular mass and is thought to play a role in sperm maturation and binding of sperm to the oviduct epithelium. Somatic ACE has two functionally active domains, N and C, w...
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Absorption: Rapidly absorbed with peak plasma concentrations occurring approximately 1 hour after oral administration. Bioavailability is 65-75%. Following absorption, perindopril is hydrolyzed to perindoprilat, which has an average bioavailability of 20%. The rate and extent of absorption is unaffected by food. However, food decreases the extent of biotransformation to peridoprilat and reduces its bioavailability by 35%.
Protein binding: Perindoprilat, 10-20% bound to plasma proteins
Biotransformation: Extensively metabolized, with only 4-12% of the dose recovered in urine following oral administration. Six metabolites have been identified: perindoprilat, perindopril glucuronide, perindoprilat glucuronide, a perindopril lactam, and two perindoprilat lactams. Only perindoprilat is pharmacologically active. Peridoprilat and perindoprilat glucuronide are the two main circulating metabolites.
Route of elimination: Perindopril is extensively metabolized following oral administration, with only 4 to 12% of the dose recovered unchanged in the urine.
Half Life: Perindopril, 1.2 hours; Peridoprilat, 30-120 hours. The long half life of peridoprilat is due to its slow dissociation from ACE binding sites.
Clearance: 219 - 362 mL/min [oral administration]
Toxicity: The most likely symptom of overdose is severe hypotension. The most common adverse effects observed in controlled clinical trials include cough, digestive symptoms, fatigue, headache, and dizziness.
Affected organisms: Humans and other mammals
Food interaction:
Herbs that may attenuate the antihypertensive effect of perindopril include: bayberry, blue cohash, cayenne, ephedra, ginger, ginseng (American), kola and licorice.
Perindopril may decrease the excretion of potassium. Salt substitutes containing potassium may increase the risk of hyperkalemia.
Take without regard to meals.
High salt intake may attenuate the antihypertensive effect of perindopril.
Drug interaction:
LithiumThe ACE inhibitor increases serum levels of lithium
TizanidineTizanidine increases the risk of hypotension with the ACE inhibitor
TobramycinIncreased risk of nephrotoxicity
SpironolactoneIncreased risk of hyperkalemia
PotassiumIncreased risk of hyperkalemia
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