Peringatan Keamanan

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.

Perindopril

DB00790

small molecule approved

Deskripsi

Perindopril is a nonsulfhydryl prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications. It is rapidly metabolized in the liver to perindoprilat, its active metabolite, following oral administration. Perindoprilat is a potent, competitive inhibitor of ACE, the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Perindopril may be used to treat 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.

Struktur Molekul 2D

Berat 368.4678
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (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.
Volume Distribusi -
Klirens (Clearance) * 219 - 362 mL/min [oral administration]

Absorpsi

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%.

Metabolisme

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.

Rute Eliminasi

Perindopril is extensively metabolized following oral administration, with only 4 to 12% of the dose recovered unchanged in the urine.

Interaksi Makanan

4 Data
  • 1. Avoid hypertensive herbs (e.g. bayberry, blue cohosh, cayenne, ephedra, and licorice).
  • 2. Avoid potassium-containing products. Potassium products increase the risk of hyperkalemia.
  • 3. Limit salt intake. Salt may attenuate the antihypertensive effect.
  • 4. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1302 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Perindopril is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Perindopril is combined with Levodopa.
Risperidone Perindopril may increase the hypotensive activities of Risperidone.
Alfuzosin Alfuzosin may increase the hypotensive activities of Perindopril.
Amifostine Perindopril may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Perindopril.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Perindopril.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Perindopril.
Obinutuzumab Perindopril may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Perindopril.
Rituximab Perindopril may increase the hypotensive activities of Rituximab.
Phentermine Phentermine may decrease the antihypertensive activities of Perindopril.
Midodrine Midodrine may decrease the antihypertensive activities of Perindopril.
Eletriptan Eletriptan may decrease the antihypertensive activities of Perindopril.
Isoetharine Isoetharine may decrease the antihypertensive activities of Perindopril.
Methysergide Methysergide may decrease the antihypertensive activities of Perindopril.
Cabergoline Cabergoline may decrease the antihypertensive activities of Perindopril.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Perindopril.
Dihydroergotamine Dihydroergotamine may decrease the antihypertensive activities of Perindopril.
Protriptyline Protriptyline may decrease the antihypertensive activities of Perindopril.
Methylergometrine Methylergometrine may decrease the antihypertensive activities of Perindopril.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Perindopril.
Mirtazapine Mirtazapine may decrease the antihypertensive activities of Perindopril.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Perindopril.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Perindopril.
Droperidol Droperidol may decrease the antihypertensive activities of Perindopril.
Doxapram Doxapram may decrease the antihypertensive activities of Perindopril.
Lisuride Lisuride may decrease the antihypertensive activities of Perindopril.
Metaraminol Metaraminol may decrease the antihypertensive activities of Perindopril.
Trazodone Trazodone may decrease the antihypertensive activities of Perindopril.
Epinephrine Epinephrine may decrease the antihypertensive activities of Perindopril.
Ergotamine Ergotamine may decrease the antihypertensive activities of Perindopril.
Nicergoline Nicergoline may decrease the antihypertensive activities of Perindopril.
Methoxamine Methoxamine may decrease the antihypertensive activities of Perindopril.
Trimipramine Trimipramine may decrease the antihypertensive activities of Perindopril.
Alfentanil Alfentanil may decrease the antihypertensive activities of Perindopril.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Perindopril.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Perindopril.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Perindopril.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Perindopril.
Benzphetamine Benzphetamine may decrease the antihypertensive activities of Perindopril.
Ritodrine Ritodrine may decrease the antihypertensive activities of Perindopril.
Bitolterol Bitolterol may decrease the antihypertensive activities of Perindopril.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Perindopril.
Salmeterol Salmeterol may decrease the antihypertensive activities of Perindopril.
Naratriptan Naratriptan may decrease the antihypertensive activities of Perindopril.
Formoterol Formoterol may decrease the antihypertensive activities of Perindopril.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Perindopril.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Perindopril.
Ergoloid mesylate Ergoloid mesylate may decrease the antihypertensive activities of Perindopril.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Perindopril.
Arbutamine Arbutamine may decrease the antihypertensive activities of Perindopril.
Dutasteride Dutasteride may decrease the antihypertensive activities of Perindopril.
Pergolide Pergolide may decrease the antihypertensive activities of Perindopril.
Finasteride Finasteride may decrease the antihypertensive activities of Perindopril.
Ergometrine Ergometrine may decrease the antihypertensive activities of Perindopril.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Perindopril.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Perindopril.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Perindopril.
Mephentermine Mephentermine may decrease the antihypertensive activities of Perindopril.
Procaterol Procaterol may decrease the antihypertensive activities of Perindopril.
Yohimbine Yohimbine may decrease the antihypertensive activities of Perindopril.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Perindopril.
MMDA MMDA may decrease the antihypertensive activities of Perindopril.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Perindopril.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Perindopril.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Perindopril.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Perindopril.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Perindopril.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Perindopril.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Perindopril.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Perindopril.
Periciazine Periciazine may decrease the antihypertensive activities of Perindopril.
Acepromazine Acepromazine may decrease the antihypertensive activities of Perindopril.
Thioproperazine Thioproperazine may decrease the antihypertensive activities of Perindopril.
Zuclopenthixol Zuclopenthixol may decrease the antihypertensive activities of Perindopril.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Perindopril.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Perindopril.
Lysergic acid diethylamide Lysergic acid diethylamide may decrease the antihypertensive activities of Perindopril.
Amineptine Amineptine may decrease the antihypertensive activities of Perindopril.
Dronedarone Dronedarone may decrease the antihypertensive activities of Perindopril.
Flibanserin Flibanserin may decrease the antihypertensive activities of Perindopril.
Iloperidone Iloperidone may decrease the antihypertensive activities of Perindopril.
Indacaterol Indacaterol may decrease the antihypertensive activities of Perindopril.
Amibegron Amibegron may decrease the antihypertensive activities of Perindopril.
Naluzotan Naluzotan may decrease the antihypertensive activities of Perindopril.
Cariprazine Cariprazine may decrease the antihypertensive activities of Perindopril.
Mianserin Mianserin may decrease the antihypertensive activities of Perindopril.
Solabegron Solabegron may decrease the antihypertensive activities of Perindopril.
Asenapine Asenapine may decrease the antihypertensive activities of Perindopril.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Perindopril.
Vilazodone Vilazodone may decrease the antihypertensive activities of Perindopril.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Perindopril.
Xylometazoline Xylometazoline may decrease the antihypertensive activities of Perindopril.
Isometheptene Isometheptene may decrease the antihypertensive activities of Perindopril.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Perindopril.
Naphazoline Naphazoline may decrease the antihypertensive activities of Perindopril.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Perindopril.
Cinitapride Cinitapride may decrease the antihypertensive activities of Perindopril.
Lurasidone Lurasidone may decrease the antihypertensive activities of Perindopril.

Target Protein

Angiotensin-converting enzyme ACE
Secreted frizzled-related protein 4 SFRP4

Referensi & Sumber

Synthesis reference: Michel Vincent, Jean Baliarda, Bernard Marchand, Georges Remond, "Process for the industrial synthesis of perindopril." U.S. Patent US4914214, issued April 03, 1990.
Artikel (PubMed)
  • PMID: 11398915
    Hurst M, Jarvis B: Perindopril: an updated review of its use in hypertension. Drugs. 2001;61(6):867-96.
  • PMID: 15673060
    Jastrzebskal M, Widecka K, Naruszewicz M, Ciechanowicz A, Janczak-Bazan A, Foltynska A, Goracy I, Chetstowski K, Wesotowska T: Effects of perindopril treatment on hemostatic function in patients with essential hypertension in relation to angiotensin converting enzyme (ACE) and plasminogen activator inhibitor-1 (PAI-1) gene polymorphisms. Nutr Metab Cardiovasc Dis. 2004 Oct;14(5):259-69.
  • PMID: 15982858
    Parker E, Aarons L, Rowland M, Resplandy G: The pharmacokinetics of perindoprilat in normal volunteers and patients: influence of age and disease state. Eur J Pharm Sci. 2005 Sep;26(1):104-13.
  • PMID: 12076191
    Simpson D, Noble S, Goa KL: Perindopril: in congestive heart failure. Drugs. 2002;62(9):1367-77; discussion 1378-9.
  • PMID: 15449186
    Yasumatsu R, Nakashima T, Masuda M, Ito A, Kuratomi Y, Nakagawa T, Komune S: 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 Oct;130(10):567-73. Epub 2004 Jul 27.
  • PMID: 11309359
    Yoshiji H, Kuriyama S, Kawata M, Yoshii J, Ikenaka Y, Noguchi R, Nakatani T, Tsujinoue H, Fukui H: The angiotensin-I-converting enzyme inhibitor perindopril suppresses tumor growth and angiogenesis: possible role of the vascular endothelial growth factor. Clin Cancer Res. 2001 Apr;7(4):1073-8.

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