Peringatan Keamanan

The oral LD50 in rats is 3541mg/kg and in mice is 1739mg/kg.L8429

Patients experiencing an overdose may present with symptoms of severe hypotension.L8420,L8423 Due to the extensive protein binding of quinapril and the active metabolite quinaprilat, hemodialysis is not expected to remove the drug from circulation.L8420,L8423 Treat patients with symptomatic and supportive measures, including normal saline infusions to restore normal blood pressure.L8420,L8423

Quinapril

DB00881

small molecule approved investigational

Deskripsi

Quinapril is the ethyl ester prodrug of the non-sulfhydryl angiotensin converting enzyme inhibitor quinaprilat.L8420,L8423 It is used to treat hypertension and heart failure.L8420,L8423 ACE inhibitors are commonly used as a first line therapy in the treatment of hypertension, along with thiazide diuretics or beta blockers.A184844

Quinapril was granted FDA approval on 19 November 1991.L8420 A combination tablet with hydrochlorothiazide was also approved on 28 December 1999.L8423

Struktur Molekul 2D

Berat 438.5161
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The active metabolite quinaprilat has an elimination half life of 2.3 hours.[A1329,L8420]
Volume Distribusi The mean volume of distribution of quinaprilat is 13.9L.[A1329]
Klirens (Clearance) The clearance of quinaprilat is 68mL/min.[A1329]

Absorpsi

Quinapril if 50-80% bioavailable.A1329 Quinapril has a Tmax of <1 hour,L8420 while quinaprilat has a Tmax of 2.5h.A1329 The Cmax of quinaprilat is highly variable but reaches 1526ng/mL with an AUC of 2443ng\*h/mL in healthy males given a 10mg dose.A1329 A high fat meal reduces the absorption of quinapril by 25-30%.A1329

Metabolisme

Quinapril is de-esterified to the active quinaprilat or dehydrated to form the inactive PD109488.A1329,A184943 PD109488 can undergo O-deethylation to form another inactive metabolite, PD113413.A1329,A184943

Rute Eliminasi

Quinaprilat is up to 96% eliminated in the urine.L8420 The eliminated metabolites PD109488 and PD113413 account for approximately 6% of a dose of quinapril each.A1329,A184943 A small fraction of the dose recovered in the urine is accounted for by unmetabolized quinapril.A184943

Interaksi Makanan

4 Data
  • 1. Avoid fatty foods.
  • 2. Avoid hypertensive herbs (e.g. bayberry, blue cohosh, cayenne, ephedra, and licorice).
  • 3. Avoid potassium-containing products. Potassium products increase the risk of hyperkalemia.
  • 4. Limit salt intake. Salt may attenuate the antihypertensive effect.

Interaksi Obat

960 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Quinapril is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Quinapril is combined with Levodopa.
Risperidone Quinapril may increase the hypotensive activities of Risperidone.
Alfuzosin Alfuzosin may increase the hypotensive activities of Quinapril.
Amifostine Quinapril may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Quinapril.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Quinapril.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Quinapril.
Obinutuzumab Quinapril may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Quinapril.
Rituximab Quinapril may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Quinapril.
Phentermine Phentermine may decrease the antihypertensive activities of Quinapril.
Midodrine Midodrine may decrease the antihypertensive activities of Quinapril.
Eletriptan Eletriptan may decrease the antihypertensive activities of Quinapril.
Isoetharine Isoetharine may decrease the antihypertensive activities of Quinapril.
Methysergide Methysergide may decrease the antihypertensive activities of Quinapril.
Cabergoline Cabergoline may decrease the antihypertensive activities of Quinapril.
Atomoxetine Atomoxetine may decrease the antihypertensive activities of Quinapril.
Etomidate Etomidate may decrease the antihypertensive activities of Quinapril.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Quinapril.
Dihydroergotamine Dihydroergotamine may decrease the antihypertensive activities of Quinapril.
Amitriptyline Amitriptyline may decrease the antihypertensive activities of Quinapril.
Protriptyline Protriptyline may decrease the antihypertensive activities of Quinapril.
Methylergometrine Methylergometrine may decrease the antihypertensive activities of Quinapril.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Quinapril.
Mirtazapine Mirtazapine may decrease the antihypertensive activities of Quinapril.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Quinapril.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Quinapril.
Promazine Promazine may decrease the antihypertensive activities of Quinapril.
Droperidol Droperidol may decrease the antihypertensive activities of Quinapril.
Buspirone Buspirone may decrease the antihypertensive activities of Quinapril.
Nortriptyline Nortriptyline may decrease the antihypertensive activities of Quinapril.
Amoxapine Amoxapine may decrease the antihypertensive activities of Quinapril.
Doxapram Doxapram may decrease the antihypertensive activities of Quinapril.
Atropine Atropine may decrease the antihypertensive activities of Quinapril.
Lisuride Lisuride may decrease the antihypertensive activities of Quinapril.
Metaraminol Metaraminol may decrease the antihypertensive activities of Quinapril.
Trazodone Trazodone may decrease the antihypertensive activities of Quinapril.
Epinephrine Epinephrine may decrease the antihypertensive activities of Quinapril.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Quinapril.
Ergotamine Ergotamine may decrease the antihypertensive activities of Quinapril.
Nicergoline Nicergoline may decrease the antihypertensive activities of Quinapril.
Methoxamine Methoxamine may decrease the antihypertensive activities of Quinapril.
Trimipramine Trimipramine may decrease the antihypertensive activities of Quinapril.
Propiomazine Propiomazine may decrease the antihypertensive activities of Quinapril.
Alfentanil Alfentanil may decrease the antihypertensive activities of Quinapril.
Fentanyl Fentanyl may decrease the antihypertensive activities of Quinapril.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Quinapril.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Quinapril.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Quinapril.
Dobutamine Dobutamine may decrease the antihypertensive activities of Quinapril.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Quinapril.
Benzphetamine Benzphetamine may decrease the antihypertensive activities of Quinapril.
Ritodrine Ritodrine may decrease the antihypertensive activities of Quinapril.
Terbutaline Terbutaline may decrease the antihypertensive activities of Quinapril.
Flupentixol Flupentixol may decrease the antihypertensive activities of Quinapril.
Bitolterol Bitolterol may decrease the antihypertensive activities of Quinapril.
Almotriptan Almotriptan may decrease the antihypertensive activities of Quinapril.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Quinapril.
Salmeterol Salmeterol may decrease the antihypertensive activities of Quinapril.
Naratriptan Naratriptan may decrease the antihypertensive activities of Quinapril.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Quinapril.
Formoterol Formoterol may decrease the antihypertensive activities of Quinapril.
Dopamine Dopamine may decrease the antihypertensive activities of Quinapril.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Quinapril.
Albuterol Salbutamol may decrease the antihypertensive activities of Quinapril.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Quinapril.
Ergoloid mesylate Ergoloid mesylate may decrease the antihypertensive activities of Quinapril.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Quinapril.
Arbutamine Arbutamine may decrease the antihypertensive activities of Quinapril.
Dutasteride Dutasteride may decrease the antihypertensive activities of Quinapril.
Doxepin Doxepin may decrease the antihypertensive activities of Quinapril.
Nefazodone Nefazodone may decrease the antihypertensive activities of Quinapril.
Desipramine Desipramine may decrease the antihypertensive activities of Quinapril.
Pergolide Pergolide may decrease the antihypertensive activities of Quinapril.
Finasteride Finasteride may decrease the antihypertensive activities of Quinapril.
Ergometrine Ergometrine may decrease the antihypertensive activities of Quinapril.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Quinapril.
Paliperidone Paliperidone may decrease the antihypertensive activities of Quinapril.
Arformoterol Arformoterol may decrease the antihypertensive activities of Quinapril.
Fenoterol Fenoterol may decrease the antihypertensive activities of Quinapril.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Quinapril.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Quinapril.
Ephedrine Ephedrine may decrease the antihypertensive activities of Quinapril.
Mephentermine Mephentermine may decrease the antihypertensive activities of Quinapril.
Procaterol Procaterol may decrease the antihypertensive activities of Quinapril.
Yohimbine Yohimbine may decrease the antihypertensive activities of Quinapril.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Quinapril.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Quinapril.
Bambuterol Bambuterol may decrease the antihypertensive activities of Quinapril.
MMDA MMDA may decrease the antihypertensive activities of Quinapril.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Quinapril.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Quinapril.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Quinapril.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Quinapril.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Quinapril.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Quinapril.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Quinapril.
Metamfetamine Metamfetamine may decrease the antihypertensive activities of Quinapril.

Target Protein

Angiotensin-converting enzyme ACE

Referensi & Sumber

Synthesis reference: Om P. Goel, Uldis Krolls, "Crystalline quinapril and a process for producing the same." U.S. Patent US4761479, issued August, 1982.
Artikel (PubMed)
  • PMID: 19761414
    Kieback AG, Felix SB, Reffelmann T: Quinaprilat: a review of its pharmacokinetics, pharmacodynamics, toxicological data and clinical application. Expert Opin Drug Metab Toxicol. 2009 Oct;5(10):1337-47. doi: 10.1517/17425250903282773.
  • PMID: 14747423
    Tsikouris JP, Suarez JA, Meyerrose GE, Ziska M, Fike D, Smith J: Questioning a class effect: does ACE inhibitor tissue penetration influence the degree of fibrinolytic balance alteration following an acute myocardial infarction? J Clin Pharmacol. 2004 Feb;44(2):150-7.
  • PMID: 2539761
    Kaplan HR, Taylor DG, Olson SC, Andrews LK: Quinapril--a preclinical review of the pharmacology, pharmacokinetics, and toxicology. Angiology. 1989 Apr;40(4 Pt 2):335-50. doi: 10.1177/000331978904000403.
  • PMID: 8891468
    Goa KL, Balfour JA, Zuanetti G: Lisinopril. A review of its pharmacology and clinical efficacy in the early management of acute myocardial infarction. Drugs. 1996 Oct;52(4):564-88. doi: 10.2165/00003495-199652040-00011.
  • PMID: 29667175
    Wright JM, Musini VM, Gill R: First-line drugs for hypertension. Cochrane Database Syst Rev. 2018 Apr 18;4:CD001841. doi: 10.1002/14651858.CD001841.pub3.

Contoh Produk & Brand

Produk: 249 • International brands: 6
Produk
  • Accupril
    Tablet, film coated • 5 mg/1 • Oral • US • Approved
  • Accupril
    Tablet, film coated • 10 mg/1 • Oral • US • Approved
  • Accupril
    Tablet, film coated • 20 mg/1 • Oral • US • Approved
  • Accupril
    Tablet, film coated • 40 mg/1 • Oral • US • Approved
  • Accupril
    Tablet, film coated • 10 mg/1 • Oral • US • Approved
  • Accupril
    Tablet, film coated • 20 mg/1 • Oral • US • Approved
  • Accupril
    Tablet, film coated • 40 mg/1 • Oral • US • Approved
  • Accupril
    Tablet, film coated • 5 mg/1 • Oral • US • Approved
Menampilkan 8 dari 249 produk.
International Brands
  • Accuprin — Pfizer (Italy)
  • Accupro — Pfizer (Austria, Denmark, Finland, Germany, Hungary, Ireland, Sweden, Switzerland, United Kingdom, Ukraine), Godecke (Czech Republic, Germany, Poland, Russia), Parke, Davis (Germany)
  • Acequin
  • Acuitel
  • Korec
  • Quinazil

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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