Peringatan Keamanan

Adverse experiences occurring in 0.5 to 1.0 percent of patients in controlled clinical trials included: myocardial infarction, fatigue, dizziness, fever, rash and constipation.
Angioedema has also been reported in patients receiving enalaprilat, with an incidence higher in black than in non-black patients. Angioedema associated with laryngeal edema may be fatal. If angioedema of the face, extremities, lips, tongue, glottis and/or larynx occurs, treatment with enalaprilat should be discontinued and appropriate therapy instituted immediately .

Rarer adverse effects that are less likely, but should be monitored for, include development of anaphylaxis, hypotension, agranulocytosis, hepatic failure, hyperkalemia, and persistent cough.

Furthermore, ACE inhibitors should be avoided during pregnancy as they can cause fetal and neonatal morbidity and death. When pregnancy is detected, ACE inhibitors should be discontinued as soon as possible. Use during the second and third trimesters of pregnancy has been associated with fetal and neonatal injury, including hypotension, neonatal skull hypoplasia, anuria, reversible or irreversible renal failure, and death.

Enalaprilat

DB09477

small molecule approved

Deskripsi

Enalaprilat is the active metabolite of the orally available pro-drug, enalapril. Used in the treatment of hypertension, enalapril is an ACE inhibitor that prevents Angiotensin Converting Enzyme (ACE) from transforming angiotensin I into angiotensin II. As angiotensin II is responsible for vasoconstriction and sodium reabsorption in the proximal tubule of the kidney, down-regulation of this protein results in reduced blood pressure and blood fluid volume. Enalaprilat was originally created to overcome the limitations of the first ACE inhibitor, captopril, which had numerous side effects and left a metallic taste in the mouth. Removal of the problematic thiol group from captopril resulted in enalaprilat, which was then modified further with an ester to create the orally available pro-drug enalapril.

Enalaprilat is poorly orally available and is therefore only available as an intravenous injection for the treatment of hypertension when oral therapy is not possible.

Struktur Molekul 2D

Berat 348.3936
Wujud -

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 11 hr
Volume Distribusi -
Klirens (Clearance) The disposition of enalaprilat in patients with renal insufficiency is similar to that in patients with normal renal function until the glomerular filtration rate is 30 mL/min or less. Renal clearance was 158 ± 47 ml/min.

Absorpsi

Enalaprilat is poorly absorbed following oral administration, and is therefore only available as an intravenous injection.

Metabolisme

Both enalapril and enalaprilat undergo renal excretion without further metabolism.

Rute Eliminasi

Excretion of enalaprilat is primarily renal with more than 90 percent of an administered dose recovered in the urine as unchanged drug within 24 hours.

Interaksi Obat

1303 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Enalaprilat is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Enalaprilat is combined with Levodopa.
Risperidone Enalaprilat may increase the hypotensive activities of Risperidone.
Alfuzosin Alfuzosin may increase the hypotensive activities of Enalaprilat.
Amifostine Enalaprilat may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Enalaprilat.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Enalaprilat.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Enalaprilat.
Obinutuzumab Enalaprilat may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Enalaprilat.
Rituximab Enalaprilat may increase the hypotensive activities of Rituximab.
Phentermine Phentermine may decrease the antihypertensive activities of Enalaprilat.
Midodrine Midodrine may decrease the antihypertensive activities of Enalaprilat.
Eletriptan Eletriptan may decrease the antihypertensive activities of Enalaprilat.
Isoetharine Isoetharine may decrease the antihypertensive activities of Enalaprilat.
Methysergide Methysergide may decrease the antihypertensive activities of Enalaprilat.
Cabergoline Cabergoline may decrease the antihypertensive activities of Enalaprilat.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Enalaprilat.
Dihydroergotamine Dihydroergotamine may decrease the antihypertensive activities of Enalaprilat.
Protriptyline Protriptyline may decrease the antihypertensive activities of Enalaprilat.
Methylergometrine Methylergometrine may decrease the antihypertensive activities of Enalaprilat.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Enalaprilat.
Mirtazapine Mirtazapine may decrease the antihypertensive activities of Enalaprilat.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Enalaprilat.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Enalaprilat.
Promazine Promazine may decrease the antihypertensive activities of Enalaprilat.
Droperidol Droperidol may decrease the antihypertensive activities of Enalaprilat.
Nortriptyline Nortriptyline may decrease the antihypertensive activities of Enalaprilat.
Amoxapine Amoxapine may decrease the antihypertensive activities of Enalaprilat.
Doxapram Doxapram may decrease the antihypertensive activities of Enalaprilat.
Atropine Atropine may decrease the antihypertensive activities of Enalaprilat.
Lisuride Lisuride may decrease the antihypertensive activities of Enalaprilat.
Metaraminol Metaraminol may decrease the antihypertensive activities of Enalaprilat.
Trazodone Trazodone may decrease the antihypertensive activities of Enalaprilat.
Epinephrine Epinephrine may decrease the antihypertensive activities of Enalaprilat.
Ergotamine Ergotamine may decrease the antihypertensive activities of Enalaprilat.
Nicergoline Nicergoline may decrease the antihypertensive activities of Enalaprilat.
Methoxamine Methoxamine may decrease the antihypertensive activities of Enalaprilat.
Trimipramine Trimipramine may decrease the antihypertensive activities of Enalaprilat.
Propiomazine Propiomazine may decrease the antihypertensive activities of Enalaprilat.
Alfentanil Alfentanil may decrease the antihypertensive activities of Enalaprilat.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Enalaprilat.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Enalaprilat.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Enalaprilat.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Enalaprilat.
Benzphetamine Benzphetamine may decrease the antihypertensive activities of Enalaprilat.
Ritodrine Ritodrine may decrease the antihypertensive activities of Enalaprilat.
Flupentixol Flupentixol may decrease the antihypertensive activities of Enalaprilat.
Bitolterol Bitolterol may decrease the antihypertensive activities of Enalaprilat.
Oxymetazoline Oxymetazoline may decrease the antihypertensive activities of Enalaprilat.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Enalaprilat.
Salmeterol Salmeterol may decrease the antihypertensive activities of Enalaprilat.
Naratriptan Naratriptan may decrease the antihypertensive activities of Enalaprilat.
Formoterol Formoterol may decrease the antihypertensive activities of Enalaprilat.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Enalaprilat.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Enalaprilat.
Ergoloid mesylate Ergoloid mesylate may decrease the antihypertensive activities of Enalaprilat.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Enalaprilat.
Arbutamine Arbutamine may decrease the antihypertensive activities of Enalaprilat.
Dutasteride Dutasteride may decrease the antihypertensive activities of Enalaprilat.
Pergolide Pergolide may decrease the antihypertensive activities of Enalaprilat.
Finasteride Finasteride may decrease the antihypertensive activities of Enalaprilat.
Ergometrine Ergometrine may decrease the antihypertensive activities of Enalaprilat.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Enalaprilat.
Fenoterol Fenoterol may decrease the antihypertensive activities of Enalaprilat.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Enalaprilat.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Enalaprilat.
Ephedrine Ephedrine may decrease the antihypertensive activities of Enalaprilat.
Mephentermine Mephentermine may decrease the antihypertensive activities of Enalaprilat.
Procaterol Procaterol may decrease the antihypertensive activities of Enalaprilat.
Yohimbine Yohimbine may decrease the antihypertensive activities of Enalaprilat.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Enalaprilat.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Enalaprilat.
Bambuterol Bambuterol may decrease the antihypertensive activities of Enalaprilat.
MMDA MMDA may decrease the antihypertensive activities of Enalaprilat.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Enalaprilat.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Enalaprilat.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Enalaprilat.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Enalaprilat.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Enalaprilat.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Enalaprilat.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Enalaprilat.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Enalaprilat.
Solifenacin Solifenacin may decrease the antihypertensive activities of Enalaprilat.
Periciazine Periciazine may decrease the antihypertensive activities of Enalaprilat.
Acepromazine Acepromazine may decrease the antihypertensive activities of Enalaprilat.
Thioproperazine Thioproperazine may decrease the antihypertensive activities of Enalaprilat.
Zuclopenthixol Zuclopenthixol may decrease the antihypertensive activities of Enalaprilat.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Enalaprilat.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Enalaprilat.
Lysergic acid diethylamide Lysergic acid diethylamide may decrease the antihypertensive activities of Enalaprilat.
Amineptine Amineptine may decrease the antihypertensive activities of Enalaprilat.
Dronedarone Dronedarone may decrease the antihypertensive activities of Enalaprilat.
Flibanserin Flibanserin may decrease the antihypertensive activities of Enalaprilat.
Iloperidone Iloperidone may decrease the antihypertensive activities of Enalaprilat.
Indacaterol Indacaterol may decrease the antihypertensive activities of Enalaprilat.
Amibegron Amibegron may decrease the antihypertensive activities of Enalaprilat.
Naluzotan Naluzotan may decrease the antihypertensive activities of Enalaprilat.
Cariprazine Cariprazine may decrease the antihypertensive activities of Enalaprilat.
Mianserin Mianserin may decrease the antihypertensive activities of Enalaprilat.

Target Protein

Angiotensin-converting enzyme ACE
B1 bradykinin receptor BDKRB1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 6301792
    Ulm EH: Enalapril maleate (MK-421), a potent, nonsulfhydryl angiotensin-converting enzyme inhibitor: absorption, disposition, and metabolism in man. Drug Metab Rev. 1983;14(1):99-110.
  • PMID: 6099737
    Davies RO, Gomez HJ, Irvin JD, Walker JF: An overview of the clinical pharmacology of enalapril. Br J Clin Pharmacol. 1984;18 Suppl 2:215S-229S.

Contoh Produk & Brand

Produk: 16 • International brands: 0
Produk
  • Enalaprilat
    Injection • 1.25 mg/1mL • Intravenous • US • Generic • Approved
  • Enalaprilat
    Injection • 2.5 mg/2mL • Intravenous • US • Generic • Approved
  • Enalaprilat
    Injection • 1.25 mg/1mL • Intravenous • US • Generic • Approved
  • Enalaprilat
    Injection • 1.25 mg/1mL • Intravenous • US • Generic • Approved
  • Enalaprilat
    Injection • 1.25 mg/1mL • Intravenous • US • Generic • Approved
  • Enalaprilat
    Injection • 1.25 mg/1mL • Intravenous • US • Generic • Approved
  • Enalaprilat
    Injection • 2.5 mg/2mL • Intravenous • US • Generic • Approved
  • Enalaprilat
    Injection, solution • 1.25 mg/1mL • Intravenous • US • Approved
Menampilkan 8 dari 16 produk.

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