Peringatan Keamanan

The oral LD50 in rats is 173-187mg/kg and the highest known dose an adult human has survived is 10g orally.L8782

Patients experiencing an overdose may present with hypotension, tachycardia, headache, flushing, myocardial ischemia, myocardial infarction, cardiac arrhythmia, and shock.L8782 Overdose can be treated through emptying the gastric contents and administering activated charcoal, though these treatments may cause further arrhythmias and shock.L8782 Supportive and symptomatic treatment should be administered.L8782

Hydralazine

DB01275

small molecule approved

Deskripsi

Originally developed in the 1950s as a malaria treatment, hydralazine showed antihypertensive ability and was soon repurposed.A186841 Hydralazine is a hydrazine derivative vasodilator used alone or as adjunct therapy in the treatment of hypertension and only as adjunct therapy in the treatment of heart failure.A186820,L8782,L8785 Hydralazine is no longer a first line therapy for these indications since the development of newer antihypertensive medications.T691

Hydralazine hydrochloride was FDA approved on 15 January 1953.L8779

Struktur Molekul 2D

Berat 160.1759
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Hydralazine has a half life of 2.2-7.8h in rapid acetylators and 2.0-5.8h in slow acetylators.[A186310,L8782] The half life in heart failure patients is 57-241 minutes with an average of 105 minutes and in hypertensive patients is 200 minutes for rapid acetylators and 297 minutes for slow acetylators.[A186817] Hydralazine is subject to polymorphic acetylation;[A244480] slow acetylators generally have higher plasma levels of hydralazine and require lower doses to maintain control of pressure. However, other factors, such as acetylation being a minor metabolic pathway for hydralazine, will contribute to differences in elimination rates.
Volume Distribusi The volume of distribution is 1.34±0.79L/kg in congestive heart failure patients and 1.98±0.22L/kg in hypertensive patients.[A186817]
Klirens (Clearance) The majority of hydralazine clearance is extrahepatic- 55% for rapid acetylators and 70% for slow acetylators.[A186817] The average clearance in congestive heart failure patients is 1.77±0.48L/kg/h,[A186817] while hypertensive patients have an average clearance of 42.7±8.9mL/min/kg.[A186838]

Absorpsi

Taking oral hydralazine with food improves the bioavailability of the drug.A186835 An intravenous dose of 0.3mg/kg leads to an AUC of 17.5-29.4µM\*min and a 1mg/kg oral dose leads to an AUC of 4.0-30.4µM\*min.A186838 The Cmax of oral hydralazine is 0.12-1.31µM depending on the acetylator status of patients.A186838

Metabolisme

Acetylation is a minor metabolic pathway for hydralazine; the major pathway is hydroxylation followed by glucuronidation.A186310 There are 5 identified metabolic pathways for hydralazine.A186301,A186754,A186316,A186310,A186319,A186769 Hydralazine can be metabolized to phthalazine or ?-ketoglutarate hydrazone.A186301,A186310 These metabolites can be further converted to phthalazinone or hydralazine can be metabolized directly to phthalazinone.A186301,A186310 Hydralazine can undergo a reversible converstion to the active hydralazine acetone hydrazone.A186319,A186769 Hydralazine is spontaneously converted to the active pyruvic acid hydrazone or the pyruvic acid hydrazone tricyclic dehydration product, and these metabolites can convert back and forth between these 2 forms.A186301,A186316 Hydralazine can be converted to hydrazinophthalazinone, which is further converted to the active acetylhydrazinophthalazinone.A186301,A186310 The final metabolic process hydralazine can undergo is the conversion to an unnamed hydralazine metabolite, which is further metabolized to 3-methyl-s-triazolophthalazine (MTP).A186301 MTP can be metabolized to 9-hydroxy-methyltriazolophthalazine or 3-hydroxy-methyltriazolophthalazine; the latter is converted to triazolophthalazine.A186301

Rute Eliminasi

<10% of hydralazine is recovered in the feces; 65-90% is recovered in the urine.A186817

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food increases exposure to hydralazine, though this may not be clinically significant.

Interaksi Obat

1258 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Hydralazine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Hydralazine is combined with Levodopa.
Risperidone Hydralazine may increase the hypotensive activities of Risperidone.
Amifostine Hydralazine may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Hydralazine.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Hydralazine.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Hydralazine.
Obinutuzumab Hydralazine may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Hydralazine.
Rituximab Hydralazine may increase the hypotensive activities of Rituximab.
Midodrine Midodrine may decrease the antihypertensive activities of Hydralazine.
Isoetharine Isoetharine may decrease the antihypertensive activities of Hydralazine.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Hydralazine.
Protriptyline Protriptyline may decrease the antihypertensive activities of Hydralazine.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Hydralazine.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Hydralazine.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Hydralazine.
Droperidol Droperidol may decrease the antihypertensive activities of Hydralazine.
Amoxapine Amoxapine may decrease the antihypertensive activities of Hydralazine.
Doxapram Doxapram may decrease the antihypertensive activities of Hydralazine.
Atropine Atropine may decrease the antihypertensive activities of Hydralazine.
Metaraminol Metaraminol may decrease the antihypertensive activities of Hydralazine.
Epinephrine Epinephrine may decrease the antihypertensive activities of Hydralazine.
Nicergoline Nicergoline may decrease the antihypertensive activities of Hydralazine.
Methoxamine Methoxamine may decrease the antihypertensive activities of Hydralazine.
Propiomazine Propiomazine may decrease the antihypertensive activities of Hydralazine.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Hydralazine.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Hydralazine.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Hydralazine.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Hydralazine.
Ritodrine Ritodrine may decrease the antihypertensive activities of Hydralazine.
Flupentixol Flupentixol may decrease the antihypertensive activities of Hydralazine.
Bitolterol Bitolterol may decrease the antihypertensive activities of Hydralazine.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Hydralazine.
Naratriptan Naratriptan may decrease the antihypertensive activities of Hydralazine.
Formoterol Formoterol may decrease the antihypertensive activities of Hydralazine.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Hydralazine.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Hydralazine.
Arbutamine Arbutamine may decrease the antihypertensive activities of Hydralazine.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Hydralazine.
Fenoterol Fenoterol may decrease the antihypertensive activities of Hydralazine.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Hydralazine.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Hydralazine.
Ephedrine Ephedrine may decrease the antihypertensive activities of Hydralazine.
Mephentermine Mephentermine may decrease the antihypertensive activities of Hydralazine.
Procaterol Procaterol may decrease the antihypertensive activities of Hydralazine.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Hydralazine.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Hydralazine.
Bambuterol Bambuterol may decrease the antihypertensive activities of Hydralazine.
MMDA MMDA may decrease the antihypertensive activities of Hydralazine.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Hydralazine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Hydralazine.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Hydralazine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Hydralazine.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Hydralazine.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Hydralazine.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Hydralazine.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Hydralazine.
Periciazine Periciazine may decrease the antihypertensive activities of Hydralazine.
Acepromazine Acepromazine may decrease the antihypertensive activities of Hydralazine.
Thioproperazine Thioproperazine may decrease the antihypertensive activities of Hydralazine.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Hydralazine.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Hydralazine.
Amineptine Amineptine may decrease the antihypertensive activities of Hydralazine.
Amibegron Amibegron may decrease the antihypertensive activities of Hydralazine.
Naluzotan Naluzotan may decrease the antihypertensive activities of Hydralazine.
Pizotifen Pizotifen may decrease the antihypertensive activities of Hydralazine.
Solabegron Solabegron may decrease the antihypertensive activities of Hydralazine.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Hydralazine.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Hydralazine.
Xylometazoline Xylometazoline may decrease the antihypertensive activities of Hydralazine.
Isometheptene Isometheptene may decrease the antihypertensive activities of Hydralazine.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Hydralazine.
Naphazoline Naphazoline may decrease the antihypertensive activities of Hydralazine.
Saralasin Saralasin may decrease the antihypertensive activities of Hydralazine.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Hydralazine.
Cinitapride Cinitapride may decrease the antihypertensive activities of Hydralazine.
Tyramine Tyramine may decrease the antihypertensive activities of Hydralazine.
Adrafinil Adrafinil may decrease the antihypertensive activities of Hydralazine.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Hydralazine.
Hexoprenaline Hexoprenaline may decrease the antihypertensive activities of Hydralazine.
Etilefrine Etilefrine may decrease the antihypertensive activities of Hydralazine.
Butriptyline Butriptyline may decrease the antihypertensive activities of Hydralazine.
Olodaterol Olodaterol may decrease the antihypertensive activities of Hydralazine.
Dosulepin Dosulepin may decrease the antihypertensive activities of Hydralazine.
Cirazoline Cirazoline may decrease the antihypertensive activities of Hydralazine.
Synephrine Synephrine may decrease the antihypertensive activities of Hydralazine.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Hydralazine.
Iofetamine I-123 Iofetamine I-123 may decrease the antihypertensive activities of Hydralazine.
Racepinephrine Racepinephrine may decrease the antihypertensive activities of Hydralazine.
Amitraz Amitraz may decrease the antihypertensive activities of Hydralazine.
Medetomidine Medetomidine may decrease the antihypertensive activities of Hydralazine.
Xylazine Xylazine may decrease the antihypertensive activities of Hydralazine.
Atipamezole Atipamezole may decrease the antihypertensive activities of Hydralazine.
Ractopamine Ractopamine may decrease the antihypertensive activities of Hydralazine.
Romifidine Romifidine may decrease the antihypertensive activities of Hydralazine.
Detomidine Detomidine may decrease the antihypertensive activities of Hydralazine.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Hydralazine.
Anisodamine Anisodamine may decrease the antihypertensive activities of Hydralazine.
PF-00610355 PF-00610355 may decrease the antihypertensive activities of Hydralazine.

Target Protein

Amine oxidase [copper-containing] 3 AOC3
Hypoxia-inducible factor 1-alpha HIF1A
Prolyl 4-hydroxylase subunit alpha-1 P4HA1

Referensi & Sumber

Synthesis reference: U.S. Patent 2,484,029.
Artikel (PubMed)
  • PMID: 7924901
    Hofstra AH: Metabolism of hydralazine: relevance to drug-induced lupus. Drug Metab Rev. 1994;26(3):485-505. doi: 10.3109/03602539408998315.
  • PMID: -
    Bolattin M, Nandibewoor S, Joshi S, Dixit S, Chimatadar S: Interaction of Hydralazine with Human Serum Albumin and Effect of β-Cyclodextrin on Binding: Insights from Spectroscopic and Molecular Docking Techniques Industrial & Engineering Chemistry Research. 2016 Apr 24;55(19):5454-5464.
  • PMID: 12411398
    Machado JD, Gomez JF, Betancor G, Camacho M, Brioso MA, Borges R: Hydralazine reduces the quantal size of secretory events by displacement of catecholamines from adrenomedullary chromaffin secretory vesicles. Circ Res. 2002 Nov 1;91(9):830-6. doi: 10.1161/01.res.0000039530.30495.6f.
  • PMID: 4584155
    Reidenberg MM, Drayer D, DeMarco AL, Bello CT: Hydralazine elimination in man. Clin Pharmacol Ther. 1973 Nov-Dec;14(6):970-7. doi: 10.1002/cpt1973146970.
  • PMID: 7358814
    Haegele KD, Skrdlant HB, Talseth T, McNay JL, Shepherd AM, Clementi WA: Quantitative analysis of hydralazine pyruvic acid hydrazone, the major plasma metabolite of hydralazine. J Chromatogr. 1980 Jan 4;187(1):171-9. doi: 10.1016/s0021-9673(00)87883-8.
  • PMID: 6177931
    Talseth T, McNay JL, Haegele KD: Hypotensive effect of the hydralazine--acetone hydrazone in conscious rabbits: evidence for its back-conversion to hydralazine in vivo. J Cardiovasc Pharmacol. 1982 May-Jun;4(3):370-4. doi: 10.1097/00005344-198205000-00005.
  • PMID: 7050561
    Reece PA: Hydralazine and related compounds: chemistry, metabolism, and mode of action. Med Res Rev. 1981 Spring;1(1):73-96.
  • PMID: 2600796
    Iwaki M, Ogiso T, Ito Y: Pharmacokinetics and biotransformation of hydralazine acetone hydrazone, a metabolite of hydralazine, in the rat. J Pharm Sci. 1989 Oct;78(10):867-73. doi: 10.1002/jps.2600781018.
Menampilkan 8 dari 16 artikel.
Textbook
  • ISBN: 978-0-323-03961-1
    McInnes G (2007). 84. In Comprehensive Hypertension (pp. 1037-1048). Elsevier.

Contoh Produk & Brand

Produk: 381 • International brands: 8
Produk
  • Apo-hydralazine
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Apo-hydralazine
    Tablet • 25 mg • Oral • Canada • Generic • Approved
  • Apo-hydralazine
    Tablet • 50 mg • Oral • Canada • Generic • Approved
  • Apresoline
    Solution • 20 mg / mL • Intravenous • Canada • Approved
  • Apresoline hydrochloride
    Tablet, coated • 50 mg/1 • Oral • US • Approved
  • Apresoline hydrochloride
    Tablet, coated • 10 mg/1 • Oral • US • Approved
  • Apresoline hydrochloride
    Tablet, coated • 25 mg/1 • Oral • US • Approved
  • Apresoline hydrochloride
    Tablet, coated • 50 mg/1 • Oral • US • Approved
Menampilkan 8 dari 381 produk.
International Brands
  • Alphapress — Alphapharm
  • Aprezin — Johnson
  • Cesoline W — Pharmasant
  • Cesoline Y — Pharmasant
  • Diazide — The Central
  • Hidral — Biocontrol
  • Pressfall — Nisshin Seiyaku
  • Serpathiazide — Washington

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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