Peringatan Keamanan

Symptoms of overdose include dyspnea, hypotension or hypertension, rapid weak pulse, delirium, nausea, vomiting, and bradycardia. The excessive use of ergoloid mesylate can lead to ergotism.T90 To know more about the individual components of the ergoloid mixture, please visit DB11274, DB11273 and DB13345.

Ergoloid mesylate

DB01049

small molecule approved

Deskripsi

Ergoloid Mesylate is an equiproportional preparation of three different ergotamantriones: dihydroergocornine, dihydroergocristine, and dihydroergocryptine.A32912 All these components are produced by the fungus Claviceps purpurea and are all derivatives of the tetracyclic compound 6-methylergonovine.T90 The derivatives of this fungus are identified to be about 350 different substances from which the components of the ergoloid mesylate mixture are composed of the dihydrogenated ergot alkaloid derivatives.A32914 The mixture of ergoloid mesylate was first developed by Novartis and FDA approved on November 5, 1953, but this specific formulation is now discontinued.L2639Later in 1991, the mixture of ergoloid mesylates was retaken by Sun Pharmaceutical Industries and approved by the FDA.L2640 To know more about the individual components of the ergoloid mixture, please visit DB11275, DB11274, DB11273 and DB13345.

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The reported plasma half-life of ergoloid mesylate is 3.5 hours while the terminal half-life is of 13 hours.[T53] To know more about the individual components of the ergoloid mixture, please visit [DB11274].
Volume Distribusi The volume of distribution is about 2 L/kg.[T90] To know more about the individual components of the ergoloid mixture, please visit [DB11274] and [DB13345].
Klirens (Clearance) To know more about the individual components of the ergoloid mixture, please visit [DB11274] and [DB13345].

Absorpsi

The maximal plasma concentration of the components of the mixture of ergoloid mesylates is approximately 0.04 mcg/l. The analysis of the concentration of the major metabolites of each component indicates that all ergoloid mesylate are rapidly transformed after absorption. This finding is supported as they were found in one order of magnitude higher in concentration when compared to the original form.A32914 Ergoloid mesylate seems to have a very low absorption of only 25%. From this absorption by the GI tract, approximately 50% of the absorbed dose is eliminated by first-pass metabolism. After absorption, the maximal plasma concentration is attained after 3-4 hours and the oral bioavailability is very low.T53 Simultaneous food ingestion has no effect on the extent of absorption but it does lower the absorption rate.A32937 To know more about the individual components of the ergoloid mixture, please visit DB11274, DB11273 and DB13345.

Metabolisme

Most of the metabolism of ergoloid mesylate is hepatic and it is performed very rapidly after absorption. After exposition in vitro, the major metabolites identified are hydroxy-dihydroergocornine, hydroxy-dihydroergocryptine and hydroxy-dihydroergocristine.A32926 All metabolic transformations seem to be related to the activity of the cytochrome CYP3A4.L2681 To know more about the individual components of the ergoloid mixture, please visit DB11274, DB11273 and DB13345.

Rute Eliminasi

The ergoloid mesylate mixture is mainly excreted via bile in feces. The ratio of the eliminated dose via urine after intravenous and oral administration is 8.4% and 2% respectively.T53 Urinary excretion of the unchanged drug is very small and bile excretion is represented mainly by ergot metabolites conformed as conjugated compounds.T191 To know more about the individual components of the ergoloid mixture, please visit DB11274, DB11273 and DB13345.

Interaksi Makanan

1 Data
  • 1. Take with or without food. Taking ergoloid mesylate with food may reduce gastrointestinal upset.

Interaksi Obat

1224 Data
Valsartan Ergoloid mesylate may decrease the antihypertensive activities of Valsartan.
Ramipril Ergoloid mesylate may decrease the antihypertensive activities of Ramipril.
Remikiren Ergoloid mesylate may decrease the antihypertensive activities of Remikiren.
Torasemide Ergoloid mesylate may decrease the antihypertensive activities of Torasemide.
Guanadrel Ergoloid mesylate may decrease the antihypertensive activities of Guanadrel.
Olmesartan Ergoloid mesylate may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Ergoloid mesylate may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Ergoloid mesylate may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Ergoloid mesylate may decrease the antihypertensive activities of Minoxidil.
Treprostinil Ergoloid mesylate may decrease the antihypertensive activities of Treprostinil.
Bendroflumethiazide Ergoloid mesylate may decrease the antihypertensive activities of Bendroflumethiazide.
Prazosin Ergoloid mesylate may decrease the antihypertensive activities of Prazosin.
Fosinopril Ergoloid mesylate may decrease the antihypertensive activities of Fosinopril.
Trandolapril Ergoloid mesylate may decrease the antihypertensive activities of Trandolapril.
Metolazone Ergoloid mesylate may decrease the antihypertensive activities of Metolazone.
Benazepril Ergoloid mesylate may decrease the antihypertensive activities of Benazepril.
Cyclothiazide Ergoloid mesylate may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Ergoloid mesylate may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Ergoloid mesylate may decrease the antihypertensive activities of Mecamylamine.
Moexipril Ergoloid mesylate may decrease the antihypertensive activities of Moexipril.
Lisinopril Ergoloid mesylate may decrease the antihypertensive activities of Lisinopril.
Hydroflumethiazide Ergoloid mesylate may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Ergoloid mesylate may decrease the antihypertensive activities of Cryptenamine.
Perindopril Ergoloid mesylate may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Ergoloid mesylate may decrease the antihypertensive activities of Candesartan cilexetil.
Eprosartan Ergoloid mesylate may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Ergoloid mesylate may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Ergoloid mesylate may decrease the antihypertensive activities of Quinapril.
Telmisartan Ergoloid mesylate may decrease the antihypertensive activities of Telmisartan.
Hydrochlorothiazide Ergoloid mesylate may decrease the antihypertensive activities of Hydrochlorothiazide.
Trichlormethiazide Ergoloid mesylate may decrease the antihypertensive activities of Trichlormethiazide.
Deserpidine Ergoloid mesylate may decrease the antihypertensive activities of Deserpidine.
Pentolinium Ergoloid mesylate may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Ergoloid mesylate may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Ergoloid mesylate may decrease the antihypertensive activities of Diazoxide.
Bretylium Ergoloid mesylate may decrease the antihypertensive activities of Bretylium.
Terazosin Ergoloid mesylate may decrease the antihypertensive activities of Terazosin.
Captopril Ergoloid mesylate may decrease the antihypertensive activities of Captopril.
Epoprostenol Ergoloid mesylate may decrease the antihypertensive activities of Epoprostenol.
Polythiazide Ergoloid mesylate may decrease the antihypertensive activities of Polythiazide.
Cilazapril Ergoloid mesylate may decrease the antihypertensive activities of Cilazapril.
Saprisartan Ergoloid mesylate may decrease the antihypertensive activities of Saprisartan.
Spirapril Ergoloid mesylate may decrease the antihypertensive activities of Spirapril.
Tienilic acid Ergoloid mesylate may decrease the antihypertensive activities of Tienilic acid.
Debrisoquine Ergoloid mesylate may decrease the antihypertensive activities of Debrisoquine.
Diethylnorspermine Ergoloid mesylate may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Ergoloid mesylate may decrease the antihypertensive activities of Temocapril.
Trimazosin Ergoloid mesylate may decrease the antihypertensive activities of Trimazosin.
Nicorandil Ergoloid mesylate may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Ergoloid mesylate may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Ergoloid mesylate may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Ergoloid mesylate may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Ergoloid mesylate may decrease the antihypertensive activities of Imidapril.
BQ-123 Ergoloid mesylate may decrease the antihypertensive activities of BQ-123.
Cicletanine Ergoloid mesylate may decrease the antihypertensive activities of Cicletanine.
Dihydralazine Ergoloid mesylate may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Ergoloid mesylate may decrease the antihypertensive activities of Zofenopril.
Guanoxan Ergoloid mesylate may decrease the antihypertensive activities of Guanoxan.
Delapril Ergoloid mesylate may decrease the antihypertensive activities of Delapril.
Vincamine Ergoloid mesylate may decrease the antihypertensive activities of Vincamine.
Linsidomine Ergoloid mesylate may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Ergoloid mesylate may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Ergoloid mesylate may decrease the antihypertensive activities of Tolonidine.
Endralazine Ergoloid mesylate may decrease the antihypertensive activities of Endralazine.
Cadralazine Ergoloid mesylate may decrease the antihypertensive activities of Cadralazine.
Cyclopenthiazide Ergoloid mesylate may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Ergoloid mesylate may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Ergoloid mesylate may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Ergoloid mesylate may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Ergoloid mesylate may decrease the antihypertensive activities of Guanoclor.
Muzolimine Ergoloid mesylate may decrease the antihypertensive activities of Muzolimine.
Xipamide Ergoloid mesylate may decrease the antihypertensive activities of Xipamide.
Candesartan Ergoloid mesylate may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Ergoloid mesylate may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Ergoloid mesylate may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Ergoloid mesylate may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Ergoloid mesylate may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Ergoloid mesylate may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Ergoloid mesylate may decrease the antihypertensive activities of Quinaprilat.
Furosemide Ergoloid mesylate may decrease the antihypertensive activities of Furosemide.
Enalapril Ergoloid mesylate may decrease the antihypertensive activities of Enalapril.
Amlodipine Ergoloid mesylate may decrease the antihypertensive activities of Amlodipine.
Nimodipine Ergoloid mesylate may decrease the antihypertensive activities of Nimodipine.
Nisoldipine Ergoloid mesylate may decrease the antihypertensive activities of Nisoldipine.
Lercanidipine Ergoloid mesylate may decrease the antihypertensive activities of Lercanidipine.
Bosentan Ergoloid mesylate may decrease the antihypertensive activities of Bosentan.
Doxazosin Ergoloid mesylate may decrease the antihypertensive activities of Doxazosin.
Losartan Ergoloid mesylate may decrease the antihypertensive activities of Losartan.
Eplerenone Ergoloid mesylate may decrease the antihypertensive activities of Eplerenone.
Indapamide Ergoloid mesylate may decrease the antihypertensive activities of Indapamide.
Tadalafil Ergoloid mesylate may decrease the antihypertensive activities of Tadalafil.
Felodipine Ergoloid mesylate may decrease the antihypertensive activities of Felodipine.
Irbesartan Ergoloid mesylate may decrease the antihypertensive activities of Irbesartan.
Nitrendipine Ergoloid mesylate may decrease the antihypertensive activities of Nitrendipine.
Guanethidine Ergoloid mesylate may decrease the antihypertensive activities of Guanethidine.
Bepridil Ergoloid mesylate may decrease the antihypertensive activities of Bepridil.
Hydralazine Ergoloid mesylate may decrease the antihypertensive activities of Hydralazine.
Mibefradil Ergoloid mesylate may decrease the antihypertensive activities of Mibefradil.
Sitaxentan Ergoloid mesylate may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Ergoloid mesylate may decrease the antihypertensive activities of Ambrisentan.

Target Protein

Dopamine receptor DRD1
Alpha adrenergic receptor ADRA1A
Beta adrenergic receptor ADRB1
Serotonin Receptors HTR1A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 2082953
    Thompson TL 2nd, Filley CM, Mitchell WD, Culig KM, LoVerde M, Byyny RL: Lack of efficacy of hydergine in patients with Alzheimer's disease. N Engl J Med. 1990 Aug 16;323(7):445-8. doi: 10.1056/NEJM199008163230704.
  • PMID: 9787282
    Delagarza VW: New drugs for Alzheimer's disease. Am Fam Physician. 1998 Oct 1;58(5):1175-82.
  • PMID: 13209453
    PERCHESON PB, CARROLL JJ: The use of hydergine in obstetrics. Can Med Assoc J. 1954 Dec;71(6):588-94.
  • PMID: 17941060
    Bicalho B, Giolo JM, Lilla S, De Nucci G: Identification and human pharmacokinetics of dihydroergotoxine metabolites in man: preliminary results. Biopharm Drug Dispos. 2008 Jan;29(1):17-28. doi: 10.1002/bdd.585.
  • PMID: 3207855
    Schran HF, McDonald S, Lehr R: Pharmacokinetics and bioavailability of ergoloid mesylates. Biopharm Drug Dispos. 1988 Jul-Aug;9(4):349-61. doi: 10.1002/bod.2510090404.
Textbook
  • Seyffart G. (1992). Drug dosage in renal insufficiency (2nd ed.). Springer Science+Business Media Dordrecht.
  • Pillay V.V. (2013). Modern medical toxicology (4th ed.). Jaypee Brothers.
  • ISBN: 978-0-470-33447-4
    Barceloux D. (2008). Medical toxicology of natural substances. Wiley.
  • ISBN: 978-3-642-66777-0
    Berde B. and Schild H. (1978). Ergot alkaloids and related compounds. Springer-Verlag.
Attachment

Contoh Produk & Brand

Produk: 4 • International brands: 4
Produk
  • Hydergine
    Tablet • 1 mg/1 • Oral • US • Approved
  • Hydergine
    Liquid • 1 mg/1mL • Oral • US • Approved
  • Hydergine LC
    Capsule, liquid filled • 1 mg/1 • Oral • US • Approved
  • Hydergine Tablets, 1mg
    Tablet • 1 mg • Oral • Canada • Approved
International Brands
  • Alkergot — Eon Labs
  • Circanol — 3M
  • Deapril — Bristol Myers Squibb
  • Gerimal

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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