Peringatan Keamanan

Alpha-dihydroergocryptine does not have effect in fertility and it does not present mutagenic potential.^A33005 To know more about the ergoloid mesylate mixture please visit DB01049.

Dihydro-alpha-ergocryptine

DB11274

small molecule approved

Deskripsi

Alpha-dihydroergocryptine is usually referred to the mixture of the alpha and beta dihydroergocryptine. These two compounds are differentiated in the position of a methyl group. This structural difference is due to a proteinogenic amino acid replacement from leucine to isoleucine.T195 Both compounds are hydrogenated ergot derivatives. Alpha-dihydroergocryptine approved drug product is as a part of an ergoloid mixture. To know more about this mixture, please visit DB01049

Struktur Molekul 2D

Berat 577.726

Wujud solid

Peta Jejaring Molekuler

Obat Target Gen Interaksi Enzim Transporter Carrier

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

1. Pendahuluan & Konsep

Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).

2. Sumber Data (Validasi)

Data Obat: Diekstraksi dari elemen drugbank-id dan name pada skema XML DrugBank.
Target Protein: Diambil dari elemen targets/target yang memuat polipeptida sasaran.
Genetik: Disinkronisasi dari sub-elemen gene-name dan varian snp-effects.
Genetik: Jumlah titik node dibatasi pada maksimal 10 (Slice=10) interaksi untuk menghindari tumpukan data.

3. Algoritma Visualisasi

Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.

4. Legenda Visual

Obat Utama (Pusat Analisis)

Target Protein (Mekanisme)

Gen (Faktor Genetik)

Metode ini mendukung analisis Precision Medicine dan evaluasi risiko Drug-Drug Interaction (DDI).

Profil Farmakokinetik

Waktu Paruh (Half-Life) Alpha-dihydroergocryptine has been studied in Parkinson disease models and it has shown a half-life of 12-16 hours.[A32986] To know more about the ergoloid mesylate mixture please visit [DB01049].

Volume Distribusi In preclinical studies, the volume of distribution after intravenous or oral administration was registered to be 11.054 L and 218.630 L respectively.[A33003] To know more about the ergoloid mesylate mixture please visit [DB01049].

Klirens (Clearance) In preclinical studies, the clearance rate after intravenous or oral administration was registered to be 1.129 L/h and 25.98 L/h respectively.[A33003] To know more about the ergoloid mesylate mixture please visit [DB01049].

Absorpsi

Alpha-dihydroergocryptine is rapidly absorbed but it presents a very low bioavailability as it is part of a first-pass hepatic metabolism and thus less of 5% of the administered dose reaches blood circulation. The peak plasma concentration is attained after 30-120 minutes. The absorption of alpha-dihydroergocryptine is not affected by the co-administration with food.^A32987 When administered in repeated oral doses the Cmax after 1 hour was registered to be 2157 pg/ml.^A32994 To know more about the ergoloid mesylate mixture please visit DB01049.

Metabolisme

Alpha-dihydroergocryptine presents a linear metabolism with the formation of active metabolites and the metabolism kinetics of this compound has no interference with L-dopa.^A32996 It is highly metabolized with a rate of 2.4 ng/min/mg protein in the microsomal system and a formation of eight different metabolites.^A33000 the metabolism of alpha-dihydroergocryptine seems to be highly marked by the action of CYP 3A4.^A33001 To know more about the ergoloid mesylate mixture please visit DB01049.

Rute Eliminasi

Alpha-dihydroergocryptine is eliminated mainly by feces^A32996 and to present a very low urinary excretion.^A33002 To know more about the ergoloid mesylate mixture please visit DB01049.

Interaksi Obat

106 Data

Pitolisant	The serum concentration of Dihydro-alpha-ergocryptine can be decreased when it is combined with Pitolisant.
Metreleptin	The metabolism of Dihydro-alpha-ergocryptine can be increased when combined with Metreleptin.
Cenobamate	The serum concentration of Dihydro-alpha-ergocryptine can be decreased when it is combined with Cenobamate.
Ritonavir	The serum concentration of Dihydro-alpha-ergocryptine can be increased when it is combined with Ritonavir.
Haloperidol	The serum concentration of Haloperidol can be increased when it is combined with Dihydro-alpha-ergocryptine.
Tucatinib	The metabolism of Tucatinib can be decreased when combined with Dihydro-alpha-ergocryptine.
Abametapir	The serum concentration of Dihydro-alpha-ergocryptine can be increased when it is combined with Abametapir.
Satralizumab	The serum concentration of Dihydro-alpha-ergocryptine can be decreased when it is combined with Satralizumab.
Sotorasib	The serum concentration of Dihydro-alpha-ergocryptine can be decreased when it is combined with Sotorasib.
Cyclosporine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Cyclosporine.
Fluvoxamine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Fluvoxamine.
Fluconazole	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Fluconazole.
Erythromycin	The serum concentration of Dihydro-alpha-ergocryptine can be increased when it is combined with Erythromycin.
Ziprasidone	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Ziprasidone.
Isradipine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Isradipine.
Diltiazem	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Diltiazem.
Clozapine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Clozapine.
Ciprofloxacin	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Ciprofloxacin.
Nicardipine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Nicardipine.
Verapamil	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Verapamil.
Aprepitant	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Aprepitant.
Isoniazid	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Isoniazid.
Primaquine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Primaquine.
Miconazole	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Miconazole.
Fusidic acid	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Fusidic acid.
Zimelidine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Zimelidine.
Dronedarone	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Dronedarone.
Milnacipran	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Milnacipran.
Simeprevir	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Simeprevir.
Isavuconazonium	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Isavuconazonium.
Desvenlafaxine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Desvenlafaxine.
Nilvadipine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Nilvadipine.
Seproxetine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Seproxetine.
Linagliptin	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Linagliptin.
Indalpine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Indalpine.
Netupitant	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Netupitant.
Barnidipine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Barnidipine.
Benidipine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Benidipine.
Venetoclax	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Venetoclax.
Isavuconazole	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Isavuconazole.
Fosnetupitant	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Fosnetupitant.
Berotralstat	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Berotralstat.
Midostaurin	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Midostaurin.
Voriconazole	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Voriconazole.
Danazol	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Danazol.
Nelfinavir	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Nelfinavir.
Indinavir	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Indinavir.
Terfenadine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Terfenadine.
Efavirenz	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Efavirenz.
Ergotamine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Ergotamine.
Amprenavir	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Amprenavir.
Delavirdine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Delavirdine.
Methimazole	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Methimazole.
Conivaptan	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Conivaptan.
Tipranavir	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Tipranavir.
Telithromycin	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Telithromycin.
Ketoconazole	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Ketoconazole.
Atazanavir	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Atazanavir.
Amiodarone	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Amiodarone.
Nefazodone	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Nefazodone.
Itraconazole	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Itraconazole.
Clarithromycin	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Clarithromycin.
Saquinavir	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Saquinavir.
Posaconazole	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Posaconazole.
Darunavir	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Darunavir.
Lopinavir	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Lopinavir.
Ditiocarb	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Ditiocarb.
Nilotinib	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Nilotinib.
Telaprevir	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Telaprevir.
Lonafarnib	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Lonafarnib.
Boceprevir	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Boceprevir.
Elvitegravir	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Elvitegravir.
Stiripentol	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Stiripentol.
Ribociclib	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Ribociclib.
Danoprevir	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Danoprevir.
Troleandomycin	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Troleandomycin.
Phenytoin	The metabolism of Dihydro-alpha-ergocryptine can be increased when combined with Phenytoin.
Pentobarbital	The metabolism of Dihydro-alpha-ergocryptine can be increased when combined with Pentobarbital.
Carbamazepine	The metabolism of Dihydro-alpha-ergocryptine can be increased when combined with Carbamazepine.
Mitotane	The metabolism of Dihydro-alpha-ergocryptine can be increased when combined with Mitotane.
Primidone	The metabolism of Dihydro-alpha-ergocryptine can be increased when combined with Primidone.
Rifampin	The metabolism of Dihydro-alpha-ergocryptine can be increased when combined with Rifampicin.
Phenobarbital	The metabolism of Dihydro-alpha-ergocryptine can be increased when combined with Phenobarbital.
Dexamethasone	The metabolism of Dihydro-alpha-ergocryptine can be increased when combined with Dexamethasone.
Fosphenytoin	The metabolism of Dihydro-alpha-ergocryptine can be increased when combined with Fosphenytoin.
St. John's Wort	The metabolism of Dihydro-alpha-ergocryptine can be increased when combined with St. John's Wort.
Enzalutamide	The serum concentration of Dihydro-alpha-ergocryptine can be decreased when it is combined with Enzalutamide.
Lumacaftor	The metabolism of Dihydro-alpha-ergocryptine can be increased when combined with Lumacaftor.
Apalutamide	The serum concentration of Dihydro-alpha-ergocryptine can be decreased when it is combined with Apalutamide.
Rifapentine	The metabolism of Dihydro-alpha-ergocryptine can be increased when combined with Rifapentine.
Curcumin	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Curcumin.
Somatrogon	The metabolism of Dihydro-alpha-ergocryptine can be increased when combined with Somatrogon.
Levoketoconazole	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Levoketoconazole.
Mavacamten	The serum concentration of Dihydro-alpha-ergocryptine can be decreased when it is combined with Mavacamten.
Viloxazine	The metabolism of Dihydro-alpha-ergocryptine can be decreased when combined with Viloxazine.
Ivosidenib	The metabolism of Dihydro-alpha-ergocryptine can be increased when combined with Ivosidenib.
Dabrafenib	The serum concentration of Dihydro-alpha-ergocryptine can be decreased when it is combined with Dabrafenib.
Telotristat ethyl	The serum concentration of Dihydro-alpha-ergocryptine can be decreased when it is combined with Telotristat ethyl.
Avanafil	The serum concentration of Avanafil can be increased when it is combined with Dihydro-alpha-ergocryptine.
Omaveloxolone	The serum concentration of Dihydro-alpha-ergocryptine can be decreased when it is combined with Omaveloxolone.

Target Protein

5-hydroxytryptamine receptor 7 HTR7

5-hydroxytryptamine receptor 2B HTR2B

D(2) dopamine receptor DRD2

D(1) dopamine receptor DRD1

D(3) dopamine receptor DRD3

Referensi & Sumber

Artikel (PubMed)

PMID: 6805543
Elliott JM, Grahame-Smith DG: The binding characteristics of 3H-dihydroergocryptine on intact human platelets. Br J Pharmacol. 1982 May;76(1):121-30.
PMID: 9925236
Battistin L, Bardin PG, Ferro-Milone F, Ravenna C, Toso V, Reboldi G: Alpha-dihydroergocryptine in Parkinson's disease: a multicentre randomized double blind parallel group study. Acta Neurol Scand. 1999 Jan;99(1):36-42.
PMID: 11332869
Micieli G, Cavallini A, Marcheselli S, Mailland F, Ambrosoli L, Nappi G: Alpha-dihydroergocryptine and predictive factors in migraine prophylaxis. Int J Clin Pharmacol Ther. 2001 Apr;39(4):144-51.
PMID: 14523624
Gerlach M, Double K, Arzberger T, Leblhuber F, Tatschner T, Riederer P: Dopamine receptor agonists in current clinical use: comparative dopamine receptor binding profiles defined in the human striatum. J Neural Transm (Vienna). 2003 Oct;110(10):1119-27. doi: 10.1007/s00702-003-0027-5.
PMID: 19709931
Antonini A, Tolosa E, Mizuno Y, Yamamoto M, Poewe WH: A reassessment of risks and benefits of dopamine agonists in Parkinson's disease. Lancet Neurol. 2009 Oct;8(10):929-37. doi: 10.1016/S1474-4422(09)70225-X. Epub 2009 Aug 24.
PMID: 12713527
Albanese A, Colosimo C: Dihydroergocriptine in Parkinson's disease: clinical efficacy and comparison with other dopamine agonists. Acta Neurol Scand. 2003 May;107(5):349-55.
PMID: 16618013
de Mey C, Stamenova P, Daskalov M, Orozova M, Staikov I, Vlahov V, Wangemann M: Bioequivalence of a novel high-dose oral formulation of alpha-dihydroergocryptine. Arzneimittelforschung. 2006;56(3):205-11. doi: 10.1055/s-0031-1296712.
PMID: 15553103
Mailland E, Magnani P, Ottillinger B: Alpha-dihydroergocryptine in the long-term therapy of Parkinson's disease. Arzneimittelforschung. 2004;54(10):647-54. doi: 10.1055/s-0031-1297016.

Menampilkan 8 dari 15 artikel.

Textbook

ISBN: 3-7692-3483-9
Steinhilber, D., Schubert M. and Roth H. (2005). Medizinische Chemie. Deutscher Apotheker Verlag.

Link

DIMDI Drug Product Information: Almirid-Cripar (dihydro-alpha-ergocryptine) oral tablets

Contoh Produk & Brand

Produk: 6 • International brands: 0

Produk

Ergoloid Mesylates

Tablet • - • Oral • US • Generic • Approved
Ergoloid Mesylates

Tablet • - • Oral • US • Generic • Approved
Ergoloid Mesylates

Tablet • - • Oral • US • Generic • Approved
Ergoloid Mesylates

Tablet • - • Oral • US • Generic • Approved
Ergoloid Mesylates

Tablet • - • Oral • US • Generic • Approved
Ergoloid Mesylates

Tablet, orally disintegrating • - • Oral • US • Generic • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.