Peringatan Keamanan

Overdosage might be expected to produce nasal congestion, syncope, or hallucinations.

Cabergoline

DB00248

small molecule approved

Deskripsi

Cabergoline, an ergot derivative, is a long-acting dopamine agonist and prolactin inhibitor. It is used to treat hyperprolactinemic disorders and Parkinsonian Syndrome. Cabergoline possesses potent agonist activity on dopamine D2 receptors.

Struktur Molekul 2D

Berat 451.6043
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life is estimated from urinary data of 12 healthy subjects to range between 63 to 69 hours.
Volume Distribusi -
Klirens (Clearance) * renal cl=0,008 L/min * nonrenal cl=3.2 L/min

Absorpsi

First-pass effect is seen, however the absolute bioavailability is unknown.

Metabolisme

Hepatic. Cabergoline is extensively metabolized, predominately via hydrolysis of the acylurea bond of the urea moiety. Cytochrome P-450 mediated metabolism appears to be minimal. The main metabolite identified in urine is 6-allyl-8b-carboxy-ergoline (4-6% of dose). Three other metabolites were identified urine (less than 3% of dose).

Rute Eliminasi

After oral dosing of radioactive cabergoline to five healthy volunteers, approximately 22% and 60% of the dose was excreted within 20 days in the urine and feces, respectively. Less than 4% of the dose was excreted unchanged in the urine.

Interaksi Makanan

3 Data
  • 1. Exercise caution with grapefruit products. Cabergoline is partially metabolized through the CYP3A4 pathway. Therefore coadministration with grapefruit, a CYP3A4 inhibitor, may increase its serum concentration.
  • 2. Exercise caution with St. John's Wort. Cabergoline is partially metabolized through the CYP3A4 pathway. Therefore coadministration with St. John's Wort, a CYP3A4 inducer, may reduce its serum concentration.
  • 3. Take with or without food. Taking cabergoline with food may reduce gastric irritation.

Interaksi Obat

1593 Data
Modafinil The metabolism of Cabergoline can be increased when combined with Modafinil.
Armodafinil The metabolism of Cabergoline can be increased when combined with Armodafinil.
Valsartan Cabergoline may decrease the antihypertensive activities of Valsartan.
Ramipril Cabergoline may decrease the antihypertensive activities of Ramipril.
Remikiren Cabergoline may decrease the antihypertensive activities of Remikiren.
Torasemide Cabergoline may decrease the antihypertensive activities of Torasemide.
Guanadrel Cabergoline may decrease the antihypertensive activities of Guanadrel.
Olmesartan Cabergoline may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Cabergoline may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Cabergoline may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Cabergoline may decrease the antihypertensive activities of Minoxidil.
Treprostinil Cabergoline may decrease the antihypertensive activities of Treprostinil.
Bendroflumethiazide Cabergoline may decrease the antihypertensive activities of Bendroflumethiazide.
Fosinopril Cabergoline may decrease the antihypertensive activities of Fosinopril.
Trandolapril Cabergoline may decrease the antihypertensive activities of Trandolapril.
Metolazone Cabergoline may decrease the antihypertensive activities of Metolazone.
Benazepril Cabergoline may decrease the antihypertensive activities of Benazepril.
Cyclothiazide Cabergoline may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Cabergoline may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Cabergoline may decrease the antihypertensive activities of Mecamylamine.
Moexipril Cabergoline may decrease the antihypertensive activities of Moexipril.
Lisinopril Cabergoline may decrease the antihypertensive activities of Lisinopril.
Hydroflumethiazide Cabergoline may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Cabergoline may decrease the antihypertensive activities of Cryptenamine.
Perindopril Cabergoline may decrease the antihypertensive activities of Perindopril.
Eprosartan Cabergoline may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Cabergoline may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Cabergoline may decrease the antihypertensive activities of Quinapril.
Hydrochlorothiazide Cabergoline may decrease the antihypertensive activities of Hydrochlorothiazide.
Trichlormethiazide Cabergoline may decrease the antihypertensive activities of Trichlormethiazide.
Deserpidine Cabergoline may decrease the antihypertensive activities of Deserpidine.
Pentolinium Cabergoline may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Cabergoline may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Cabergoline may decrease the antihypertensive activities of Diazoxide.
Bretylium Cabergoline may decrease the antihypertensive activities of Bretylium.
Epoprostenol Cabergoline may decrease the antihypertensive activities of Epoprostenol.
Polythiazide Cabergoline may decrease the antihypertensive activities of Polythiazide.
Saprisartan Cabergoline may decrease the antihypertensive activities of Saprisartan.
Spirapril Cabergoline may decrease the antihypertensive activities of Spirapril.
Tienilic acid Cabergoline may decrease the antihypertensive activities of Tienilic acid.
Diethylnorspermine Cabergoline may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Cabergoline may decrease the antihypertensive activities of Temocapril.
Trimazosin Cabergoline may decrease the antihypertensive activities of Trimazosin.
Nicorandil Cabergoline may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Cabergoline may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Cabergoline may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Cabergoline may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Cabergoline may decrease the antihypertensive activities of Imidapril.
BQ-123 Cabergoline may decrease the antihypertensive activities of BQ-123.
Cicletanine Cabergoline may decrease the antihypertensive activities of Cicletanine.
Dihydralazine Cabergoline may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Cabergoline may decrease the antihypertensive activities of Zofenopril.
Guanoxan Cabergoline may decrease the antihypertensive activities of Guanoxan.
Delapril Cabergoline may decrease the antihypertensive activities of Delapril.
Vincamine Cabergoline may decrease the antihypertensive activities of Vincamine.
Linsidomine Cabergoline may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Cabergoline may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Cabergoline may decrease the antihypertensive activities of Tolonidine.
Endralazine Cabergoline may decrease the antihypertensive activities of Endralazine.
Cadralazine Cabergoline may decrease the antihypertensive activities of Cadralazine.
Cyclopenthiazide Cabergoline may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Cabergoline may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Cabergoline may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Cabergoline may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Cabergoline may decrease the antihypertensive activities of Guanoclor.
Muzolimine Cabergoline may decrease the antihypertensive activities of Muzolimine.
Xipamide Cabergoline may decrease the antihypertensive activities of Xipamide.
Tocopherylquinone Cabergoline may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Cabergoline may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Cabergoline may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Cabergoline may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Cabergoline may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Cabergoline may decrease the antihypertensive activities of Quinaprilat.
Furosemide Cabergoline may decrease the antihypertensive activities of Furosemide.
Lercanidipine Cabergoline may decrease the antihypertensive activities of Lercanidipine.
Indapamide Cabergoline may decrease the antihypertensive activities of Indapamide.
Guanethidine Cabergoline may decrease the antihypertensive activities of Guanethidine.
Pinacidil Cabergoline may decrease the antihypertensive activities of Pinacidil.
Riociguat The serum concentration of Cabergoline can be increased when it is combined with Riociguat.
Macitentan Cabergoline may decrease the antihypertensive activities of Macitentan.
Aliskiren Cabergoline may decrease the antihypertensive activities of Aliskiren.
Lacidipine Cabergoline may decrease the antihypertensive activities of Lacidipine.
Naftopidil Cabergoline may decrease the antihypertensive activities of Naftopidil.
Amlodipine The metabolism of Cabergoline can be decreased when combined with Amlodipine.
Nimodipine Cabergoline may decrease the antihypertensive activities of Nimodipine.
Prazosin Cabergoline may decrease the antihypertensive activities of Prazosin.
Enalapril Cabergoline may decrease the antihypertensive activities of Enalapril.
Candesartan cilexetil Cabergoline may decrease the antihypertensive activities of Candesartan cilexetil.
Tadalafil Cabergoline may decrease the antihypertensive activities of Tadalafil.
Telmisartan Cabergoline may decrease the antihypertensive activities of Telmisartan.
Nitrendipine Cabergoline may decrease the antihypertensive activities of Nitrendipine.
Terazosin Cabergoline may decrease the antihypertensive activities of Terazosin.
Captopril Cabergoline may decrease the antihypertensive activities of Captopril.
Bepridil Cabergoline may decrease the antihypertensive activities of Bepridil.
Cilazapril Cabergoline may decrease the antihypertensive activities of Cilazapril.
Debrisoquine Cabergoline may decrease the antihypertensive activities of Debrisoquine.
Candesartan Cabergoline may decrease the antihypertensive activities of Candesartan.
Nisoldipine Cabergoline may decrease the antihypertensive activities of Nisoldipine.
Eplerenone Cabergoline may decrease the antihypertensive activities of Eplerenone.
Buthiazide Cabergoline may decrease the antihypertensive activities of Buthiazide.

Target Protein

D(2) dopamine receptor DRD2
5-hydroxytryptamine receptor 2B HTR2B
D(3) dopamine receptor DRD3
5-hydroxytryptamine receptor 2A HTR2A
Alpha-2B adrenergic receptor ADRA2B
5-hydroxytryptamine receptor 1D HTR1D
D(4) dopamine receptor DRD4
Alpha-2A adrenergic receptor ADRA2A
5-hydroxytryptamine receptor 1A HTR1A
Alpha-2C adrenergic receptor ADRA2C
D(1B) dopamine receptor DRD5
D(1A) dopamine receptor DRD1
5-hydroxytryptamine receptor 1B HTR1B
5-hydroxytryptamine receptor 2C HTR2C
5-hydroxytryptamine receptor 7 HTR7
Alpha-1A adrenergic receptor ADRA1A
Alpha-1B adrenergic receptor ADRA1B
Alpha-1D adrenergic receptor ADRA1D
Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2
D(1) dopamine receptor DRD1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 12721865
    Pastor P, Tolosa E: Cabergoline in the treatment of Parkinson's disease. Neurologia. 2003 May;18(4):202-9.
  • PMID: 15341508
    Curran MP, Perry CM: Cabergoline : a review of its use in the treatment of Parkinson's disease. Drugs. 2004;64(18):2125-41.
  • PMID: 15330687
    Bracco F, Battaglia A, Chouza C, Dupont E, Gershanik O, Marti Masso JF, Montastruc JL: The long-acting dopamine receptor agonist cabergoline in early Parkinson's disease: final results of a 5-year, double-blind, levodopa-controlled study. CNS Drugs. 2004;18(11):733-46.
  • PMID: 8951172
    Miyagi M, Arai N, Taya F, Itoh F, Komatsu Y, Kojima M, Isaji M: Effect of cabergoline, a long-acting dopamine D2 agonist, on reserpine-treated rodents. Biol Pharm Bull. 1996 Nov;19(11):1499-502.

Contoh Produk & Brand

Produk: 27 • International brands: 1
Produk
  • Act Cabergoline
    Tablet • 0.5 mg • Oral • Canada • Approved
  • Apo-cabergoline
    Tablet • 0.5 mg • Oral • Canada • Generic • Approved
  • Cabergoline
    Tablet • 0.5 mg/1 • Oral • US • Generic • Approved
  • Cabergoline
    Tablet • 0.5 mg/1 • Oral • US • Generic • Approved
  • Cabergoline
    Tablet • 0.5 mg/1 • Oral • US • Approved
  • Cabergoline
    Tablet • 0.5 mg/1 • Oral • US • Generic • Approved
  • Cabergoline
    Tablet • 0.5 mg/1 • Oral • US • Generic • Approved
  • Cabergoline
    Tablet • 0.5 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 27 produk.
International Brands
  • Cabaser — Pfizer

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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