Peringatan Keamanan

Symptoms of overdosage include nausea, vomiting, and severe hypotension. The most common adverse effects include nausea, headache, vertigo, constipation, light-headedness, abdominal cramps, nasal congestion, diarrhea, and hypotension.

Bromocriptine

DB01200

small molecule approved investigational withdrawn

Deskripsi

Bromocriptine mesylate is a semisynthetic ergot alkaloid derivative with potent dopaminergic activity. It inhibits prolactin secretion and may be used to treat dysfunctions associated with hyperprolactinemia. Bromocriptine is also indicated for the management of signs and symptoms of Parkinsonian Syndrome, as well as the treatment of acromegaly. Bromocriptine has been associated with pulmonary fibrosis, and can also cause sustained suppression of somatotropin (growth hormone) secretion in some patients with acromegaly.

In 1995, the FDA withdrew the approval of bromocriptine mesylate for the prevention of physiological lactation after finding that bromocriptine was not shown to be safe for use.L43942,L43947 It continues to be used for the indications mentioned above.

Struktur Molekul 2D

Berat 654.595
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 2-8 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Approximately 28% of the oral dose is absorbed; however due to a substantial first pass effect, only 6% of the oral dose reaches the systemic circulation unchanged. Bromocriptine and its metabolites appear in the blood as early as 10 minutes following oral administration and peak plasma concentration are reached within 1-1.5 hours. Serum prolactin may be decreased within 2 hours or oral administration with a maximal effect achieved after 8 hours. Growth hormone concentrations in patients with acromegaly is reduced within 1-2 hours with a single oral dose of 2.5 mg and decreased growth hormone concentrations persist for at least 4-5 hours.

Metabolisme

Completely metabolized by the liver, primarily by hydrolysis of the amide bond to produce lysergic acid and a peptide fragment, both inactive and non-toxic. Bromocriptine is metabolized by cytochrome P450 3A4 and excreted primarily in the feces via biliary secretion.

Rute Eliminasi

Parent drug and metabolites are almost completely excreted via the liver, and only 6% eliminated via the kidney.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with food. Food reduces irritation.

Interaksi Obat

1713 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Bromocriptine.
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Bromocriptine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Bromocriptine is combined with Levodopa.
Risperidone Bromocriptine may increase the hypotensive activities of Risperidone.
Cyclosporine The serum concentration of Cyclosporine can be increased when it is combined with Bromocriptine.
Vapreotide The serum concentration of Bromocriptine can be increased when it is combined with Vapreotide.
Pasireotide The serum concentration of Bromocriptine can be increased when it is combined with Pasireotide.
Lanreotide The serum concentration of Bromocriptine can be increased when it is combined with Lanreotide.
Somatostatin The serum concentration of Bromocriptine can be increased when it is combined with Somatostatin.
Valsartan Bromocriptine may decrease the antihypertensive activities of Valsartan.
Ramipril Bromocriptine may decrease the antihypertensive activities of Ramipril.
Remikiren Bromocriptine may decrease the antihypertensive activities of Remikiren.
Guanadrel Bromocriptine may decrease the antihypertensive activities of Guanadrel.
Olmesartan Bromocriptine may decrease the antihypertensive activities of Olmesartan.
Nitroprusside Bromocriptine may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Bromocriptine may decrease the antihypertensive activities of Minoxidil.
Treprostinil Bromocriptine may decrease the antihypertensive activities of Treprostinil.
Fosinopril Bromocriptine may decrease the antihypertensive activities of Fosinopril.
Trandolapril Bromocriptine may decrease the antihypertensive activities of Trandolapril.
Candoxatril Bromocriptine may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Bromocriptine may decrease the antihypertensive activities of Mecamylamine.
Moexipril Bromocriptine may decrease the antihypertensive activities of Moexipril.
Lisinopril Bromocriptine may decrease the antihypertensive activities of Lisinopril.
Cryptenamine Bromocriptine may decrease the antihypertensive activities of Cryptenamine.
Perindopril Bromocriptine may decrease the antihypertensive activities of Perindopril.
Eprosartan Bromocriptine may decrease the antihypertensive activities of Eprosartan.
Quinapril Bromocriptine may decrease the antihypertensive activities of Quinapril.
Omapatrilat Bromocriptine may decrease the antihypertensive activities of Omapatrilat.
Deserpidine Bromocriptine may decrease the antihypertensive activities of Deserpidine.
Pentolinium Bromocriptine may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Bromocriptine may decrease the antihypertensive activities of Trimethaphan.
Bretylium Bromocriptine may decrease the antihypertensive activities of Bretylium.
Rescinnamine Bromocriptine may decrease the antihypertensive activities of Rescinnamine.
Epoprostenol Bromocriptine may decrease the antihypertensive activities of Epoprostenol.
Saprisartan Bromocriptine may decrease the antihypertensive activities of Saprisartan.
Spirapril Bromocriptine may decrease the antihypertensive activities of Spirapril.
Tienilic acid Bromocriptine may decrease the antihypertensive activities of Tienilic acid.
Diethylnorspermine Bromocriptine may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Bromocriptine may decrease the antihypertensive activities of Temocapril.
Rauwolfia serpentina root Bromocriptine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Bromocriptine may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Bromocriptine may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Bromocriptine may decrease the antihypertensive activities of Imidapril.
BQ-123 Bromocriptine may decrease the antihypertensive activities of BQ-123.
Cicletanine Bromocriptine may decrease the antihypertensive activities of Cicletanine.
Dihydralazine Bromocriptine may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Bromocriptine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Bromocriptine may decrease the antihypertensive activities of Guanoxan.
Delapril Bromocriptine may decrease the antihypertensive activities of Delapril.
Vincamine Bromocriptine may decrease the antihypertensive activities of Vincamine.
Linsidomine Bromocriptine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Bromocriptine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Bromocriptine may decrease the antihypertensive activities of Tolonidine.
Endralazine Bromocriptine may decrease the antihypertensive activities of Endralazine.
Cadralazine Bromocriptine may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Bromocriptine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Bromocriptine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Bromocriptine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Bromocriptine may decrease the antihypertensive activities of Guanoclor.
Muzolimine Bromocriptine may decrease the antihypertensive activities of Muzolimine.
Tocopherylquinone Bromocriptine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Bromocriptine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Bromocriptine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Bromocriptine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Bromocriptine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Bromocriptine may decrease the antihypertensive activities of Quinaprilat.
Guanethidine Bromocriptine may decrease the antihypertensive activities of Guanethidine.
Pinacidil Bromocriptine may decrease the antihypertensive activities of Pinacidil.
Riociguat Bromocriptine may decrease the antihypertensive activities of Riociguat.
Macitentan Bromocriptine may decrease the antihypertensive activities of Macitentan.
Aliskiren Bromocriptine may decrease the antihypertensive activities of Aliskiren.
Enalapril Bromocriptine may decrease the antihypertensive activities of Enalapril.
Candesartan cilexetil Bromocriptine may decrease the antihypertensive activities of Candesartan cilexetil.
Telmisartan Bromocriptine may decrease the antihypertensive activities of Telmisartan.
Captopril Bromocriptine may decrease the antihypertensive activities of Captopril.
Cilazapril Bromocriptine may decrease the antihypertensive activities of Cilazapril.
Debrisoquine Bromocriptine may decrease the antihypertensive activities of Debrisoquine.
Ambrisentan Bromocriptine may decrease the antihypertensive activities of Ambrisentan.
Selexipag Bromocriptine may decrease the antihypertensive activities of Selexipag.
Candesartan Bromocriptine may decrease the antihypertensive activities of Candesartan.
Losartan Bromocriptine may decrease the antihypertensive activities of Losartan.
Eplerenone Bromocriptine may decrease the antihypertensive activities of Eplerenone.
Irbesartan Bromocriptine may decrease the antihypertensive activities of Irbesartan.
Hydralazine Bromocriptine may decrease the antihypertensive activities of Hydralazine.
Sitaxentan Bromocriptine may decrease the antihypertensive activities of Sitaxentan.
Buprenorphine Bromocriptine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Bromocriptine.
Dronabinol The serum concentration of Dronabinol can be increased when it is combined with Bromocriptine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Bromocriptine.
Hydrocodone Bromocriptine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Bromocriptine.
Magnesium sulfate The therapeutic efficacy of Bromocriptine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Bromocriptine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Bromocriptine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Bromocriptine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Bromocriptine.
Orphenadrine Bromocriptine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Bromocriptine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Bromocriptine.
Pramipexole Bromocriptine may increase the sedative activities of Pramipexole.

Target Protein

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

Referensi & Sumber

Synthesis reference: Luigi Moro, Achille Fiori, Alberto Natali, "Processes for the preparation of pharmaceutical compositions containing bromocriptine having high stability and related products." U.S. Patent US5066495, issued May, 1988.
Artikel (PubMed)
  • PMID: 12351703
    Banihashemi B, Albert PR: Dopamine-D2S receptor inhibition of calcium influx, adenylyl cyclase, and mitogen-activated protein kinase in pituitary cells: distinct Galpha and Gbetagamma requirements. Mol Endocrinol. 2002 Oct;16(10):2393-404.
  • PMID: 18691132
    Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67.
  • PMID: 10641988
    Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S.
  • PMID: 2443499
    Malgaroli A, Vallar L, Elahi FR, Pozzan T, Spada A, Meldolesi J: Dopamine inhibits cytosolic Ca2+ increases in rat lactotroph cells. Evidence of a dual mechanism of action. J Biol Chem. 1987 Oct 15;262(29):13920-7.
  • PMID: 16410672
    Nishina Y, Takano K, Yasufuku-Takano J, Teramoto A, Fujita T: Mechanism of D(2) agonist-induced inhibition of GH secretion from human GH-secreting adenoma cells. Endocr J. 2005 Dec;52(6):775-9.
  • PMID: 2655242
    Vallar L, Meldolesi J: Mechanisms of signal transduction at the dopamine D2 receptor. Trends Pharmacol Sci. 1989 Feb;10(2):74-7.
  • PMID: 2839476
    Vallar L, Vicentini LM, Meldolesi J: Inhibition of inositol phosphate production is a late, Ca2+-dependent effect of D2 dopaminergic receptor activation in rat lactotroph cells. J Biol Chem. 1988 Jul 25;263(21):10127-34.

Contoh Produk & Brand

Produk: 43 • International brands: 5
Produk
  • Bromocriptine
    Tablet • 2.5 mg • Oral • Canada • Approved
  • Bromocriptine
    Capsule • 5 mg • Oral • Canada • Approved
  • Bromocriptine
    Tablet • 2.5 mg • Oral • Canada • Approved
  • Bromocriptine
    Capsule • 5 mg • Oral • Canada • Approved
  • Bromocriptine Mesylate
    Tablet • 2.5 mg/1 • Oral • US • Approved
  • Bromocriptine Mesylate
    Tablet • 2.5 mg/1 • Oral • US • Generic • Approved
  • Bromocriptine Mesylate
    Capsule • 5 mg/1 • Oral • US • Generic • Approved
  • Bromocriptine Mesylate
    Capsule • 5 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 43 produk.
International Brands
  • Apo-Bromocriptine — Apotex
  • Bagren — Serono (Brazil)
  • Ergoset
  • Parlodel Snaptabs — Novartis
  • Pravidel — Meda (Germany, Sweden), Novartis (Canada, discontinued)

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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