Peringatan Keamanan

Most commonly observed adverse effects are nausea, vomiting, headache, dizziness and fatigue that usually appear in the beginning of initial therapy. Less frequent side effects (1 to 10%) include anorexia, abdominal pain, constipation or diarrhoea, insomnia, oedema, flushing, nasal congestion and hypotension. Orthostatic hypotension may result in faintness or syncope FDA Label. Quinagolide demonstrates carcinogenic potential in animal studies but with no known relevance in humans. It is not demonstrated to be embryotoxic or teratogenic, but it is associated with reduced pregnancy rates L870. Oral LD50 values in mouse, rat and rabbit are 300 mg/kg, 980 mg/kg and 3200 mg/kg, respectively MSDS.

Quinagolide

DB09097

small molecule approved investigational

Deskripsi

Quinagolide is a non-ergot-derived selective dopamine D2 receptor agonist used for the treatment of elevated levels of prolactin or hyperprolactinaemia. Hyperprolalctinaemia is associated with gonadal dysfunction, including infertility and reduced libido, as well as long-term complications such as osteoporosis A19684. Newer dopamine receptor agonists such as quinagolide and DB00248 are shown to effectively inhibit prolactin secretion with improved efficacy over DB01200. These drugs are effective in patients who are intolerant or resistant to DB01200. Quinagolide exists as a racemate and its relevant clinical activity is mediated predominantly by the (-) enantiomer. It is typically present in the hydrochloride salt form and is marketed as oral tablets under the brand name Norprolac contained as a racemate. Quinagolide is currently available in several countries including Canada, but not approved for treatment in the United States.

Struktur Molekul 2D

Berat 395.56
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal half-life for parent drug is 11.5 hours following single dose and 17 hours at steady state.
Volume Distribusi Approximate volume of distribution is 100L following a single oral admininstration. The parent drug and metabolites is predicted to be extensively distributed in the extravascular compartment with primary target organs being the liver, kidneys, salivary glands and pituitary [FDA Label].
Klirens (Clearance) -

Absorpsi

The absorption of quinagolide is rapid and extensive with 95% of the dose absorbed after oral ingestion, however the absolute bioavailability is low (4 %) due to pre-systemic metabolism. The time to reach peak plasma concentration is 30-60 minutes. Prolactin-lowering effect of quinagolide at recommended therapeutic doses occurs within 2 hours after ingestion reaches a maximum within 4 to 6 hours and is maintained for at least 24 hours L871.

Metabolisme

Quinagolide undergoes extensive first pass metabolism with sulfate and glucuronide conjugates being the major circulating metabolites. N-desethyl analogue is a biologically active metabolite while sulfate or glucuronide conjugates and N,N-didesethyl analogue are inactive metabolites.

Rute Eliminasi

More than 95% of total dose is excreted as metabolites and the excretion via urine and feces is approximately equal. Renal elimination accounts for 50% of total elimination, where sulfate or glucuronide conjugates, N-desethyl and N,N-didesethyl analogues can be detected in the urine. Unconjugated forms of sulfate or glucuronide conjugates, N-desethyl and N,N-didesethyl analogues are excreted into feces, and fecal elimination accounts for 40% of the total elimination of the drug.

Interaksi Makanan

2 Data
  • 1. Avoid excessive or chronic alcohol consumption. Alcohol may increase the risk of dizziness, thereby reducing the tolerability of quinagolide.
  • 2. Take with a light meal or snack. Food reduces gastric irritation.

Interaksi Obat

125 Data
Reserpine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Reserpine.
Olanzapine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Olanzapine.
Clozapine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Clozapine.
Thiethylperazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Thiethylperazine.
Sulpiride The therapeutic efficacy of Quinagolide can be decreased when used in combination with Sulpiride.
Loxapine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Loxapine.
Remoxipride The therapeutic efficacy of Quinagolide can be decreased when used in combination with Remoxipride.
Promazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Promazine.
Prochlorperazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Prochlorperazine.
Droperidol The therapeutic efficacy of Quinagolide can be decreased when used in combination with Droperidol.
Chlorpromazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Chlorpromazine.
Triflupromazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Triflupromazine.
Amoxapine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Amoxapine.
Fluphenazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Fluphenazine.
Thioridazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Thioridazine.
Moricizine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Moricizine.
Risperidone The therapeutic efficacy of Quinagolide can be decreased when used in combination with Risperidone.
Trifluoperazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Trifluoperazine.
Perphenazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Perphenazine.
Flupentixol The therapeutic efficacy of Quinagolide can be decreased when used in combination with Flupentixol.
Mesoridazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Mesoridazine.
Acetophenazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Acetophenazine.
Promethazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Promethazine.
Pimozide The therapeutic efficacy of Quinagolide can be decreased when used in combination with Pimozide.
Quetiapine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Quetiapine.
Chlorprothixene The therapeutic efficacy of Quinagolide can be decreased when used in combination with Chlorprothixene.
Alimemazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Alimemazine.
Paliperidone The therapeutic efficacy of Quinagolide can be decreased when used in combination with Paliperidone.
Lithium cation The therapeutic efficacy of Quinagolide can be decreased when used in combination with Lithium cation.
Methotrimeprazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Methotrimeprazine.
Periciazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Periciazine.
Acepromazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Acepromazine.
Aceprometazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Aceprometazine.
Molindone The therapeutic efficacy of Quinagolide can be decreased when used in combination with Molindone.
Pipotiazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Pipotiazine.
Thioproperazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Thioproperazine.
Thiothixene The therapeutic efficacy of Quinagolide can be decreased when used in combination with Thiothixene.
Zuclopenthixol The therapeutic efficacy of Quinagolide can be decreased when used in combination with Zuclopenthixol.
Fluspirilene The therapeutic efficacy of Quinagolide can be decreased when used in combination with Fluspirilene.
Osanetant The therapeutic efficacy of Quinagolide can be decreased when used in combination with Osanetant.
Bifeprunox The therapeutic efficacy of Quinagolide can be decreased when used in combination with Bifeprunox.
Iloperidone The therapeutic efficacy of Quinagolide can be decreased when used in combination with Iloperidone.
BL-1020 The therapeutic efficacy of Quinagolide can be decreased when used in combination with BL-1020.
Cariprazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Cariprazine.
Lumateperone The therapeutic efficacy of Quinagolide can be decreased when used in combination with Lumateperone.
Sertindole The therapeutic efficacy of Quinagolide can be decreased when used in combination with Sertindole.
Asenapine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Asenapine.
Amisulpride The therapeutic efficacy of Quinagolide can be decreased when used in combination with Amisulpride.
Lurasidone The therapeutic efficacy of Quinagolide can be decreased when used in combination with Lurasidone.
Perospirone The therapeutic efficacy of Quinagolide can be decreased when used in combination with Perospirone.
Amperozide The therapeutic efficacy of Quinagolide can be decreased when used in combination with Amperozide.
Cyamemazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Cyamemazine.
Blonanserin The therapeutic efficacy of Quinagolide can be decreased when used in combination with Blonanserin.
Melperone The therapeutic efficacy of Quinagolide can be decreased when used in combination with Melperone.
Zotepine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Zotepine.
Brilaroxazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Brilaroxazine.
Methylene blue The therapeutic efficacy of Quinagolide can be decreased when used in combination with Methylene blue.
Pipamperone The therapeutic efficacy of Quinagolide can be decreased when used in combination with Pipamperone.
Azaperone The therapeutic efficacy of Quinagolide can be decreased when used in combination with Azaperone.
Propiopromazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Propiopromazine.
Tetrahydropalmatine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Tetrahydropalmatine.
Ecopipam The therapeutic efficacy of Quinagolide can be decreased when used in combination with Ecopipam.
Bromperidol The therapeutic efficacy of Quinagolide can be decreased when used in combination with Bromperidol.
Raclopride The therapeutic efficacy of Quinagolide can be decreased when used in combination with Raclopride.
Ritanserin The therapeutic efficacy of Quinagolide can be decreased when used in combination with Ritanserin.
Perazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Perazine.
Benperidol The therapeutic efficacy of Quinagolide can be decreased when used in combination with Benperidol.
Prothipendyl The therapeutic efficacy of Quinagolide can be decreased when used in combination with Prothipendyl.
Tiapride The therapeutic efficacy of Quinagolide can be decreased when used in combination with Tiapride.
Butaperazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Butaperazine.
Clothiapine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Clothiapine.
Sultopride The therapeutic efficacy of Quinagolide can be decreased when used in combination with Sultopride.
Chlorproethazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Chlorproethazine.
Oxypertine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Oxypertine.
Thiazinam The therapeutic efficacy of Quinagolide can be decreased when used in combination with Thiazinam.
Veralipride The therapeutic efficacy of Quinagolide can be decreased when used in combination with Veralipride.
Trifluperidol The therapeutic efficacy of Quinagolide can be decreased when used in combination with Trifluperidol.
Moperone The therapeutic efficacy of Quinagolide can be decreased when used in combination with Moperone.
Thiopropazate The therapeutic efficacy of Quinagolide can be decreased when used in combination with Thiopropazate.
Fluanisone The therapeutic efficacy of Quinagolide can be decreased when used in combination with Fluanisone.
Mosapramine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Mosapramine.
Dixyrazine The therapeutic efficacy of Quinagolide can be decreased when used in combination with Dixyrazine.
Penfluridol The therapeutic efficacy of Quinagolide can be decreased when used in combination with Penfluridol.
Clopenthixol The therapeutic efficacy of Quinagolide can be decreased when used in combination with Clopenthixol.
Aripiprazole lauroxil The therapeutic efficacy of Quinagolide can be decreased when used in combination with Aripiprazole lauroxil.
Perphenazine enanthate The therapeutic efficacy of Quinagolide can be decreased when used in combination with Perphenazine enanthate.
Aripiprazole The therapeutic efficacy of Quinagolide can be decreased when used in combination with Aripiprazole.
Brexpiprazole The therapeutic efficacy of Quinagolide can be decreased when used in combination with Brexpiprazole.
Levosulpiride The therapeutic efficacy of Quinagolide can be decreased when used in combination with Levosulpiride.
Cabergoline The risk or severity of adverse effects can be decreased when Cabergoline is combined with Quinagolide.
Ropinirole The risk or severity of adverse effects can be decreased when Ropinirole is combined with Quinagolide.
Dihydroergotamine The risk or severity of adverse effects can be decreased when Dihydroergotamine is combined with Quinagolide.
Pramipexole The risk or severity of adverse effects can be decreased when Pramipexole is combined with Quinagolide.
Lisuride The risk or severity of adverse effects can be decreased when Lisuride is combined with Quinagolide.
Apomorphine The risk or severity of adverse effects can be decreased when Apomorphine is combined with Quinagolide.
Fenoldopam The risk or severity of adverse effects can be decreased when Fenoldopam is combined with Quinagolide.
Ergoloid mesylate The risk or severity of adverse effects can be decreased when Ergoloid mesylate is combined with Quinagolide.
Pergolide The risk or severity of adverse effects can be decreased when Pergolide is combined with Quinagolide.
Bromocriptine The risk or severity of adverse effects can be decreased when Bromocriptine is combined with Quinagolide.
Rotigotine The risk or severity of adverse effects can be decreased when Rotigotine is combined with Quinagolide.

Target Protein

D(2) dopamine receptor DRD2
D(1) dopamine receptor DRD1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 16452531
    Barlier A, Jaquet P: Quinagolide--a valuable treatment option for hyperprolactinaemia. Eur J Endocrinol. 2006 Feb;154(2):187-95.
  • PMID: 10931080
    Di Sarno A, Landi ML, Marzullo P, Di Somma C, Pivonello R, Cerbone G, Lombardi G, Colao A: The effect of quinagolide and cabergoline, two selective dopamine receptor type 2 agonists, in the treatment of prolactinomas. Clin Endocrinol (Oxf). 2000 Jul;53(1):53-60.
  • PMID: 11788012
    Schultz PN, Ginsberg L, McCutcheon IE, Samaan N, Leavens M, Gagel RF: Quinagolide in the management of prolactinoma. Pituitary. 2000 Dec;3(4):239-49.
  • PMID: 20139430
    Busso C, Fernandez-Sanchez M, Garcia-Velasco JA, Landeras J, Ballesteros A, Munoz E, Gonzalez S, Simon C, Arce JC, Pellicer A: The non-ergot derived dopamine agonist quinagolide in prevention of early ovarian hyperstimulation syndrome in IVF patients: a randomized, double-blind, placebo-controlled trial. Hum Reprod. 2010 Apr;25(4):995-1004. doi: 10.1093/humrep/deq005. Epub 2010 Feb 6.
Textbook
  • ISBN: 978-0-7020-3471-8
    32. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 397-398). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 4 • International brands: 0
Produk
  • Norprolac
    Tablet • 0.025 mg • Oral • Canada • Approved
  • Norprolac
    Tablet • 0.05 mg • Oral • Canada • Approved
  • Norprolac
    Tablet • 0.075 mg • Oral • Canada • Approved
  • Norprolac
    Tablet • 0.15 mg • Oral • Canada • Approved

Sekuens Gen/Protein (FASTA)

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