Peringatan Keamanan

Overdosage may lead to cardiovascular side effects like cardiac arrhythmias, psychiatric disturbances like confusion and insomnia, gastrointestinal effects like nausea and vomiting, and abnormal involuntary movements F2, L2553.

Various LD50 values have been established for the rat model, including an oral LD50 of 5300 mg/kg in rats MSDS.

Benserazide

DB12783

small molecule approved investigational

Deskripsi

When levodopa is used by itself as a therapy for treating Parkinson's disease, its ubiquitous metabolism into dopamine is responsible for a resultant increase in the levels of circulating dopamine in the blood and to various extracerebral tissues. This can result in a number of side effects like nausea, vomiting, or even cardiac arrhythmias that may diminish patient adherence F2, L2553. A decarboxylase inhibitor like benserazide is consequently an effective compound to combine with levadopa as it is incapable of crossing the blood-brain barrier itself but acts to prevent the formation of dopamine from levadopa in extracerebral tissues - thereby acting to minimize the occurrence of extracerebral side effects F2, L2553.

Levodopa/benserazide combination products are used commonly worldwide for the management of Parkinson's disease. In particular, although the specific levodopa/benserazide combination is formally approved for use in Canada and much of Europe, the FDA has approved another similar levodopa/dopa decarboxylase inhibitor combination in the form of levodopa and carbidopa.

Moreover, the European Medcines Agency has conferred an orphan designation upon benseraside since 2015 for its potential to be used as a therapy for beta thalassaemia as well F3.

Struktur Molekul 2D

Berat 257.246
Wujud -

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of benserazide is documented as 1.5 hours [T181].
Volume Distribusi Readily accessible data regarding the volume of distribution of benserazide is not available [T181].
Klirens (Clearance) Readily accessible data regarding the clearance of benserazide is not available.

Absorpsi

In a study, three patients were administered 50 mg of radiolabelled 14C-benserazide by both intravenous and oral routes F2, L2553. Three additional patients received oral doses of 50 mg 14C-benserazide alone F2, L2553. Comparison of the time-plasma concentration curves of total radioactivity in the patients receiving oral and intravenous 14C-benserazide indicated that between 66% and 74% of the administered dose was absorbed from the gastrointestinal tract F2, L2553. Peak plasma concentrations of radioactivity were detected one hour after oral administration in five of the six patients F2, L2553.

Metabolisme

Benserazide is hydrolyzed to trihydroxybenzylhydrazine in the intestinal mucosa and the liver.F2, L2553 Trihydroxybenzylhydrazine is a potent inhibitor of the aromatic acid decarboxylase,F2, L2553 and it is believed that the levodopa in a levodopa/benserazide combination product is largely protected against decarboxylation mainly by way of this benserazide metabolite.T181

Rute Eliminasi

Benserazide is rapidly excreted in the urine in the form of metabolites, mostly within the first 6 hours of administration, 85% of urinary excretion occurs within 12 hours T181. Elimination of radiolabelled 14C-benserazide was primarily by urinary excretion with 86% to 90% of an intravenous dose recovered in the urine while 53% to 64% of an oral dose was detected in the urine F2, L2553. The majority of the 14C-benserazide was ultimately accounted for in the urine within 48 hours after administration F2, L2553. Fecal recovery studies conducted over five to eight days accounted for the majority (about 30%) of the remainder of the administered 14C-benserazide F2, L2553. Ultimately, benserazide is almost entirely eliminated by metabolism F2, L2553. These metabolites are mainly excreted in the urine (64%) and to a smaller extent in the feces (24%) F2, L2553.

Interaksi Makanan

1 Data
  • 1. Take with or without food. Benserazide is normally given in combination with levodopa as the combination product Prolopa. Levodopa should not be given with protein-rich foods as they may reduce its absorption.

Interaksi Obat

766 Data
Methylphenidate The risk or severity of adverse effects can be increased when Methylphenidate is combined with Benserazide.
Dexmethylphenidate The risk or severity of adverse effects can be increased when Dexmethylphenidate is combined with Benserazide.
Metoclopramide The therapeutic efficacy of Benserazide can be decreased when used in combination with Metoclopramide.
Ziprasidone The therapeutic efficacy of Benserazide can be decreased when used in combination with Ziprasidone.
Olanzapine The therapeutic efficacy of Benserazide can be decreased when used in combination with Olanzapine.
Clozapine The therapeutic efficacy of Benserazide can be decreased when used in combination with Clozapine.
Risperidone The therapeutic efficacy of Benserazide can be decreased when used in combination with Risperidone.
Quetiapine The therapeutic efficacy of Benserazide can be decreased when used in combination with Quetiapine.
Aripiprazole The therapeutic efficacy of Benserazide can be decreased when used in combination with Aripiprazole.
Paliperidone The therapeutic efficacy of Benserazide can be decreased when used in combination with Paliperidone.
Bifeprunox The therapeutic efficacy of Benserazide can be decreased when used in combination with Bifeprunox.
Iloperidone The therapeutic efficacy of Benserazide can be decreased when used in combination with Iloperidone.
Cariprazine The therapeutic efficacy of Benserazide can be decreased when used in combination with Cariprazine.
Lumateperone The therapeutic efficacy of Benserazide can be decreased when used in combination with Lumateperone.
Sertindole The therapeutic efficacy of Benserazide can be decreased when used in combination with Sertindole.
Asenapine The therapeutic efficacy of Benserazide can be decreased when used in combination with Asenapine.
Lurasidone The therapeutic efficacy of Benserazide can be decreased when used in combination with Lurasidone.
Perospirone The therapeutic efficacy of Benserazide can be decreased when used in combination with Perospirone.
Brexpiprazole The therapeutic efficacy of Benserazide can be decreased when used in combination with Brexpiprazole.
Blonanserin The therapeutic efficacy of Benserazide can be decreased when used in combination with Blonanserin.
Melperone The therapeutic efficacy of Benserazide can be decreased when used in combination with Melperone.
Zotepine The therapeutic efficacy of Benserazide can be decreased when used in combination with Zotepine.
Brilaroxazine The therapeutic efficacy of Benserazide can be decreased when used in combination with Brilaroxazine.
Amisulpride The therapeutic efficacy of Benserazide can be decreased when used in combination with Amisulpride.
Loxapine The therapeutic efficacy of Benserazide can be decreased when used in combination with Loxapine.
Promazine The therapeutic efficacy of Benserazide can be decreased when used in combination with Promazine.
Prochlorperazine The therapeutic efficacy of Benserazide can be decreased when used in combination with Prochlorperazine.
Droperidol The therapeutic efficacy of Benserazide can be decreased when used in combination with Droperidol.
Chlorpromazine The therapeutic efficacy of Benserazide can be decreased when used in combination with Chlorpromazine.
Haloperidol The therapeutic efficacy of Benserazide can be decreased when used in combination with Haloperidol.
Fluphenazine The therapeutic efficacy of Benserazide can be decreased when used in combination with Fluphenazine.
Thioridazine The therapeutic efficacy of Benserazide can be decreased when used in combination with Thioridazine.
Trifluoperazine The therapeutic efficacy of Benserazide can be decreased when used in combination with Trifluoperazine.
Perphenazine The therapeutic efficacy of Benserazide can be decreased when used in combination with Perphenazine.
Mesoridazine The therapeutic efficacy of Benserazide can be decreased when used in combination with Mesoridazine.
Pimozide The therapeutic efficacy of Benserazide can be decreased when used in combination with Pimozide.
Chlorprothixene The therapeutic efficacy of Benserazide can be decreased when used in combination with Chlorprothixene.
Methotrimeprazine The therapeutic efficacy of Benserazide can be decreased when used in combination with Methotrimeprazine.
Periciazine The therapeutic efficacy of Benserazide can be decreased when used in combination with Periciazine.
Molindone The therapeutic efficacy of Benserazide can be decreased when used in combination with Molindone.
Thioproperazine The therapeutic efficacy of Benserazide can be decreased when used in combination with Thioproperazine.
Thiothixene The therapeutic efficacy of Benserazide can be decreased when used in combination with Thiothixene.
Zuclopenthixol The therapeutic efficacy of Benserazide can be decreased when used in combination with Zuclopenthixol.
Azaperone The therapeutic efficacy of Benserazide can be decreased when used in combination with Azaperone.
Bupropion The risk or severity of adverse effects can be increased when Bupropion is combined with Benserazide.
Cyclosporine Cyclosporine may decrease the excretion rate of Benserazide which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Benserazide which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Benserazide which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Benserazide which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Benserazide which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Benserazide which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Benserazide which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Benserazide which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Benserazide which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Benserazide which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Benserazide which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Benserazide which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Benserazide which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Benserazide which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Benserazide which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Benserazide which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Benserazide which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Benserazide which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Benserazide which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Benserazide which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Benserazide which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Benserazide which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Benserazide which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Benserazide which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Benserazide which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Benserazide which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Benserazide which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Benserazide which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Benserazide which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Benserazide which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Benserazide which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Benserazide which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Benserazide which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Benserazide which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Benserazide which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Benserazide which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Benserazide which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Benserazide which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Benserazide which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Benserazide which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Benserazide which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Benserazide which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Benserazide which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Benserazide which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Benserazide which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Benserazide which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Benserazide which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Benserazide which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Benserazide which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Benserazide which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Benserazide which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Benserazide which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Benserazide which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Benserazide which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Benserazide which could result in a higher serum level.

Target Protein

Aromatic-L-amino-acid decarboxylase DDC

Referensi & Sumber

Textbook
  • ISBN: 1498794610
    Caroline Ashley, Aileen Dunleavy (2017). The Renal Drug Handbook: The Ultimate Prescribing Guide for Renal Practitioners (4th ed.). CRC Press.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Prolopa Cap 100-25
    Capsule • - • Oral • Canada • Approved
  • Prolopa Cap 200-50
    Capsule • - • Oral • Canada • Approved
  • Prolopa Cap 50-12.5
    Capsule • - • Oral • Canada • Approved

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