Peringatan Keamanan

The LD50 of carbidopa is reported to be in the rat of 4810 mg/kg.MSDS In animal studies, carbidopa showed no incidences on neoplasia and showed no effect on the fertility status and development.FDA label

No reports of overdosage have been registered with the carbidopa-only product. In the event of overdosage, immediate gastric lavage is recommended as well as intravenous fluid administration. Continuous electrocardiographic monitoring is required.FDA label

Carbidopa

DB00190

small molecule approved

Deskripsi

Carbidopa presents a chemical denomination of N-amino-alpha-methyl-3-hydroxy-L-tyrosine monohydrate. It potently inhibits aromatic amino acid decarboxylase (DDC) and due to its chemical properties, it does not cross the blood-brain barrier. Due to its activity, carbidopa is always administered concomitantly with levodopa. An individual formulation containing solely carbidopa was generated to treat nausea in patients where the combination therapy levodopa/carbidopa is not efficient reducing nausea.T394

The first approved product by the FDA containing only carbidopa was developed by Amerigens Pharmaceuticals Ltd and approved on 2014.L5110 On the other hand, the combination treatment of carbidopa/levodopa was originally developed by Watson Labs but the historical information by the FDA brings back to the approval of this combination therapy developed by Mayne Pharma in 1992.L5113

Struktur Molekul 2D

Berat 226.2292
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The reported half-life of carbidopa is of approximately 107 minutes.[A173944]
Volume Distribusi The volume of distribution reported for the combination therapy of carbidopa/[levodopa] is of 3.6 L/kg.[A173947] However, carbidopa is widely distributed in the tissues, except in the brain.[L5116] After one hour, carbidopa is found mainly in the kidney, lungs, small intestine and liver.[A274]
Klirens (Clearance) The reported clearance rate for the combination therapy of [levodopa]/carbidopa is 51.7 L/h.[A173947]

Absorpsi

When levodopa/carbidopa is administered orally, 40-70% of the administered dose is absorbed.L5116 Once absorbed, carbidopa shows bioavailability of 58%.A173941 A maximum concentration of 0.085 mcg/ml was achieved after 143 min with an AUC of 19.28 mcg.min/ml.A173944

Metabolisme

The loss of the hydrazine functional group (probably as molecular nitrogen) represents the major metabolic pathway for carbidopa. There are several metabolites of carbidopa metabolism including 3-(3,4-dihydroxyphenyl)-2-methylpropionic acid, 3-(4-hydroxy-3-methoxyphenyl)-2-methylpropionic acid, 3-(3-hydroxyphenyl)-2-methylpropionic acid, 3-(4-hydroxy-3-methoxyphenyl)-2-methyllactic acid, 3-(3-hydroxyphenyl)-2-methyllactic acid, and 3,4-dihydroxyphenylacetone (1,2).A274

Rute Eliminasi

In animal studies, 66% of the administered dose of carbidopa was eliminated via the urine while 11% was found in feces. These studies were performed in humans and it was observed a urine excretion covering 50% of the administered dose.A274

Interaksi Obat

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

Target Protein

Aromatic-L-amino-acid decarboxylase DDC

Referensi & Sumber

Synthesis reference: Sweta GUPTA, "EXTENDED RELEASE PHARMACEUTICAL DOSAGE FORMS OF CARBIDOPA AND LEVODOPA AND PROCESS OF PREPARATION THEREOF." U.S. Patent US20130195973, issued August 01, 2013.
Artikel (PubMed)
  • PMID: 4150141
    Vickers S, Stuart EK, Bianchine JR, Hucker HB, Jaffe ME, Rhodes RE, Vandenheuvel WJ: Metabolism of carbidopa (1-(-)-alpha-hydrazino-3,4-dihydroxy-alpha-methylhydrocinnamic acid monohydrate), an aromatic amino acid decarboxylase inhibitor, in the rat, rhesus monkey, and man. Drug Metab Dispos. 1974 Jan-Feb;2(1):9-22.
  • PMID: 804550
    Vickers S, Stuart EK, Hucker HB: Further studies on the metabolism of carbidopa, (minus)-L-alpha-hydrazino-3,4-dihydroxy-alpha-methylbenzenepropanoic acid monohydrate, in the human, Rhesus monkey, dog, and rat. J Med Chem. 1975 Feb;18(2):134-8.
  • PMID: 28236251
    Mittur A, Gupta S, Modi NB: Pharmacokinetics of Rytary((R)), An Extended-Release Capsule Formulation of Carbidopa-Levodopa. Clin Pharmacokinet. 2017 Sep;56(9):999-1014. doi: 10.1007/s40262-017-0511-y.
  • PMID: 11106255
    Gilbert JA, Frederick LM, Ames MM: The aromatic-L-amino acid decarboxylase inhibitor carbidopa is selectively cytotoxic to human pulmonary carcinoid and small cell lung carcinoma cells. Clin Cancer Res. 2000 Nov;6(11):4365-72.
  • PMID: 2685649
    Yeh KC, August TF, Bush DF, Lasseter KC, Musson DG, Schwartz S, Smith ME, Titus DC: Pharmacokinetics and bioavailability of Sinemet CR: a summary of human studies. Neurology. 1989 Nov;39(11 Suppl 2):25-38.
  • PMID: 22549097
    Nyholm D, Lewander T, Gomes-Trolin C, Backstrom T, Panagiotidis G, Ehrnebo M, Nystrom C, Aquilonius SM: Pharmacokinetics of levodopa/carbidopa microtablets versus levodopa/benserazide and levodopa/carbidopa in healthy volunteers. Clin Neuropharmacol. 2012 May-Jun;35(3):111-7. doi: 10.1097/WNF.0b013e31825645d1.
  • PMID: 12942590
    Chana P, Fierro A, Reyes-Parada M, Saez-Briones P: Pharmacokinetic comparison of Sinemet and Grifoparkin (levodopa/carbidopa 250/25 mg) in Parkinson s disease: a single dose study. Rev Med Chil. 2003 Jun;131(6):623-31.
Textbook
  • ISBN: 978-0-7020-3471-8
    Rang, H. P. and Dale, M. M. (2012). Rang and Dale's Pharmacology (7th ed.). Edinburgh: Elsevier/Churchill Livingstone.
  • ISBN: 978-0-19-537177-2
    Ahlskog J. (2009). Parkinson's disease treatment guide for physicians. Oxford University Press.

Contoh Produk & Brand

Produk: 510 • International brands: 0
Produk
  • Aa-levocarb CR
    Tablet, extended release • - • Oral • Canada • Generic • Approved
  • Aa-levocarb CR
    Tablet, extended release • - • Oral • Canada • Generic • Approved
  • Ag-levocarb
    Tablet • - • Oral • Canada • Generic • Approved
  • Ag-levocarb
    Tablet • - • Oral • Canada • Generic • Approved
  • Ag-levocarb
    Tablet • - • Oral • Canada • Generic • Approved
  • Apo-levocarb
    Tablet • - • Oral • Canada • Generic • Approved
  • Apo-levocarb
    Tablet • - • Oral • Canada • Generic • Approved
  • Apo-levocarb
    Tablet • - • Oral • Canada • Generic • Approved
Menampilkan 8 dari 510 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul