Peringatan Keamanan

Overdosage with hydrocodone presents as opioid intoxication including respiratory depression, somnolence, coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, pulmonary edema, bradycardia, hypotension, partial or complete airway obstruction, atypical snoring, and death.L7913

In case of oversdosage the foremost priority is the maintenance of a patent and protected airway with the provision of assisted ventilation if necessary. Supportive measures such as IV fluids, supplemental oxygen, and vasopressors may be used to manage circulatory shock.L7913 Advanced life support may be necessary in the case of cardiac arrest or arrhythmias. Opioid antagonists such as naloxone may be used to reverse the respiratory and circulatory effects of hydrocodone. Emergency monitoring is still required after naloxone administration as the opioid effects may reappear. Additionally, if used in an opioid tolerant patient, naloxone may produce opioid withdrawal symptoms.

Hydrocodone

DB00956

small molecule approved illicit investigational

Deskripsi

Hydrocodone is a synthetic opioid derivative of codeine.T116 It is commonly used in combination with acetaminophen to control moderate to severe pain. Historically, hydrocodone has been used as a cough suppressant although this has largely been replaced by dextromethorphan in current cough and cold formulations. Hydrocodone's more potent metabolite, hydromorphone has also found wide use as an analgesic and is frequently used in cases of severe pain. The FDA first approved Hydrocodone for use as part of the cough suppressant syrup Hycodan in March of 1943.L9025

Struktur Molekul 2D

Berat 299.3642
Wujud solid

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 elimination reported for hydrocodone is 7-9 h.[label,A182564,A182582]
Volume Distribusi The apparent volume of distribution ranges widely in published literature. The official FDA labeling reports a value of 402 L.[label] Pharmacokinetic studies report values from 210-714 L with higher values associated with higher doses or single dose studies and lower values associated with lower doses and multiple dose studies.[A182498,A182504,A182507,A182510] Hydrocodone has been observed in human breast milk at levels equivalent to 1.6% of the maternal dosage.[A182612] Only 12 of the 30 women studied had detectable concentrations of hydromorphone at mean levels of 0.3 mcg/kg/day.
Klirens (Clearance) Official FDA labeling reports an apparent clearance of 83 L/h.[label] Pharmacokinetic studies report values ranging from 24.5-58.8 L/h largely dependent on CYP2D6 metabolizer status.[A182498,A182504,A182507,A182510]

Absorpsi

The absolute bioavailability of hydrocodone has not been characterized due to lack of an IV formulation. The liquid formulations of hydrocodone have a Tmax of 0.83-1.33 h.A182504,A182510 The extended release tablet formulations have a Tmax of 14-16 h.label The Cmax remains dose proportional over the range of 2.5-10 mg in liquid formulations and 20-120 mg in extended release formulations.A182504,A182510,label Administration with food increases Cmax by about 27% while Tmax and AUC remain the same.A182564 Administration with 40% ethanol has been observed to increase Cmax 2-fold with an approximate 20% increase in AUC with no change in Tmax. 20% alcohol produces no significant effect.

Metabolisme

Hydrocodone undergoes oxidative O-demethylation to form hydromorphone, a more potent active metabolite.A182114 Though hydromorphone is active it is not present in sufficient quantities to contribute significantly to hydrocodone's therapeutic effects.A182150 Both hydrocodone and hydromorphone form 6-?- and 6-?-hydroxy metabolites through 6-ketoreduction. The hydroxy metabolites and hydromorphone can form glucuronide conjugates. Hydrocodone also undergoes oxidative N-demthylation to norhydrocodone. O-demethylation is primarily catalyzed by CYP2D6 while N-demethylation is primarily CYP3A4.A14920

Rute Eliminasi

Most hydrocodone appears to be eliminated via a non-renal route as renal clearance is substantially lower than total apparent clearance.label Hepatic metabolism may account for a portion of this, however the slight increase in serum concentration and AUC seen in hepatic impairment indicates a different primary route of elimination.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Profound CNS depression, including sedation, respiratory depression, coma, and death may occur.
  • 2. Take with or without food. Cmax and AUC are not altered by food in a clinically significant way.

Interaksi Obat

1134 Data
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Botulinum toxin type B Botulinum toxin type B may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Botulinum toxin type A Botulinum toxin type A may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Ethchlorvynol Ethchlorvynol may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Succinylcholine Succinylcholine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Reserpine Reserpine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Enflurane Enflurane may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Reboxetine Reboxetine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Butabarbital Butabarbital may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Methysergide Methysergide may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Clemastine Clemastine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Etomidate Etomidate may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Talbutal Talbutal may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Tolcapone Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Cetirizine Cetirizine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Trimethadione Trimethadione may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Chlorzoxazone Chlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Meprobamate Meprobamate may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Thiethylperazine Thiethylperazine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Sulpiride Sulpiride may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Dexbrompheniramine Dexbrompheniramine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Remoxipride Remoxipride may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Metocurine iodide Metocurine iodide may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Methocarbamol Methocarbamol may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Triprolidine Triprolidine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Prochlorperazine Prochlorperazine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Cyproheptadine Cyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Metharbital Metharbital may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Gallamine triethiodide Gallamine triethiodide may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Entacapone Entacapone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Triflupromazine Triflupromazine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Mephenytoin Mephenytoin may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Lamotrigine Lamotrigine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Cisatracurium Cisatracurium may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Ethosuximide Ethosuximide may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Paramethadione Paramethadione may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Fluphenazine Fluphenazine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Dexmedetomidine Dexmedetomidine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Dyclonine Dyclonine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Trimethobenzamide Trimethobenzamide may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Moricizine Moricizine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Tizanidine Tizanidine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Rocuronium Rocuronium may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Atracurium besylate Atracurium besylate may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Meclizine Meclizine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Riluzole Riluzole may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Scopolamine Scopolamine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Carbinoxamine Carbinoxamine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Isoflurane Isoflurane may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Clidinium Clidinium may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Propiomazine Propiomazine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Trifluoperazine Trifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Phensuximide Phensuximide may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Progabide Progabide may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Donepezil Donepezil may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Perphenazine Perphenazine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Alprenolol Alprenolol may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Tiagabine Tiagabine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Zonisamide Zonisamide may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Mesoridazine Mesoridazine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hexafluronium Hexafluronium may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Zaleplon Zaleplon may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Desloratadine Desloratadine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Alosetron Alosetron may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Ramelteon Ramelteon may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Dimenhydrinate Dimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Guanfacine Guanfacine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Methoxyflurane Methoxyflurane may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Acetophenazine Acetophenazine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Melatonin Melatonin may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Vigabatrin Vigabatrin may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Levocabastine Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Methyprylon Methyprylon may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Phenacemide Phenacemide may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Doxacurium Doxacurium may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Bupropion Bupropion may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Halothane Halothane may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Cyclizine Cyclizine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Chlormezanone Chlormezanone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Desflurane Desflurane may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Zopiclone Zopiclone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Tubocurarine Tubocurarine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Levetiracetam Levetiracetam may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Dantrolene Dantrolene may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Mivacurium Mivacurium may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Sevoflurane Sevoflurane may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Chlorprothixene Chlorprothixene may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Decamethonium Decamethonium may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Metocurine Metocurine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Pancuronium Pancuronium may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Pipecuronium Pipecuronium may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Vecuronium Vecuronium may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Butobarbital Butobarbital may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Heptabarbital Heptabarbital may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Penbutolol Penbutolol may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Glutethimide Glutethimide may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
gamma-Hydroxybutyric acid gamma-Hydroxybutyric acid may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Bufotenine Bufotenine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Diamorphine Diamorphine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.

Target Protein

Mu-type opioid receptor OPRM1
Delta-type opioid receptor OPRD1
Sigma non-opioid intracellular receptor 1 SIGMAR1

Referensi & Sumber

Synthesis reference: Anne M. Hailes, Christopher E. French, Neil C. Bruce, "Morphinone reductase for the preparation of hydromorphone and hydrocodone." U.S. Patent US5571685, issued November, 1990.
Artikel (PubMed)
  • PMID: 23719682
    Melhem MR, Rubino CM, Farr SJ, Robinson CY: Population pharmacokinetic analysis for hydrocodone following the administration of hydrocodone bitartrate extended-release capsules. Clin Pharmacokinet. 2013 Oct;52(10):907-17. doi: 10.1007/s40262-013-0081-6.
  • PMID: 25621429
    Linares OA, Fudin J, Daly AL, Boston RC: Individualized Hydrocodone Therapy Based on Phenotype, Pharmacogenetics, and Pharmacokinetic Dosing. Clin J Pain. 2015 Dec;31(12):1026-35. doi: 10.1097/AJP.0000000000000214.
  • PMID: 25196888
    Liu W, Dutta S, Kearns G, Awni W, Neville KA: Pharmacokinetics of hydrocodone/acetaminophen combination product in children ages 6-17 with moderate to moderately severe postoperative pain. J Clin Pharmacol. 2015 Feb;55(2):204-11. doi: 10.1002/jcph.394. Epub 2014 Sep 26.
  • PMID: 7693389
    Otton SV, Schadel M, Cheung SW, Kaplan HL, Busto UE, Sellers EM: CYP2D6 phenotype determines the metabolic conversion of hydrocodone to hydromorphone. Clin Pharmacol Ther. 1993 Nov;54(5):463-72. doi: 10.1038/clpt.1993.177.
  • PMID: 27662264
    Deng S, Huang W, Ni X, Zhang M, Lu H, Wang Z, Hu J, Zhu X, Qiu C, Shang D, Zhang Y, Xiong L, Wen Y: Pharmacokinetics of guaifenesin, pseudoephedrine and hydrocodone in a combination oral liquid formulation, administered as single and multiple doses in healthy Chinese volunteers, and comparison with data for individual compounds formulated as Antuss(R). Xenobiotica. 2017 Oct;47(10):870-878. doi: 10.1080/00498254.2016.1241451. Epub 2016 Oct 24.
  • PMID: 25653563
    Farr SJ, Robinson CY, Rubino CM: Effects of food and alcohol on the pharmacokinetics of an oral, extended-release formulation of hydrocodone in healthy volunteers. Clin Pharmacol. 2015 Jan 19;7:1-9. doi: 10.2147/CPAA.S70831. eCollection 2015.
  • PMID: 30327606
    Cardia L, Calapai G, Quattrone D, Mondello C, Arcoraci V, Calapai F, Mannucci C, Mondello E: Preclinical and Clinical Pharmacology of Hydrocodone for Chronic Pain: A Mini Review. Front Pharmacol. 2018 Oct 1;9:1122. doi: 10.3389/fphar.2018.01122. eCollection 2018.
  • PMID: 28931
    Cone EJ, Darwin WD, Gorodetzky CW, Tan T: Comparative metabolism of hydrocodone in man, rat, guinea pig, rabbit, and dog. Drug Metab Dispos. 1978 Jul-Aug;6(4):488-93.
Menampilkan 8 dari 13 artikel.
Textbook
  • ISBN: 978-1-25-958473-2
    Brunton LL, Hilal-Dandan R, Knollmann BC. eds (2018). Goodman & Gilman's: The Pharmacological Basis of Therapeutics (13th ed.). McGraw-Hill Education.

Contoh Produk & Brand

Produk: 1196 • International brands: 0
Produk
  • Antitussive hydrocodone bitartrate and homatropine methylbromide
    Tablet • - • Oral • US • Generic • Approved
  • Atuss HS Tannate
    Suspension • - • Oral • US
  • Caldomine Dh Adulte
    Liquid • - • Oral • Canada • Approved
  • Caldomine Dh Enfant
    Liquid • - • Oral • Canada • Approved
  • Co-gesic
    Tablet • - • Oral • US • Generic • Approved
  • Codofen
    Tablet • - • Oral • Canada • Approved
  • Coristine-DH Liq
    Syrup • - • Oral • Canada • Approved
  • Dalmacol
    Syrup • - • Oral • Canada • Approved
Menampilkan 8 dari 1196 produk.

Sekuens Gen/Protein (FASTA)

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