Peringatan Keamanan

Overdosage with benzhydrocodone 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.L4894

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.L4894 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.

Benzhydrocodone

DB15465

small molecule approved

Deskripsi

Benzhydrocodone is a benzylic prodrug of hydrocodone.L4894 It was developed in an effort to reduce parenteral bioavailability of the active metabolite as a deterrent to abuse.A182177 Benzhydrocodone is indicated for use in the short-term management of pain. It was first approved by the FDA in February 2018 in combination with acetaminophen under the trade name Apadaz, marketed by KVK Tech and developed by KemPharm.L7859,L7862

Struktur Molekul 2D

Berat 403.478
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The hydrocodone metabolite has a half life of elimination of 4.5 h.[L4894]
Volume Distribusi The hydrocodone metabolite of benzhydrocodone has an apparent volume of distribution of 714 L.[A182150]
Klirens (Clearance) The apparent clearance of the hydrocodone metabolite is 64.4 L/h.[A182150]

Absorpsi

The absorption profile of benzhydrocodone meets the FDA bioequivalence requirements for similar hydrocodone immediate-release products.L4894 Benzhydrocodone itself is rapidly metabolized by intestinal enzymes to the active metabolite, hydrocodone, with no detectable benzhydrocodone reaching circulation. Single oral doses of 6.67 mg benzhydrocodone produces a Cmax of 19.18 ng/mL with a Tmax of 1.25 h and an AUC of 125.73 h*ng/mL. Administration with food may slightly delay absorption but has no significant effect on AUC.

Metabolisme

Benzhydrocodone is rapidly metabolized to hydrocodone by intestinal enzymes.L4894 Hydrocodone undergoes oxidative metabolism by CYP3A4 and CYP2D6 which contribute to N-demethylation and O-demethylation respectively.L4894,A14920 The dealkylated metabolites undergo further 6-ketoreduction to the 6-?- and 6-?-hydroxy metabolites as well as glucuronide conjugation.A182114

Rute Eliminasi

The hydrocodone metabolite is eliminated through a mix of metabolism and renal excretion.L4894,A182150

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Ingesting alcohol may increase the CNS depressive effects of benzhydrocodone. Apadaz also contains acetaminophen, which, when combined with alcohol, may increase the risk of hepatotoxicity.
  • 2. Take with or without food. Co-administration with food slightly alters pharmacokinetics, but not to a clinically significant extent.

Interaksi Obat

492 Data
Alvimopan The risk or severity of adverse effects can be increased when Benzhydrocodone is combined with Alvimopan.
Desmopressin The risk or severity of hyponatremia can be increased when Benzhydrocodone is combined with Desmopressin.
Morphine The risk or severity of adverse effects can be increased when Morphine is combined with Benzhydrocodone.
Codeine The risk or severity of adverse effects can be increased when Codeine is combined with Benzhydrocodone.
Hydromorphone The risk or severity of adverse effects can be increased when Hydromorphone is combined with Benzhydrocodone.
Meperidine The risk or severity of adverse effects can be increased when Meperidine is combined with Benzhydrocodone.
Oxycodone The risk or severity of adverse effects can be increased when Oxycodone is combined with Benzhydrocodone.
Dextropropoxyphene The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Benzhydrocodone.
Naltrexone The therapeutic efficacy of Benzhydrocodone can be decreased when used in combination with Naltrexone.
Sufentanil The risk or severity of adverse effects can be increased when Sufentanil is combined with Benzhydrocodone.
Alfentanil The risk or severity of adverse effects can be increased when Alfentanil is combined with Benzhydrocodone.
Fentanyl The risk or severity of adverse effects can be increased when Fentanyl is combined with Benzhydrocodone.
Levorphanol The risk or severity of adverse effects can be increased when Levorphanol is combined with Benzhydrocodone.
Remifentanil The risk or severity of adverse effects can be increased when Remifentanil is combined with Benzhydrocodone.
Hydrocodone The risk or severity of adverse effects can be increased when Hydrocodone is combined with Benzhydrocodone.
Diphenoxylate The risk or severity of adverse effects can be increased when Diphenoxylate is combined with Benzhydrocodone.
Oxymorphone The risk or severity of adverse effects can be increased when Oxymorphone is combined with Benzhydrocodone.
Dezocine The risk or severity of adverse effects can be increased when Dezocine is combined with Benzhydrocodone.
Methadyl acetate The risk or severity of adverse effects can be increased when Methadyl acetate is combined with Benzhydrocodone.
Dihydroetorphine The risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Benzhydrocodone.
Diamorphine The risk or severity of adverse effects can be increased when Diamorphine is combined with Benzhydrocodone.
Bezitramide The risk or severity of adverse effects can be increased when Bezitramide is combined with Benzhydrocodone.
Ethylmorphine The risk or severity of adverse effects can be increased when Ethylmorphine is combined with Benzhydrocodone.
Etorphine The risk or severity of adverse effects can be increased when Etorphine is combined with Benzhydrocodone.
Dextromoramide The risk or severity of adverse effects can be increased when Dextromoramide is combined with Benzhydrocodone.
Desomorphine The risk or severity of adverse effects can be increased when Desomorphine is combined with Benzhydrocodone.
Carfentanil The risk or severity of adverse effects can be increased when Carfentanil is combined with Benzhydrocodone.
Dihydrocodeine The risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Benzhydrocodone.
Alphacetylmethadol The risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Benzhydrocodone.
Dihydromorphine The risk or severity of adverse effects can be increased when Dihydromorphine is combined with Benzhydrocodone.
Tapentadol The risk or severity of adverse effects can be increased when Tapentadol is combined with Benzhydrocodone.
Ketobemidone The risk or severity of adverse effects can be increased when Ketobemidone is combined with Benzhydrocodone.
DPDPE The risk or severity of adverse effects can be increased when DPDPE is combined with Benzhydrocodone.
Lofentanil The risk or severity of adverse effects can be increased when Lofentanil is combined with Benzhydrocodone.
Opium The risk or severity of adverse effects can be increased when Opium is combined with Benzhydrocodone.
Normethadone The risk or severity of adverse effects can be increased when Normethadone is combined with Benzhydrocodone.
Piritramide The risk or severity of adverse effects can be increased when Piritramide is combined with Benzhydrocodone.
Alphaprodine The risk or severity of adverse effects can be increased when Alphaprodine is combined with Benzhydrocodone.
Nicomorphine The risk or severity of adverse effects can be increased when Nicomorphine is combined with Benzhydrocodone.
Meptazinol The therapeutic efficacy of Benzhydrocodone can be decreased when used in combination with Meptazinol.
Phenoperidine The risk or severity of adverse effects can be increased when Phenoperidine is combined with Benzhydrocodone.
Phenazocine The risk or severity of adverse effects can be increased when Phenazocine is combined with Benzhydrocodone.
Tilidine The risk or severity of adverse effects can be increased when Tilidine is combined with Benzhydrocodone.
Carfentanil, C-11 The risk or severity of adverse effects can be increased when Carfentanil, C-11 is combined with Benzhydrocodone.
Naloxegol The risk or severity of adverse effects can be increased when Naloxegol is combined with Benzhydrocodone.
Oliceridine The risk or severity of adverse effects can be increased when Oliceridine is combined with Benzhydrocodone.
Pegvisomant The therapeutic efficacy of Pegvisomant can be decreased when used in combination with Benzhydrocodone.
Succinylcholine The risk or severity of bradycardia can be increased when Succinylcholine is combined with Benzhydrocodone.
Fluvoxamine The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Fluvoxamine.
Citalopram The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Citalopram.
Duloxetine The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Duloxetine.
Trazodone The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Trazodone.
Sertraline The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Sertraline.
Sibutramine The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Sibutramine.
Nefazodone The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Nefazodone.
Zimelidine The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Zimelidine.
Dapoxetine The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Dapoxetine.
Milnacipran The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Desvenlafaxine.
Seproxetine The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Seproxetine.
Indalpine The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Indalpine.
Ritanserin The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Ritanserin.
Alaproclate The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Alaproclate.
Amphetamine Amphetamine may increase the analgesic activities of Benzhydrocodone.
Phentermine Phentermine may increase the analgesic activities of Benzhydrocodone.
Pseudoephedrine Pseudoephedrine may increase the analgesic activities of Benzhydrocodone.
Benzphetamine Benzphetamine may increase the analgesic activities of Benzhydrocodone.
Diethylpropion Diethylpropion may increase the analgesic activities of Benzhydrocodone.
Lisdexamfetamine Lisdexamfetamine may increase the analgesic activities of Benzhydrocodone.
Mephentermine Mephentermine may increase the analgesic activities of Benzhydrocodone.
MMDA MMDA may increase the analgesic activities of Benzhydrocodone.
Midomafetamine Midomafetamine may increase the analgesic activities of Benzhydrocodone.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may increase the analgesic activities of Benzhydrocodone.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may increase the analgesic activities of Benzhydrocodone.
Tenamfetamine Tenamfetamine may increase the analgesic activities of Benzhydrocodone.
Chlorphentermine Chlorphentermine may increase the analgesic activities of Benzhydrocodone.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may increase the analgesic activities of Benzhydrocodone.
Dextroamphetamine Dextroamphetamine may increase the analgesic activities of Benzhydrocodone.
Metamfetamine Metamfetamine may increase the analgesic activities of Benzhydrocodone.
Iofetamine I-123 Iofetamine I-123 may increase the analgesic activities of Benzhydrocodone.
Ritobegron Ritobegron may increase the analgesic activities of Benzhydrocodone.
Mephedrone Mephedrone may increase the analgesic activities of Benzhydrocodone.
Methoxyphenamine Methoxyphenamine may increase the analgesic activities of Benzhydrocodone.
Gepefrine Gepefrine may increase the analgesic activities of Benzhydrocodone.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may increase the analgesic activities of Benzhydrocodone.
Phendimetrazine Phendimetrazine may increase the analgesic activities of Benzhydrocodone.
Tramadol The risk or severity of adverse effects can be increased when Tramadol is combined with Benzhydrocodone.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Benzhydrocodone.
Levacetylmethadol The risk or severity of adverse effects can be increased when Levacetylmethadol is combined with Benzhydrocodone.
Fluoxetine The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Fluoxetine.
Paroxetine The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Paroxetine.
Escitalopram The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Escitalopram.
Trospium The risk or severity of adverse effects can be increased when Trospium is combined with Benzhydrocodone.
Oxyphenonium The risk or severity of adverse effects can be increased when Oxyphenonium is combined with Benzhydrocodone.
Butabarbital The risk or severity of adverse effects can be increased when Butabarbital is combined with Benzhydrocodone.
Butalbital The risk or severity of adverse effects can be increased when Butalbital is combined with Benzhydrocodone.
Benzatropine The risk or severity of adverse effects can be increased when Benzatropine is combined with Benzhydrocodone.
Ziprasidone The risk or severity of adverse effects can be increased when Ziprasidone is combined with Benzhydrocodone.
Disopyramide The risk or severity of adverse effects can be increased when Disopyramide is combined with Benzhydrocodone.
Talbutal The risk or severity of adverse effects can be increased when Talbutal is combined with Benzhydrocodone.

Target Protein

Mu-type opioid receptor OPRM1

Referensi & Sumber

Synthesis reference: U.S. Patent 2018 / 0055836 A1.
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: 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.
  • PMID: 14998425
    Hutchinson MR, Menelaou A, Foster DJ, Coller JK, Somogyi AA: CYP2D6 and CYP3A4 involvement in the primary oxidative metabolism of hydrocodone by human liver microsomes. Br J Clin Pharmacol. 2004 Mar;57(3):287-97.
  • PMID: 29025138
    Guenther SM, Mickle TC, Barrett AC, Roupe KA, Zhou J, Lam V: Relative Bioavailability, Intranasal Abuse Potential, and Safety of Benzhydrocodone/Acetaminophen Compared with Hydrocodone Bitartrate/Acetaminophen in Recreational Drug Abusers. Pain Med. 2018 May 1;19(5):955-966. doi: 10.1093/pm/pnx195.

Contoh Produk & Brand

Produk: 9 • International brands: 0
Produk
  • Apadaz
    Tablet • - • Oral • US • Approved
  • Apadaz
    Tablet • - • Oral • US • Approved
  • Apadaz
    Tablet • - • Oral • US • Approved
  • Apadaz
    Tablet • - • Oral • US • Approved
  • Apadaz
    Tablet • - • Oral • US • Approved
  • Apadaz
    Tablet • - • Oral • US • Approved
  • Benzhydrocodone and Acetaminophen
    Tablet • - • Oral • US • Generic • Approved
  • Benzhydrocodone and Acetaminophen
    Tablet • - • Oral • US • Generic • Approved
Menampilkan 8 dari 9 produk.

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