Hydrocodone


Description

Narcotic analgesic related to codeine, but more potent and more addicting by weight. It is used also as cough suppressant.

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Pharmacology

Indication

Hydrocodone is indicated for the management of acute pain, sometimes in combination with [acetaminop... Read more

Pharmacodynamic

Hydrocodone inhibits pain signaling in both the spinal cord and brain [ Read more

Mechanism of action

Hydrocodone binds to the mu opioid receptor (MOR) with the highest affinity followed by the delta (D... Read more

Absorption

The absolute bioavailability of hydrocodone has not been characterized due to lack of an IV formulat... Read more

Protein binding

Hydrocodone is 36% bound to plasma proteins.[label]

Volume of distribution

The apparent volume of distribution ranges widely in published literature. The official FDA labeling... Read more

Clearance

Official FDA labeling reports an apparent clearance of 83 L/h.[label] Pharmacokinetic studies report... Read more

Half life

The half-life of elimination reported for hydrocodone is 7-9 h.[label, Read more

Route of elimination

Most hydrocodone appears to be eliminated via a non-renal route as renal clearance is substantially... Read more

Toxicity

Overdosage with hydrocodone presents as opioid intoxication including respiratory depression, somnol... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Headache US
  • Kind: experimental
    • Percent: 27%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 22%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 22%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 21%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 14%
  • Clinical Trial
    Dyspepsia US
  • Kind: experimental
    • Percent: 12%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 8-11%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Neck Pain US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Pain in extremity US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Osteoarthritis US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Lethargy US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Migraine US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Paresthesia US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Depression US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Dyspnea US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Cough US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Hyperhidrosis US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Night Sweats US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Hot flush US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Andominal discomfort US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Pain US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Non-Cardiac Chest Pain US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Gastroesophageal Reflux Disease US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Contusion US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Pyrexia US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Peripheral Edema US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Foot fracture US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Fall US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Muscle Strain US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Joint injury US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Joint sprain US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Increased blood cholesterol US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Increased gamma-glutamyltransferase US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Skin laceration US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Hypokalemia US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Dehydration US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Arthralgia US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Musculoskeletal Pain US
  • Kind: experimental
    • Percent: ≥1%-<10%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 7-10%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: 3-9%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 3-9%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 3-9%
  • Clinical Trial
    Infection US
  • Kind: experimental
    • Percent: 3-9%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 3-9%
  • Clinical Trial
    Sweating US
  • Kind: experimental
    • Percent: 3-9%
  • Clinical Trial

    Contraindications

    • Recommended Actions:
      • Allow 2 weeks washout time before use.
    • Regions: Canada
    • With Categories:
        • Name: Monoamine Oxidase Inhibitors
        • Drugbank Id: DBCAT001004
        • Mesh Id: D008996
    • Regions: Canada
    • Patient Conditions:
        • Name: Head Injury
        • Drugbank Id: DBCOND0028168
    • Regions: Canada
    • Patient Conditions:
        • Name: Increased Intracranial Pressure
        • Drugbank Id: DBCOND0035283
    • Regions: Canada
    • Patient Conditions:
        • Name: Increased cerebrospinal pressure
        • Drugbank Id: DBCOND0108655
    • Regions: Canada
    • Patient Conditions:
        • Name: Severe CNS depression
        • Drugbank Id: DBCOND0107893
        • Modification Of:
          • Base:
            • Name: CNS depression
            • Drugbank Id: DBCOND0094584
          • Severity:
            • Includes:
              • severe
    • Regions: Canada
    • Patient Conditions:
        • Name: Convulsive disorder
        • Drugbank Id: DBCOND0100202
    • Regions: Canada
    • Patient Conditions:
        • Name: Delirium tremens
        • Drugbank Id: DBCOND0011983
    • Regions: Canada
    • Patient Conditions:
        • Name: Acute alcoholism
        • Drugbank Id: DBCOND0107892
        • Modification Of:
          • Base:
            • Name: Alcoholism
            • Drugbank Id: DBCOND0006017
          • Severity:
            • Includes:
              • acute
    • Regions: Canada
    • Patient Conditions:
        • Name: Cor Pulmonale
        • Drugbank Id: DBCOND0042897
    • Regions: Canada
    • Patient Conditions:
        • Name: Elevated carbon dioxide levels in the blood
        • Drugbank Id: DBCOND0107891
    • Regions: Canada
    • Patient Conditions:
        • Name: Status Asthmaticus
        • Drugbank Id: DBCOND0001831
    • Regions: Canada
    • Patient Conditions:
        • Name: Chronic obstructive airway
        • Drugbank Id: DBCOND0107887
    • Regions: Canada
    • Patient Conditions:
        • Name: Suspected surgical abdomen
        • Drugbank Id: DBCOND0107886
    • Regions: US
    • Below Age:
      • Amount: 6
      • Unit: year
    • Hypersensitivity:
      • true
    • Regions: US
    • Regions: US
    • With Therapies:
        • Name: Paralytic Ileus
        • Drugbank Id: DBCOND0047064
    • Regions: US
    • Patient Conditions:
        • Name: Gastrointestinal obstruction
        • Drugbank Id: DBCOND0010786
    • Regions: US
    • Patient Conditions:
        • Name: Unmonitored severe bronchial asthma
        • Drugbank Id: DBCOND0108052
    • Regions: US
    • Patient Conditions:
        • Name: Unmonitored acute bronchial asthma
        • Drugbank Id: DBCOND0107581
    • Regions: US
    • Patient Conditions:
        • Name: Acute bronchial asthma in the absence of resuscitative equipment
        • Drugbank Id: DBCOND0121758
    • Regions: US
    • Patient Conditions:
        • Name: Severe bronchial asthma in the absence of resuscitative equipment
        • Drugbank Id: DBCOND0121759
    • Regions: US
    • Patient Conditions:
        • Name: Significant respiratory depression
        • Drugbank Id: DBCOND0107580

    Food Interactions

    • Avoid alcohol.
    • Take with food.
    • To avoid constipation: increase your daily intake of fiber (beans, whole grains, vegetables).

    Interactions

    Type in a drug name to check for interaction with Hydrocodone

    The metabolism of (R)-warfarin can be decreased when combined with Hydrocodone.
    The metabolism of (S)-Warfarin can be decreased when combined with Hydrocodone.
    The metabolism of Hydrocodone can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
    The risk or severity of serotonin syndrome can be increased when Hydrocodone is combined with 2,5-Dimethoxy-4-ethylamphetamine.
    The risk or severity of serotonin syndrome can be increased when Hydrocodone is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Hydrocodone.
    The risk or severity of serotonin syndrome can be increased when Hydrocodone is combined with 4-Bromo-2,5-dimethoxyamphetamine.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Hydrocodone.
    4-Methoxyamphetamine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
    The metabolism of 5-androstenedione can be decreased when combined with Hydrocodone.
    The risk or severity of serotonin syndrome can be increased when Hydrocodone is combined with 5-methoxy-N,N-dimethyltryptamine.
    The metabolism of Hydrocodone can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Hydrocodone.
    The metabolism of Hydrocodone can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    7-Nitroindazole may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
    7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the serotonergic and central nervous system depressant (CNS depressant) activities of Hydrocodone.
    The metabolism of 9-aminocamptothecin can be decreased when combined with Hydrocodone.
    The metabolism of Hydrocodone can be increased when combined with Abatacept.
    The metabolism of Abemaciclib can be decreased when combined with Hydrocodone.
    The metabolism of Hydrocodone can be decreased when combined with Abiraterone.

    References

    • 1 . 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. [PubMed: 23719682]
    • 2 . 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. [PubMed: 25621429]
    • 3 . 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. [PubMed: 25196888]
    • 4 . 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. [PubMed: 7693389]
    • 5 . 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. [PubMed: 27662264]
    • 6 . 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. [PubMed: 25653563]
    • 7 . 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. [PubMed: 30327606]
    • 8 . 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. [PubMed: 28931]
    • 9 . 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. [PubMed: 14998425]
    • 10 . Kapil RP, Cipriano A, Wen W, Yu Lynch S, He E, Colucci SV, Harris SC: Pharmacokinetic Profile and Sustained 24-hour Analgesia of a Once-daily Hydrocodone Bitartrate Extended-release Tablet with Abuse-deterrent Properties. Clin Ther. 2016 Feb;38(2):302-14. doi: 10.1016/j.clinthera.2015.12.003. Epub 2015 Dec 31. [PubMed: 26749219]
    • 11 . Sauberan JB, Anderson PO, Lane JR, Rafie S, Nguyen N, Rossi SS, Stellwagen LM: Breast milk hydrocodone and hydromorphone levels in mothers using hydrocodone for postpartum pain. Obstet Gynecol. 2011 Mar;117(3):611-7. doi: 10.1097/AOG.0b013e31820ca504. [PubMed: 21343764]
    • 12 . Trescot AM, Datta S, Lee M, Hansen H: Opioid pharmacology. Pain Physician. 2008 Mar;11(2 Suppl):S133-53. [PubMed: 18443637]
    • 13 . Olson KM, Duron DI, Womer D, Fell R, Streicher JM: Comprehensive molecular pharmacology screening reveals potential new receptor interactions for clinically relevant opioids. PLoS One. 2019 Jun 6;14(6):e0217371. doi: 10.1371/journal.pone.0217371. eCollection 2019. [PubMed: 31170174]
    • 14 . FDA Label: Hydrocodone Tab ER [Link]
    • 15 . DPD Monograph: Dimetane Syrup [Link]

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