Description

Simple

A medication used to treat severe pain.

Clinical

An opioid agonist used as an analgesic and antitussive agent.

Overview

Hydrocodone is a synthetic opioid derivative of codeine.[14] 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 Historically, hydrocodone has been used as a cough suppressant although this has largely been replaced by [dextromethorphan] in current cough and cold formulations.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.[17]

Pharmacology

Indication

Hydrocodone is indicated for the management of acute pain, sometimes in combination with [acetaminophen] or [ibuprofen], as well as the symptomatic treatment of the common cold and allergic rhinitis in combination with decongestants, antihistamines, and expectorants.[label, Read more

Pharmacodynamic

Hydrocodone inhibits pain signaling in both the spinal cord and brain [12]. Its actions in the brain also produce euphoria, respirat... Read more

Mechanism of action

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

Absorption

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.[ 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 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 dos... Read more

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.[ 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 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 diff... Read more

Toxicity

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.[ Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Nausea US
  • Kind: experimental
    • Percent: 8-16
  • Kind: placebo
    • Percent: 5
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 3-9
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 8
  • Kind: placebo
    • Percent: 5
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 6-7
  • Kind: placebo
    • Percent: 3
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 2-7
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 3-7
  • Kind: placebo
    • Percent: 2
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 6
  • Kind: placebo
    • Percent: 3
  • Clinical Trial
    Chest Pain US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Abdominal Pain Upper US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Arthralgia US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Chills US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Sedation US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Depression US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Nasopharyngitis US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Hypertension US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Gastroenteritis US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Hyperhidrosis US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Gastroenteritis viral US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Influenza US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Cough US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Oropharyngeal pain US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Migraine US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Pyrexia US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Edema peripheral US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Gastro-esophageal Reflux Disease (GERD) US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Muscle Spasms US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Bronchitis US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Pain US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Decreased appetite US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Sinusitis US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Back Pain US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Musculoskeletal Pain US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Pain in extremity US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Hot flush US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Muscle Strain US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Urinary Tract Infection US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Nasal Congestion US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Pruritus US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Fall US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Dyspepsia US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Lethargy US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Tinnitus US
  • Kind: experimental
    • Percent: 1-5
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: ≥5
  • 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. Profound CNS depression, including sedation, respiratory depression, coma, and death may occur.

    Take with or without food. Cmax and AUC are not altered by food in a clinically significant way.