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    Hydrocodone molecular structure

    Hydrocodone Stats & Data

    Vike Vics Norco Hydro Lortab vicodin
    NPS DataHub
    MW299.37
    FormulaC18H21NO3
    CAS125-29-1
    IUPAC4,5α-epoxy-3-methoxy-17-methylmorphinan-6-one
    SMILESCOc1ccc2CC3N(C)CCC45C3CCC(=O)C5Oc1c24
    InChIKeyLLPOLZWFYMWNKH-CMKMFDCUSA-N
    Chemical Class Opioid
    Psychoactive Class Depressant
    Half-Life IR ≈ 4 h; ER ≈ 7–9 h

    Pharmacology

    DrugBank
    State Solid

    Description

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 Historically, hydrocodone has been used as a cough suppressant although this has largely been replaced by dextromethorphan in current cough and cold formulations.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

    Mechanism of Action

    Hydrocodone binds to the mu opioid receptor (MOR) with the highest affinity followed by the delta opioid receptors (DOR). Hydrocodone's agonist effect at the MOR is considered to contribute the most to its analgesic effects. Both MOR and DOR are Gi/o coupled and and produces its signal through activation of inward rectifier potassium (GIRK) channels, inhibition of voltage gated calcium channel opening, and decreased adenylyl cyclase activity. In the dorsal horn of the spinal cord, activation of pre-synaptic MOR on primary afferents the inhibition of calcium channel opening and increased activity of GIRK channels hyperpolarizes the neuron and prevents release of neurotransmitters. Post-synaptic MOR can also prevent activation of neurons by glutamate through the aforementioned mechanisms. Hydrocodone can also produce several actions in the brain similarly to other opioids. Activation of MOR in the periaquaductal gray (PAG) inhibits the GABAergic tone on medulo-spinal neurons. This allows these neurons, which project to the dorsal horn of the spinal cord, to suppress pain signalling in secondary afferents by activating inhibitory interneurons. MOR can also inhibit GABAergic neurons in the ventral tegmental area, removing the inhibitory tone on dopaminergic neurons in the nucleus accumbens and contributing to the activation of the brain's reward and addiction pathway.

    Pharmacodynamics

    Hydrocodone inhibits pain signaling in both the spinal cord and brain . Its actions in the brain also produce euphoria, respiratory depression, and sedation.

    Metabolism

    Hydrocodone undergoes oxidative O-demethylation to form hydromorphone, a more potent active metabolite. Though hydromorphone is active it is not present in sufficient quantities to contribute significantly to hydrocodone's therapeutic effects. Both hydrocodone and hydromorphone form 6-α- and 6-β-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.

    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. The extended release tablet formulations have a Tmax of 14-16 h. The Cmax remains dose proportional over the range of 2.5-10 mg in liquid formulations and 20-120 mg in extended release formulations. Administration with food increases Cmax by about 27% while Tmax and AUC remain the same. 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.

    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. 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. 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.

    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.

    Half-life

    The half-life of elimination reported for hydrocodone is 7-9 h.

    Protein Binding

    Hydrocodone is 36% bound to plasma proteins.

    Elimination

    Most hydrocodone appears to be eliminated via a non-renal route as renal clearance is substantially lower than total apparent clearance. 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.

    Volume of Distribution

    The apparent volume of distribution ranges widely in published literature. The official FDA labeling reports a value of 402 L. 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. Hydrocodone has been observed in human breast milk at levels equivalent to 1.6% of the maternal dosage. Only 12 of the 30 women studied had detectable concentrations of hydromorphone at mean levels of 0.3 mcg/kg/day.

    Clearance

    Official FDA labeling reports an apparent clearance of 83 L/h. Pharmacokinetic studies report values ranging from 24.5-58.8 L/h largely dependent on CYP2D6 metabolizer status.

    Receptor Profile

    Receptor Actions

    Agonists
    μ-opioid receptor agonist (full)
    δ-opioid receptor agonist (lower affinity)

    Receptor Binding

    Mu-type opioid receptor agonist
    Delta-type opioid receptor agonist

    History & Culture

    1920–1943

    Hydrocodone was first synthesized in Germany in 1920 by chemists Carl Mannich and Helene Löwenheim as a semi-synthetic derivative of codeine. The compound was patented in 1923 and first marketed by the pharmaceutical company Knoll under the trade name Dicodid beginning in February 1924. This naming convention followed Knoll's established pattern for their opioid product line, which included Dilaudid (hydromorphone, 1926), Dinarkon (oxycodone, 1917), Dihydrin (dihydrocodeine, 1911), and Dimorphan (dihydromorphine). The United States Food and Drug Administration approved hydrocodone on March 23, 1943, initially for use as the cough suppressant syrup Hycodan. Health Canada subsequently approved the drug under the same brand name for the Canadian market.

    Hydrocodone became predominantly prescribed within the United States, with the International Narcotics Control Board reporting that 99% of the worldwide supply was consumed in the United States as of 2007, a figure that remained consistent through 2010. The drug reached its peak prevalence in 2010 when it became the most prescribed medication in the country, with 131.2 million prescriptions written for hydrocodone-paracetamol combinations that year. The most widely recognized hydrocodone formulation has been Vicodin, produced by Knoll Laboratories. The trade name reportedly derives from the Roman numeral VI, referencing hydrocodone's approximately six-fold potency relative to codeine—where 5 mg of hydrocodone produces effects comparable to 30 mg of codeine.

    2006–2014

    Beginning in late 2006, the FDA initiated recalls of numerous hydrocodone-containing cough formulations following reports of deaths in infants and children under six years of age. By August 2010, enforcement actions had resulted in the removal of 88% of these hydrocodone-containing medications from the market. Concurrently, the FDA began considering restrictions on hydrocodone and oxycodone fixed-combination products due to paracetamol-related liver toxicity concerns. In late 2012, Vicodin's manufacturer reformulated their hydrocodone tablets to reduce the acetaminophen content to 300 mg per tablet, addressing the risk of liver damage associated with higher paracetamol doses. A long-acting formulation was approved for medical use in the United States in 2013, with Zohydro ER becoming the only hydrocodone brand available without acetaminophen, offered in doses up to 50 mg. The US government imposed more restrictive prescribing requirements in 2014, reclassifying all hydrocodone products from Schedule III to Schedule II effective October 6, 2014. This change followed a 2013 FDA advisory panel recommendation responding to DEA concerns about abuse potential. Prior to rescheduling, products containing 15 mg or less of hydrocodone per dosage unit had been classified as Schedule III, encompassing nearly all prescribed hydrocodone formulations including Vicodin. By 2011, hydrocodone products were involved in approximately 100,000 abuse-related emergency department visits in the United States, more than double the number recorded in 2004.

    Effect Profile

    Curated + 307 Reports
    Opioid 8.0

    Strong euphoria, itching/nausea, pain relief, and sedation

    Euphoria / Warmth×3
    107.9
    Analgesia×2
    91.4
    Sedation / Relaxation×1
    84.9
    Itching / Nausea×1
    106.3
    Catalog Erowid

    Tolerance & Pharmacokinetics

    drugs.wiki
    Half-Life
    IR ≈ 4 h; ER ≈ 7–9 h
    Addiction Potential
    High. Hydrocodone carries significant risk for tolerance, dependence, and opioid use disorder, with overdose risk driven primarily by respiratory depression and, for combination products, acetaminophen hepatotoxicity.

    Cross-Tolerances

    Other opioids (e.g., morphine, oxycodone, codeine)
    70% ●○○

    Experience Report Analysis

    Erowid BlueLight
    266 Reports
    1995–2025 Date Range
    58 With Age Data
    29 Effects Detected

    Demographics

    Gender Distribution

    Age Distribution

    Reports Over Time

    Effect Analysis

    Erowid + Bluelight

    Effects aggregated from 307 experience reports (266 Erowid + 41 Bluelight)

    307 Reports
    95 Effects Detected
    43 Positive
    33 Adverse
    19 Neutral

    Effect Sentiment Distribution

    Confidence Distribution

    Positive Effects 43

    Euphoria 47.2% 89%
    Contentment 41.5% 84%
    Sedation 35.2% 86%
    Anxiety Suppression 27.7% 82%
    Stimulation 25.9% 70%
    Sociability Enhancement 24.4% 84%
    Thought Deceleration 22.0% 78%
    Music Enhancement 21.2% 85%
    Empathy 21.2% 80%
    Hot Flashes 19.5% 82%
    Drowsiness 19.5% 90%
    Tingling 17.1% 85%
    Body High 16.0% 88%
    Vivid Dreams 14.6% 82%
    Tactile Enhancement 13.1% 85%
    Focus Enhancement 12.4% 80%
    Color Enhancement 10.5% 70%
    Numbness 9.8% 85%
    Heaviness 9.8% 81%
    Lightness 7.3% 77%

    Adverse Effects 33

    Nausea 29.0% 83%
    Dizziness 22.0% 84%
    Vomiting 19.5% 90%
    Itching 19.5% 84%
    Confusion 12.7% 85%
    Stomach Cramps 12.2% 77%
    Motor Impairment 11.7% 75%
    Headache 11.4% 75%
    Thought Disorganization 9.8% 76%
    Blurred Vision 7.3% 83%
    Irritability 7.3% 73%
    Sweating 5.6% 80%
    Memory Suppression 5.2% 75%
    Amnesia 4.9% 95%
    Muscle Tension 3.4% 70%
    Increased Heart Rate 3.0% 70%
    Seizure 2.6% 70%
    Lightheadedness 2.4% 80%
    Panic 2.4% 80%
    Dysphoria 2.4% 85%

    Dose-Response Correlation

    How effect frequency changes across dose levels

    View data table
    Effect Light (n=25) Common (n=94) Strong (n=21) Heavy (n=20)
    Euphoria 44.0% 42.6% 52.4% 65.0%
    Nausea 20.0% 30.9% 38.1% 50.0%
    Stimulation 16.0% 27.7% 42.9% 35.0%
    Anxiety Suppression 36.0% 24.5% 28.6% 40.0%
    Sedation 24.0% 39.4% 38.1% 25.0%
    Music Enhancement 16.0% 34.0% 28.6% 20.0%
    Focus Enhancement 28.0% 14.9% 0% 25.0%
    Confusion 28.0% 14.9% 0% 15.0%
    Empathy 24.0% 26.6% 19.0% 20.0%
    Body High 16.0% 20.2% 0% 15.0%
    Dissociation 20.0% 10.6% 14.3% 10.0%
    Visual Distortions 12.0% 8.5% 9.5% 20.0%
    Tactile Enhancement 12.0% 16.0% 9.5% 20.0%
    Headache 0% 17.0% 0% 10.0%
    Introspection 16.0% 3.2% 0% 0%

    Subjective Effect Ontology

    Experience Reports

    Structured effect tags extracted from 307 Erowid & Bluelight experience reports using a controlled vocabulary of 220+ canonical effects across 15 domains.

    Emotional

    euphoria 145 47.2%

    Motor

    sedation 108 35.2%

    2 unique effects extracted · Derived from Erowid & Bluelight reports

    Dose–Effect Mapping

    Experience Reports

    How reported effects shift across dose tiers, based on 266 experience reports.

    Oral dose range: 10.0–23.0 mg (median 15.0 mg)
    Effect Light (n=25) Common (n=94) Strong (n=21) Heavy (n=20)
    euphoria
    44%
    43%
    52%
    65%
    nausea
    20%
    31%
    38%
    50%
    stimulation
    16%
    28%
    43%
    35%
    anxiety suppression
    36%
    24%
    29%
    40%
    sedation
    24%
    39%
    38%
    25%
    music enhancement
    16%
    34%
    29%
    20%
    focus enhancement
    28%
    15%
    25%
    confusion
    28%
    15%
    15%
    empathy
    24%
    27%
    19%
    20%
    body high
    16%
    20%
    15%
    dissociation
    20%
    11%
    14%
    10%
    visual distortions
    12%
    8%
    10%
    20%
    tactile enhancement
    12%
    16%
    10%
    20%
    headache
    17%
    10%
    introspection
    16%
    3%
    auditory effects
    8%
    15%
    15%
    motor impairment
    12%
    15%
    color enhancement
    8%
    13%
    10%
    10%
    closed-eye visuals
    12%
    11%
    hospital
    6%
    10%

    Showing top 20 of 33 effects

    Risk Escalation

    Sentiment Analysis

    Average frequency of positive vs adverse effects across dose tiers

    Light n=25
    10 positive 18.8% 5 adverse 20.8%
    Common n=94
    11 positive 18.6% 13 adverse 10.0%
    Strong n=21
    6 positive 27.0% 3 adverse 25.4%
    Heavy n=20
    8 positive 26.2% 5 adverse 25.0%
    View effect breakdown

    Adverse Effects

    Effect Light (n=25) Common (n=94) Strong (n=21) Heavy (n=20) Change
    Nausea
    20%
    31%
    38%
    50%
    +150%
    Anxiety Suppression
    36%
    24%
    29%
    40%
    +11%
    Confusion
    28%
    15%
    15%
    -46%
    Headache
    17%
    10%
    -41%
    Motor Impairment
    12%
    15%
    +24%
    Sweating
    5%
    10%
    10%
    +88%
    Memory Suppression
    8%
    5%
    -33%
    Muscle Tension
    4%
    0%
    Increased Heart Rate
    3%
    0%
    Pupil Dilation
    3%
    0%
    Jaw Clenching
    2%
    0%
    Seizure
    2%
    0%
    Appetite Suppression
    2%
    0%

    Positive Effects

    Effect Light (n=25) Common (n=94) Strong (n=21) Heavy (n=20) Change
    Euphoria
    44%
    43%
    52%
    65%
    +47%
    Stimulation
    16%
    28%
    43%
    35%
    +118%
    Music Enhancement
    16%
    34%
    29%
    20%
    +25%
    Focus Enhancement
    28%
    15%
    25%
    -10%
    Empathy
    24%
    27%
    19%
    20%
    -16%
    Body High
    16%
    20%
    15%
    -6%
    Tactile Enhancement
    12%
    16%
    10%
    20%
    +66%
    Introspection
    16%
    3%
    -80%
    Color Enhancement
    8%
    13%
    10%
    10%
    +25%
    Creativity Enhancement
    8%
    2%
    -73%
    Pain Relief
    4%
    0%

    Dosage Distribution

    Dose distribution from experience reports

    Median: 15.0 mg IQR: 10.0–23.0 mg n=165

    Real-World Dose Distribution

    62K Doses

    From 465 individual dose entries

    Oral (n=358)

    Median: 12.5mg 25th: 7.5mg 75th: 20.0mg 90th: 30.0mg
    mg/kg median: 0.182 mg/kg 75th: 0.315

    Insufflated (n=17)

    Median: 10.0mg 25th: 5.0mg 75th: 15.0mg 90th: 20.0mg
    mg/kg median: 0.127 mg/kg 75th: 0.174

    Common Combinations

    Most co-occurring substances in experience reports

    Form / Preparation

    Most common forms and preparations reported

    Body-Weight Dosing

    Dose relative to body weight from reports with weight data

    Oral

    Median: 0.236 mg/kg IQR: 0.157–0.368 mg/kg n=166

    Insufflated

    Median: 0.147 mg/kg IQR: 0.053–0.301 mg/kg n=6

    Redose Patterns

    Redosing behavior across 231 reports

    24.2% Redosed
    1.3 Avg Doses
    45m Median Interval

    Opioid Equivalence (MME)

    NIH HEAL 2024 & CDC 2022
    ⚠ Citation & Disclaimer: Conversion factors sourced from the NIH HEAL Initiative MME Calculator (Adams et al., PAIN 2025), the CDC 2022 Clinical Practice Guideline for Prescribing Opioids for Pain, and the MDCalc MME Calculator. These are approximate equianalgesic ratios for educational reference only. Individual responses vary significantly based on genetics, tolerance, cross-tolerance, and route of administration. This is not medical advice. Do not use these conversions to adjust opioid dosing without professional medical guidance.
    10 mg Hydrocodone 10 mg Morphine (oral)
    MME factor 1.0×

    Hydrocodone 10 mg oral ≈ 10 mg Morphine oral

    Evidence level: High (A).

    Legal Status

    Country Status Notes
    Australia Schedule 8 (S8) Classified as a controlled drug requiring a prescription. Schedule 8 substances are considered drugs of addiction with recognized therapeutic use.
    Austria Controlled (Suchtmittelgesetz) Regulated under the Austrian Suchtmittelgesetz (SMG) in a similar manner to Germany. Since 2002, hydrocodone products from Germany and elsewhere in the European Union have been available under Article 76 of the Schengen Treaty.
    Belgium Not available Hydrocodone is no longer available for medical use in Belgium.
    Canada Schedule I (CDSA) Controlled under the Controlled Drugs and Substances Act. Available only by prescription, both as a single-ingredient formulation and in proprietary combinations with NSAIDs or paracetamol.
    France Prohibited narcotic Classified as a prohibited narcotic substance. Hydrocodone is no longer available for medical use in France.
    Germany Anlage III BtMG Listed under Anlage III of the Betäubungsmittelgesetz (Narcotics Act) as a Suchtgift. Can only be prescribed using a special narcotic prescription form (Betäubungsmittelrezept).
    Luxembourg Prescription only Available by prescription under the trade name Biocodone. Prescriptions are more commonly issued for use as a cough suppressant (antitussive) rather than for pain relief.
    Mexico Prescription only Requires a valid prescription for legal acquisition. Not available over-the-counter despite contrary rumors.
    Netherlands List I (Opiumwet) Classified as a List I substance under the Opium Law (Opiumwet). Hydrocodone is not available for medical use and possession without a prescription or license is illegal.
    Russia Schedule I Classified as a Schedule I controlled substance under Russian drug control legislation.
    Sweden Not available Hydrocodone is no longer available for medical use in Sweden. The last remaining formulation was deregistered in 1967.
    Switzerland Controlled (Verzeichnis A) Listed as a controlled substance under Verzeichnis A of Swiss narcotics legislation. Medicinal use is permitted with appropriate authorization.
    United Kingdom Class A (Schedule 2) Listed as a Class A drug under the Misuse of Drugs Act 1971 and Schedule 2 under the Misuse of Drugs Regulations. Hydrocodone is not available for medical use in the UK; dihydrocodeine formulations are commonly used as alternatives.
    United States Schedule II As of October 6, 2014, all hydrocodone products are designated Schedule II controlled substances under the Controlled Substances Act. Prior to this date, combination products containing 15 mg or less per dosage unit were classified as Schedule III. Prescriptions cannot be refilled and require a new written prescription for each fill.

    Harm Reduction

    drugs.wiki

    Most hydrocodone IR products are co‑formulated with acetaminophen (APAP); keep total APAP from all sources ≤ 4,000 mg in 24 h (lower in hepatic disease or chronic alcohol use) to reduce risk of severe liver injury. Dose‑dumping and fatal overdose can occur if extended‑release hydrocodone (e.g., Hysingla ER, Zohydro ER) is crushed, chewed, or dissolved—swallow whole only. Respiratory depression risk is highest during initiation, after dose increases, or when combined with other CNS depressants; avoid mixing with alcohol, benzodiazepines, Z‑drugs, barbiturates, or GHB/GBL. Hydrocodone is metabolized by CYP2D6 to hydromorphone (active) and by CYP3A4 to norhydrocodone (inactive); strong CYP3A4 inhibitors (including ritonavir in Paxlovid) can dangerously raise hydrocodone levels, while inducers can reduce analgesia and precipitate withdrawal; CYP2D6 inhibitors can blunt hydromorphone formation and alter response. Combination with serotonergic drugs (e.g., SSRIs/SNRIs/TCAs, some muscle relaxants, tramadol) has produced serotonin‑toxicity cases; monitor or avoid high‑risk combinations. Counterfeit opioid tablets adulterated with potent synthetic opioids (e.g., nitazenes/fentanils) have been reported in Europe; avoid non‑pharmacy pills and consider carrying naloxone; do not use alone. Opioid‑naïve individuals and those with reduced tolerance after a break are at particularly high overdose risk—start low, go slow, and space doses ≥ 4–6 h. Common adverse effects include sedation, miosis, pruritus, nausea, and constipation; maintain bowel regimen (hydration, fiber, stimulant + stool softener as needed). Avoid driving or hazardous tasks while sedated; impairment can persist beyond subjective effects. Seek urgent care for severe drowsiness, slowed or irregular breathing, cyanosis, or unresponsiveness; naloxone is the first‑line reversal for life‑threatening respiratory depression.

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