U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry ABSOLUTE
Molecular Formula C18H21NO3.HI
Molecular Weight 427.2767
Optical Activity UNSPECIFIED
Defined Stereocenters 4 / 4
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of HYDROCODONE HYDROIODIDE

SMILES

I.COC1=C2O[C@H]3C(=O)CC[C@H]4[C@H]5CC(C=C1)=C2[C@@]34CCN5C

InChI

InChIKey=HLMZUCYYQGNVGA-RNWHKREASA-N
InChI=1S/C18H21NO3.HI/c1-19-8-7-18-11-4-5-13(20)17(18)22-16-14(21-2)6-3-10(15(16)18)9-12(11)19;/h3,6,11-12,17H,4-5,7-9H2,1-2H3;1H/t11-,12+,17-,18-;/m0./s1

HIDE SMILES / InChI
Molecular Formula HI
Molecular Weight 127.91241
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula C18H21NO3
Molecular Weight 299.3642
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 4 / 4
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

Benzhydrocodone is a prodrug of hydrocodone. Benzhydrocodone is formed by covalently bonding hydrocodone to benzoic acid. Benzhydrocodone itself is not pharmacologically active, but must be metabolized to hydrocodone by enzymes in the intestinal tract to optimally deliver its pharmacologic effects. Hydrocodone is a full agonist of the opioid receptors with a higher affinity for the mu-opioid receptor. Upon binding, hydrocodone produces an analgesic effect with no ceiling. APADAZ a combination of benzhydrocodone and acetaminophen is FDA approved and indicated for the short-term (no more than 14 days) management of acute pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate. APADAZ, even when taken as recommended, can result in addiction, abuse, and misuse, which can lead to overdose and death.

CNS Activity

Approval Year

1943
64
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
ZOHYDRO ER

Approved Use

ZOHYDRO ER is an opioid agonist indicated for the management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate.

Launch Date

2013
Primary
Approved
8583
APADAZ

Approved Use

APADAZ is a combination of benzhydrocodone, a prodrug of the opioid agonist hydrocodone, and acetaminophen, and is indicated for the short-term (no more than 14 days) management of acute pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate.

Launch Date

2019
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
13 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/27138027/
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROCODONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
10.1 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/27138027/
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROCODONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
23.6 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/005213s039lbl.pdf
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
16.04 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/208653s007lbl.pdf#page=30
6.12 mg single, oral
dose: 6.12 mg
route of administration: Oral
experiment type: SINGLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
19.18 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/208653s007lbl.pdf#page=30
6.12 mg single, oral
dose: 6.12 mg
route of administration: Oral
experiment type: SINGLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
33.95 ng/mL
OTHER GOV'T
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208653Orig1s000ClinPharmR.pdf#page=25
12.24 mg 6 times / day multiple, oral
dose: 12.24 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
62.79 ng/mL
OTHER GOV'T
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208653Orig1s000ClinPharmR.pdf#page=25
12.24 mg 6 times / day multiple, oral
dose: 12.24 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
208 ng/mL
OTHER GOV'T
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208653Orig1s000ClinPharmR.pdf#page=27
73.44 mg single, oral
dose: 73.44 mg
route of administration: Oral
experiment type: SINGLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
9.4 ng/mL
OTHER GOV'T
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208653Orig1s000ClinPharmR.pdf#page=29
6.12 mg single, nasal
dose: 6.12 mg
route of administration: Nasal
experiment type: SINGLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
27 ng/mL
OTHER GOV'T
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208653Orig1s000ClinPharmR.pdf#page=29
24.48 mg single, nasal
dose: 24.48 mg
route of administration: Nasal
experiment type: SINGLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
25.6 ng/mL
OTHER GOV'T
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208653Orig1s000ClinPharmR.pdf#page=31 | https://pubmed.ncbi.nlm.nih.gov/29092079/
12.24 mg single, nasal
dose: 12.24 mg
route of administration: Nasal
experiment type: SINGLE
co-administered:
HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
40.4 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29025138/
12.24 mg single, oral
dose: 12.24 mg
route of administration: Oral
experiment type: SINGLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
34.7 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29025138/
12.24 mg single, nasal
dose: 12.24 mg
route of administration: Nasal
experiment type: SINGLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
269 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/27138027/
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROCODONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
155 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/27138027/
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROCODONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
130.91 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/208653s007lbl.pdf#page=30
6.12 mg single, oral
dose: 6.12 mg
route of administration: Oral
experiment type: SINGLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
125.73 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/208653s007lbl.pdf#page=30
6.12 mg single, oral
dose: 6.12 mg
route of administration: Oral
experiment type: SINGLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
92.94 ng × h/mL
OTHER GOV'T
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208653Orig1s000ClinPharmR.pdf#page=25
12.24 mg 6 times / day multiple, oral
dose: 12.24 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
195.07 ng × h/mL
OTHER GOV'T
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208653Orig1s000ClinPharmR.pdf#page=25
12.24 mg 6 times / day multiple, oral
dose: 12.24 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1272 ng × h/mL
OTHER GOV'T
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208653Orig1s000ClinPharmR.pdf#page=27
73.44 mg single, oral
dose: 73.44 mg
route of administration: Oral
experiment type: SINGLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
194.7 ng × h/mL
OTHER GOV'T
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208653Orig1s000ClinPharmR.pdf#page=31 | https://pubmed.ncbi.nlm.nih.gov/29092079/
12.24 mg single, nasal
dose: 12.24 mg
route of administration: Nasal
experiment type: SINGLE
co-administered:
HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
252.7 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29025138/
12.24 mg single, oral
dose: 12.24 mg
route of administration: Oral
experiment type: SINGLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
278.3 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29025138/
12.24 mg single, nasal
dose: 12.24 mg
route of administration: Nasal
experiment type: SINGLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
10.5 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/27138027/
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROCODONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
10.2 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/27138027/
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROCODONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
4 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/005213s039lbl.pdf
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
4.51 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/208653s007lbl.pdf#page=30
6.12 mg single, oral
dose: 6.12 mg
route of administration: Oral
experiment type: SINGLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
4.33 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/208653s007lbl.pdf#page=30
6.12 mg single, oral
dose: 6.12 mg
route of administration: Oral
experiment type: SINGLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
4.45 h
OTHER GOV'T
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208653Orig1s000ClinPharmR.pdf#page=25
12.24 mg 6 times / day multiple, oral
dose: 12.24 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
4.87 h
OTHER GOV'T
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208653Orig1s000ClinPharmR.pdf#page=25
12.24 mg 6 times / day multiple, oral
dose: 12.24 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
5 h
OTHER GOV'T
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208653Orig1s000ClinPharmR.pdf#page=27
73.44 mg single, oral
dose: 73.44 mg
route of administration: Oral
experiment type: SINGLE
co-administered: ACETAMINOPHEN
ACETAMINOPHEN
 HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
5.29 h
OTHER GOV'T
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208653Orig1s000ClinPharmR.pdf#page=31 | https://pubmed.ncbi.nlm.nih.gov/29092079/
12.24 mg single, nasal
dose: 12.24 mg
route of administration: Nasal
experiment type: SINGLE
co-administered:
HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
55%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/005213s039lbl.pdf
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
HYDROCODONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
30 mg multiple, oral
Overdose
Dose: 30 mg
Route: oral
Route: multiple
Dose: 30 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/20837591
unhealthy, 5 years
Health Status: unhealthy
Age Group: 5 years
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/20837591
Other AEs: Adverse event...
Other AEs:
Adverse event (grade 5)
Sources:
https://pubmed.ncbi.nlm.nih.gov/20837591
160 mg 1 times / day multiple, oral
Highest studied dose
Dose: 160 mg, 1 times / day
Route: oral
Route: multiple
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
Other AEs: Electrocardiogram QTc interval prolonged...
Other AEs:
Electrocardiogram QTc interval prolonged
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
pregnant, adult
Health Status: pregnant
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
Other AEs: Withdrawal syndrome neonatal...
Other AEs:
Withdrawal syndrome neonatal
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
Other AEs: Respiratory depression, Addiction...
Other AEs:
Respiratory depression (grade 5)
Addiction
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
20 mg 1 times / day multiple, oral
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
Disc. AE: Vomiting, Nausea...
AEs leading to
discontinuation/dose reduction:
Vomiting (1%)
Nausea (1%)
Headache (1%)
Dizziness (1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
13.34 mg 1 times / day steady-state, intranasal
Studied dose
Dose: 13.34 mg, 1 times / day
Route: intranasal
Route: steady-state
Dose: 13.34 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29025138/
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/29025138/
Other AEs: Nasal discomfort, Nasal congestion...
Other AEs:
Nasal discomfort (16 patients)
Nasal congestion (7 patients)
Rhinorrhea (7 patients)
Throat irritation (6 patients)
Oropharyngeal pain (1 pt)
Dry throat (1 pt)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29025138/
AEs

AEs

AESignificanceDosePopulation
Adverse event grade 5
30 mg multiple, oral
Overdose
Dose: 30 mg
Route: oral
Route: multiple
Dose: 30 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/20837591
unhealthy, 5 years
Health Status: unhealthy
Age Group: 5 years
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/20837591
Electrocardiogram QTc interval prolonged
160 mg 1 times / day multiple, oral
Highest studied dose
Dose: 160 mg, 1 times / day
Route: oral
Route: multiple
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
Withdrawal syndrome neonatal
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
pregnant, adult
Health Status: pregnant
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
Addiction
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
Respiratory depression grade 5
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206627s000lbl.pdf
Dizziness 1%
Disc. AE
20 mg 1 times / day multiple, oral
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
Headache 1%
Disc. AE
20 mg 1 times / day multiple, oral
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
Nausea 1%
Disc. AE
20 mg 1 times / day multiple, oral
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
Vomiting 1%
Disc. AE
20 mg 1 times / day multiple, oral
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206627Orig1s000MedR.pdf
Dry throat 1 pt
13.34 mg 1 times / day steady-state, intranasal
Studied dose
Dose: 13.34 mg, 1 times / day
Route: intranasal
Route: steady-state
Dose: 13.34 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29025138/
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/29025138/
Oropharyngeal pain 1 pt
13.34 mg 1 times / day steady-state, intranasal
Studied dose
Dose: 13.34 mg, 1 times / day
Route: intranasal
Route: steady-state
Dose: 13.34 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29025138/
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/29025138/
Nasal discomfort 16 patients
13.34 mg 1 times / day steady-state, intranasal
Studied dose
Dose: 13.34 mg, 1 times / day
Route: intranasal
Route: steady-state
Dose: 13.34 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29025138/
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/29025138/
Throat irritation 6 patients
13.34 mg 1 times / day steady-state, intranasal
Studied dose
Dose: 13.34 mg, 1 times / day
Route: intranasal
Route: steady-state
Dose: 13.34 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29025138/
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/29025138/
Nasal congestion 7 patients
13.34 mg 1 times / day steady-state, intranasal
Studied dose
Dose: 13.34 mg, 1 times / day
Route: intranasal
Route: steady-state
Dose: 13.34 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29025138/
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/29025138/
Rhinorrhea 7 patients
13.34 mg 1 times / day steady-state, intranasal
Studied dose
Dose: 13.34 mg, 1 times / day
Route: intranasal
Route: steady-state
Dose: 13.34 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29025138/
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/29025138/
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946
substrate
1388
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2B6
776

CYP2C19
1119
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP2B6
776
 minor
CYP2C19
1119
 minor
CYP2D6
1388
 yes
yes (co-administration study)
Comment: The 90% confidence interval (CI) of the geometric means for hydrocodone AUCinf (98 to 115%), AUCt (98 to 115%), and Cmax (93 to 121%) values were within the range of 80 to 125% when a single dose of HYSINGLA ER 20 mg was co-administered with CYP2D6 inhibitor paroxetine
CYP3A4
1946
 yes
yes (co-administration study)
Comment: Co-administration of HYSINGLA ER and CYP3A4 inhibitor ketoconazole increased mean hydrocodone AUC and Cmax by 135% and 78%, respectively;
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
2263
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:5779
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:5779
eMolecules
29539213
https://www.emolecules.com/cgi-bin/more?vid=29539213
ZINC
ZINC000001280665
http://zinc15.docking.org/substances/ZINC000001280665
PubMed

PubMed

TitleDatePubMed
Efficacy and tolerability of celecoxib versus hydrocodone/acetaminophen in the treatment of pain after ambulatory orthopedic surgery in adults.
2001 Feb
[Does the inhalation of a 1% L-menthol solution in the premedication of fiberoptic bronchoscopy affect coughing and the sensation of dyspnea?].
2001 Mar
Complications of intranasal prescription narcotic abuse.
2002 Feb
Esophageal cancer and the esophagus: challenges and potential strategies for selective cytoprotection of the tumor-bearing organ during cancer treatment.
2002 Jan
Combination hydrocodone and ibuprofen versus combination oxycodone and acetaminophen in the treatment of moderate or severe acute low back pain.
2002 Jan
A phase II study of hydrocodone for cough in advanced cancer.
2002 Jan-Feb
Effect of narcotic pain reliever on pulp tests in women.
2002 Jul
Gateways to clinical trials.
2002 Jul-Aug
Photodynamic therapy for Barrett's esophagus and high grade dysplasia: results of a patient satisfaction survey.
2002 Jul-Aug
A double-blind, single-dose comparison of the analgesic efficacy of tramadol/acetaminophen combination tablets, hydrocodone/acetaminophen combination tablets, and placebo after oral surgery.
2002 Jun
Simultaneous quantitation of opioids in blood by GC-EI-MS analysis following deproteination, detautomerization of keto analytes, solid-phase extraction, and trimethylsilyl derivatization.
2002 Oct
A field evaluation of five on-site drug-testing devices.
2002 Oct
Withdrawal hyperalgesia after acute opioid physical dependence in nonaddicted humans: a preliminary study.
2003 Nov
1000 office-based hysteroscopies prior to in vitro fertilization: feasibility and findings.
2004 Apr-Jun
A message of hope.
2004 Fall
Refractory status epilepticus.
2004 Feb
Effective treatment of laparoscopic cholecystectomy pain with intravenous followed by oral COX-2 specific inhibitor.
2004 Feb
Postoperative pain management after anterior cruciate ligament reconstruction.
2004 Jan
Loss prevention case of the month. Monitoring remains critical.
2004 Jan
Patient characteristics and risks factors for development of dependence on hydrocodone and oxycodone.
2004 Jan-Feb
Hallucinations with zolpidem and fluoxetine in an impaired driver.
2004 Mar
CYP2D6 and CYP3A4 involvement in the primary oxidative metabolism of hydrocodone by human liver microsomes.
2004 Mar
Topical metronidazole (10 percent) decreases posthemorrhoidectomy pain and improves healing.
2004 May
[Origin and growth of the National Program of Continuous Academic Development for the General Physician].
2004 May-Jun
Local anesthetic infusion pumps improve postoperative pain after inguinal hernia repair: a randomized trial.
2004 Nov
Continuous local anesthetic infusion for pain management after outpatient inguinal herniorrhaphy.
2004 Oct
Presurgical intravenous parecoxib sodium and follow-up oral valdecoxib for pain management after laparoscopic cholecystectomy surgery reduces opioid requirements and opioid-related adverse effects.
2004 Oct
Metaxalone (Skelaxin)-related death.
2004 Sep
A 35-year-old physician with opioid dependence.
2004 Sep 15
Selective potentiation of opioid analgesia by nonsteroidal anti-inflammatory drugs.
2005 Apr 8
Detection of hypoventilation during thoracoscopy: combined cutaneous carbon dioxide tension and oximetry monitoring with a new digital sensor.
2005 Feb
A preclinical comparison between different opioids: antinociceptive versus adverse effects.
2005 Feb
The GC-MS detection and characterization of neopine resulting from opium use and codeine metabolism and its potential as an opiate-product-use marker.
2005 Jun
A 46-year-old man with excruciating shoulder pain.
2005 Mar
Oral analgesics for acute nonspecific pain.
2005 Mar 1
Patents

Patents

04272541
12
07321038
10
08491935
43
08569329
43
JP2000501709A
76
JP2005506351A
26
JP2010163446A
20
JP2010509227A
65
JP2011511782A
10
JP2011520977A
50
JP2013241461A
10
JP4806507B2
10

Sample Use Guides

In Vivo Use Guide
APADAZ Immediate-release tablets: 6.12 mg benzhydrocodone (equivalent to 6.67 mg benzhydrocodone hydrochloride) and 325 mg acetaminophen. Initiate treatment with APADAZ at 1 or 2 tablets every 4 to 6 hours as needed for pain. Dosage should not exceed 12 tablets in a 24­ hour period.
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Mon Mar 31 22:45:12 GMT 2025
Edited
by admin
on Mon Mar 31 22:45:12 GMT 2025
Record UNII
6D04Y0152T
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
HYDROCODONE HYDROIODIDE
Common Name English
CODEINONE, DIHYDRO-, HYDRIODIDE
Preferred Name English
DIHYDROCODEINONE HYDROIODIDE
Common Name English
MORPHINAN-6-ONE, 4,5-EPOXY-3-METHOXY-17-METHYL-, HYDRIODIDE, (5.ALPHA.)-
Systematic Name English
DIHYDROCODEINONE HYDROIODIDE, (-)-
Common Name English
HYDROCODONE HYDRIODIDE
Common Name English
Code System Code Type Description
FDA UNII
6D04Y0152T
Created by admin on Mon Mar 31 22:45:12 GMT 2025 , Edited by admin on Mon Mar 31 22:45:12 GMT 2025
PRIMARY
PUBCHEM
92135673
Created by admin on Mon Mar 31 22:45:12 GMT 2025 , Edited by admin on Mon Mar 31 22:45:12 GMT 2025
PRIMARY
DRUG BANK
DBSALT000051
Created by admin on Mon Mar 31 22:45:12 GMT 2025 , Edited by admin on Mon Mar 31 22:45:12 GMT 2025
PRIMARY
CAS
5965-15-1
Created by admin on Mon Mar 31 22:45:12 GMT 2025 , Edited by admin on Mon Mar 31 22:45:12 GMT 2025
PRIMARY
Related Record Type Details
Structure of HYDROCODONE
PARENT -> SALT/SOLVATE
Related Record Type Details
Structure of HYDROCODONE
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