U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula 2C17H17NO2.2ClH.H2O
Molecular Weight 625.582
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of APOMORPHINE HYDROCHLORIDE

SMILES

O.Cl.Cl.[H][C@@]12CC3=C(C(O)=C(O)C=C3)C4=C1C(CCN2C)=CC=C4.[H][C@@]56CC7=C(C(O)=C(O)C=C7)C8=C5C(CCN6C)=CC=C8

InChI

InChIKey=CXWQXGNFZLHLHQ-DPFCLETOSA-N
InChI=1S/2C17H17NO2.2ClH.H2O/c2*1-18-8-7-10-3-2-4-12-15(10)13(18)9-11-5-6-14(19)17(20)16(11)12;;;/h2*2-6,13,19-20H,7-9H2,1H3;2*1H;1H2/t2*13-;;;/m11.../s1

HIDE SMILES / InChI
Molecular Formula C17H17NO2
Molecular Weight 267.3224
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED
Molecular Formula H2O
Molecular Weight 18.0153
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Apomorphine (brand names: Apokyn, Ixense, Spontane, Uprima) is indicated for the acute, intermittent treatment of hypomobility, “off” episodes (“end-of-dose wearing off” and unpredictable “on/off” episodes) in patients with advanced Parkinson’s disease. Apomorphine has been studied as an adjunct to other medications. It is a non-ergoline dopamine agonist with high in vitro binding affinity for the dopamine D4 receptor, and moderate affinity for the dopamine D2, D3, and D5, and adrenergic α1D, α2B, α2C receptors. The precise mechanism of action as a treatment for Parkinson’s disease is unknown, although it is believed to be due to stimulation of post-synaptic dopamine D2-type receptors within the caudate-putamen in the brain.

CNS Activity

CNS Active
3913
Curator's Comment: Apomorphine quickly passes the nasal and intestinal mucosa as well as the blood-brain barrier (depending on the administration route)

Approval Year

1880
8
Targets

Targets

Primary TargetPharmacologyConditionPotency
Agonist
2678
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Approved
8429
APOKYN

Approved Use

APOKYN (apomorphine hydrochloride injection) is indicated for the acute, intermittent treatment of hypomobility, off episodes (end-of-dose wearing off and unpredictable on/off episodes) in patients with advanced Parkinson's disease. APOKYN has been studied as an adjunct to other medications [see Clinical Studies (14)

Launch Date

2004
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
47.5 pmol/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/2774511/
30 μg/kg bw single, subcutaneous
dose: 30 μg/kg bw
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
APOMORPHINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
41.7 pmol × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/2774511/
30 μg/kg bw single, subcutaneous
dose: 30 μg/kg bw
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
APOMORPHINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
33.6 min
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/2774511/
30 μg/kg bw single, subcutaneous
dose: 30 μg/kg bw
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
APOMORPHINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
4 mg single, respiratory
Highest studied dose
Dose: 4 mg
Route: respiratory
Route: single
Dose: 4 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
unhealthy, 30 - 90 years
n = 5
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 30 - 90 years
Sex: unknown
Population Size: 5
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
1.5 mg single, respiratory
Recommended
Dose: 1.5 mg
Route: respiratory
Route: single
Dose: 1.5 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
unhealthy, 30 - 90 years
n = 32
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 30 - 90 years
Sex: unknown
Population Size: 32
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
Other AEs: Somnolence, Dysgeusia...
Other AEs:
Somnolence (1 patient)
Dysgeusia (1 patient)
Dizziness (1 patient)
Orthostatic hypotension (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
2.3 mg single, respiratory
Recommended
Dose: 2.3 mg
Route: respiratory
Route: single
Dose: 2.3 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
unhealthy, 30 - 90 years
n = 18
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 30 - 90 years
Sex: unknown
Population Size: 18
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
3 mg single, respiratory
Recommended
Dose: 3 mg
Route: respiratory
Route: single
Dose: 3 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
unhealthy, 30 - 90 years
n = 12
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 30 - 90 years
Sex: unknown
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
Other AEs: Somnolence, Yawning...
Other AEs:
Somnolence (1 patient)
Yawning (1 patient)
Flushing (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
unhealthy, 44 - 87 years
n = 114
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 44 - 87 years
Sex: M+F
Population Size: 114
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
Disc. AE: Cognitive impairment, Skin reaction...
AEs leading to
discontinuation/dose reduction:
Cognitive impairment (16 patients)
Skin reaction (14 patients)
Posture abnormal (12 patients)
Psychosis (11 patient)
Anxiety/depression (11 patient)
Hypotension (3 patients)
Gastrointestinal disorder (NOS) (1 patient)
Cardiovascular disorder (1 patient)
Weight loss (1 patient)
Excessive daytime sleepiness (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
4 mg 1 times / day multiple, subcutaneous (mean)
Highest studied dose
Dose: 4 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 4 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/18978491/
unhealthy, 65.21 years
n = 546
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 65.21 years
Sex: M+F
Population Size: 546
Sources:
https://pubmed.ncbi.nlm.nih.gov/18978491/
Disc. AE: Nausea and vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea and vomiting (187 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/18978491/
10 mg 1 times / day steady, subcutaneous (max)
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Co-administed with::
trimethobenzamide
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Page: 4
unhealthy, adult
n = 522
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adult
Sex: unknown
Population Size: 522
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Page: 4
Disc. AE: Nausea, Vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea (3%)
Vomiting (2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Page: 4
10 mg 1 times / day steady, subcutaneous (max)
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Page: 5
unhealthy, adult
n = 522
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adult
Sex: unknown
Population Size: 522
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Page: 5
Disc. AE: Hallucination...
AEs leading to
discontinuation/dose reduction:
Hallucination (1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Page: 5
35 mg 1 times / day steady, sublingual (max)
Recommended
Dose: 35 mg, 1 times / day
Route: sublingual
Route: steady
Dose: 35 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31818699/
unhealthy, mean 62.9 years
n = 54
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: mean 62.9 years
Sex: M+F
Population Size: 54
Sources:
https://pubmed.ncbi.nlm.nih.gov/31818699/
Disc. AE: Respiratory tract signs and symptoms...
AEs leading to
discontinuation/dose reduction:
Respiratory tract signs and symptoms (9 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/31818699/
AEs

AEs

AESignificanceDosePopulation
Dizziness 1 patient
1.5 mg single, respiratory
Recommended
Dose: 1.5 mg
Route: respiratory
Route: single
Dose: 1.5 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
unhealthy, 30 - 90 years
n = 32
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 30 - 90 years
Sex: unknown
Population Size: 32
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
Dysgeusia 1 patient
1.5 mg single, respiratory
Recommended
Dose: 1.5 mg
Route: respiratory
Route: single
Dose: 1.5 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
unhealthy, 30 - 90 years
n = 32
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 30 - 90 years
Sex: unknown
Population Size: 32
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
Orthostatic hypotension 1 patient
1.5 mg single, respiratory
Recommended
Dose: 1.5 mg
Route: respiratory
Route: single
Dose: 1.5 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
unhealthy, 30 - 90 years
n = 32
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 30 - 90 years
Sex: unknown
Population Size: 32
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
Somnolence 1 patient
1.5 mg single, respiratory
Recommended
Dose: 1.5 mg
Route: respiratory
Route: single
Dose: 1.5 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
unhealthy, 30 - 90 years
n = 32
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 30 - 90 years
Sex: unknown
Population Size: 32
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
Flushing 1 patient
3 mg single, respiratory
Recommended
Dose: 3 mg
Route: respiratory
Route: single
Dose: 3 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
unhealthy, 30 - 90 years
n = 12
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 30 - 90 years
Sex: unknown
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
Somnolence 1 patient
3 mg single, respiratory
Recommended
Dose: 3 mg
Route: respiratory
Route: single
Dose: 3 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
unhealthy, 30 - 90 years
n = 12
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 30 - 90 years
Sex: unknown
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
Yawning 1 patient
3 mg single, respiratory
Recommended
Dose: 3 mg
Route: respiratory
Route: single
Dose: 3 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
unhealthy, 30 - 90 years
n = 12
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 30 - 90 years
Sex: unknown
Population Size: 12
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Page: Table 2
Cardiovascular disorder 1 patient
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
unhealthy, 44 - 87 years
n = 114
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 44 - 87 years
Sex: M+F
Population Size: 114
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
Excessive daytime sleepiness 1 patient
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
unhealthy, 44 - 87 years
n = 114
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 44 - 87 years
Sex: M+F
Population Size: 114
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
Gastrointestinal disorder (NOS) 1 patient
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
unhealthy, 44 - 87 years
n = 114
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 44 - 87 years
Sex: M+F
Population Size: 114
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
Weight loss 1 patient
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
unhealthy, 44 - 87 years
n = 114
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 44 - 87 years
Sex: M+F
Population Size: 114
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
Anxiety/depression 11 patient
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
unhealthy, 44 - 87 years
n = 114
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 44 - 87 years
Sex: M+F
Population Size: 114
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
Psychosis 11 patient
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
unhealthy, 44 - 87 years
n = 114
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 44 - 87 years
Sex: M+F
Population Size: 114
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
Posture abnormal 12 patients
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
unhealthy, 44 - 87 years
n = 114
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 44 - 87 years
Sex: M+F
Population Size: 114
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
Skin reaction 14 patients
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
unhealthy, 44 - 87 years
n = 114
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 44 - 87 years
Sex: M+F
Population Size: 114
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
Cognitive impairment 16 patients
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
unhealthy, 44 - 87 years
n = 114
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 44 - 87 years
Sex: M+F
Population Size: 114
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
Hypotension 3 patients
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
unhealthy, 44 - 87 years
n = 114
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 44 - 87 years
Sex: M+F
Population Size: 114
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Page: Fig. 1
Nausea and vomiting 187 patients
Disc. AE
4 mg 1 times / day multiple, subcutaneous (mean)
Highest studied dose
Dose: 4 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 4 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/18978491/
unhealthy, 65.21 years
n = 546
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 65.21 years
Sex: M+F
Population Size: 546
Sources:
https://pubmed.ncbi.nlm.nih.gov/18978491/
Vomiting 2%
Disc. AE
10 mg 1 times / day steady, subcutaneous (max)
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Co-administed with::
trimethobenzamide
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Page: 4
unhealthy, adult
n = 522
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adult
Sex: unknown
Population Size: 522
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Page: 4
Nausea 3%
Disc. AE
10 mg 1 times / day steady, subcutaneous (max)
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Co-administed with::
trimethobenzamide
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Page: 4
unhealthy, adult
n = 522
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adult
Sex: unknown
Population Size: 522
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Page: 4
Hallucination 1%
Disc. AE
10 mg 1 times / day steady, subcutaneous (max)
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Page: 5
unhealthy, adult
n = 522
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: adult
Sex: unknown
Population Size: 522
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Page: 5
Respiratory tract signs and symptoms 9 patients
Disc. AE
35 mg 1 times / day steady, sublingual (max)
Recommended
Dose: 35 mg, 1 times / day
Route: sublingual
Route: steady
Dose: 35 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31818699/
unhealthy, mean 62.9 years
n = 54
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: mean 62.9 years
Sex: M+F
Population Size: 54
Sources:
https://pubmed.ncbi.nlm.nih.gov/31818699/
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inducer
781
inhibitor
1767
inhibitor
1852

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2B6
810

CYP2C8
911

CYP2C19
1478

CYP3A4/5
278

BCRP
699

BSEP
402

P-gp
1461

MRP2
383

MRP3
157

MRP4
204

MATE1
306

MATE2
263

OATP1B1
788

OATP1B3
706

OAT1
599

OAT3
642

OCT1
512

OCT2
647
UGT
192

sulfotransferases
38

CYP2B6
664

CYP2C8
693

CYP3A4/5
85
CYP1A2
701

CYP2B6
547

OCT1
35

P-gp
257

MRP2
111

MRP3
53

OATP1B1
26

BCRP
75
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
BCRP
773
 no
BSEP
403
 no
apomorphine glucuronide
3
CYP1A2
1692
 no
apomorphine glucuronide
3
CYP1A2
1692
 no
apomorphine glucuronide
3
CYP2B6
1001
 no
CYP2B6
1001
 no
apomorphine glucuronide
3
CYP2B6
1001
 no
apomorphine glucuronide
3
CYP2C19
1553
 no
apomorphine glucuronide
3
CYP2C8
965
 no
apomorphine glucuronide
3
CYP2C9
1819
 no
apomorphine glucuronide
3
CYP2D6
1891
 no
apomorphine glucuronide
3
CYP3A4
1925
 no
CYP3A4
1925
 no
apomorphine glucuronide
3
CYP3A4/5
335
 no
apomorphine glucuronide
3
MATE2
263
 no
apomorphine glucuronide
3
MRP2
475
 no
MRP2
475
 no
apomorphine glucuronide
3
MRP3
207
 no
MRP4
238
 no
apomorphine glucuronide
3
OATP1B1
803
 no
OATP1B1
803
 no
apomorphine glucuronide
3
OATP1B3
715
 no
apomorphine glucuronide
3
OCT1
543
 no
OCT1
543
 no
apomorphine glucuronide
3
OCT2
648
 no
apomorphine glucuronide
3
P-gp
1650
 no
P-gp
1650
 no
apomorphine glucuronide
3
BCRP
773
 weak [Inhibition 50 uM]
apomorphine glucuronide
3
MATE1
308
 weak [Inhibition 50 uM]
apomorphine glucuronide
3
OAT1
603
 weak [Inhibition 50 uM]
apomorphine glucuronide
3
OAT3
644
 weak [Inhibition 50 uM]
apomorphine glucuronide
3
MRP3
207
 yes [IC50 50 uM]
apomorphine glucuronide
3
CYP1A2
1692
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP2B6
664
 yes
CYP2C8
693
 yes
CYP3A4/5
85
 yes
UGT
192
 yes
sulfotransferases
38
 yes
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:48538
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:48538
ZINC
ZINC000000009073
http://zinc15.docking.org/substances/ZINC000000009073
eMolecules
901400
https://www.emolecules.com/cgi-bin/more?vid=901400
PubMed

PubMed

TitleDatePubMed
Catalepsy induced by morphine or haloperidol: effects of apomorphine and anticholinergic drugs.
1976 Aug
Cardiovascular responses to intrathecal dopamine receptor agonists in conscious DOCA-salt hypertensive rats.
1999
Modification of naloxone-induced withdrawal signs by dextromethorphan in morphine-dependent mice.
1999 Jul 14
Effects of continuous exposure to light on behavioral dopaminergic supersensitivity.
1999 Jun 15
Worsening of levodopa-induced dyskinesias by motor and mental tasks.
1999 Mar
Catecholamines participate in the induction of ornithine decarboxylase gene expression in normal and hyperplastic mouse kidney.
1999 May 31
Inhibition of amphetamine- and apomorphine-induced behavioural effects by neuropeptide Y Y(1) receptor antagonist BIBO 3304.
2000 Apr 27
Effect of dopamine agonists and antagonists on the lorazepam withdrawal syndrome in rats.
2000 Mar
Test conditions influence the response to a drug challenge in rodents.
2000 Mar
Activation of gamma-aminobutyric acid(A) receptors in the paraventricular nucleus of the hypothalamus reduces apomorphine-, N-methyl-D-aspartic acid- and oxytocin-induced penile erection and yawning in male rats.
2000 Mar 10
Involvement of GABAergic neurotransmission in the neurobiology of the apomorphine-induced aggressive behavior paradigm, a model of psychotic behavior in rats.
2000 Oct
The serotonin 5-HT(2A) receptor subtype does not mediate apomorphine-induced aggressive behaviour in male Wistar rats.
2000 Oct
Apomorphine: an update of clinical trial results.
2000 Oct
The pharmacokinetic and clinical effects of tolcapone on a single dose of sublingual apomorphine in Parkinson's disease.
2000 Oct 1
The Posturo-Locomotion-Manual Test. A simple method for the characterization of neurological movement disturbances.
2001
Dopaminergic mRNA expression in the intact substantia nigra of unilaterally 6-OHDA-lesioned and grafted rats: an in situ hybridization study.
2001
Effects of systemic injections of dopaminergic agents on the habituation of rats submitted to an open field test.
2001
Inhibition of baclofen on morphine-induced hyperactivity, reverse tolerance and postsynaptic dopamine receptor supersensitivity.
2001 Apr
The effects of apomorphine and haloperidol on memory consolidation in the day-old chick.
2001 Apr
Attenuation of paraquat-induced dopaminergic toxicity on the substantia nigra by (-)-deprenyl in vivo.
2001 Apr 1
Comparison of the effects of infant handling, isolation, and nonhandling on acoustic startle, prepulse inhibition, locomotion, and HPA activity in the adult rat.
2001 Feb
Apomorphine in the treatment of Parkinson's disease.
2001 Feb
Dopamine increases glial cell line-derived neurotrophic factor in human fetal astrocytes.
2001 Feb
Intravenous apomorphine therapy in Parkinson's disease: clinical and pharmacokinetic observations.
2001 Feb
Melatonin protects against 6-OHDA-induced neurotoxicity in rats: a role for mitochondrial complex I activity.
2001 Jan
Neurotoxic regimen of methamphetamine produces evidence of behavioral sensitization in the rat.
2001 Jan
Regulation by the medial amygdala of copulation and medial preoptic dopamine release.
2001 Jan 1
The localization of dopamine D2 receptor mRNA in the human placenta and the anti-angiogenic effect of apomorphine in the chorioallantoic membrane.
2001 Jan 19
Clinical and electrophysiological effects of apomorphine in Parkinson's disease patients are not paralleled by amino acid release changes: a microdialysis study.
2001 Jan-Mar
Neural modulation of visuomotor functions underlying prey-catching behaviour in anurans: perception, attention, motor performance, learning.
2001 Mar
Apomorphine-induced aggressive behaviour in para-chlorophenylalanine-treated male rats: implications to brain.
2001 Mar
Potent, hydroxyl radical-scavenging effect of apomorphine with iron and dopamine perfusion in rat striatum.
2001 Mar 30
Additive effect of clonidine and fluoxetine on apomorphine-induced aggressive behavior in adult male Wistar rats.
2001 May-Jun
Patents

Patents

05939094
3
JP2009526755A
447
JP2011526596A
7
JP4800219B2
65
JPH083043A
3

Sample Use Guides

In Vivo Use Guide
The recommended starting dose of is 0.2 mL (2 mg). Titrate on the basis of effectiveness and tolerance, up to a maximum recommended dose of 0.6 mL (6 mg)
Route of Administration: Other
In Vitro Use Guide
Apomorphine at concentrations of higher than 2 x 10(-5) M dramatically reduced the growth-stimulatory effect of retinal pigment epithelium (RPE) cells on the scleral chondrocytes, whereas the inhibitory effect of apomorphine on the proliferation of scleral chondrocytes without RPE cells was very little
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:36:03 GMT 2023
Edited
by admin
on Fri Dec 15 15:36:03 GMT 2023
Record UNII
F39049Y068
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
APOMORPHINE HYDROCHLORIDE
EMA EPAR   EP   ORANGE BOOK   USP   USP-RS   VANDF   WHO-DD  
Common Name English
APOMORPHINE HYDROCHLORIDE HYDRATE
JAN  
Common Name English
TALUVIAN
Brand Name English
APOMORPHINUM MURIATICUM [HPUS]
Common Name English
APOMORPHINE HYDROCHLORIDE HEMIHYDRATE
EP   MI  
Common Name English
UPRIMA
Brand Name English
APOMORPHINE HCL
Common Name English
APOMORPHINE HYDROCHLORIDE [USP MONOGRAPH]
Common Name English
APOMORPHINE HYDROCHLORIDE HEMIHYDRATE [EP MONOGRAPH]
Common Name English
APOMORPHINE HYDROCHLORIDE HEMIHYDRATE [MI]
Common Name English
APOKYN
Brand Name English
APOMORPHINE HYDROCHLORIDE [VANDF]
Common Name English
APOMORPHINE HYDROCHLORIDE [ORANGE BOOK]
Common Name English
APOMORPHINE HYDROCHLORIDE [USP-RS]
Common Name English
IXENSE
Brand Name English
NSC-755875
Code English
KW-6500
Common Name English
APOMORPHINE HYDROCHLORIDE HYDRATE [JAN]
Common Name English
APOMORPHINE HYDROCHLORIDE [EMA EPAR]
Common Name English
6aβ-Aporphine-10,11-diol hydrochloride hemihydrate
Common Name English
(6AR)-5,6,6A,7-TETRAHYDRO-6-METHYL-4H-DIBENZO(DE,G)QUINOLINE-10,11-DIOL HYDROCHLORIDE HEMIHYDRATE
Common Name English
4H-DIBENZO(DE,G)QUINOLINE-10,11-DIOL, 5,6,6A,7-TETRAHYDRO-6-METHYL-, HYDROCHLORIDE, HEMIHYDRATE, (R)-
Common Name English
KYNMOBI
Brand Name English
Apomorphine hydrochloride [WHO-DD]
Common Name English
APOMORPHINUM MURIATICUM
HPUS  
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C66884
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
EMA ASSESSMENT REPORTS IXENSE (WITHDRAWN: ERECTILE DYSFUNCTIONS)
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
EU-Orphan Drug EU/3/06/349
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
NCI_THESAURUS C38149
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
FDA ORPHAN DRUG 204305
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
FDA ORPHAN DRUG 57591
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
EMA ASSESSMENT REPORTS UPRIMA (WITHDRAWN: ERECTILE DYSFUNCTIONS)
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
Code System Code Type Description
DAILYMED
F39049Y068
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
WIKIPEDIA
Apomorphine hydrochloride
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
CAS
41372-20-7
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
NSC
755875
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
EPA CompTox
DTXSID0048185
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
CHEBI
31228
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
DRUG BANK
DB00714
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
ChEMBL
CHEMBL53
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
RXCUI
71225
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY RxNorm
FDA UNII
F39049Y068
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
RS_ITEM_NUM
1041008
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
MERCK INDEX
m2003
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
NCI_THESAURUS
C47400
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
EMA ASSESSMENT REPORTS
TALUVIAN (WITHDRAWN: ERECTILE DYSFUNCTIONS)
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
PUBCHEM
107882
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
EVMPD
SUB12924MIG
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
SMS_ID
100000092009
Created by admin on Fri Dec 15 15:36:03 GMT 2023 , Edited by admin on Fri Dec 15 15:36:03 GMT 2023
PRIMARY
Related Record Type Details
Structure of APOMORPHINE HYDROCHLORIDE
BASIS OF STRENGTH->SUBSTANCE
ASSAY (TITRATION)
USP
Structure of APOMORPHINE HYDROCHLORIDE
BASIS OF STRENGTH->SUBSTANCE
ASSAY (TITRATION)
EP
Structure of APOMORPHINE HYDROCHLORIDE ANHYDROUS
ANHYDROUS->SOLVATE
Structure of APOMORPHINE
PARENT -> SALT/SOLVATE
Related Record Type Details
Structure of MORPHINE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Related Record Type Details
Structure of APOMORPHINE
ACTIVE MOIETY
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