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Details

Stereochemistry ABSOLUTE
Molecular Formula C13H17N
Molecular Weight 187.2813
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SELEGILINE

SMILES

C#CCN(C)[C@]([H])(C)Cc1ccccc1

InChI

InChIKey=MEZLKOACVSPNER-GFCCVEGCSA-N
InChI=1S/C13H17N/c1-4-10-14(3)12(2)11-13-8-6-5-7-9-13/h1,5-9,12H,10-11H2,2-3H3/t12-/m1/s1

HIDE SMILES / InChI

Molecular Formula C13H17N
Molecular Weight 187.2813
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: description was created based on several sources, including https://www.drugbank.ca/drugs/DB01037 | https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/021708s000_021336s000lbl.pdf | https://www.ncbi.nlm.nih.gov/pubmed/18237459 | https://www.ncbi.nlm.nih.gov/pubmed/28108387

Selegiline, also known as L-deprenyl, is a substituted phenethylamine, a selective, irreversible inhibitor of Type B monoamine oxidase. Selegiline is available in pill form under many brand names (Eldepryl, Carbex, Atapryl) and is used to reduce symptoms in early-stage Parkinson's disease. Selegiline delays the time point when the L-DOPA (levodopa) treatment becomes necessary from about 11 months to about 18 months after diagnosis, which is beneficial despite not being definitive evidence of neuroprotection. The rationale for adding selegiline to levodopa is to decrease the required dose of levodopa and thus reduce the motor complications of levodopa therapy. Selegiline is also delivered via a transdermal patch (brand name, Emsam) and in this form, Selegiline is used as a treatment for the major depressive disorder. Selegiline (brand name Anipryl) is also used (at extremely high dosages relative to humans) in veterinary medicine to treat the symptoms of Cushing's disease and cognitive dysfunction (Canine Cognitive Dysfunction) in dogs. Side effects of the pill form include, in decreasing order of frequency, nausea, hallucinations, confusion, depression, loss of balance, insomnia, increased involuntary movements, agitation, arrhythmia, slow heart rate, delusions, hypertension, new or increased angina pectoris, and syncope. The main side effects of the patch form for depression included application site reactions, insomnia, diarrhea, and sore throat.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
9.0 nM [IC50]
47.9 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
EMSAM

Approved Use

Selegiline Hydrochloride Tablets USP are indicated as an adjunct in the management of Parkinsonian patients being treated with levodopa/carbidopa who exhibit deterioration in the quality of their response to this therapy. There is no evidence from controlled studies that selegiline has any beneficial effect in the absence of concurrent levodopa therapy. Evidence supporting this claim was obtained in randomized controlled clinical investigations that compared the effects of added selegiline or placebo in patients receiving levodopa/carbidopa. Selegiline was significantly superior to placebo on all three principal outcome measures employed: change from baseline in daily levodopa/carbidopa dose, the amount of 'off' time, and patient self-rating of treatment success. Beneficial effects were also observed on other measures of treatment success (e.g., measures of reduced end of dose akinesia, decreased tremor and sialorrhea, improved speech and dressing ability and improved overall disability as assessed by walking and comparison to previous state).

Launch Date

1.14099841E12
Primary
EMSAM

Approved Use

Selegiline Hydrochloride Tablets USP are indicated as an adjunct in the management of Parkinsonian patients being treated with levodopa/carbidopa who exhibit deterioration in the quality of their response to this therapy. There is no evidence from controlled studies that selegiline has any beneficial effect in the absence of concurrent levodopa therapy. Evidence supporting this claim was obtained in randomized controlled clinical investigations that compared the effects of added selegiline or placebo in patients receiving levodopa/carbidopa. Selegiline was significantly superior to placebo on all three principal outcome measures employed: change from baseline in daily levodopa/carbidopa dose, the amount of 'off' time, and patient self-rating of treatment success. Beneficial effects were also observed on other measures of treatment success (e.g., measures of reduced end of dose akinesia, decreased tremor and sialorrhea, improved speech and dressing ability and improved overall disability as assessed by walking and comparison to previous state).

Launch Date

1.14099841E12
Primary
EMSAM

Approved Use

Selegiline Hydrochloride Tablets USP are indicated as an adjunct in the management of Parkinsonian patients being treated with levodopa/carbidopa who exhibit deterioration in the quality of their response to this therapy. There is no evidence from controlled studies that selegiline has any beneficial effect in the absence of concurrent levodopa therapy. Evidence supporting this claim was obtained in randomized controlled clinical investigations that compared the effects of added selegiline or placebo in patients receiving levodopa/carbidopa. Selegiline was significantly superior to placebo on all three principal outcome measures employed: change from baseline in daily levodopa/carbidopa dose, the amount of 'off' time, and patient self-rating of treatment success. Beneficial effects were also observed on other measures of treatment success (e.g., measures of reduced end of dose akinesia, decreased tremor and sialorrhea, improved speech and dressing ability and improved overall disability as assessed by walking and comparison to previous state).

Launch Date

1.14099841E12
Primary
EMSAM

Approved Use

Selegiline Hydrochloride Tablets USP are indicated as an adjunct in the management of Parkinsonian patients being treated with levodopa/carbidopa who exhibit deterioration in the quality of their response to this therapy. There is no evidence from controlled studies that selegiline has any beneficial effect in the absence of concurrent levodopa therapy. Evidence supporting this claim was obtained in randomized controlled clinical investigations that compared the effects of added selegiline or placebo in patients receiving levodopa/carbidopa. Selegiline was significantly superior to placebo on all three principal outcome measures employed: change from baseline in daily levodopa/carbidopa dose, the amount of 'off' time, and patient self-rating of treatment success. Beneficial effects were also observed on other measures of treatment success (e.g., measures of reduced end of dose akinesia, decreased tremor and sialorrhea, improved speech and dressing ability and improved overall disability as assessed by walking and comparison to previous state).

Launch Date

1.14099841E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
8.9 ng/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEGILINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
11 ng × h/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEGILINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
1.3 h
1.25 mg single, oral
dose: 1.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEGILINE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1.8 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEGILINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
15%
1.25 mg single, oral
dose: 1.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEGILINE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
12 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 116
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 116
Sources:
Other AEs: Headache, Infection...
Other AEs:
Headache (16%)
Infection (15%)
Back pain (6%)
Diarrhea (11%)
Nausea (7%)
Insomnia (32%)
Dry mouth (13%)
Dizziness (14%)
Nervousness (10%)
Somnolence (5%)
Anxiety (5%)
Abnormal dreams (5%)
Pharyngitis (7%)
Application site reaction (44%)
Sources:
12 mg 1 times / day multiple, transdermal (max)
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 817
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 817
Sources:
Other AEs: Headache, Infection...
Other AEs:
Headache (18%)
Infection (9%)
Back pain (3%)
Diarrhea (9%)
Nausea (5%)
Insomnia (12%)
Dry mouth (8%)
Dizziness (5%)
Nervousness (4%)
Somnolence (3%)
Anxiety (3%)
Abnormal dreams (2%)
Pharyngitis (3%)
Application site reaction (24%)
Sources:
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Other AEs: Back pain, Chest pain...
Other AEs:
Back pain (5%)
Chest pain (2%)
Pain (8%)
Hypertension (3%)
Constipation (4%)
Diarrhea (2%)
Dysphagia (2%)
Dyspepsia (5%)
Flatulence (2%)
Nausea (11%)
Stomatitis (5%)
Tooth disorder (2%)
Vomiting (3%)
Ecchymosis (2%)
Hypokalemia (2%)
Leg cramps (3%)
Myalgia (3%)
Ataxia (3%)
Depression (2%)
Dizziness (11%)
Dry mouth (4%)
Dyskinesia (6%)
Hallucinations (4%)
Headache (7%)
Insomnia (7%)
Somnolence (3%)
Tremor (3%)
Dyspnea (3%)
Pharyngitis (4%)
Rhinitis (7%)
Rash (4%)
Skin disorder (6%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Nervousness 10%
12 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 116
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 116
Sources:
Diarrhea 11%
12 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 116
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 116
Sources:
Dry mouth 13%
12 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 116
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 116
Sources:
Dizziness 14%
12 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 116
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 116
Sources:
Infection 15%
12 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 116
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 116
Sources:
Headache 16%
12 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 116
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 116
Sources:
Insomnia 32%
12 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 116
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 116
Sources:
Application site reaction 44%
12 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 116
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 116
Sources:
Abnormal dreams 5%
12 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 116
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 116
Sources:
Anxiety 5%
12 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 116
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 116
Sources:
Somnolence 5%
12 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 116
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 116
Sources:
Back pain 6%
12 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 116
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 116
Sources:
Nausea 7%
12 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 116
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 116
Sources:
Pharyngitis 7%
12 mg 1 times / day multiple, transdermal
Highest studied dose
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 116
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 116
Sources:
Insomnia 12%
12 mg 1 times / day multiple, transdermal (max)
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 817
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 817
Sources:
Headache 18%
12 mg 1 times / day multiple, transdermal (max)
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 817
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 817
Sources:
Abnormal dreams 2%
12 mg 1 times / day multiple, transdermal (max)
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 817
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 817
Sources:
Application site reaction 24%
12 mg 1 times / day multiple, transdermal (max)
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 817
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 817
Sources:
Anxiety 3%
12 mg 1 times / day multiple, transdermal (max)
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 817
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 817
Sources:
Back pain 3%
12 mg 1 times / day multiple, transdermal (max)
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 817
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 817
Sources:
Pharyngitis 3%
12 mg 1 times / day multiple, transdermal (max)
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 817
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 817
Sources:
Somnolence 3%
12 mg 1 times / day multiple, transdermal (max)
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 817
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 817
Sources:
Nervousness 4%
12 mg 1 times / day multiple, transdermal (max)
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 817
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 817
Sources:
Dizziness 5%
12 mg 1 times / day multiple, transdermal (max)
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 817
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 817
Sources:
Nausea 5%
12 mg 1 times / day multiple, transdermal (max)
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 817
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 817
Sources:
Dry mouth 8%
12 mg 1 times / day multiple, transdermal (max)
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 817
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 817
Sources:
Diarrhea 9%
12 mg 1 times / day multiple, transdermal (max)
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 817
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 817
Sources:
Infection 9%
12 mg 1 times / day multiple, transdermal (max)
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
n = 817
Health Status: unhealthy
Condition: major depressive disorder
Age Group: adult
Sex: M+F
Population Size: 817
Sources:
Dizziness 11%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Nausea 11%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Chest pain 2%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Depression 2%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Diarrhea 2%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Dysphagia 2%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Ecchymosis 2%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Flatulence 2%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Hypokalemia 2%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Tooth disorder 2%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Ataxia 3%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Dyspnea 3%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Hypertension 3%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Leg cramps 3%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Myalgia 3%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Somnolence 3%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Tremor 3%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Vomiting 3%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Constipation 4%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Dry mouth 4%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Hallucinations 4%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Pharyngitis 4%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Rash 4%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Back pain 5%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Dyspepsia 5%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Stomatitis 5%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Dyskinesia 6%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Skin disorder 6%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Headache 7%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Insomnia 7%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Rhinitis 7%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Pain 8%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Co-administed with::
levodopa
Sources:
unhealthy, adult
n = 194
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Sex: M+F
Population Size: 194
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG



Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
yes [IC50 67.2 uM]
yes [Ki 15.6 uM]
yes [Ki 22 uM]
Drug as victim

Drug as victim

PubMed

PubMed

TitleDatePubMed
Selegiline treatment facilitates recovery after stroke.
2001
Pharmacological options for the treatment of Tourette's disorder.
2001
The effect of low oral doses of (-)-deprenyl and its metabolites on DSP-4 toxicity.
2001
[The effect of selegiline and vitamin E in the treatment of ALS: an open randomized clinical trials].
2001
Monoamine oxidase-inhibition and MPTP-induced neurotoxicity in the non-human primate: comparison of rasagiline (TVP 1012) with selegiline.
2001
Role of free radicals in the neurodegenerative diseases: therapeutic implications for antioxidant treatment.
2001
Effect of longevity treatment with (-)deprenyl on lifespan and sexual behavior in female rats.
2001
[Current strategies of pathogenetic therapy of Alzheimer's disease].
2001
Do antioxidant strategies work against aging and age-associated disorders? Propargylamines: a possible antioxidant strategy.
2001 Apr
Evaluation of antiparkinsonian drugs in pharmacy records as a marker for Parkinson's disease.
2001 Aug
Changes in vascular alpha 1- and alpha 2-adrenoceptor responsiveness by selegiline treatment.
2001 Aug
[Parkinson's disease].
2001 Aug
Simultaneous determination of selegiline-N-oxide, a new indicator for selegiline administration, and other metabolites in urine by high-performance liquid chromatography-electrospray ionization mass spectrometry.
2001 Aug 5
Investigating potential anxiolytic, antidepressant and memory enhancing activity of deprenyl.
2001 Dec
Zonisamide has beneficial effects on Parkinson's disease patients.
2001 Dec
Antiaging compounds: (-)deprenyl (selegeline) and (-)1-(benzofuran-2-yl)-2-propylaminopentane, [(-)BPAP], a selective highly potent enhancer of the impulse propagation mediated release of catecholamine and serotonin in the brain.
2001 Fall
Current advances in Parkinson's disease.
2001 Jul
Selegiline and mortality in subjects with Parkinson's disease: a longitudinal community study.
2001 Jul 24
Selegiline and mortality in subjects with Parkinson's disease: a longitudinal community study.
2001 Jul 24
Paroxysmal hypertensive crises induced by selegiline in a patient with Parkinson's disease.
2001 Jun
Rescue of dying neurons by (R)-deprenyl in the MPTP-mouse model of Parkinson's disease does not include restoration of neostriatal dopamine.
2001 Jun
[Dopaminomimetic psychosis in Parkinson's disease: first symptom of early dementia?].
2001 Jun 1-15
Eldepryl prevents 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced nigral neuronal apoptosis in mice.
2001 Mar
Parkinson's disease therapy: treatment of early and late disease.
2001 Mar
Role of monoamine oxidase inhibition and monoamine depletion in fenfluramine-induced neurotoxicity and serotonin release.
2001 Nov
The effects of oral selegiline hydrochloride on learning and training in the dog: a psychobiological interpretation.
2001 Nov
CYP2B6 and CYP2C19 as the major enzymes responsible for the metabolism of selegiline, a drug used in the treatment of Parkinson's disease, as revealed from experiments with recombinant enzymes.
2001 Nov
(-)-D-Deprenyl attenuates apoptosis in experimental brain ischaemia.
2001 Nov 2
Chronic daily administration of selegiline and EGb 761 increases brain's resistance to ischemia in mice.
2001 Nov 2
Switching from bromocriptine to ropinirole in patients with advanced Parkinson's disease: open label pilot responses to three different dose-ratios.
2001 Nov-Dec
Incorporation of selegiline metabolites into hair after oral selegiline intake.
2001 Oct
Drug-induced psychotic symptoms in Parkinson's disease. Problems, management and dilemma.
2001 Sep
Medical treatment of canine pituitary-dependent hyperadrenocorticism (Cushing's disease).
2001 Sep
Antidepressants for smoking cessation.
2002
The potential of dopamine agonists in drug addiction.
2002 Apr
Toxicokinetics of amphetamines: metabolism and toxicokinetic data of designer drugs, amphetamine, methamphetamine, and their N-alkyl derivatives.
2002 Apr
Antiapoptotic effect of (-)-deprenyl in rat kidney after ischemia-reperfusion.
2002 Feb
Pirlindole and dehydropirlindole protect rat cultured neuronal cells against oxidative stress-induced cell death through a mechanism unrelated to MAO-A inhibition.
2002 Feb
The effect of selegiline in the treatment of people with Alzheimer's disease: a meta-analysis of published trials.
2002 Feb
Neuroprotective actions of selegiline.
2002 Feb 1
Effect of repeated treatment with high doses of selegiline on behaviour, striatal dopaminergic transmission and tyrosine hydroxylase mRNA levels.
2002 Jan
The influence of metabolism on the MAO-B inhibitory potency of selegiline.
2002 Jan
Neuroprotective and neurotoxic effects of monoamine oxidase-B inhibitors and derived metabolites under ischemia in PC12 cells.
2002 Jan 11
Deprenyl protects from MPTP-induced Parkinson-like syndrome and glutathione oxidation in rat striatum.
2002 Jan 25
Practice parameter: initiation of treatment for Parkinson's disease: an evidence-based review: report of the Quality Standards Subcommittee of the American Academy of Neurology.
2002 Jan 8
Uncertainties in the pharmacotherapy of Parkinson's disease and how to solve them.
2002 Jan-Feb
Treatment of periodic limb movements in sleep with selegiline HCl.
2002 Mar
Placebo-associated improvements in motor function: comparison of subjective and objective sections of the UPDRS in early Parkinson's disease.
2002 Mar
Inhibition of human LDL oxidation by the neuroprotective drug l-deprenyl.
2002 Mar
[Psychological and cognitive problems in Parkinson disease--therapeutic possibilities].
2002 Mar 6
Patents

Sample Use Guides

Usual Adult Dose for Parkinson's Disease: Recommended dose: 5 mg orally twice a day, Maximum dose: 10 mg orally per day Usual Adult Dose for Depression: Initial dose: Apply one 6 mg/24 hours transdermal patch to intact skin once every 24 hours, Maintenance dose: One 6 mg/24 hours to 12 mg/24 hours transdermal patch applied to the skin once a day, Maximum dose: 12 mg/24 hours transdermal patch applied to the skin once a day
Route of Administration: Other
BEAS-2B cells were seeded in 6 cm dishes. Cells were pretreated with 100 nM selegiline for 30 min before further exposed to 2% CSM for 24 h. Total protein was extracted. Monoamine Oxidase Activity Fluorometric Assay Kit (BioVision Inc., Milpitas, CA, USA), Superoxide Dismutase (SOD) Detection kit (Nanjing Jiancheng Bioenginering Inst., China), Amplex Red Catalase Assay kit (Molecular Probes, Inc., Eugene, OR, USA) and Oxidative Glutathi-one (GSSG) Detection Kit (Nanjing Jiancheng Bioenginering Y. Cui et al. / Toxicology Letters 268 (2017) 44–50 45Inst., China) were used for MAO, SOD and CAT activities and GSH/GSSG ratio measurement, respectively.
Substance Class Chemical
Created
by admin
on Sat Jun 26 08:18:39 UTC 2021
Edited
by admin
on Sat Jun 26 08:18:39 UTC 2021
Record UNII
2K1V7GP655
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SELEGILINE
INN   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
SELEGILINE [ORANGE BOOK]
Common Name English
SELEGILINE [VANDF]
Common Name English
SELEGILINE [WHO-DD]
Common Name English
EMSAM
Brand Name English
SELEGILINE [MI]
Common Name English
SELEGILINE [INN]
Common Name English
BENZENEETHANAMINE, N,.ALPHA.-METHYL-N-2-PROPYNYL-, (.ALPHA.R)-
Common Name English
(-)-(N)-METHYL-N-((1R)-1-METHYL-2-PHENYLETHYL)PROP-2-YN-1-AMINE
Common Name English
L-SELEGILINE
Common Name English
SELEGILINE [USAN]
Common Name English
Classification Tree Code System Code
NDF-RT N0000175761
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
NDF-RT N0000175762
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
WHO-VATC QN04BD01
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
CFR 21 CFR 520.2098
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
WHO-ATC N04BD01
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
NCI_THESAURUS C667
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
NDF-RT N0000175744
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
NDF-RT N0000000184
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
WHO-VATC QN06AX90
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
LIVERTOX 877
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
Code System Code Type Description
DRUG BANK
DB01037
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY
EPA CompTox
14611-51-9
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY
NCI_THESAURUS
C61938
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY
EVMPD
SUB10474MIG
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY
FDA UNII
2K1V7GP655
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY
RXCUI
9639
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY RxNorm
WIKIPEDIA
SELEGILINE
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY
PUBCHEM
26757
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY
CAS
14611-51-9
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY
DRUG CENTRAL
2429
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY
MERCK INDEX
M9835
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY Merck Index
EVMPD
SUB127352
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY
LACTMED
Selegiline
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY
MESH
D012642
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY
INN
4436
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY
IUPHAR
6639
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY
ChEMBL
CHEMBL972
Created by admin on Sat Jun 26 08:18:39 UTC 2021 , Edited by admin on Sat Jun 26 08:18:39 UTC 2021
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
BINDER->LIGAND
BINDING
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
MAJOR
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
MAJOR
METABOLIC ENZYME -> SUBSTRATE
MAJOR
EXCRETED UNCHANGED
AMOUNT EXCRETED
URINE
LABELED -> NON-LABELED
METABOLIC ENZYME -> SUBSTRATE
MINOR
METABOLIC ENZYME -> SUBSTRATE
MAJOR
Related Record Type Details
METABOLITE -> PARENT
IN-VIVO
URINE
METABOLITE -> PARENT
average over 48 hours
MAJOR
URINE
METABOLITE LESS ACTIVE -> PARENT
MAJOR
PLASMA
METABOLITE -> PARENT
MAJOR
PLASMA
METABOLITE -> PARENT
METABOLITE -> PARENT
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ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC