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This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry ABSOLUTE
Molecular Formula C13H17N.ClH
Molecular Weight 223.742
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SELEGILINE HYDROCHLORIDE

SMILES

Cl.C[C@H](CC1=CC=CC=C1)N(C)CC#C

InChI

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

HIDE SMILES / InChI

Molecular Formula C13H17N
Molecular Weight 187.2808
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

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
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

2006
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

2006
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

2006
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

2006
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
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Insomnia 12%
12 mg 1 times / day multiple, transdermal
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Headache 18%
12 mg 1 times / day multiple, transdermal
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Abnormal dreams 2%
12 mg 1 times / day multiple, transdermal
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Application site reaction 24%
12 mg 1 times / day multiple, transdermal
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Anxiety 3%
12 mg 1 times / day multiple, transdermal
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Back pain 3%
12 mg 1 times / day multiple, transdermal
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Pharyngitis 3%
12 mg 1 times / day multiple, transdermal
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Somnolence 3%
12 mg 1 times / day multiple, transdermal
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Nervousness 4%
12 mg 1 times / day multiple, transdermal
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Dizziness 5%
12 mg 1 times / day multiple, transdermal
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Nausea 5%
12 mg 1 times / day multiple, transdermal
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Dry mouth 8%
12 mg 1 times / day multiple, transdermal
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Diarrhea 9%
12 mg 1 times / day multiple, transdermal
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Infection 9%
12 mg 1 times / day multiple, transdermal
Recommended
Dose: 12 mg, 1 times / day
Route: transdermal
Route: multiple
Dose: 12 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
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 effects on cocaine-induced changes in medial temporal lobe metabolism and subjective ratings of euphoria.
1999 Jun
Selegiline-induced postural hypotension in Parkinson's disease: a longitudinal study on the effects of drug withdrawal.
1999 Mar
Sleep attacks and Parkinson's disease treatment.
2000 Apr 15
Sleep attacks (sleep episodes) with pergolide.
2000 Apr 15
Workshop IV: drug treatment guidelines for the long-term management of Parkinson's disease.
2000 Sep
Adverse drug reactions to selegiline: a review of the French pharmacovigilance database.
2000 Sep-Oct
Selegiline treatment facilitates recovery after stroke.
2001
The effect of low oral doses of (-)-deprenyl and its metabolites on DSP-4 toxicity.
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
Anti-apoptotic and apoptotic action of (-)-deprenyl and its metabolites.
2001
Selective inhibition of MAO-B through chronic low-dose (R)-deprenyl treatment in C57BL/6 mice has no effect on basal neostriatal dopamine levels.
2001 Apr
Attenuation of paraquat-induced dopaminergic toxicity on the substantia nigra by (-)-deprenyl in vivo.
2001 Apr 1
Evaluation of antiparkinsonian drugs in pharmacy records as a marker for Parkinson's disease.
2001 Aug
Possible applications for dopaminergic agents following traumatic brain injury: part 2.
2001 Feb
The economic consequences of a drug-drug interaction.
2001 Feb
Selegiline and mortality in subjects with Parkinson's disease: a longitudinal community study.
2001 Jul 24
The frissonnant mutant mouse, a model of dopamino-sensitive, inherited motor syndrome.
2001 Jun
[Dopaminomimetic psychosis in Parkinson's disease: first symptom of early dementia?].
2001 Jun 1-15
Freezing of gait in PD: prospective assessment in the DATATOP cohort.
2001 Jun 26
Parkinson's disease therapy: treatment of early and late disease.
2001 Mar
L-dopa and selegiline for tyrosine hydroxylase deficiency.
2001 Mar
[A behavioral and neurochemical study on the mechanism of the anxiolytic effect of monoamine oxidase inhibitors].
2001 May
[Parkinson patients. Normal life expectancy with selegiline?].
2001 May 28
Practice parameter: management of dementia (an evidence-based review). Report of the Quality Standards Subcommittee of the American Academy of Neurology.
2001 May 8
Role of monoamine oxidase inhibition and monoamine depletion in fenfluramine-induced neurotoxicity and serotonin release.
2001 Nov
Ten-year follow-up of three different initial treatments in de-novo PD: a randomized trial.
2001 Nov 13
(-)-D-Deprenyl attenuates apoptosis in experimental brain ischaemia.
2001 Nov 2
Incorporation of selegiline metabolites into hair after oral selegiline intake.
2001 Oct
The potential of dopamine agonists in drug addiction.
2002 Apr
Antiapoptotic effect of (-)-deprenyl in rat kidney after ischemia-reperfusion.
2002 Feb
The effect of selegiline in the treatment of people with Alzheimer's disease: a meta-analysis of published trials.
2002 Feb
The influence of metabolism on the MAO-B inhibitory potency of selegiline.
2002 Jan
Uncertainties in the pharmacotherapy of Parkinson's disease and how to solve them.
2002 Jan-Feb
Placebo-associated improvements in motor function: comparison of subjective and objective sections of the UPDRS in early Parkinson's disease.
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 Mon Mar 31 17:52:56 GMT 2025
Edited
by admin
on Mon Mar 31 17:52:56 GMT 2025
Record UNII
6W731X367Q
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SELEGILINE HYDROCHLORIDE
EP   GREEN BOOK   HSDB   JAN   MART.   MI   ORANGE BOOK   USAN   USP   USP-RS   VANDF   WHO-DD  
USAN  
Official Name English
ELDEPRYL
Preferred Name English
Selegiline hydrochloride [WHO-DD]
Common Name English
SELEGILINE HYDROCHLORIDE [MI]
Common Name English
(-)-(R)-N,.ALPHA.-DIMETHYL-N-2-PROPYNYLPHENETHYLAMINE HYDROCHLORIDE
Systematic Name English
SELEGILINE HYDROCHLORIDE [JAN]
Common Name English
SELEGILINE HYDROCHLORIDE [USAN]
Common Name English
L-DEPRENYL
Common Name English
SELEGILINE HYDROCHLORIDE [USP MONOGRAPH]
Common Name English
SELEGILINE HCL
Common Name English
ZELAPAR
Brand Name English
BENZENEETHANAMINE, N,.ALPHA.-DIMETHYL-N-2-PROPYNYL-, HYDROCHLORIDE, (R)-
Systematic Name English
NSC-759259
Code English
SELEGILINE HYDROCHLORIDE [GREEN BOOK]
Common Name English
SELEGILINE HYDROCHLORIDE [HSDB]
Common Name English
SELEGILINE HYDROCHLORIDE [VANDF]
Common Name English
SELEGILINE HYDROCHLORIDE [EP MONOGRAPH]
Common Name English
SELEGILINE HYDROCHLORIDE [ORANGE BOOK]
Common Name English
SELEGILINE HYDROCHLORIDE [USP-RS]
Common Name English
SELEGILINE HYDROCHLORIDE [MART.]
Common Name English
ENSAM
Brand Name English
Classification Tree Code System Code
NCI_THESAURUS C667
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
FDA ORPHAN DRUG 583
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
Code System Code Type Description
USAN
EE-47
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
CHEBI
9087
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
RXCUI
203137
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY RxNorm
MERCK INDEX
m9835
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY Merck Index
ChEMBL
CHEMBL972
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
PUBCHEM
26758
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
EVMPD
SUB04347MIG
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
EVMPD
SUB127352
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
DAILYMED
6W731X367Q
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
RS_ITEM_NUM
1611900
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
SMS_ID
100000091038
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
HSDB
7183
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
NCI_THESAURUS
C47714
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
EPA CompTox
DTXSID9044584
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
FDA UNII
6W731X367Q
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
NSC
759259
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
DRUG BANK
DBSALT000260
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
CAS
14611-52-0
Created by admin on Mon Mar 31 17:52:56 GMT 2025 , Edited by admin on Mon Mar 31 17:52:56 GMT 2025
PRIMARY
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