Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C13H17N |
Molecular Weight | 187.2808 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@H](CC1=CC=CC=C1)N(C)CC#C
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
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 |
DescriptionSources: https://www.drugs.com/dosage/selegiline.htmlCurator'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
Sources: https://www.drugs.com/dosage/selegiline.html
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.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2039 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26337020 |
9.0 nM [IC50] | ||
Target ID: CHEMBL1951 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26278660 |
47.9 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | EMSAM Approved UseSelegiline 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 Date1.14099841E12 |
|||
Primary | EMSAM Approved UseSelegiline 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 Date1.14099841E12 |
|||
Primary | EMSAM Approved UseSelegiline 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 Date1.14099841E12 |
|||
Primary | EMSAM Approved UseSelegiline 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 Date1.14099841E12 |
|||
Primary | EMSAM Approved UseSelegiline 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 Date1.14099841E12 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
8.9 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/10215747 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
11 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/10215747 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/10215747 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Dose | Population | Adverse 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%) Sources: 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%) |
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%) Sources: 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%) |
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%) Sources: 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%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes [IC50 67.2 uM] | ||||
yes [Ki 15.6 uM] | ||||
yes [Ki 22 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
major | ||||
major | ||||
minor | ||||
minor | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes |
PubMed
Title | Date | PubMed |
---|---|---|
Selegiline effects on cocaine-induced changes in medial temporal lobe metabolism and subjective ratings of euphoria. | 1999 Jun |
|
Sleep attacks and Parkinson's disease treatment. | 2000 Apr 15 |
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Workshop IV: drug treatment guidelines for the long-term management of Parkinson's disease. | 2000 Sep |
|
A hypertensive reaction induced by concurrent use of selegiline and dopamine. | 2000 Sep |
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Antioxidant activity of the monoamine oxidase B inhibitor lazabemide. | 2000 Sep 1 |
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Selegiline treatment facilitates recovery after stroke. | 2001 |
|
Pharmacological options for the treatment of Tourette's disorder. | 2001 |
|
[The effect of selegiline and vitamin E in the treatment of ALS: an open randomized clinical trials]. | 2001 |
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Role of free radicals in the neurodegenerative diseases: therapeutic implications for antioxidant treatment. | 2001 |
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Freezing of gait in patients with advanced Parkinson's disease. | 2001 |
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Selegiline pharmacokinetics are unaffected by the CYP3A4 inhibitor itraconazole. | 2001 Apr |
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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 |
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Attenuation of paraquat-induced dopaminergic toxicity on the substantia nigra by (-)-deprenyl in vivo. | 2001 Apr 1 |
|
[Parkinson's disease]. | 2001 Aug |
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Investigating potential anxiolytic, antidepressant and memory enhancing activity of deprenyl. | 2001 Dec |
|
Selegiline combined with enriched-environment housing attenuates spatial learning deficits following focal cerebral ischemia in rats. | 2001 Feb |
|
SKF-38393, a dopamine receptor agonist, attenuates 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced neurotoxicity. | 2001 Feb 23 |
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Selective inhibition of amine oxidases differently potentiate the hypophagic effect of benzylamine in mice. | 2001 Feb 9 |
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Biphasic effects of selegiline on striatal dopamine: lack of effect on methamphetamine-induced dopamine depletion. | 2001 Jan |
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Different sensitivity of mitochondrial and cytosolic monoamine oxidases to in vivo but not in vitro inhibition by specific irreversible inhibitors. | 2001 Jan-Feb |
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Selegiline and mortality in subjects with Parkinson's disease: a longitudinal community study. | 2001 Jul 24 |
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Selegiline and mortality in subjects with Parkinson's disease: a longitudinal community study. | 2001 Jul 24 |
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Paroxysmal hypertensive crises induced by selegiline in a patient with Parkinson's disease. | 2001 Jun |
|
Practice parameters for the treatment of narcolepsy: an update for 2000. | 2001 Jun 15 |
|
Oxygen inhalation enhances striatal dopamine metabolism and monoamineoxidase enzyme inhibition prevents it: a microdialysis study. | 2001 Jun 22 |
|
Cardiovascular sympathomimetic amine interactions in rats treated with monoamine oxidase inhibitors and the novel oxazolidinone antibiotic linezolid. | 2001 May |
|
Semicarbazide-sensitive amine oxidase substrates stimulate glucose transport and inhibit lipolysis in human adipocytes. | 2001 May |
|
[Parkinson patients. Normal life expectancy with selegiline?]. | 2001 May 28 |
|
Evidence that L-deprenyl treatment for one week does not inhibit MAO A or the dopamine transporter in the human brain. | 2001 May 4 |
|
A favorable response to antiparkinsonian treatment in juvenile neuronal ceroid lipofuscinosis. | 2001 May 8 |
|
Practice parameter: management of dementia (an evidence-based review). Report of the Quality Standards Subcommittee of the American Academy of Neurology. | 2001 May 8 |
|
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 |
|
Neuroprotective and neurotoxic effects of monoamine oxidase-B inhibitors and derived metabolites under ischemia in PC12 cells. | 2002 Jan 11 |
|
[Psychological and cognitive problems in Parkinson disease--therapeutic possibilities]. | 2002 Mar 6 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/dosage/selegiline.html
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28108387
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
Edited
Sat Dec 16 16:51:21 UTC 2023
by
admin
on
Sat Dec 16 16:51:21 UTC 2023
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Record UNII |
2K1V7GP655
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Record Status |
Validated (UNII)
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Classification Tree | Code System | Code | ||
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NDF-RT |
N0000175761
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NDF-RT |
N0000175762
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WHO-VATC |
QN04BD01
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CFR |
21 CFR 520.2098
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WHO-ATC |
N04BD01
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NCI_THESAURUS |
C667
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NDF-RT |
N0000175744
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NDF-RT |
N0000000184
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WHO-VATC |
QN06AX90
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LIVERTOX |
NBK548891
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DB01037
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100000084107
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DTXSID6023575
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C61938
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SUB10474MIG
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2K1V7GP655
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9639
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2K1V7GP655
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50217
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SELEGILINE
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26757
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9086
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14611-51-9
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2429
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m9835
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SUB127352
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Selegiline
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D012642
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4436
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QQ-25
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6639
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CHEMBL972
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METABOLIC ENZYME -> SUBSTRATE |
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AMOUNT EXCRETED
URINE
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METABOLIC ENZYME -> SUBSTRATE |
MINOR
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METABOLIC ENZYME -> SUBSTRATE |
MAJOR
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METABOLITE -> PARENT |
average over 48 hours
MAJOR
URINE
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METABOLITE LESS ACTIVE -> PARENT |
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METABOLITE -> PARENT |
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PLASMA
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Biological Half-life | PHARMACOKINETIC |
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