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
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
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 |
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 |
---|---|---|
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 |
|
Do antioxidant strategies work against aging and age-associated disorders? Propargylamines: a possible antioxidant strategy. | 2001 Apr |
|
Deprenyl stimulates the efflux of monoamines from the rat hypothalamus in vitro. | 2001 Apr |
|
Evaluation of antiparkinsonian drugs in pharmacy records as a marker for Parkinson's disease. | 2001 Aug |
|
[Parkinson's disease]. | 2001 Aug |
|
Inhibition of rat liver microsomal CYP1A2 and CYP2B1 activity by N-(2-heptyl)-N-methyl-propargylamine and by N-(2-heptyl)-propargylamine. | 2001 Aug |
|
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 |
|
Biphasic effects of selegiline on striatal dopamine: lack of effect on methamphetamine-induced dopamine depletion. | 2001 Jan |
|
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 |
|
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 |
|
Inhibition of MAO-A activity enhances behavioural activity of rats assessed using water maze and open arena tasks. | 2001 Jun |
|
The frissonnant mutant mouse, a model of dopamino-sensitive, inherited motor syndrome. | 2001 Jun |
|
PET with 11C-deuterium-deprenyl and 18F-FDG in focal epilepsy. | 2001 Jun |
|
Advances in managing Parkinson's disease. | 2001 Jun 15 |
|
Practice parameters for the treatment of narcolepsy: an update for 2000. | 2001 Jun 15 |
|
Freezing of gait in PD: prospective assessment in the DATATOP cohort. | 2001 Jun 26 |
|
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 |
|
Current and emerging treatments in Parkinson's disease. | 2001 Mar |
|
[A behavioral and neurochemical study on the mechanism of the anxiolytic effect of monoamine oxidase inhibitors]. | 2001 May |
|
CYP2C19 polymorphism is not important for the in vivo metabolism of selegiline. | 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 |
|
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 |
|
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 |
|
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 |
|
Future of neuroprotection in Parkinson's disease. | 2001 Oct |
|
Drug-induced psychotic symptoms in Parkinson's disease. Problems, management and dilemma. | 2001 Sep |
|
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 |
|
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 |
|
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 |
|
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 |
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
Wed Jul 05 22:48:31 UTC 2023
by
admin
on
Wed Jul 05 22:48:31 UTC 2023
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Record UNII |
6W731X367Q
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C667
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FDA ORPHAN DRUG |
583
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EE-47
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9087
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203137
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M9835
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CHEMBL972
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26758
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SUB04347MIG
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SUB127352
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6W731X367Q
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1611900
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100000091038
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7183
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C47714
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DTXSID9044584
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6W731X367Q
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759259
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DBSALT000260
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14611-52-0
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Related Record | Type | Details | ||
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PARENT -> SALT/SOLVATE | |||
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (TITRATION)
EP
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Related Record | Type | Details | ||
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IMPURITY -> PARENT |
UNSPECIFIED
EP
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IMPURITY -> PARENT |
UNSPECIFIED
EP
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IMPURITY -> PARENT |
UNSPECIFIED
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
EP
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
UNSPECIFIED
EP
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Related Record | Type | Details | ||
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ACTIVE MOIETY |