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 Date2006 |
|||
| 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 Date2006 |
|||
| 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 Date2006 |
|||
| 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 Date2006 |
|||
| 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 Date2006 |
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 |
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 Recommended Dose: 12 mg, 1 times / day Route: transdermal Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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
| 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 |
|---|---|---|
| The potential of dopamine agonists in drug addiction. | 2002-04 |
|
| Toxicokinetics of amphetamines: metabolism and toxicokinetic data of designer drugs, amphetamine, methamphetamine, and their N-alkyl derivatives. | 2002-04 |
|
| [Psychological and cognitive problems in Parkinson disease--therapeutic possibilities]. | 2002-03-06 |
|
| Treatment of periodic limb movements in sleep with selegiline HCl. | 2002-03 |
|
| Placebo-associated improvements in motor function: comparison of subjective and objective sections of the UPDRS in early Parkinson's disease. | 2002-03 |
|
| Inhibition of human LDL oxidation by the neuroprotective drug l-deprenyl. | 2002-03 |
|
| Uncertainties in the pharmacotherapy of Parkinson's disease and how to solve them. | 2002-02-15 |
|
| Neuroprotective actions of selegiline. | 2002-02-01 |
|
| Antiapoptotic effect of (-)-deprenyl in rat kidney after ischemia-reperfusion. | 2002-02 |
|
| Pirlindole and dehydropirlindole protect rat cultured neuronal cells against oxidative stress-induced cell death through a mechanism unrelated to MAO-A inhibition. | 2002-02 |
|
| The effect of selegiline in the treatment of people with Alzheimer's disease: a meta-analysis of published trials. | 2002-02 |
|
| Deprenyl protects from MPTP-induced Parkinson-like syndrome and glutathione oxidation in rat striatum. | 2002-01-25 |
|
| Switching from bromocriptine to ropinirole in patients with advanced Parkinson's disease: open label pilot responses to three different dose-ratios. | 2002-01-22 |
|
| Neuroprotective and neurotoxic effects of monoamine oxidase-B inhibitors and derived metabolites under ischemia in PC12 cells. | 2002-01-11 |
|
| 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. | 2002-01-08 |
|
| Effect of repeated treatment with high doses of selegiline on behaviour, striatal dopaminergic transmission and tyrosine hydroxylase mRNA levels. | 2002-01 |
|
| The influence of metabolism on the MAO-B inhibitory potency of selegiline. | 2002-01 |
|
| Antidepressants for smoking cessation. | 2002 |
|
| Investigating potential anxiolytic, antidepressant and memory enhancing activity of deprenyl. | 2001-12 |
|
| Zonisamide has beneficial effects on Parkinson's disease patients. | 2001-12 |
|
| Ten-year follow-up of three different initial treatments in de-novo PD: a randomized trial. | 2001-11-13 |
|
| (-)-D-Deprenyl attenuates apoptosis in experimental brain ischaemia. | 2001-11-02 |
|
| Chronic daily administration of selegiline and EGb 761 increases brain's resistance to ischemia in mice. | 2001-11-02 |
|
| Role of monoamine oxidase inhibition and monoamine depletion in fenfluramine-induced neurotoxicity and serotonin release. | 2001-11 |
|
| The effects of oral selegiline hydrochloride on learning and training in the dog: a psychobiological interpretation. | 2001-11 |
|
| 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. | 2001-11 |
|
| Incorporation of selegiline metabolites into hair after oral selegiline intake. | 2001-10 |
|
| Future of neuroprotection in Parkinson's disease. | 2001-10 |
|
| [Dopaminomimetic psychosis in Parkinson's disease: first symptom of early dementia?]. | 2001-09-20 |
|
| Drug-induced psychotic symptoms in Parkinson's disease. Problems, management and dilemma. | 2001-09 |
|
| Medical treatment of canine pituitary-dependent hyperadrenocorticism (Cushing's disease). | 2001-09 |
|
| Simultaneous determination of selegiline-N-oxide, a new indicator for selegiline administration, and other metabolites in urine by high-performance liquid chromatography-electrospray ionization mass spectrometry. | 2001-08-05 |
|
| Evaluation of antiparkinsonian drugs in pharmacy records as a marker for Parkinson's disease. | 2001-08 |
|
| Changes in vascular alpha 1- and alpha 2-adrenoceptor responsiveness by selegiline treatment. | 2001-08 |
|
| [Parkinson's disease]. | 2001-08 |
|
| Selegiline and mortality in subjects with Parkinson's disease: a longitudinal community study. | 2001-07-24 |
|
| Paroxysmal hypertensive crises induced by selegiline in a patient with Parkinson's disease. | 2001-06 |
|
| [A behavioral and neurochemical study on the mechanism of the anxiolytic effect of monoamine oxidase inhibitors]. | 2001-05 |
|
| Do antioxidant strategies work against aging and age-associated disorders? Propargylamines: a possible antioxidant strategy. | 2001-04 |
|
| Eldepryl prevents 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced nigral neuronal apoptosis in mice. | 2001-03 |
|
| Parkinson's disease therapy: treatment of early and late disease. | 2001-03 |
|
| Selegiline treatment facilitates recovery after stroke. | 2001 |
|
| Pharmacological options for the treatment of Tourette's disorder. | 2001 |
|
| The effect of low oral doses of (-)-deprenyl and its metabolites on DSP-4 toxicity. | 2001 |
|
| [The effect of selegiline and vitamin E in the treatment of ALS: an open randomized clinical trials]. | 2001 |
|
| Monoamine oxidase-inhibition and MPTP-induced neurotoxicity in the non-human primate: comparison of rasagiline (TVP 1012) with selegiline. | 2001 |
|
| 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 |
|
| Role of free radicals in the neurodegenerative diseases: therapeutic implications for antioxidant treatment. | 2001 |
|
| Effect of longevity treatment with (-)deprenyl on lifespan and sexual behavior in female rats. | 2001 |
|
| [Current strategies of pathogenetic therapy of Alzheimer's disease]. | 2001 |
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
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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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1611900
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100000091038
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7183
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C47714
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759259
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DBSALT000260
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14611-52-0
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PARENT -> SALT/SOLVATE | |||
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USP
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IMPURITY -> PARENT |
UNSPECIFIED
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IMPURITY -> PARENT |
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EP
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IMPURITY -> PARENT |
UNSPECIFIED
EP
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CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
EP
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IMPURITY -> PARENT |
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ACTIVE MOIETY |