pharmacopeia
GET
/api/v1/drug/selegiline
2D structure
(2R)-N-methyl-1-phenyl-N-prop-2-ynylpropan-2-amine
SMILES C[C@H](CC1=CC=CC=C1)N(C)CC#C
InChIKey MEZLKOACVSPNER-GFCCVEGCSA-N

Mechanism of action

Sourced from openFDA

Mechanism-of-action classes: Monoamine Oxidase-B Inhibitors; Monoamine Oxidase Inhibitors.

Monoamine OxidaseMonoamine Oxidase-B

Indications

Sourced from openFDA
  • Selegiline Hydrochloride Tablets USP are indicated as an adjunct in the management of Parkinsonian patients being treated with levodopa/carbidopa who exhibit deterioration in the quality of their response to this therapy. There is no evidence from controlled studies that selegiline has any beneficial effect in the absence of concurrent levodopa therapy.

Contraindications

Sourced from openFDA
  • Selegiline hydrochloride is contraindicated in patients with a known hypersensitivity to this drug. Selegiline is contraindicated for use with meperidine.contraindicated

Dosage & administration

Sourced from openFDA

Selegiline hydrochloride tablets USP are intended for administration to Parkinsonian patients receiving levodopa/carbidopa therapy who demonstrate a deteriorating response to this treatment. The recommended regimen for the administration of Selegiline Hydrochloride Tablets USP is 10 mg per day administered as divided doses of 5 mg each taken at breakfast and lunch. There is no evidence that additional benefit will be obtained from the administration of higher doses. Moreover, higher doses should ordinarily be avoided because of the increased risk of side effects. After two to three days of selegiline treatment, an attempt may be made to reduce the dose of levodopa/carbidopa. A reduction of 10 to 30% was achieved with the typical participant in the domestic placebo controlled trials who was assigned to selegiline treatment. Further reductions of levodopa/carbidopa may be possible during continued selegiline therapy.

Warnings & precautions

Sourced from openFDA

Selegiline should not be used at daily doses exceeding those recommended (10 mg/day) because of the risks associated with non-selective inhibition of MAO. (See CLINICAL PHARMACOLOGY .) The selectivity of selegiline for MAO B may not be absolute even at the recommended daily dose of 10 mg a day. Rare cases of hypertensive reactions associated with ingestion of tyramine-containing foods have been reported in patients taking the recommended daily dose of selegiline. The selectivity is further diminished with increasing daily doses. The precise dose at which selegiline becomes a non-selective inhibitor of all MAO is unknown, but may be in the range of 30 to 40 mg a day. Severe CNS toxicity associated with hyperpyrexia and death have been reported with the combination of tricyclic antidepressants and non-selective MAOIs (Phenelzine, Tranylcypromine). A similar reaction has been reported for a patient on amitriptyline and selegiline. Another patient receiving protriptyline and selegiline developed tremors, agitation, and restlessness followed by unresponsiveness and death two weeks after selegiline was added. Related adverse events including hypertension, syncope, asystole, diaphoresis, seizures, changes in behavioral and mental status, and muscular rigidity have also been reported in some patients receiving selegiline and various tricyclic antidepressants.

Adverse reactions

Sourced from openFDA

Introduction The number of patients who received selegiline in prospectively monitored pre-marketing studies is limited. While other sources of information about the use of selegiline are available (e.g., literature reports, foreign post-marketing reports, etc.) they do not provide the kind of information necessary to estimate the incidence of adverse events. Thus, overall incidence figures for adverse reactions associated with the use of selegiline cannot be provided. Many of the adverse reactions seen have also been reported as symptoms of dopamine excess. Moreover, the importance and severity of various reactions reported often cannot be ascertained. One index of relative importance, however, is whether or not a reaction caused treatment discontinuation. In prospective pre-marketing studies, the following events led, in decreasing order of frequency, to discontinuation of treatment with selegiline: nausea, hallucinations, confusion, depression, loss of balance, insomnia, orthostatic hypotension, increased akinetic involuntary movements, agitation, arrhythmia, bradykinesia, chorea, delusions, hypertension, new or increased angina pectoris and syncope. Events reported only once as a cause of discontinuation are ankle edema, anxiety, burning lips/mouth, constipation, drowsiness/lethargy, dystonia, excess perspiration, increased freezing, gastrointestinal bleeding, hair loss, increased tremor, nervousness, weakness and weight loss.

Use in specific populations

Sourced from openFDA

Pregnancy Pregnancy Category C No teratogenic effects were observed in a study of embryo-fetal development in Sprague-Dawley rats at oral doses of 4, 12, and 36 mg/kg or 4, 12 and 35 times the human therapeutic dose on a mg/m 2 basis. No teratogenic effects were observed in a study of embryo-fetal development in New Zealand White rabbits at oral doses of 5, 25, and 50 mg/kg or 10, 48, and 95 times the human therapeutic dose on a mg/m 2 basis; however, in this study, the number of litters produced at the two higher doses was less than recommended for assessing teratogenic potential. In the rat study, there was a decrease in fetal body weight at the highest dose tested. In the rabbit study, increases in total resorptions and % post-implantation loss, and a decrease in the number of live fetuses per dam occurred at the highest dose tested. In a peri- and postnatal development study in Sprague-Dawley rats (oral doses of 4, 16, and 64 mg/kg or 4, 15, and 62 times the human therapeutic dose on a mg/m 2 basis), an increase in the number of stillbirths and decreases in the number of pups per dam, pup survival, and pup body weight (at birth and throughout the lactation period) were observed at the two highest doses. At the highest dose tested, no pups born alive survived to Day 4 postpartum.

Overdosage

Sourced from openFDA

Selegiline No specific information is available about clinically significant overdoses with selegiline hydrochloride. However, experience gained during selegiline's development reveals that some individuals exposed to doses of 600 mg of d,l-selegiline suffered severe hypotension and psychomotor agitation. Since the selective inhibition of MAO B by selegiline hydrochloride is achieved only at doses in the range recommended for the treatment of Parkinson's disease (e.g., 10 mg/day), overdoses are likely to cause significant inhibition of both MAO A and MAO B. Consequently, the signs and symptoms of overdose may resemble those observed with marketed non-selective MAO inhibitors (e.g., tranylcypromine, isocarboxazide, and phenelzine). Overdose with Non-Selective MAO Inhibition NOTE: This section is provided for reference; it does not describe events that have actually been observed with selegiline in overdose. Characteristically, signs and symptoms of non-selective MAOI overdose may not appear immediately. Delays of up to 12 hours between ingestion of drug and the appearance of signs may occur.

Approval history

Sourced from openFDA
  • Aug 2, 1996ANDAANDA074565Chartwell Molecules
  • Apr 1, 1997ANDAANDA074672I3 Pharms
  • Jun 6, 1997ANDAANDA074871Apotex
  • Nov 30, 1998ANDAANDA075352Novitium Pharma
  • Dec 4, 1998ANDAANDA075321Apotex
  • Feb 27, 2006NDANDA021336Somerset
  • Jun 14, 2006NDANDA021479Bausch
  • Apr 2, 2019ANDAANDA206803Rising

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
3,469 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Drug Ineffective36010%
  2. 2Hallucination2276.5%
  3. 3Insomnia2045.9%
  4. 4Dizziness1945.6%
  5. 5Application Site Erythema1855.3%
  6. 6Fall1855.3%
  7. 7Dyskinesia1765.1%
  8. 8Drug Interaction1634.7%
  9. 9Depression1474.2%
  10. 10Anxiety1444.2%
  11. 11Tremor1424.1%
  12. 12Nausea1353.9%
  13. 13Application Site Rash1273.7%
  14. 14Fatigue1273.7%
  15. 15Application Site Pruritus1223.5%

Literature

View JSON

Recent PubMed references pinned to Selegiline as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

View JSON

The 10 most recently updated of 35 ClinicalTrials.gov registrations naming Selegiline as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Selegiline work?
Mechanism-of-action classes: Monoamine Oxidase-B Inhibitors; Monoamine Oxidase Inhibitors.
What is Selegiline used for?
According to FDA labeling, Selegiline carries indications including: Selegiline Hydrochloride Tablets USP are indicated as an adjunct in the management of Parkinsonian patients being treated with levodopa/carbidopa who exhibit deterioration in the quality of their response to this therapy. There is no evidence from controlled studies that selegiline has any beneficial effect in the absence of concurrent levodopa therapy.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Selegiline?
Selegiline is classified as Monoamine oxidase B inhibitors, Monoamine Oxidase Inhibitor, Monoamine Oxidase Type B Inhibitor, Monoamine Oxidase-B Inhibitors, Monoamine Oxidase Inhibitors, Increased Central Nervous System Dopamine Activity.
What are the brand names for Selegiline?
Selegiline is marketed under brand names including Anipryl, Emsam, Zelapar.
What are the contraindications for Selegiline?
Selegiline labeling lists contraindications including: Selegiline hydrochloride is contraindicated in patients with a known hypersensitivity to this drug. Selegiline is contraindicated for use with meperidine.. Always consult the full prescribing information and a clinician.
Note. Data for selegiline is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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