a.

Introduction:
Selegiline is also known as deprenyl, which selectively inhibits MAO Type B at low to moderate
doses but doesn’t inhibit MAO Type A unless given at above recommended doses where it loses
it selectivity.
b. Generic name:
Selegiline
c. Brand name:
Eldepryl, Emsam, Selgin
d. Pharmacological class:
Monoamine oxidase Type B inhibitor
e. Pregnancy risk category:
B
f. Indications:
i. Parkinson’s disease
ii. Major depressive disorder
iii. Attention Deficit Hyperactivity Disorder (ADHD)
g. Pharmacokinetics:
i. Absorption: Selegiline undergoes extensive first-pass metabolism in the liver and
gastrointestinal tract. As a result, the oral formulation has low bioavailability (4%).
ii. Distribution: The peak plasma levels of metabolites are approximately 4 to 20 times higher
than the maximum plasma concentration of selegiline. However, the concentrations of
amphetamine and methamphetamine do not induce stimulatory effects. Selegiline exhibits
high plasma protein binding, specifically with macroglobulin and albumin.
iii. Metabolism: Selegiline undergoes metabolism to produce N-desmethylselegiline, L-
amphetamine, and L-methamphetamine. Notably, N-desmethylselegiline possesses MAO-B
inhibitory activity.
iv. Excretion: The mean elimination half-life of selegiline is 2 hours. However, under steady-
state concentration, the elimination half-life extends to 10 hours.
h. Mechanism of action:
Selegiline acts as an irreversible MAO inhibitor (MAOI). The MAO enzymes are responsible for
catabolizing neurotransmitters such as norepinephrine, serotonin, and dopamine. Blocking these
enzymes from functioning will inhibit the reuptake of these neurotransmitters in the central
nervous system (CNS), resulting in elevated levels of biologically active monoamines at the
synaptic cleft.
At lower doses, selegiline exhibits selective inhibition of B-type monoamine oxidase (MAO-B).
The cause of Parkinson disease is the loss of dopamine-containing neurons in the substantia nigra
of the midbrain, leading to a depletion of dopamine in the striatum. Therefore, the treatment of
Parkinson disease aims for selective MAO-B inhibition, as MAO-B is primarily responsible for
metabolizing dopamine.
i. Dosages:
1-2 mg/day orally initially, maximum dose upto 15mg/day in divided doses.
j. Available forms:
capsule and oral disintegrating tablet (ODT).
k. Drug-Drug interactions:
Patients should discontinue taking transdermal selegiline for at least 2 weeks before starting any
 of the following medications: carbamazepine, selective serotonin reuptake inhibitors, tricyclic
antidepressants such as clomipramine and imipramine, tramadol, propoxyphene, methadone,
pentazocine, and dextromethorphan. On the other hand, it is not recommended to begin
transdermal selegiline treatment until 5 half-lives have passed since taking the medications listed
earlier.
Selegiline should not be used via oral route concomitantly with cyclobenzaprine,
dextromethorphan, St. John's wort, methadone, propoxyphene, tramadol, or other MAOIs.
Patients who have previously shown hypersensitivity to selegiline should not use any form of the
medication. Furthermore, it is also not recommended to use any dose forms of selegiline while
taking meperidine.
Selegiline metabolism involves various subunits of the cytochrome P450 system, of which the
2B6 subunit is of particular significance as it plays a vital role in metabolism. Therefore,
interactions and impairments involving this enzyme can have clinically significant implications.
Patients with hepatic impairment may necessitate dose adjustment, and selegiline ODT is not
recommended for patients with severe hepatic impairment. Likewise, selegiline in ODT form
should be avoided in patients with a CrCl <30 mL/min
l. Contraindications:
Selegiline use within 10 days before elective surgery is contraindicated due to its adverse effects
on blood pressure. Transdermal selegiline is contraindicated in children younger than 12 and
patients of any age with pheochromocytoma.
m. Adverse effects:
i. Dizziness
ii. Nervousness
iii. Drowsiness
iv. Weakness
v. Headache
vi. Confusion
vii. Blurred Vision
viii. Mydriasis
ix. Tachycardia
x. Orthostatic Hypotension
xi. Dry Mouth
xii. Nausea
xiii. Constipation
xiv. Vomiting
xv. Urinary Retention
xvi. Decreased Sweating
n. Nursing considerations:
i. Assess Parkinsonism and extrapyramidal symptoms. Medications should be tapered
gradually.
ii. Caution patient to make positive changes slowly to minimize orthostatic hypotension.
iii. Instruct patient about frequent rinsing of mouth and good oral hygiene.
iv. Caution patient that this medication decreases perspiration, and overheating may occur
during hot weather.
References:

Shreevani, R. A guide to Mental Health & Psychiatric Nursing (4th Ed.) . Jaypee

Karen W., Lippincott Illustrated Reviews Pharmacology (5th Ed.).

www.ncbi.nlm.nih.gov

Pearson, J., Linda, Nurse Practitioner’s Handbook (3rd Ed.), Springhouse Corporation.

Gupta, Bibha, Manual of Basic Integrated Science- II (2nd Ed.), Samiksha