Selegiline (Transdermal)

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[edit] BRAND NAMES

[edit] STRUCTURE

Selegiline.jpg

[edit] MECHANISM OF ACTION

Selegiline is a selective irreversible inhibitor of monoamine oxidase (MAO). MAO exists as two isoenzymes, referred to as MAO-A and MAO-B.
In humans, intestinal MAO is predominantly type-A, while most of that in the brain is type-B. Selegiline has a greater affinity for MAO-B, compared to MAO-A. However, at antidepressant doses, selegiline inhibits both isoenzymes activities in the brain.
In the CNS, MAO-A and MAO-B play important roles in the catabolism of catecholamines (dopamine, noradrenaline and adrenaline) and serotonin. The mechanism of action of Selegiline as an antidepressant is presumed to be linked to potentiation of monoamine neurotransmitter activity in the central nervous system (CNS).

MAO in the gastrointestinal tract and liver (primarily type-A) for example, is thought to provide vital protection from exogenous amines (e.g. tyramine) that have the capacity, if absorbed intact, to cause a 'hypertensive crisis', the so-called 'cheese reaction'. This has been documented with nonselective MAO inhibitors (MAOIs).

Patients should be informed that tyramine-rich foods and beverages should be avoided beginning on the first day of Selegiline (Transdermal) 9 mg/24 hours or 12 mg/24 hours treatment and should continue to be avoided for 2 weeks after a dose reduction to 6 mg/24 hours or following the discontinuation of Selegiline (Transdermal) 9 mg/24 hours or 12 mg/24 hours

[edit] INDICATIONS

  • Treatment of major depressive disorder. A major depressive episode implies a prominent and relatively persistent (nearly every day for at least 2 weeks) depressed or dysphoric mood that usually interferes with daily functioning, and includes at least five of the following nine symptoms: depressed mood, loss of interest in usual activities, significant change in weight and/or appetite, insomnia or hypersomnia, psychomotor agitation or retardation, increased fatigue, feelings of guilt or worthlessness, slowed thinking or impaired concentration, and suicide attempt or suicidal ideation.

[edit] DOSAGE

Selegiline transdermal system should be applied to dry, intact skin on the upper torso (below the neck and above the waist), upper thigh or the outer surface of the upper arm once every 24 hours. The recommended starting dose and target dose is 6 mg/24 hours. If dose increases are indicated, they should occur in dose increments of 3 mg/24 hours (up to a maximum dose of 12 mg/24 hours) at intervals of no less than 2 weeks.

As with all antidepressant drugs, full antidepressant effect may be delayed.

[edit] CONTRAINDICATIONS

[edit] PRECAUTIONS

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

[edit] SIDE EFFECTS

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Antidepressants
Tricyclic antidepressants Amitriptyline (Elavil, Laroxyl)   Clomipramine (Anafranil)   Doxepin (Sinequan)   Imipramine (Tofranil)   Nortriptyline (Aventyl, Pamelor)   Trimipramine (Surmontil)
Selective serotonin reuptake inhibitors (SSRIs) Citalopram (Celexa, Seropram)   Escitalopram (Cipralex, Lexapro)   Fluoxetine (Prozac)   Fluvoxamine (Luvox, Maveral)   Paroxetine (Paxil, Seroxat)   Sertraline (Zoloft)
Serotonin–norepinephrine reuptake inhibitors (SNRIs) Desvenlafaxine (Pristiq)   Duloxetine (Cymbalta, Xeristar)   Venlafaxine (Efexor, Effexor)
Serotonin antagonists and reuptake inhibitors (SARIs) Trazodone (Desyrel, Oleptro)
Norepinephrine reuptake inhibitors (NRIs) Maprotiline (Ludiomil)   Reboxetine (Edronax)
Norepinephrine-dopamine reuptake inhibitors (NDRIs) Bupropion (Wellbutrin)
Noradrenergic and specific serotonergic antidepressants (NaSSAs) Mianserin (Lantanon)   Mirtazapine (Remeron)
Norepinephrine-dopamine disinhibitors (NDDIs) Agomelatine (Valdoxan, Thymanax)
Monoamine oxidase inhibitors Nonselective Tranylcypromine (Parnate)
Monoamine oxidase inhibitors B-Selective Selegiline (Transdermal) (Emsam)
Others 5-Hydroxytryptophan   S-Adenosyl methionine   Hypericum (St John's wort)