selegiline transdermal

Action and Spectrum

Actions and Spectrum: 

Actions 

selegiline acts by inhibiting the enzyme monoamine oxidase-B (MAO-B). By blocking this enzyme, selegiline increases dopamine levels in the brain, which helps alleviate the motor symptoms associated with Parkinson’s disease.  

Spectrum 

selegiline is primarily indicated for treating Parkinson’s disease, particularly during the early stages. It is an adjunct to levodopa/carbidopa therapy to help manage motor symptoms such as tremors, stiffness, and movement difficulties. It may also benefit mood and depressive symptoms associated with Parkinson’s disease.

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Application site reaction (24%) 

1-10% 

Hypotension (3-10%) 

Weight loss (5%) 

Diarrhea (9%) 

Xerostomia (8%) 

Rash (4%) 

Dyspepsia (4%) 

Sinusitis (3%) 

Pharyngitis (3%) 

Black Box Warning

Black Box Warning: 

Antidepressants increase the risk of suicidal thoughts and altered behavior in children.  

The risk of hypertensive crisis increases in children below 12 years. 

Contraindication / Caution

Contraindication/Caution: 

• Hypersensitivity 
• Concomitant use 
• Hepatic impairment 
• Hypertension 
• Surgery 

Pregnancy / Lactation

Pregnancy consideration:  

Pregnancy category: C 

Breastfeeding warnings:  

Use caution if the drug is taken during lactation  

Pregnancy category: 

Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology:  

selegiline is a selective inhibitor of monoamine oxidase-B (MAO-B). By inhibiting MAO-B, selegiline increases dopamine levels, a neurotransmitter that regulates movement and mood. This increased dopamine availability helps alleviate the motor symptoms associated with Parkinson’s disease. 

Pharmacodynamics: 

selegiline transdermal exerts its pharmacodynamic effects primarily through the selective inhibition of MAO-B. MAO-B is an enzyme responsible for the breakdown of dopamine in the brain. By inhibiting MAO-B, selegiline increases dopamine levels, which helps restore the imbalance of neurotransmitters observed in Parkinson’s disease. 

Pharmacokinetics: 

Absorption 

25-30% of the drug is absorbed 

Distribution 

Rapid distribution takes place in all body tissues 

The protein-bound is 90% 

Metabolism 

Metabolism takes place by CYP2B6, CYP3A4, CYP2C8, CYP2D6, CYP2A6 and CYP1A2 

Elimination and Excretion 

The drug is excreted 10% in urine and 2% in feces 

Adminstartion

Administration: 

Before applying the patch, ensure the skin is clean, dry, and free from any cuts, irritation, or rashes. Avoid areas with excessive hair, as it may interfere with proper adhesion. Select a relatively hairless area on the upper torso, such as the upper arm, upper back, or chest.

Rotating the application site to avoid skin irritation from prolonged use in the same area is recommended. Avoid applying the patch to areas that are oily, irritated, or likely to be subjected to friction or pressure (e.g., near the waistline or under tight clothing). 

Remove the protective liner from the patch, do not touch the adhesive side with your fingers. Apply the adhesive side firmly to the selected area of the skin. Press the patch firmly  to ensure it adheres properly. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: selegeline transdermal 

Why do we use selegiline transdermal? 

selegiline transdermal is used to treat depression. It is available in the form of transdermal patches.