Adult: As conventional tab or cap: As monotherapy in early Parkinson's disease for symptomatic relief to delay the need for levodopa or as an adjunct to levodopa (with or without decarboxylase inhibitor): 10 mg daily, given as a single dose (in the morning) or in 2 divided doses (at breakfast and lunch). As orally disintegrating tab: As an adjunct to levodopa/carbidopa therapy: Initially, 1.25 mg once daily (in the morning before breakfast and without liquid; avoid consuming food or liquid for 5 minutes before and after administration) for at least 6 weeks; may increase dose to 2.5 mg once daily if needed. Treatment recommendations may vary among countries and between individual products (refer to specific product guidelines).
Transdermal Major depressive disorder
Adult: As transdermal patch: Initially, 6 mg/24 hours patch once daily. Dose may be increased in increments of 3 mg/24 hours every 2 weeks up to a Max of 12 mg/24 hours based on clinical response. Apply the patch to clean, dry, intact skin on the upper torso (below the neck and above the waist), upper thigh or outer surface of the upper arm every 24 hours.
What are the brands available for Selegiline in Singapore?
Oral:
As orally disintegrating tab:
ESRD: Not recommended.
CrCl (mL/min)
Dosage
<30
Not recommended.
Hepatic Impairment
Oral:
As orally disintegrating tab: Mild to moderate (Child-Pugh class A and B): 1.25 mg once daily according to patient's response and tolerability. Severe (Child-Pugh class C): Not recommended.
Administration
Should be taken with food.
Contraindications
Active duodenal or gastric ulcer; extrapyramidal disorders not related to dopamine deficiency. Concomitant use with other MAOIs or other potent inhibitors of monoamine oxidase (e.g. linezolid), opioids (e.g. pethidine), TCAs, SNRIs, SSRIs, cyclobenzaprine, dextromethorphan, or St. John's wort. Transdermal: Phaeochromocytoma, children <12 years; concomitant use with carbamazepine, SSRIs, SNRIs, clomipramine, imipramine, tramadol, propoxyphene, pethidine, methadone, pentazocine, or dextromethorphan. Contraindications may vary between individual products (refer to specific product labelling for detailed information).
Special Precautions
Patient with labile hypertension, cardiac arrhythmias, severe angina pectoris, psychosis, history of peptic ulceration, cerebrovascular disease, hypovolaemia, history of hepatic dysfunction; bipolar disorder (transdermal patch). Patient undergoing surgery. Avoid abrupt withdrawal. Hepatic and severe renal impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Hypertension, orthostatic hypotension; elevated liver enzymes (prolonged use); dyskinesia; CNS depression; irritation of buccal mucosa, new or worsening mental status and behavioural changes (orally disintegrating tab); increased risk of suicidal thoughts and behaviours (transdermal patch). Rarely, impulse control disorders and compulsions (e.g. pathological gambling, increased libido or hypersexuality, binge eating, different kinds of compulsive or repetitive activities). Cardiac disorders: Bradycardia. Ear and labyrinth disorders: Vertigo. Gastrointestinal disorders: Stomatitis, nausea, diarrhoea, constipation. General disorders and administration site conditions: Fatigue; application site reaction (transdermal). Injury, poisoning and procedural complications: Fall. Musculoskeletal and connective tissue disorders: Muscle cramps, back pain, arthralgia. Nervous system disorders: Dizziness, headache, impaired balance, tremor, akinesia, bradykinesia. Psychiatric disorders: Sleeping disorders, confusion, hallucinations, depression. Respiratory, thoracic and mediastinal disorders: Sore throat, nasal congestion. Skin and subcutaneous tissue disorders: Increased sweating.
This drug may cause dizziness, drowsiness, or impaired mental abilities, if affected, do not drive or operate machinery. Avoid or limit consumption of tyramine-containing food or beverages. Transdermal: Avoid exposing the application site and surrounding area to direct external heat sources (e.g. heating pads, electric blankets, heated water beds, saunas, heat lamps, hot tubs, prolonged direct sunlight).
Monitoring Parameters
Monitor blood pressure, mood and behaviour. Transdermal: Screen for personal or family history of bipolar disorder, mania or hypomania before treatment initiation. Closely monitor for clinical worsening and emergence of suicidal ideation or behaviour (particularly during the 1st 1-2 months or during dosage adjustments).
Drug Interactions
May increase the risk of hypertensive crisis with other MAOIs (selective or non-selective), sympathomimetic agents (e.g. ephedrine) and carbamazepine. Concomitant use with dextromethorphan may result in brief episodes of psychosis or bizarre behaviour. May potentiate the effects of levodopa and may cause or exacerbate dyskinesia. Increased risk of side effects with amantadine and anticholinergic agents. Concomitant use with oral contraceptives may increase bioavailability. Dopamine antagonists (e.g. metoclopramide, certain antipsychotic agents) may diminish the effect of selegiline. Potentially Fatal: Increased risk of serotonin syndrome with opioids (e.g. pethidine, tramadol, buprenorphine), SSRIs (e.g. fluoxetine, fluvoxamine, paroxetine, sertraline), SNRIs (e.g. venlafaxine), and TCAs (e.g. amitriptyline).
Food Interaction
Increased risk of serotonin syndrome with St. John's wort. Rarely, concomitant intake of tyramine-containing foods may cause hypertensive reactions.
Lab Interference
May cause a false-positive result in the urine detection of amphetamine or methamphetamine.
Action
Description: Mechanism of Action: Selegiline is a selective and irreversible monoamine oxidase type B (MAO-B) inhibitor that inhibits the breakdown of dopamine in the brain and prevents dopamine reuptake at the presynaptic dopamine receptor. These effects enhance dopaminergic activity in the brain and help to even out and prolong the effect of endogenous and exogenous dopamine. Its exact mechanism of action as an antidepressant is not completely understood; however, it is thought to be related to the potentiation of monoamine neurotransmitter activity in the CNS through its irreversible inhibition of the monoamine oxidase enzyme. Pharmacokinetics: Absorption: Readily absorbed from the gastrointestinal tract. Bioavailability: Approx 10% (conventional tab); 4% (cap); 73% (patch). Time to peak plasma concentration: 0.86 hours (cap); 10-15 minutes (orally disintegrating tab); 20 hours (transdermal patch). Distribution: Rapidly distributed throughout the body; crosses the blood-brain barrier. Plasma protein binding: 85-90%. Metabolism: Metabolised in the liver mainly by CYP2B6, CYP3A4, CYP2C9, and possibly CYP2A6 (minor) into active metabolites, N-desmethylselegiline, amphetamine, and methamphetamine, and inactive metabolites. Undergoes extensive first-pass metabolism (conventional tab or cap). Excretion: Mainly via urine (as metabolites); faeces (approx 15%). Elimination half-life: 10 hours (oral); 20 hours (transdermal).
Chemical Structure
Selegiline Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 26757, Selegiline. https://pubchem.ncbi.nlm.nih.gov/compound/Selegiline. Accessed Oct. 31, 2024.
Storage
Store between 20-25°C. Protect from light and moisture.
N04BD01 - selegiline ; Belongs to the class of dopaminergic agents, monoamine oxidase B inhibitors. Used in the management of Parkinson's disease.
References
Anon. Selegiline. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 30/08/2024.Brayfield A, Cadart C (eds). Selegiline Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/08/2024.Eldepryl 5 mg Tablets (Orion Corporation). MHRA. https://products.mhra.gov.uk. Accessed 30/08/2024.Emsam Patch (Mylan Specialty L.P.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 30/08/2024.Joint Formulary Committee. Selegiline Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/08/2024.Sefmex Tablet (Unison Laboratories Co Ltd). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 20/09/2024.Selegiline Hydrochloride Capsule (Rising Pharma Holdings, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 20/09/2024.Selegiline Hydrochloride Tablet (Golden State Medical Supply, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 30/08/2024.Selegiline. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 30/08/2024.Zelapar Tablet, Orally Disintegrating (Bausch Health US, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 30/08/2024.
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