Selegiline (Eldepryl) - Uses, Dose, Side effects, MOA, Brands

Selegiline (Eldepryl) belongs to the class of drugs called MAO inhibitors (Monoamine oxidase) that inhibits the degradation of dopamine, serotonin, and norepinephrine. It is used in the treatment of Parkinsons disease and depression.

Selegiline (Eldepryl) Uses:

  • Parkinson disease:

    • Supplemental care of Parkinson's disease patients on levodopa/carbidopa treatment who exhibit diminished response to this medication (oral products).

  • Major depressive disorder:

    • Treatment of major depressive disorder (MDD) in adults (transdermal patch)

  • Off Label Use of Selegiline in Adults:

    • Attention-deficit/hyperactivity disorder (ADHD);
    • Early Parkinson's disease

Selegiline (Eldepryl) Dose in Adults

Selegiline (Eldepryl) Dose in the treatment of Depression:

  • Transdermal: Starting dose: 6 mg/24 hours once per day; target dose: 6 mg/24 hours once per day; may titrate based on clinical response in increases of 3 mg/day every two weeks up to a maximum of 12 mg/24 hours

Selegiline (Eldepryl) Dose in the treatment of Parkinson disease:

  • Capsule, tablet:
    • For concomitant carbidopa/levodopa therapy, take 5 mg twice day with breakfast and lunch; the daily limit is 10 mg.
  • Orally disintegrating tablet:
    • The starting dose is 1.25 mg once day with concomitant carbidopa/levodopa therapy for at least 6 weeks; the dose may be increased to 2.5 mg once daily based on clinical response and tolerance (maximum: 2.5 mg/day).

  • Concomitant therapy with carbidopa/levodopa:

    • Try lowering the levodopa/carbidopa dosage by 10% to 30% after two to three days.
    • Levodopa/carbidopa dosage reductions may still be possible when using selegiline.

  • Discontinuation of therapy:

    • When discontinuing antidepressant treatment that has lasted for >3 weeks, gradually taper the dose (eg, over 2 to 4 weeks) to avoid withdrawal symptoms and detect recurring symptoms.
    • Reasons for a slower titration (eg, over 4 weeks) include use of a drug with a half-life <24 hours (eg, paroxetine, venlafaxine), previous history of antidepressant withdrawal symptoms, or high doses of antidepressants.
    • More severe symptoms have been associated with MAOIs; more conservative tapers may be needed.
    • If intolerable withdrawal symptoms occur, resume the previously prescribed dose and/or decrease dose at a slower rate.
    • Certain patients (eg, those with a history of discontinuation syndrome) on long-term treatment (>6 months) may be benefit from tapering over >3 months.
    • Evidence supporting ideal taper rates is limited.

MAO inhibitor recommendations:

  • Switching to or from an MAO inhibitor intended to treat psychiatric disorders:

    • The interval between stopping an alternative antidepressant (e.g., TCAs, paroxetine, fluvoxamine, venlafaxine) or MAO inhibitor intended to treat psychiatric illnesses and beginning selegiline should be 2 weeks (or a period equal to 4 to 5 half-lives of the drug).
    • Allow 5 weeks to pass between stopping the psychiatric disorder treatment fluoxetine (which has long-acting metabolites) and beginning selegiline.
    • To treat psychiatric illnesses, wait two weeks before stopping selegiline and beginning an alternative antidepressant or MAO inhibitor.

Selegiline (Eldepryl) Dose in Children

Selegiline (Eldepryl) Dose in the treatment of Depression:

  • Adolescents >17 years:

    • Transdermal: Refer to adult dosing.

    • Discontinuation of therapy:

      • Refer to adult dosing.

    • MAO inhibitor recommendations:

      • Refer to adult dosing.

Pregnancy Risk Factor C

  • Studies on animal reproduction have revealed certain negative impacts.
  • The use of selegiline during pregnancy to treat depression or Parkinson's disease is not well understood.

Use of selegiline during breastfeeding

  • Selegiline may secrete in breast milk, however this is uncertain.
  • The manufacturer doesn't recommend breastfeeding due to the possibility of serious side effects in infants breastfed.
  • Consider quitting all medications that are not essential for breastfeeding mothers.
  • Do not breastfeed if the selegiline patch has been stopped. Wait 5 days after the last dose.

Selegiline (Eldepryl) Dose in Kidney Disease:

  • Oral:

    • Capsules, tablets:
      • The manufacturer's labelling does not mention dosage modifications (has not been studied).
      • Use cautiously.

  • Orally disintegrating tablet:

    • CrCl 30 to 89 mL/minute:
      • No dosage adjustment needed.
    • CrCl <30 mL/minute:
      • Use is not recommended.
    • End-stage renal disease:
      • Use is not recommended.

  • Transdermal:

    • eGFR ≥15 mL/minute/1.73 m²:
      • No dosage adjustment needed.
    • eGFR <15 mL/minute/1.73 m²:
      • The manufacturer's labelling does not mention dosage modifications (has not been studied).
    • ESRD requiring dialysis:
      • The manufacturer's labelling does not mention dosage modifications (has not been studied).

Selegiline (Eldepryl) Dose in Liver disease:

  • Oral:

    • Capsules/tablets:
      • The manufacturer's labelling does not mention dosage modifications (has not been studied).

  • Orally disintegrating tablet:

    • Mild to moderate impairment (Child-Pugh class A and B):
      • 25 mg once daily
    • Severe impairment (Child-Pugh class C):
      • Use not recommended.

  • Transdermal:

    • Mild to moderate impairment (Child-Pugh class A and B):
      •  dose adjustment not needed 
    • Severe impairment (Child-Pugh class C):
      • The manufacturer's labelling does not mention dosage modifications (has not been studied).

Common Side Effects of Selegiline (Eldepryl):

  • Central Nervous System:

    • Headache
    • Dizziness
    • Insomnia

  • Gastrointestinal:

    • Nausea

  • Local:

    • Application Site Reaction

Less Common Side Effects of Selegiline (Eldepryl):

  • Cardiovascular:

    • Hypotension
    • Hypertension
    • Chest Pain
    • Palpitations
    • Peripheral Edema

  • Central Nervous System:

    • Pain
    • Confusion
    • Hallucination
    • Vivid Dream
    • Ataxia
    • Drowsiness
    • Depression
    • Lethargy
    • Abnormality In Thinking
    • Agitation
    • Amnesia
    • Paresthesia

  • Dermatologic:

    • Skin Rash
    • Acne Vulgaris
    • Diaphoresis
    • Pruritus

  • Endocrine & Metabolic:

    • Weight Loss
    • Hypokalemia

  • Gastrointestinal:

    • Diarrhea
    • Xerostomia
    • Abdominal Pain
    • Dyspepsia
    • Stomatitis
    • Constipation
    • Vomiting
    • Dental Caries
    • Dysgeusia
    • Dysphagia
    • Flatulence
    • Anorexia
    • Gastroenteritis

  • Genitourinary:

    • Urinary Retention
    • Dysmenorrhea
    • Sexual Disorder
    • Urinary Frequency
    • Urinary Tract Infection
    • Uterine Hemorrhage

  • Hematologic & Oncologic:

    • Bruise

  • Neuromuscular & Skeletal:

    • Dyskinesia
    • Back Pain
    • Leg Cramps
    • Myalgia
    • Tremor
    • Neck Pain

  • Otic:

    • Tinnitus

  • Respiratory:

    • Rhinitis
    • Pharyngitis
    • Dyspnea
    • Sinusitis
    • Bronchitis
    • Cough

Rare Side effects of Selegiline (Eldepryl):

  • Cardiovascular:

    • Atrial Fibrillation
    • Bradycardia
    • Cardiac Arrhythmia
    • Facial Edema
    • Myocardial Infarction
    • Peripheral Vascular Disease
    • Syncope
    • Tachycardia
    • Vasodilation

  • Central Nervous System:

    • Altered Sense Of Smell
    • Behavioral Changes
    • Chorea
    • Delusions
    • Depersonalization
    • Emotional Lability
    • Euphoria
    • Heatstroke
    • Hostility
    • Hyperesthesia
    • Hypertonia
    • Impulse Control Disorder (Including Binge Eating, Hypersexuality, Pathological Gambling)
    • Loss Of Balance
    • Mania
    • Migraine
    • Mood Changes
    • Myasthenia
    • Myoclonus
    • Oral Paresthesia
    • Paranoia
    • Psychoneurosis
    • Twitching
    • Vertigo

  • Dermatologic:

    • Maculopapular Rash
    • Skin Hypertrophy
    • Urticaria
    • Vesiculobullous Dermatitis

  • Endocrine & Metabolic:

    • Dehydration
    • Hypercholesterolemia
    • Hyperglycemia
    • Hypoglycemia
    • Hyponatremia
    • Increased Lactate Dehydrogenase
    • Increased Libido

  • Gastrointestinal:

    • Colitis
    • Eructation
    • Gastritis
    • Glossitis
    • Increased Appetite
    • Melena
    • Periodontal Abscess
    • Sialorrhea

  • Genitourinary:

    • Benign Prostatic Hypertrophy
    • Hematuria (Females)
    • Hernia
    • Mastalgia
    • Pelvic Pain
    • Urinary Urgency
    • Urination Disorder (Males; Impairment)
    • Vaginal Hemorrhage
    • Vaginitis
    • Vulvovaginal Candidiasis

  • Hematologic & Oncologic:

    • Benign Skin Neoplasm
    • Breast Neoplasm (Female)
    • Leukocytosis
    • Leukopenia
    • Lymphadenopathy
    • Neoplasm
    • Rectal Hemorrhage

  • Hepatic:

    • Abnormal Hepatic Function Tests
    • Hyperbilirubinemia
    • Increased Serum Alkaline Phosphatase

  • Hypersensitivity:

    • Tongue Edema

  • Infection:

    • Bacterial Infection
    • Candidiasis
    • Fungal Infection
    • Parasitic Infection
    • Viral Infection

  • Neuromuscular & Skeletal:

    • Bradykinesia
    • Hyperkinesia
    • Muscle Spasm (Generalized)
    • Osteoporosis
    • Tenosynovitis

  • Ophthalmic:

    • Visual Field Defect

  • Otic:

    • Otitis Externa

  • Renal:

    • Nephrolithiasis (Females)
    • Polyuria (Females)

  • Respiratory:

    • Asthma
    • Epistaxis
    • Laryngismus
    • Pneumonia

  • Miscellaneous:

    • Fever

Contraindications to Selegiline (Eldepryl):

  • Hypersensitivity to selegiline and any component of the formulation
  • Concomitant meperidine use

Orally disintegrating tablets

  • Usage of tramadol, propoxyphene, or other MAO inhibitors (selective or non-selective) concurrently within 14 days of selegiline.
  • concurrent usage with dextromethorphan, cyclobenzaprine, or St. John's wort

Transdermal: Additional contraindications

  • Pheochromocytoma
  • Patients under 12 years old;
  • Use of clomipramine, imipramine, and SSRI/SNRI/SSB serotonin reuptake inhibitors (concurrently, within two weeks of selegiline discontinuation or selegiline usage within 4 to five half-lives [approximately one week for most medications; 5 for fluoxetine] after stopping the contraindicated medication)

Canadian labeling: Additional contraindications not in US labeling

  • Psychosis severe;
  • severe dementia
  • Active peptic ulcer
  • extrapyramidal conditions

Warnings and precautions

  • Blood pressure effects

    • Oral medications may exacerbate hypertension.
    • Orthostatic hypotension may also be caused by this medication.
    • Patients at high risk or those with hypovolemia (cerebrovascular disease or cardiovascular disease), or who are taking concurrent medications that could lead to hypotension/bradycardia should be cautious.
    • In older adults, orthostatic hypotension might worsen, especially when the dose is titrated.
    • After using selegiline, patients should be watched for hypotension, newly developing hypertension, or uncontrolled hypertension.

  • Depression in the CNS:

    • CNS depression can lead to mental or physical impairments.
    • Patients should be cautious about driving or operating machinery that requires mental alertness.
    • The orally disintegrating tablet has been associated with somnolence and falling asleep while performing daily activities (including driving a motor vehicle); some people reported that they did not notice any warning signs.
    • Some symptoms may appear as soon as treatment begins; others can occur up to one year after treatment has ended.
    • Consider factors such as the presence of sleep disorders or concurrent sedating medication before you start treatment.
    • Pay attention to signs of sleepiness and drowsiness.
    • Stop taking selegiline if you experience significant sleepiness during the day or episodes of falling asleep while engaging in activities such as driving, talking, eating, etc.
    • These symptoms can be resolved by dose reductions, but there is not enough data.
    • Continue therapy and counsel patients against driving or participating in other risky activities.

  • Dyskinesia

    • Oral formulations may cause dyskinesia by increasing the dopaminergic side effect of levodopa.

  • Disorders of impulse control:

    • Dopaminergic medications used to treat Parkinson's disease have been associated to compulsive behaviours or loss of impulse control. Pathological gambling, hypersexuality, heightened libido, impulsive spending of money, binge eating, and/or other strong cravings can all be signs of this.
    • It is not clear if this phenomenon is caused by an underlying disease or previous addictions. There is also some debate about whether it is related to drug therapy.
    • These behaviors can be reversed by discontinuing therapy or reducing dosages in certain cases, but not all.

  • Melanoma

    • Patients with Parkinson's disease are at higher risk of developing melanoma. However, it is not known if there is a drug cause or other factors that contribute to the increased risk.
    • Patients must be watched closely and should examine their skin regularly.

  • Psychosis

    • Orally disintegrating tablets can cause mental changes and behavior that may be serious. This includes hallucinations, psychotic-like behavior, and increased doses.
    • Paranoid ideation, hallucinations and confusion may be present.
    • Patients with major psychotic disorders should not use this medication.

  • Serotonin syndrome

    • Potentially life-threatening serotonin disorder (SS) has been linked to concurrent use of serotonergic drugs (e.g. SSRIs and SNRIs), triptans or TCAs.
    • Watch out for signs and symptoms of SS in patients, such as mental changes (eg. agitation, hallucinations or coma); autonomic stability (eg. tachycardias, labile pressure, diaphoresis); neuromuscular disorders (eg. tremors, rigidity, myoclonus); GI symptoms like nausea, vomiting, diarrhea; and/or seizures.
    • If you notice any signs or symptoms, stop taking serotonergic agents and all concomitant treatment.

  • Hepatic impairment

    • Patients with severe hepatic impairment should be cautious. Dosage adjustments may be necessary for patients taking orally disintegrating tablets (Child–Pugh classes A and B).

  • Hypomania and mania:

    • Transdermal patches can make bipolar illness patients experience mania or hypomania.
    • Monotherapy is not appropriate for the treatment of bipolar disorder patients.
    • Bipolar disorder testing should be performed on patients who have depressed symptoms. This covers family history, bipolar disorder, depression, and depression in the family.
    • The FDA has not approved selegiline for the treatment of bipolar disorder.

  • Renal impairment

    • When utilising oral products, patients with kidney impairment should exercise caution. Patients with severe renal impairment (CrCl 30 mL/min) should not take orally disintegrating pills.

Selegiline: Drug Interaction

Risk Factor C (Monitor therapy)

Alfuzosin

May enhance the hypotensive effect of Blood Pressure Lowering Agents.

Altretamine

May enhance the orthostatic hypotensive effect of Monoamine Oxidase Inhibitors.

Amifampridine

Agents With Seizure Threshold Lowering Potential may enhance the neuroexcitatory and/or seizure-potentiating effect of Amifampridine.

Antiemetics (5HT3 Antagonists)

Could make serotonin modulators' serotonergic effects stronger. Serotonin syndrome might occur from this.

Antipsychotic Agents

Serotonin modulators might make antipsychotic drugs more harmful or toxic. Serotonin modulators, in particular, may enhance dopamine blockade, potentially raising the risk for neuroleptic malignant syndrome. Serotonin modulators' serotonergic effects may be strengthened by antipsychotic drugs. Serotonin syndrome might occur from this.

Antipsychotic Agents (Second Generation [Atypical])

Antipsychotic drugs' hypotensive effects may be enhanced by blood pressure-lowering medications (Second Generation [Atypical]).

Barbiturates

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Benperidol

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Beta2-Agonists

Beta2Agonists may have a more negative or toxic effect when combined with monoamine oxidase inhibitors.

Betahistine

The serum concentration of betahistine may rise in response to monoamine oxidase inhibitors.

Blood Glucose Lowering Agents

Blood Glucose Lowering Agents' hypoglycemic effects may be strengthened by monoamine oxidase inhibitors.

Blood Pressure Lowering Agents

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Brexanolone

Brexanolone's CNS depressive impact may be strengthened by selegiline.

Brimonidine (Ophthalmic)

Monoamine Oxidase Inhibitors might make brimonidine more harmful or poisonous (Ophthalmic). Brimonidine serum levels may rise in response to monoamine oxidase inhibitors (Ophthalmic).

Brimonidine (Topical)

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Brimonidine (Topical)

Monoamine Oxidase Inhibitors might make brimonidine more harmful or poisonous (Topical). Brimonidine serum levels may rise in response to monoamine oxidase inhibitors (Topical).

Cerebrolysin

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Chlorphenesin Carbamate

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Codeine

Monoamine Oxidase Inhibitors might make codeine more harmful or poisonous.

CYP2B6 Inducers (Moderate)

May decrease the serum concentration of CYP2B6 Substrates (High risk with Inducers).

Dabrafenib

May decrease the serum concentration of CYP2B6 Substrates (High risk with Inducers).

Diazoxide

May enhance the hypotensive effect of Blood Pressure Lowering Agents.

Dihydrocodeine

The serotonergic effects of monoamine oxidase inhibitors may be enhanced. Serotonin syndrome might occur from this.

Domperidone

Monoamine Oxidase Inhibitors may intensify Domperidone's negative/toxic effects. Monoamine Oxidase Inhibitors may lessen Domperidone's therapeutic efficacy. Monoamine Oxidase Inhibitors' therapeutic effects may be lessened by dolperidone.

Doxapram

Doxapram's hypertensive effect may be strengthened by monoamine oxidase inhibitors.

EPINEPHrine (Nasal)

Epinephrine's ability to increase blood pressure may be enhanced by monoamine oxidase inhibitors (Nasal).

Epinephrine (Racemic)

Epinephrine's ability to increase blood pressure may be enhanced by monoamine oxidase inhibitors (Racemic)

EPINEPHrine (Systemic)

Epinephrine's ability to increase blood pressure may be enhanced by monoamine oxidase inhibitors (Systemic).

Esketamine

The hypertensive effects of monoamine oxidase inhibitors might be enhanced.

Estrogen Derivatives (Contraceptive)

Selegiline serum levels might rise.

Herbs (Hypotensive Properties)

May enhance the hypotensive effect of Blood Pressure Lowering Agents.

Hypotension-Associated Agents

Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents.

Ioflupane I 123

Ioflupane I 123's diagnostic effectiveness may be reduced by selegiline.

Lormetazepam

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Lumacaftor

May lower the serum level of CYP2B6 substrates (High risk with Inducers).

Metaraminol

Metaraminol's hypertensive effect may be strengthened by monoamine oxidase inhibitors.

Metaxalone

Could make serotonin modulators' serotonergic effects stronger. Serotonin syndrome might occur from this.

Metoclopramide

Serotonin modulators may intensify Metoclopramide's harmful or hazardous effects. These could appear as signs of neuroleptic malignant syndrome or serotonin syndrome.

MiFEPRIStone

May elevate CYP2B6 substrates' serum levels (High risk with Inhibitors).

Molsidomine

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Naftopidil

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Nicergoline

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Nicorandil

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Nitroprusside

Nitroprusside's hypotensive impact may be strengthened by blood pressure-lowering medications

Norepinephrine

Monoamine Oxidase Inhibitors may increase Norepinephrine's ability to raise blood pressure.

Opioid Agonists

May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.

Pentoxifylline

May enhance the hypotensive effect of Blood Pressure Lowering Agents.

Phosphodiesterase 5 Inhibitors

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Pipamperone [INT]

May reduce the therapeutic impact of Parkinson's drugs (Monoamine Oxidase Inhibitor). Pipamperone [INTtherapeutic ]'s impact may be reduced by anti-Parkinson drugs (monoamine oxidase inhibitors).

Progestins (Contraceptive)

Selegiline serum levels might rise.

Prostacyclin Analogues

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Quinagolide

The hypotensive effects of blood pressure-lowering medications may be strengthened.

Thiotepa

May elevate CYP2B6 substrates' serum levels (High risk with Inhibitors).

Risk Factor D (Consider therapy modification)

Amifostine

Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, blood pressure lowering medications should be withheld for 24 hours prior to amifostine administration. If blood pressure lowering therapy cannot be withheld, amifostine should not be administered.

Benzhydrocodone

The serotonergic effects of monoamine oxidase inhibitors may be enhanced. Serotonin syndrome might occur from this. Treatment: Patients on monoamine oxidase inhibitors (MAOIs) or those who have stopped taking MAOIs within 14 days shouldn't use benzhydrocodone.

COMT Inhibitors

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

DOPamine

DOPamine's ability to increase blood pressure may be enhanced by monoamine oxidase inhibitors. Treatment: Patients who are taking (or have recently taken) monoamine oxidase inhibitors should start dopamine at no more than one-tenth (1/10) of the typical dose. Keep an eye out for a heightened hypertensive reaction to dopamine.

HYDROcodone

Monoamine Oxidase Inhibitors may intensify Hydrocodone's harmful or hazardous effects. Management: When possible, look into alternatives to this pairing.

Iohexol

The negative/toxic effects of iohexol may be amplified by substances with the potential to lower seizure thresholds. More specifically, there may be a higher chance of seizures. Treatment: Stop using medications 48 hours before using intrathecal iohexol that could lower the seizure threshold. To restart using such agents, give the treatment at least 24 hours. Prophylactic anticonvulsants may be used in nonelective surgeries.

Iomeprol

The negative/toxic effect of Iomeprol may be increased by substances with the potential to lower seizure thresholds. More specifically, there may be a higher chance of seizures. Treatment: Stop using medications 48 hours before using intrathecal iomeprol if they could lower the seizure threshold. To restart using such agents, give the treatment at least 24 hours. Prophylactic anticonvulsants may be used in nonelective surgeries.

Iopamidol

Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iopamidol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iopamidol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic anticonvulsants.

Levodopa-Containing Products

The negative or hazardous effects of monoamine oxidase inhibitors can be increased. The emergence of hypertensive responses when levodopa is combined with nonselective MAOI is of special concern. Treatment: It is not advised to take levodopa and nonselective MAO inhibitors (MAOIs) together. Levodopa should be started at least two weeks after stopping the nonselective MAOI. Observe patients who are on levodopa with a selective MAOI.

Lithium

Monoamine Oxidase Inhibitors might make lithium's harmful/toxic effects worse. Management: Use extreme caution when using this combo. When combination treatment is therapeutically necessary, keep a vigilant eye out for any symptoms of serotonin syndrome or toxicity.

Obinutuzumab

The hypotensive effects of blood pressure-lowering medications may be strengthened. Management: Take into account temporarily stopping blood pressure-lowering drugs starting 12 hours before the start of the obinutuzumab infusion and lasting until 1 hour after it.

OxyCODONE

The serotonergic effects of monoamine oxidase inhibitors may be enhanced. Serotonin syndrome might occur from this. Management: When possible, look for alternatives. Use of oxycodone/naltrexone should be avoided during and for 14 days following monoamine oxidase inhibitor therapy. Certain oxycodone products' non-US labels suggest that such use is not advised.

Pindolol

Pindolol's hypotensive impact may be strengthened by monoamine oxidase inhibitors. Management: Pindolol's Canadian labelling warns against using a monoamine oxidase inhibitor at the same time.

Reserpine

Monoamine Oxidase Inhibitors may intensify Reserpine's harmful or hazardous effects. Adding reserpine to current MAOI medication may have paradoxical effects (e.g., excitation, hypertension). Treatment: When a patient is concurrently getting reserpine, monoamine oxidase inhibitors (MAOIs) should be avoided or used very cautiously.

Serotonin Modulators

The serotonergic impact of serotonin modulators may be enhanced by anti-Parkinson drugs (monoamine oxidase inhibitors). Serotonin syndrome might occur from this. If selegiline, rasagiline, or safinamide is taken with a serotonin modulator, keep an eye out for any signs and symptoms of serotonin syndrome or serotonin poisoning. It is not advised to use transdermal selegiline with serotonin modulators. The exception is nigroline.

Risk Factor X (Avoid combination)

Alcohol (Ethyl)

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Alpha-/Beta-Agonists (Indirect-Acting)

Alpha-/Beta-Agonists may have a stronger hypertensive effect when combined with monoamine oxidase inhibitors (Indirect-Acting). Although this is the expected mode of action for linezolid, management guidelines are different from those for other monoamine oxidase inhibitors. Details can be found in linezolid-specific monographs.

Alpha1-Agonists

Alpha1Agonists may have a stronger hypertensive effect when combined with monoamine oxidase inhibitors. Although this is the expected mode of action for linezolid, management guidelines are different from those for other monoamine oxidase inhibitors. Details can be found in linezolid-specific monographs.

Amphetamines

Amphetamines' tendency to cause hypertension may be increased by monoamine oxidase inhibitors. However, unlike other monoamine oxidase inhibitors, linezolid and tedizolid have different management recommendations. For more information, consult the monographs for those agents.

Apraclonidine

Monoamine Oxidase Inhibitors might make acrolonidine more harmful or poisonous. The concentration of araclonidine in the serum may rise after using monoamine oxidase inhibitors.

AtoMOXetine

Monoamine Oxidase Inhibitors may intensify AtoMOXetine's neurotoxic (central) impact.

Atropine (Ophthalmic)

Atropine's ability to increase blood pressure may be enhanced by monoamine oxidase inhibitors (Ophthalmic).

Bezafibrate

Monoamine Oxidase Inhibitors may intensify Bezafibrate's harmful or hazardous effects.

Bromperidol

The hypotensive impact of bromperidol may be enhanced by blood pressure lowering medications. Blood Pressure Lowering Drugs' hypotensive effects may be lessened by bromperidol.

Buprenorphine

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

BuPROPion

BuPROPion's ability to raise blood pressure may be enhanced by monoamine oxidase inhibitors.

BusPIRone

The negative or hazardous effects of monoamine oxidase inhibitors can be increased. Increases in blood pressure have specifically been recorded.

CarBAMazepine

The negative or hazardous effects of monoamine oxidase inhibitors can be increased. Management: Avoid from using carbamazepine concurrently with monoamine oxidase inhibitor therapy or within 14 days of stopping it.

Cyclobenzaprine

The serotonergic effects of monoamine oxidase inhibitors may be enhanced. Serotonin syndrome might occur from this.

Cyproheptadine

Monoamine oxidase inhibitors may boost Cyproheptadine's anticholinergic effects. The serotonergic impact of monoamine oxidase inhibitors may be lessened by cyproheptadine.

Dapoxetine

Serotonin modulators' harmful or toxic effects could be exacerbated.

Deutetrabenazine

Monoamine Oxidase Inhibitors may make deutetrabenazine's harmful or hazardous effects worse.

Dexmethylphenidate

Dexmethylphenidate may have a stronger hypertensive effect when used with monoamine oxidase inhibitors.

Dextromethorphan

Monoamine oxidase inhibitors might improve dextromethorphan's serotonergic effects. It might result in serotonin syndrome.

Diethylpropion

Diethylpropion may have a stronger hypertensive effect when used with monoamine oxidase inhibitors.

Diphenoxylate

The hypertensive effects of monoamine oxidase inhibitors might be enhanced.

EPINEPHrine (Oral Inhalation)

Epinephrine's ability to increase blood pressure may be enhanced by monoamine oxidase inhibitors (Oral Inhalation).

FentaNYL

The serotonergic effects of monoamine oxidase inhibitors may be enhanced. Serotonin syndrome might occur from this.

Guanethidine

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Heroin

Monoamine Oxidase Inhibitors might make heroin more harmful or poisonous.

HYDROmorphone

Monoamine Oxidase Inhibitors may intensify HYDROmorphone's harmful or hazardous effects.

Indoramin

Indoramin's hypotensive impact may be strengthened by monoamine oxidase inhibitors.

Iobenguane Radiopharmaceutical Products

Iobenguane radiopharmaceutical products' therapeutic effects may be reduced by monoamine oxidase inhibitors. Treatment: Before administering iobenguane, stop taking any medications that could impede or interfere with catecholamine transport or uptake for at least five biological half-lives. After each dose of iobenguane, wait at least 7 days before administering these medications.

Isometheptene

Monoamine Oxidase Inhibitors might make isotheptene more harmful or poisonous.

Levomethadone

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Levonordefrin

Levonordefrin's ability to increase blood pressure may be enhanced by monoamine oxidase inhibitors.

Linezolid

Monoamine Oxidase Inhibitors may intensify Linezolid's negative/toxic effects.

Maprotiline

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Meperidine

Meperidine's serotonergic action may be enhanced by monoamine oxidase inhibitors. It might result in serotonin syndrome.

Meptazinol

Monoamine Oxidase Inhibitors may intensify Meptazinol's harmful or hazardous effects.

Mequitazine

Mequitazine's anticholinergic effects may be enhanced by monoamine oxidase inhibitors.

Methyldopa

Monoamine Oxidase Inhibitors may intensify Methyldopa's harmful or hazardous effects.

Methylene Blue

Methylene Blue may have a stronger serotonergic impact when taken with monoamine oxidase inhibitors. Serotonin syndrome might occur from this.

Methylene Blue

Could make serotonin modulators' serotonergic effects stronger. Serotonin syndrome might occur from this.

Methylphenidate

Methylphenidate's ability to raise blood pressure may be enhanced by monoamine oxidase inhibitors.

Mianserin

The neurotoxic effect of Mianserin may be increased by monoamine oxidase inhibitors.

Mirtazapine

Monoamine Oxidase Inhibitors may intensify Mirtazapine's neurotoxic (central) impact. While interactions between methylene blue and linezolid are anticipated, their usage is not advised in the same way as other monoamine oxidase inhibitors. For more information, consult the monographs for those agents.

Moclobemide

Monoamine Oxidase Inhibitors may intensify Moclobemide's harmful or hazardous effects.

Monoamine Oxidase Inhibitors

Certain monoamine oxidase inhibitors have the potential to increase their hypertensive effects. Other monoamine oxidase inhibitors' serotonergic effects may be enhanced by monoamine oxidase inhibitors. Serotonin syndrome might occur from this.

Morphine (Systemic)

Monoamine Oxidase Inhibitors might make morphine more harmful or poisonous (Systemic).

Nefopam

Monoamine Oxidase Inhibitors may intensify Nefopam's harmful or hazardous effects.

Opium

Monoamine Oxidase Inhibitors might make opium more harmful or poisonous.

Oxcarbazepine

Selegiline's serotonergic effects should be improved.

OxyMORphone

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Pheniramine

Monoamine oxidase inhibitors' anticholinergic effects might be strengthened.

Pholcodine

The serotonergic effects of monoamine oxidase inhibitors may be enhanced. Serotonin syndrome might occur from this.

Pizotifen

Monoamine Oxidase Inhibitors may strengthen Pizotifen's anticholinergic effects.

Reboxetine

Monoamine Oxidase Inhibitors may intensify Reboxetine's harmful or hazardous effects.

Selective Serotonin Reuptake Inhibitors

Selective Serotonin Reuptake Inhibitors' serotonergic effects may be enhanced by monoamine oxidase inhibitors. It might result in serotonin syndrome. Although this interaction between methylene blue and linezolid is anticipated, management guidelines for this drug are different from those for other monoamine oxidase inhibitors. For more information, consult the monographs for those agents.

Serotonin 5-HT1D Receptor Agonists

Serotonin 5-HT1D Receptor Agonists' metabolism may be slowed down by monoamine oxidase inhibitors. Management: Naratriptan, eletriptan, or frovatriptan may be suitable 5-HT1D agonists to use if MAO inhibitor medication is necessary. Eletriptan, Frovatriptan, and Naratriptan are exceptions.

Serotonin Reuptake Inhibitor/Antagonists

Serotonin Reuptake Inhibitor/Antagonists' harmful or toxic effects may be increased by monoamine oxidase inhibitors. While interactions between methylene blue and linezolid are anticipated, their usage is not advised in the same way as other monoamine oxidase inhibitors. For more information, consult the monographs for those agents.

Serotonin/Norepinephrine Reuptake Inhibitors

Serotonin/Norepinephrine Reuptake Inhibitors' serotonergic effects may be enhanced by monoamine oxidase inhibitors. It might result in serotonin syndrome. Although this interaction between methylene blue and linezolid is anticipated, management guidelines for this drug are different from those for other monoamine oxidase inhibitors. For more information, consult the monographs for those agents.

Solriamfetol

Solriamfetol's ability to raise blood pressure may be enhanced by monoamine oxidase inhibitors.

SUFentanil

The negative or hazardous effects of monoamine oxidase inhibitors can be increased. Particularly, there may be an elevated risk for serotonin syndrome or opioid toxicities (such as respiratory depression or coma). Management: Due to the risk of serotonin syndrome and/or severe CNS depression, fentanyl should not be administered in conjunction with monoamine oxidase (MAO) inhibitors (or within 14 days of discontinuing an MAO inhibitor).

Tapentadol

The negative or hazardous effects of monoamine oxidase inhibitors can be increased. In particular, norepinephrine's cumulative actions could have harmful cardiovascular repercussions. The serotonergic action of monoamine oxidase inhibitors may be enhanced by tapentadol. Serotonin syndrome might occur from this.

Tetrabenazine

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Tetrahydrozoline (Nasal)

Monoamine Oxidase Inhibitors may increase Tetrahydrozoline's hypertensive impact (Nasal).

Tricyclic Antidepressants

Tricyclic antidepressants' serotonergic action may be strengthened by monoamine oxidase inhibitors. It might result in serotonin syndrome. Although this interaction between methylene blue and linezolid is anticipated, management guidelines for this drug are different from those for other monoamine oxidase inhibitors. For more information, consult the monographs for those agents.

Tryptophan

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Valbenazine

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Monitoring parameters:

  • Blood pressure
  • symptoms of parkinsonism
  • general mood and behavior 
  • suicidal ideation
  • periodic skin examinations
  • symptoms of serotonin syndrome (transdermal patch)

How to administer Selegiline (Eldepryl)?

  • Tablet that can be taken orally:

    • Before you use the tablet, take it out of the pouch.
    • Each morning, take one pill before breakfast. Avoid swallowing. Put it on the tongue, then let it to dissolve.
    • For five minutes before and after the administration, refrain from eating or drinking.

Topical: Transdermal

  • Apply to the upper trunk (below the waist and below the neck), upper thigh, or outer surface of the upper arm only clean, dry, and intact skin.
  • Avoid wearing tight clothes.
  • You can apply at the same moment every day, and you can also change your application site.
  • After handling, wash your hands with soapy water.
  • Avoid touching the sticky sides of the patch.
  • Fold the sticky ends of any used or unused patches together and throw them away.

Mechanism of action of Selegiline (Eldepryl):

  • It is an irreversible and potent inhibitor of monoamineoxidase (MAO).
  • Selegiline is drawn to MAO-B rather than MAO-A. (intestinal MAO tends to be type A, but in the brain both types of isoenzymes are present).
  • Serotonin and dopamine are catabolized in the Brain by the enzyme MAO.
  • At lower levels, selegiline selectively inhibits MAOB. Yet, as selegiline concentrations increase, MAOB selectivity declines.
  • Selegiline can alter the absorption of dopamine at synapses by increasing dopaminergic activity.
  • Its metabolites include methamphetamine (amphetamine) and methamphetamine (methamphetamine), which can also have neuronal effects and increase neurotransmitter release (eg, dopamine, serotonin).
  • It is not known how much these metabolites affect the effects of selegiline.
  • When oral dosage forms are taken in the recommended amounts, plasma concentrations are reached that selectively inhibit MAO type B.
  • In comparison to oral dosing, selegiline delivered transdermally has a higher blood level and a much lower exposure to all metabolites.
  • If selegiline is to be used in a manner that isn't restricted by diet or other drugs, it must be taken into consideration the dose dependence of its selectivity.

Absorption:

  • Taken with meals, capsules/tablets: Increases in bioavailability by 3- to 4-fold
  • Tablets that dissolve in the mouth quickly; more bioavailability than tablets and capsules. Fasting reduces C and AUC by 60%.
  • Transdermal: 25 to 30% of total selegiline in 24 hours

Protein binding:

  • 85% to 90%

Metabolism:

  • Hepatic, primarily via CYP2B6, CYP2C9, CYP3A4, and CYP2A6 (minor) to active (N-desmethylselegiline, amphetamine, methamphetamine) and inactive metabolites

Half-life elimination:

  • Oral: 10 hours

Excretion:

  • Urine (primarily metabolites);
  • feces

International Brand Names of Selegiline:

  • Eldepryl
  • Emsam
  • Zelapar
  • APO-Selegiline
  • DOM-Selegiline
  • MYLAN-Selegiline
  • PMS-Selegiline
  • TEVA Selegiline
  • Antiparkin
  • Apo-Selegiline
  • Brintenal
  • Cognitiv
  • Cognitive
  • Deprenyl
  • Eldepryl
  • Endopryl
  • FP-OD
  • Jin Si Ping
  • Julab
  • Jumex
  • Jumexal
  • Mao-B
  • MAOtil
  • Movergan
  • Niar
  • Parkilyne
  • Plurimen
  • Procythol
  • Sefmex
  • Segan
  • Seldepar
  • Selegil
  • Selegos
  • Selezin
  • Selgene
  • Selgin
  • Selgina
  • Siltin
  • Xilopar

Selegiline Brand Names in Pakistan:

Selegiline HCl Tablets 5 mg in Pakistan
Eklin Evron (Pvt) Ltd.
Juline Genome Pharmaceuticals (Pvt) Ltd
Jumalline Al-Habib Pharmaceuticals.
Jumex Sanofi Aventis (Pakistan) Ltd.
Selgin Glaxosmithkline
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