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:
- Adjunct in the management of patients with Parkinson disease being treated with levodopa/carbidopa who show decreased response to this therapy (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: Initial: 6 mg/24 hours once daily
- target dose: 6 mg/24 hours once daily; may titrate based on clinical response in increases of 3 mg/day every 2 weeks up to a maximum of 12 mg/24 hours
Selegiline (Eldepryl) Dose in the treatment of Parkinson disease:
- Capsule, tablet:
- 5 mg twice daily with breakfast and lunch with concurrent carbidopa/levodopa therapy;
- maximum: 10 mg/day.
- Orally disintegrating tablet:
- Initial: 1.25 mg once daily with concurrent carbidopa/levodopa therapy for at least 6 weeks;
- may increase the dose to 2.5 mg once daily based on clinical response and tolerance (maximum: 2.5 mg/day).
-
Concomitant therapy with carbidopa/levodopa:
- After 2 to 3 days, try reducing dose of levodopa/carbidopa by 10% to 30%.
- Further reductions of levodopa/carbidopa may be possible during continued selegiline therapy.
-
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:
- Allow 2 weeks (or a time equal to 4 to 5 half-lives of the drug) to pass between discontinuing an alternative antidepressant without long half-life metabolites (eg, TCAs, paroxetine, fluvoxamine, venlafaxine) or MAO inhibitor intended to treat psychiatric disorders and starting selegiline.
- Let 5 weeks to pass between discontinuing fluoxetine (with long half-life metabolites) intended to treat psychiatric disorders and starting selegiline.
- Let 2 weeks pass between discontinuing selegiline and starting an alternative antidepressant or MAO inhibitor for treatment of psychiatric disorders.
Selegiline (Eldepryl) Dose in Childrens
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
- Some animal reproduction studies have shown side effects.
- Limited information is available on the use of selegiline during pregnancy for treatment of Parkinson's disease or depression.
Use of selegiline during breastfeeding
- It is unknown if selegiline secretes in breast milk. Limited information is available on the use of selegiline by breastfeeding mothers.
- 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:
- There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).
- Use cautiously.
- Capsules, tablets:
-
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.
- CrCl 30 to 89 mL/minute:
-
Transdermal:
- eGFR ≥15 mL/minute/1.73 m²:
- No dosage adjustment needed.
- eGFR <15 mL/minute/1.73 m²:
- There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).
- ESRD requiring dialysis:
- There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).
- eGFR ≥15 mL/minute/1.73 m²:
Selegiline (Eldepryl) Dose in Liver disease:
-
Oral:
- Capsules/tablets:
- There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied). Use cautiously.
- Capsules/tablets:
-
Orally disintegrating tablet:
- Mild to moderate impairment (Child-Pugh class A and B):
- 25 mg once daily based on clinical response and tolerance.
- Severe impairment (Child-Pugh class C):
- Use not recommended.
- Mild to moderate impairment (Child-Pugh class A and B):
-
Transdermal:
- Mild to moderate impairment (Child-Pugh class A and B):
- No dose adjustment required.
- Severe impairment (Child-Pugh class C):
- There are no dose adjustments provided in the manufacturer’s labeling (has not been studied).
- Mild to moderate impairment (Child-Pugh class A and B):
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
- Use of methadone and other MAO inhibitors (selective/non-selective), propoxyphene or tramadol concurrently within 14 days after selegiline.
- Concurrent use with cyclobenzaprine or dextromethorphan or St John's Wort
Transdermal: Additional contraindications
- Pheochromocytoma
- Patients under 12 years old;
- Use of serotonin reuptake inhibitors (including SSRIs, SNRIs), clomipramine and imipramine (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, such as excessive tremor and tardive dyskinesia
Warnings and precautions
-
Blood pressure effects
- Oral formulations may cause hypertension to worsen.
- 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.
- Orthostatic hypotension can also increase in older adults, especially when the dose is titrated.
- Monitor patients for hypotension, new-onset hypertension, or uncontrolled hypertension after taking selegiline.
-
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 advise patients not to drive or engage in other dangerous activities.
-
Dyskinesia
- Oral formulations may cause dyskinesia by increasing the dopaminergic side effect of levodopa.
-
Disorders of impulse control:
- Compulsive behaviors or loss of impulse control have been linked to dopaminergic drugs used in Parkinson disease. This can manifest as pathological gambling, hypersexuality, increased libido, uncontrolled spending of cash, binge-eating, and/or other intense urges.
- 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 patch may cause mania or hypomania in bipolar disorder patients.
- Patients with bipolar disorder must not be treated in monotherapy.
- Patients suffering from depressive symptoms should be tested for bipolar disorder. This includes family history of suicide, bipolar disorder, depression, and family history.
- Selegiline has not been approved by the FDA for treatment of bipolar disorder.
-
Renal impairment
- Patients with kidney impairment should be cautious when using oral products. Orally disintegrating tablets should not be used in patients suffering from severe renal dysfunction (CrCl 30 mL/minute).
Selegiline: Drug Interaction
|
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) |
|
|
Antipsychotic Agents |
Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. |
|
Antipsychotic Agents (Second Generation [Atypical]) |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). |
|
Barbiturates |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Benperidol |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Beta2-Agonists |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Beta2Agonists. |
|
Betahistine |
Monoamine Oxidase Inhibitors may increase the serum concentration of Betahistine. |
|
Blood Glucose Lowering Agents |
Monoamine Oxidase Inhibitors may enhance the hypoglycemic effect of Blood Glucose Lowering Agents. |
|
Blood Pressure Lowering Agents |
May enhance the hypotensive effect of HypotensionAssociated Agents. |
|
Brexanolone |
Selegiline may enhance the CNS depressant effect of Brexanolone. |
|
Brimonidine (Ophthalmic) |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Brimonidine (Ophthalmic). Monoamine Oxidase Inhibitors may increase the serum concentration of Brimonidine (Ophthalmic). |
|
Brimonidine (Topical) |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Brimonidine (Topical). Monoamine Oxidase Inhibitors may increase the serum concentration of Brimonidine (Topical). |
|
Brimonidine (Topical) |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Cerebrolysin |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. |
|
Chlorphenesin Carbamate |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. |
|
Codeine |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Codeine. |
|
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 |
May enhance the serotonergic effect of Monoamine Oxidase Inhibitors. This could result in serotonin syndrome. |
|
Domperidone |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Domperidone. Monoamine Oxidase Inhibitors may diminish the therapeutic effect of Domperidone. Domperidone may diminish the therapeutic effect of Monoamine Oxidase Inhibitors. |
|
Doxapram |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of Doxapram. |
|
EPINEPHrine (Nasal) |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of EPINEPHrine (Nasal). |
|
Epinephrine (Racemic) |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of Epinephrine (Racemic). |
|
EPINEPHrine (Systemic) |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of EPINEPHrine (Systemic). |
|
Esketamine |
May enhance the hypertensive effect of Monoamine Oxidase Inhibitors. |
|
Estrogen Derivatives (Contraceptive) |
May increase the serum concentration of Selegiline. |
|
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 |
Selegiline may diminish the diagnostic effect of Ioflupane I 123. |
|
Lormetazepam |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Lumacaftor |
May decrease the serum concentration of CYP2B6 Substrates (High risk with Inducers). |
|
Metaraminol |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of Metaraminol. |
|
Metaxalone |
May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. |
|
Metoclopramide |
Serotonin Modulators may enhance the adverse/toxic effect of Metoclopramide. This may be manifest as symptoms consistent with serotonin syndrome or neuroleptic malignant syndrome. |
|
MiFEPRIStone |
May increase the serum concentration of CYP2B6 Substrates (High risk with Inhibitors). |
|
Molsidomine |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Naftopidil |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Nicergoline |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Nicorandil |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Nitroprusside |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. |
|
Norepinephrine |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of Norepinephrine. |
|
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 |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Pipamperone [INT] |
May diminish the therapeutic effect of Anti-Parkinson Agents (Monoamine Oxidase Inhibitor). Anti-Parkinson Agents (Monoamine Oxidase Inhibitor) may diminish the therapeutic effect of Pipamperone [INT]. |
|
Progestins (Contraceptive) |
May increase the serum concentration of Selegiline. |
|
Prostacyclin Analogues |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Quinagolide |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Thiotepa |
May increase the serum concentration of CYP2B6 Substrates (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 |
|
|
COMT Inhibitors |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. |
|
DOPamine |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of DOPamine. Management: Initiate dopamine at no greater than one-tenth (1/10) of the usual dose in patients who are taking (or have taken within the last 2 to 3 weeks) monoamine oxidase inhibitors. Monitor for an exaggerated hypertensive response to dopamine. |
|
HYDROcodone |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of HYDROcodone. Management: Consider alternatives to this combination when possible. |
|
Iohexol |
Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iohexol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iohexol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic anticonvulsants. |
|
Iomeprol |
Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iomeprol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iomeprol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic anticonvulsants. |
|
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 |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. Of particular concern is the development of hypertensive reactions when levodopa is used with nonselective MAOI. Management: The concomitant use of nonselective monoamine oxidase inhibitors (MAOIs) and levodopa is contraindicated. Discontinue the nonselective MAOI at least two weeks prior to initiating levodopa. Monitor patients taking a selective MAOIs and levodopa. |
|
Lithium |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Lithium. Management: This combination should be undertaken with great caution. When combined treatment is clinically indicated, monitor closely for signs of serotonin toxicity/serotonin syndrome. |
|
Obinutuzumab |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. |
|
OxyCODONE |
May enhance the serotonergic effect of Monoamine Oxidase Inhibitors. This could result in serotonin syndrome. Management: Seek alternatives when possible. Avoid use of oxycodone/naltrexone during and within 14 days after monoamine oxidase inhibitor treatment. Non-US labeling for some oxycodone products states that such use is contraindicated. |
|
Pindolol |
Monoamine Oxidase Inhibitors may enhance the hypotensive effect of Pindolol. Management: Canadian labeling for pindolol states that concurrent use with a monoamine oxidase inhibitor is not recommended. |
|
Reserpine |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Reserpine. Existing MAOI therapy can result in paradoxical effects of added reserpine (e.g., excitation, hypertension). Management: Monoamine oxidase inhibitors (MAOIs) should be avoided or used with great caution in patients who are also receiving reserpine. |
|
Serotonin Modulators |
Anti-Parkinson Agents (Monoamine Oxidase Inhibitor) may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity if selegiline, rasagiline, or safinamide is combined with a serotonin modulator. Use of transdermal selegiline with serotonin modulators is contraindicated. Exceptions: Nicergoline. |
|
Risk Factor X (Avoid combination) |
|
|
Alcohol (Ethyl) |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. |
|
Alpha-/Beta-Agonists (Indirect-Acting) |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of Alpha-/Beta-Agonists (Indirect-Acting). While linezolid is expected to interact via this mechanism, management recommendations differ from other monoamine oxidase inhibitors. Refer to linezolid specific monographs for details. |
|
Alpha1-Agonists |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of Alpha1Agonists. While linezolid is expected to interact via this mechanism, management recommendations differ from other monoamine oxidase inhibitors. Refer to linezolid specific monographs for details. |
|
Amphetamines |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of Amphetamines. While linezolid and tedizolid may interact via this mechanism, management recommendations differ from other monoamine oxidase inhibitors. Refer to monographs specific to those agents for details. |
|
Apraclonidine |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Apraclonidine. Monoamine Oxidase Inhibitors may increase the serum concentration of Apraclonidine. |
|
AtoMOXetine |
Monoamine Oxidase Inhibitors may enhance the neurotoxic (central) effect of AtoMOXetine. |
|
Atropine (Ophthalmic) |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of Atropine (Ophthalmic). |
|
Bezafibrate |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Bezafibrate. |
|
Bromperidol |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Bromperidol may diminish the hypotensive effect of Blood Pressure Lowering Agents. |
|
Buprenorphine |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. |
|
BuPROPion |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of BuPROPion. |
|
BusPIRone |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. Specifically, blood pressure elevations been reported. |
|
CarBAMazepine |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. Management: Avoid concurrent use of carbamazepine during, or within 14 days of discontinuing, treatment with a monoamine oxidase inhibitor. |
|
Cyclobenzaprine |
May enhance the serotonergic effect of Monoamine Oxidase Inhibitors. This could result in serotonin syndrome. |
|
Cyproheptadine |
Monoamine Oxidase Inhibitors may enhance the anticholinergic effect of Cyproheptadine. Cyproheptadine may diminish the serotonergic effect of Monoamine Oxidase Inhibitors. |
|
Dapoxetine |
May enhance the adverse/toxic effect of Serotonin Modulators. |
|
Deutetrabenazine |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Deutetrabenazine. |
|
Dexmethylphenidate |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of Dexmethylphenidate. |
|
Dextromethorphan |
Monoamine Oxidase Inhibitors may enhance the serotonergic effect of Dextromethorphan. This may cause serotonin syndrome. |
|
Diethylpropion |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of Diethylpropion. |
|
Diphenoxylate |
May enhance the hypertensive effect of Monoamine Oxidase Inhibitors. |
|
EPINEPHrine (Oral Inhalation) |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of EPINEPHrine (Oral Inhalation). |
|
FentaNYL |
May enhance the serotonergic effect of Monoamine Oxidase Inhibitors. This could result in serotonin syndrome. |
|
Guanethidine |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. |
|
Heroin |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Heroin. |
|
HYDROmorphone |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of HYDROmorphone. |
|
Indoramin |
Monoamine Oxidase Inhibitors may enhance the hypotensive effect of Indoramin. |
|
Iobenguane Radiopharmaceutical Products |
Monoamine Oxidase Inhibitors may diminish the therapeutic effect of Iobenguane Radiopharmaceutical Products. Management: Discontinue all drugs that may inhibit or interfere with catecholamine transport or uptake for at least 5 biological half-lives before iobenguane administration. Do not administer these drugs until at least 7 days after each iobenguane dose. |
|
Isometheptene |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Isometheptene. |
|
Levomethadone |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. |
|
Levonordefrin |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of Levonordefrin. |
|
Linezolid |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Linezolid. |
|
Maprotiline |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. |
|
Meperidine |
Monoamine Oxidase Inhibitors may enhance the serotonergic effect of Meperidine. This may cause serotonin syndrome. |
|
Meptazinol |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Meptazinol. |
|
Mequitazine |
Monoamine Oxidase Inhibitors may enhance the anticholinergic effect of Mequitazine. |
|
Methyldopa |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Methyldopa. |
|
Methylene Blue |
Monoamine Oxidase Inhibitors may enhance the serotonergic effect of Methylene Blue. This could result in serotonin syndrome. |
|
Methylene Blue |
May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. |
|
Methylphenidate |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of Methylphenidate. |
|
Mianserin |
Monoamine Oxidase Inhibitors may enhance the neurotoxic effect of Mianserin. |
|
Mirtazapine |
Monoamine Oxidase Inhibitors may enhance the neurotoxic (central) effect of Mirtazapine. While methylene blue and linezolid are expected to interact, specific recommendations for their use differ from other monoamine oxidase inhibitors. Refer to monographs specific to those agents for details. |
|
Moclobemide |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Moclobemide. |
|
Monoamine Oxidase Inhibitors |
May enhance the hypertensive effect of other Monoamine Oxidase Inhibitors. Monoamine Oxidase Inhibitors may enhance the serotonergic effect of other Monoamine Oxidase Inhibitors. This could result in serotonin syndrome. |
|
Morphine (Systemic) |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Morphine (Systemic). |
|
Nefopam |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Nefopam. |
|
Opium |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Opium. |
|
Oxcarbazepine |
May enhance the serotonergic effect of Selegiline. |
|
OxyMORphone |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. |
|
Pheniramine |
May enhance the anticholinergic effect of Monoamine Oxidase Inhibitors. |
|
Pholcodine |
May enhance the serotonergic effect of Monoamine Oxidase Inhibitors. This could result in serotonin syndrome. |
|
Pizotifen |
Monoamine Oxidase Inhibitors may enhance the anticholinergic effect of Pizotifen. |
|
Reboxetine |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Reboxetine. |
|
Selective Serotonin Reuptake Inhibitors |
Monoamine Oxidase Inhibitors may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. While methylene blue and linezolid are expected to interact via this mechanism, management recommendations differ from other monoamine oxidase inhibitors. Refer to monographs specific to those agents for details. |
|
Serotonin 5-HT1D Receptor Agonists |
Monoamine Oxidase Inhibitors may decrease the metabolism of Serotonin 5-HT1D Receptor Agonists. Management: If MAO inhibitor therapy is required, naratriptan, eletriptan or frovatriptan may be a suitable 5-HT1D agonist to employ. Exceptions: Eletriptan; Frovatriptan; Naratriptan. |
|
Serotonin Reuptake Inhibitor/Antagonists |
Monoamine Oxidase Inhibitors may enhance the adverse/toxic effect of Serotonin Reuptake Inhibitor/Antagonists. While methylene blue and linezolid are expected to interact, specific recommendations for their use differ from other monoamine oxidase inhibitors. Refer to monographs specific to those agents for details. |
|
Serotonin/Norepinephrine Reuptake Inhibitors |
Monoamine Oxidase Inhibitors may enhance the serotonergic effect of Serotonin/Norepinephrine Reuptake Inhibitors. This may cause serotonin syndrome. While methylene blue and linezolid are expected to interact via this mechanism, management recommendations differ from other monoamine oxidase inhibitors. Refer to monographs specific to those agents for details. |
|
Solriamfetol |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of Solriamfetol. |
|
SUFentanil |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. Specifically, the risk for serotonin syndrome or opioid toxicities (eg, respiratory depression, coma) may be increased. Management: Sufentanil should not be used with monoamine oxidase (MAO) inhibitors (or within 14 days of stopping an MAO inhibitor) due to the potential for serotonin syndrome and/or excessive CNS depression. |
|
Tapentadol |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. Specifically, the additive effects of norepinephrine may lead to adverse cardiovascular effects. Tapentadol may enhance the serotonergic effect of Monoamine Oxidase Inhibitors. This could result in serotonin syndrome. |
|
Tetrabenazine |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. |
|
Tetrahydrozoline (Nasal) |
Monoamine Oxidase Inhibitors may enhance the hypertensive effect of Tetrahydrozoline (Nasal). |
|
Tricyclic Antidepressants |
Monoamine Oxidase Inhibitors may enhance the serotonergic effect of Tricyclic Antidepressants. This may cause serotonin syndrome. While methylene blue and linezolid are expected to interact via this mechanism, management recommendations differ from other monoamine oxidase inhibitors. Refer to monographs specific to those agents for details. |
|
Tryptophan |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. |
|
Valbenazine |
May enhance the adverse/toxic effect of Monoamine Oxidase Inhibitors. |
Monitoring parameters:
- Blood pressure
- symptoms of parkinsonism
- general mood and behavior (increased anxiety, presence of mania or agitation)
- suicidal ideation (especially at the beginning of therapy or when doses are increased or decreased)
- 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.
- Take one tablet each morning, before breakfast. Do not swallow. Place on the tongue and let it dissolve.
- Avoid eating or drinking for 5 minutes prior to and after the administration.
Topical: Transdermal
- Clean, dry, and intact skin should be applied to the upper trunk (below the waist and below the neck), upper thigh or outer surface of upper arm.
- Apply to skin that is oily, hairy, irritated or scarred.
- 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.
- You can dispose of any unused or used patches by folding the adhesive ends together.
Mechanism of action of Selegiline (Eldepryl):
- It is an irreversible and potent inhibitor of monoamineoxidase (MAO).
- Selegiline is more attracted to MAO–B than MAO–A (intestinal MAO tends to be type A, but in the brain both types of isoenzymes are present).
- MAO is a key component of the CNS' catabolism of serotonin and dopamine.
- Selegiline is a selective inhibitor of MAOB at lower doses. However, MAOB selectivity decreases as selegiline concentrations rise.
- Selegiline can increase dopaminergic activity, interfering with dopamine uptake at the synapse.
- 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.
- Concentrations in plasma that are achieved by administration of oral dosage forms in the recommended doses confer selective inhibition on MAO type B.
- Transdermally administered selegiline has a higher blood level and significantly lower exposure to all metabolites than oral dosing.
- 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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