Селегилин

Quick links

Choose a section

Quick links to important sections

Advertisements

Селегилин

Advertisements
Advertisements

Treatment option: Parkinson Disease, Parkinsonism

Advertisements

Overview of Селегилин

1. Что такое Селегилин и к какому классу относится? (What is Selegiline and What Class Does it Belong To?)

Property Description
Active ingredient Selegiline hydrochloride
Form Oral tablet, capsule, ODT, transdermal patch
Pharmacological class Selective MAO-B Inhibitor
General purpose Enhances dopamine signaling in the brain
Origin Synthetic

Селегилин is a prescription medication whose active substance is Selegiline hydrochloride, a synthetically produced phenethylamine derivative, also known as L-deprenyl. This drug is officially classified as a Dopaminergic Antiparkinsonism Agent and belongs to the broader category of Monoamine Oxidase Inhibitors (MAOI), specifically serving as a highly selective, irreversible inhibitor of the enzyme Monoamine Oxidase B (MAO-B). The pharmacological profile indicates that Selegiline’s unique structure allows it to irreversibly block the MAO-B enzyme, which is a key process in the central nervous system. This selective characteristic is a differentiating factor from older, less selective MAOI agents.

2. Формы выпуска и общее назначение препарата (Dosage Forms and General Purpose of the Drug)

The medication is available for both oral and transdermal administration, offering distinct options for delivering the active substance, Selegiline. Oral forms include the standard tablet, the capsule, and the orally disintegrating tablet (ODT), all relying on pharmaceutical excipients for absorption. The transdermal system (patch) is a notable form, utilizing an adhesive matrix to deliver the drug through the skin. Pharmacological characteristics support enhanced dopaminergic neurotransmission. This capability makes it generally useful for managing conditions where the body requires additional support to increase and preserve dopamine levels in the brain.

Regulatory References

  1. MedlinePlus
  2. NIH
Advertisements

What side effects are possible with Селегилин?

Possible Side Effects and Safety Information

The safety profile for Selegiline, as documented in official government regulatory sources, defines adverse reactions based on their frequency of occurrence and the physiological system affected. The most common effects generally involve the gastrointestinal and nervous systems.

Officially Documented Adverse Reactions

Frequency Classification Examples of Effects (System-Organ Class)
Very Common (ge 1/10) Nausea, Insomnia, Fatigue, Stomatitis (mouth sores, primarily with ODT)
Common (ge 1/100 to <1/10) Dizziness, Headache, Orthostatic Hypotension, Confusion, Hallucinations, Dyskinesia, Depression, Constipation, Dry Mouth

Serious Adverse Reactions and Safety Constraints

Regulatory documentation highlights several potentially serious adverse reactions, often linked to high doses or specific drug combinations. These include Serotonin Syndrome, a severe condition reported when Selegiline is co-administered with certain antidepressants or opioids, and Hypertensive Crisis, particularly when oral doses exceed the selective range. Other reported serious effects involve the development of Impulse Control/Compulsive Behaviors and instances of suddenly Falling Asleep During Activities of Daily Living.

Safety notes specify that effects like dizziness and low blood pressure (Orthostatic Hypotension) may be more common when treatment is first initiated. Specific populations require caution: the use of some formulations is not recommended in patients with severe renal or hepatic impairment.

Advertisements

Overdose and Emergency Response

The official documentation describes overdosage with Selegiline as potentially resulting in severe neurological and cardiovascular manifestations. Documented presentations include signs of CNS hyperactivity such as agitation, severe dizziness, drowsiness, confusion, hallucinations, and generalized convulsions (seizures). Effects on the autonomic and cardiovascular systems can involve a fast or irregular pulse, high or low blood pressure, and muscular rigidity, including a stiff neck and jaw tightness.

Regulatory information confirms that severe or life-threatening outcomes can occur, notably Serotonin Syndrome and Hypertensive Crisis, which carry the risk of leading to coma or death. These severe outcomes are a particular risk at high doses where the drug's selectivity is lost.

In any situation where an overdose is suspected, or if severe symptoms such as a severe headache, chest pain, or troubled breathing are present, regulatory guidance mandates that patients must seek immediate medical attention or contact emergency services immediately. The official treatment approach for overdosage is entirely symptomatic and supportive, as no specific antidote is known. Close observation in a hospital setting may be required due to the potential for delayed onset of severe MAOI toxicity.

Advertisements

Therapeutic Uses of Селегилин

What Селегилин Treats: Main Uses and Benefits

Селегилин is commonly used to help manage symptoms associated with certain neurological and mood disorders. Its primary therapeutic role is applied across domains where additional symptomatic support is needed in Parkinson's disease, and it is also relevant in treating Major Depressive Disorder.

The drug is generally used for managing movement difficulties like stiffness, slowness of movement, and tremor, and for providing supportive relief for mood symptoms. In Parkinson's, it is applied as an adjunct treatment to help manage motor fluctuations—specifically the "wearing off" phenomenon—and may be part of symptomatic management in early stages. This approach is applied in scenarios where supportive symptom management is appropriate.

Quick Fact: Symptomatic Assistance for Motor Symptoms This medication is often used during phases when symptoms of increased neurological or muscular activity become more noticeable, and may assist with maintaining functional stability.

Regulatory References

  1. NIH MedlinePlus Drug Information
Advertisements

Eligibility and Restrictions for Use

Official Population Eligibility for Selegiline

Regulatory documentation defines strict eligibility rules for the use of Selegiline based on patient status, age, organ function, and concurrent medication use.

Contraindicated Populations: Selegiline is strictly contraindicated for patients with a known hypersensitivity to the drug. It must not be used concurrently with other Monoamine Oxidase Inhibitors (MAOIs), certain opioid drugs (such as meperidine, tramadol), or serotonergic agents (including many SSRIs, SNRIs, and TCAs), due to the mandated risk of severe adverse reactions. The transdermal system is further contraindicated for pediatric patients under 12 years of age and individuals with pheochromocytoma.

Age and Life-Stage Restrictions: Safety and efficacy of oral selegiline have not been established for the pediatric population. Use is not recommended for adolescents aged 12 to 17 (transdermal system). For individuals who are pregnant, use may cause fetal harm based on animal data, while the use in breastfeeding individuals is not recommended, with the regulatory instruction to discontinue nursing or discontinue the drug.

Organ Function and Comorbidities: Regulatory labeling advises that use is not recommended for populations experiencing severe renal impairment (CrCl <30 mL/min) or severe hepatic impairment. Patients with a history of mania, psychosis, or uncontrolled hypertension require mandated caution. Additionally, the orally disintegrating tablet form is restricted for patients with Phenylketonuria (PKU) because it contains phenylalanine.

Advertisements

What should I know about interactions with other medicines?

The official interaction profile for selegiline is characterized by strict regulatory prohibitions against co-administration with multiple substance classes due to documented safety concerns. Combinations are formally contraindicated with all serotonergic agents, including SSRIs and tricyclic antidepressants (TCAs), as well as other Monoamine Oxidase Inhibitors (MAOIs) such as linezolid. Certain opioid drugs, specifically meperidine, tramadol, and methadone, are also prohibited combinations due to the documented risk of precipitating Serotonin Syndrome.

Pharmacodynamic interactions extend to sympathomimetics (e.g., ephedrine), where co-use carries an officially documented risk of uncontrolled hypertension. Due to the severity of these combinations, a mandatory 14-day washout period is required after selegiline discontinuation before initiating therapy with any contraindicated medication.

Pharmacokinetic modification is documented with certain substances; for example, oral contraceptives may officially increase selegiline's systemic exposure. Furthermore, the regulatory guidance includes specific dietary constraints: tyramine-containing foods must be avoided or limited with oral selegiline forms due to the documented potential for a Hypertensive Crisis. Caution is also advised regarding use in individuals with severe liver dysfunction, as this condition may lead to higher selegiline blood levels.

Advertisements

Mechanism of Action

Селективное Ингибирование Фермента MAO-B

Селегилин действует как селективный, необратимый ингибитор фермента Моноаминоксидазы B ( MAO-B), который отвечает за метаболический распад (катаболизм) дофамина в головном мозге. Путем создания прочной химической связи, препарат инактивирует MAO-B на длительный срок, что является основным молекулярным действием, инициирующим дальнейший физиологический эффект.

Блокирование Метаболизма Дофамина и Усиление Нейротрансмиссии

Необратимая блокировка MAO-B предотвращает разрушение дофамина внутри нервных окончаний. Это приводит к повышению концентрации свободного дофамина в синаптической щели, что, в свою очередь, усиливает передачу дофаминергических сигналов в центральной нервной системе. Физиологический эффект является пролонгированным, поскольку активность MAO-B восстанавливается только после синтеза новых молекул фермента, обеспечивая sustained effect на активность дофаминергических путей.

Advertisements

Dosage and Administration Information

Instruction Map: How to use Selegiline — Official Administration Guidelines

Administration Scope Detail
Route of administration Oral (tablet, capsule, orally disintegrating tablet) and Transdermal (patch).
Dosing schedule Oral Tablet/Capsule (PD): 5 mg twice daily; maximum 10 mg/day. ODT (PD): Initial 1.25 mg once daily, may increase to 2.5 mg once daily after at least 6 weeks. Transdermal Patch (MDD): Initial 6 mg/24 hr once daily; maximum 12 mg/24 hr, titrated in 3 mg/24 hr increments every 2 weeks.
Timing in relation to meals (if applicable) Oral tablets/capsules must be taken with food (typically breakfast and lunch). Orally disintegrating tablets must be taken in the morning, before breakfast.
Preparation requirements (if applicable) The ODT must be handled with dry hands, placed on the tongue to disintegrate, and administered without liquid.
Age-group administration rules Use in children is not established. For adults with mild to moderate hepatic impairment, the ODT daily dose should be reduced (e.g., from 2.5 mg to 1.25 mg).
Missed-dose rules If a dose is missed, guidance generally advises taking it as soon as possible, unless it is close to the time for the next scheduled dose, in which case the missed dose should be skipped.
Special procedural conditions Ingesting food or liquids must be avoided for 5 minutes before and after taking the ODT. A tyramine-restricted diet is required for transdermal patch doses of 9 mg/24 hr and 12 mg/24 hr and must continue for two weeks after dose reduction.

Instruction Classifications (High-Level)

Instruction Classification Detail
Administration method type Oral (non-disintegrating and orally disintegrating) and Transdermal.
Frequency pattern Once daily or Twice daily.
Basis of guidelines Standardized clinical protocols.
Use-context constraints Must be used as adjunct to levodopa; dose adjustments are mandated for specific forms in certain patient populations.

Resulting Procedural Structure

Official step sequence:

  • The conventional oral form requires twice-daily administration with meals, contrasting with the once-daily patch or ODT forms.
  • The Orally Disintegrating Tablet must be administered buccally in a fasted state, defining strict five-minute intake conditions around the dose.
  • When used in conjunction with levodopa, instructions indicate that the levodopa dose may require a 10% to 30% reduction two to three days after selegiline initiation.

Connection to the overall use protocol:

The official administration protocol for Selegiline is distinctly defined by the formulation used, requiring different daily frequencies and intake relationships to food. These instructions standardize the use of the conventional tablet, the ODT, and the transdermal patch, establishing the required initial dosing, titration rules, and specific handling conditions. The instructions mandate specific patient adherence to dietary restrictions and dose reductions for certain populations, all without relying on clinical interpretation.

Advertisements

Recent Clinical Evidence

Selegiline: Recent Clinical Evidence

Clinical research has focused on the use of selegiline both as a single intervention (monotherapy) and as an addition to other established therapies for Parkinson’s disease (PD) and major depressive disorder (MDD).


Evidence in Early Parkinson’s Disease

Large, randomized, controlled trials (RCTs) investigating selegiline monotherapy in individuals newly diagnosed with PD have consistently reported a delay in the initiation of levodopa treatment. This effect suggests that selegiline provides symptomatic benefit in the early stages of the condition. Follow-up studies, however, suggest that this benefit is primarily symptomatic, and the long-term impact on overall disability progression remains a subject of ongoing discussion.


Combination Therapy and Long-Term Use

When used as an adjunct to levodopa in patients with more advanced PD, studies indicate that selegiline is associated with several effects:

  • Levodopa-Sparing Effect: Research has demonstrated that the combination therapy enabled patients to maintain optimal clinical status while requiring a lower total daily dose of levodopa compared to levodopa monotherapy.
  • Motor Fluctuations: The addition of selegiline was associated with a delay in the emergence of motor complications, such as wearing-off phenomena.

Safety Profile

The most common adverse events reported in clinical trials for selegiline monotherapy include insomnia, nausea, and dizziness. When combined with levodopa, the drug may increase the incidence of levodopa-related adverse effects, such as dyskinesias and orthostatic hypotension, which can often be managed by levodopa dose adjustment. Early concerns regarding increased mortality with the combination of selegiline and levodopa were not supported by subsequent robust meta-analyses.

Key Studies & References

  1. NICE Guideline NG71: Parkinson's disease in adults - Diagnosis and management
Advertisements

Frequently Asked Questions (FAQ)

Common questions about Селегилин (FAQ)

Q: Селегилин is for Parkinson's disease, but what else is it approved for?

According to official product information, Selegiline is approved for the management of Parkinson’s disease. Additionally, a specific version of the medication, the transdermal patch, is approved by some regulatory bodies for the treatment of Major Depressive Disorder (MDD) in adults.

Q: How long does the effect of Селегилин last each day?

Selegiline acts as an irreversible inhibitor of the MAO-B enzyme in the body. This means that once the enzyme is blocked, the effect on dopamine breakdown is long-lasting. Full enzyme activity is only recovered after the body produces new enzyme molecules, a process that may take up to two weeks after discontinuation.

Q: Is Селегилин different from other MAO-B inhibitors?

Studies and regulatory information indicate that Selegiline's profile is distinct from some other drugs in the same class. One key difference is that Selegiline is broken down (metabolized) in the body into active compounds, including L-amphetamine and L-methamphetamine, which may contribute to its effects.

Q: Is Селегилин a long-term medication?

The medical conditions that Селегилин is used to manage are generally chronic. Clinical studies have assessed its use for extended treatment periods, such as up to 56 weeks in some Parkinson’s disease trials.

Q: Does Селегилин affect driving ability?

Official product warnings note that caution is required when driving, operating machinery, or performing any hazardous activity. This caution is necessary due to the risk of common side effects like dizziness and drowsiness, as well as the risk of suddenly falling asleep during daily activities.

Q: Can Селегилин affect memory or concentration?

Yes, official product information lists confusion and difficulty concentrating as possible side effects. Other effects on the central nervous system, such as impairment in thinking and judgment, have also been noted, particularly in older adults.

Q: Is there a risk of interaction between Селегилин and cold medicines?

Yes, the prescribing information includes a warning against using over-the-counter cold and cough products. Many of these contain sympathomimetic amines (like pseudoephedrine), which can dangerously increase blood pressure when combined with Selegiline.

Q: Are there any warnings about using Селегилин before a major event?

Regulatory warnings caution against engaging in activities that require a high degree of mental alertness, especially when starting the medication. Regulatory guidance suggests assessing the effects of the medication before undertaking tasks that require heightened concentration or quick responses.

Q: What is the difference in side effects between high and low doses of Селегилин?

The primary difference relates to the selectivity of the drug's action. At doses higher than those typically used for Parkinson's disease, Selegiline loses its ability to selectively block the MAO-B enzyme. This non-selective action significantly increases the risk of severe drug and food interactions, including a tyramine-related hypertensive crisis.

Q: What is the difference between Селегилин and Rasagiline?

Both are used to treat Parkinson's disease. One distinction is the available formulations, as Selegiline comes in multiple forms including oral tablets, an orally disintegrating tablet (ODT), and a transdermal patch. Rasagiline is typically available only as an oral tablet.

Q: Does taking Селегилин with coffee or caffeine cause an issue?

Regulatory information recommends limiting or avoiding large amounts of caffeinated food or beverages, such as coffee, tea, or cola, particularly at higher doses. This caution is based on the general stimulant properties and the potential for increased adverse effects on the nervous system.

Q: Can older adults use Селегилин safely?

Official data indicates that the older adult population may require clinical monitoring when Selegiline is used. Older adults may be more susceptible to certain side effects, such as low blood pressure (hypotension), dizziness, and difficulties with movement coordination.

Q: Is Селегилин a controlled substance?

In the United States, Selegiline is generally not classified as a controlled substance under regulatory scheduling.

Q: What interactions does Селегилин have with herbal supplements?

According to the official product information, Selegiline is strictly contraindicated for use with the herbal supplement St. John’s Wort. This prohibition is due to the serious risk of Serotonin Syndrome, a condition that occurs when serotonin levels become too high.

Q: Is weight change a possible side effect of Селегилин?

Regulatory data lists changes to appetite as possible side effects. Anorexia, which is a loss of appetite, is listed as a common side effect, and weight loss has also been reported in clinical studies.

Q: Does Селегилин interact with anesthesia for surgery?

Yes, official product information contraindicates Selegiline's use with certain opioids, such as meperidine, which are often administered during surgery. A patient is required to undergo a washout period of at least 14 days before starting treatment with these prohibited agents.

Q: Is the effect of Селегилин immediate or gradual?

The MAO-B inhibiting action of the medication is rapid, beginning shortly after an oral dose is taken. However, the full symptomatic effects can be more gradual and may take time to become fully noticeable.

Q: What should be done if a potential drug interaction is suspected?

If a patient suspects a severe reaction is occurring, such as a sudden, intense headache, confusion, or a rapid or irregular heartbeat, official regulatory instructions state that a patient should seek medical attention or go to an emergency room immediately.

Q: Is Селегилин available as a generic drug?

Yes, official sources confirm that lower-cost, generic versions of the selegiline tablets and capsules are widely available.

Q: Can Селегилин cause vision problems?

Vision changes are not listed as a primary side effect, but blurred vision can occur as a secondary symptom. Orthostatic hypotension (low blood pressure upon standing) is a common side effect of the drug, which can lead to lightheadedness and temporary blurring of vision.

Q: Does Селегилин interact with alcohol?

Official warnings advise against the consumption of alcohol while taking Selegiline. Using alcohol may increase the risk of certain central nervous system side effects, including dizziness, confusion, and difficulty concentrating.

Q: Is it normal to feel anxious or irritable when taking Селегилин?

Yes, the official product information lists mood and behavioral changes as potential side effects. Anxiety, agitation, and irritability are among the mood changes reported in association with this medication.

Q: Can a person stop taking Селегилин suddenly?

Regulatory guidance notes that abrupt discontinuation of the medication is typically not recommended. This is because stopping suddenly may potentially lead to serious withdrawal symptoms, such as high fever (hyperpyrexia) and severe confusion, or a return of existing symptoms.

Q: Does Селегилин have a black box warning?

Only the transdermal patch formulation of Selegiline carries a Boxed Warning—the most stringent regulatory warning. This warning highlights an increased risk of suicidal thoughts and behaviors in patients being treated for Major Depressive Disorder.

Advertisements

How should Селегилин be stored and disposed of?

Storage and Disposal Requirements for Selegiline

Selegiline must be stored according to official regulatory labeling to maintain its stability and effectiveness. The product should be kept at controlled room temperature, specifically within the range of 15°C to 30°C (59°F to 86°F).

Tablets must be dispensed and stored in a tight, light-resistant container to provide protection against light and moisture. As a mandatory safety requirement, the medication must be kept out of the reach of children.

Disposal

For Selegiline transdermal systems (patches), official instructions specify that used systems should be discarded in household trash using a method that prevents accidental application or ingestion by children or pets. Other unused or expired forms should be disposed of in accordance with local regulations.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

Available in countries:

Equivalent of Селегилин found in:

A-Z Index: