Elepril

Elepril Uses, Dosage, Side Effects, Food Interaction and all others data.

Although the mechanisms for selegiline's beneficial action in the treatment of Parkinson's disease are not fully understood, the selective, irreversible inhibition of monoamine oxidase type B (MAO-B) is thought to be of primary importance. MAO-B is involved in the oxidative deamination of dopamine in the brain. Elepril binds to MAO-B within the nigrostriatal pathways in the central nervous system, thus blocking microsomal metabolism of dopamine and enhancing the dopaminergic activity in the substantial nigra. Elepril may also increase dopaminergic activity through mechanisms other than inhibition of MAO-B. At higher doses, selegiline can also inhibit monozmine oxidase type A (MAO-A), allowing it to be used for the treatment of depression.

Dopamine is an essential chemical that occurs in many parts of the body. It is the premature degradation of dopamine that results in the symptoms of Parkinson's disease. Monoamine oxidase (MAO) is an enzyme which accelerates the breakdown of dopamine. Elepril can prolong the effects of dopamine in the brain by preventing its breakdown through seletively blocking MAO-B. It also may prevent the removal of dopamine between nerve endings and enhance release of dopamine from nerve cells.

Trade Name Elepril
Availability Prescription only
Generic Selegiline
Selegiline Other Names L-Deprenalin, Selegilina, Selegiline, Selegilinum
Related Drugs Rexulti, Gocovri, Rytary, Sinemet, Sinemet CR, sertraline, trazodone, Lexapro, Zoloft, citalopram
Type
Formula C13H17N
Weight Average: 187.286
Monoisotopic: 187.136099551
Protein binding

> 99.5%

Groups Approved, Investigational, Vet approved
Therapeutic Class Antiparkinsonian Drug
Manufacturer
Available Country Brazil
Last Updated: September 19, 2023 at 7:00 am
Elepril
Elepril

Uses

Elepril is used for an adjunct in the management of Parkinsonian patients being treated with levodopa/carbidopa who exhibit deterioration in the quality of their response to this therapy. There is no evidence from controlled studies that selegiline has any beneficial effect in the absence of concurrent levodopa therapy.

Evidence supporting this claim was obtained in randomized controlled clinical investigations that compared the effects of added selegiline or placebo in patients receiving levodopa/carbidopa. Elepril was significantly superior to placebo on all three principal outcome measures employed: change from baseline in daily levodopa/carbidopa dose, the amount of 'off' time, and patient selfrating of treatment success. Beneficial effects were also observed on other measures of treatment success (e.g., measures of reduced end of dose akinesia, decreased tremor and sialorrhea, improved speech and dressing ability and improved overall disability as assessed by walking and comparison to previous state).

Elepril is also used to associated treatment for these conditions: Attention Deficit Hyperactivity Disorder (ADHD), Major Depressive Disorder (MDD), Parkinson's Disease (PD)

How Elepril works

Although the mechanisms for selegiline's beneficial action in the treatment of Parkinson's disease are not fully understood, the selective, irreversible inhibition of monoamine oxidase type B (MAO-B) is thought to be of primary importance. MAO-B is involved in the oxidative deamination of dopamine in the brain. Elepril binds to MAO-B within the nigrostriatal pathways in the central nervous system, thus blocking microsomal metabolism of dopamine and enhancing the dopaminergic activity in the substantial nigra. Elepril may also increase dopaminergic activity through mechanisms other than inhibition of MAO-B. At higher doses, selegiline can also inhibit monozmine oxidase type A (MAO-A), allowing it to be used for the treatment of depression.

Dosage

Elepril dosage

Elepril Hydrochloride is intended for administration to Parkinsonian patients receiving levodopa/carbidopa therapy who demonstrate a deteriorating response to this treatment. The recommended regimen for the administration of Elepril Hydrochloride is 10 mg per day administered as divided doses of 5 mg each taken at breakfast and lunch. There is no evidence that additional benefit will be obtained from the administration of higher doses. Moreover, higher doses should ordinarily be avoided because of the increased risk of side effects.

After two to three days of selegiline treatment, an attempt may be made to reduce the dose of levodopa/carbidopa. A reduction of 10 to 30% was achieved with the typical participant in the domestic placebo controlled trials who was assigned to selegiline treatment. Further reductions of levodopa/carbidopa may be possible during continued selegiline therapy

Toxicity

LD50=63 mg/kg (rats, IV)

Precaution

Some patients given selegiline may experience an exacerbation of levodopa associated side effects, presumably due to the increased amounts of dopamine reaction with super sensitive, post-synaptic receptors. These effects may often be mitigated by reducing the dose of levodopa/carbidopa by approximately 10 to 30%.

The decision to prescribe selegiline should take into consideration that the MAO system of enzymes is complex and incompletely understood and there is only a limited amount of carefully documented clinical experience with selegiline. Consequently, the full spectrum of possible responses to selegiline may not have been observed in pre-marketing evaluation of the drug. It is advisable, therefore, to observe patients closely for atypical responses.

Food Interaction

  • Avoid tyramine-containing foods and supplements. Consuming foods containing tyramine such as yogurt, aged cheese, ripe bananas, wine, and sourdough bread may increase the risk of having an uncontrolled hypertensive reaction.
  • Take before a meal. Take selegiline oral disintegrating tablets before breakfast and at least 5 minutes before or after any food or drink. Taking selegiline with food reduces the AUC by approximately 60%.
  • Take with food. Take selegiline capsules or tablets with breakfast and lunch. Food can increase the exposure to selegiline by 3-4 fold.

[Major] GENERALLY AVOID: Foods that contain large amounts of tyramine may precipitate a hypertensive crisis in patients treated with monoamine oxidase inhibitors (MAOIs).

The mechanism is inhibition of MAO-A, the enzyme responsible for metabolizing exogenous amines such as tyramine in the gut and preventing them from being absorbed intact.

Once absorbed, tyramine is metabolized to octopamine, a substance that is believed to displace norepinephrine from storage granules.

Although selegiline is considered a selective inhibitor of MAO-B, the selectivity may not be absolute even at recommended dosages.

Rare cases of hypertensive reactions associated with ingestion of tyramine-containing foods have been reported in patients taking the recommended daily oral dose of selegiline.

Data for transdermal selegiline indicate that the 6 mg<24 hour dosage may be given safely without dietary restrictions.

However, limited data are available for higher dosages.

MANAGEMENT: Patients treated with oral selegiline and transdermal selegiline (greater than 6 mg<24 hour) should preferably avoid consumption of products that contain large amounts of amines and protein foods in which aging or breakdown of protein is used to increase flavor.

These foods include cheese (particularly strong, aged or processed cheeses), sour cream, wine (particularly red wine), champagne, beer, pickled herring, anchovies, caviar, shrimp paste, liver (particularly chicken liver), dry sausage, salamis, figs, raisins, bananas, avocados, chocolate, soy sauce, bean curd, sauerkraut, yogurt, papaya products, meat tenderizers, fava bean pods, protein extracts, yeast extracts, and dietary supplements.

Caffeine may also precipitate hypertensive crisis so its intake should be minimized as well.

At least 14 days should elapse following discontinuation of selegiline therapy before these foods may be consumed.

Specially designed reference materials and dietary consultation are recommended so that an appropriate and safe diet can be planned.

Patients should also be advised to promptly seek medical attention if they experience potential signs and symptoms of a hypertensive crisis such as severe headache, visual disturbances, difficulty thinking, stupor or coma, seizures, chest pain, unexplained nausea or vomiting, and stroke-like symptoms.

The recommended dosages of selegiline should not be exceeded, as it can increase the risk of nonselective MAO inhibition and a hypertensive crisis.

Elepril Alcohol interaction

[Moderate] GENERALLY AVOID:

Alcohol may potentiate some of the pharmacologic effects of central nervous system (CNS)-active agents.

Use in combination may result in additive CNS depression and/or impairment of judgment, thinking, and psychomotor skills.

Patients receiving CNS-active agents should be advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled against driving, operating machinery, or engaging in potentially hazardous activities requiring mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Elepril Hypertension interaction

[Moderate] Elepril can cause hypertensive reactions and it should be used with caution in patients with hypertension.

Patients should report any symptoms such as occipital headache, palpitations, neck stiffness or soreness, nausea, sweating, dilated pupils and photophobia.

Patients receiving therapy need to have monitored their blood pressure frequently to detect any evidence of pressor response.

Additionally, patients should be advised to avoid foods and drinks with high tyramine content such as cheese, sour cream, beer, liver, bananas and others, as these might trigger a hypertensive crisis.

Elimination Route

Rapidly absorbed from the gastrointestinal tract.

Half Life

1.2-2 hours

Pregnancy & Breastfeeding use

Pregnancy Category C. No teratogenic effects were observed in a study of embryo-fetal development in Sprague-Dawley rats at oral doses of 4, 12, and 36 mg/kg or 4, 12 and 35 times the human therapeutic dose on a mg/m2 basis.

Nursing Mothers: It is not known whether selegiline hydrochloride is excreted in human milk. Because many drugs are excreted in human milk, consideration should be given to discontinuing the use of all but absolutely essential drug treatments in nursing women.

Contraindication

Elepril is contraindicated in patients with a known hypersensitivity to this drug. Elepril is contraindicated for use with meperidine. This contraindication is often extended to other opioids.

Special Warning

Renal Impairment: No pharmacokinetic information is available on selegiline or its metabolites in renally impaired subjects.

Hepatic Impairment: No pharmacokinetic information is available on selegiline or its metabolites in hepatically impaired subjects.

Pediatric Use: The effects of selegiline hydrochloride in children have not been evaluated.

Innovators Monograph

You find simplified version here Elepril

Elepril contains Selegiline see full prescribing information from innovator Elepril Monograph, Elepril MSDS, Elepril FDA label

FAQ

What is Elepril used for?

Elepril used in the treatment of Parkinson's disease and major depressive disorder.

How safe is Elepril?

Elepril has been well tolerated when given alone. The most frequent adverse events seen during monotherapy have been insomnia, nausea, benign cardiac arrhythmias, dizziness and headache.

What are the common side effects of Elepril?

Elepril may cause common side effects are include:

  • dizziness
  • lightheadedness
  • fainting
  • dry mouth
  • nausea
  • vomiting
  • stomach pain
  • difficulty swallowing
  • heartburn
  • diarrhea
  • gas
  • constipation
  • difficulty falling asleep or staying asleep
  • unusual dreams
  • sleepiness
  • depression
  • pain, especially in the legs or back
  • muscle pain or weakness
  • purple blotches on the skin
  • rash
  • redness, irritation, or sores in the mouth (if you are taking the orally disintegrating tablets)

Is Elepril safe during pregnancy?

Data are insufficient to inform a drug-associated risk of adverse pregnancy related outcomes; animal data has shown developmental toxicity at doses greater than those used clinically.
Insufficient animal reproduction studies have been performed to conclude that this drug poses no teratogenic risk.

Is Elepril safe during breastfeeding?

Due to the potential for serious adverse reactions in breastfed infant, including hypertensive crisis, breastfeeding is not recommended during treatment.
Some authorities recommend avoiding breastfeeding for 7 days after the final dose.

Can I drink alcohol with Elepril?

You should avoid or limit the use of alcohol while being treated with Elepril.

Can I drive after taking Elepril?

If you experience increased sleepiness or fall asleep during the day, do not drive or take part in other possibly dangerous activities until you have discussed this effect with your doctor.

How does Elepril work?

Elepril works by increasing the amount of dopamine (a natural substance that is needed to control movement) in the brain.

How does Elepril increase dopamine?

Elepril increases dopamine content in the central nervous system.

Is Elepril controlled?

Elepril is not scheduled as a controlled substance.

Does Elepril affect sleep?

Insomnia and sleep disorder were reported as very common side effects.

How long does take to work?

Between four and 12 weeks most dogs show some improvement after one month of treatment and there may be continued improvement over time.

Does may cause weight gain?

Elepril may causes is the most likely to result in weight gain.

Does Elepril raise blood pressure?

You are using Elepril can raise your blood pressure to dangerous levels which could cause life-threatening side effects.

How is Elepril metabolized?

Elepril is mostly metabolized in the intestines and liver; it and its metabolites are excreted in the urine.

When is the best time to take Elepril?

It is best to take the capsules or tablets in the morning during breakfast and lunch. You should not use it with dinner because you may have trouble sleeping.

Is Elepril a stimulant?

It belongs to a class of drugs known as stimulants.

Who should not take Elepril?

Do not take Elepril if you have used narcotic pain medicines.

Can you overdose on Elepril?

Overdose symptoms may include severe headache, hallucinations, vision problems, sweating, cool or clammy skin, fast or uneven heart rate, feeling light-headed, fainting, or seizure.

What happen If I missed Elepril?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose of Elepril?

Seek emergency medical attention .Overdose symptoms may include severe headache, hallucinations, vision problems, sweating, cool or clammy skin, fast or uneven heart rate, feeling light-headed, fainting, or seizure.

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