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Eldepryl Review Article

 

Eldepryl, generic name selegiline (known in Europe under brand name Jumex) protects against aging of the brain and enhances mental function. A powerful remedy against Parkinson's disease, Eldepryl is effective also as an antidepressant and as a protector against Alzheimer's disease. Professor Knoll, who developed Selegiline is convinced of its anti-aging effect and recommends for this a dose 5 mg per week (in two doses of 2.5 mg each).

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Eldepryl generic (generic - what is it?)

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ELDEPRYL (Generic name: Selegiline HCl) is an anti-Parkinsonism drug approved by the FDA as a supportive therapy to Levodopa and other anti-Parkinsonism drugs.

It is an irreversible, first-generation monoamine oxidase (MAO) inhibitor only acting on a certain form (MAO-B) at approved dosage levels. Its action delays the breakdown of dopamine in the brain and then prolonging the therapeutic effect of Levodopa.


TextWhat is parkinsonism?

Parkinsonism (Parkinson disease, Parkinson's disease, PD, or paralysis agitans) is a common disease of the elderly (second after Alzheimer’s disease) characterized by muscle rigidity, curved posture, sluggishness of voluntary movement, festinating gait, and resting tremor. It affects the central nervous system, most specifically on the neurons that produce dopamine in the substantia nigra of the midbrain.

During the condition, these neurons in the substantia nigra gradually degenerate resulting to decreased production of dopamine in the brain. Decreased dopamine levels affect certain body functions which are mostly on motor skills or movement. Mental functions are also altered but less characterized and these may include dementia.

Causes of Parkinsonism are unknown, but some studies have shown that this condition can be inherited either as a dominant or recessive trait.

With Eldepryl (Selegiline HCl), a MAO-B inhibitor like Rasagiline, and other anti-Parkinsonism drugs, these symptoms of PD are reduced and. the condition is suppressed. Furthermore, movement and cognitive function are improved. (Katzung, 2009)

How many people have Parkinsonism?

Recent statistics showed that around 1.5 million people in the United States suffer from Parkinsonism or PD. In addition, almost 200 cases of Parkinson’s disease are diagnosed in the U.S. everyday. (NIH, 2011) In most cases, people are usually diagnosed with this disease on its later stage. The average age of patients diagnosed with PD is 62-70; but it also strikes people at an early age if they have a family history of the said disease. (Mangpaisan, 2011) As of 2005, the direct annual cost of patients suffering from Parkinsonism is around $23,100 and the total annual cost in the US alone is around $23 billion. (Huse, 2005)

Worldwide statistics on PD are also increasing every year. Currently, there are seven to ten million people with Parkinsonism found all over the world with an incidence rate of 10-13 in every 100,000 individuals per age. (Mangpaisan, 2011)


TextWhat are the effects of Eldepryl in the body?

Dopamine is an inhibitory neurotransmitter in the brain that acts mostly as a stabilizer, most especially on movement. When decreased in levels in Parkinsonism, the effects of excitatory neurotransmitters will continue and will lead to the distinct features in motor and neuropsychiatric symptoms. To relieve from these symptoms, an enzyme called monoamine oxidase (MAO) can be irreversibly inhibited. Monoamine oxidase is medically proven to be responsible for the destruction of most of the dopamine after it has been secreted from the neurons in the basal ganglia.

Monoamine oxidase is an enzyme found in the outer mitochondrial membrane. It is present in cells not only with dopamine receptors but with phenylthelamine, benzylamine, epinephrine, tyramine and tryptamine receptors. It occurs in two isoforms with different substrate specificities. These two forms, MAO-A and MAO-B, had been differentiated by their sensitivity to a certain MAO inhibitor clorgyline. MAO-A is inhibited by low doses of clorgyline, whereas MAO-B is relatively insensitive to clorgyline inhibition.

Drugs that inhibit MAO-A are at more risk for dietary tyramine-provoked hypertensive crisis because its metabolites, amphetamine and metamphetamine, can inhibit peripheral MAO-A (mostly found in the liver, kidney, stomach and small intestines) which is essential for tyramine metabolism. Theoretically, Eldepryl only inhibits MAO-B that is only found in the brain but it can also possibly inhibit MAO-A at large doses. However, control in food intake rich in tyramine, such as pickled, smoked or fermented meat and cheese, is still advised. (Lohle, 2011)

Moreover, Eldepryl should not be taken with SSRI’s and tricyclic antidepressants for risk of serotonin syndrome. Serotonin syndrome is characterized as fever, involuntary muscle twitching, altered mental status, over-responsive reflexes, diarrhea, lack of muscle coordination, tremor, mood alteration and/or shivering. Recent studies had failed to prove this syndrome at prescribed doses of Eldepryl but given the higher specificity of a second-generation MAO-B inhibitor (Rasagiline), Eldepryl has a higher likelihood of causing the said syndrome than the latter, (Barrett, 1996)


How does the body react to Eldepryl intake?

Eldepryl is a drug with low bioavailabilty and should be taken with a meal, most preferably rich in fat. It is taken orally in tablet form and is currently available in two doses (5mg, 10mg).

For early parkinsonism, it is usually taken 10 mg daily in single or divided doses, preferably during breakfast and lunch because it causes insomnia when taken at night. Initially, it should also be taken 2.5 mg daily due to first-pass effect. (Rang, 2007)

As it passes through the liver, it produces 3 major metabolites: desmethylselegiline, amphetamine and metamphetamine. The drug’s neuroprotective properties are associated with desmethylselegiline and this is metabolized by cytochrome-P450, most specifically CYP2B6. Levels of amphetamine and metamphetamine were not found to be psychoactive but they contribute to the stimulatory effect of the drug to motor activity. (Kamada, 2002)

Excretion of the drug is via urine and mainly consisting of metamphetamine (37% of the dose). Free forms were also found in the urine but in minimum amount. (Shin, 1997)


What are the do’s and don’ts during Eldepryl intake?

Eldepryl should be taken with a full stomach and it is not advised in patients with history of gastric and/or peptic ulcer. Special precautions on this drug should also be done in patients with uncontrolled hypertension and other cardiovascular diseases.

Furthermore, it is under the US FDA Pregnancy Category C and should not be taken by pregnant or lactating women. This drug may also increase the adverse effects of other anti-Parkinsonism drugs and should not be taken with another MAO inhibitor and/or Amantadine because of potential risk of hypertensive crisis or the famous “cheese effect”.

Recently, this drug is also used for management in early parkinsonism and treatment of clinical depression. However, it is not advised to be taken together with selective serotonin reuptake inhibitors (SSRI’s) and/or tricyclic antidepressants for possible risks of serotonin syndrome. (Barrett, 1996)


What are the recent breakthroughs and recommended studies on Eldepryl?

There are current ongoing studies on the therapeutic effect of Eldepryl (Selegiline) on smoking cessation. (Kahn, 2011) There are also ongoing studies of Eldepryl against drug abuse. (NIH, 2011)

On the other hand, there are still no detailed and published studies on the association of the structure of selegiline on its therapeutic effects. (Lohle, 2011)

Written by S. N. Caoili

REFERENCES

Barrett JS, Rohatagi S, DeWitt KE, Morales RJ, DiSanto AR. The Effect of Dosing Regimen and Food on the Bioavailability of the Extensively Metabolized, Highly Variable Drug Eldepryl (Selegiline Hydrochloride) Am J Ther 1996 Apr;3(4):298-313

Huse DM et. al. Burden of illness in Parkinson's disease. Mov Disord. 2005 Nov;20(11):1449-54.

Kahn R, et. al. Selegiline Transdermal System (STS) as an Aid for Smoking Cessation. Nicotine Tob Res. 2011 Aug 16.

Kamada T, et. al. Metabolism of selegiline hydrochloride, a selective monoamine b-type inhibitor, in human liver microsomes. Drug Metab Pharmacokinet. 2002;17(3):199-206.

Lohle M., Reichmann H. Controversies in Neurology: Why Monoamine Oxidase B Inhibitors Could Be a Good Choice for the Initial Treatment of Parkinson's Disease. BMC Neurology September 2011, 11:112.

Muangpaisan W, Mathews A, Hori H, Seidel D. A systematic review of the worldwide prevalence and incidence of Parkinson's disease. J Med Assoc Thai. 2011 Jun;94(6):749-55.

Shin HS. Metabolism of Selegiline in Humans: Identification, Excretion, and Stereochemistry of Urine Metabolites Drug Metab Dispos. 1997 Jun;25(6):657-62.

Robottom BJ. Efficacy, safety, and patient preference of monoamine oxidase B inhibitors in the treatment of Parkinson's disease. Patient Prefer Adherence. 2011 Jan 20;5:57-64.

Katzung, et. al. Basic and Clinical Pharmacology 11th edition. LANGE Basic Science. McGraw Hill Companies Inc. USA. 2009. Chapter 28.
Rang HP et. al. Rang and Dale’s Pharmacology 6th edition. Elsevier Inc. USA. 2007. PP. 517-521.

U.S. Department of Health and Human Services, National Institutes of Health, National Institute of Neurological Disorders and Stroke.


 

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