AZILECT ® AGILECT ® A novel new MAO-B inhibitor

Azilect contains Rasagiline and is also known as Agilect. Azilect has recently been approved in Europe as a new treatment for Parkinson’s disease.

Azilect helps to prevent the breakdown of dopamine, the neurotransmitter most affected in Parkinson’s disease. It achieves this by inhibiting an enzyme called monoamine oxidase B, (or MAO-B). The only other drug known to be as specific as this specific is Deprenyl (Selegiline), however Azilect is believed to be 5 to 10 times more potent.

Also, unlike Deprenyl (for which a tiny amount is converted into the by-product of amphetamine), Azilect is bio-transformed to aminoindan, a non-amphetamine compound. Aminoindan, by-itself appears to have some neuroprotective qualities.

Azilect is likely to also act beneficially through its ability to act as an anti-oxidant and an anti-apoptotic agent.

In clinical trials, Azilect has been found to be effective as a monotherapy (i.e. taken on its own), or when taken together with Levodopa (Sinemet), for both early and late stage Parkinson’s disease.

Azilect has shown itself to have no more side effects than those taking placebo and there has been no sign of any of the so-called “cheese” effects; a condition which reacts with tyrosine-containing foods such as dairy produce.

In one trial of 404 subjects treated with 1 mg. or 2 mg. of Azilect daily for 1-year, showed less functional decline than those given placebo. Another 26-week double-blind study concluded that Azilect was effective at 1 mg. or 2 mg. daily for early Parkinson symptoms.

Azilect is also believed to offer protection against dementias, through its MAO-B inhibiting activity, anti-oxidant and anti-apoptotic properties, as well as its propargylamine moiety. This protects mitochondrial viability, activating Bc1-2 genes and down regulating the Bax family of proteins. This is turn processes amyloid precursors protein (which would otherwise lead to the formation of plagues) and increases nerve growth factor. Because of these reasons, Azilect is now also in clinical trials to study its efficacy in Alzheimer’s disease.

Typically dosages for dementia are 1 mg. daily, maximum 2 mg. daily, although persons using it for preventative measures may want to consider 0.25 mg. to 0.5 mg. (dependant upon need).

It is known that at dosages greater than 2 mg. daily Azilect can also become a MAO-A inhibitor and therefore will interfere more readily with other drugs such as SSRI anti-depressants etc.

Unless under the guidance of a health professional, the concurrent use of any other MAO inhibiting products, such as Deprenyl, Gerovital, St. John’s Wort, as well as other anti-depressants, particularly SSRI’s such as Paxil and Prozac etc., should be avoided, (please see the manufacturer’s insert link below for further details).

The effect of a long-term regimen of Azilect on human lifespan is unknown, yet since Deprenyl has increased both life-expectancy and maximum lifespan in animal studies, it is possible, that Azilect’s metabolic profile may have similar advantages for antiaging.

For those with Parkinson’s disease, particularly who are undergoing a multi-approach therapy, Azilect may well be the drug of choice.

Further clinical trials on Azilect

New data presented in an oral presentation session, at the 9th congress of the European Federation of Neurological Societies, showed that treatment with Azilect (rasagiline 1 mg) once daily can provide significant additional benefits to levodopa treated patients with moderate to advanced Parkinson's disease (PD). These benefits were seen regardless of whether patients were receiving additional, optimized treatment with a dopamine agonist.

The new sub-analysis of the LARGO trial (Lasting effect in Adjunct therapy with Rasagiline Given Once daily), found that giving Azilect to patients already optimized on levodopa, with or without concomitant dopamine agonist (DA) treatment, significantly reduced daily “OFF” time (when the effects of medication wear off and PD symptoms return) by an average of 1.2 hours when compared to placebo, resulting in a clinically meaningful improvement in daily function for patients, without a related increase in dopaminergic adverse events. Patients experienced a corresponding increase in “ON” time (when medication is working) without troublesome dyskinesias, the involuntary movement’s characteristic of long-term PD therapy.

Principle investigator, Professor Olivier Rascol, of University Hospital Toulouse, France, commented: “This data shows that people with Parkinson's disease can achieve additional symptom benefits with Azilect, even when already receiving optimized levodopa treatment and irrespective of whether they are also receiving a dopamine agonist.”

The significant improvements in functioning demonstrated by Azilect, on top of DA treatment, were also shown with all additional end points, such as Clinical Global Impressions measures during “ON” time, UPDRS-motor during "ON" time (symptoms of tremor, slowness of movement, stability and rigidity), and UPDRS-Activities of Daily Living scores during “OFF” time, (measuring the ability of patients to walk, speak, swallow, dress and get out of bed.)

The active comparator in the study, entacapone, demonstrated comparable reductions in daily "OFF" time, but results for some of the additional measures mentioned above did not achieve significance.

The LARGO study investigated the response to treatment in 687 levodopa treated patients who were randomized to receive Azilect, entacapone or placebo. Two thirds of patients in each arm were also receiving DA therapy, allowing for comparison of the effectiveness of Azilect given alone or on top of a dopamine agonist.

This data from the LARGO study adds to the growing body of evidence for Azilect as an effective and well-tolerated treatment for Parkinson's disease. The findings from LARGO are consistent with the recently published study PRESTO, which also demonstrated that once daily Azilect, as an adjunctive therapy, significantly increases daily “ON” time and improves the cardinal symptoms of Parkinson's disease.

In addition, data from the TEMPO trial, a study of Azilect as monotherapy, demonstrated that Azilect is an effective and well-tolerated treatment in early disease and can significantly delay the progression of PD symptoms.

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What our customers say...

My father is doing much, much better. He has replaced his 5mg selegiline-twice per day with rasagiline-once per day. There seems to be no adverse reactions to replacing selegiline immediately with rasagiline...at least in my fathers case. The improvement in my father began on about the fourth day on rasagiline. He was moving better, thinking more clearly, speaking much better and in a better mood, all with no adverse reactions thus far. I think this drug will be a huge success. Since my father has severe short-term memory problems he didn't even remember he was on a new drug so I sincerely doubt this is a placebo effect type thing. I spent the whole day with my father today and he was the best I have seen him in at least two years.
Joseph, Arizona.