Product Information

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. (dependent 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 anti-aging.

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.

Manufacturer's Insert

Azilect / Agilect / Rasagiline 1 mg

What Azilect is and what it is used for:
Azilect tablets are presented as white to off-white, round, flat, bevelled tablets, debossed with “GIL” and “1” underneath on one side and plain on the other side. The tablets are available in blister packs of 7, 10, 28, 30, 100 and 112 tablets or in a bottle containing 30 tablets. Azilect is used for the treatment of Parkinson’s disease as monotherapy (without levodopa) or as adjunct (with levodopa). In Parkinson’s disease there is a loss of cells producing dopamine in certain areas in the brain. Azilect enables increased and sustained levels of dopamine in these areas.

Before you take Azilect:
Before you take Azilect it is important that you read the following sections and discuss any questions you might have with your doctor.

Do not take Azilect:
- If you are hypersensitive (allergic) to rasagiline or to any of the ingredients of Azilect.
- If you have a severe liver insufficiency.
Do not take monoamine oxidase (MAO) inhibitors whether used as antidepressants, for the treatment of Parkinson’s disease, or for any other indication including medicinal and natural products without prescription (e.g. St Johns Wort), while taking Azilect. Do not take the strong pain killer, pethidine, while taking Azilect. You should wait at least 14 days after stopping Azilect treatment and starting treatment with MAO inhibitors or pethidine.

Take special care with Azilect:
- if you have mild to moderate liver insufficiency
- If you take medicines containing fluoxetine, fluvoxamine, dextromethorphan or sympathomimetics, please see section “Taking other medicines”.
- Azilect is not recommended for use under the age of 18.

Pregnancy:
If you are pregnant or planning to become pregnant, ask your doctor or pharmacist for advice before taking Azilect.

Breast Feeding:
Ask your doctor or pharmacist for advice before taking Azilect.

Taking other medicines:
Please ask your doctor or pharmacist for advice if you are taking or have recently taken any other medicines, even those obtained without prescription.
The following medicines require specific medical advice before being taken together with Azilect: Certain antidepressants (selective serotonin reuptake inhibitors, tricyclic or tretracyclic antidepressants), the antibiotic ciproflaxin used against infections, the cough suppressant dextromethorphan, sympathomimetics such as those present in nasal and oral decongestants and cold medications containing ephedrine or pseudoephedrine. The use of Azilect together with the antidepressants containing fluoxetine or fluvoxamine should be avoided. You should wait at least five weeks after stopping fluoxetine treatment and starting treatment with Azilect. You should wait at least 14 days after stopping Azilect treatment and starting treatment with fluoxetine or fluvoxamine.

How to take Azilect:
Take Azilect exactly as instructed by your doctor. You should talk with your physician or pharmacist if you are unsure. The recommended dose of Azilect is one tablet of 1mg take orally once daily. Azilect may be taken with or without food.

If you take more Azilect than you should:
If you think that you have taken too many Azilect tablets, contact your doctor or pharmacist immediately. Take the Azilect carton/ bottle with you to show the doctor or pharmacist.

If you forget to take Azilect:
If you have forgotten to take a dose of Azilect take the next dose at the usual time. Do not take a double dose to make up for the one you missed.

Possible Side Effects
Like all medicines, Azilect can have side effects.
The following side effects have been reported:
Very common (more than 10% of the patients): Abnormal movements (dyskinesia), headache.
Common (between 1-10% of the patients): Abdominal pain, accidental injury (primarily falls), allergic reaction, fever, flu syndrome, malaise, neck pain, angina pectoris, low blood pressure when rising to a standing position (postural hypotension), anorexia, constipation, dyspepsia, dry mouth, vomiting, abnormal results in blood tests (leucopenia), joint pain (arthralgia) arthritis, tenosynovitis, weight loss, abnormal dreams, difficulty in muscular co-ordination (ataxia) depression, vertigo, prolonged muscle contractions (dystonia) rhinitis, contact dermatitis, rash, vesiculobullous rash, conjunctivitis, urinary urgency.
Uncommon (between 0.1-1% of the patients): Stroke (cerebrovascular accident), myocardial infarct.
In addition, skin cancer was reported in around 1% of patients in the clinical trials.
Nevertheless, scientific evidence suggests that Parkinson’s disease, and not any drug in particular, is associated with higher risk of skin cancer (not exclusively melanoma). You should speak to with your doctor about any suspicious skin changes.

If you notice any side effects not mentioned in this leaflet, please contact your doctor or pharmacist.

Storing Azilect:
Keep out of the reach and sight of children. Do not sore above 25 degrees C. Store in the original package. Do not use after the expiry date stated on the carton, bottle or blister.