Azilect - a new modern medicine for Parkinson's disease

Parkinson's disease, shaking palsy, idiopathic parkionism syndrome are all names for one pathology. After the first signs of the disease appear, within a few years the patient without proper treatment may become disabled or even die. It is about the newest medicine of our time, Azilect, which is used for this dangerous disease that will be discussed in the article.

Release form, composition and packaging

Pills

white or almost white, round, flat-cylindrical, chamfered, with “GIL 1” engraved on one side of the tablet.

Excipients: mannitol - 159.24 mg, colloidal silicon dioxide - 1.2 mg, corn starch - 20 mg, pregelatinized corn starch - 20 mg, stearic acid - 4 mg, talc - 4 mg.

10 pieces. - blisters (3) - cardboard packs. 10 pieces. - blisters (10) - cardboard packs.

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General information about the drug

Azilect inhibits MAO-B and increases both extra- and intracellular dopamine content in the corpus nigra, reducing the manifestations of Parkinson's disease.

Drug group, INN, scope of application

Azilect belongs to the group of antiparkinsonian drugs. The main active ingredient, razalgine mesylate, belongs to the class of selective monoamine oxygenase inhibitors. The drug is most popular among neurological and neuropsychiatric patients.

Azilecta's INN is Razalgin (Rasagiline).

Release forms and prices for the drug

The drug is produced in the form of round, white, odorless tablets, with a chamfer on one side and the inscription “GIL”. The package contains 30 or 100 tablets, which are packaged in blisters.

The price of Azilect in the Russian Federation in various pharmacy chains is presented in the table.

Analogues of the drug

Speaking about the group of inhibitory effects of MAO on dopamine, the only direct analogue of Azilect is Selegiline. Unlike Azilect, it is less toxic, has a higher distribution coefficient in the body and is practically not inferior in therapeutic effect.

However, Selegiline is completely contraindicated in patients with myocardial conduction disorders, uncontrolled arterial hypertension and prostate diseases, which, given the age of Parkinson's patients, significantly reduces the group of patients suitable for this treatment. Nevertheless, the low price of Selegiline (about 2,500 rubles for 50 tablets) makes it an attractive alternative in the absence of contraindications.

For Parkinson's disease, agents based on other components can also be used:

1. Azilect pilyule_nervi-216.
2. Akineton pilyule_nervi-217.
3. Amantadine pilyule_nervi-218.
4. Levodopa pilyule_nervi-223.
5. Levodopa carbidopa pilyule_nervi-224.
6. Madopar pilyule_nervi-225.
7. Mendylex pilyule_nervi-226.
8. Midantan pilyule_nervi-227.
9. Mirapex pilyule_nervi-228.
10. Name pilyule_nervi-229.

pharmachologic effect

Antiparkinsonian drug. Azilect is a selective irreversible inhibitor of MAO type B, an enzyme that determines 80% of MAO activity in the brain and dopamine metabolism. Rasagiline is 30-80 times more active against MAO type B compared to MAO type A.

As a result of the inhibitory effect of the drug on MAO type B, the level of dopamine in the central nervous system increases and the formation of toxic free radicals, the excessive formation of which is observed in Parkinson's disease, decreases. Rasagiline also has neuroprotective effects.

Unlike non-selective MAO inhibitors, the drug in therapeutic doses does not block the metabolism of biogenic amines (for example, tyramine) supplied with food, and therefore does not cause tyramine-induced hypertensive syndrome (“cheese” effect).

Azilect: patient reviews

Feedback from patients is positive; there is an improvement in the condition of patients of different age groups. In many cases, in the first months of taking the drug, side effects develop, which then disappear. Rare side effects may be a complication of the underlying disease; such complications are often found in those suffering from Parkinson's disease and not taking Azilect. When taking Azilect for Parkinson's disease, the dose of the drug is not increased, side effects are less common than with treatment with other anti-Parkinson's drugs.

Pharmacokinetics

Suction

Rasagiline is rapidly absorbed after oral administration, Cmax in blood plasma is reached after 0.5 hours. The absolute bioavailability of the drug after a single administration is about 36%. Food does not affect the time it takes for rasagiline to reach Cmax in the blood, however, when consuming a high-fat meal, Cmax and AUC are reduced by 60% and 20%, respectively.

The pharmacokinetics of the drug is linear in the dose range of 0.5-2 mg.

Distribution

Plasma protein binding ranges from 60% to 70%.

Metabolism

Rasagiline is almost completely metabolized in the liver. Biotransformation is carried out by N-dealkylation and/or hydroxylation with the formation of the main biologically inactive metabolite - 1-aminoindane, as well as two other metabolites - 3-hydroxy-N-propargyl-1-aminoindane and 3-hydroxy-1-aminoindane. Metabolism of the drug is carried out with the participation of the CYP1A2 isoenzyme.

Removal

Rasagiline is excreted primarily by the kidneys (more than 60%) and to a lesser extent through the intestines (more than 20%). Less than 1% of the administered dose of the drug is excreted unchanged. T1/2 is 0.6-2 hours.

Pharmacokinetics in special clinical situations

The pharmacokinetic parameters of rasagiline remain virtually unchanged in patients with mild to moderate renal impairment.

In mild liver failure, an increase in AUC and Cmax values ​​by 80% and 38% may be observed, and in patients with moderate liver dysfunction, these parameters reach more than 500% and 80%, respectively.

Contraindications

- hypersensitivity to rasagiline or any of the components of the drug;

- simultaneous use with other MAO inhibitors (including medications and nutritional supplements containing St. John's wort), pethidine. The interval between discontinuation of rasagiline and initiation of therapy with these drugs should be at least 14 days;

- moderate to severe liver failure (classes B and C on the Child-Pugh scale);

- children and adolescents under 18 years of age (no data on effectiveness and safety).

Carefully

- mild liver failure (class A on the Child-Pugh scale);

- simultaneous use with selective serotonin reuptake inhibitors (SSRIs) (including fluoxetine, fluvoxamine), selective serotonin and norepinephrine reuptake inhibitors (SNRIs), tricyclic and tetracyclic antidepressants, potent inhibitors of the CYP1A2 isoenzyme.

Side effects

A total of 1,361 patients were enrolled in the rasagiline clinical trial program, representing a total of 3,076.4 patient-years. In the double-blind, placebo-controlled studies, 529 patients received rasagiline 1 mg/day for 212 patient-years and 539 patients received placebo for 213 patient-years.

Monotherapy

The following list describes adverse reactions that were reported with increased frequency in placebo-controlled studies in patients receiving rasagiline 1 mg/day (rasagiline group - n=149, placebo group - n=151).

Adverse reactions with differences greater than 2% compared to the placebo group are indicated in italics

.

The frequency of adverse reactions (% of patients): rasagiline/placebo is indicated in parentheses.

Adverse reactions are distributed according to the following frequency: very often (≥1/10), often (≥1/100 to <1/10), infrequently (≥1/1000 to <1/100), rarely (≥1/10 000 to <1/1000), very rare (<1/10,000).

Infectious and parasitic diseases:

often - influenza (4.7%/0.7%).

Benign, malignant and unspecified neoplasms (including cysts and polyps):

often - skin cancer (1.3%/0.7%).

From the hematopoietic system:

often - leukopenia (1.3%/0%).

From the immune system:

often - allergic reactions (1.3%/0.7%).

Metabolism and nutrition:

uncommon - decreased appetite (0.7%/0%).

Mental disorders:

often - depression (5.4%/2%), hallucinations (1.3%/0.7%).

From the nervous system:

very often - headache (4.1%/11.9%); infrequently - cerebrovascular accident (0.7%/0%).

From the side of the organ of vision:

often - conjunctivitis (2.7%/0.7%).

Hearing and labyrinth disorders:

often - vertigo (2.7%/1.3%).

From the cardiovascular system:

often - angina pectoris (1.3%/0%); uncommon - myocardial infarction (0.7%/0%).

From the digestive system:

bloating (1.3%/0%).

From the respiratory system:

often - rhinitis (3.4%/0.7%).

For the skin and subcutaneous tissues:

often - dermatitis (2%/0%); uncommon - vesicular bullous rash (0.7%/0%).

From the musculoskeletal system:

often - musculoskeletal pain (6.7%/2.6%), neck pain (2.7%/0%), arthritis (1.3%/0.7%).

From the urinary system:

often - the urge to urinate (1.3%/0.7%).

Other:

often - fever (2.7%/1.3%),
malaise (2%/0%)
.

When used as adjuvant therapy

The following list includes adverse reactions that were reported with increased frequency in placebo-controlled studies in patients receiving rasagiline 1 mg/day (rasagiline group - n=380, placebo group - n=388). The frequency of adverse reactions (% of patients): rasagiline/placebo is indicated in parentheses.

Adverse reactions with differences greater than 2% compared to the placebo group are indicated in italics

.

The frequency of adverse reactions (% of patients): rasagiline/placebo is indicated in parentheses.

Adverse reactions are distributed according to the following frequency: very often (≥1/10), often (≥1/100 to <1/10), infrequently (≥1/1000 to <1/100), rarely (≥1/10 000 to <1/1000), very rare (<1/10,000).

Benign, malignant and unspecified neoplasms (including cysts and polyps):

uncommon - skin melanoma (0.5%/0.3%).

Metabolism and nutrition:

often - decreased appetite (2.4%/0.8%).

Mental disorders:

often - hallucinations (2.9%/2.1%), nightmares (2.1%/0.8%); infrequently - confusion (0.8%/0.5%).

From the nervous system:

very often -
dyskinesia (10.5%/6.2%)
,
often -
dystonia (2.4%/0.8%), carpal tunnel syndrome (1.3%/0%), imbalance (1.6%/0.3%); uncommon - cerebrovascular accident (0.5%/0.3%).

From the cardiovascular system:

infrequently - angina pectoris (0.5%/0%);
often - orthostatic hypotension (3.9%/0.8%)
.

From the digestive system:

often -
abdominal pain (4.2%/1.3%), constipation (4.2%/2.1%), nausea and vomiting (8.4%/6.2%)
, dry mouth (3.4%/1.8%).

For the skin and subcutaneous tissues:

often - rash (1.1%/0.3%).

From the musculoskeletal system:

often - arthralgia (2.4%/2.1%), neck pain (1.3%/0.5%).

Other:

often -
weight loss (4.5%/1.5%)
, falls (4.7%/3.4%).

Parkinson's disease causes hallucinations and confusion. According to post-marketing experience, these symptoms were observed in patients with Parkinson's disease receiving rasagiline.

Serious adverse reactions occurring with concomitant use of SSRIs, SNRIs, tricyclic/tetracyclic antidepressants and MAO inhibitors are well known. In the post-marketing period, cases of serotonin syndrome, manifested by agitation, confusion, rigidity, fever and myoclonus, have been reported in patients concomitantly taking antidepressants/SNRIs and rasagiline.

In clinical studies of rasagiline, co-administration of rasagiline with fluoxetine or fluvoxamine was not permitted. However, the following antidepressants were approved at the indicated doses: amitriptyline not more than 50 mg/day, trazodone not more than 100 mg/day, citalopram not more than 20 mg/day, sertraline not more than 100 mg/day and paroxetine not more than 30 mg/day. In a clinical trial program in which rasagiline was co-administered with tricyclic antidepressants (115 patients) and SSRIs/SNRIs (141 patients), no cases of serotonin syndrome were observed.

Increases in blood pressure, including rare cases of hypertensive crises, have been reported during post-marketing use of rasagiline in patients consuming unspecified amounts of tyramine-rich foods in their diet.

There are known cases of drug interactions with the simultaneous use of MAO inhibitors with sympathomimetic drugs.

In the post-registration period, a case of increased blood pressure was reported in a patient who used the ophthalmic vasoconstrictor tetrahydrozoline and was simultaneously treated with rasagiline.

Impulsive personality disorder

Cases of increased libido, hypersexuality, gambling addiction, compulsive need to buy or acquire, overeating and binge eating have been reported in patients treated with dopamine receptor agonists and/or other dopaminomimetics. A similar pattern of impulsive personality disorder was observed in the post-marketing period in patients taking rasagiline and was characterized by compulsive and impulsive behavior and obsessions.

The newest medicine of our time

The newest medicine of our time, Azilect, is a drug for the treatment of Parkinson's disease, which is a selective inhibitor of monoamine oxidase, which serves as an enzyme that triggers the process of removing the amino group from molecules.

One of the actions of MAO (monoamine oxidase) is the destruction of dopamine, which acts as a neurotransmitter that transmits nerve impulses from cell to cell. Dopamine deficiency, along with the death of nerve cells, provokes the development of Parkinson's disease in people.

The selective inhibitor "Azilect" prevents the destruction of monoamines using the MAO enzyme. Thus, this element preserves dopamine, serotonin, norepinephrine, tryptamine, phenylethylamine and octopamine, causing an increase in their concentrations between nerve and effector cells.

Next, let's talk about the newest medicine of our time, Azilect, in more detail.

Description of the drug

So, the presented remedy is classified as an antiparkinsonian medication. Its active component is a powerful selective irreversible inhibitor of monoamine oxidase, which helps to increase the extracellular content of dopamine in the brain.

During the experiments, scientists proved an increase in the level of this neurotransmitter and an additional increase in dopaminergic activity, which contributes to the therapeutic effects of the drug. The medicine can be well absorbed, and its highest concentration is achieved after thirty minutes.

“Azilect” is the newest medicine of our time; today it is recognized as one of the best medicines against Parkinson’s disease. It is characterized by rapid absorption and rapid onset of action.

This drug is destroyed, as a rule, in the liver and is excreted from the human body in urine.

It differs from alternative drugs in its dosage stability and, importantly, in the virtual absence of many side effects.

Parkinson's disease

The ICD-10 code for Parkinson's disease is G20. It is a slowly developing disease of the central nervous system, characterized by slowness of movement, trembling at rest, and impaired reflexes. The disease is based on damage to the nerve cells of the brain stem. Therapy is carried out throughout the patient's life.

Release form

Azilect tablets are produced in blister packs of ten pieces, in cardboard packages. The pills are flat and round, white in color with the GIL 1 logo and a bevel on one side. The active component of the drug in question is rasagiline mesylate.

Composition of the tablet

One Azilecta tablet contains 1.56 milligrams of rasagiline mesylate. Excipients include corn and pregelatinized starch, colloidal silicon dioxide, as well as mannitol, talc and stearic acid.

The active substance rasagiline is highly active against MAO (monoamine oxidase) and helps increase dopamine levels, reducing the formation of free radicals that are characteristic of Parkinson's disease.

In addition, this drug has a neuroprotective effect that does not block the metabolic processes of biogenic amines that come from food. Thanks to this effect, tyramine-related hypertensive syndrome is not caused.

The drug is good for relieving tremors in Parkinson's disease.

Indications for use

The presented medical product is intended for the treatment of Parkinson's disease in people (according to ICD-10 G20). It can be used for monotherapy, as well as as part of a combination course with Levodopa.

It is worth recalling that you should not choose an antiparkinsonian drug without consulting qualified specialists. The fact is that the effect that this drug produces is, as a rule, very individual, and therefore it should be prescribed exclusively by the treating doctor.

Instructions and application

The described pharmaceutical medicine is prescribed to patients orally in a dosage of 1 milligram once a day with or without Levodopa. The drug can be used regardless of food intake. For elderly people, dose adjustment is usually not required.

Separately, it is worth highlighting patients who suffer from impaired liver function. They should avoid rasagiline if moderate organ failure is diagnosed.

With great caution, therapy is allowed for people with mild liver failure.

But, nevertheless, in such patients, if the condition begins to progress and worsen, treatment with Azilect should be stopped immediately.

As for people with impaired renal function, it should be noted that dosage adjustment is not required for them.

Side effects

When taking the drug, disturbances in the form of anorexia, convulsions, depression, headache, nausea and dizziness may occur. In fact, quite a lot of possible negative manifestations can be provoked, so it is worth considering this issue in more detail:

• The nervous system may react with headaches, depression, dizziness, anorexia, convulsions, and more rarely, cerebrovascular accident may occur.
• The digestive system responds, as a rule, with a decrease in appetite, dyspeptic symptoms, and so on.
• Arthralgia may be noticed in the skeletal and muscular systems along with arthritis and neck pain.
• Dermatologic reactions include vesiculobullous rash combined with contact dermatitis, and skin carcinoma may rarely occur.
• The cardiac and vascular systems react with the appearance of angina. Myocardial infarction is extremely rare.
• Other undesirable manifestations, according to the instructions, include the development of a flu-like syndrome along with fever, leukopenia, rhinitis, general weakness, conjunctivitis, acute disorders of the urinary system and allergic reactions.

If Azilect is taken together with Levodopa, the following pathological symptoms may appear:

• The nervous system sometimes responds with dyskinesia, muscular dystonia, anorexia, unusual dreams, ataxia, and extremely rarely, disturbances in cerebral circulation and confusion occur.
• The digestive system may react with constipation, vomiting, abdominal pain, or dry mouth.
• The work of the skeletal and muscular system is accompanied by arthralgia, pain in the neck and tenosynovitis.
• Dermatological reactions include rash and, extremely rarely, skin melanoma.
• From the cardiac and vascular systems, postural hypotension is possible. Quite rarely, angina pectoris occurs in this case.
• Other undesirable effects include accidental falls, weight loss and allergic reactions.

To date, there have been two reports of rhabdomyolysis and problems in the secretion of antidiuretic hormones. Both cases were observed in post-marketing trials without placebo control. The relationship between these complications and the use of rasagiline is difficult to determine.

Overdose

Symptoms of an overdose of the drug "Azilect" are similar to those with an excess of non-selective MAO inhibitors. In this case, patients may experience arterial and postural hypotension. As part of treatment, doctors resort to gastric lavage, activated charcoal and symptomatic therapy. There is no specific antidote.

special instructions

It is recommended to avoid the combined use of rasagiline with Fluoxetine or Fluvoxamine. The total break between the start and the start of treatment with Azilect should be at least five weeks. And between the abolition of rasagiline and the start of Fluvoxamine therapy, there should be at least fourteen days.

Manufacturers of the drug do not recommend taking rasagiline simultaneously with dextromethorphan or with sympathomimetics, such as those included in oral and nasal vasoconstrictor medications or cold medications that contain ephedrine or pseudoephedrine. As noted earlier, treatment with Azilect should be initiated with great caution among patients who suffer from liver damage.

It is important, among other things, to take into account that the main component of the drug, rasagiline, can provoke drowsiness in patients during the day, and sometimes, especially in the case of simultaneous use with alternative dopaminergic drugs, it is even possible to fall asleep while performing a particular activity.

Given this, patients should be warned about the need to exercise caution when operating vehicles or other machinery. And it is best to avoid such actions altogether during the treatment period.

Reviews from Parkinson's patients about Azilect

You can read positive comments about the drug on the Internet. People talk about their condition improving. It is worth noting that reviews of the effectiveness of the drug are left by patients belonging to different age groups. Thus, most reports confirm the effectiveness of the drug in question.

But there are also negative comments in which patients write that in many cases, especially in the first few months of use, they experienced the development of various side effects, which, however, subsequently went away.

Doctors, in turn, comment on this by saying that rare side effects can be a complication of the underlying disease; such consequences are often found among those suffering from the disease and who do not use Azilect to treat parkinsonism syndrome. When taking this medication, the dose of the drug is not increased, and adverse reactions are less common than during therapy with alternative antiparkinsonian drugs.

Can I take this drug at night?

Many people are interested in the question of whether it is permissible to use the newest modern medicine, Azilect, before bedtime. The answer in this case is positive. The main condition is that this medicine must be taken every day, preferably at the same time.

Price

The price of Azilect largely depends on the pricing policy of the pharmacy chain in which it is sold. As a rule, the average today is 5.5 thousand rubles per package. In this regard, it is necessary to take into account that this medicine is not cheap, and for targeted treatment you must be prepared to spend a lot of money. This drug is produced in Israel.

"Azilect": INN

The international name (INN) of the drug in question is the name Rasagiline (rasagiline). The generic definition of the active ingredient provides basic information about a drug in the international pharmaceutical market.

The fact is that very often medications with the same active ingredient are produced under different trade names, that is, in fact, they are the same drug, but produced by different manufacturers.

It is the INN that provides doctors with the opportunity to navigate a large number of all kinds of medications that are sold today all over the world.

Source: https://FB.ru/article/474315/noveyshee-lekarstvo-sovremennosti-azilekt-deystvuyuschee-veschestvo-forma-vyipuska-pokazaniya-instruktsiya-po-primeneniyu-otzyivyi-bolnyih

Drug interactions

Concomitant use of rasagiline with other MAO inhibitors, incl. with medications and food supplements containing St. John's wort is contraindicated, because there is a risk of developing a severe hypertensive crisis due to non-selective MAO inhibition.

The development of serious adverse reactions has been reported with the simultaneous use of pethidine and MAO inhibitors, incl. selective MAO-B inhibitors. Concomitant use of rasagiline and pethidine is contraindicated.

Interactions between MAO inhibitors and sympathomimetic drugs have been reported when used concomitantly. Due to the MAO-inhibiting properties of rasagiline, concomitant use of rasagiline with sympathomimetics, such as decongestants or oral or nasal complex cold products containing ephedrine or pseudoephedrine, is not recommended.

Interactions between dextromethorphan and non-selective MAO inhibitors have been reported when used concomitantly. Due to the property of rasagiline to inhibit MAO, the simultaneous use of rasagiline with dextromethorphan and combination drugs containing it is not recommended.

Concomitant use of rasagiline with fluoxetine or fluvoxamine should be avoided. The interval between discontinuation of rasagiline and initiation of therapy with these drugs should be at least 14 days. At least 5 weeks should elapse after stopping treatment with fluoxetine or fluvoxamine (long half-life) and starting treatment with rasagiline.

Information on the simultaneous use of SSRIs/SNRIs and rasagiline in clinical studies is presented in the “Side Effects” section.

The development of serious adverse reactions has been reported with the simultaneous use of SSRIs, SNRIs, tricyclic and tetracyclic antidepressants with MAO inhibitors.

Due to the property of rasagiline to inhibit MAO, caution must be exercised when used simultaneously with SSRIs, SNRIs, tricyclic and tetracyclic antidepressants.

In patients with Parkinson's disease receiving long-term levodopa as adjuvant therapy, levodopa had no significant effect on the clearance of rasagiline.

In vitro studies have shown that the main enzyme involved in the metabolism of rasagiline is the CYP1A2 isoenzyme. The simultaneous use of ciprofloxacin and rasagiline increases the AUC of the latter by 83%.

The simultaneous use of rasagiline and theophylline (a substrate of the CYP1A2 isoenzyme) did not affect the pharmacokinetics of either of them. Thus, potent inhibitors of the CYP1A2 isoenzyme may alter the plasma concentrations of rasagiline and require careful simultaneous use.

There is a risk that due to the induction of the CYP1A2 isoenzyme in smoking patients, the concentration of rasagiline in the blood plasma may decrease.

In vitro studies have shown that rasagiline at a concentration of 1 mcg/ml (equivalent to a concentration exceeding 160 times the mean Cmax (5.9-8.5 ng/ml) after repeated administration of 1 mg rasagiline to patients with Parkinson's disease) does not inhibit the isoenzymes CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4 and CYP4A. This indicates that therapeutic concentrations of rasagiline are not likely to be affected clinically by substrates of these isoenzymes.

With simultaneous use of entacapone with rasagiline, the clearance of the latter increased by 28%.

Clinical studies of the interaction of tyramine and rasagiline in volunteers and patients with Parkinson's disease (0.5-1 mg/day rasagiline or placebo as adjunctive therapy to levodopa for 6 months without restriction of tyramine intake) showed that there is no interaction between rasagiline and tyramine, and, rasagiline can be used safely without dietary tyramine restriction.

What is the novelty and advantage of the drug?

In the fight against Parkinson's disease, Azilect is the latest medicine of our time. The uniqueness of this medication lies in its high therapeutic effectiveness, due to which the first clinical improvements occur in the shortest possible time and with a low concentration. The MAO group itself has been known since the 80s of the 20th century, when drugs based on non-selective monoamine oxidase inhibition were used to treat depression.

However, in the treatment of parkinsonism, the effect on both subtypes led to the development of a large number of adverse reactions, which often not only did not improve the patient’s condition, but also led to severe cognitive impairment.

Advantages of the drug

Selective and irreversible inhibition of MAO-B helps maintain the level of endogenous dopamine, and razalgin directly increases the tropism of dopaminergic structures to this neurotransmitter. When administered simultaneously with Levodopa, pilyule_nervi-223 razalgan has two effects at once - an increase in dopamine in the intersynaptic cleft and an increase in the amount of extracellular dopamine.

The above actions contribute not only to reducing the rate of progression of the pathology, but also to the rapid relief of parkinsonian syndromes.

special instructions

The simultaneous use of Azilect and fluoxetine or fluvoxamine should be avoided. The interval between stopping fluoxetine and starting treatment with Azilect should be 5 weeks, and 14 days between stopping Azilect and starting fluoxetine or fluvoxamine.

Cases of impulsive personality disorder have been reported in patients treated with dopamine receptor agonists and/or other dopaminomimetics. The same disorders were observed in the post-registration period in patients taking the drug Azilect. Patients should be monitored for the possibility of developing impulsive personality disorder. Patients and caregivers should be informed of the potential for behavioral disturbances to develop in patients taking Azilect, including compulsive behavior, obsessions, gambling addiction, increased libido, hypersexuality, impulsive behavior, and compulsive buying or acquiring.

Concomitant use of Azilect with dextromethorphan, sympathomimetics or complex anti-cold medications for oral or nasal use containing ephedrine or pseudoephedrine is not recommended.

There is evidence that Parkinson's disease, and not the use of any drug, incl. Azilect is a risk factor for the development of skin cancer, in particular melanoma. It is necessary to warn the patient about the need to consult a doctor if any pathological changes in the skin appear.

It must be borne in mind that symptoms such as hallucinations and confusion that appear during treatment with Azilect can be considered both as a manifestation of Parkinson's disease and as adverse reactions of the drug Azilect.

Azilect should be used with caution in patients with mild hepatic impairment. The use of Azilect in patients with moderate liver dysfunction is not recommended. If the severity of liver failure changes from mild to moderate, the use of Azilect should be discontinued.

Impact on the ability to drive vehicles and operate machinery

The effect of rasagiline on the ability to drive vehicles and operate machinery has not been studied. However, given the possibility of significant side effects from the central nervous system, during treatment with Azilect, patients should be informed about the need to be careful when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions until they are sure that the drug does not have a negative effect.

Indications and instructions for use

Azilect is prescribed to patients with idiopathic Parkinson's disease both as monotherapy and in combination with Levodopa to enhance its effect. It is important to read the instructions before starting to take Azilect, and if you have any questions, contact your doctor.

Restrictions

The drug is contraindicated in patients with hypersensitivity reactions to the components of Azilect. The drug is also prohibited when taking other MAO inhibitors simultaneously, as this can lead to pronounced side effects and “cheese syndrome”. A somatic contraindication to taking MAO-B inhibitors is severe liver failure.

"Cheese Syndrome"

Clinical studies have not shown a teratogenic effect on the fetus in animals; however, there is no data on the use of rasalgin in pregnant women. What is known is that it is capable of inhibiting the synthesis of prolactin, and as a result lead to hypogalactia. Therefore, you should stop breastfeeding during treatment with razalgin. Clinical studies have not been conducted in children due to the fact that the pathology is not typical for this age group.

Dosage

The drug is prescribed in a daily dosage of 1 mg orally, which is taken in one dose. The dose does not change even with simultaneous treatment with Levodopa.

The effect of razalgin and its metabolization directly depends on the state of the hepatobiliary system. Therefore, you should carefully consider the condition of patients with concomitant first-degree liver failure; for moderate and severe forms there is a strict contraindication for use.

Azilect can be taken regardless of meals. However, it is worth considering the fact that the presence of a large number of fatty foods on the menu slows down the absorption of the active substance.

Precautionary measures

When taking antidepressants, you should completely stop taking razalgin. This is especially true for other MAO inhibitors and selective serotonin and dopamine inhibitors, since their interaction uncontrollably increases side effects: disturbance and confusion, muscle rigidity, myoclonic spasms and chills.

The high hepatotoxicity of Azilect should also be taken into account when prescribing antibiotics, the metabolism of which requires the normal functioning of the cytochrome P-450 system and its coenzymes. These drugs include derivatives of Ciprofloxacin.

Features of taking the drug

Long-term therapy with razalgin can lead to mental disorders. This is manifested by increased gambling, mania, and hypersexuality. Therefore, careful monitoring of such patients by a psychiatrist is necessary.

Taking Azilect may cause a feeling of drowsiness during the day and even lead to falling asleep. At the same time, the adequate reaction to surrounding events decreases, and the basic reflexes become dulled. Therefore, it is recommended to refrain from driving vehicles for the entire period of therapy.

Special attention should be paid to smoking patients. It is known that tobacco smoke causes the induction of isoenzyme structures of cytochrome P-450, which leads to a decrease in the absolute concentration of Azilect in tissues and organs.

Pregnancy and lactation

There are no data on the use of rasagiline in pregnant women. Results from animal studies do not indicate any direct or indirect adverse effects on pregnancy, embryofetal development, childbirth or postnatal development. If it is necessary to use rasagiline in pregnant women, it is necessary to balance the expected benefit for the mother and the risk to the fetus.

Experimental evidence suggests that rasagiline inhibits prolactin secretion and may thus suppress lactation. There is no information about the penetration of rasagiline into breast milk. If it is necessary to use rasagiline during breastfeeding, it is necessary to compare the expected benefits for the mother and child.