Azilect tablets 1mg, No. 30

• Monotherapy or combination therapy for Parkinson's disease (with levodopa drugs).

Rasagiline is administered orally at a dose of 1 mg once a day, both in monotherapy and during the use of levodopa, for a long time.

Taking the drug does not depend on food intake.

active substance: rasagiline mesylate - 1.56 mg (equivalent to 1 mg of rasagiline base)

excipients: mannitol, colloidal silicon dioxide, corn starch, pregelatinized corn starch, stearic acid, talc

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

• concomitant therapy with pethidine or other MAO inhibitors, fluoxetine and fluvoxamine. The interval between the cancellation of rasagiline and the initiation of therapy with these drugs should be at least 14 days;

• moderate or severe hepatic impairment (Child-Pugh);

• joint therapy with decongestants, sympathomimetics (including drugs containing them), dextromethorphan.

• pheochromocytoma;

• age under 18;

• pregnancy;

• lactation period (the risk of inhibition of milk production against the background of inhibition of prolactin formation).

With care
Mild liver failure; co-administration with selective serotonin reuptake inhibitors, tricyclic and tetracyclic antidepressants, active inhibitors of CYP1A2.

Trade name of the drug : Azilekt

International non-proprietary name : Rasagiline

Dosage form : tablets

Composition

active substance: rasagiline mesylate 1.56 mg (equivalent to 1 mg of rasagiline base)

excipients: mannitol, colloidal silicon dioxide, corn starch, pregelatinized corn starch, stearic acid, talc

Description

White or almost white round, flat-cylindrical tablets with a bevel. One side of the tablet is engraved with 'GIL 1'

Pharmacotherapeutic group : antiparkinsonian agent - MAO inhibitor

ATX code : N04BD02

Pharmacological properties

Pharmacodynamics
Rasagiline is a selective irreversible inhibitor of monoamine oxidase type B (MAO-B), an enzyme that determines 80% of monoamine oxidase activity in the brain and dopamine metabolism. It is 30-80 times more active in relation to MAO-B than to another type of this enzyme, MAO-A. As a result of the inhibitory effect of the drug on MAO-B in the central nervous system, the level of dopamine increases, the formation of toxic free radicals decreases, the excessive formation of which is observed in patients with Parkinson's disease. Rasagiline also has a neuroprotective effect. Unlike indiscriminate 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-related hypertensive syndrome ('cheese effect').

Pharmacokinetics
Razagiline is rapidly absorbed after oral administration; its maximum concentration in blood plasma (Cmax) 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 to reach the maximum concentration of rasagiline in the blood, however, with the consumption of fatty foods, Cmax and the area under the drug concentration curve (AUC) decrease by 60% and 20%, respectively. The pharmacokinetics of the drug is linear in the dose range of 0.5-2 mg. The connection with blood plasma proteins ranges from 60 to 70%.
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 2 other metabolites - 3-hydroxy-N-propargyl-1 aminoindane and 3-hydroxy-1-aminoindane. The metabolism of the drug is carried out with the participation of the CYP 1A2 isoform of the cytochrome P-450 system. Rasagiline is excreted mainly 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. The half-life is 0.6-2 hours. The pharmacokinetic parameters of rasagiline practically do not change in patients with mild to moderate renal failure. With mild hepatic impairment, there may be an increase in the values ??of the AUC and Cmax parameters by 80% and 38%,and in patients with moderate hepatic dysfunction, these parameters reach more than 500% and 80%, respectively.

Indications for use

• Monotherapy or combination therapy for Parkinson's disease (with levodopa drugs).

Contraindications

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

• concomitant therapy with pethidine or other MAO inhibitors, fluoxetine and fluvoxamine. The interval between the cancellation of rasagiline and the initiation of therapy with these drugs should be at least 14 days;

• moderate or severe hepatic impairment (Child-Pugh);

• joint therapy with decongestants, sympathomimetics (including drugs containing them), dextromethorphan.

• pheochromocytoma;

• age under 18;

• pregnancy;

• lactation period (the risk of inhibition of milk production against the background of inhibition of prolactin formation).

With care
Mild liver failure; co-administration with selective serotonin reuptake inhibitors, tricyclic and tetracyclic antidepressants, active inhibitors of CYP1A2.

Method of administration and dosage

Rasagiline is administered orally at a dose of 1 mg once a day, both in monotherapy and during the use of levodopa, for a long time.

Taking the drug does not depend on food intake.

Side effect

The listed side effects occurred with a frequency of more than 1/100, side effects occurring with a frequency of 1/100 - 1/1000 are indicated as rare.
With rasagiline monotherapy:
From the nervous system: headaches, depression, dizziness, anorexia, convulsions, rarely: cerebrovascular accident.
From the gastrointestinal tract: decreased appetite, dyspeptic symptoms.
From the musculoskeletal system : arthralgia, arthritis, pain in the neck.
On the part of the skin: vesiculobullous rash, contact dermatitis; rarely: skin carcinoma.
From the side of the cardiovascular system: angina pectoris, rarely: myocardial infarction.
Others:fippa-like syndrome, fever, leukopenia, rhinitis, general weakness, conjunctivitis, acute disorders of the urinary system, allergic reactions.
When used together with levodopa:
From the nervous system: dyskinesia, muscular dystopia, anorexia, unusual dreams, ataxia, rarely: cerebrovascular accident.
From the organs of the gastrointestinal tract: constipation, vomiting, abdominal pain, dry mouth.
From the musculoskeletal system: arthralgia, pain in the neck, tendosynovitis.
From the side of the skin: rash, rarely: skin mslanoma.
From the side of the cardiovascular system: postural hypotension, rarely: angina pectoris.
Others:accidental falls, weight loss, allergic reactions.
There are two reports of the development of rhabdomyolysis and impaired secretion of antidiuretic hormone. Both cases were recorded during post-registration studies without placebo control, developed against the background of a fall and subsequent prolonged immobilization. The relationship between these complications and the use of rasagiline cannot be determined.

Overdose

Symptoms of an overdose of the drug are similar to those of an overdose with indiscriminate MAO inhibitors (arterial hypertension, postural hypotension, etc.).
Treatment: There is no specific antidote. Gastric lavage, intake of activated charcoal, symptomatic therapy.

Interaction with other medicinal products

Due to the fact that the mechanism of action of rasagiline is associated with inhibition of MAO, as is the case with other drugs of a similar mechanism of action, it cannot be administered simultaneously with other inhibitors of this enzyme due to the risk of developing a hypertensive crisis. Avoid the combined use of rasagiline with drugs, the mechanism of action of which includes inhibition of the reverse neuronal uptake of serotonin (fluoxetine, fluvoxamine, etc.), tricyclic and tetracyclic antidepressants, MAO inhibitors, since this may lead to the development of 'serotonergic syndrome', manifested in confusion , hypomanic state, motor restlessness, chills, tremors, diarrhea. If it is necessary to use similar drugs by patients receiving rasagiline, they should be used with caution.
The combined use of rasagiline with sympathomimetic drugs, including ephedrine, pseudoephedrine, contained in preparations for the treatment of rhinitis or colds (decongestants) is also not recommended. In addition, the administration of rasagiline with the analgesic / antitussive drug dextromethorphan and combination agents containing it is not recommended. Due to the fact that the isoform of the enzyme cytochrome P450 1A2 (CYP1A2) is involved in the metabolism of rasagiline, active inhibitors of this enzyme (for example, ciprofloxacin) can increase the concentration of the drug in the blood plasma, which determines caution when combining such drugs with rasagiline.
In patients with Parkinson's disease, the use of levodopa drugs does not affect the clearance of rasagiline.

special instructions

The use of rasagiline in the recommended therapeutic dose does not cause 'tyramine syndrome' ('cheese effect'), which allows patients to use foods containing significant amounts of tyramine (cheeses, chocolate, etc.) in their food without restrictions. The study of the effect of rasagiline on driving a car and controlling other mechanisms has not been carried out.

Release form

Tablets 1 mg. There are 10 tablets in a blister. 1, 3, 10 blisters with instructions for use in a cardboard box.

Shelf life

3 years. Do not use after the expiration date printed on the package.

Storage conditions

At a temperature not higher than 25 ? C. Keep out of the reach of children.

Conditions of dispensing from pharmacies

On prescription.