Buy Azilect® pills 1 mg 100 pcs
  • Buy Azilect® pills 1 mg 100 pcs

Azilect® [Rasagiline]

Teva
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2019-09-19
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Clinical Pharmacology

inhibitory MAO-B, anti-parkinsonian.

Rasagiline is a selective, irreversible inhibitor of MAO type B, an enzyme that 80% determines the activity of MAO in the brain and the metabolism of dopamine. Rasagiline 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 CNS, 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 non-selective MAO inhibitors, the drug in therapeutic doses does not block the metabolism of biogenic amines ingested with food (for example, tyramine), and therefore does not cause tyramine-related hypertensive syndrome ("cheese effect").

Indications

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

Composition

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

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Azilect® [Rasagiline]

Dosage and Administration

Orally, regardless of the meal, at a dose of 1 mg 1 time per day, both in monotherapy and in combination with levodopa.

Elderly patients

Dose adjustment in elderly patients is not required.

Patients with impaired liver function

The use of rasagiline in patients with moderate and severe liver failure is contraindicated.

When applying rasagiline in patients with mild hepatic impairment, caution should be exercised. If during the treatment with rasagiline progression of liver failure to a moderate degree is noted, the use of the drug should be discontinued.

Patients with renal failure

Dose adjustment is not required.

Adverse reactions

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

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 discontinuation of rasagiline and initiation of therapy with these drugs should be at least 14 days;
  • moderate or severe liver failure (Child-Pugh);
  • combined therapy with decongestants, sympathomimetics (including those containing them), dextromethorphan.
  • pheochromocytoma;
  • age under 18;
  • pregnancy;
  • lactation period (risk of inhibition of milk products against the background of inhibition of prolactin formation).

Drug interactions

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 prescribed simultaneously with other inhibitors of this enzyme due to the risk of a hypertensive crisis. The combined use of rasagiline with drugs whose mechanism of action includes inhibition of the reverse neuronal seizure of serotonin (fluoxetine, fluvoxamine, etc.), tricyclic and tetracyclic antidepressants, MAO inhibitors, should be avoided, since this may cause the development of a “serotonergic syndrome” that manifests itself in confusion , hypomania, motor restlessness, chills, tremor, diarrhea.If necessary, use by patients receiving rasagiline, such drugs - they are used with caution.
The combined use of rasagiline with sympathomimetic drugs, including ephedrine, pseudoephedrine, contained in preparations for the treatment of rhinitis or the common cold (decongestants) is also not recommended. In addition, the appointment of rasagiline with the analgesic / antitussive drug dextromethorphan and the combined agents containing it are not recommended. Due to the fact that the cytochrome P450 1A2 isoform of the enzyme (CYP1A2) participates in rasagiline metabolism, active inhibitors of this enzyme (for example, ciprofloxacin) can increase the plasma concentration of the drug, which determines caution when combining such drugs with rasagiline.
In patients with Parkinson's disease, the use of levodopa preparations does not affect the clearance of rasagiline.

Pregnancy and Lactation

Data on the use of rasagiline in pregnant women are not available. The results of animal studies do not indicate the presence of direct or indirect adverse effects on pregnancy, fetal development, childbirth and postnatal development. If necessary, the use of rasagiline in pregnant women is necessary to correlate the expected benefits to the mother and the risk to the fetus.

According to experimental data, rasagiline inhibits prolactin secretion and, thus, can suppress lactation. Information about the penetration of rasagilin into breast milk is missing.

If necessary, the use of rasagiline during breastfeeding is necessary to correlate the expected benefits for mother and child.

Special instructions

The use of rasagiline in the recommended therapeutic dose does not cause a "tyramine syndrome" ("cheese effect"), which allows patients to use food containing meaningful amounts of tyramine (cheese, chocolate, etc.) without any restrictions. The study of the effect of rasagiline on driving a car and controlling other mechanisms was not conducted.

Overdosage

Symptoms of drug overdose are similar to those in overdose with non-selective MAO inhibitors (arterial hypertension, postural hypotension, etc.).
Treatment: There is no specific antidote. Gastric lavage, Activated charcoal intake, symptomatic therapy.

  • Brand name: Azilect®
  • Active ingredient: Rasagiline
  • Dosage form: pills of white or almost white color, round, flat-cylindrical, with a facet, with an engraving "GIL 1" on one side of the tablet.
  • Manufacturer: Teva
  • Country of Origin: Israel

Studies and clinical trials of Rasagiline (Click to expand)

  1. Rasagiline, a monoamine oxidase-B inhibitor, protects NGF-differentiated PC12 cells against oxygen-glucose deprivation
  2. Irreversible Inhibition of Monoamine Oxidase B by the Antiparkinsonian Medicines Rasagiline and Selegiline: A Computational Study
  3. Irreversible Inhibition of Monoamine Oxidase B by the Antiparkinsonian Medicines Rasagiline and Selegiline: A Computational Study (Eur. J. Org. Chem. 32/2011)
  4. Rasagiline: Neurodegeneration, neuroprotection, and mitochondrial permeability transition
  5. Double-blind, randomized, controlled trial of rasagiline as monotherapy in early Parkinson's disease patients
  6. Rasagiline improves quality of life in patients with early Parkinson's disease
  7. Effects of tyramine administration in Parkinson's disease patients treated with selective MAO-B inhibitor rasagiline
  8. Rasagiline improves freezing in a patient with primary progressive freezing gait
  9. A randomized, double-blind, placebo-controlled, delayed start study to assess rasagiline as a disease modifying therapy in Parkinson's disease (the ADAGIO study): Rationale, design, and baseline characteristics
  10. Long-term outcome of early versus delayed rasagiline treatment in early Parkinson's disease
  11. Rasagiline-induced spontaneous ejaculation
  12. Rasagiline-induced serotonin syndrome
  13. The effects of rasagiline on cognitive deficits in Parkinson's disease patients without dementia: A randomized, double-blind, placebo-controlled, multicenter study
  14. Reversible Pisa syndrome in patients with Parkinson's disease on rasagiline therapy
  15. Explaining ADAGIO: A critical review of the biological basis for the clinical effects of rasagiline
  16. Multifunctional neuroprotective derivatives of rasagiline as anti-alzheimer’s disease drugs
  17. Validated LC–MS/MS method for quantitative determination of rasagiline in human plasma and its application to a pharmacokinetic study
  18. Development and validation of a reverse phase liquid chromatography method for the quantification of rasagiline mesylate in biodegradable PLGA microspheres
  19. Parkinson : rasagiline, entre espoirs et interrogations
  20. Transfection-enforced Bcl-2 overexpression and an anti-Parkinson drug, rasagiline, prevent nuclear accumulation of glyceraldehyde-3-phosphate dehydrogenase induced by an endogenous dopaminergic neurotoxin, N-methyl(R)salsolinol
  21. Mitochondrial permeability transition mediates apoptosis induced by N-methyl(R)salsolinol, an endogenous neurotoxin, and is inhibited by Bcl-2 and rasagiline, N-propargyl-1(R)-aminoindan
  22. Rasagiline ethanedisulfonate: an inhibitor for monoamine oxygenase B (MAOB)
  23. From a Parkinson's disease expert: Rasagiline and the Future of Therapy
  24. Rasagiline alone and in combination with riluzole prolongs survival in an ALS mouse model

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