The latest modern drug Azilekt 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 removal of amino groups from molecules. One of the actions of MAO (monoamine oxidase) is the destruction of dopamine, which acts as a neurotransmitter, transmitting nerve impulses from cell to cell. Dopamine deficiency along with nerve cell death provokes the development of Parkinson's disease in people. The selective inhibitor Azilekt prevents the destruction of monoamines using the enzyme MAO. Thus, this element retains dopamine, serotonin, norepinephrine, tryptamine, phenylethylamine and octopamine, causing an increase in their concentrations between nerve and effector cells. Next, we’ll talk about the latest modern medicine “Azilekt” in more detail.
Description of the drug
So, the presented remedy is referred to as antiparkinsonian medicines. Its active ingredient is a powerful selective irreversible monoamine oxidase inhibitor, which contributes to an increase in the extracellular content of dopamine in the brain.
In the course of experiments, scientists have proved an increase in the level of this neurotransmitter and an additional increase in dopaminergic activity, which contributes to the therapeutic effect of the drug. The medicine can be well absorbed, and its maximum concentration is reached after thirty minutes.
Azilekt 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 exposure. This remedy is destroyed, as a rule, in the liver and is excreted from the human body with urine. It differs from alternative drugs in the stability of the dosage and, importantly, in the absence of many side effects.
Parkinson's disease
The ICD-10 code for Parkinson's disease is G20. This is a slowly developing disease of the central nervous system, characterized by slow motion, trembling at rest and impaired reflexes. At the heart of the disease is damage to the nerve cells of the brain stem. Therapy is carried out throughout the life of the patient.
Release form
Azilekt tablets are produced in a blister pack of ten pieces, in cardboard packages. The pills are flat and round, have a white color with the GIL 1 logo and a chamfer on one side. The active component of the drug in question is rasagiline mesylate.
Tablet composition
One tablet of Azilekt contains 1.56 milligrams of rasagiline mesylate. Excipients are corn and pregelatinized starch, colloidal silicon dioxide, as well as mannitol, talc and stearic acid.
pharmachologic effect
The active substance rasagiline is highly active in relation to MAO (monoamine oxidase) and helps to 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 metabolism of biogenic amines that come from food. Due to this effect, tyramine-induced hypertensive syndrome is not caused. The drug relieves tremor in Parkinson's disease.
Pharmacokinetics
The active component in tablets "Azilekt" rasagiline is rapidly absorbed in the body after ingestion. The maximum concentration in the blood plasma is reached, as a rule, after half an hour. The absolute bioavailability of the drug after a single use is about thirty-six percent. It is worth emphasizing that foods do not affect the time to reach the highest rasagiline level in the blood, however, with the use of fatty foods, this figure may decrease by twenty percent. The pharmacokinetics of the drug is linear in the range of doses from 0.5 to 2 milligrams. Linking blood proteins ranges from sixty to seventy percent.
Indications for use
The presented medical device 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 combined course with Levodopa.
It is worth recalling that you should not choose an antiparkinsonian drug without consulting with qualified specialists. The fact is that the effect that turns out to be this drug is usually very individual, and therefore it should be prescribed exclusively by the attending doctor.
Contraindications
According to the instructions for use with Azilekt, the drug is not suitable for use in therapy if the following diseases and conditions are present in patients:
- Against the background of concomitant treatment with “Petidine” or other MAO inhibitors (it is worth noting that the interval between the cancellation of “Azilect” and the start of the course of therapy with this drug should be at least two weeks).
- In severe or moderate liver failure.
- As part of joint therapy with sympathomimetics (whether it be pseudoephedrine or ephedrine), as well as with other decongestants and with pharmaceutical preparations that contain them. Contraindications "Azilekt" should be strictly observed.
- With pheochromocytoma.
- In childhood and adolescence (up to eighteen years old).
- Pregnancy, as well as the period of lactation, is also a ban on the use of Azilekt, since there is a risk of inhibition of milk production due to inhibition of prolactin production.
- With increased sensitivity to rasagiline or one of the components of the pharmaceutical agent in question.
With great caution, an antiparkinsonian drug is prescribed in case of mild liver failure, as with combined use with selective inhibitors (Fluoxetine and Fluvoxamine), tetracyclic and tricyclic antidepressants.
Instruction and use
The described pharmaceutical drug 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 the reception of products. For older people, dose adjustment is usually not required.
Separately, it is worth highlighting patients who suffer from impaired liver function. They need to avoid the use of razagiline in the event that an average degree of insufficiency of this organ is diagnosed. With great caution, it is allowed to carry out therapy for people with mild liver failure. But, nevertheless, in such cases, in the case of the onset of progression and aggravation of the condition, 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, violations may be observed in the form of anorexia, convulsions, depression, headache, nausea and dizziness. In fact, quite a lot of possible negative manifestations can be provoked, so you should consider this issue in more detail:
- The nervous system can react with headaches, depression, dizziness, anorexia, cramps, more rarely, a disturbance in the process of cerebral circulation is possible.
- The digestive system responds, as a rule, with a decrease in appetite, dyspeptic symptoms, and so on.
- Arthralgia along with arthritis and neck pain can be seen in the work of the bony and muscle systems.
- Dermatological reactions include a vesiculobullous rash in combination with contact dermatitis, and skin carcinoma can rarely occur.
- The cardiac and vascular systems react with the appearance of angina pectoris. 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.
In the event that Azilekt 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 a disturbance in cerebral circulation and confusion is extremely rare.
- The digestive system can respond by constipation, vomiting, abdominal pain, or dry mouth.
- The work of the bone and muscle system is accompanied by arthralgia, pain in the neck and tendosynovitis.
- Dermatological reactions include rash, extremely rarely melanoma of the skin.
- From the cardiac and vascular systems, postural hypotension is possible. Rarely, in this case, angina pectoris occurs.
- Other unwanted effects include accidental falls along with weight loss and allergic reactions.
To date, two reports have been recorded about the occurrence of rhabdomyolysis and problems in the secretion of antidiuretic hormones. Both cases were seen as part of post-registration tests without placebo control. The relationship between these complications and the use of razagilin is problematic to determine.
Overdose
Symptoms of an overdose of the drug "Azilekt" is similar to that with an overabundance of non-selective MAO inhibitors. In this case, patients may experience arterial and postural hypotension. As part of the treatment, doctors resort to gastric lavage, taking activated charcoal and symptomatic therapy. There is no specific antidote.
special instructions
It is recommended to avoid the combined use of razagilin with Fluoxetine or Fluvoxamine. The total break between the discontinuation of the drug “Fluoxetine” and the start of treatment with “Azilect” should be at least five weeks. And between the withdrawal of razagilin and the start of Fluvoxamine therapy, this should be at least fourteen days.
Manufacturers of the drug are not advised to take razagiline with Dextromethorphan or with sympathomimetics, for example, those that are included in oral and nasal vasoconstrictor drugs or cold medicines that contain ephedrine or pseudoephedrine. As noted earlier, with great caution should begin treatment with Azilekt 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 the daytime in patients, and sometimes, especially when used with alternative dopaminergic drugs, it is even possible to fall asleep in the process of performing one or another activity.
Given this, patients should be warned about the need to exercise caution while driving or using other mechanisms. And it is best to abandon such actions during the treatment period.
Reviews of patients with Parkinson about "Azilekt"
On the Internet you can read positive comments about the drug. People talk about improvement. It is worth noting that patients related to different age groups leave reviews on the effectiveness of the drug. 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 admission, they observed the development of various side effects, which, however, subsequently passed.
Doctors, in turn, comment on this with the fact that rare side effects can be a complication of the underlying disease, such consequences are often found among those suffering from the disease and not using Azilekt to treat Parkinson's syndrome. If this medicine is taken, the dose of the drug does not increase, and adverse reactions are less common than during treatment with alternative anti-Parkinsonian drugs.
Can I take this medication at night?
Many are interested in the question of whether the use of the latest Azilekt modern medicine is allowed before bedtime. The answer in this case is positive. The main condition is that you need to drink this medicine every day, preferably at the same time.
Cost
The price of Azilekt is largely dependent on the pricing policy of the pharmacy chain in which it is implemented. As a rule, on average today it is 5.5 thousand rubles per package. In this regard, it must be borne in mind that this medicine is not cheap, and for targeted treatment it is necessary to be prepared for serious expenses. This drug is produced in Israel.
Azilekt: INN
The international name (INN) of the drug in question is the name Rasagiline (razagilin). The generic definition of the active ingredient provides basic drug information in the international pharmaceutical market. The fact is that very often medicines with the same active ingredient are released under different trade names, that is, in fact, this is the same drug, but produced by different manufacturers. It is INN that provides doctors with the opportunity to navigate a large number of all kinds of medicines that are currently sold around the world.