In the article, we consider MAO inhibitors, what applies to them?
The pharmacological properties of this group of drugs suggest the division of such drugs into reversible selective, non-selective, irreversible and irreversible selective. Irreversible non-selective MAO inhibitors are similar in structure to iproniazides, they normalize the general condition of patients with depression and fight angina attacks. Reversible selective - have psycho-energizing and antidepressant effects, actively inhibit deamination of norepinephrine and serotonin. Irreversible selective - have an antiparkinsonian effect, participate in the metabolism of catecholamines and dopamine. The list of MAO irreversible nonselective inhibitors that are used to treat parkinsonism includes:
- "Fenelzin";
- "Isocarboxazide";
- Iproniazide;
- Nialamide;
- "Tranylcypromine."
Selective irreversible inhibitors of MAO "Selegilin" refers. Irreversible non-selective drugs are prescribed in the treatment of depression and chronic alcoholism, and selective irreversible drugs are used in the treatment of parkinsonian pathologies. According to the instructions for use, "Selegiline" is a medication intended for the treatment of symptoms of Parkinson's disease. One of the main categories of medicines that are used in the treatment of this disease is considered to be Levodopa and its analogues. However, against the background of prolonged use of these drugs, a “wear-out effect” occurs, which manifests itself in the form of the termination of the drug long before taking a new dose, exacerbation of pathological symptoms, etc.
To prevent such complications, neurologists often prescribe psychostimulants from the class of monoamine oxidase inhibitors (MAOs), which are used to treat depression. MAO is a biological compound that regulates the breakdown of one of the main neurotransmitters of the human body - dopamine. With a lack of this substance in the synapses located in the main structures of the central nervous system, information is transmitted in a distorted form to the cholinergic underlying synapses. Acetylcholine provides the subsequent distribution of pathological signals, which provokes motor disorders in patients. The point of application of the drug "Selegiline" is the prolongation of exposure to dopamine. At the same time, the medication does not affect the functionality of other catecholamines, which allows it to be used with Levodopa and other drugs to eliminate Parkinson's disease.
Pharmacological properties of the drug "Selegiline"
The drug is sold under the trade name Selegilin AL by the German pharmaceutical company Aliud Pharma. The corporation is one of the world's largest manufacturers of high-quality generics. In 1996, the company became a structural unit of the pharmaceutical corporation Stada Group.
As indicated by the instructions for use, "Selegiline" is an anti-Parkinsonian medication, a selective inhibitor of MAO-B, which is involved in the metabolism of catecholamines and dopamine. This drug inhibits dopamine metabolism, its reuptake at the level of presynaptic nerve endings, which increases its concentration in the nuclei of the extrapyramidal system and other parts of the brain.
What is the mechanism of action of "Selegilin"? A single dose of 5 mg of this medication inhibits 50% of MAO in the central nervous system. The recovery time of the enzyme is 2 weeks. In therapeutic doses, it does not affect the intestinal MAO and does not contribute to the breakdown of tyramine, which enters the body with food.
Release form "Selegilina"
This medical product is produced in tablet form, 1 tablet contains the main substance - selegiline hydrochloride in a dose of 5 mg. Tablets are packaged in blisters of 10 pcs., In a cardboard package contains 5 blisters.
Indications for use
The list of indications for “Selegilin” is indicated in the annotation. The medicine is prescribed for the following pathological conditions:
- Parkinson's disease;
- additional therapy for people with Parkinson’s disease who, with prolonged use of the drug “Levodopa,” noted a decrease in the effectiveness of treatment - akinesia (in the early morning or night);
- symptomatic parkinsonism.
Possible analogues of the drug
The list of Selegilin analogues includes:
- “Cognitive”;
- "Segan";
- "Niar";
- "Selgin."
A doctor should select a replacement.
Contraindications
In accordance with the instructions for use, "Selegilin" is contraindicated in the following cases:
- high sensitivity to components;
- extrapyramidal disorders not caused by dopamine deficiency (Huntington's chorea, essential tremor);
- concomitant use of antidepressants and a period of less than 5 weeks after their withdrawal;
- period of pregnancy, lactation.
With caution, the medicine is prescribed for progressive dementia, severe psychosis, tardive dyskinesia, large tremor, peptic ulcers of the gastrointestinal tract, thyrotoxicosis, pheochromocytoma, prostatic hyperplasia, angle-closure glaucoma, tachycardia, severe angina pectoris, diffuse toxic age of 18 years.
When combined with Levodopa, the medication is used with caution in case of open-angle glaucoma (chronic course), renal or hepatic insufficiency, melanoma, central nervous system depression, convulsive seizures, bronchial asthma, emphysema, myocardial infarction, less than 12 years of age.
Instructions for use
"Selegiline" should be taken orally (washed down with liquid, without chewing). With monotherapy with this medication, 5 mg (1 tablet) is prescribed 1-2 times a day. When taken once a day - the medicine is taken before breakfast, with a double dose - before bedtime and before breakfast.
When combined with Levodopa and Carbidopa medications, it is prescribed in a dosage of 5-10 mg, which allows to reduce the dose of Levodopa by 10-30% per day without impairing the patient’s motor activity.
Side effects
The medicine "Selegiline" can provoke the development of the following adverse reactions:
- CNS: excessive fatigue, cephalgia, dizziness, anxiety, mental and motor agitation, hallucinations, insomnia, dyskinesia, psychosis, confusion.
- Heart and blood vessels: arrhythmia, increased blood pressure, orthostatic hypotension.
- Digestive system: nausea, decreased appetite, constipation or diarrhea, dysphagia, dry mouth, increased liver transaminase activity.
- Sense organs: diplopia, impaired visual acuity.
- Urinary system: nocturia, urinary retention, painful urination.
- Allergic reactions: shortness of breath, skin rash, photosensitivity, bronchospasm.
- Other: hypoglycemia, hyperperspiration, hair loss.
Special recommendations
When treating patients with parkinsonism in combination with the Levodopa medication according to the instructions, the number and severity of adverse reactions are less than with monotherapy with this medication.
When used simultaneously with sympathomimetic amines, the dosage of Selegiline should not exceed 10 mg / day.
Caution should be exercised in patients with diabetes mellitus, since MAO inhibitors can provoke an increase and prolongation of hypoglycemia.
Against the background of therapy, one should refrain from potentially dangerous types of activity that require the speed of motor and mental reactions, as well as increased attention.
Drug interaction
Treatment with the drug "Selegilin" enhances the effects of ethanol, the drug "Levodopa", increases the likelihood of adverse reactions of amantadine.
Enhances the effect of adrenostimulants and drugs that suppress the activity of the central nervous system.
Taking the drug is incompatible with opioid analgesics, non-specific MAO inhibitors.
While taking Fluoxetine medication, the risk of "serotonin syndrome" increases, which is accompanied by mania, fever, hyperhidrosis and increased blood pressure.
Mixed indirect adrenostimulants and actions increase the likelihood of a pronounced increase in pressure from taking the Selegilin medication.
"Levodopa" in Parkinson's disease
An anti-Parkinsonian drug (levorotatory isomer of DOPA), which is a precursor of dopamine. This medication eliminates hypokinesia, salivation, tremors, stiffness, dysphagia. The anti-Parkinsonian effect of the drug is due to the conversion of the main substance into dopamine in the central nervous system, which contributes to the replenishment of its deficiency. The bulk is converted to dopamine in peripheral tissues. Such dopamine is not involved in achieving an antiparkinsonian effect (does not penetrate the central nervous system) and is responsible for most side effects. In this regard, it is advisable to combine the drug with peripheral dopa-decarboxylase inhibitors (Benserazide, Carbidopa), which can significantly reduce the dose of Levodopa according to the instructions and the severity of adverse reactions.
Other funds
All the medicines used in Parkinson's disease can be divided into several categories:
- Cholinergic drugs: Tremblex (central long-acting anticholinergic), Cyclodolum.
- Dopaminergic drugs: medications that stimulate the release of dopamine from vesicles (Midantan); drugs that suppress the reuptake of dopamine - Melipramin (an activating antidepressant plan) and Aminotriptyline (an antidepressant tricyclic sedative effect).
- Inhibitors of MAO - Nuredal, Deprinil.
- Antiparkinsonian drugs that stimulate the activity of dopamine receptors - “Bromocriptine”, “Lysurid”, “Pyribedil”, “Pergolid”, “Apomorphine”, etc.
- Medications that stimulate the production of dopamine (dopamine-containing drugs of prolonged exposure) - Levodopa, Madopar.
These anti-Parkinsonian drugs are used in the treatment of patients with idiopathic Parkinson's disease, as well as in patients with Parkinsonism syndrome of various origin. Such a syndrome can occur with various lesions of the nervous system: vascular, infectious, toxic, oncological, traumatic and degenerative. This is a chronic disease caused by damage to the nuclei of the extrapyramidal system.
The black substance is gradually discolored, since neurons that contain the neuromelanin pigment die in it. This pigment is formed from dopamine and catecholamines DOPA. These substances, in turn, are formed in the body from phenylalanine, which passes into tyrosine, tyrosine into DOPA, and DOPA turns into dopamine, from which at the end of the chain noradrenaline and adrenaline are obtained. Each of the steps requires a specific enzyme. When the processes occurring at any stage are disrupted, Parkinson's disease begins to develop, which implies the intake of appropriate drugs with a specific direction of exposure.