Segan

Segan is a pharmaceutical used to treat Parkinson's disease. Consider its medicinal properties, dosage, possible side reactions.

The drug is used for the therapy of a slowly progressing chronic neurologic disease, characteristic for persons of the older age category. Segan facilitates the symptoms of idiopathic parkinsonism syndrome. Its use in the early stages of the disease, inhibits the development of the pathological process.

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Indications of the segana

According to the instruction, Segan has the following indications for use:

• Parkinson's disease.
• Symptomatic tremor paralysis.

The medication is used as an adjuvant therapy for patients with Parkinson who take levodopa for a long period of time. And also with akinensia in the night or early morning period.

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Release form

The medicine has a tablet form of release. In one package there is a blister for 20 capsules. Each tablet contains 5 mg of selegiline hydrochloride active ingredient, as well as magnesium stearate, a mixture of lactose monohydrate, crospovidone and povidone K30.

Pharmacodynamics

The selective MAO-B inhibitor participates in the metabolism of catecholamines, in particular dopamine. Pharmacodynamics of the active substance indicates the inhibition of the metabolism of neurotransmitters and their re-uptake at the level of presynaptic endings. This leads to an increase in the concentration of the active substance in the brain regions and the nuclei of the extrapyramidal system.

A single dose of 5 mg of the drug is able to inhibit about 50% of the monoamine oxidase in the central nervous system. The recovery period of the enzyme takes 14 days. If the drug is used in therapeutic doses, it does not affect the MAO GIT and does not stop the cleavage of the tyramine.

Selegilin prolongs and intensifies the action of levodopa. If Segan is used in the early stages of an idiopathic disorder, the need for levodopa is no longer necessary. If the drug is used in combination therapy, the dosage of levodopa is reduced by 30%.

Pharmacokinetics

After ingestion, selegiline is rapidly absorbed from the digestive tract, the maximum concentration occurs 30 minutes after application. Pharmacokinetics indicates a low bioavailability of the active component, it is about 10%. If the medicine is used during a meal, then its bioavailability increases by 3-4 times. This is due to the fact that selegiline refers to lipophilic substances with a weak alkaline reaction.

About 75-85% of the drug binds to blood plasma proteins. The active substance quickly penetrates the brain and spreads through all tissues of the body. Rapidly metabolizes into the liver and small intestine to N-dimethylselegiline (MAO-B inhibitor). The highest concentration of metabolites in the plasma, which exceeds the maximum concentration of selegiline 4-20 times. With repeated use, the concentration of metabolites of the active component increases.

The inhibitory effect on the activity of MAO-B enzymes develops after a single dose of 10 mg and persists for 24 hours. Since the inhibition of MAO-B by selegiline is irreversible, the reduction of MAO-B after discontinuation of the drug is completely dependent on the synthesis of the enzymatic protein. When taking a single dose, the half-life is 120 minutes, but in the equilibrium state it can increase to 10 hours. The half-life of metabolites is about 20 hours. Metabolites are excreted in the urine, 15% goes with feces.

Dosing and administration

Tablets are taken orally, without chewing and washing with water. The method of administration and dose is prescribed by the attending physician. If Segan is used as a monotherapy, then apply 5 mg 1-2 times a day, that is, before breakfast and before bedtime. With combined therapy with levodopa and carbidopa, 5-10 mg is prescribed. This dosage makes it possible to reduce the dose of levodopa by 10-30% without disturbing the patient's motor functions.

If, after Segan, fluoxetine therapy is prescribed, then you must wait at least 14 days. During therapy, you should not drive the car and engage in potentially dangerous activities that require increased attention, speed of motor and mental reactions.

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Use of the segana during pregnancy

To date, there is no reliable data on the safety of Segan for future mothers. That is, its use during pregnancy is not recommended. This is associated with a risk of intrauterine anomalies in the fetus. If the drug is used during lactation, selegiline can penetrate into breast milk, which is also unsafe for the baby.

Contraindications

The main contraindications to the use of the preparation Segan are based on the activity of its active substance:

• Individual intolerance of the components of the drug.
• Extrapyramidal disorders not associated with a deficiency of dopamine.
• Pregnancy and lactation.
• Horea Huntington.
• An essential tremor.
• Progressive dementia.
• Late dyskinesia.
• Peptic ulcer of the gastrointestinal tract.
• Hyperplasia of the prostate.
• Closed-angle glaucoma.
• Tachycardia and severe angina.
• Diffuse toxic goiter.
• Age of patients under 18 years.

If Segan is prescribed in combination with levodopa, the drugs are contraindicated in such conditions: melanoma, CNS depression, bronchial asthma, renal or hepatic insufficiency, emphysema, myocardial infarction, patient under 12 years.

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Side effects of the segana

In some cases, Segan can cause side effects. The most common symptoms are:

• Decreased appetite, nausea, vomiting, stools and dry mouth.
• Increased fatigue, headaches and dizziness, sleep and wakefulness, hallucinations.
• Increased blood pressure, arrhythmia.
• Impaired visual acuity.
• Retention of urine, painful urination.
• Skin allergic reactions.

In rare cases, hypoglycemia and hair loss are observed. There is no specific antidote, treatment is symptomatic.

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Overdose

Non-compliance with the prescribed dosage by the doctor, causes various pathological reactions. Overdose is most often manifested by such symptoms:

• Headaches and dizziness.
• Psychomotor agitation.
• Convulsions.
• Arterial hypertension.
• Increased sweating.
• Violation of the heart rate.
• Inhibition of breathing.

For treatment is shown induction of vomiting, the use of activated carbon, gastric lavage. With convulsions, intravenous diazepam is needed.

Interactions with other drugs

If Segan is used in combination therapy, then it is necessary to monitor its interactions with other drugs. Selegilin enhances the action of ethanol and levodopa, which increases the risk of adverse reactions of amantadine. There is also an increase in the effect of adrenostimulants, which depress the central nervous system.

The drug is incompatible with nonspecific MAO inhibitors and opioid analgesics. The interaction with fluoxetine increases the risk of developing serotonin syndrome, which is characterized by an increase in blood pressure and fever. Adrenostimulators of indirect action increase the risk of increasing blood pressure.

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Storage conditions

Tablets should be stored in a dry place, protected from sunlight and inaccessible to children. Storage conditions imply a temperature regime of no higher than 25 ° C. Violation of these recommendations leads to deterioration of the medicament and the loss of its pharmaceutical properties.

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Shelf life

Segan has a shelf life of 36 months from the production date (indicated on the package and blister with tablets). At the end of this period, the drug must be disposed of. The shelf life also affects shelf life. Therefore, if the tablets have changed color, got an unpleasant smell or began to crumble, do not take them. 

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