Selegiline Hydrochloride Tablets

Selegiline hydrochloride is a levorotatory acetylene derivative of phenylethylamine. It is an irreversible inhibitor of monoamine oxidase type B (MAO-B). It can selectively inhibit MAO-B at the clinically recommended dose (such as 10 mg/day). After selegiline is converted by MAO, its active part irreversibly binds to the active center of MAO and/or its coenzyme isoflavone adenine dinucleotide (FAD), suicidal inhibition of MAO activity. MAO can be divided into type A and type B. MAO-B is mainly present in the human brain, while MAO-A is dominant in the intestine. MAO can degrade a variety of catecholamine compounds and 5-hydroxytryptamine by oxidative deamination. As an adjuvant drug for levodopa/carbidopa, selegiline inhibits MAO-B in the brain, blocks the degradation of dopamine, relatively increases dopamine content, and supplements the insufficient ability of neurons to synthesize dopamine. It is generally believed that the effect of selegiline is mainly produced by inhibiting the activity of MAO-B, but there is also evidence that selegiline can enhance the function of dopaminergic nerves through other mechanisms. For example, it interferes with the reuptake of dopamine by synapses, or interferes with the uptake of various neurotransmitters by neurons through its metabolites (amphetamine and methamphetamine), enhancing the release of transmitters (norepinephrine, dopamine, 5-HT) to strengthen the function of dopaminergic nerves. MAO also has a degrading effect on various exogenous amines in food and drugs. MAO (mainly MAO-B) in the intestines and liver plays an important role in preventing the absorption of exogenous amines from triggering hypertensive crises (called cheese reactions). If the amines contained in fermented cheese, red wine, herring, and cough/cold medicines enter the blood circulation in large quantities, they will be absorbed by adrenergic neurons and replace norepinephrine in the cyst storage sites. The latter is released into the blood, which can cause reactions such as increased blood pressure. Selegiline has a greater affinity for the active center of MAO-B than for MAO-A. Therefore, in theory, at the clinically recommended dose, it can selectively inhibit MAO-B without significantly inhibiting MAO-A in the intestine.

The main ingredient of this product is selegiline hydrochloride. Chemical name: (R)-N-a-dimethyl-N-(2-propynyl)phenylethylamine hydrochloride.

This product is white tablets.

It is used alone to treat early Parkinson's disease or in combination with levodopa or with levodopa and a peripheral dopa decarboxylase inhibitor. The combination of sinocycline and levodopa is particularly suitable for the treatment of motor fluctuations such as end-of-dose fluctuations caused by high-dose levodopa therapy.

Oral. The starting dose is 5 mg (one tablet) in the morning. The dose of selegiline hydrochloride tablets can be increased to 10 mg (two tablets) per day (taken once in the morning or divided into two doses in the morning and afternoon). If the patient shows adverse reactions similar to levodopa when taking levodopa preparations, the levodopa dose should be reduced. Or follow the doctor's advice.

Strategin is well tolerated when taken alone. There are reports that patients taking Strategin have an increased incidence of dry mouth, transient increases in serum aminotransferase values, and sleep disorders (such as insomnia) compared to patients taking placebo. Because Strategin can increase the effect of levodopa, the side effects of levodopa will also increase. Adding Strategin to patients who have taken the maximum tolerated dose of levodopa may cause involuntary movements, nausea, agitation, confusion, hallucinations, headache, positional hypotension, and dizziness. Dysuria and rash have also been reported. Potential side effects should be monitored. Therefore, when adding Strategin to treatment, the levodopa dose should be reduced by an average of 30 percent.

Selegiline Hydrochloride Tablets are contraindicated for patients who are allergic to them, have severe mental illness, severe dementia, delayed dyskinesia, or have a history of peptic ulcer. When used in combination with levodopa, it should also be contraindicated for patients with hyperthyroidism, adrenal medullary tumors (pheochromocytoma), or glaucoma (angle-closure glaucoma).

Precautions for children: There is no information on the use of the drug in children. Precautions for pregnancy and lactation: There is insufficient literature on the safety of taking the drug during pregnancy and lactation, so it is not recommended to take the drug during pregnancy and lactation.

During treatment with Strategine, attention should be paid to the hypertensive reactions caused by the interaction with indirect sympathomimetics. No hypertensive reactions were found when Strategine doses used to treat Parkinson's disease were taken simultaneously with foods containing tyramine. This product may cause severe hypotension when used in combination with non-selective monoamine oxidase inhibitors. There are no reports of drug resistance when taken simultaneously with the monoamine oxidase A inhibitor moclobemide. However, taking such drugs (MAOA and MAOB inhibitors) and tyramine substances (e.g., tyramine-containing foods such as fermented foods and beverages, cheese, sausages, cured meats, game, liver, beef broth, salted fish, beans and peas, sauerkraut and yeast products) at the same time will slightly increase the hypertensive reaction. However, since there are no detailed reports in the literature on the simultaneous use of this product and moclobemide, these two drugs should not be taken at the same time. There are reports of interactions between Strategine and pethidine. Since some interactions can be fatal and the mechanism has not been determined, simultaneous use should be avoided. Severe reactions have been reported when seraquine is taken with fluoxetine, such as ataxia, tremor, hyperthermia, hyper/hypotension, convulsions, palpitations, sweating, flushing, dizziness, and mental changes (agitation, confusion, and hallucinations) progressing to delirium and coma. Similar reports have been reported when seraquine is taken with two other 5-HT reuptake inhibitors, sertraline and paroxetine. The mechanism of interaction is not clearly understood, and these drugs should be avoided when taken with seraquine. Due to the long half-life of fluoxetine and its metabolites, seraquine should be taken at least five weeks after fluoxetine is discontinued. On the other hand, since seraquine and its metabolites have a short half-life, fluoxetine can be taken two weeks after seraquine is discontinued. There was no clinical, pharmacodynamic, or pharmacokinetic interaction when seraquine and citalopram were taken together in healthy volunteers. However, caution should be exercised when seraquine is taken with all selective serotonin reuptake inhibitors such as velafaxine and fluoxetine. Be careful when using styglycine and tricyclic antidepressants together. Serious central nervous system symptoms have been reported. Several deaths have been reported with high fever, tremor, and agitation. Other reports of adverse reactions from taking styglycine and tricyclic antidepressants together include high/low blood pressure, dizziness, increased sweating, tremor, convulsions, behavioral and mental changes. Because the mechanism of interaction is not yet clear, it is necessary to be cautious when adding these drugs to patients taking styglycine.

Store at room temperature +15 to +25°C. The shelf life is tentatively 24 months.

5 mg

24 months