New generation antileukotriene drugs: a list of the best

Antileukotriene drugs are a new class of agents that reduce inflammatory processes that have an infectious or allergic etiology.

In order to understand the principle of action of such drugs, it is worthwhile to understand what the leukotrienes are.

Leukotrienes

They are mediators of inflammatory processes. By their chemical structure, they are fatty acids, which are formed by arachidonic acid.

Leukotrienes take part in the development of bronchial asthma. Like histamine, they are a mediator of allergic reactions of immediate type. Histamine is able to cause a rapid but short-term spasm of the bronchi, and leukotrienes cause a delayed and more prolonged spasm.

How are antileukotriene drugs classified?

At present, the following leukotrienes are classified: A ₄ , B ₄ , C ₄ , D ₄ , E ₄ .

The synthesis of leukotrienes is derived from arachidonic acid. She under the influence of 5-lipoxygenase passes into leukotriene A ₄ . After this, a cascade reaction occurs, resulting in the formation of the following leukotrienes B ₄ -C ₄ -D ₄ -E ₄ . The final product of such a reaction is LTE ₄ .

Found that LTE ₄ , D ₄ , E ₄ are able to cause bronchoconstrictor effect, increase the secretion of mucus, can promote the development of edema, inhibit mucociliary clearance.

B ₄ , D ₄ , E ₄ have chemotactic activity, that is, they can attract neutrophils and eosinophils into the inflammatory zone.

Scientists have proved that leukotrienes are produced by macrophages, mast cells, eosinophils, neutrophils, T-lymphocytes, which take a direct part in the inflammatory reaction. Antileukotriene drugs with bronchial asthma are often used.

After the cells come into contact with the allergen and the cooling of the respiratory tract either after physical exertion, the synthesis of LT is activated. That is, the synthesis begins when the osmolality of the bronchial contents increases.

Four groups of drugs

At present, only four groups of antileukotriene drugs are known:

1. "Zileuton", which is a direct inhibitor of 5-lipoxygenase.
2. Drugs that are inhibitors of FLAP, which prevent the binding of this protein to arachidonic acid.
3. "Zafirlukast", "Pabilukast", "Montelukast", "Pranlukast", "Verlucast", which are antagonists of receptors of sulfide-peptidic leukotrienes.
4. Drugs that are antagonists of leukotriene receptors B ₄ .

The most researched are the antileukotriene preparations of the first group and the means of the third group. Consider the representatives of these groups a little more.

Zileuton

"Zileuton" is a reversible inhibitor of 5-lipoxygenase. It is able to inhibit the formation of sulfidopeptidic RT and LTB ₄ . The drug may have a bronchodilating effect lasting up to five hours. He is also able to prevent the occurrence of bronchial spasm, which is a consequence of exposure to cold air or "Aspirin".

Numerous studies prove that "Zileuton", assigned to patients suffering from bronchial asthma for one to six months, is able to reduce the patient's need for inhalation of β2-adrenomimetics and glucocorticoids. A single dose of "Zileuton" prevents the onset of sneezing and obstructed nasal breathing in those patients who suffer from allergic rhinitis after the administration of the allergen nasally.

Six-week therapy with the use of "Zileuton" patients with atopic asthma showed a significant result. Physicians note a qualitative decrease in the level of eosinophils and neutrophils. Also, the tumor necrosis factor in the lavage fluid of the bronchoalveolar type was decreased after the test with an allergen. That is why antileukotriene drugs are unique, the mechanism of action is based on this.

"Zileuton" is characterized by a fairly short period, during which its half-elimination occurs. This suggests that the drug should be taken often enough, up to four times a day. In addition, "Zileuton" is able to lower the clearance of theophylline. This must be taken into account if a parallel intake of theophylline and Zeleuton is contemplated. That is, the dose of the former should be reduced. If "Zileuton" is appointed for a long period, then the level of liver enzymes should be monitored.

But there are antileukotriene drugs of a new generation, a list of them is presented below.

Means that are antagonists of sulfide-peptidic leukotrienes are highly selective competitors and reversible blockers of RT D ₄ receptors. Such drugs include "Pranlukast", "Zafirlukast", "Montelukast".

"Akolat" ("Zafirlukast")

"Zafirlukast", also called "Akolat", is the most studied preparation of this group of antileukotriene substances. It also has broncho-enlarging activity. The effect lasts a fairly long time, up to five hours. "Zafirlukast" is able to prevent the development of asthmatic reaction in case of inhalation by an allergen. Its effectiveness has been proven in the prevention of spasm of the bronchi, which is provoked by cold air, aspirin, exercise, pollutants. This drug, as well as the preparation "Montelukast" can enhance the broncholytic activity of β2-adrenomimetics.

"Acolat" ("Zafirlukast") has good absorption, the peak of its concentration in the blood is reached after three hours after its reception. The period of its half-elimination is slightly longer than that of the "Zeleuton", and is 10 hours. In addition, it has no effect on the clearance of theophylline. Take this drug should be either an hour before meals, or after two hours after it, as food significantly reduces its ability to suck. The drug is well tolerated by patients.

Conclusion

Antileukotriene drugs for allergies can be used for children, but not earlier than they reach the age of two. With the help of these medicines, children are treated with relapsing bronchitis, allergic rhinitis, mild bronchial asthma.