- The mechanism of action of buspirone
- What should you be careful about when using buspiron?
- Contraindications to the use of buspirone
- Buspiron - interactions with other drugs
- Buspiron - side effects
Buspirone is an organic chemical compound with psychotropic properties. Currently, it is used primarily in the treatment of anxiety occurring during depression. The substance is not addictive. Contrary to the majority of anxiolytic drugs, it does not exhibit anticonvulsant and sedative effects. When is buspirone used?
Buspironis a drug successfully used in the treatment of anxiety conditions accompanying depression. The anxiolytic effect of the substance is visible only after 7-14 days of use. For this reason, buspirone cannot be used as a reliever in panic attacks. Medicines containing this substance are used for long-term treatment of anxiety disorders.
Preparations containing buspirone are also being investigated as drugs for the treatment of addiction. This is due to the ability of this substance to reduce the activity of the brain's reward center.
The mechanism of action of buspirone
The therapeutic effect of buspirone is related to its activity on serotonin and dopamine receptors. This compound is a partial agonist of 5-HT1A receptors and an antagonist of D3 and D4. By acting on them, buspirone influences brain function with an anxiolytic effect.
Serotonin: role in the body. Symptoms of Serotonin Deficiency
Dopamine: role in the body. Symptoms of dopamine deficiency and excess
The drug, however, does not show activity against GABA receptors, unlike many anti-anxiety substances. Therefore, the drug has no hypnotic and anticonvulsant properties.
Buspirone has a strong blocking effect on dopamine receptors. This is important in addiction therapy. Currently, it is believed that the dopaminergic system plays an important role in the development of physical and mental dependence on narcotic substances.
Increased dopamine concentration in synaptic clefts occurs, for example, after administering cocaine. Therefore, administration of buspirone reduces the positive feelings resulting from the administration of this drug. The mechanism of the drug's activity can also be applied to other substances that stimulate the brain's reward center.
5-HT1A receptors play the role of presynaptic and postsynaptic receptors. Stimulation of the presynaptic receptors blocks the secretion of serotonin into the cleftsynaptic. The process is driven by a feedback mechanism. This leads to a reduction in transmission in serotonergic neurons.
It is estimated that 5-HT1A receptors play an important role in the mechanism of depression. Studies have shown a reduced concentration of these receptors in the prefrontal and temporal areas of the cerebral cortex. On the other hand, in suicide victims, an increased concentration of presynaptic 5-HT1A receptors was observed in the area of the nuclei of the suture stem. It has also been estimated that more receptors of this type are responsible for reducing the number of serotonin neurons.
What should you be careful about when using buspiron?
Buspirone should not be combined with drugs depressing the nervous system. Before introducing a preparation containing this ingredient into therapy, you should gradually discontinue:
- benzodiazepine derivatives
- sedatives
- sleeping pills
In some people, buspirone may affect psychomotor performance. For this reason, at the beginning of the use of the drug, you should refrain from driving a car and other vehicles. This is to make sure how the substance works on our brain.
Contraindications to the use of buspirone
- severe kidney failure
- epilepsy
- severe liver failure
Buspiron - interactions with other drugs
Unfortunately, buspirone is a drug with many interactions with other medical preparations and food. Be especially careful about the following connections:
- MAO inhibitors - this combination may cause an increase in blood pressure
- alcohol - may increase anxiety
- grapefruit juice - may cause a sudden increase in the concentration of the drug in the blood
- erythromycin
- itraconazole
- nefazodone
- verapamil
- diltiazem
- diazepam
Buspiron - side effects
Side effects during buspirone treatment are relatively rare. They most often appear during initiation of the drug and disappear during long-term therapy. The most common complaints related to the use of buspirone are:
- headaches
- dizziness
- nervousness
- arousal
- imbalance
- palpitations
- convulsions
- fatigue
- dry mucous membranes
- excessive sweating
- chest pains
Anxiety disorders are one of the most common mental he alth problems. They often accompany depression and other diseases, worsening their course.The problems resulting from anxiety are often neglected by society and doctors. It is often difficult for a he althy person to understand that anxiety can be a form of a mental disorder. Patients often hear that they are exaggerating or that they "should pull themselves together".
Patients struggling with anxiety disorders perceive it as a source of suffering. Fear, next to pain, is one of the most difficult sensations for a human being. The immediate and long-term treatment of these disorders is therefore one of the most urgent challenges for both doctors and medicine as a science.
About the authorSara Janowska, MA in pharmacyPhD student of interdisciplinary doctoral studies in the field of pharmaceutical and biomedical sciences at the Medical University of Lublin and the Institute of Biotechnology in Białystok. A graduate of pharmaceutical studies at the Medical University of Lublin with a specialization in Plant Medicine. She obtained a master's degree defending a thesis in the field of pharmaceutical botany on the antioxidant properties of extracts obtained from twenty species of mosses. Currently, in his research work, he deals with the synthesis of new anti-cancer substances and the study of their properties on cancer cell lines. For two years she worked as a master of pharmacy in an open pharmacy.Read more articles by this author