Buspirone

As Buspirone is called an anti-anxiety agent. It is used to treat anxiety disorders.

What is buspirone?

Buspirone is a drug that has an anxiolytic effect. It intervenes in the metabolism of the neurotransmitter serotonin. In contrast to other anti-anxiety preparations such as benzodiazepines, buspirone only develops its positive effects after several weeks. However, the active ingredient has the advantage of not making you tired and dependent.

Buspirone was discovered in 1972 by a team of scientists working for the Mead Johnson Nutrition Company, a producer of food for children. Buspirone was patented in 1975. The drug came onto the American market in 1986 through the pharmaceutical company Bristol-Myers Squibb. From 1996 Buspiron could also be offered in Germany. Since the expiry of patent protection in 2001, buspiron can also be sold as a generic.

Pharmacological effect

Buspirone works in the treatment of anxiety disorders. Anxiety disorders are persistent fears that can often not be clearly justified and that have a negative impact on many areas of life. This can be about professional life, social contacts or health. It is not uncommon for those affected to suffer from physical problems such as tension, dizziness, racing heart, tremors, sleep problems, nausea or headaches.

Anxiety can be relieved by anti-anxiety preparations, which primarily include benzodiazepines. In this way, both psychological and physical symptoms can be improved by taking them. However, most of the remedies of this type have the major disadvantage that they become dependent after a few weeks of use. If it is then stopped, the symptoms of anxiety and their unpleasant side effects reappear more intensely.

However, taking buspirone can prevent addiction. After several weeks of use, the neuronal structures of the brain rearrange themselves. The interconnection of nerve cells (neurons) is changed by activating certain docking points, also called receptors, on the messenger substance serotonin. For this reason, the positive effect of the anxiety reliever only shows up after a while.

In addition to the so-called happiness hormone serotonin, buspirone also has an effect on dopamine and noradrenaline, which stimulate the psychological drive. In contrast to the benzodiazepines, buspirone has no effect on the GABA receptors, which are important for human sleep. Therefore, there are hardly any sleep-inducing effects from the administration of the agent.

The absorption of buspirone into the blood takes place quickly after its ingestion through the intestinal wall. From there, the active ingredient is transported in the blood towards the liver. There it is deactivated by around 95 percent. After 60 to 90 minutes, buspirone has reached its maximum level in the body. After two to three hours, the level drops again by 50 percent. Buspirone is eliminated from the organism with urine and stool.

Medical application & use

Buspirone is used in the treatment of anxiety disorders and states of tension. The remedy is also considered helpful for internal restlessness. The use of buspirone does not cause addiction, but the drug should only be used for a maximum of four months.

Buspirone can be administered in the form of tablets. The daily dose is divided into three individual administrations. They are taken independently of meals. In the initial stage of therapy, the patient only takes a small dose of buspirone. This consists of 5 milligrams three times a day. In the further course, the dose is gradually increased, provided there are no undesirable side effects, to 10 milligrams, which the patient takes three times a day. In severe cases, a maximum dose of 20 milligrams is also possible.

Buspirone is subject to prescription. The drug can only be obtained from the pharmacy by presenting a doctor's prescription.

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Risks & side effects

Occasionally there are side effects from taking buspirone. These are mostly dizziness and sleepiness. Ten out of 100 patients also have undesirable side effects such as confusion, anger, visual disturbances, profuse sweating, rashes on the skin, paresthesia, muscle pain, nasal congestion, sore throat, chest pain, tinnitus and nightmares. Occasionally gastrointestinal complaints, nausea, vomiting, concentration problems, dry mouth, eczema, numbness or clammy hands occur. Mood swings, circulatory disorders in the brain, allergic reactions, serotonin syndrome, diseases of the heart muscle or even a heart attack are very rare.

Buspirone must not be used at all if the patient suffers from severe kidney or liver disorders, muscle weakness, seizures or acute narrow-angle glaucoma. During pregnancy, buspirone should only be administered with the consent of the doctor. The product should not be taken while breastfeeding. Children under the age of 18 should also not take buspirone.

Interactions between buspirone and other drugs are also considered possible. For this reason, the patient should be monitored consistently if he is also taking high blood pressure drugs, anti-anxiety drugs such as benzodiazepines, anticoagulant drugs, heart medication or birth control pills.

In addition, it is important not to administer buspirone at the same time as MAOIs. The reason for this is an impending crisis from high blood pressure. We also advise against taking erythromycin, nefazodone, verapamil, itraconazole or cimetidine at the same time. These drugs enhance the effects of buspiron.