Buspirone: Effects, Uses & Risks

Buspirone is the name given to an anti-anxiety agent. It is used for the treatment of anxiety disorders.

What is buspirone?

Buspirone is the name given to an antianxiety agent. It is used in the therapy of anxiety disorders. Buspirone is a drug that has an anxiety-relieving effect. It interferes with the metabolism of the neurotransmitter serotonin. Unlike other anti-anxiety drugs such as benzodiazepines, buspirone does not produce its positive effects for several weeks. In return, however, the active ingredient has the advantage of not making patients tired or dependent. Buspirone was discovered in 1972 by a team of scientists working for the Mead Johnson Nutrition Company, a producer of food for children. The patenting of buspirone took place in 1975. The drug was introduced to the American market in 1986 by the pharmaceutical company Bristol-Myers Squibb. From 1996, buspirone was also allowed to be sold in Germany. Since patent protection expired in 2001, buspirone can also be marketed as a generic drug.

Pharmacologic action

Buspirone exerts its effects in the treatment of anxiety disorders. Anxiety disorders refer to persistent fears that often cannot be clearly justified and have a negative impact on numerous 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, rapid heartbeat, tremors, sleep problems, nausea or headaches. Anxiety states can be alleviated by anxiety-relieving preparations, which primarily include benzodiazepines. Thus, their use can improve both the mental and physical symptoms. However, most drugs of this type have the major disadvantage that they become addictive after a few weeks of use. If they are then discontinued, the anxiety symptoms and their unpleasant side effects reappear with increased intensity. However, dependence can be avoided by taking buspirone. After several weeks of use, the neuronal structures of the brain rearrange themselves. The switching of the nerve cells (neurons) is changed by the activation of certain docking sites, also called receptors, on the messenger substance serotonin. For this reason, the positive effect of the anxiety reliever only becomes apparent after some time. In addition to the so-called happiness hormone serotonin, buspirone also exerts its effect on dopamine and norepinephrine, which stimulate mental drive. Unlike the benzodiazepines, buspirone has no effect on the GABA receptors, which are important for human sleep. Therefore, there are few soporific effects from administering the drug. The absorption of buspirone into the blood takes place rapidly through the intestinal wall after its ingestion. From there, the active ingredient is transported with the blood toward the liver. About 95 percent of the active ingredient is deactivated there. Buspirone reaches its maximum level in the body after 60 to 90 minutes. After just two to three hours, the level drops again by 50 percent. Buspirone is excreted from the organism in urine and stool.

Medical use and application

Buspirone is used in the treatment of anxiety disorders and tension states. The drug is also considered helpful for inner restlessness. Although taking buspirone does not cause dependence, the drug should still be used for a maximum of only four months. Buspirone is administered in the form of tablets. The daily dose is divided into three individual administrations. The tablets are taken independently of meals. In the initial stage of therapy, the patient takes only a small dose of buspirone. This consists of three times 5 milligrams a day. In the further course, provided that no undesirable side effects occur, the dose gradually increases 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. Thus, the drug can be obtained in the pharmacy only by presenting a doctor’s prescription.

Risks and side effects

Sometimes side effects are manifested by taking buspirone. These are mostly dizziness and drowsiness.Ten out of one hundred patients also experience undesirable side effects such as confusion, anger, visual disturbances, profuse sweating, rashes on the skin, sensory disturbances, pain in the muscles, nasal congestion, sore throat, chest pain, tinnitus and nightmares. Sometimes gastrointestinal complaints, nausea, vomiting, concentration problems, dry mouth, eczema, numbness or clammy hands also occur. Very rarely, there is a risk of mood swings, circulatory disorders of the brain, allergic reactions, serotonin syndrome, diseases of the heart muscle or even a heart attack. Buspirone should not be used at all if the patient suffers from severe kidney or liver dysfunction, muscle weakness, seizures or acute narrow-angle glaucoma. In pregnancy, buspirone should be administered only with the consent of the physician. Use of the drug during breastfeeding should be completely avoided. Children under 18 years of age should also not take buspirone. Interactions between buspirone and other medications are also considered possible. For this reason, consistent monitoring of the patient should take place if he or she is also taking high blood pressure medication, anxiety-relieving preparations such as benzodiazepines, anticoagulant drugs, heart medication or the contraceptive pill. In addition, it is important not to administer buspirone at the same time as MAO inhibitors. The reason for this is an impending crisis due to high blood pressure. It is also not recommended to take erythromycin, nefazodone, verapamil, itraconazole or cimetidine at the same time. These drugs potentiate the effects of buspirone.