How buspirone works
Buspirone belongs to the group of anxiolytics (anti-anxiety drugs). It mediates its effect by binding to a specific type of docking sites (receptors) of the nerve messenger serotonin (5-HT1A receptors). Unlike other anxiolytics, the drug does not have a sedative, muscle relaxant, or anticonvulsant effect.
Being afraid in certain situations is a completely natural reaction of the body. Evolutionarily, fear is an important protective and survival mechanism that enables us to behave appropriately in potentially dangerous situations.
In anxiety disorders, however, a patient suffers from persistent anxiety that can relate to many areas of life and is usually unfounded. For example, the constant fears and worries may relate to social relationships, work, health, money, or other things. They are usually accompanied by physical complaints such as nausea, restlessness, trembling, palpitations, dizziness, tension, headaches and sleep disturbances.
Buspirone works differently in this respect. When the active ingredient is taken over several weeks, the complex neuronal brain structures that can trigger anxiety disorders begin to reorganize:
By activating certain docking sites (receptors) of the nerve messenger serotonin, buspirone changes the “wiring” of nerve cells, as studies have shown. This circumstance also explains the delayed onset of effect of the anxiety reliever.
Complementary psychotherapy helps sufferers to get their anxiety symptoms under better and longer-term control.
Absorption, breakdown and excretion
After ingestion, the active ingredient is rapidly and completely absorbed into the blood through the intestinal wall. From the intestine, it travels with the blood to the liver, where more than 95 percent of it is deactivated (“first-pass metabolism”).
The buspirone blood level, which reaches its maximum one to one-and-a-half hours after ingestion, is therefore already half again after about two to three hours. About two-thirds of the breakdown products of buspirone are excreted in the urine and one-third in the stool.
When is buspirone used?
How buspirone is used
Buspirone is taken in tablet form. The total daily dose is divided into three individual doses, which are taken independently of meals with a glass of water.
Treatment is started gradually, beginning with a low dose, usually five milligrams of buspirone three times a day. The dose is then slowly increased – depending on the effect and the occurrence of side effects – up to ten milligrams three times a day.
In severe cases, the doctor may prescribe up to 20 milligrams three times a day.
The effect of buspirone does not occur immediately, but with a time delay.
What are the side effects of buspirone?
The most common side effects include dizziness, headache, and drowsiness.
Side effects such as chest pain, nightmares, anger, hostility, confusion, drowsiness, ringing in the ears, sore throat, stuffy nose, blurred vision, muscle pain, paresthesias, skin rashes, and increased sweating show up in one in ten to one hundred patients.
What should be considered when taking buspirone?
Contraindications
Buspirone must not be taken in case of:
- hypersensitivity to the active substance or to any of the other components of the drug
- severe kidney or liver dysfunction
- epilepsy
- acute intoxication with alcohol or certain medications (antipsychotics, analgesics, or hypnotics)
Drug interactions
Although no interactions between alcohol and buspirone have been observed in clinical studies, it is generally recommended not to drink alcohol during treatment with psychotropic drugs.
Buspirone is broken down by the enzyme CYP3A4. Substances that inhibit the enzyme in its action or increase its production can therefore theoretically enhance or weaken the effect of buspirone.
There are no studies on possible interactions between buspirone and other psychotropic drugs (such as antipsychotics, antidepressants). Therefore, an experienced physician should always be consulted before concomitant use.
The same applies to combinations with hormonal contraceptives, anticoagulants, anti-diabetic agents and other agents.
Driving and operating machines
It is possible that reaction time may be impaired by taking buspirone. Therefore, patients should not operate heavy machinery or drive vehicles during treatment until individual tolerance is known.
Age Limitation
Buspirone should not be used in children and adolescents under 18 years of age due to lack of data.
Pregnancy and Lactation
There is no experience with the use of buspirone in pregnancy. Animal studies have not shown direct or indirect adverse effects on the unborn child. The decision whether to continue buspirone therapy during pregnancy is made on an individual basis.
It is not known whether buspirone or its breakdown products (metabolites) pass into breast milk. Experts believe that breastfeeding is conditionally acceptable with monotherapy (treatment with buspirone alone and no other drug) and good observation of the infant.
To receive medication with buspirone
How long has buspirone been known?
Buspirone was discovered by a team of scientists in 1972. However, it was not patented until 1975 and was launched on the market in the USA in 1986.
It was approved in Germany in 1996, and patent protection expired in 2001. In the meantime, there is also a generic drug with the active ingredient buspirone.
