Buspirone

Buspirone is an anti-anxiety drug and Serotonin- agonist antidepressant used to treat certain anxiety disorders or to temporarily ease feelings of anxiety. It has no chemical affinity for barbiturates or benzodiazepines like diazepam. Furthermore, buspirone doesn’t cause noticeable sleepiness or substantially impair memory or cognition like those other drugs do. Buspirone’s limited ability for misuse is its main benefit. It is not subject to the same regulations as drugs that are banned, such as barbiturates and benzodiazepines. 

• For those with a history of drinking and drug abuse, it is a better choice because it does not seem to cause dependence.   

Additionally, unlike benzodiazepines, buspirone can be quickly stopped without causing withdrawal symptoms, and it does not require lengthy tapering before termination.

What is the mechanism of action of buspirone?

The therapeutic activity of buspirone at certain receptors in the brain may account for its efficacy in treating anxiety. A neurotransmitter attaches itself to certain receptors on the membrane of nerve cells to produce a signal. A neurotransmitter’s neurochemical signal is converted to an electrical or other chemical signal and sent along the neuron once it has locked onto the receptor. 

Buspirone’s activity on serotonin receptors, namely at a particular subtype of serotonin receptor (5-HT1A), may be the reason for its ability to reduce anxiety. 

• Buspirone has no muscle relaxant or anticonvulsant properties, unlike benzodiazepines, which act on several kinds of receptors, including γ-aminobutyric acid [GABA] receptors.

What is the recommended dose of buspirone?

Usually, buspirone is started at a beginning dose of 5 mg twice or three times a day (10–15 mg/day). From there, dosages are increased by 5 mg/day every two to three days until an ideal therapeutic dose of 20–30 mg/day in split doses is reached.

•  The daily maximum dosage shouldn’t be more than 60 mg.

What are the common side effects of buspirone?

Common side effects are often reported as buspirone side effects. These adverse effects normally disappear within a week or so of starting medication, however, they might return soon after. 

Buspirone is less sedating and doesn’t seem to affect coordination or cognition like benzodiazepines do. Although nervousness and excitement may be experienced by people who metabolize the medicine slowly or who may be more susceptible to its effects on the central nervous system (CNS).

• Buspirone is typically well tolerated and has very few problematic side effects.

Common side effects include abdominal pain, anger, anxiety, chest pain, cold sweat, concentration impairment, confusion, constipation, depression, diarrhea, dizziness, drowsiness, dry mouth, fatigue, headache, laryngeal pain, movement disorders, musculoskeletal pain, nasal congestion, nausea, parathesia, skin reactions, sleep disorders, tachycardia, tinnitus, tremor, vision disorders, and vomiting.

• Rare side effects: include changes in personality, emotional lability, hallucinations, memory loss, parkinsonism, syncope, seizures, and serotonin syndrome. 

What are the precautions for buspirone usage?

The drug may impair awareness and coordination; therefore, patients should use caution when driving or performing other tasks that require alertness while taking this medicine.   

Seniors may be more vulnerable due to impaired coordination and reflexes, perhaps leading to falls and injuries.

• It is unknown if long-term buspirone usage results in dependency.
• The dose should be reduced when there is concurrent administration with CYP3A4.
•  It is possible to stop using the drug abruptly without experiencing withdrawal symptoms. 

For the majority of users, buspirone doesn’t seem to interact significantly with alcohol and doesn’t make the sleepy effects of alcohol stronger.

•  Buspirone does not have the same impact as benzodiazepines, which are centrally acting depressants that can also lower breathing. 
• Patients with emphysema, chronic obstructive pulmonary disease, and sleep apnea—a condition in which breathing is disrupted by prolonged pauses in the sleep cycle—can safely use it.

Buspirone should not be taken with a type of antidepressant called monoamine oxidase inhibitors (MAOIs).

• The combination can precipitate a dangerous elevation of blood pressure.

If you miss a dose, take it right away. If it is near the next planned dose, cancel the missed dose and resume your normal dosing schedule. Avoid taking double the prescribed dose.  

• Buspirone can be taken before or after meals.   
• Keep the medication in the original labeled, light-resistant container, away from heat and moisture, to avoid drug degradation by them.   
• Keep buspirone away from your children.  

How does buspirone affect pregnancy and lactation?

• Buspirone is classified as pregnancy category B.

The use of buspirone during pregnancy has not been clinically studied, and our understanding of its risks is limited.

Nursing mothers should not take buspirone because it will pass into breast milk and be ingested by the baby. 

• If stopping the drug is not an alternative, breastfeeding should not be started or should be discontinued.   

Buspirone should be avoided during pregnancy, particularly in the first trimester. The use of buspirone during pregnancy should be considered only when the need for the medication outweighs its risk and alternative therapies have failed.    

What happens when you take an overdose of buspirone?

Buspirone overdoses are rarely lethal.

• Drowsiness, confusion, somnolence, weariness, dropped coordination, clumsiness while walking (ataxia), and sluggish reflexes are some of the mild indications of buspirone overdose.   

When taken alone, buspirone hardly causes death. When some drugs (CNS depressants) participate in buspirone overdose, severe symptoms such as trouble breathing, slowing heart rate, decreased blood pressure, lack of coordination, and loss of consciousness lead to coma and death.  

• Every potential overdose should be considered an emergency at the ER. The prescription bottle of the drug along with any extra drugs linked to the overdose should also be brought, as the data on the prescription label can help the treating physician estimate the quantity of pills consumed.  

What are the drugs contraindicated with buspirone usage?

• Erythromycin and clarithromycin may inhibit the metabolism of buspirone and lead to adverse side effects.

Antifungals such as ketoconazole and itraconazole may inhibit the metabolism of buspirone and increase the likelihood of adverse side effects.

•  Nefazodone may markedly increase the blood levels of buspirone and increase the likelihood of adverse side effects.

 Monoaminoxidase inhibitors (MAOIs) such as phenelzine and tranylcypromine should not be combined with buspirone.

• There have been reports of elevated blood pressure when buspirone was added to medication regimens, including an MAOI.