Buspirone

Buspirone is a drug belonging to the anxiolytic class of drugs that is used to treat anxiety disorders. It acts as an anxiolytic, i.e. An anti-anxiety drug, but unlike benzodiazepines (for example, diazepam or alprazolam), it is not hypnotic and does not cause sedation.

Buspirone is usually used to treat generalized anxiety disorder (GAD), but can also be used for short-term relief of anxiety symptoms. It does not cause physical dependence, as some other anxiolytics can, and has fewer side effects.

This drug does not begin to work immediately, but gradually, so its effects may take several days or weeks to appear after you start taking it. The dosage and regimen of buspirone is usually determined by the doctor depending on the specific symptoms and individual characteristics of the patient.

Indications Buspirone

1. Generalized Anxiety Disorder (GAD): Buspirone may be used as a long-term treatment to reduce anxiety symptoms in patients with GAD. OTD is characterized by feelings of unreasonable anxiety or worry most of the time for several months.
2. Short-term relief of anxiety symptoms: Buspirone can also be used for short-term relief of anxiety symptoms, especially in cases where quick relief from anxiety is needed.
3. Social anxiety disorder: In some cases, buspirone may be used to treat social anxiety disorder, characterized by intense anxiety about social or work situations.

Release form

1. Tablets: This is the most common form of buspirone. The tablets come in different strengths, such as 5 mg, 10 mg, 15 mg or 30 mg, and are usually taken orally with water.
2. Solution: Buspirone can also be provided as an oral solution.
3. Capsules: Some capsules may contain buspirone and are also taken orally with water.

Pharmacodynamics

1. Action on serotonin receptors: Buspirone is a partial agonist of 5-hydroxytryptamine (5-HT1A) receptors, which are associated with serotonin in the central nervous system. This leads to increased activity of the serotonergic system, which may help reduce anxiety.
2. Modulation of neurochemical balance: Buspirone may also affect the dopamine and norepinephrine systems, although its precise mechanism of action on these systems is not entirely clear.
3. No effect on benzodiazepine receptors: Unlike benzodiazepines, buspirone does not bind to GABA-A receptors, making it less likely to cause dependence or tolerance.
4. Slow onset of action: Unlike benzodiazepines, the onset of action of buspirone may take several days or weeks after the start of treatment, which may be due to the need to build up the concentration of the drug in the body.
5. Long-lasting action: Buspirone has a long-lasting effect, which allows it to be used as an anxiolytic for a long time.
6. Minimal Impact on Cognitive Function: Unlike benzodiazepines, buspirone does not typically cause drowsiness or lethargy, and it has minimal effects on cognitive function, making it more acceptable for patients who need to remain alert and alert.
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Pharmacokinetics

1. Absorption: After oral administration, buspirone is rapidly and completely absorbed from the gastrointestinal tract. Peak plasma concentrations are usually achieved 1-1.5 hours after administration.
2. Distribution: Buspirone is well distributed throughout the organs and tissues of the body. It has a high affinity for blood plasma proteins, mainly albumin.
3. Metabolism: Buspirone is metabolized in the liver to form the active metabolite, hydroxybuspirone. The main metabolic pathway is hydroxylation followed by conjugation. Metabolites of buspirone and hydroxybuspirone are pharmacologically active.
4. Excretion: Buspirone and its metabolites are excreted mainly in the urine in the form of conjugates and unconjugated forms.
5. Half-life: The half-life of buspirone is approximately 2-3 hours, and the half-life of hydroxybuspirone is approximately 3-6 hours.

Dosing and administration

1. Dosage for adults for general anxiety disorder:

   • The starting dose is usually 7.5 mg twice daily.
   • The dose can be gradually increased at intervals of several days. The usual maintenance dose is 15 to 30 mg per day, divided into several doses.
   • The maximum recommended dose is 60 mg per day, divided into several doses.

2. Recommendations for use:

   • The tablets should be taken regularly, at the same time every day, to maintain an even level of medication in the blood.
   • The tablets should be swallowed whole, without chewing or crushing, with water.
   • Buspirone should be taken at the same time every day, regardless of meals, but it is best to take it in the same regimen - either always with food or always without food, since food can change the absorption of the drug.

3. Special instructions:

   • The effect of using buspirone does not develop immediately and may require several days to several weeks of regular use to achieve noticeable improvement.
   • You should not stop taking buspirone suddenly, as this may cause withdrawal symptoms. If it is necessary to stop treatment, the dose should be gradually reduced under the supervision of a physician.

Use Buspirone during pregnancy

1. FDA classification:

   • Buspirone is classified as a Category B drug by the FDA. This means that animal studies have shown no risk to the fetus, but no controlled studies have been conducted in pregnant women. Therefore, the drug should be used during pregnancy only in cases where the potential benefit justifies the potential risk to the fetus.

2. Data and recommendations:

   • There is insufficient data on the safety of buspirone during pregnancy. Although animal studies have shown no direct negative effects on fetal development, the lack of sufficient data from human studies warrants extreme caution.

3. Potential risks and precautions:

   • As with any medication during pregnancy, it is important to minimize any drug exposure. If possible, it is best to consider alternative treatments for anxiety, such as psychotherapy or lifestyle changes, which are safer for the child's development.

4. Consultation with a doctor:

   • If you are pregnant or planning a pregnancy and are prescribed buspirone, it is important to discuss the risks and benefits with your doctor. Your doctor can help you evaluate your condition and make an informed decision about whether to continue using buspirone.

Contraindications

1. Individual intolerance: People with a known individual intolerance to buspirone or any other component of the drug should avoid its use.
2. Severe hepatic impairment: In patients with severe hepatic impairment, the use of buspirone may be contraindicated due to the potential for increased side effects and toxicity.
3. Severe renal impairment: In patients with severe renal impairment, the use of buspirone may be contraindicated due to the potential for increased side effects and increased elimination time from the body.
4. Combination with MAO inhibitors: Buspirone should not be used concomitantly with monoamine oxidase (MAO) inhibitors as this may result in serious adverse interactions, including an increased risk of serotonin syndrome.
5. Pregnancy and breastfeeding: The safety of buspirone during pregnancy and breastfeeding has not been fully established. Use must be agreed with a physician, and the risk to the fetus or child must be assessed.
6. Pediatrics: Buspirone is not recommended for use in children and adolescents under 18 years of age due to insufficient data on efficacy and safety in this age group.
7. Acute life-threatening or severe mental disorders: Buspirone is not the drug of choice in case of acute threat

Side effects Buspirone

1. Dizziness or drowsiness: These symptoms may occur especially when starting to take the drug or when changing the dosage.
2. Headache: Some people may experience headaches while taking buspirone.
3. Feeling sick or tired: Some patients may feel weak or tired.
4. Dry mouth: This side effect is quite common and can be uncomfortable, but usually does not cause serious problems.
5. Gastrointestinal disorders: Possible side effects include nausea, vomiting, constipation, or diarrhea.
6. Muscle cramps: Some people may experience muscle cramps or unusual movements.
7. Insomnia: Some patients may experience difficulty falling asleep or insomnia.
8. Sensitivity to light: Some people may have trouble tolerating bright light.

Overdose

1. Drowsiness and lethargy: Increased drowsiness and lethargy may occur, which may be accompanied by difficulty concentrating and coordinating movements.
2. Dizziness and headache: Increased dizziness and headache may occur.
3. Tachycardia and cardiac disorders: Increased cardiac activity may occur, which can lead to tachycardia or arrhythmias.
4. Respiratory depression: In rare cases, a decrease in the frequency and depth of breathing may occur, especially with concomitant use of other central nervous system depressants.
5. Convulsive conditions: Convulsions may occur, especially in persons with a predisposition to this.

Interactions with other drugs

1. Liver enzyme inhibitors (cimetidine, erythromycin, clarithromycin): Liver enzyme inhibitors may increase the blood level of buspirone, which may increase its effects and increase the risk of side effects.
2. CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir): CYP3A4 enzyme inhibitors may also increase the blood level of buspirone, which may result in increased effects and an increased risk of side effects.
3. Liver enzyme inducers (carbamazepine, phenytoin): Liver enzyme inducers may reduce the blood level of buspirone, which may reduce its effectiveness.
4. Alcohol and sedatives: Buspirone may increase the effects of alcohol and other sedatives such as hypnotics and anxiolytics, which may result in an increased risk of side effects such as drowsiness and slower reactions.
5. Drugs affecting the cardiovascular system (β-blockers, antihypertensives): Buspirone may increase the effects of drugs affecting the cardiovascular system, which may result in increased blood pressure or slowed heart rate.
6. Drugs for the treatment of mental disorders (MAO inhibitors): Buspirone is not recommended concomitantly with drugs that inhibit monoamine oxidase (MAO inhibitors) as this can lead to serious side effects such as hypertensive crisis.