Buspar 10 mg Tablets

Brand name

The trade name of the drug is Buspar. This is the registered name under which the drug is known on the pharmaceutical market and used in clinical practice.

International Nonproprietary Name (INN)

The international nonproprietary name is buspirone. It denotes the active active ingredient and is used in medical documentation worldwide.

Form of release

Buspar is available as tablets with dosages of 5 mg, 10 mg and 15 mg, packed in blisters of 10, 20 or 30 pieces. Tablets have a white color, flat shape and a risk for easy division. The drug is not available in other forms, such as capsules or solutions, which simplifies its use and dosing at home.

Composition

Active substance

The main active ingredient is buspirone hydrochloride. One tablet contains 5 mg, 10 mg or 15 mg of buspirone hydrochloride, depending on the dosage.

Auxiliary Components

The tablets include excipients such as lactose monohydrate, microcrystalline cellulose, sodium starch glycolate, magnesium stearate, and colloidal anhydrous silicon dioxide. These components provide stability, solubility and convenience of the drug.

Pharmacologic Properties

Pharmacodynamics

Buspirone, the active ingredient of Buspar, has a unique anxiolytic action that differs from the mechanisms of benzodiazepines or barbiturates. It acts as a partial agonist of serotonin 5-HT1A receptors located in presynaptic and postsynaptic regions of the brain. This interaction modulates serotoninergic transmission, reducing the overactivity of neurons associated with anxiety. In addition, buspirone has a weak effect on dopamine D2 receptors, which may contribute to its calming effect without significant central nervous system depression.

In contrast to drugs acting via GABA receptors, Buspar does not cause sedation, muscle relaxation, or habituation, making it safe for long-term use. The therapeutic effect develops gradually: the first signs of anxiety relief appear after 1-2 weeks, and maximum effectiveness is achieved after 4-6 weeks of regular use. The drug does not affect cognitive functions and does not interfere with daily activity, which is especially important for patients with an active lifestyle.

Pharmacokinetics

Absorption

Buspirone is rapidly absorbed from the gastrointestinal tract after oral administration. The maximum plasma concentration is reached in 0.5-1 hour, but bioavailability is only 4% due to the significant effect of first passage through the liver. Food intake slows the rate of absorption, but increases total bioavailability due to decreased hepatic metabolism.

Distribution

The drug actively binds to blood plasma proteins (86-95%), mainly to albumin. The volume of distribution is about 5.3 l/kg, indicating good penetration into the tissues of the body, including the brain. Buspirone crosses the blood-brain barrier, ensuring its action on the central nervous system.

Metabolism

Buspirone undergoes extensive metabolism in the liver with the participation of cytochrome P450 enzymes, mainly CYP3A4. The major active metabolite, 1-(2-pyrimidinyl)-piperazine (1-PP), has weak pharmacologic activity and contributes little to the overall effect. Metabolism proceeds in several steps, including hydroxylation and oxidation.

Excretion

The half-life of buspirone is 2-3 hours, which requires multiple doses throughout the day to maintain therapeutic concentrations. The drug is excreted mainly through the kidneys (about 60%) in the form of metabolites, and the rest - through the intestine. Complete elimination from the body takes about 24 hours.

Indications for Use

Buspar is prescribed for the treatment of the following conditions:

• Generalized anxiety disorder (GAD) with symptoms of anxiety, tension and irritability;
• Anxiety states associated with depression (as part of a complex therapy);
• Short-term treatment of acute anxiety caused by stressful situations;
• Symptomatic relief of psychosomatic manifestations of anxiety (palpitations, sweating).

The drug is effective for patients who require anxiety reduction without sedation or risk of dependence.

Contraindications

The use of Buspar is prohibited in:

• Hypersensitivity to buspirone or auxiliary components;
• Severe hepatic insufficiency (due to slow metabolism);
• Severe renal insufficiency (creatinine clearance less than 20 ml/min);
• Simultaneous administration of MAO inhibitors (a break of 14 days is required);
• Pregnancy and lactation;
• Children under 18 years of age (due to insufficient data).

Prescribe with caution in epilepsy, glaucoma, or moderate liver and renal dysfunction.

Method of Administration and Dosage

How to take

Buspar tablets are taken orally, drinking water (100-150 ml). For stable absorption it is recommended to take the drug at the same time of day, preferably with food to increase bioavailability. Tablets can be divided by risk for accurate dosing.

Dosages for adults and children

Adults

The initial dose is 5 mg 2 to 3 times daily. After 2-3 days, the dose is increased by 5 mg every 2-3 days until the effect is achieved (usually 20-30 mg/day divided into 2-3 doses). The maximum daily dose is 60 mg.

Children

The drug is not used in children under 18 years of age due to lack of sufficient data on safety and efficacy.

Dose adjustment in certain conditions

In moderate hepatic or renal insufficiency the initial dose is reduced to 5 mg 1-2 times a day with a slow increase under the supervision of a doctor. In severe disorders the drug is contraindicated.

Side Effects

Possible adverse reactions include:

• Nervous system: dizziness, headache, insomnia, nervousness;
• Gastrointestinal system: nausea, dry mouth, abdominal discomfort;
• Cardiovascular system: tachycardia, feeling of tightness in the chest;
• Allergic reactions: rash, itching, rarely - angioedema;
• Other: weakness, sweating, tremor.

The side effects are usually mild and decrease with adaptation to the drug.

Overdose

Symptoms of overdose

Doses above 60-100 mg may cause nausea, vomiting, drowsiness, confusion, in severe cases - depression of consciousness.

First aid measures

Stop taking, call a doctor. Before medical assistance, the stomach is washed (if less than one hour has passed) and activated charcoal is given.

Drug Interactions

Influence on the effects of other drugs

Buspirone enhances the effects of sedatives and antidepressants. CYP3A4 inhibitors (ketoconazole, erythromycin) increase its concentration in the blood, and inducers (rifampicin) reduce its efficacy.

Compatibility with alcohol and food

Alcohol increases mild CNS side effects. Food increases bioavailability, which is beneficial for efficacy.

Special Precautions

Use in pregnancy and breastfeeding

Buspar is not recommended in pregnancy and lactation due to insufficient data. Breastfeeding should be discontinued if treatment is necessary.

Effects on driving and mechanisms

The drug may cause dizziness, so caution is required when driving or operating machinery.

Particularities of use in elderly people and children

In the elderly, the dose is adjusted in case of hepatic or renal dysfunction. In children under 18 years of age the drug is not used.