Buspirone is an anti-anxiety medication that modulates brain chemicals that give the user a sense of calmness. However, unlike other drugs of this class, its mechanism of action does not imply binding with GABA receptors.
It is used to treat the signs and symptoms of anxiety, such as irritability, fear, tension, dizziness, tachycardia, and other physical symptoms.
It is also used to treat depression. Buspirone has the chemical formula 8- [4- [4- (2-pyrimidinyl) -1-piperazinyl] butyl] -8-azaspiro [4.5] decane-7,9-dione monohydrochloride. Its molecular weight is 422, and it has the following structural formula:
The most used trade for buspirone is BuSpar.
The exact mechanism of action of buspirone is unknown. However, in vitro studies have shown that it has a high affinity for both presynaptic 5HT serotonin and postsynaptic 1A receptor.
Serotonin is a molecule that binds to these receptors and through various experiments has been shown to have a positive influence on our moods and cognition.
Thus, while the exact mechanism of action is unknown, it is believed that the drug maintains a balance of the activity of these receptors and therefore plays a role in improving mood.
Buspirone is also a weak antagonist of dopamine D2 receptors. These receptors are presynaptic receptors, and when they are activated, they decrease the production and release of dopamine.
These receptors are particularly abundant in the nigrostriatal pathway, so when these receptors are blocked, the amount of dopamine in this pathway increases and this also improves mood.
Since its mechanism of action is unique and does not involve binding to GABA receptors, buspirone is the only anxiolytic drug that does not cause sedation.
The FDA has approved the use of buspirone for anxiety disorders and symptoms associated with them, such as fear, insomnia, irritability, palpitations, sweaty hands, and other physical signs and symptoms. A selective serotonin reuptake inhibitor (SSRI) augmentation drug has also been indicated for the treatment of depression.
Out-of-label uses include treating the negative symptoms of schizophrenia, hypoactive sexual desire disorder in women, attention deficit hyperactivity disorder and agitation and aggression in elderly patients with dementia.
It is noteworthy that all these outside uses of the label are still under investigation and, therefore, the doctor must first try other drugs, proven in the treatment of these diseases. Buspirone should only be given if the FDA approved medications for these diseases do not show the desired effect.
The recommended initial dose of buspirone to treat general anxiety disorders is 15 mg (7.5 mg, twice daily). However, if the desired effect of the dose is not obtained, it can be increased to a maximum of 60 mg per day. The recommended form of dose increase is that the dose should be increased after 5 mg every two or three days.
While the prescription of the drug for off-label uses, the doctor can use their experience and the severity of the disease, since there are no guidelines for the dosage of these diseases.
In mild liver or moderate to moderate renal failure, the dose of buspirone needs to be adjusted. The reduction of the recommended dose is 25-50%.
In severe kidney or liver disease, the drug must be discontinued because the drug is metabolized by the liver and excreted primarily by the kidneys.
Buspirone has a unique mechanism of action than other anxiolytics. Therefore, its onset of action also differs from other anxiolytics.
While benzodiazepines and barbiturates take only hours to exert their effects, buspirone can take 2 to 4 weeks to fully exert its effect on the body. So this medication is not indicated during short periods of anxiety such as exams.
Buspirone remains in the system usually 18-24 hours. Buspirone is excreted up to 63% in 24 hours. It has a half-life of only a few hours. Due to its short half-life, this drug excretes urine, blood, hair, and saliva within 18-24 hours.
Usually, the drug leaves the body as fecal excretion and metabolites. It is absorbed quickly in the body.
Suffers significant first-pass metabolism. When the buspirone levels were verified in the patients after their treatment, the results came out in which it was evident that this drug remains unchanged in the blood only about 1% and this occurs in 2-3 hours. The rest of the drug is eliminated from the body.
When buspirone is administered in the body, 86% of them are bound to plasma proteins. Flurazepam decreases free plasma levels of buspirone in the blood. Flurazepam does this by almost 20%.
For another hand, aspirin increases blood levels of free buspirone. Aspirin raises the levels of free buspirone by almost 23%. Both of these rising and decreasing effects on free blood buspirone levels due to the effect of flurazepam and aspirin are observed in vitro.
This can not be said if similar effects would be observed inside the body or not.
The first-pass metabolism of buspirone is very effective, and its metabolism is mediated by the CYP3A4 enzyme. Any drug that causes any change in the action of the CYP3A4 enzyme will make the change in metabolism and the effects of buspirone in the body.
Buspirone is a fast-acting medication and has a short half-life. This is very beneficial since it prevents the body from the adverse effects of this drug. The short half-life, excreted hair, urinate blood and saliva.
Buspirone is a selective anxiolytic, with minimal CNS depressant effects. It does not affect driving ability and does not have muscle relaxant or anticonvulsant properties.
The drug interacts with 5HT 1Atype of serotonin receptor brain as a partial agonist, but the exact mechanism of this anxiolytic effect is unexplained. Buspirone has a slow onset of action (2-4 weeks).
The development of tolerance is minimal with chronic use, and there is little rebound anxiety or withdrawal symptoms when discontinuing. Buspirone is metabolized by the CYP3A4 enzyme, and its levels in plasma are considerably raised by drugs such as erythromycin and ketoconazole.
Side effects of buspirone include tachycardia, paresthesia, pupillary constriction, and GIT anguish. Buspirone has minimal risk of abuse and is not a controlled drug schedule. The drug seems to be safe during pregnancy. However, if a pregnant woman is going to take this medication, then she should inform her doctor about it.
It is chemically not linked to barbiturates, anxiolytics, sedatives or benzodiazepines. Buspirone also has an affinity for D2 receptors in the brain. Other neurotransmitters can also be affected by buspirone. To summarize, due to the low half-life, this drug, i.e., buspirone, exits the system within 24 hours.
It does not appear on a drug test. Technically speaking, buspirone should never appear on a drug test as something positive. It is always a negative result as far as the buspirone is considered.
But lately, many false positives have appeared, and now this issue is under discussion. If it appears on a drug test result as positive, then it is most likely to appear as the benzodiazepine.
In most cases and false positive results, the substance that causes the false positive result is benzodiazepine. Well, the false positive result may be due to the poor quality of the tests, but it can not be said with certainty, it could be benzodiazepine, this is still under debate.
In all cases in which the result was false positive, the medication appeared as benzodiazepine, but as it is stated that this class of anxiolytic drugs has no connection with the benzodiazepines. This is the complex point in the drug tests of this drug. Some pharmacists now believe that buspirone can show as benzodiazepine in a drug test.
Above all, the result of the drug test for buspirone is negative, which means that it does not show up on the drug test, but only a few cases have been seen in which the buspirone shows up as the benzodiazepines.
edications buspirone (BuSpar) is spitomin. Reviews of patients showed that its action is identical to the action of buspiron.
Many of the subjects had depressive symptoms. Reception of buspirone hydrochloride in tablets eased the anxiety of the subjects as well as helping to get rid of depressive symptoms.
The evaluated patients in these studies had symptoms of these mental disorders for 1 month and more than 1 year before the study, with an average duration of anxiety symptoms of 6 months.
The following is a list of symptoms that subjects may have felt when taking buspirone (BuSpar) during the course of studies: profuse sweating, nervousness, trembling in the limbs, constant tension, muscle pain, fatigue, inability to relax, twitching eyelids eyes, constant tense facial expression, fussiness, anxiety, light unreasonable fright, sticky hands, dry mouth, dizziness, paresthesia (tingling in hands or feet), stomach upset, frequent urination, diarrhea, discomfort in the epigastric region of the Stomach, lump in the throat, hyperemia, pallor, high pulse at rest of the body, high respiratory rate.
Also, during the study, about 10% of 2200 patients who took buspiron for 3 to 4 weeks-stopped treatment due to adverse effects on their body.
The most common cases of discontinuation of the drug were: disorders of the nervous system (3.4% of the subjects), mainly the following symptoms were established: dizziness, insomnia, nervousness, drowsiness, gastrointestinal disorders.
In 1.2% of the subjects were identified the following negative effects of the drug: nausea and mixed disorders listed above. Also, 1.1% of the subjects were constantly observed headaches and fatigue.
Do not use buspirone (BuSpar) if you have taken medicines related to MAO inhibitors (Phenelzine, Iproniazid, Isocarboxazid, Nialamide, Tranylcypromine) during the last 14 days.
Combination with MAO inhibitors is not recommended due to the risk of hypertensive crisis. This drug can be used during pregnancy only in cases of urgent need.
Studies conducted on animals have not revealed any damage to the fetus, but to date, studies on pregnant women have not been conducted.
Animal studies have not shown an increased incidence of intrauterine injuries and have failed to prove the risk to the fetus. Also, this drug should not be used during breastfeeding, if its use is not clinically necessary.
Buspirone (BuSpar) increases serum prolactin levels. However, the mother’s prolactin level cannot affect her ability to feed her baby. However, there is no available information about the long — term use of this drug during breastfeeding.
According to studies in a woman who took buspiron 15 mg 3 times a day during pregnancy and in the postpartum period — on the 13th day after birth, buspirone (BuSpar) was not found in breast milk.
Also Buspirone (BuSpar) was not detected in the serum of the baby during the necessary tests. The blood of the child was taken for testing between 13 and 21 days after birth.
However, these studies do not confirm the possibility of taking buspirone (BuSpar) nursing mothers because the results can be achieved due to the individual characteristics of the organism of the nursing mother.
Do not use buspirone (BuSpar) if you are allergic to buspirone (the active substance). To make sure that buspirone (BuSpar) is safe for you, tell your doctor if you have kidney disease or liver disease.
Only after passing the necessary tests and doctor’s permission You can take this medicine.
There are some restrictions in case of violations of the functioning of internal organs. For example, in the presence of liver problems should be careful during treatment and constantly monitor the changes that occur in the body.
Contraindications are only severe disorders in the functioning of the organs. The same applies to the kidneys.Buspiron should not be taken by persons under 18 years of age (unless otherwise prescribed by your doctor).
Before you start taking this medicine, consult your doctor. Your doctor will select a more professional dose of medication that you will need to take.
Do not take buspirone (BuSpar) in larger or smaller amounts (prescribed by your doctor) or for longer than recommended.
You can take buspirone (BuSpar) at any time convenient for you (before meals, during or after meals).
Tablets of some manufacturers of buspirone (BuSpar) are specially made so that they can be divided into several parts.
Do not use the tablet if it has not been properly broken/separated and the medication proves to be more or less than the dose you need.
If you have switched to buspirone (BuSpar) after using another drug that suppresses anxiety, do not stop taking this drug abruptly and immediately, as this can lead to degradation of the previously obtained results (this effect occurs especially often with prolonged use of a certain drug).
Buspiron can also cause false positive results during some medical tests. Therefore, it is recommended to stop taking the medicine 48 hours before the test, as well as notify your doctor that you are using buspar (buspar).
If you have missed the drug, simply continue to take buspirone (BuSpar) at the appointed time. Do not try to take an additional dose of medication to make up for the missed dose. If you overdose with buspirone (BuSpar), consult your doctor immediately.
Also, this drug can cause damage to the processes of thinking (perhaps a certain clouding of thoughts) or deterioration of the reaction. Be careful if you notice such a reaction to the drug-inform your doctor. Alcohol consumption while taking buspirone (BuSpar) is not recommended.
In addition, grapefruit and grapefruit juice when interacting with buspiron can lead to undesirable side effects. Discuss the use of these products with your doctor.
If this is not possible, a dose of buspiron should be taken at least 2 hours before or 8 hours after consuming grapefruit or grapefruit juice.
A large amount of grapefruit and grapefruit juice can cause an increase in the level of the active substance in your blood, which in turn can lead to an increase in side effects, such as drowsiness.
During treatment, it is not recommended to drive a vehicle (at least in the initial stage of treatment) as possible manifestations of adverse reactions from the Central nervous system and psyche.
• You may have difficulty breathing,
• Your face, lips, tongue or throat swells,
• Chest pain,
• Erratic breathing,
• Sensitivity to light,
• Dizziness, drowsiness,
• Sleep problems (insomnia),
• Nausea, indigestion,
• Skin rash or hives,
• Confusion in the head,
• This list is not exhaustive.
• Symptoms of overdose:
• Dizziness or weakness, especially often this symptom manifests itself with a sharp change in body position (lie down or stand up sharply),
• Loss of consciousness,
• Nausea or vomiting,
• Constriction of the pupils of the eyes,
• Blurred vision,
• Excessive sweating,
• The decrease in the concentration of,
• Dry mouth,
• Muscle aches, cramps, cramps,
• Sleep problems (nightmares or too vivid dreams)
• Unusual fatigue or weakness.
Some of the side effects that can occur when taking buspiron do not require medical attention and further self-removal with continued treatment.
If any of the above side effects continue to bother you for a long time, consult your doctor.
Initial dose: 7.5 mg orally (oral medication) twice a day or 5 mg 3 times a day. Penetrating into the body, for a short period of time the drug is completely absorbed into the gastrointestinal tract.
As a result of intensive metabolism, bioavailability is only 4%. The maximum level of the active substance is reached in the blood about an hour after entering the gastrointestinal tract. Half-life of the drug is carried out in 2-3 hours.
Plasma protein binding corresponds to 95%. Continuous use of the drug does not affect its effectiveness.
Buspirone tablets (BuSpar) should be taken only as a whole, they can not be dissolved in water or other liquid, as well as grind and chew.
The duration of the recommended course of treatment involves 4 months. Longer than this time to take buspirone (BuSpar) is not recommended.
The daily dose can be increased by 5 mg for every 2 to 3 days and brought to 20 to 60 mg per day. Maximum dose: 60 mg per day.
Children from 6 to 18 years recommended initial dose-from 2.5 to 10 mg per day.
As a result of the use of buspirone (BuSpar) reviews of patients undergoing treatment, rarely carry information about serious side effects.
The course should be based on the characteristics of the body being treated, his health and in the optimal doses for each case. Despite the constant control of the doctor, the patient is obliged to study the instructions before starting treatment.
Buspirone (BuSpar) – a drug that usually does not lead to the development of side effects and overdose, almost non-addictive, negative manifestations after its cancellation and in most cases copes with the task.
Replacement of this drug with an analogue should be performed after receiving a doctor’s advice. A good analogue of the medications buspirone (BuSpar) is spitomin. Reviews of patients showed that its action is identical to the action of buspiron.
This is due to the presence of the same active component in the formula of the drug. This drug should be taken at the same time every day, the usual therapeutic dose is from 15 to 30 mg daily in separate doses, the dosage must be individualized for each patient.
This drug should be reviewed periodically if you take it for an extended period. The effectiveness of this drug is manifested in the reception of 3 to 4 weeks, but no more.
Also, buspirone (BuSpar) is not usually used to treat anxiety or psychological tension associated with stressful situations in everyday life.
Buspirone should not be taken during or within 14 days of use of monoamine oxidase inhibitors (MAOI), due to the risk of developing serotonin syndrome (characterized by high blood pressure, fever, sweating, and tremors).
Since buspirone has no proven effectiveness in the treatment of psychotic disorders, it should not be used as a first-line antipsychotic drug.
Buspirone is a drug classified in category B of the FDA. This means that there are not many studies on the safety of buspirone in pregnant women have been carried out. However, animal studies show no harm to the fetus. So if the doctor considers it essential, then buspirone is not contraindicated.
The use of buspirone in breastfeeding mothers remains controversial. An exclusively breast milk 11-week-old infant whose mother took 10 mg of this drug and 300 mg of venlafaxine a day did not show adverse reactions, but since limited information on this topic, the drug should be avoided until it is necessary.
Medications that are notorious for interacting with buspirone include:
If you are in any of the above medications or have recently finished the chronic use of the above drugs, it is advisable to inform your doctor.
Patients with severe kidney disease and acute liver disorders should not take buspirone. It is contraindicated in these patients.
If patients are hypersensitive to buspirone hydrochloride, then it should not be taken. Otherwise, it would lead to a severe hypersensitivity reaction in these patients. One thing that is very important is that if the patient has taken any type of monoamine oxidase inhibitor in the last 14 days, then he should not take this medication, ie buspirone.
If the patient takes buspirone along with monoamine oxidase inhibitors, then it is more likely that it would result in high blood pressure.