Buspirone

Chemical name

8-[4-[4-(2-Пиримидинил)-1-п��перазинил]бутил]-8-аза спиро[4.5]декан-7,9-дион (and as hydrochloride)

Gross

C21-H31-N5-O2

Characteristics

Buspiron hydrochloride, a white crystalline powder. It is soluble in water.

Of drugs

Drugs, the anxiolytic. For high affinnostew to form (agonist), and postsinapticski (partial agonist) serotoninovm receptor subtype 5-NT_1A. Decreases synthesis and the release of serotonin, activity serotoninergicakih neuronal incl. in the dorsal nucleus seam. Yes blocks (antagonist) pre - and postsinapticalkie D_2-dofaminove receptors (with a moderate affinity), and increases the speed of an dofamine secondary neuronal brain. Some evidence suggests an impact on other neiromediatorne system. It has an affinity to benzodiazepinovm receptors does not affect the binding Gamk.effect has gradually been through 14 days and reaches its maximum at 4 weeks. Has no adverse effects on psychomotor functions, it is tolerance, drug dependence and withdrawal symptoms. Not potenziruet of alcohol. Studies have shown the effectiveness buspirona in autism, обсессивно-компульси��ных disorders, predmenstrualnom syndrome, sexual dysfunction and easing symptoms for end Kurenia.pri a long rats (within 2 years) in doses of 133 loads MRDC or mice (within 1.5 years) in doses 167 times exceeding MRDC, cancer is not detected. There has mutagenic properties. In rats and rabbits with doses 30 times higher than MRDC, the impact on fertility, and the adverse effects of a fetus were observed. Buspiron and its metabolites infiltrating breast milk Kras.posle intake of rapidly and completely absorbed from the intestine and are extensive presistemnomu metabolizmu. The "first pass" through the liver and gidrauxiliruetsa dealkiliruetsa (bioavailability-4%). N-dealkilirovanny ethyl - 1-пиримидинилпиперази н is pharmacologically active (anksiolitical activity is 1 / 4 buspirona it). After receiving doses of 20 mg C_max achieved through 40-90 minutes at 1-6 ng / J Linking plasma protein-95%. Simultaneous eating reduces the intake, but increases the number of unchanged drug reaching systemic blood flow (AUC and C_max buspirona increased by 84% and 116%, respectively) as a result of braking presistemnogo ground). Write memory (29-63%) in the form of metabolites and unchanged to (1%), as well as blood (18-38%). T_1/2 buspirona - 2-3 hour T_1/2 active metabolita 4.8 hours

Indications

Generalizovannoe disturbing disorder, panic disorder syndrome vegetative dystonia, alcohol syndrome symptoms (secondary treatment), depression (secondary treatment).

Restrictions on the use of

Age 18 (safety and efficacy of the application of non-identified).

Pregnancy and lactation

Contraindicated in pregnancy. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, severe violations of the kidneys and liver, glaucoma, male gravis, pregnancy, breast-feeding.

Side-Effects

From the nervous system and sensory organs : dizziness (12%), drowsiness (10%), headache (6%), nervousness (5%), fatigue (4%), insomnia (3%), decreasing ability to focus (2%); Ekstrapiramidnye disorders (very rarely); 2% clear view sputannosti consciousness or depression, weakness, numbness; 1% neurological symptoms (muscle weakness, pricking, pain or weakness in the hands or legs, uncontrollable body movements). From the circulatory system and blood (blood, gemostaz) : 1% tachycardia / strong Serdzebienie.so part of the intestine : nausea (8%), dry mouth (3%), diarrhea (2%); 1% vomiting, constipation; demotion Appetita.prochie : 1% mialgia, cramps, stiffness or rigidity of muscles, skin rashes, skin.

Specific guidance

It should be borne in mind that anxiety or stress in the day-to-day stress, usually do not require treatment anxiolitikami.

Patient interaction

When combined with MAO inhibitors may develop gipertoniceski kriza.

Overdosing

Symptoms : nausea, and vomiting, etc. gastrointestinale disorders, dizziness, unconsciousness, Sonlivosti.lechenie : washing stomach, the appointment of activated carbon symptomatic therapy. Dialysis ineffective.

Precautions

To apply caution while neiroleptikami, antidepressants, cardiac glycosides, and antigipertenzivei antidiabeticakimi means oral contraceptives. In kidney and liver failure mild, cirrhosis of the liver designate smaller doses and under strict medical supervision. The treatment should be deleted alcohol. Early treatment with a caution during the drivers of vehicles and people skills relate to the high concentration of attention.

Dosing and Administration

Inside. The recommended initial dose, 5 mg three times a day, if necessary it can be increased by 5 mg every 2-3 days. The average daily intake of 20 to 30-mg. The maximum single dose of 30 mg daily to 60 mg.

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