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|Buspar 10 mg|
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Characteristics of the substance Buspirone
Anxiolytic of non-benzodiazepine structure. Buspirone hydrochloride is a white crystalline powder. Let's well dissolve in water. Molecular weight 422.0.
Pharmacological action - anxiolytic.
It has a high affinity for pre- (agonist) and postsynaptic (partial agonist) serotonin receptors of the 5-HTsubtype1A. Reduces the synthesis and release of serotonin, the activity of serotonergic neurons, incl. in the dorsal nucleus of the suture. Selectively blocks (antagonist) pre- and postsynaptic D2-dopamine receptors (has moderate affinity) and increases the rate of excitation of dopamine neurons in the midbrain. Some evidence suggests the presence of an effect on other neurotransmitter systems. It has no affinity for benzodiazepine receptors, does not affect the binding of GABA.
The effect develops gradually, manifests itself after 7-14 days and reaches a maximum after 4 weeks. It does not adversely affect psychomotor functions, does not cause tolerance, drug dependence and withdrawal symptoms. Does not potentiate the effects of alcohol. Studies have shown the effectiveness of buspirone in autism, obsessive-compulsive disorders, premenstrual syndrome, sexual dysfunction, and symptom relief with smoking cessation.
With long-term administration to rats (within 2 years) at doses 133 exceeding the MRDC, or to mice (within 1.5 years) at doses 167 times higher than the MRDC, no carcinogenic effect was found. Does not possess mutagenic properties. In rats and rabbits, when using doses 30 times higher than the MRDC, no effect on fertility and adverse effects on the fetus was observed. Buspirone and its metabolites pass into the breast milk of rats.
After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract and undergoes extensive first-pass metabolism. At the "first pass" through the liver, it is hydroxylated and dealkylated (bioavailability - 4%). N-dealkylated metabolite - 1-pyrimidinylpiperazine is pharmacologically active (anxiolytic activity is 1/4 that of buspirone). After taking a dose of 20 mg, Cmax is reached in 40–90 minutes and is 1–6 ng / ml. Plasma protein binding - 95%. Simultaneous food intake reduces the rate of absorption, but increases the amount of unchanged drug that reaches the systemic circulation (AUC and Cmax of buspirone increases by 84 and 116%, respectively) due to inhibition of presystemic clearance). It is excreted by the kidneys (29-63%) in the form of metabolites and unchanged (1%), as well as the gastrointestinal tract (18-38%). T1/2 buspirone - 2-3 hours, T1/2 of the active metabolite - 4.8 hours
Application of the substance Buspirone
Generalized anxiety disorder, panic disorder, vegetative dystonia syndrome, alcohol withdrawal syndrome (auxiliary therapy), depression (auxiliary therapy).
Hypersensitivity, severe renal and hepatic dysfunction, glaucoma, myasthenia gravis, pregnancy, breastfeeding.
Restrictions on use
Age up to 18 years (safety and efficacy have not been determined).
Application during pregnancy and lactation
During pregnancy, use only if necessary.
FDA action category on the fetus is B.
Breastfeeding should be discontinued during treatment.
Symptoms: nausea, vomiting, and other gastrointestinal disorders, dizziness, miosis, drowsiness.
Treatment: gastric lavage, the appointment of activated carbon, symptomatic therapy. Dialysis is ineffective.
Precautions for the substance Buspirone
Use with caution in conjunction with neuroleptics, antidepressants, cardiac glycosides, antihypertensive and antidiabetic agents, oral contraceptives. With renal and hepatic insufficiency of mild and moderate severity, liver cirrhosis is prescribed in smaller doses and under the strict supervision of a physician. During the period of treatment, alcohol consumption should be excluded. At the beginning of treatment, use with caution while working for drivers of vehicles and people whose profession is associated with increased concentration of attention.
It should be borne in mind that anxiety or tension associated with everyday stress usually does not require treatment with anxiolytics.
Side effects of Buspirone
From the nervous system and sensory organs: dizziness (12%), drowsiness (10%), headache (6%), nervousness (5%), fatigue (4%), sleep disturbance (3%), decreased ability to concentrate (2%); extrapyramidal disorders (very rare); ≤2% - blurred vision, confusion or depression, weakness, numbness; ≤1% - neurological symptoms (muscle weakness, tingling, pain or weakness in the arms or legs, uncontrolled trunk movements).
From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): ≤1% - tachycardia / palpitations.
From the digestive tract: nausea (8%), dry mouth (3%), diarrhea (2%); ≤1% - vomiting, constipation; decreased appetite.
Others: ≤1% - myalgia, spasms, cramps or muscle stiffness, rash, sweating.