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Product trade name: Buspisal
Pharmaceutical active ingredients containing related brand and generic drugs, medications or other health care products: Buspisal available forms, composition, doses: Buspisal destination | category: Indications and usages, anatomical therapeutic chemical and diseases classification codes: Pharmaceutical companies, researchers, developers, manufacturers, distributors and suppliers: Online pharmacy, drugstores, pharma, health and beauty shops selling this or related pharmaceutical products: There is an additional general information about this medication active ingredient buspirone: Pharmacological action Buspisal is an anxiolytic drug, a derivative azaspirodecanedione. The mechanism of action is not established. On pharmacological properties this medication does not apply to benzodiazepines or barbiturates. Buspisal has a selective anxiolytic effect. This medicine has no anticonvulsant activity, it has no myorelaxant action. It has no sedative effects, especially in low doses. Buspisal has a high affinity for serotonin 5-HT1A-receptors in the neurons of the dorsal suture, and moderate affinity for dopamine D2-receptors in the brain. Buspirone has no pronounced affinity for the benzodiazepine receptors, it does not affect the binding of GABA. Unlike benzodiazepines, the level of spontaneous excitation of noradrenergic cells in locus ceruleus (locus ceruleus) under the action of buspirone increases rather than decreases. These specific differences in the scene due to differences in the development of dependence and tolerance between benzodiazepines and buspirone. It is believed that Buspisal does not cause tolerance, physical or psychological dependence. Pharmacokinetics After oral administration Buspisal is rapidly absorbed from the gastrointestinal tract, Cmax plasma levels achieved after 40-90 min. The bioavailability is low due to the pronounced effect in the "first pass" through the liver. When Buspisal is administered together with food it may increase the bioavailability of buspirone due to violation of absorption from the gastrointestinal tract and therefore reduce the first-pass clearance. The binding of buspirone to plasma proteins is about 95%. This medication is subjected to intensive metabolism in the liver, with the participation of isoenzyme CYP3A4. As a result of hydroxylation is produced several inactive metabolites, oxidative dealkylation leads to the formation of 1-(2-pyrimidinyl)-piperazine, which has anxiolytic activity. T1/2 of buspirone is typically 2-4 hours, but the end of T1/2 may be 11 hours. Buspisal derived mainly as metabolites in the urine, as well as in feces. Why is Buspisal prescribed? A treatment of anxiety disorders or the temporary relief of anxiety symptoms. Dosage and administration Buspisal is taken orally, for adults at the beginning of treatment - 5 mg 3 times / day. If necessary the dose increases to 5 mg / day every 2-3 days until the desired effect. The maximum dose is 45-60 mg / day. Buspisal side effects, adverse reactions Possible: dizziness, headache, a syndrome of motor restlessness. Rarely: blurred vision, decreased ability to concentrate, dry mouth, myalgia, muscle cramps, muscle cramps and stiffness, ringing in the ears, sleep disorders, nightmares, fatigue, indigestion, chest pain, depression, tachycardia, paresthesia, sore throat, fever. Buspisal contraindications Pronounced renal dysfunction, pronounced hepatic dysfunction, hypersensitivity to buspirone. Using during pregnancy and breastfeeding Avoid using Buspisal during pregnancy and lactation. Category of the fetus by FDA - B. Special instructions Buspisal is not used to treat anxiety and reduce stress associated with the stresses of everyday life. This medicine should not be used in patients with epilepsy or a history of guidance on the propensity to develop seizures. Use Buspisal with caution in patients with impaired liver and / or kidneys function. Patients who abuse drugs or indications for a history of drug dependence, during treatment require careful monitoring to detect the development of tolerance or dependence to buspirone. In controlled studies it was found that buspirone is not effective for long-term (more than 3-4 weeks) treatment of anxiety. However, when applying Buspisal for a few months there were found no adverse effects. If buspirone is used for a long time, its effectiveness should be checked at regular intervals. During treatment, patients should refrain from activities associated with the need to focus and speed of psychomotor reactions. Safety and efficacy of buspirone in children and adolescents under the age of 18 have not been identified. Buspisal drug interactions Buspirone is metabolized in the liver, with the participation of isoenzyme CYP3A4 and, apparently, may interact with drugs that are inhibitors or inducers of this isoenzyme. In combination with MAO inhibitors it may developed a hypertensive crisis. Buspisal in case of emergency / overdose Symptoms: nausea, vomiting, gastrointestinal and other disorders, dizziness, cramps, drowsiness. Treatment: gastric lavage, the appointment of activated charcoal, symptomatic therapy. Dialysis is ineffective.
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