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Quetiapine: General information
Quetiapine is an atypical antipsychotic. Quetiapine and its active metabolite that interacts with receptors in the brain. Quetiapine exhibit high affinity for serotonin 5HT2 receptors of the type of receptors and dopamine D1 and D2 in the brain. Greater selectivity for serotonin 5HT2 receptors of than dopamine receptors of the D2, determines the basic properties of the clinical antipsychotic drug Quetiapine Prolong and low incidence of extrapyramidal side effects. Furthermore, it exhibits high affinity to norepinephrine transporter.
Quetiapine has high affinity for histamine and ?1- adrenoceptors and less affinity for ?2- adrenoceptors and serotonin 5HT1 receptors. Quetiapine shows no appreciable affinity for muscarinic cholinergic, and benzodiazepine receptors. In standard tests Quetiapine exhibit antipsychotic activity. Before use Quetiapine, please consider the following information. The specific contribution of the metabolite in pharmacological activity of Quetiapine is not installed. Results of the study of extrapyramidal symptoms (EPS) in animals showed that Quetiapine causes weak catalepsy at doses effectively blocking receptors of the D2. Quetiapine produces a selective reduction of activity A10 mesolimbic dopaminergic neurons compared to A9 nigrostriatal neurons involved in motor function. One can get Quetiapine at online pharmacy or by visiting local one.
-Schizophrenia, including the prevention of relapse in stable patients;
-bipolar disorder, including:
Quetiapine Prolong is well tolerated when taken in recommended doses, including elderly patients.
Patients age group from 66 to 89 years with dementia receive the drug Quetiapine Prolong in doses from 50 to 300 mg / day reduces the symptoms of depression.
Frequency of EPS and weight stable patients with schizophrenia does not increase during prolonged therapy with Quetiapine Prolong.
Before use Quetiapine, you should know that in studies of major depressive disorder according to the criteria of DSM-IV (Diagnostic and Statistical Manual of Mental Disorders (4th ed.) – Handbook of Diagnostic and Statistical Manual of mental disorders, 4th edition) did not observe an increased risk of suicidal behavior and suicidal ideation while taking the drug Quetiapine Prolong compared to placebo.
If you are looking how to use Quetiapine, you should first consider the information below.
Quetiapine is well absorbed from the gastrointestinal tract. Cmax of Quetiapine and N- dezalkilkvetiapina in plasma is approximately 6 hours after administration of the drug Quetiapine Prolong. Equilibrium molar concentration of the active metabolite N- dezalkilkvetiapina is 35 % of that of Quetiapine.
The pharmacokinetics of Quetiapine and N- dezalkilkvetiapina linear and is dose-dependent nature of the employment drug Quetiapine Prolong at doses up to 800 mg 1 time a day.
Before use Quetiapine, you should know that the treatment with the medicine requires individual dosage.
While taking the drug Quetiapine Prolong 1 time a day at a dose equivalent to a daily dose of the drug Quetiapine, taken as 2 receptions, observed similar AUC, but Cmax was 13% less. Bandwidth AUC metabolite N- dezalkilkvetiapina was 18% less.
Research on the influence of food on the bioavailability of Quetiapine showed that eating a high-fat resulted in a statistically significant increase in Cmax and AUC for the drug Quetiapine Prolong – to approximately 50 and 20 %, respectively. Eating a low -fat diet had no significant effect on the Cmax and AUC of Quetiapine. Recommended to take Quetiapine Prolong 1 time a day away from food.
Approximately 83% of Quetiapine binds to plasma proteins.
Quetiapine and some of its metabolites (including N- dezalkilkvetiapin) have weak inhibitory activity towards cytochrome P450 isoenzymes 1A2, 2C9, 2C19, 2D6 and 3A4, but only at concentrations 5-50 times greater than the concentration observed at the effective dose is usually used 300-800 mg / day.
Based on the results of in vitro, one should not expect that the simultaneous use of Quetiapine with other drugs will result in clinically significant inhibition of the metabolism of other drugs, mediated by cytochrome P450.
Differences in pharmacokinetic parameters in men and women is not observed.
Quetiapine: Side effects
Average Cl Quetiapine in elderly patients is 30-50 % less than in patients aged 18 to 65 years.
Average plasma Cl Quetiapine is reduced by approximately 25 % in patients with severe renal insufficiency (Cl creatinine <30 ml/min/1 73 m2), but the individual clearance figures are within the range identified in healthy volunteers. In patients with hepatic insufficiency (compensated alcoholic cirrhosis), the average plasma Cl Quetiapine reduced by about 25%. As Quetiapine is extensively metabolized in the liver, in patients with hepatic insufficiency may increase plasma concentrations of Quetiapine that require dose adjustment.