Đăng xuất
Pharmacology: Pharmacodynamics: Sulpirides belong to the benzamide group, which has antipsychotic effects through selective blockade of dopamine D receptors in the brain. Sulpirides can be thought of as an intermediate between neuroleptics and antidepressants, as sulpirides have both. Sulpirides are mainly used to treat psychotic diseases such as schizophrenia. The mood increases after a few days of treatment, accompanied by the loss of all the symptoms of the disease. Sulpirides do not cause drowsiness and loss of feeling like classic sedatives such as phenothiazine or butyrophenone. High-dose sulpirides control the rampant positive symptoms of schizophrenia, but low doses have the effect of making people with schizophrenia apathetic, withdrawn and out of contact with society. Although there are some properties of classical neuroleptics, sulpirides differ from them in chemical structure and do not cause postural retention, do not affect the dopamine-sensitive adenylcyclase system, do not affect the circulation of noradrenaline and 5-HT, have almost no anticholinesterase effect, and do not affect muscarinic receptors or GABA.
Pharmacokinetics: Taken orally, sulpiride is absorbed in 4.5 hours; The peak plasma sulpiride concentration was 0.25 mg/L after taking 50 mg capsules. The bioavailability of the oral form is between 25 and 35%, there can be significant differences between one person and another; The concentration of sulpiride in plasma is linearly related to the dosage. Sulpiride is rapidly diffused to tissues, especially to the liver and kidneys; diffusion to the brain is poor, mainly to the pituitary gland.
The rate of adhesion to plasma protein is less than 40%; the distribution coefficient to red blood cells and plasma is 1. Excretion through breast milk is estimated to be 1/1000 of the daily dose. Figures made on animals with marked sulpiride (C14) demonstrate that excretion through the placental barrier is very poor. Contrary to animal records, sulpiride is very rarely metabolized in humans; 92% of intramuscular doses of sulpiride are found in the urine as unchanged.
The pharmacokinetics of sulpiride include the absorption phase, followed by the distribution phase, followed by the elimination phase. The half-life of elimination in plasma is 7 hours; the volume of distribution is 0.94 L/kg. Total purge is 126 mL/min.
Sulpiride is excreted mainly through the kidneys, thanks to filtration in the glomeruli. Clearance in the kidneys is usually close to total clearance.
