Paracetamol (syrup) (Paracetamolum)

General characteristic:
international and chemical names: paracetamol; N-(4-hydroxyphenyl) acetamide;
main physical and chemical properties: transparent viscous liquid of pink color with sweet taste and a characteristic smell of raspberry;
structure: 5 ml of syrup contain 120 mg of paracetamol;
excipients: propylene glycol, glycerin, alcohol ethyl 96, sorbitol, methylparahydroxybenzoate, propilparagidroksibenzoat, fragrance food "Malines", ponso 4R, the water purified.
Release form. Syrup.
Farmakoterapevtichesky group. Analgetiki and antipiretik. Code of automatic telephone exchange N02B E01.
Pharmacological properties.
Farmakodinamika. Possesses analgetichesky, febrifugal and weak anti-inflammatory action. The mechanism of action is connected with inhibition of synthesis of prostaglandins and influence on the center of thermal control in a gipotalamus.
Pharmacokinetics. After intake paracetamol is quickly soaked up from a gastrointestinal tract, mainly in a small intestine, generally by passive transport. After single reception in a dose of 500 mg the maximum concentration in plasma of blood is reached in 10-60 min. and makes about 6 mkg/ml, then gradually decreases and in 6 h makes 11-12 mkg/ml. It is well distributed in fabrics and generally in liquid environments of an organism, except for fatty tissue and cerebrospinal fluid. Linkng with proteins makes less than 10% and slightly increases at increase in a dose. Sulphatic and glyukuronidny metabolites do not contact proteins of plasma even in rather high concentration. Paracetamol is metabolized mainly in a liver by conjugation from glyukuronida, conjugation with sulfate and oxidations with the participation of the mixed oxidases of a liver and P450 cytochrome. The Gidroksilirovanny metabolite with negative action - N-acetyl-r-benzokhinonimin which is formed in very small amounts in a liver and kidneys under the influence of the mixed oxidases and is usually detoxified by binding with glyutationy can collect at overdose of paracetamol and cause damages of fabrics. At adults the most part of paracetamol contacts glyukuronovy acid and in smaller quantity - sulfuric acid. These conjugated metabolites do not possess biological activity. At premature children, newborns and on the first year of life the sulphatic metabolite prevails. The period of semi-removal makes 1 - 3 h. At patients with cirrhosis the period of semi-removal is slightly more. The kidney clearance of paracetamol makes 5%. The preparation is removed with urine mainly in the form of glyukuronidny and sulphatic conjugates. Less than 5% are brought in the form of not changed paracetamol.
Indications to application. Pain syndrome of small and average intensity of various genesis (head and tooth pains, neuralgia, muscle pain; pain at a teething; at injuries; burns; pharyngitis, rheumatic pains). Fever at infectious and inflammatory diseases.