Paratsel - Acetaminophen (Paracetamol)

TRADE NAME OF DRUG: Paratsel

International Nonproprietary Name: Paracetamol

PHARMACEUTICAL FORM
Solution for intramuscular injection.

INGREDIENTS:
The active ingredient - acetaminophen 150mg/ml.
Excipients: 1% benzyl alcohol, water for injection.

Pharmacological groups:
Analgesic-antipyretic
ATC code: N02BE01

Mode of action:
Mode of action - an analgesic, antipyretic.
Pharmacokinetics:
Cmax plasma levels achieved after 15 min, and 15-30 ug / ml. The volume of distribution - 1 liter / kg. Weakly bound to plasma proteins. Passes through the BBB. Metabolized in the liver to form glucuronide and sulfate.
A small portion (4%) метаболизируетсяцитохромом P450 to form an intermediate metabolite (N-atsetilbenzohinonimina). Under normal circumstances, it is quickly neutralized reduced glutathione and excreted in the urine after binding to the cysteine and merkaptopurinovoy acid. With a massive intoxication concentration of this toxic metabolite increases. T1 / 2 in adults is 2.7 hours in children - 1.5-2 hours, the newborn - 3.5 hours total clearance - 18 l / h Displayed mainly in the urine and 90% of the dose - for 24 hours as the glucuronide (60-80%) and sulfate (20-30%). Less than 5% is excreted unchanged. In severe renal insufficiency (Clkreatinina below 10-30 ml / min) the excretion of paracetamol slows down somewhat, T1 / 2 is 2-5,3 hours elimination rate glucuronide and sulfate in patients with severe renal insufficiency is 3 times less than that of healthy people.
Pharmacodynamics:
It has a predominantly analgesic and antipyretic activity. Blocks cyclooxygenase I and II in the central nervous system, affects centers of pain and thermoregulation. In inflamed tissues kletochnyeperoksidazy neutralize the effect of paracetamol on the cyclo-oxygenase, which explains the absence of an anti-inflammatory effect. No effect on PG synthesis in peripheral tissues, so do not adversely affect the water-salt metabolism (sodium and water retention), and gastrointestinal mucosa.