Paracap Suspension Mechanism of Action

Pharmacology: Pharmacodynamics: 120 mg/5 mL: Although not fully elucidated, believed to inhibit the synthesis of prostaglandins in the central nervous system and work peripherally to block pain impulse generation; produces antipyresis from inhibition of hypothalamic heat-regulating center.
250 mg/5 mL: Paracetamol (Acetaminophen) is the active metabolite of phenacetin and has antipyretic and analgesic activities.
Pharmacokinetics: 120 mg/5 mL: Onset of action: Oral: <1 hour.
Duration: Oral: Analgesia: 4-6 hours.
Absorption: Primarily absorbed in small intestine (rate of absorption dependent upon gastric emptying); minimal absorption from stomach; varies by dosage form.
Distribution: ~1 L/kg at therapeutic doses.
Protein binding: 10% to 25% at therapeutic concentrations; 8% to 43% at toxic concentrations.
Metabolism: At normal therapeutic dosages, primarily hepatic metabolism to sulfate and glucuronide conjugates, while a small amount is metabolized by CYP2E1 to a highly reactive intermediate, N-acetyl-p-benzoquinone imine (NAPQI), which is conjugated rapidly with glutathione and inactivated to nontoxic cysteine and mercapturic acid conjugates. At toxic doses (as little as 4 g daily) glutathione conjugation becomes insufficient to meet the metabolic demand causing an increase in NAPQI concentrations, which may cause hepatic cell necrosis. Oral administration is subject to first pass metabolism.
Half-life elimination: Prolonged following toxic doses.
Neonate: 7 hours (range: 4-10 hours).
Infants: ~4 hours (range: 1-7 hours).
Children: 3 hours (range: 2-5 hours).
Adolescents: ~3 hours (range: 2-4 hours).
Adults: ~2 hours (range: 2-3 hours); may be slightly prolonged in severe renal insufficiency.
(Cl_cr < 30 mL/minute ): 2-5.3 hours.
Time to peak, serum: Oral: Immediate release: 10-60 minutes (may be delayed in acute overdoses).
Excretion: Urine (<5% unchanged; 60% to 80% as glucuronide metabolites; 20% to 30% as sulphate metabolites; ~8% cysteine and mercapturic acid metabolites).
250 mg/5 mL: Paracetamol is absorbed rapidly, and peak plasma levels are reached in 30 to 60 minutes. Approximately 90% of paracetamol usually undergoes hepatic conjugation with glucuronide (40% to 67%) and sulfate (20% to 46%) to form inactive metabolites that area excreted in the urine.
Toxicology: Preclinical safety data: 250 mg/5 mL: Not applicable.