Fever, headache, toothache, earache, bodyache, myalgia, dysmenorrhoea, neuralgia & sprains. colic pain, back pain, chronic pain of cancer, inflammatory pain, post-vaccination pain & fever of children. Rheumatism & osteoarthritic pain & stiffness of joints in fingers, hips, knees, wrists, elbows, feet, ankles & top & bottom of the spine.
Para-aminophenol Derivative; Analgesic
Paracetamol exhibits analgesic action by peripheral blockage of pain impulse generation. It produces antipyresis by inhibiting the hypothalamic heat-regulating centre. Its weak anti-inflammatory activity is related to inhibition of prostaglandin synthesis in the CNS.
Paracetamol (Acetaminophen) is thought to act primarily in the CNS, increasing the pain threshold by inhibiting both isoforms of cyclooxygenase, COX-1, COX-2, and COX-3 enzymes involved in prostaglandin (PG) synthesis. Unlike NSAIDs, acetaminophen does not inhibit cyclooxygenase in peripheral tissues and, thus, has no peripheral anti-inflammatory affects. While aspirin acts as an irreversible inhibitor of COX and directly blocks the enzyme's active site, studies have found that acetaminophen indirectly blocks COX, and that this blockade is ineffective in the presence of peroxides. This might explain why acetaminophen is effective in the central nervous system and in endothelial cells but not in platelets and immune cells which have high levels of peroxides. Studies also report data suggesting that acetaminophen selectively blocks a variant of the COX enzyme that is different from the known variants COX-1 and COX-2. This enzyme is now referred to as COX-3. Its exact mechanism of action is still poorly understood, but future research may provide further insight into how it works. The antipyretic properties of acetaminophen are likely due to direct effects on the heat-regulating centres of the hypothalamus resulting in peripheral vasodilation, sweating and hence heat
Tablet: Adult 1-2 tablets every 4 to 6 hours up to a maximum of 4 g (8 tablets) daily. Children (6-12 years) 1/2 to 1 tablet 3 to 4 times daily. XR Tablet: 2 tablet every 6 to 8 hourly upto a maximum of 6 tablets daily. Syrup & Suspension: Children from 3 months to 1 year : 1/2 to 1 teaspoonful 3 to 4 times daily. 1-5 years: 1-2 teaspoonful 3 to 4 times daily. 6-12 years : 2-4 teaspoonful 3 to 4 times daily. Adults 4-8 teaspoonful 3 to 4 times daily. Paediatric Drop: Children Upto 3 months: 0.5 ml (40 mg) 4 to 11 months: 1.0 ml (80 mg). 1 to 2 years: 1.5 ml (120 mg) Dose can be repeated, every 4 hours. Suppository: Suppository should be administered rectaly. Children 3 months – 1 year : 60-120 mg 4 times daily. Children below 5 years : 125-250 mg, 4 times daily. Children 6-12 years : 250-500 mg, 4 times daily. Adults & children over 12 years : 0.5 - 1 mg, 4 times daily.
Patients who have taken barbiturates, tricyclic antidepressants and alcohol may show diminished ability to metabolise large doses of Paracetamol. Alcohol can increase the hepatotoxicity of Paracetamol overdosage. Chronic ingestion of anticonvulsants or oral steroid contraceptives induce liver enzymes and may prevent attainment of therapeutic Paracetamol levels by increasing first-pass metabolism or clearance.
Known sensitivity to Paracetamol.
Side Effects are significantly mild, though haematological reactions have been reported. Pancreatitis, skin rashes, & other allergic reactions occur occasionally.
Paracetamol is safe in all stages of pregnancy & lactation.
Liver damage is possible in adults who have taken 10 g or more of Paracetamol. Ingestion of 5 g or more of Paracetamol may lead to liver damage if the patient has following risk factors: If the patient is on long term treatment with Carbamazepine, Phenobarbitone, Phenytoin, Primidone, Rifampicin, St John’s Wort or other drugs that induce liver enzymes, or regularly consumes Ethanol in excess of recommended amounts, or is likely to be Glutathione deplete e.g. eating disorders, cystic fibrosis, HIV infection, starvation, cachexia.
Symptoms: Symptoms of Paracetamol overdose in the first 24 hours are pallor, nausea, vomiting, anorexia and abdominal pain. Liver damage may become apparent 12 to 48 hours after ingestion. Abnormalities of glucose metabolism and metabolic acidosis may occur. In severe poisoning, hepatic failure may progress to encephalopathy, haemorrhage, hypoglycaemia, cerebral oedema and death. Acute renal failure with acute tubular necrosis, strongly suggested by loin pain, haematuria and proteinuria, may develop even in the absence of severe liver damage. Cardiac arrhythmias and pancreatitis have been reported. Immediate treatment is essential in the management of Paracetamol overdose. Treatment with activated charcoal should be considered if the overdose has been taken within 1 hour. Plasma Paracetamol concentration should be measured at 4 hours or later after ingestion (earlier concentrations are unreliable). Treatment with N-acetylcysteine may be used up to 24 hours after ingestion of Paracetamol. However, the maximum protective effect is obtained up to 8 hours post-ingestion. The effectiveness of the antidote declines sharply after this time. If required the patient should be given intravenous N-acetylcysteine, in line with the established dosage schedule. If vomiting is not a problem, oral Methionine may be a suitable alternative for remote areas, outside hospital. Management of patients who present with serious hepatic dysfunction beyond 24 hours from ingestion should be discussed with the NPIS or a liver unit.
Keep in a dry place away from light and heat. Keep out of the reach of children.
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