500 mg: Each tablet contains Paracetamol 500 mg.
600 mg: Each tablet contains Paracetamol 650 mg.
Pharmacology: Pharmacodynamics: Paracetamol is a centrally acting analgesic and antipyretic with minimal anti-inflammatory properties.
Analgesic: The mechanism of analgesic action has not been fully determined. Paracetamol may act predominantly by inhibiting prostaglandin synthesis in the central nervous system (specifically cyclooxygenase (COX)-2) and, to a lesser extent, through a peripheral action by blocking pain-impulse generation.
The peripheral action may also be due to inhibition of prostaglandin synthesis or inhibition of the synthesis or actions of other substances that sensitize pain receptors to mechanical or chemical stimulation.
Antipyretic: Paracetamol act centrally on the hypothalamic heat-regulating center to produce peripheral vasodilation resulting in increase blood flow through the skin, sweating and heat loss.
Paracetamol reduces fever by inhibiting the formulation and release of prostaglandins in the CNS and by inhibiting endogenous pyrogens at the hypothalamic thermoregulator center.
Pharmacokinetics: Following oral administration paracetamol is rapidly absorbed.
Paracetamol absorption takes place mainly in the small intestine and therefore the rate of absorption is depending on the rate of gastric emptying. It has been shown that drugs which delay gastric emptying also delay the absorption of paracetamol whereas metoclopramide (a drug which increases the rate of gastric emptying) accelerates absorption of the analgesic through the total amount absorbed doses.
The presence of food in the stomach has also been reported to reduce the rate of absorption of paracetamol. Alterations in gastric pH have no significant effect on paracetamol absorption.
During absorption, the amount of paracetamol which is inactivated is negligible and it has been shown that paracetamol does not affect gastric mucosal permeability and does not produce mucosal bleeding.
Peak plasma concentrations reached 1 hour after absorption. The plasma half life is 1 to 3 hours.
Paracetamol penetrates the brain and is present in breast milk of human.
Paracetamol is metabolized by the microsomal enzyme system of the liver. This metabolism is mainly to the glucuronide and sulphate conjugates, accounting for approximately 49% and 26% of the ingested dose respectively. About 4% is excreted as free paracetamol. Other minor pathways include the production of catechol derivatives and cysteine conjugates (via glutathione). Paracetamol excretion is rapid and occurs via the urine.
500 mg: For the relief from fever.
For the relief from mild to moderate pain including: headache, migraine, backache, musculoskeletal pain, myalgia and neuralgia, dysmenorrhea, pain of osteoarthritis, toothache, pain after dental procedures/tooth extraction, pain after vaccination and the discomfort from colds, influenza and sore throats.
600 mg: Relief of headache, backache, period pain, and aches due to cold and flu, pain related to mild arthritis and fever.
500 mg: Adults and children aged 12 years and over: 500mg or 1 g paracetamol, taken every 4-6 hours as required up to a maximum of 4g daily.
Children 6 - 11 years: 250mg - 500mg every 4 to 6 hours as required. Maximum daily dose: 60mg/kg presented in divided doses of 10-15mg/kg throughout 24 hour period.
600 mg: Adults: 1 to 1½, tablets, three or four times a day. (Maximum: 6 tablets a day.)
Route of Administration: Oral.
650 mg: Liver damage is possible in adults who have taken 10g or more of paracetamol. Ingestion of 5g or more of paracetamol may lead to liver damage if the patient has risk factors (see as follows).
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: 500 mg: Toxic symptoms include vomiting, abdominal pain, hypotension and sweating. The most serious adverse effect of acute overdose of paracetamol is a dose-dependent, potentially fatal hepatic necrosis. Clinical and laboratory evidence of hepatoxicity may be delayed for up to one week. Major manifestations of liver failure such as jaundice, hypoglycemia and metabolic acidosis may take at least 3 days to develop.
650 mg: Symptoms of paracetamol overdosage 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.
Treatment: 500 mg: In cases of overdose, methods of reducing the absorption of ingested drug are important. Gastric lavage is essential even if several hours have elapsed. Prompt administration of 50 g activated charcoal and 500ml iced mannitol 20% by mouth, may reduce absorption. If the history suggests that 15g Paracetamol or more has been ingested, administer one of the following antidotes: Acetylcysteine 20% i.v.: Administer intravenously, 20% acetylcysteine immediately without waiting for positive urine test or plasma level results: initial dose of 150mg/kg over 15 minutes, followed by continuous infusion of 50mg/kg in 500ml 5% glucose/dextrose over 4 hours and 100mg/kg in 1 L 5% glucose/dextrose over 16 hours; or
Oral Methionine: 2.5 g immediately followed by three further doses of 2.5g at four hourly intervals. For a 3 year old child, 1 g methionine every four hours for four doses has been used; or
Oral Acetylcysteine 5%: 140mg/kg as a loading dose, then 70mg/kg every 4 hours for a total of 17 maintenance doses. If more than ten hours have elapsed since the overdosage was taken, the antidote may be ineffective.
650 mg: Immediate treatment is essential in the management of paracetamol overdose. Despite a lack of significant early symptoms, patients should be referred to hospital urgently for immediate medical attention. Symptoms may be limited to nausea or vomiting and may not reflect the severity of overdose or the risk of organ damage. Management should be in accordance with established treatment guidelines, see BNF.
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 24h from ingestion should be discussed with the NPIS or a liver unit.
Hypersensitivity to paracetamol or any of the other ingredients/components of the product.
Severe and active hepatic impairment.
This preparation contains PARACETAMOL. Do not take any other PARACETAMOL containing medicines at the same time.
Allergy alert: Paracetamol may cause severe skin reactions. Symptoms may include skin reddening, blisters or rash. These could be signs of serious conditions. If these reactions occur, stop use and seek medical assistance right away.
Do not take if allergic to paracetamol.
Patients should contact their health care provider if symptoms persist (if the pain lasts for more than 10 days, if there is redness or fever lasts more than 3 days).
Paracetamol should be given with care to patients with impaired kidney or liver function.
Large doses should be avoided in patients with hepatic impairment. Paracetamol overdose may harm the liver.
Do not exceed recommended dose.
It should be given with care to patients with alcohol dependence.
Paracetamol provides symptomatic relief only, additional therapy to treat the cause of the pain or fever should be initiated when necessary.
Effects on Ability to Drive and Use of Machines: It is unlikely to impair a patient's ability to drive or use machinery.
Use in pregnancy: Considered to be the analgesic of choice in pregnant patients.
Although it crosses placenta, paracetamol is considered to be safe in normal therapeutic doses for short-term use as a minor analgesic/antipyretic in pregnancy.
Use in lactation: Excreted in breast milk.
Maternal ingestion of paracetamol in normal therapeutic doses does not appear to present a risk to the nursing infant.
Side effects of paracetamol are rare and usually mild, though hematological reactions have been reported. Cutaneous hypersensitivity reactions including skin rashes, angioedema, Stevens Johnson syndrome/Toxic Epidermal Necrolysis had been reported.
The anticoagulant effect of warfarin and other coumarins may be enhanced by prolonged regular daily use of paracetamol with increased risk of bleeding; occasional doses have no significant effect.
Store below 30°C. Protect from light and moisture.
N02BE01 - paracetamol ; Belongs to the class of anilide preparations. Used to relieve pain and fever.
Actimol tab 500 mg
10 × 10's;100 × 10's;3 × 10's
Actimol tab 650 mg
10 × 10's;100 × 10's;3 × 10's
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