Paracetamol solution for infusion 1gm/100ml
For the use only of a Registered Medical Practitioner or a Hospital or a Laboratory
Paracetamol solution for infusion is a clear and slightly yellowish solution. It contains 10mg/mL of paracetamol. Paracetamol is a white crystalline solid or powder chemically described as 4 - acetamidophenol.
The precise mechanism of the analgesic and antipyretic properties of paracetamol has yet to be established; it may involve central and peripheral actions.
Paracetamol 10 mg/mL, solution for infusion provides onset of pain relief within 5 to 10 minutes after the start of administration. The peak analgesic effect is obtained in 1 hour and the duration of this effect is usually 4 to 6 hours.
Paracetamol 10 mg/mL, solution for infusion reduces fever within 30 minutes after the start of administration with a duration of the antipyretic effect of at least 6 hours.
Paracetamol pharmacokinetics are linear after a single administration of up to 2 g and after repeated administration during 24 hours.
The volume of distribution of paracetamol is approximately 1 L/kg.
Paracetamol is not extensively bound to plasma proteins.
Following infusion of 2g proparacetamol, (equivalent to 1g of paracetamol) significant concentrations of paracetamol (about 1.5 µg/mL) were observed in the cerebrospinal fluid 20 minutes after infusion.
Paracetamol is metabolised mainly in the liver following two major hepatic pathways: glucuronic acid conjugation and sulphuric acid conjugation. The latter route is rapidly saturable at doses that exceed the therapeutic doses. A small fraction (less than 4%) is metabolised by cytochrome P450 to a reactive intermediate (N-acetyl benzoquinone imine) which, under normal conditions of use, is rapidly detoxified by reduced glutathione and eliminated in the urine after conjugation with cysteine and mercapturic acid. However, during massive poisoning, the quantity of this toxic metabolite is increased.
The metabolites of paracetamol are mainly excreted in the urine. 90% of the dose administered is excreted in 24 hours, mainly as glucuronide (60-80%) and sulphate (20-30%) conjugates. Less than 5% is eliminated unchanged. Plasma half-life is 2.7 hours and total body clearance is 18 L/h.
Paracetamol should be administered with caution to patients with renal impairment. In cases of severe renal impairment (creatinine clearance ≤30 mL/min), the elimination of paracetamol is slightly delayed, the elimination half-life ranging from 2 to 5.3 hours. For the glucuronide and sulphate conjugates, the elimination rate is 3 times slower in subjects with severe renal impairment than in healthy subjects Therefore, when giving Paracetamol to patients with severe Renal impairement (Creatinine Clearance 30mL/min),the minimum interval between each administration should be increased to 6 hours.
The pharmacokinetics and the metabolism of paracetamol are not modified in elderly subjects. No dose adjustment is required in this
Paracetamol is indicated for the short-term treatment of moderate pain, especially following surgery and for the short-term treatment of fever, when administration by intravenous route is clinically justified by an urgent need to treat pain or hyperthermia and/or when other routes of administration are not possible.
Dosage And Administration:
Paracetamol 10 mg/mL, solution for infusion should not be mixed with other medicinal products.
Paracetamol 1g per administration, i.e. one 100 mL vial, up to four times a day. The minimum interval between each administration must be 4 hours in patients without hepatic or renal impairment. In patients with renal and/or hepatic impairment the minimum interval between doses must not be less than 6 hours.
The maximum daily dose from all sources of paracetamol must not exceed 4 g.
No dosage adjustment is required in elderly subjects.
Method of administration
In cases of severe hepatocellular insufficiency.
In patients with hepatic failure It is recommended to use a suitable analgesic oral treatment as soon as this administration route is possible.
In order to avoid the risk of overdose; check that other medicines administered do not contain paracetamol.
It is recommended to use a suitable analgesic oral treatment as soon as this administration route is possible.
In order to avoid the risk of overdose, check that other medicines administered do not contain paracetamol. Administration of paracetamol doses higher than recommended entails the risk for very serious liver damage. Clinical symptoms and signs of liver damage are usually first seen after two days of paracetamol overdose. Maximum liver damage symptoms are usually observed after 4-6 days. Treatment with antidote should be given as soon as possible.
This medicinal product contains less than 1 mmol sodium (23mg) per 100ml of Paracetamol, i.e. essentially "sodium free".
Paracetamol should be used with caution in cases of:
Severe renal insufficiency (creatinine clearance ≤ 30 mL/min) (see DOSAGE AND ADMINISTRATION AND Pharmacokinetics)
Chronic malnutrition (low reserves of hepatic glutathione)
Use In Special Population :
Pregnancy Category (Category A)
Paracetamol has been taken by a large number of pregnant women and women of childbearing age without any proven increase in the frequency of malformations or other direct or indirect harmful effects on the fetus having been observed.
Lactation After oral administration, paracetamol is excreted into breast milk in small quantities. No undesirable effects on nursing infants have been reported. Consequently, Paracetamol solution for infusion may be used in breast-feeding women.
There is a risk of poisoning, particularly in elderly subjects, in young children, in patients with liver , in cases of chronic alcoholism, in patients with chronic malnutrition and in patients receiving enzyme inducers. Poisoning may be fatal in these cases. Acute overdose with paracetamol may also lead to acute renal tubular necrosis.
Symptoms generally appear within the first 24 hours and comprise of nausea, vomiting, anorexia, pallor and abdominal pain. Overdose, 7.5 g or more of paracetamol in a single administration in adults or 140 mg/kg of body weight in a single administration in children, causes hepatic cytolysis likely to induce complete and irreversible necrosis, resulting in hepatocellular insufficiency, metabolic acidosis and encephalopathy which may lead to coma and death. Simultaneously, increased levels of hepatic transaminases (AST, ALT), lactate dehydrogenase and bilirubin are observed together with decreased prothrombin levels that may appear 12 to 48 hours after administration. Clinical symptoms of liver damage are usually evident initially after two days, and reach a maximum after 4 to 6 days.
- Immediate hospitalisation.
- Before beginning treatment, take blood for plasma paracetamol assay, as soon as possible after the overdose.
- Treatment of paracetamol overdose may include the antidote N-acetyl cysteine (NAC) by the IV or oral route. In overdoses of oral paracetamol.
NAC is administered, if possible, before 10 hours but may give some degree of protection form liver toxicity even after this time. The optimal time for administration of NAC and necessary duration of therapy have not been established for overdoses of paracetamol.
Manufacture in India for:
|Store protected from light, temperature not exceeding 30°C.
|Do not refrigerate or freeze.
||Paracetamol solution single infusion bottle (100 ml)
|Keep the container in the outer packaging
||Packed in a carton
|For single use only
||SHELF LIFE : 24 Months
Cygnus Healthcare Specialities Pvt Ltd.
Thane - 400607 India