1. Name Of The Medicinal Product
Paracetamol 120mg/5ml Oral Suspension
2. Qualitative And Quantitative Composition
Paracetamol (micronised) 120mg/5ml
3. Pharmaceutical Form
Oral Suspension
4. Clinical Particulars
4.1 Therapeutic Indications
For the treatment of mild to moderate pain, including headache, migraine, neuralgia, toothache, sore throat, period pains, aches and pains.
For the reduction of fever and to be used as an adjunctive treatment to relieve symptoms of cold and flu.
4.2 Posology And Method Of Administration
For oral administration only
Recommended doses:
120 mg/5ml | ||
CHILDREN | 3 - 12 months | 2.5 - 5ml |
1 - 5 years | 5 - 10ml | |
6 - 12 years | 10 - 20ml |
These doses may be repeated every 4 - 6 hours when necessary with a maximum of 4 doses in 24 hours.
Adults and children over 12: 20 - 40ml every 4 - 6 hours to a maximum of 4g daily.
If pyrexia develops after immunisation, a child can be given a dose of Paracetamol followed, if necessary, by a second dose 4 - 6 hours later. The dose of Paracetamol for post immunisation pyrexia in an infant aged 2 - 3 months is 60mg (2.5ml of the 120mg/5ml presentation); an oral syringe can be obtained from any Pharmacy to give the small dose volume required. The parents should be warned that if the pyrexia persists after the second dose medical advice should be sought.
4.3 Contraindications
Hypersensitivity to paracetamol and/or other constituents.
Patients with severe hepatic dysfunction.
4.4 Special Warnings And Precautions For Use
Care is advised in the administration of paracetamol to patients with severe renal or severe hepatic impairment. The hazards of overdose are greater in those with non-cirrhotic alcoholic liver disease.
Do not give with any other paracetamol-containing products.
Immediate medical advice should be sought in the event of an overdose, even if you feel well, because of the risk of delayed serious liver damage.
Do not exceed the recommended dose.
If symptoms persist consult your doctor.
Keep out of the reach and sight of children.
Excipients in the formulation
This product contains hydroxybenzoates. These may cause allergic reactions (possibly delayed). The product also contains sucrose (3g per 5ml dose) and sorbitol. This should be taken into account in patients with diabetes mellitus. Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicine.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
The hepatotoxicity of Paracetamol, particularly after overdosage, may be increased by drugs which induce liver microsomal enzymes such as barbiturates, tricyclic antidepressants, and alcohol.
The speed of absorption of paracetamol may be increased by metoclopramide or domperidone and absorption reduced by colestyramine.
The anticoagulant effect of warfarin and other coumarins may be enhanced by prolonged regular use of paracetamol with increased risk of bleeding; occasional doses have no significant effect.
Antivirals: Regular use of Paracetamol possibly reduces metabolism of Zidovudine (increased risk of neutropenia).
4.6 Pregnancy And Lactation
Epidemiological studies in human pregnancy have shown no ill effects due to paracetamol used in the recommended dosage, but patients should follow the advice of their doctor regarding its use.
Paracetamol is excreted in breast milk but not in clinically significant quantities. Available published data do not contraindicate breast feeding.
4.7 Effects On Ability To Drive And Use Machines
None.
4.8 Undesirable Effects
Adverse effects of paracetamol are rare but hypersensitivity including skin rash may occur. There have been reports of blood dyscrasias including thrombocytopenia and agranulocytosis, but these were not necessarily causality related to paracetamol.
Cases of acute pancreatitis have been reported. Paracetamol has been widely used and reports of adverse reactions are rare, and are generally associated with overdosage.
Allergic reactions occur occasionally.
Nephrotoxic effects are uncommon and have not been reported in association with therapeutic doses, except after prolonged administration.
4.9 Overdose
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 below).
Risk factors
If the patient
a) Is on long term treatment wih carbamazepine, phenobarbital, phenytoin, primidone, rifampicin, St John's Wort or other drugs that induce liver enzymes.
Or
b) Regularly consumes ethanol in excess of recommended amounts
Or
c) Is likely to be glutathione depleted e.g. eating disorders, cystic fibrosis, HIV infection, starvation, cachexia.
Symptoms
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.
Management
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 overdose section.
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.
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
The mechanism of analgesic action has not been fully determined. Paracetamol may act predominantly by inhibiting prostaglandin synthesis in the central nervous system (CNS) 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 to inhibition of the synthesis or actions of other substances that sensitise pain receptors to mechanical or chemical stimulation.
Paracetamol probably produces antipyresis by acting centrally on the hypothalamic heat regulating centre to produce peripheral vaso-dilation resulting in increased blood flow through the skin, sweating and heat loss. The central action probably involves inhibition of prostaglandin synthesis in the hypothalamus.
5.2 Pharmacokinetic Properties
Oral absorption is rapid and almost complete, it may be decreased if Paracetamol is taken following a high carbohydrate meal.
There is no significant protein binding with doses producing plasma concentrations of below 60mcg (µg)/ml, but may reach moderate levels with high or toxic doses.
Approximately 90 - 95% of a dose is metabolised in the liver, primarily by conjugation with glucuronic acid, sulphuric acid and cysteine. An intermediate metabolite, which may accumulate in overdosage after primary metabolic pathways become saturated, is hepatotoxic and possibly nephrotoxic.
Half life is 1 to 4 hours; does not change with renal failure but may be prolonged in acute overdosage, in some forms of hepatic disease, in the elderly, and in the neonate; may be somewhat shortened in children.
Time to peak concentration, 0.5 - 2 hours; peak plasma concentrations, 5 - 20mcg (µg)/ml (with doses up to 650mg); time to peak effect, 1- 3 hours; duration of action, 3- 4 hours.
Elimination is by the renal route, as metabolites, primarily conjugates, 3% of a dose may be excreted unchanged.
Peak concentration of 10 - 15mcg(µg)/ml have been measured in breast milk, 1 - 2 hours following maternal ingestion of a single 650mg dose. Half life in breast milk is 1.35 - 3.5 hours.
5.3 Preclinical Safety Data
None stated
6. Pharmaceutical Particulars
6.1 List Of Excipients
Propylene glycol, methyl hydroxybenzoate, propyl hydroxybenzoate, xanthan gum, sorbitol solution 70%, sucrose, mango flavour 545329E and purified water.
6.2 Incompatibilities
None stated
6.3 Shelf Life
24 months
6.4 Special Precautions For Storage
Store below 25°C. Protect from light
6.5 Nature And Contents Of Container
Amber (Type III) glass bottle with capacity of 60ml, 100ml, 125ml, 500ml and 1000ml.
Closure: | 1. Aluminium, wadded, roll-on, pilfer proof closure.
|
6.6 Special Precautions For Disposal And Other Handling
None
Administrative Data
7. Marketing Authorisation Holder
Rosemont Pharmaceuticals Ltd
Rosemont House
Yorkdale Industrial Park
Braithwaite Street
Leeds
LS11 9XE
8. Marketing Authorisation Number(S)
PL 0427/0077
9. Date Of First Authorisation/Renewal Of The Authorisation
11 January 1995
10. Date Of Revision Of The Text
Oct 2009
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