1. Name Of The Medicinal Product
Extra Power Pain Reliever Tablets
Extra Power Pain Reliever Caplets
Alka XS GO
Pain Relief Extra Caplets
Aspirin Extra Tablets
Paramed Extra Power Pain Reliever Tablets
Superdrug Extra Power Pain Reliever
Wilko Extra Power Pain Reliever Tablets
Teva Extra Power Pain Reliever Tablets
2. Qualitative And Quantitative Composition
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3. Pharmaceutical Form
Tablet
4. Clinical Particulars
4.1 Therapeutic Indications
For the treatment of mild to moderate pain including headache, migraine, neuralgia, toothache, sore throat, period pains, symptomatic relief of sprains, strains, rheumatic pain, sciatica, lumbago, fibrositis, muscular aches and pains, joint swelling and stiffness, influenza, feverishness and feverish colds.
4.2 Posology And Method Of Administration
For oral administration.
Adults and young persons over 16 years:-
1 or 2 tablets every 4 hours as required. Dose not to be taken more frequently than every 4 hours, with a maximum of 6 tablets in 24 hours.
Do not give to children under 16 years, unless specifically indicated (e.g. for Kawasaki's disease).
Adult dosage is suitable for the elderly.
4.3 Contraindications
Peptic ulceration and those with a history of peptic ulceration; haemophilia; concurrent anti-coagulant therapy; hypersensitivity to aspirin, paracetamol and/or other constituents; children under 16 years and when breast feeding because of possible risk of Reye's Syndrome.
4.4 Special Warnings And Precautions For Use
Hypersensitivity – asthma – aspirin may provoke or worsen asthma.
There is a possible association between aspirin and Reye's syndrome when given to children. Reye's syndrome is a very rare disease, which affects the brain and liver and can be fatal. For this reason aspirin should not be given to children under 16 years unless specifically indicated (e.g. for Kawasaki's disease).
The following warnings will appear on the pack:-
If symptoms persist consult your doctor.
Do not exceed 6 tablets in any 24 hours.
Do not give to children under 16 unless your doctor tells you to.
Keep all medicines out of reach and sight of children.
CONTAINS ASPIRIN AND PARACETAMOL.
Do not exceed the stated dose.
“Do not take any other paracetamol-containing products whilst taking this product” and “Immediate medical advice should be sought in the event of an overdose, even if you feel well.”
Care is advised in the administration of paracetamol to patients with severe renal or hepatic impairment. The hazards of overdose are greater in those with non-cirrhotic alcoholic liver disease.
The leaflet shall say “Immediate medical advice should be sought in the event of an overdose, even if you feel/the child seems well, because of the risk of delayed, serious liver damage”.
Patients with rare hereditary problems of fructose intolerance should not take this medicine.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
The following are noted, but are unlikely to apply when the product is used for a short-term symptomatic relief, as directed:-
ASPIRIN
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PARACETAMOL
The speed of absorption of paracetamol may be increased by metoclopramide or domperidone. Colestyramine may reduce the absorption of paracetamol.
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.
4.6 Pregnancy And Lactation
There is clinical and epidemiological evidence of safety of aspirin in pregnancy but it may prolong labour and contribute to maternal and neonatal bleeding, and so is best discontinued in late pregnancy.
Aspirin appears in breast milk, and regular high doses may affect neonatal clotting. Not recommended with breast feeding due to possible risk of Reye's Syndrome as well as neonatal bleeding due to hypoprothrombinaemia.
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 a clinically significant amount. Available published data do not contraindicate breast feeding.
Caffeine appears in breast milk. Irritability and poor sleeping pattern in the infant have been reported.
4.7 Effects On Ability To Drive And Use Machines
None Stated.
4.8 Undesirable Effects
Side effects are mild and infrequent, but there is a high incidence of gastro-intestinal irritation with slight asymptomatic blood loss. Increased bleeding time. Bronchospasm and skin reactions in hypersensitive patients. Aspirin may induce gastro-intestinal haemorrhage, occasionally major. It may precipitate gout in susceptible individuals. Possible risk of Reye's Syndrome in children.
Adverse effects of paracetamol are rare but hypersensitivity including skin rash may occur. There have been rare reports of blood dyscrasias including thrombocytopenia and agranulocytosis, but these were not necessarily causally related to paracetamol.
4.9 Overdose
PARACETAMOL
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 with carbamazepine, phenobarbitone, 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 deplete 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.
SALICYLATES/ASPIRIN
Salicylate poisoning is usually associated with plasma concentrations >350 mg/L (2.5 mmol/L). Most adult deaths occur in patients whose concentrations exceed 700 mg/L (5.1 mmol/L). Single doses less than 100 mg/kg are unlikely to cause serious poisoning.
Symptoms
Common features include vomiting, dehydration, tinnitus, vertigo, deafness, sweating, warm extremities with bounding pulses, increased respiratory rate and hyperventilation. Some degree of acid-base disturbance is present in most cases.
A mixed respiratory alkalosis and metabolic acidosis with normal or high arterial pH (normal or reduced hydrogen ion concentration) is usual in adults and children over the age of four years. In children aged four years or less, a dominant metabolic acidosis with low arterial pH (raised hydrogen ion concentration) is common. Acidosis may increase salicylate transfer across the blood brain barrier.
Uncommon features include haematemesis, hyperpyrexia, hypoglycaemia, hypokalaemia, thrombocytopaenia, increased INR/PTR, intravascular coagulation, renal failure and non-cardiac pulmonary oedema.
Central nervous system features including confusion, disorientation, coma and convulsions are less common in adults than in children.
Management
Give activated charcoal if an adult presents within one hour of ingestion of more than 250 mg/kg. The plasma salicylate concentration should be measured, although the severity of poisoning cannot be determined from this alone and the clinical and biochemical features must be taken into account. Elimination is increased by urinary alkalinisation, which is achieved by the administration of 1.26% sodium bicarbonate. The urine pH should be monitored. Correct metabolic acidosis with intravenous 8.4% sodium bicarbonate (first check serum potassium). Forced diuresis should not be used since it does not enhance salicylate excretion and may cause pulmonary oedema.
Haemodialysis is the treatment of choice for severe poisoning and should be considered in patients with plasma salicylate concentrations >700 mg/L (5.1 mmol/L), or lower concentrations associated with severe clinical or metabolic features. Patients under ten years or over 70 have increased risk of salicylate toxicity and may require dialysis at an earlier stage.
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
ASPIRIN
White powder or crystals soluble in alcohol and slightly soluble in water.
Mechanism of action/effect:
Salicylate inhibit the activity of the enzyme cyclo-oxygenase to decrease the formation of precursors of prostaglandin's and thromboxanes from arachidonic acid. Although many of the therapeutic effects may result from inhibition of prostaglandin synthesis (and consequent reduction of prostaglandin activity) in various tissues, other actions may also contribute significantly to the therapeutic effects.
Analgesic:
Produces analgesia through a peripheral action by blocking pain impulse generation and via a central action, possibly in the hypothalamus.
Anti-inflammatory (non-steroidal):
Exact mechanisms have not been determined. Salicylates may act peripherally in inflamed tissue probably by inhibiting the synthesis of prostaglandins and possibly by inhibiting the synthesis and/or actions of other mediators of the inflammatory response.
PARACETAMOL
Analgesic:
The mechanism of analgesic action has not been fully determined. Paracetamol may act predominantly by inhibiting a 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.
Antipyretic:
Paracetamol probably produces antipyresis by acting centrally on the hypothalamic heat-regulating centre to produce peripheral vasodilation resulting in increased blood flow through the skin, sweating and heat loss. The central action probably involves inhibition of prostaglandin synthesis in the hypothalamus.
CAFFEINE
Central nervous system stimulant – Caffeine stimulates all levels of the CNS, although its cortical effects are milder and of shorter duration than those of amfetamines.
Analgesia Adjunct:
Caffeine constricts cerebral vasculature with an accompanying decrease in cerebral blood flow and in the oxygen tension of the brain. It is believed that caffeine helps to relieve headache by providing a more rapid onset of action and/or enhanced pain relief with lower doses of analgesic. Recent studies with ergotamine indicate that the enhancement of effect by the addition of caffeine may also be due to improved gastrointestinal absorption of ergotamine when administered with caffeine.
ATC code: R05X
5.2 Pharmacokinetic Properties
ASPIRIN
Absorption and Fate
Absorption is generally rapid and complete following oral administration.
It is largely hydrolysed in the gastrointestinal tract, liver and blood to salicylate which is further metabolised primarily in the liver.
PARACETAMOL
Absorption and Fate
Paracetamol is readily absorbed from the gastro-intestinal tract with peak plasma concentrations occurring about 30 minutes to 2 hours after ingestion. It is metabolised in the liver and excreted in the urine mainly as the glucuronide and sulphate conjugates. Less than 5% is excreted as unchanged paracetamol. The elimination half-life varies from about 1 – 4 hours. Plasma-protein is negligible at usual therapeutic concentrations but increases with increasing concentrations.
A minor hydroxylated metabolite which is usually produced in very small amounts by mixed-function oxidases in the liver and which is usually detoxified by conjugation with liver glutathione may accumulate following paracetamol overdosage and cause liver damage.
5.3 Preclinical Safety Data
None stated.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Methyl cellulose
Maize Starch
Microcrystalline Cellulose
Sorbitol
Sodium Lauryl Sulphate
Hydrogenated Cotton Seed Oil
6.2 Incompatibilities
None other than those listed under 4.5 interactions.
6.3 Shelf Life
3 years.
6.4 Special Precautions For Storage
None.
6.5 Nature And Contents Of Container
1. Blister packs of the following construction –
(i) 250 micron UPVC./20 micron aluminium foil blister.
(ii) 30 micron pyramidally embossed hard temper aluminium (with 250 micron PVC blisters).
(iii) 35/9 Paper/Foil with PVC blister.
(iv) 250 micron PVC lid/Foil 1.0 g/m2 lacquer, 20 micron hardened aluminium, seal.
2. Polypropylene drums with HDPE Child Resistant Caps.
The blister packs are packed into boxboard cartons in blister counts of 8, 12, 16, 24, 32, 48 and 96 tablets.
Polypropylene drums of 25, 50 and 100 tablets.
6.6 Special Precautions For Disposal And Other Handling
None.
ADMINISTRATIVE DATA
7. Marketing Authorisation Holder
Wrafton Laboratories Limited
Wrafton
Braunton
North Devon
EX33 2DL
8. Marketing Authorisation Number(S)
PL 12063/0009.
9. Date Of First Authorisation/Renewal Of The Authorisation
11.January 1994.
10. Date Of Revision Of The Text
10 February 2011
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