Aspirin 300mg Tablets
Out of date information, search anotherSUMMARY OF PRODUCT CHARACTERISTICS
1 NAME OF THE MEDICINAL PRODUCT
Aspirin 300mg Tablets BP
2 QUALITATIVE AND QUANTITATIVE COMPOSITION
Each tablet contains aspirin 300mg For excipients, see section 6.1.
3 PHARMACEUTICAL FORM
Tablets
White biconvex tablets; breakline on one side and debossed <A> on other side
4 CLINICAL PARTICULARS
4.1 Therapeutic indications
For the relief of mild to moderate pain, including headaches, migraine, neuralgia, toothache, sore throat, period pains, aches and pains.
Also used for the secondary prevention of thrombotic cerebrovascular or cardiovascular disease and following by-pass surgery.
Aspirin has an anti-thrombotic action, mediated through inhibition of platelet activation, which has been shown to be useful in secondary prophylaxis following myocardial infarction, and in patients with unstable angina or ischaemic stroke including cerebral transient attacks.
For the symptomatic relief of influenza, feverishness, feverish colds
For the symptomatic relief of sprains, strains, rheumatic pain, sciatica, lumbago, fibrositis, muscular aches and pains, joint swelling & stiffiness.
4.2 Posology and method of administration
For Oral use
Adults & children over 16 years of age:
Analgesic, antipyretic and anti-inflammatory actions: One to three tablets.
Dose should not be repeated more frequently than 4 hour intervals and not more than 4 times in any 24 hour period.
In acute rheumatic disorders the dose is in the range of 4-8g, taken in divided doses.
Antithrombotic action: Patients should seek the advice of a doctor before commencing therapy for the first time. The usual dosage for long term use following myocardial infarction, transient ischaemic attack, or in patients with unstable angina,
is 75- 150mg once daily. In some circumstances a higher dose may be appropriate, especially in the short term, and up to 300mg a day may be used on the advice of a doctor.
Elderly:
Analgesic, antipyretic and anti-inflammatory actions: As for adults. The elderly are more likely to experience gastric side-effects and tinnitus.
Antithrombotic action: The risk-benefit ratio has not been fully established
If symptoms persist for more than 3 days, consult your doctor.
Children: Do not give to children under 16 years, unless specifically indicated (e.g. for Kawasaki’s Disease). See ‘Special warnings and Special Precautions for Use’.
4.3 Contraindications
i) Children under 16 years unless specifically indicated (e.g. for Kawasaki’s disease).
ii) Active peptic ulceration or a history of peptic ulceration
iii) Haemophilia, other coagulopathies or concurrent anticoagulant therapy.
iv) Hypersensitivity to aspirin, any other NSAIDs, or any of the excipients (See section 6.1)
v) Gout
4.4 Special warnings and precautions for use
Caution should be exercised in patients-with asthma, allergic disease, impairment of hepatic or renal function (avoid if severe) and-dehydration.
Patients with hypertension should be should be carefully monitored.
The elderly may be more susceptible to the toxic effects of salicylates. Continuous, prolonged use of aspirin should be avoided in the elderly because of the risk of gastrointestinal bleeding. Salicylates should be used with caution in patients with a history of peptic ulceration or coagulation abnormalities. They may also induce gastrointestinal haemorrhage, occasionally major.
Caution should be used in patients with glucose 6-phosphate dehydrogenase (G6PD) deficiency as haemolytic anaemia may occur.
Aspirin may interfere with insulin and glucagon in diabetes.
Aspirin prolongs bleeding time, mainly by inhibiting platelet aggregation and therefore it should be discontinued several days before scheduled surgical procedures. Haematological and haemorrhagic effects can occur, and may be severe. Patients should report any unusual bleeding symptoms to their physician.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucosegalactose malabsorption should not take this medicine.
Do not take if you have a stomach ulcer.
If symptoms persists for more than 3 days consult your doctor.
They may also precipitate bronchospasm or induce attacks of asthma in susceptible subjects.
Aspirin should be used with caution in patients with impaired renal function (avoid if severe), or in patients who are dehydrated.
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 aged under 16 years unless specifically indicated (e.g. for Kawasaki’s disease).
Before commencing long term aspirin therapy for the management of cerebrovascular or cardiovascular disease patients should consult their doctor who can advise on the relative benefits versus the risks for the individual patient.
4.5 Interaction with other medicinal products and other forms of interaction
Alcohol: Some of the effects of aspirin on the gastrointestinal tract are enhanced by alcohol.
Antacids and adsorbents: The excretion of aspirin is increased in alkaline urine; kaolin possibly reduces absorption.
Anticoagulants: Aspirin may enhance the effects of anticoagulants: concurrent use is contraindicated (see section 4.3)
Antiepileptics: May enhance the effects of phenytoin and sodium valproate.
Antimetabolites: The activity of methotrexate may be markedly enhanced and its toxicity increased.
ACE inhibitors: Aspirin may reduce the antihypertensive effect of ACE inhibitors.
Antibacterials: Inhibits the uricosuric effect of probenecid and may increase the toxicity of sulfonamides.
Antiemetics: Metoclopramide enhances the effects of aspirin by increasing the rate of absorption.
Aspirin may potentiate the effect of heparin and increases the risk of bleeding with oral anticoagulants, antiplatelet agents and fibrinolytics.
Corticosteroids: The risk of gastrointestinal bleeding and ulceration is increased. Corticosteroids reduce the plasma salicylate concentration.
Diuretics: Antagonism of the diuretic effect of spironolactone. Reduced excretion of acetazolamide with an increased risk of toxicity. Salicytate intoxication has occurred in patients on high dose salicylate regimens and carbonic anhydrase inhibitors.
Hypoglycaemic agents: Aspirin may enhance the effects of insulin and oral hypoglycaemic agents.
Leukotriene antagonists: The plasma concentration of zafirlukast is increased.
Mifepristone: The manufacturer of Mifepristone recommends that aspirin should be avoided until eight to twelve days after Mifepristone has been discontinued.
Other non-steroidal anti-inflammatory drugs
(NSAIDS): Concurrent administration can increase side effects. Increased risk of serious gastrointestinal haemorrhage
Thyroid function tests: Aspirin may interfere with thyroid function tests.
Uricosurics: Effect of probenecid and sulfinyrazone reduced.
4.6 Pregnancy and lactation
Pregnancy: Although clinical and epidemiological evidence suggests the safety of aspirin in pregnancy, caution should be exercised when considering use in pregnant patients.
Aspirin has the ability to alter platelet function and there may be a risk of haemorrhage in infants whose mothers have consumed aspirin during pregnancy.
Prolonged pregnancy and labour, with increased bleeding before and after delivery, decreased birth weight and increased rate of stillbirth have been reported with high blood salicylates levels. With high doses there may be premature closure of the ductus arteriosus and possible persistent pulmonary hypertension in the newborn. Analgesis doses of aspirin should be avoided during the last trimester of pregnancy.Maternal use of aspirin prior to birth may increase the risk of intracranial haemorrhage in premature or low birth weight infants. Regular use of high doses could impair platelet function and produce hypoprothrombinaemia in the infant if neonatal Vitamin K stores are low. The use of aspirin during pregnancy may cause premature closure of the foetal ductus arteriosus and pulmonary hypertension.
Lactation: As aspirin is excreted in human milk,
Aspirin should not be taken by patients who are breast-feeding, as there is a risk of Reye’s syndrome in the infant. High maternal doses may impair platelet function in the infant.
4.7 Effects on ability to drive and use machines
Aspirin does not usually affect the ability to drive or operate machinery.
4.8 Undesirable effects
Side effects are generally mild and infrequent.
Blood disorders: Aspirin increases bleeding time, decreases platelet adhesiveness and, in large doses, may cause hypoprothrombinaemia. It may also cause other blood disorders including thrombocytopenia. Haemolytic anaemia can occur in patients with glucose 6-phosphate dehydrogenase deficiency (G6PD). Fatalities have occurred.
Immune System: Aspirin may precipitate bronchospasm, and induce asthma attacks, rhinitis, angioedema, or other hypersensitivity reaction in susceptible individuals includes skin rashes, urticaria, and rarely anaphylaxis.
Gastro-intestinal: There is a relatively high incidence of gastro-intestinal irritation with a slight asymptomatic blood loss. Nausea, vomiting, dyspepsia, gastritis, gastrointestinal erosions and ulceration have been reported. Anaemia may occur following chronic gastrointestinal blood loss or acute haemorrhage.
Skin: Skin reactions may occur in susceptible patients.
Others: urate kidney stones and tinnitus.
4.9 Overdose
Salicylate poisoning is usually associated with plasma concentrations > 350mg/L (2.5mmol/L) Most adult deaths occur in patients whose concentrations exceed 700mg/L (5.1mmol/L). Single doses less than 100mg/kg are unlikely to cause serious poisoning.
a) 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, thrombocytopenia, 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.
b) Treatment
Give activated charcoal if an adult presents within one hour of ingestion of more than 250mg/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 >700mg/L (5.1mmol/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
N02B A01- (Nervous system- analgesics/antipyretics)
Aspirin is an analgesic and antipyretic with anti-inflammatory properties. Aspirin inhibits prostaglandin synthetase.
It also has antithrombotic action, which is mediated through inhibition of platelet activation.
5.2 Pharmacokinetic properties
Absorption
Aspirin is rapidly absorbed after oral administration, with some hydrolysis to salicylate before absorption. Absorption is delayed by the presence of food and is impaired in patients suffering migraine attacks. Absorption is more rapid in patients with achlorhydria and also following administration of polysorbates and antacids.
Blood concentration
Peak plasma concentrations of approximately 45mcg/ml are attained 1 to 2 hours after an oral dose of 640mg, but stabilise at approximately 270mcg/ml after oral doses of 3g daily. After an oral dose of about 2g, peak plasma concentrations of approximately 15mcg/ml of aspirin are attained in about one hour and peak plasma concentrations of approximately 130mcg/ml of salicylate are attained in 2 to 4 hours.
Half-life
Plasma / Aspirin Approximately 17 minutes
Plasma / Salicylate Low doses 2-4 hours
High doses up to 19 hours
Distribution
Aspirin is found in the saliva, milk, plasma and synovial fluid at concentrations less than blood and crosses the placenta.
Salicylate - extensive protein binding.
Aspirin - protein binding to a small extent.
Metabolism
In the blood, rapid hydrolysis to salicylic acid; glucuronic acid/glycine conjugation to form glucuronides and salicyluronic acid; oxidation of a small proportion.
Excretion
Excreted in the urine mainly as salicyluronic acid. Salicylate reabsorbed by renal tubules in acid urine, and alkaline diuresis will increase the rate of excretion; 85% of dose excreted as free salicylate.
5.3 Preclinical safety data
There are no pre-clinical data of relevance to the prescriber which are additional to that already included in other sections of the SmPC.
6 PHARMACEUTICAL PARTICULARS
6.1 List of excipients
Starch
Lactose monohydrate Purified talc (E553b)
6.2 Incompatibilities
Not applicable.
6.3 Shelf life
3 years.
6.4 Special precautions for storage
Do not store above 25°C.
Blister packs: store in the original package.
6.5 Nature and contents of container
Blister packs: 8, 10, 12 or 16 as GSL.
Blister strips consist of a 35gsm paper/9p soft tempered aluminium foil lid and 250p PVC film base in cartons.
6.6 Special precautions for disposal
None
7 MARKETING AUTHORISATION HOLDER
Bristol Laboratories Ltd,
Unit 3, Canalside,
Northbridge Road,
Berkhamsted,
HP4 1EG UK
8 MARKETING AUTHORISATION NUMBER(S)
PL 17907/0152
9 DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION
07/03/2011
10 DATE OF REVISION OF THE TEXT
07/03/2011