Aspirin 75mg Gastro-Resistant Tablets
SUMMARY OF PRODUCT CHARACTERISTICS
1 NAME OF THE MEDICINAL PRODUCT
Aspirin 75mg Gastro-resistant Tablets Boots Aspirin 75mg Gastro-resistant Tablets
2 QUALITATIVE AND QUANTITATIVE COMPOSITION
Each tablet contains aspirin 75mg For excipients see section 6.1
3 PHARMACEUTICAL FORM
Gastro-resistant tablet
White circular tablet, plain on both sides.
4 CLINICAL PARTICULARS
4.1 Therapeutic indications
For the secondary prevention of thrombotic cerebrovascular or cardiovascular disease and following by-pass surgery.
4.2 Posology and method of administration
For oral use.
The advice of a doctor should be sought before commencing therapy for the first time. The usual dosage, for long term use, is 75mg-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. Take the tablet with water, do not cut, chew or crush the tablet. Swallow whole.
Children:
Do not give to children aged under 16 years, unless specifically indicated (e.g. for Kawasaki’s disease).
4.3 Contraindications
• Hypersensitivity to aspirin or any other NSAIDs, or any of the excipients (see section 6.1)
• Active peptic ulceration or history of peptic ulceration
• Haemophilia, other coagulopathies or concurrent anticoagulant therapy
• Gout
• Do not give to children aged under 16 years, unless specifically indicated (e.g. for Kawasaki’s disease).
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.
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.
Caution should be taken in patients with glucose-6-phosphate dehydrogenase 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.
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).
Patients with a history of peptic ulceration or coagulation abnormalities should use this product with care.
Before commencing long term aspirin therapy for the management of cardiovascular or cerebrovascular 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)
Anti-epileptics; 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: The toxicity of sulfonamides may be increased.
Antiemetics: Metoclopramide enhances the effects of aspirin by increasing the rate of absorption.
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. Salicylate 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 zafirlukst 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.
Thyroid function tests: Aspirin may interfere with thyroid function tests.
Uricosurics: Effect of probenecid and sulfinpyrazone may be reduced.
4.6 Pregnancy and lactation
There is clinical and epidemiological evidence of the safety of aspirin in human pregnancy. Aspirin may prolong gestation, delay the onset of or prolong labour and contribute to maternal and neonatal bleeding and is best avoided at term and during breast feeding - possible risk of Reye's Syndrome.
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 the premature closure of the foetal ductus arteriosus, possibly leading to persistent pulmonary hypertension.
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 and the lymphatic system disorders: Aspirin prolongs bleeding time, decreases platelet adhesiveness and, in large doses, may cause hypoprothrombinaemia. Thrombocytopenia may also occur. Bleeding disorders such as epistaxis, haematuria, purpura, ecchymoses, haemoptysis, gastrointestinal bleeding, haematoma and cerebral haemorrhage have occasionally been reported. Fatalities have occurred. Haemolytic anaemia can occur in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency.
Immune system disorder: Hypersensitivity reactions include skin rashes, urticaria, angioedema, asthma, bronchospasm, rhinitis and rarely, anaphylaxis.
Ear & Labyrinth disorder: Tinnitus.
Gastrointestinal disorders: Gastrointestinal irritation is common in patients taking aspirin preparations, and nausea, vomiting dyspepsia, gastritis, gastrointestinal erosions and ulceration have been reported. Anaemia may occur following chronic gastrointestinal blood loss or acute haemorrhage.
Skin and subcutaneous tissue disorders: Skin reactions may occur in susceptible patients.
Renal and Urinary disorders: urate kidney stones
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important.
It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard.
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.
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 or children over the age of four years. In children 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 noncardiac pulmonary oedema.
Central nervous system features including confusion, disorientation, coma and convulsions are less common in adults than in children.
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
B01A C (blood and blood forming organs — antithrombotic agents)
Aspirin has strong analgesic, anti-inflammatory and anti-pyretic activity. It is also used for its anti-thrombotic actions. Once in the body it is rapidly converted to the salicylate form which has similar activity and works via the inhibition of the enzyme cyclo-oxygenase inhibiting prostaglandin synthesis.
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: Single and multiple 100 mg doses of enteric- coated aspirin give systemic bioavailabilities of between 15% and 20% of that seen with immediate release aspirin preparations. Cmax of aspirin for several enteric - coated preparations has been shown to be approximately 100 - 200 ng/ml with a half - life of approximately 1.7 hours. Plasma concentrations of salicylic acid increase disproportionately with dose - a 325 mg dose having a half-life of 2-3 hours and higher doses showing lower plasma concentrations in the presence of an increased half-life due to a disproportionate increase in volume of distribution.
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
None applied on the basis of the active ingredient being a well known and marketed compound with an established efficacy and side effect profile.
6 PHARMACEUTICAL PARTICULARS
6.1 List of excipients
Potato starch
Calcium hydrogen phosphate dihydrate E341 Microcrystalline cellulose E460 Talc E553b
Methacrylic acid - ethylacrylate -copolymer (1: 1) (also contains: Sodium lauryl sulphate and polysorbate 80)
Macrogol
30% Simeticone emulsion
6.2 Incompatibilities
Not applicable
6.3 Shelf life
2 years.
6.4 Special precautions for storage
Do not store above 25°C.
Store in the original package
6.5 Nature and contents of container
28 tablets in a blister pack
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 17907/0158
9 DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION
21/10/2005
10 DATE OF REVISION OF THE TEXT
16/07/2015