Aspirin Tablets 300mg
Out of date information, search anotherSUMMARY OF PRODUCT CHARACTERISTICS
1 NAME OF THE MEDICINAL PRODUCT
Dispersible Aspirin Tablets 300mg
2 QUALITATIVE AND QUANTITATIVE COMPOSITION
Each tablet contains 300mg Aspirin
3 PHARMACEUTICAL FORM
White uncoated tablets
4 CLINICAL PARTICULARS
4.1 Therapeutic indications
Aspirin has analgesic, antipyretic and anti-inflammatory actions. It is indicated for:
1) The relief of headache, toothache, migraine, neuralgia, sore throat, dysmenorrhoea.
2) The symptomatic relief of influenza, feverishness, rheumatic pains, sciatica, lumbago, fibrositis, muscular aches and pains.
4.2 Posology and method of administration
The tablets should be dispersed in water before administration.
Adults including elderly: 1-2 tablets at intervals of not less than 4 hours, to a maximum of four doses in 24 hours.
Children: Do not give to children aged under 16 years, unless specifically indicated (e.g. for Kawasaki’s disease).
To be dispersed in water for oral use.
4.3 Contraindications
Aspirin should not be taken by patients with the following conditions:
• Known hypersensitivity to aspirin, other ingredients in the product, other salicylates or non-steroidal anti-inflammatory drugs (a patient may have developed anaphylaxis, angioedema, asthma, rhinitis or urticaria induced by aspirin or other NSAIDs).
• Nasal polyps associated with asthma (high risk of severe sensitivity reactions).
• Active peptic ulceration or a past history of ulceration or dyspepsia.
• Haemophilia or other haemorrhagic disorder (including thrombocytopenia) as there is an increased risk of bleeding.
• Concurrent anticoagulant therapy should be avoided.
• Severe hepatic impairment
• Severe renal impairment
• Severe cardiac failure
• Third trimester of pregnancy
• Children under 16 years old, unless specifically indicated (e.g. Kawasaki’s disease).
4.4 Special warnings and precautions for use
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).
Aspirin should be used with caution in patients with:
• allergic disease
• anaemia (may be exacerbated by GI blood loss)
• asthma (increased risk of bronchospastic sensitivity reactions)
• cardiac failure (conditions which predispose to fluid retention)
• dehydration
• glucose-6-phosphate dehydrogenase deficiency (aspirin rarely causes haemolytic anaemia)
• gout (serum urate may be increased)
• hepatic function impairment (avoid if severe)
• renal function impairment
• Surgery. Aspirin should be discontinued several days before scheduled surgery (including dental extractions)
• systemic lupus erythematosus and other connective tissue disorders (hepatic and renal function may be impaired in these conditions)
• thyrotoxicosis (may be exacerbated by large doses of salicylates)
• Long term use in elderly patients should be avoided due to a risk of gastrointestinal bleeding.
• Vaccine recipients should avoid use of salicylates for 6 weeks after varicella vaccination (see section 4.5).
• 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.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
The following warnings are on the OTC product labelling:
Do not take if you have a stomach ulcer If symptoms persist for more than 3 days, consult your doctor Medicines should not be taken in pregnancy without consulting your doctor Keep out of the reach of children
Do not give to children aged under 16 years, unless on the advice of a doctor.
4.5 Interaction with other medicinal products and other forms of interaction
The following drug interactions should be considered when prescribing
aspirin:
• Alcohol - may enhance gastro-intestinal side effect of aspirin.
• Analgesics - avoid concomitant administration of other salicylates or other NSAIDs (including topical formulations) as increased risk of side effects.
• Alkalizers of urine (e.g. carbonic anhydrase inhibitors, antacids, citrates) -increased excretion of aspirin.
• Anticoagulants or platelet aggregation inhibitors - increased risk of bleeding.
• Antiepileptic drugs (eg phenytoin, sodium valproate) - increased effect.
• Corticosteroids - increased risk of gastro-intestinal bleeding or ulceration.
• Dipyridamole - increase in peak concentration.
• Diuretics: furosemide and acetazolamide (risk of toxic effects), spironolactone (antagonized diuretic action).
• Hypoglycaemics - enhanced activity.
• Methotrexate - increased toxicity.
• Metoclopramide and domperidone - increased rate of absorption of aspirin.
• Mifepristone - avoid aspirin until 8-12 days after mifepristone.
• Ototoxic medicine (e.g. vancomycin) - potential for ototoxicity increased. Hearing loss may occur and may progress to deafness even after discontinuation of the medication. Effects may be reversible but are usually permanent.
• Uricosurics (e.g. probenecid, sulfinpyrazone) - effects of uricosurics reduced.
• Laboratory investigations - aspirin may interfere with some laboratory tests such as urine 5-hydroxyindoleacetic acid determinations and copper sulphate urine sugar tests.
• ACE inhibitors - reduced hypotensive effect, increased risk of renal impairment and hypokalaemia. Monitoring of renal function may be required.
• Calcium-channel blockers - reduced hypotensive effects, increased antiplatelet effect which rarely results in pro-longed bleeding time.
• SSRIs - increased risk of gastrointestinal bleeding
• Varicella vaccine - Vaccine recipients should avoid use of salicylates for 6 weeks after vaccination with varicella vaccine as Reye's syndrome has
been reported following use of salicylates during wild-type varicella infection (see section 4.4).
• Ginkgo Biloba - possible increase in risk of bleeding.
• Experimental data suggest that ibuprofen may inhibit the effect of low dose acetylsalicylic acid on platelet aggregation when they are dosed concomitantly. However, the limitations of these data and the uncertainties regarding extrapolation of ex vivo data to the clinical situation imply that no firm conclusions can be made for regular ibuprofen use, and no clinically relevant effect is considered to be likely for occasional ibuprofen use (see section 5.1).
4.6 Fertility, pregnancy and lactation Pregnancy
Inhibition of prostaglandin sysnthesis may adversely affect the pregnancy and/or the embryo/fetal development. Data from epidemiology studies suggest an increased risk of miscarriage and of cardiac malformation after use of a prostaglandin synthesis inhibitor in early pregnancy. The absolute risk for cardiovascular malformation was increased from less than 1%, up to approximately 1.5%.
Studies in animals have shown that salicylates can cause birth defects including fissure of the spine and skull, facial clefts and malformations of the CNS, viscera and skeleton, pre and post implantation loss and embryo-fetal lethality. During the first and second trimester aspirin should not be given unless necessary. Regular or high dose use of salicylates late in pregnancy may result in:
- constriction or premature closing of the fetal ductus arteriosus
- increased risk of still birth or neonatal death
- decreased birth weight
- prolonged labour
- complicated deliveries and increased risk of maternal or fetal haemorrhage
- possibly persistent pulmonary hypertension of newborn
- kernicterus in jaundiced neonates
- renal dysfunction, which may progress to renal failure with oligo-hydramniosis
Administration is contraindicated in the last trimester of pregnancy and should be avoided during the late stages of labour and during the delivery of a premature infant.
Breastfeeding
Use in children under 16 years old is contraindicated due to possible risk of Reye’s syndrome. Since aspirin is distributed into breast milk, breast fed infants may also be at risk. Aspirin should be avoided while breastfeeding.
Fertility
Aspirin should not be given to women wishing to become pregnant, since it is thought that prostaglandin synthesis inhibitors can reduce fertility. The effect on fertility is reversible.
4.7 Effects on ability to drive and use machines
None known
4.8 Undesirable effects
Blood and lymphatic system disorders - anaemia, haemolytic anaemia, hypoprothrombinaemia, thrombocytopenia, aplastic anaemia, pancytopenia, prolonged bleeding time, occult blood loss, elevated transaminase levels, agranulocytosis.
Gastrointestinal disorders - gastrointestinal bleeding, erosions, perforations or ulceration which can occasionally be major (may develop bloody or black tarry stools, severe stomach pain and vomiting blood), gastrointestinal irritation (mild stomach pain, heartburn, vomiting and nausea). Fatalities have occurred.
Hepatic disorders - hepatitis (particularly in patients with SLE or connective tissue disease).
Renal and urinary disorders - disturbances of renal function Ear and labyrinth disorders - tinnitus
Salicylism - mild chronic salicylate intoxication may occur after repeated administration of large doses, symptoms include dizziness, tinnitus, deafness, sweating, nausea, vomiting, headache and mental confusion, and may be controlled by reducing the dose.
General disorders and administration site conditions - Allergic reactions -rhinitis, urticaria, purpura, Stevens-Johnson syndrome, angioneurotic oedema, angio-oedema, asthma, worsening of asthma, bronchospasms.
Children
Aspirin may be associated with the development of Reye’s Syndrome (encephalopathy and hepatic failure) in children presenting with an acute febrile illness.
4.9 Overdose
Symptoms:
Common features:
Salicylates cause nausea, vomiting, tinnitus, lethargy or dizziness in mild poisoning. Dehydration, restlessness, sweating, warm extremities with bounding pulses, increased respiratory rate and hyperventilation occur in moderate poisoning. Some degree of acid-base disturbance is present in most cases.
Uncommon features:
Haematemesis, hyperpyrexia, hypoglycaemia, hypokalaemia, thrombo-cytopaenia, increased INR/PTR, disseminated intravascular coagulation, renal failure and non-cardiogenic pulmonary oedema.
Central nervous system features including confusion, disorientation, coma and convulsions are less common in adults than in children
Treatment:
Consider oral activated charcoal (50g for an adult, 1g/kg for a child) in adults and children who have ingested more than 125mg/kg body weight salicylate, or any amount of methyl salicylate, less than 1 hour previously.
Consider gastric lavage in adults and children who have ingested more than 500mg/kg body weight salicylate less than 1 hour previously.
Plasma salicylate, U & Es, INR/PTR, blood glucose, pH and electrolytes should be measured.
Fluid losses replaced and forced alkaline diuresis (e.g. with sodium bicarbonate) should be considered when the plasma salicylate concentration is greater than 500mgl-1 (3.6mmol l-1) in adults or 300mgl-1 (2.2mmol l-1) in children.
In very severe cases of poisoning haemodialysis may be needed.
5 PHARMACOLOGICAL PROPERTIES
5.1 Pharmacodynamic properties
ATC code: N02BA01
Aspirin is an anti-inflammatory analgesic and antipyretic.
Aspirin inhibits fatty acid cyclo-oxygenase by acetylation of the active site of the enzyme, and most of its pharmacological effects are due to inhibition of the formation of cyclo-oxygenase products including thromboxanes, prostaglandins and prostacyclin. There has been much interest in the dose-response curve for aspirin, particularly in relation to its action upon platelets. The effect on platelets is cumulative over their 8-day life span because they have no capacity to resynthesie the cyclo-oxygenase enzyme.
Aspirin has an active metabolite (salicylate) which, in addition to possessing some anti-inflammatory properties in its own right, also has important effects on respiration, acid-base balance and the stomach. Salicylates stimulate respiration by a direct effect on the medulla, and at high concentrations, uncouple oxidative phosphorylation in muscle, increasing oxygen consumption and carbon dioxide production. Hyperventilation causes respiratory alkalosis which is compensated by renal excretion of bicarbonate. When large toxic doses of salicylate are ingested and carbohydrate metabolism is deranged, lactic and pyruvic acids accumulate and renal function is impaired, resulting in metabolic acidosis. Salicylates have a direct irritant effect on the gastric mucosa and further predispose to ulceration by inhibiting synthesis of vasodilator and cytoprotective prostaglandins. Large doses of salicylates (greater than 5g per day) are uricosuric, but such doses are poorly tolerated and salicylates are no longer used to treat gout.
Experimental data suggest that ibuprofen may inhibit the effect of low dose acetylsalicylic acid on platelet aggregation when they are dosed concomitantly. In one study, when a single dose of ibuprofen 400mg was taken within 8 hours before or within 30 minutes after immediate release acetylsalicylic acid dosing (81mg), a decreased effect of ASA on the formation of thromboxane or platelet aggregation occurred. However, the limitations of these data and the uncertainties regarding extrapolation of ex vivo data to the clinical situation imply that no firm conclusions can be made for regular ibuprofen use, and no clinically relevant effect is considered to be likely for occasional ibuprofen use.
5.2 Pharmacokinetic properties
Absorption of non-ionised aspirin occurs in the stomach. Hydrolysis to salicylic acid occurs rapidly in the intestine and in the circulation. Aspirin is bound to plasma proteins and is rapidly distributed to all body tissues. It appears in breast milk and crosses the placenta. The rate of excretion of aspirin depends upon urinary pH, increasing as pH rises and being greatest at pH 7.5 and above. It is excreted as salicylic acid and as glucuronide conjugates and as salicyluric and gentisic acids.
5.3 Preclinical safety data
Not applicable
6 PHARMACEUTICAL PARTICULARS
6.1 List of excipients
Citric acid Lactose Maize starch Saccharin sodium E170
6.2 Incompatibilities
Iron salts, alkalis and carbonates
6.3 Shelf life
Two years from the date of manufacture
Shelf-life after dilution/reconstitution Not applicable
Shelf-life after first opening Not applicable
6.4 Special precautions for storage
Keep tightly closed and store below 25°C in a dry place
6.5 Nature and contents of container
Child-resistant blister pack: (i) white 250pm PVC/ 30pm PE/ 90g/m2 PVdC (ii) 9pm soft aluminium/ 35g/m2 glassine paper. Compliant with BS EN 14375.
Pack sizes:
GSL: 16 P: 28, 30, 32
POM: 50, 56, 60, 100
PE tablet container with a child-resistant PP closure. A silica gel container is included in each pack. Compliant with ISO 8317.
Pack sizes:
GSL: 16 P: 30, 32
POM: 100
PP tablet container with or without polyfoam wad or polyethylene ullage filler and a PE closure for supply to nursing homes. A silica gel container is included in each pack.
Pack sizes:
POM: 500, 1000
6.6 Special precautions for disposal
Not applicable
7 MARKETING AUTHORISATION HOLDER
Actavis UK Limited (Trading style: Actavis)
Whiddon Valley Barnstaple N Devon EX32 8NS
8 MARKETING AUTHORISATION NUMBER
PL 00142/5519R
9 DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION
08/04/1980 / 27/01/2004
10 DATE OF REVISION OF THE TEXT
22/10/2010