Aspirin

Registered South African indications:

• Inhibition of platelet aggregation
  - Risk reduction of myocardial infarction in patients with unstable angina or in patients who have had a previous myocardial infarction
  - Risk reduction of recurrent transient ischaemic attacks or stroke in men who have had transient ischaemia of the brain due to fibrin platelet emboli
  - Risk reduction of graft occlusion following aorta coronary by-pass surgery
• Relief of pain and fever - mild to moderate

Contraindications 

South African recommendations

Oral (dsp)

• Hypersensitivity to aspirin or to any of the excipients
• Hypersensitivity to other non-steroidal anti-inflammatory drugs (NSAIDs)
• Peptic ulcers
• Haemophilia
• Severe renal impairment
• Hepatic impairment
• In patients receiving oral anti-coagulant therapy
• During the first and third trimesters of pregnancy
• Lactation
• History of gastrointestinal bleeding or perforation (PUB’S) related to previous NSAIDs, including aspirin dispersible tablets
• Active or history of recurrent ulcer/haemorrhage/perforations
• Heart failure
• Nasal polyps associated with asthma
• Children under the age of 16, due to a possible risk of Reye's syndrome, unless specifically indicated

Oral (ect)

• Hypersensitivity to aspirin, salicylic acid compounds or prostaglandin synthetase inhibitors (e.g. certain asthma patients who may suffer an attack or faint), or to any of the excipients
• Active, or history of recurrent peptic ulcer and/or gastric/intestinal haemorrhage, or other kinds of bleeding such as cerebrovascular haemorrhages
• Should not be administered to patients with haemorrhagic diathesis
• Coagulation disorders such as haemophilia and thrombocytopenia
• Severe hepatic impairment
• Severe renal impairment
• Gout
• Severe cardiac insufficiency
• Methotrexate used at doses >15mg/week
• Aspirin should not be taken during the first and third trimesters of pregnancy
• Lactation
• Aspirin should be discontinued one week before scheduled surgical procedures
• Do not exceed the recommended daily dose

Oral (100mg tab)

• Hypersensitivity to aspirin, or to any of the excipients
• Patients with an intolerance to aspirin (especially aspirin-sensitive asthmatics)
• Patients with aspirin induced nasal polyps
• History of asthma induced by the administration of salicylates or substances with a similar action, notably non-steroidal anti-inflammatory medicines
• Heart failure that is not well controlled
• History of gastrointestinal perforation, ulceration or bleeding (PUBs) related to previous NSAIDs, including aspirin tablets
• Active or history of recurrent ulcer/haemorrhage/perforations
• Patients with gout
• Haemorrhagic diathesis
• Severe renal impairment
• Severe hepatic impairment
• Combination with methotrexate at doses of 15mg/week or more
• Should not be taken from 20 weeks’ gestation or later in pregnancy
• Lactation

Oral (300mg tab)

• Hypersensitivity to aspirin, or to any of the excipients
• Heart failure
• History of gastrointestinal perforation, ulceration or bleeding (PUBs) related to previous non-steroidal anti-inflammatory drugs (NSAIDs)
• Active or history of recurrent ulcer, haemorrhage or perforations
• Severe renal impairment
• Concomitant oral anticoagulant therapy
• Haemophilia
• Pregnancy
• Lactation
• Not to be used in children under the age of 12 years

Recommendations in other jurisdictions

Oral (dsp)

• Previous history of peptic ulceration
• Active peptic ulceration
• Haemophilia
• Some formulations contain soy protein. If the patient is allergic to peanut or soya, they should be advised not to use this medicinal product

Cautions 

• Pregnancy <30 weeks (Recommendations in other jurisdictions) 
• Breastfeeding (Recommendations in other jurisdictions)
• Mild to moderate renal impairment (South African recommendations)
• Renal impairment (Recommendations in other jurisdictions)
• Mild to moderate hepatic impairment (ect, 100mg tab) (South African recommendations)
• Hepatic impairment (300mg tab) (South African recommendations)
• Severe hepatic impairment (Recommendations in other jurisdictions)
• Elderly
• Children <16 years
• Surgery including tooth extraction
• Menorrhagia
• History of gastric or duodenal ulcer
• Haemorrhagic episodes
• History of asthma
• History of hay fever
• History of nasal polyps
• History of chronic respiratory diseases
• History of allergic reactions to other substances
• Anaemia
• Cardiac failure
• Conditions which predispose to fluid retention
• Dehydration
• Glucose-6-phosphate dehydrogenase deficiency
• Gout
• Systemic lupus erythematosus
• Connective tissue disorders
• Thyrotoxicosis
• Within 6 weeks of varicella vaccination
• Hypertension
• Long-term (>3 months) administration every two days or more frequently
• Galactose intolerance (certain formulations)
• Lapp lactase deficiency (certain formulations)
• Glucose-galactose malabsorption (certain formulations)
• Fructose intolerance (certain formulations)
• Sucrase-isomaltase insufficiency (certain formulations)

Forms avail. in SA and covered in this monograph: tab, dsp, ect

Dosages below include:

• South African registered indications and dosages
• Indications and dosages registered in other jurisdictions

South African registered indications and dosages

Inhibition of platelet aggregation
- Risk reduction of myocardial infarction in patients with unstable angina or in patients who have had a previous myocardial infarction
- Risk reduction of recurrent transient ischaemic attacks or stroke in men who have had transient ischaemia of the brain due to fibrin platelet emboli
- Risk reduction of graft occlusion following aorta coronary by-pass surgery

80mg

• Oral (dsp): Initial: 160mg, dly on the first day; Maintenance: 80mg, dly preferably at the same time each day

100mg

• Oral (dsp, tab): 100-300mg, dly preferably at the same time each day
• Oral (ect): 100mg, dly preferably at the same time each day

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Enteric coated tablets: For reducing the risk of myocardial ischaemic events in people with increased cardiovascular risk: 100mg to be taken every day preferably at the same time each day according to the individual needs of the patient

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The enteric coated tablets should preferably be taken at least 30 minutes before meals, with plenty of water. They should not be crushed, broken, or chewed to ensure a release in the alkaline milieu of the intestine and to not destroy the protective effect of the enteric coating

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81mg

• Oral (ect): 81-243mg, dly preferably at the same time each day

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The optimal dose for inhibition of platelet aggregation in humans is not known. Aspirin should not be used for indications related to the inhibition of platelet aggregation unless directed by a doctor

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The 100mg dispersible tablet can be dispersed on the tongue without water

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Aspirin tablets should be swallowed whole

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Relief of pain and fever - mild to moderate
- Short term use

300mg

• Oral (tab): Oral (tab): 300-600mg, 8hrly; Treatment duration: ≤10 days

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Use the lowest effective dose for the shortest possible duration of treatment. Do not use continuously for longer than ten days without consulting your doctor

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The tablets should preferably be taken after meals, with plenty of water

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300mg

• Oral (dsp): 300-900mg, 4hrly as needed; Treatment duration: ≤10 days; Max: 3600mg/24hrs

500mg

• Oral (dsp): 500-1000mg, 4hrly as needed; Treatment duration: ≤10 days; Max: 4000mg/24hrs

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Patients should be advised not to use aspirin continuously for more than 10 days without consulting their doctor

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Aspirin dispersible 300mg can be dissolved in water, or if preferred, on the tongue. The 500mg dispersible tablet should be dissolved in water before being taken

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Indications and dosages registered in other jurisdictions

Relief of pain - mild to moderate
- Headaches, including migraine headaches, toothache, neuralgia, sciatica, period pains and sore throats
Reduction of temperature in feverishness, influenza and colds
Reduction of inflammation in rheumatism and lumbago

• Oral (dsp): 600-900mg, 4hrly; Max: 3900mg/24hrs

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Oral administration after dissolution in water

Paed. forms avail. in SA and covered in this monograph: tab, dsp

Dosages below include:

• South African registered indications and dosages
• Indications and dosages registered in other jurisdictions

South African registered indications and dosages

Relief of pain and fever - mild to moderate
- Short term use

300mg

Younger than 12 years

• Oral (tab): Contraindicated

Older than 12 years

• Oral (tab): See adult dosage

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The tablets should preferably be taken after meals, with plenty of water

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Use the lowest effective dose for the shortest possible duration of treatment

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Aspirin has been implicated in Reye's syndrome, a rare but serious illness in children and teenagers with chickenpox and influenza. A doctor should be consulted before aspirin is used in such patients

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300mg

Younger than 16 years

• Oral (dsp): Contraindicated

Older than 16 years

• Oral (dsp): 300-600mg, not more than 6hrly as needed; Treatment duration: ≤10 days; Max: 3000mg/24hrs

500mg

Younger than 16 years

• Oral (dsp): Contraindicated

Older than 16 years

• Oral (dsp): 500mg, repeat 4hrly as needed; Treatment duration: ≤ 10 days; Max: 4000mg/24hrs

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Aspirin dispersible 300mg can be dissolved in water, or if preferred, on the tongue. The 500mg dispersible tablet should be dissolved in water before being taken

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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 the age of 16 years unless specifically indicated by a doctor or pharmacist

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Indications and dosages registered in other jurisdictions

Relief of pain - mild to moderate
- Headaches, including migraine headaches, toothache, neuralgia, sciatica, period pains and sore throats
Reduction of temperature in feverishness, influenza and colds
Reduction of inflammation in rheumatism and lumbago

Younger than 16 years

• Oral (dsp): Not established for use

Older than 16 years

• Oral (dsp): See adult dosage

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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)

Pregnancy

South African recommendations

• Oral (dsp): First and third trimester: Contraindicated
• Regular use of non-steroidal anti-inflammatory drugs during the third trimester of pregnancy, may result in premature closure of the foetal ductus arteriosus in utero, and possibly, in persistent pulmonary hypertension of the new born. The onset of labour may be delayed, and its duration increased
   
• Oral (ect): First and third trimester: Contraindicated
• During the third trimester of pregnancy, all prostaglandin synthesis inhibitors may expose the foetus to
  - Cardiopulmonary toxicity (with premature closure of the ductus arteriosus and pulmonary hypertension)
  - Renal dysfunction, which may progress to renal failure with oligo- hydroamniosis; the mother and the neonate, at the end of pregnancy, to possible prolongation of bleeding time, an anti-aggregating effect which may occur even at very low doses
  - Inhibition of uterine contractions resulting in delayed or prolonged labour
   
• Oral (tab): 20 weeks’ gestation or later: Contraindicated
• The administration of aspirin around 20 weeks or later in pregnancy may cause foetal renal dysfunction, which may progress to renal failure with oligohydroamniosis, and in some cases neonatal renal impairment
• Complications of prolonged oligohydramnios may include limb contractures and delayed lung maturation.
• Oligohydramnios may, but not always be reversible with aspirin treatment discontinuation
• Aspirin use during the third trimester of pregnancy, may result in premature closure of the foetal ductus arteriosus in utero, and possibly, in persistent pulmonary hypertension of the new-born
• The onset of labour may be delayed, and its duration increased

Recommendations in other jurisdictions

• Oral (dsp): Caution
• There is clinical and epidemiological evidence of the safety of aspirin in human pregnancy, but it may prolong labour and contribute to maternal and neonatal bleeding and is best avoided at term

Breastfeeding

South African recommendations

• Oral (dsp): Contraindicated
   
• Oral (ect): Contraindicated
• Low quantities of salicylates and of their metabolites are excreted into the breast milk. Since adverse effects for the infant have not been reported up to now, short-term use of the recommended dose does not require suspending lactation. In cases of long-term use and/or administration of higher doses, breastfeeding should be discontinued
   
• Oral (tab): Contraindicated
• Salicylates and its metabolites pass into breastmilk. Safety is unproven. Mothers on treatment with asprin should not breastfeed their babies

Recommendations in other jurisdictions

• Caution; not recommended
• Aspirin is best avoided during breastfeeding (dsp)

Renal Impairment

South African recommendations

• Mild to moderate: Caution; no dose adjustment recommended
• Severe: Contraindicated

Recommendations in other jurisdictions

• Caution; no dose adjustment recommended

Hepatic Impairment

South African recommendations

• Oral (300mg tab): Caution; no information available
• Oral (ect, 100mg tab): Mild to moderate: Caution; no dose adjustment recommended
• Oral (ect, 100mg tab): Severe: Contraindicated
• Oral (dsp): Contraindicated

Recommendations in other jurisdictions

• Mild to moderate: No dose adjustment recommended
• Severe: Caution; no dose adjustment recommended

Elderly

• Caution; no dose adjustment recommended
  In general, aspirin should be used with caution in elderly patients who are more prone to adverse events. The usual adult dose is recommended in the absence of severe renal or hepatic insufficiency. Treatment should be reviewed at regular intervals

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Intracranial haemorrhage
• Headache
• Vertigo

Cardiovascular Disorders

• Hypertension
• Cardiac failure
• Haemorrhagic vasculitis

Respiratory Disorders

• Rhinitis
• Dyspnoea
• Bronchospasm
• Asthma attacks

Gastrointestinal Disorders

• Dyspepsia
• Severe gastrointestinal haemorrhage
• Nausea and vomiting
• Gastric or duodenal ulcers and perforation
  - Bloody or black, tarry stools
  - Severe stomach pain
  - Vomiting blood
• Gastrointestinal irritation
• Erosions
• Heartburn
• Diarrhoea

Hepatobiliary Disorders

• Hepatic insufficiency
• Hepatitis
• Increased transaminase levels

Genitourinary Disorders

• Menorrhagia
• Impaired renal function
• Salt and water retention

Endocrine and Metabolic Disorders

• Hyperuricemia

Skin and Subcutaneous Tissue Disorders

• Urticaria
• Stevens-Johnson syndrome
• Lyells syndrome
• Purpura
• Erythema nodosum
• Erythema multiforme

Immune, Blood and Lymphatic System Disorders

• Increased bleeding tendencies
• Thrombocytopenia
• Agranulocytosis
• Aplastic anaemia
• Prolonged bleeding time
• Epistaxis
• Gingival bleeding
• Anaemia
• Haemolytic anaemia
• Hypoprothrombinaemia
• Pancytopenia
• Occult blood loss
• Hypersensitivity reactions
• Angio-oedema
• Allergic oedema
• Anaphylactic reactions including shock
• Iron deficiency anaemia due to existing or occult gastrointestinal bleeding

Sensory Disorders

• Reduced hearing ability
• Tinnitus

Other

• Salicylism (after repeated administration of large doses)
  - Dizziness
  - Tinnitus
  - Deafness
  - Sweating
  - Nausea
  - Vomiting
  - Headache
  - Mental confusion

• Methotrexate
• Uricosuric agents
• Probenecid
• Anticoagulants
• Coumarin
• Heparin
• Warfarin
• Antiplatelet agents
• Clopidogrel
• Dipyridamole
• Selective serotonin reuptake inhibitors
• Sertraline
• Paroxetine
• Antidiabetic agents
• Sulphonylureas
• Digoxin
• Lithium
• Antihypertensive agents
• Diuretics
• Carbonic anhydrase inhibitors
• Acetazolamide
• Systemic corticosteroids
• Non-steroidal anti-inflammatory drugs (including topical formulations)
• Ibuprofen
• Ciclosporin
• Tacrolimus
• Phenytoin
• Sodium valproate
• Metamizole
• Analgesics
• Alkalizers of urine
• Antacids
• Citrates
• Metoclopramide
• Domperidone
• Mifepristone
• Ototoxic agents
• Vancomycin
• Calcium channel blockers
• Varicella vaccine

Other

• Alcohol
• Ginkgo biloba
• Laboratory investigations (see additional prescribing points)

None routine. Specific cases may require

• Renal function
• Hepatic function

Interaction with laboratory investigations

• Aspirin may interfere with some laboratory tests such as urine 5-hydroxyindoleacetic acid determinations and copper sulfate urine sugar tests

Aspirin inhibits platelet aggregation. Blocking the platelet cyclooxygenase by acetylation, it inhibits thromboxane A2 synthesis, a physiological activating substance released by the platelets and which would play a role in the complications of the atheromatosic lesions. Inhibition of TXA2-synthesis is irreversible, because thrombocytes, which have no nucleus, are not capable (due to lack of protein synthesis capability) to synthesise new cyclooxygenase, which had been acetylated by acetylsalicylic acid. By inhibiting the cyclooxygenase enzyme, conversion of phospholipids to prostaglandins is prevented and this prevention of prostaglandin production is believed to result in peripheral analgesia, fever reduction, reduction in inflammation and inhibition of platelet aggregation.

Tablet 81mg

• Ecotrin (Litha) originator

Tablet 100mg

• Bayer aspirin cardio ect (Bayer)
• Myoprin (iPharma)
• Soluspirin CV (Resmed Healthcare)

Tablet dispersible 100mg

• Disprin cardiocare (Reckitt) originator

Tablet 300mg     

• Be-Tabs Aspirin (Be-Tabs)
• Disprin (Reckitt) originator
• DR DU TOIT'S PAIN EXPELLER (iPharma)
• SOLEX (Gulf Drug Company)
• Soluspirin (Resmed Healthcare)

Tablet dispersible 300mg

• Disprin melts (Reckitt) originator
• Soluspirin (Resmed)

Tablet 500mg

• Disprin extra strength (Reckitt) originator