BRANDS OF ASPIRIN IN KENYA:
Ascard-75®, , ATCO
ASP – 81®,, Intas Pharmaceuticals Ltd
Aspegic®,, Sanofi Aventis
Aspirin, Beta Healthcare International Limited.
Aspirin , Biodeal Laboratories Ltd
Aspirin , Elys Chemical Industries Ltd
Aspirin, Laboratory & Allied Ltd
Aspirin , Mac’s Pharmaceuticals Ltd
Aspirin , Regal Pharmaceuticals Limited
Aspirin Cardio®,,Bayer East Africa Limited
Aspirin Junior®, ,Biodeal Laboratories Ltd
Asroho®,, Mac’s Pharmaceuticals Ltd
Cardisprin®, , Cosmos Limited
Cardilife 75®, , PSM Pharmaceuticals Ltd
Dawasprin75®, , Dawa Limited
Delisprin , Aristo Pharmaceuticals Pvt.ltd
Totoprin®, , Laboratory & Allied Ltd
Vipirin®, Laboratory & Allied Ltd
Asprin Chemical Structure
ASPIRIN MODE OF ACTION
Aspirin is an anti-inflammatory analgesic and antipyretic.
Aspirin is analgesic, anti-inflammatory, antipyretic and an inhibitor of platelet aggregation. It prolongs the bleeding time. It 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.
Aspirin has analgesic, antipyretic and anti-inflammatory actions. It is indicated for:
- The relief of headache, toothache, migraine, neuralgia, sore throat, dysmenorrhoea.
- The symptomatic relief of influenza, feverishness, rheumatic pains, sciatica, lumbago, fibrositis, muscular aches and pains.
- It also has an antithrombotic 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 and cerebral transient ischaemic attacks.
DOSAGE AND ADMINISTRATION:
Adults including elderly: 300-600mg every 3-4 hours as required, to a maximum of 3.6g daily in divided doses.
Children: Do not give to children aged under 16 years, unless specifically indicated (e.g. for Kawasaki’s disease).
Antithrombotic action: For its antithrombotic effect following myocardial infarction, transient ischaemic attack, or in patients with unstable angina, the recommended dose is 50-325mg daily.
Method of Administration
For oral administration.
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
- Methotrexate used at doses >15mg/week
- Children under 16 years old, unless specifically indicated (e.g. Kawasaki’s disease).
ASPIRIN DRUG INTERACTIONS
The following drug interactions should be considered when prescribing aspirin:
- Analgesics – avoid concomitant administration of other salicylates or other NSAIDs (including topical formulations) as increased risk of side effects.
- Alkalizers of urine (eg antacids, citrates) – increased excretion of aspirin.
- Metoclopramide and domperidone – increased rate of absorption of aspirin.
- Mifepristone – avoid aspirin until 8-12 days after mifepristone.
- Ototoxic medicine (eg 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.
- Laboratory investigations – aspirin may interfere with some laboratory tests such as urine 5-hydroxyindoleacetic acid determinations and copper sulfate urine sugar tests.
- Calcium-channel blockers – reduced hypotensive effects, increased antiplatelet effect which rarely results in pro-longed bleeding time.
- 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 .
- Ginkgo Biloba – possible increase in risk of bleeding.
Methotrexate (used at doses >15 mg/week):
The combined drugs, methotrexate and acetylsalicylic acid, enhance haematological toxicity of methotrexate due to the decreased renal clearance of methotrexate by acetylsalicylic acid. Therefore, the concomitant use of methotrexate (at doses >15 mg/week) with acetylsalicylic acid is contraindicated .
Not recommended combinations
Uricosuric agents, e.g. probenecid
Salicylates reverse the effect of probenecid. The combination should be avoided.
Combinations requiring precautions for use or to be taken into account
Anticoagulants e.g. coumarin, heparin, warfarin
Increased risk of bleeding due to inhibited thrombocyte function, injury of the duodenal mucosa and displacement of oral anticoagulants from their plasma protein binding sites. The bleeding time should be monitored (see section 4.4).
Anti-platelet agents (e.g clopidogrel and dipyridamole) and selective serotonin reuptake inhibitors (SSRIs; such as sertraline or paroxetine)
Increased risk of gastrointestinal bleeding (see section 4.4).
Antidiabetics, e.g. sulfonylureas
Salicylics may increase the hypoglycaemic effect of sulfonylureas.
Digoxin and lithium
Acetylsalicylic acid impairs the renal excretion of digoxin and lithium, resulting in increased plasma concentrations. Monitoring of plasma concentrations of digoxin and lithium is recommended when initiating and terminating treatment with acetylsalicylic acid. Dose adjustment may be necessary
Diuretics and antihypertensives
NSAIDs may decrease the antihypertensive effects of diuretics and other antihypertensive agents. As for other NSAIDs concomitant administration with ACE-inhibitors increases the risk of acute renal insufficiency.
Diuretics: Risk of acute renal failure due to the decreased glomerual filtration via decreased renal prostaglandin synthesis. Hydrating the patient and monitoring renal function at the start of the treatment is recommended.
Carbonic anhydrase inhibitors (acetazolamide)
May result in severe acidosis and increased central nervous system toxicity
The risk of gastrointestinal ulceration and bleeding may be increased when acetylsalicylic acid and corticosteroids are co-administered (see section 4.4).
Methotrexate (used at doses <15 mg/week):
The combined drugs, methotrexate and acetylsalicylic acid, may increase haematological toxicity of methotrexate due to decreased renal clearance of methotrexate by acetylsalicylic acid. Weekly blood count checks should be done during the first weeks of the combination. Enhanced monitoring should take place in the presence of even mildly impaired renal function, as well, as in elderly.
Increased risk of ulcerations and gastrointestinal bleeding due to synergistic effects.
Concomitant use of NSAIDs and ciclospoin or tacrolimus may increase the nephrotoxic effect of ciclosporin and tacrolimus. The renal function should be monitored in case of concomitant use of these agents and acetylsalicylic acid.
Acetylsalicylic acid has been reported to decrease the binding of valproate to serum albumin, thereby increasing its free plasma concentrations at steady state.
Salicylate diminishes the binding of phenytoin to plasma albumin. This may lead to decreased total phenytoin levels in plasma, but increased free phenytoin fraction. The unbound concentration, and thereby the therapeutic effect, does not appear to be significantly altered.
Concomitant administration of alcohol and acetylsalicylic acid increases the risk of gastrointestinal 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 .
Metamizole may reduce the effect of acetylsalicylic acid on platelet aggregation, when taken concomitantly. Therefore, this combination should be used with caution in patients taking low dose aspirin for cardioprotection.
ASPIRIN DRUG ADVERSE REACTIONS:
Blood and lymphatic system disorders
Increased bleeding tendencies.
Thrombocytopenia, agranulocytosis, aplastic anaemia.
Cases of bleeding with prolonged bleeding time such as epistaxis, gingival bleeding. Symptoms may persist for a period of 4–8 days after acetylsalicylic acid discontinuation. As a result there may be an increased risk of bleeding during surgical procedures.
Existing (haematemesis, melaena) or occult gastrointestinal bleeding, which may lead to iron deficiency anaemia (more common at higher doses).
anaemia, haemolytic anaemia, hypoprothrombinaemia, pancytopenia, occult blood loss, elevated transaminase levels
Immune system disorders
Hypersensitivity reactions, angio-oedema, allergic oedema, anaphylactic reactions including shock.
Metabolism and digestive system disorders
Nervous system disorders
Ear and labyrinth disorders
Reduced hearing ability; tinnitus.
Respiratory, thoracic and mediastinal disorders
Bronchospasm, asthma attacks.
Reproductive system and mammary disorders
Severe gastrointestinal haemorrhage, nausea, vomiting.
Gastric or duodenal ulcers and perforation which can occasionally be major (may develop bloody or black tarry stools, severe stomach pain and vomiting blood), gastrointestinal irritation (mild stomach pain), erosions, heartburn, Fatalities have occurred.
Hepatic insufficiency, hepatitis (particularly in patients with SLE or connective tissue disease)
Renal and urinary tract disorders
Not known: Impaired renal function
Body as a whole – general disorders
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)
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Clinical | Pharmacokinetic data
Routes of Administration: Oral
Protein Binding: 80–90%
Metabolosim: Liver, (CYP2C19 and possibly CYP3A), some is also hydrolysed to salicylate in the gut wall
Onset of Action:
Elimination Half life: Dose-dependent; 2 h to 3 h for low doses (100 mg or less), 15 h to 30 h for large doses
Excretion: Urine (80–100%), sweat, saliva, feces
Legal Status | Dosage forms & Strengths
OTC / Rx-only
Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
This Drug is not Subject to DDA drugs Act
Dosage Forms | Strengths:
|CompTox Dashboard (EPA)|
- PPB Drugs Retention Register
- Awtry, Eric H., and Joseph Loscalzo. “Aspirin.” Circulation 101.10 (2000): 1206-1218.
- Patrono, Carlo. “Aspirin as an antiplatelet drug.” New England Journal of Medicine 330.18 (1994): 1287-1294.
- Roth, Gerald J., Nancy Stanford, and Philip W. Majerus. “Acetylation of prostaglandin synthase by aspirin.” Proceedings of the National Academy of Sciences 72.8 (1975): 3073-3076.
- Vane, J. R., and R. M. Botting. “The mechanism of action of aspirin.” Thrombosis research 110.5-6 (2003): 255-258.