Enteric-coated aspirin. (famous brand Loprin)
COMPOSITION:
Enteric-coated aspirin(Loprin) 75 mg tablets: Each enteric-coated tablet contains Aspirin B.P. 75mg.
Aspirin(Loprin )150 mg tablets: Each enteric-coated tablet contains Aspirin B.P 150mg.
PHARMACOLOGICAL PROPERTIES:
Aspirin has analgesic, anti-inflammatory, and anti-pyretic activity. It also has an antithrombotic action. It is necessary for secondary prophylaxis
following myocardial infarction and patients with unstable angina or ischaemic stroke include cerebral attacks. In the body, it is converted to the salicylate form and works via the inhibition of the enzyme cyclo-oxygenase inhibiting prostaglandin synthesis. The enteric coat is intended to resist gastric fluid while allowing disintegration in the intestinal fluid. Due to the delay that the coating
imposes on the release of the active ingredient. Enteric-coated tablets(for example. aspirin) are unsuitable for the short-term relief of pain.
PHARMACOKINETIC PROPERTIES
Absorption:
Aspirin is fastly absorbed after oral administration, with
some hydrolysis to salicylate before absorption. The absorption of aspirin is slow by the presence of food. It is impaired in patients suffering from migraine attacks. Absorption of medicine is more in patients with achlorhydria.
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.
Distribution:
Aspirin is present in the saliva, milk, plasma, and synovial fluid.
It also crosses the placenta at a concentration less than blood.
Salicylate-extensive protein binding.
Aspirin binds to protein to a small extent.
Metabolism:
In the blood, the drug is rapid hydrolysis to salicylic acid. The Salicylate is reabsorbed by renal tubules in acid urine. The alkaline diuresis will
increase the rate of excretion, 85% of the dose excreted as free salicylate.
INDICATIONS:
Enteric-coated aspirin is recommended for the secondary prevention of thrombotic cerebrovascular or
cardiovascular disease and following bypass surgery.
DOSAGE AND ADMINISTRATION:
Aspirin 75 mg is used only for oral administration to adults.
The drug is Take with water. Do not cut, chew or crush the tablet.
The advice of a doctor is needed before commencing therapy for the first time.
The usual dose, for long-term use, is 75mg-150mg once daily.
In some cases, a higher dose may be necessary, especially in
the short term. The dose of drug up to 300mg a day is used on the advice of a doctor.
In Elderly: The risk-benefit ratio of the antithrombotic action of the Aspirin drug has not been fully established.
Children:
Do not give to children aged under 16 age, unless specifically
indicated (e.g.for Kawasakis disease)
CONTRAINDICATIONS:
Hypersensitivity to aspirin drug or any other NSAIDs may cause
active peptic ulceration or history of peptic ulceration.
Haemophilia.
Gout.
This drug is not given to children aged under sixteen years, unless specifically
indicated (e.g.for Kawasaki's disease).
SPECIAL WARNINGS AND PRECAUTIONS FOR USE:
Precautions are necessary for patients with allergic disease, impairment
of hepatic and dehydration.
Aspirin may also affect bronchospasm or induce attacks of asthma. The elderly may be more attached to the toxic effects of salicylates. The continuous use of aspirin is avoided in the
elderly because of the risk of gastrointestinal bleeding. Caution must be
taken in patients with glucose-6-phosphate dehydrogenase deficiency ass
hemolytic anemia may occur. Aspirin may interfere with insulin and
glucagon in diabetes. Aspirin prolongs bleeding time. Hematological & hemorrhagic
effects can occur and may be severe. Patients should report any unusual
bleeding symptoms to their physician.
Aspirin should not be taken by patients with a history of stomach ulcers. For the management of cardiovascular or cerebrovascular disease by using long-term use of aspirin,
patients should consult their doctor.
INTERACTION WITH OTHER MEDICINAL PRODUCTS AND OTHER
FORMS OF INTERACTION:
Anticoagulants:
Aspirin increased the effect of heparin.
It also increases the risk of bleeding with oral anticoagulants, antiplatelet agents, and fibrinolytic. Concomitant use is not recommended.
Other non-steroidal anti-inflammatory drugs (NSAIDs):
Concurrent administration of drugs can increase side effects. The use of more NSAIDs
increases the risk of gastrointestinal hemorrhage. Experimental data
show that ibuprofen may inhibit the activity of low-dose aspirin on platelet
aggregation.
Corticosteroids:
More use of aspirin can increase the risk of gastrointestinal bleeding and ulceration. Corticosteroids reduce the plasma salicylate concentration.
Antimetabolites:
The activity of methotrexate may be markedly
enhanced and its toxicity increased.
Alcohol:
The harmful effects of aspirin on the gastrointestinal tract are
increased by alcohol.
Antiemetics:
Metoclopramide drugs enhance the effects of aspirin by
increasing the rate of absorption.
ACE Inhibitors:
Aspirin may reduce the antihypertensive effect of ACE
inhibitors.
Ant-epileptics:
This drug may enhance the effects of phenytoin and sodium valproate.
Diuretics:
Antagonism of the diuretic effect of spironolactone.
Hypoglycaemic agents:
Aspirin(enteric-coated) may enhance the effects of insulin and oral hypoglycaemic agents.
Thyroid function tests:
Aspirin may interfere with thyroid function tests.
PREGNANCY AND LACTATION:
Pregnancy:
clinical evidence suggests the
safety of aspirin for use in pregnancy. Caution should be exercised when
considering use in pregnant patients. The use of aspirin before birth
may increase the risk of intracranial hemorrhage in low birth
weight infants. It also contributes to maternal and neonatal bleeding.
Regular use of high does impair platelet function. It produces
hypoprothrombinaemia in the infant due to the low storage of neonatal Vitamin K.
with increased bleeding before & after
delivery decreased birth weight and increased rate of stillbirth have been
reported with high blood salicylate levels. With high doses, there may be
premature closure of the ductus arteriosus.
Lactation:
As aspirin is released in breast milk. Aspirin should not take
those who are breastfeeding. High maternal doses of aspirin may impair platelet activity in the infant.
UNDESIRABLE EFFECTS
Side effects are mild and infrequent:
Blood and the lymphatic system disorders:
Aspirin prolongs bleeding time decreases platelet adhesiveness. The large doses may cause
hypoprothrombinemia, Thrombocytopenia may also occur.
Bleeding disorders such as epistaxis, purpura, ecchymoses,
hemoptysis, gastrointestinal bleeding, hematoma, and cerebral
hemorrhage have been reported. Fatalities have occurred.
Immune system disorder:
Hypersensitivity reactions include skin rashes, urticaria, angioedema, asthma, bronchospasm, rhinitis, and rarely, anaphylaxis,
Ear& Labyrinth disorder: Tinnitus,
Gastrointestinal disorders: Gastrointestinal irritation exists in
patients taking aspirin preparations. Other symptoms like nausea, vomiting, dyspepsia,
gastritis, and ulceration have been reported.
Anemia may occur.
Skin and subcutaneous tissue disorders:
Skin reactions may occur in susceptible patients.
Renal and Urinary disorders: kidney stones have formed.
OVERDOSE:
Single doses of the drug less than 100mg/kg are unlikely to cause poisoning.
"features include vomiting, dehydration, tinnitus
deafness, sweating. Extremities with bounding pulses, increase
respiratory rate, and hyperventilation. In children four years or less, a dominant metabolic acidosis
with low arterial pH is correct.
Acidosis may increase salicylate transfer across the blood-brain barrier.
MANAGEMENT:
The activated charcoal is given if an adult presents within one hour of ingestion of
more than 250mg/kg. The plasma salicylate concentration should be
measured. Elimination is increased by urinary alkalinization, which is
achieved by the administration of 1.26% sodium bicarbonate. The urine pH
should be monitored. Patients under ten years or over
seventy years have a risk of salicylate toxicity and require dialysis at an
earlier stage.
STORAGE:
Store below 25°C in a dry place. Protect from light.
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