Loprin(aspirin) 75 mg tablets contain aspirin, which is a non-steroidal anti-inflammatory drug (NSAID).Loprin(aspirin) is a salicylate Non-steroidal anti-inflammatory drug(NSAID) and has many properties in common with non-aspirin NSAID. Loprin(aspirin) and other salicylates have analgesic, anti-inflammatory and anti-pyretic properties. Loprin(aspirin) also inhibits platelet aggression while non-acetylated salicylates do not.
MECHANISM OF ACTION:
Loprin or Aspirin(acetylsalicylic acid) is an inhibitor of both prostaglandin synthesis and platelet aggregation. Aspirin inhibits platelet aggregation by irreversible inhibition of platelet cyclooxygenase and thus inhibits the generation of thromboxane A2, a powerful inducer of platelet aggregation and vasoconstriction. The differences in activity between aspirin and salicylic acid are
thought to be due to the acetyl group on the aspirin molecule. This acetyl group is responsible for the inactivation of cyclo-oxygenase via acetylation.
PHARMACOKINETICS:
Aspirin and other salicylates are absorbed rapidly from the gastrointestinal tract when taken orally but absorption after rectal doses is less reliable. Aspirin and other salicylates can also be absorbed through the skin. After oral doses, absorption of non-ionized aspirin occurs in the stomach and intestine. Some aspirin is hydrolyzed to salicylate in the gut wall.
Once absorbed, aspirin is rapidly converted to salicylate, but during the first 20 minutes after an oral dose aspirin is the main form of the drug in the plasma. Aspirin is 80 to 90% bound to plasma proteins and is widely. distributed; its volume of distribution is reported to be 170mL/kg in adults. As plasma-drug concentrations increase, the binding sites on the proteins become saturated and the volume of distribution increases.
Both aspirin and salicylate have pharmacological activity although only aspirin has an anti-platelet effect Salicylate is extensively bound to plasma proteins and is rapidly distributed to all body parts. Salicylates appears in the breast milk and crosses the placenta.
Salicylate is mainly eliminated by hepatic metabolism ; the metabolites include salicyluric acid, salicylic phenolic glucuronide, formation of the major metabolites, salicyluric acid and salicy phenolic glucuronide, is easily saturated and follows:
Michaelis-Menten routes are first-order processes. As a result; steady-state p plasma-salicylate concentrations increase disproportionately with dose. After325-mg. aspirin dose elimination is a first-dose process and plasma-salicylate half-life is about 2 to 3 hours; at high aspirin doses, the half-life increases to 15.to 30 hours. Salicylate is also excreted. unchanged in the urine; the amount excreted by the
route increases with increasing dose and also depends on urinary pH, about 30% of a dose being excreted in alkaline urine compared with 2% of a dose in excreted urine. Renal excretion involves glomerular filtration, active renal tubular secretion, and passive tubular reabsorption. Salicylate is removed by haemodialysis .
COMPOSITION:
- Loprin 75mg Tablet:
Each enteric-coated tablet contains Aspirin 75mg. - Loprin 150mg Tablet:
Each enteric-coated tablet contains Aspirin 150mg
USES OF LOPRIN:
- Cardiovascular disease ($econdary prevention).
- Management of Unstable, angina and non-ST-segment elevation myocardial infarction (NSTEMI). Management of ST-segment elevation myocardial infarction(STEMI).
- Suspected transient ischemic attack Transient ischemic attack, ischemic stroke not associated with atrial fibrillation.
- Acute ischemic stroke.
- Atrial fibrillation following a disabling ischemic stroke (before being considered for anticoagulant treatment).
- Following disabling ischemic stroke in patients receiving anticoagulation for a prosthetic heart valve and who are at significant risk of haemorrhagic transformation.
- Following Coronary by-pass surgery.
SIDE EFFECTS OF LOPRIN
The reported adverse event are as follows:
- gastrointestinal disturbances.
- dyspepsia nausea, vomiting.
- irritation of the gastric mucosa with erosion.
- ulceration, haematemesis, melaena.
- increase bleeding tendencies, bleeding time, decrease platelet adhesiveness.
- thrombocytopenia, granulocytosis, aplastic anaemia.
- Intracranial haemorrhage existing (haematemesis, melaena) or occult gastrointestinal bleeding, may lead to iron deficiency anaemia (more common at higher doses).
- Steven-Johnsons syndrome, Lyells syndrome, purpura, erythema.
- nodosum, erythema multiforme, haemorrhagic vasculitis.
- menorrhagia, hepatotoxicity, dizziness, tinnitus.
- deafness.
- Sweating. headache, confusion, symptoms of severe intoxication include hyperventilation.
- fever.
- restlessness, ketosis and respiratory alkalosis and metabolic acidosis. Cardiovascular collapse and respiratory failure may also occur.
- In children drowsiness and metabolic acidosis commonly occur
- hypoglycemia may be severe.
- In asthma patient; chronic urticarial or chronic rhinitis, exhibit hypersensitivity to aspirin which may provoke reactions including urticaria and other skin eruptions.
- oedema, anaphylactic reactions including shock have rarely occurred.
DOSAGE AND ADMINISTRATION:
- Cardiovascular disease (Secondary prevention)
Adult: 75 mg daily - Management of Unstable angina and non-ST.-segment myocardial infarction (NSTEMI).
ST-segment elevation m myocardial infarction (STEMI)
Adult: 300 mg daily - Suspected transient ischaemic attack
Adult: 300 mg once daily until diagnosis established. - Transient ischaemic attack (long-term treatment in combination
with dipyridamole Ischaemic stroke not associated with atrial
fibrillation (in combination with dipyridamole if clopidogrel
contra-indicated or not tolerated), Ischemic stroke not
associated with atrial fibrillation (used alone if clopidogrel
dipyridamole contra-indicated or not tolerated)
Adult: 75 mg once daily - Acute ischaemic stroke
Adult: 300mg once daily tor 14 days, to be initiated 24 hours
after thrombolysis or. as so0n as possible within 48 hours of
symptom onset in patients not receiving thrombolysis.
Atrial fibrillation following a disabling ischaemic stroke (before
being considered for anticoagulant treatment)
Adult: 300 mg once daily for14 days.- Following disabling ischaemic stroke in patients receiving
anticoagulation for a prosthetic heart valve and who are at
significant risk of haemorrhagic transformation.
Adult: 300mg once daily. anticoagulant reatment stoppad or 7
days and to be substituted with aspirin.
CONTRAINDICATIONS
- Hypersensitivity to salicylic acid compounds or prostaglandin synthetase inhibitors (e.g. certain asthma patients who may suffer an attack or rhinitis and certain patients who may suffer from bronchospasm, rhinitis and urticaria) and to any of the excipients.
- Peptic ulceration or history of peptic ulceration and/or gastric/intestinal haemorrhage, or other kinds of bleeding such as cerebrovascular haemorrhages.
- Severe hepatic impairment
- Severe renal impairment
- Gout
- Children under.16 (except under medical supervision for use for example in juvenile rheumatoid arthritis).
- Doses >100 mg/day during the third trimester of pregnancy.
- Breast feeding.
- Haemorrhagic diathesis; coagulation disorders such as haemophilia and thrombocytopenia and where there is concurrent anti-coagulant therapy.
OVERDOSAGE
Salicylate poisoning is usually associated with plasma concentrations 350 mg/L (2.5 mmol/L). Most adult deaths occur in patients Whose concentrations exceed 700 mg/L (5.1 mmol/L). Single doses less than 100 mg/kg are unlikely to cause serious poisoning.
Symptoms: Common features of salicylate poisoning 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 and children over the age of 4 years. In children aged 4 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 of salicylate poisoning include haematemesis, hyperpyrexia, hypoglycaemia, hypokalAemia, thrombocytopaenia, increased INRIPTR, intravascular coagulation, renal
failure and non-cardiac pulmonary oedema.
Central nervous system features
including confusion, disorientation, coma and convulsions, are less common in adults
than in children.
Management: Give activated charcoal if an adult presents within one hour of ingestion of more than 250 mg/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 alkalinization, 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 ay cause ‘pulmonary oedema.
Haemodialysis is the treatment of choice for severe poisoning and should be considered in patients with plasma I salicylate concentrations >700 mg/L (5.1 mmol/L), or lower concentrations associated with severe clinical or metabolic features. Patients under 10 years or over 70 have increased risk of salicylate toxicity and may require dialysis at an earlier stage.
DRUG INTERACTION
Contraindicated Combinations
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 >15mg/week) with Aspirin 75 mg is contraindicated:
Not recommended combinations
Uricosuric agents, for example-probenecid and sulfinpyrazone. Salicylates reverse the effect of probenecid. The combination should be avoided.
FAQs About Loprin 75 mg Tablets
1. What is Loprin 75 mg used for?
- Loprin 75 mg is primarily used to prevent heart attacks and strokes by reducing the risk of blood clots. It is also used for pain relief and to reduce inflammation in conditions like arthritis.
2. How should I take Loprin 75 mg?
- Follow your doctor’s instructions. Typically, it is taken once daily. It can be taken with food to reduce stomach upset, and the tablet should be swallowed whole without crushing or chewing.
3. Can I take Loprin 75 mg if I am pregnant or breastfeeding?
- You should consult your doctor before taking Loprin if you are pregnant, planning to become pregnant, or breastfeeding.
4. What should I do if I miss a dose?
- If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and resume your regular schedule. Do not take two doses at the same time.
5. What are the common side effects of Loprin 75 mg?
- Common side effects include stomach upset, heartburn, and minor bleeding. If you experience severe side effects such as severe stomach pain, black/tarry stools, or unusual bleeding, seek medical attention immediately.
6. Are there any medications that interact with Loprin 75 mg?
- Yes, Loprin can interact with other medications, including other NSAIDs, blood thinners, and certain antidepressants. Always inform your doctor about all the medications and supplements you are taking.
7. Can I drink alcohol while taking Loprin 75 mg?
- It is advisable to limit alcohol consumption while taking Loprin, as alcohol can increase the risk of stomach bleeding.
8. What should I do in case of an overdose?
- In case of an overdose, seek emergency medical attention immediately. Symptoms of an overdose may include ringing in the ears, confusion, dizziness, and severe stomach pain.
9. Can Loprin 75 mg be used for children?
- Loprin 75 mg is generally not recommended for children, especially those with viral infections, due to the risk of Reye’s syndrome. Consult a pediatrician before giving this medication to a child.
10. Can I take Loprin 75 mg if I have a history of ulcers or gastrointestinal bleeding?
- If you have a history of ulcers or gastrointestinal bleeding, you should inform your doctor.
Disclaimer
The information provided on this platform is for general informational purposes only and is not intended as a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health providers with any questions you may have regarding a medical condition. Never disregard professional medical advice or delay in seeking it because of something you have read on this platform.
