* After studying this topic, attempt a test on ASPIRIN under the category ‘TEST FOR YOU: TOPIC-WISE on the TEST PACKAGES page.
Aspirin for
GPAT
D.Pharm, B.Pharm, and Pharm.D. (Pharmacy Exams)
RRB Pharmacist Recruitment Exam
Common Recruitment Examination for AIIMS Pharmacist
KGMU Pharmacist Recruitment Exam
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MPESB Pharmacist Recruitment Exam
Drugs Inspector Exams
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DPEE
• Aspirin is a NON STEROIDAL ANTI-INFLAMMATORY (NSAID) agent.
• Aspirin has analgesic, antipyretic, anti-inflammatory and antiplatelet effects.
• It belongs to the SALICYLATE class of NSAID drugs.
• Chemically, it is ACETYLSALICYLIC ACID and 2-ACETOXYBENZOIC ACID is its IUPAC name.
• The name Aspirin was given to Acetylsalicylic acid by BAYER, a German Pharmaceutical Company.
• Aspirin is an International Non-proprietary (INN) name or Generic name.
• Aspirin is hygroscopic, white crystal or crystalline powder, odourless with slightly bitter taste and is water soluble.
• Esterification reaction is involved in the synthesis of aspirin.
• Aspirin is a weakly acidic drug and remains unionised in an acidic environment. So, it is lipid soluble when the medium has low pH.
• The carboxyl group of aspirin after esterification with N-acetyl p-amino phenol gives 4-acetamidophenyl-O-acetyl salicylate.
• Acetylsalicylic acid is rapidly converted in the body to salicylic acid.
• Aspirin is a NON-SELECTIVE COX (cyclooxygenase) inhibitor.
• It is THROMBOXANE SYNTHESIS INHIBITOR type of ANTIPLATELET AGENT.
• Platelets produce Thromboxane A2 that enhances platelet aggregation.
• Aspirin inhibits platelet aggregation by irreversibly inhibiting COX-1 in platelets which results in inhibition of all of the thromboxane production by platelets. Thus, it increases the bleeding time.
• NSAID except aspirin does not affect platelet aggregation because aspirin inhibits COX irreversibly while other NSAIDs are reversible COX inhibitors. Also, aspirin has more potency against COX-1 enzyme.
• Depending on the dose, adverse effects of aspirin on G.I. tract may be INDIGESTION, HEARTBURN, STOMACH PAIN, NAUSEA AND VOMITING, DIARRHOEA OR CONSTIPATION, STOMACH IRRITATION AND ULCERS, AND GASTROINTESTINAL (GI) BLEEDING. Aspirin is contraindicated in peptic ulcer.
• In airways, arachidonic acid gets converted to prostanoids by COX enzymes and leukotrienes by 5‐lipoxygenase (LOX) enzymes. Prostanoids are bronchodilators while leukotrienes are bronchoconstrictors. Aspirin can block the production of prostanoid but not of the leukotrienes. Thus, there will be no bronchodilation; only bronchospasm will be there. This is especially true for asthmatics. This is why aspirin is a trigger factor for asthma and is contraindicated in asthma.
• Aspirin may cause REYES SYNDROME in children <16 years recovering from viral infection.
• AT HIGH DOSES (3-5 gm/day or 100 mg/kg/day) needed for anti-inflammatory action in rheumatoid arthritis/rheumatic fever aspirin produces the following effects:
1) Respiration: Respiration is stimulated as a result of i) Increase consumption of oxygen primarily by the skeletal muscles leading to increased production of carbon dioxide which directly stimulates the respiratory centre. ii) Direct stimulation of the medullary respiratory centre. iii) Chemoreceptors stimulation.
2) Hepatic and renal effects: Aspirin can affect renal function in damaged kidneys by inhibiting COX-1. Large doses of aspirin particularly in children can cause hepatic damage and even necrosis.
3) Uricosuric effect: In small doses (1-2 g per day), aspirin interferes with urate excretion, increases the plasma urate level, and blocks the action of other uricosuric drugs such as probenecid. In large doses (≥ 5 gm/day) it may block urate reabsorption by nephron. This results in uricosuria.
4) Metabolic effects: Toxic doses of aspirin may lead to hyperpyrexia, increased protein catabolism, aminoaciduria and a negative nitrogen balance.
Glucose utilization is increased resulting in hypoglycemia especially in diabetics. Toxic doses may cause central sympathetic stimulation and hyperglycemia.
• Aspirin may produce METHEMOGLOBINEMIA and TINNITUS.
• ASPIRIN: INDICATIONS AND DOSAGE
Aspirin: As analgesic-antipyretics: Oral: 300-900 mg, repeated 4-6 hourly according to clinical needs. Prophylaxis of cardiovascular events in high-risk patients: Oral: 75-150 mg once daily.
• SALICYLISM:
Antiinflammatory doses (3–5 gm/day) of aspirin may produce a condition of mild salicylate intoxication termed salicylism. It is characterized by headache, dizziness, vertigo, tinnitus, reversible impairment of hearing and vision, drowsiness, lethargy and mental confusion, excitement, nausea, vomiting, diarrhoea hyperventilation and electrolyte imbalance. These symptoms may be associated with tachypnoea and respiratory alkalosis. It is reversible on stoppage of therapy.
• ACUTE SALICYLATE POISONING:
Acute salicylate poisoning may be due to accidental ingestion in children. In adults, fatal dose is estimated to be 15-30 gm.
Symptoms of acute intoxication are vomiting, dehydration, acid-base and electrolyte disturbances, hyperpyrexia, hyper/hypoglycaemia, GI irritation and occasional haemorrhages, restlessness, delirium, vertigo, tremor, apprehension, hallucinations, convulsions, coma and death due to respiratory failure and cardiovascular collapse.
• Salicylate therapy is always supported with vitamin K.
• SODIUM BICARBONATE is the antidote for salicylate poisoning.
CONTRAINDICATIONS FOR ASPIRIN INCLUDE
• Hypersensitivity
• Peptic ulcer,
• Haemorrhagic disease, coagulation disorder (e.g. haemophilia, thrombocytopenia)
• Gout
• Severe hepatic and renal impairment
• Children <16 years and recovering from viral infection.
• Pregnancy (doses >100 mg daily during 3rd trimester) and lactation.
• Concomitant use with other NSAIDs and methotrexate.
• Aspirin + Paracetamol as analgesic – antipyretic is an ADDITIVE combination.
• Codeine and aspirin as analgesics is a SYNERGISTIC combination.
• Aspirin blocks the uricosuric action of probenecid and decreases tubular secretion of methotrexate.
• Storage condition: It is hygroscopic so it should be stored in air tight containers, in a cool, dry place.
• Ecosprin, Disprin, Equagesic, Acetosal, Acetylin, Aspro, Saletin, Caprin, Asteric are some of its popular brand names.
MCQs
1. Aspirin poisoning includes following symptoms EXCEPT:
a) Dehydration
b) Hypothermia
c) Metabolic acidosis
d) Oliguria
2. Among all NSAIDs, only aspirin has a significant antiplatelet effect because _______.
a) Aspirin inhibits COX 1 irreversibly.
b) Aspirin inhibits COX 1 reversibly.
c) Aspirin blocks COX 1 less than COX 2.
d) Aspirin is a salycilate.
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Blog content and MCQs have been taken from the following:
1) Essential Pharmacy Review for Drugs Inspector Exams by Nirali Prakashan, Pune
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2) Pharmacist Recruitment Exam by Nirali Prakashan, Pune
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To know more about our DPEE book DIPLOMA IN PHARMACY EXIT EXAMINATION (DPEE) – Based on PCI-ER 2020 Syllabus (5000+ MCQs)
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PHARMACOLOGY (Second Year Diploma in Pharmacy PCI – ER 2020)
Authors: Sunil R. Bakliwal , Praneta R. Desale , Pravin P. Jawale
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